Pub Date : 2025-12-01Epub Date: 2025-09-12DOI: 10.1016/j.prmcm.2025.100685
Poloko Stephen Kheoane , Kingsley Chimaeze Mbara , Mosoatsi Lawrence Mputi , Ts’epo Arnold Lenkoe , Sebusiswe Magama , Mokonyana Mohale , Clemence Tarirai
<div><h3>Background</h3><div>Medicinal plants have been used traditionally as oral and topical herbs for treating inflammation and alleviating pain. Particularly in traditional Chinese medicine (TCM) practices, many plants from the genera <em>Malva, Prunus</em>, and <em>Cupressus</em> are used to treat various inflammation-related diseases. This study investigated <em>in vitro</em> and <em>in vivo</em> anti-inflammatory activity of the root extracts of <em>Malva parviflora</em>, the exudates of <em>Prunus persica, Cupressus sempervirens</em> and their chitosan nanoparticles and chitosan nanogels.</div></div><div><h3>Methods</h3><div><em>In vitro</em> anti-inflammatory activities of <em>M. parviflora</em> root extracts, <em>P. persica</em> and <em>C. sempervirens</em> exudates were investigated using the protein denaturation assay method. A 1% bovine albumin reaction mixture in phosphate buffer and 80% (v/v) methanol was incubated with plant extracts or exudates at 37 °C and 70 °C. Cross-linked chitosan nanoparticles loaded with plant extracts or exudates were prepared by the gelation method. The entrapment efficiency of the plants in the chitosan nanoformulation was estimated using the phenolic content of plant materials. The nanoparticles-based nanogel was formulated by suspending nanoparticles in a gel base. Inflammation was induced in Wistar rats (230 – 270 g) by subcutaneous injection of 0.1 mL of 1% (w/v) carrageenan in the plantar tissue of the right hind paw of the rats. The rats (<em>n</em> = 48) were randomly divided into two experimental groups (A and B) of 24 rats each for oral and topical administration of nanoformulations, respectively. Each group (<em>n</em> = 24) was subdivided into 6 test group (<em>n</em> = 4), where test groups 1, 2, and 3 were treated with 500 mg/kg/BW each of <em>M. parviflora, C. sempervirens</em>, and <em>P. persica</em> nanoparticle/nanogel, either orally or topically, respectively. Test groups 4, 5, and 6, respectively served as positive control, placebo nanoparticles (<em>i.e.</em>, chitosan nanoparticles), and negative control, treated orally or topically with indomethacin (50 mg/kg/BW), chitosan nanoparticle/nanogel alone (500 mg/kg/BW/100 mg/kg/BW), and saline (3 mL).</div></div><div><h3>Results</h3><div><em>P. persica</em> exudate had the highest TPC of 70.42 ± 0.53 µg of GAE/mg compared to <em>M. parviflora</em> root extract and <em>C. sempervirens</em> exudate with the 30.93 ± 1.65 µg of GAE/mg and 9.99 ± 0.65 µg of GAE/mg, respectively. <em>M. parviflora</em> root extracts had the highest <em>in vitro</em> protein denaturation (92.40%) compared to leaves and stem extracts. <em>P. persica</em> and <em>C. sempervirens</em> nanoparticles had the highest entrapment efficiencies (99.46% and 99.56%). <em>M. parviflora</em> root extract nanoparticles showed the greatest inhibition of oedema (90%) with oral administration, outperforming <em>P. persica</em> and <em>C. sempervirens</em> exudates nanoparticle
{"title":"Anti-inflammatory effects of orally and topically administered nanoformulations of Malva parviflora root extracts, and Prunus persica and Cupressus sempervirens exudates","authors":"Poloko Stephen Kheoane , Kingsley Chimaeze Mbara , Mosoatsi Lawrence Mputi , Ts’epo Arnold Lenkoe , Sebusiswe Magama , Mokonyana Mohale , Clemence Tarirai","doi":"10.1016/j.prmcm.2025.100685","DOIUrl":"10.1016/j.prmcm.2025.100685","url":null,"abstract":"<div><h3>Background</h3><div>Medicinal plants have been used traditionally as oral and topical herbs for treating inflammation and alleviating pain. Particularly in traditional Chinese medicine (TCM) practices, many plants from the genera <em>Malva, Prunus</em>, and <em>Cupressus</em> are used to treat various inflammation-related diseases. This study investigated <em>in vitro</em> and <em>in vivo</em> anti-inflammatory activity of the root extracts of <em>Malva parviflora</em>, the exudates of <em>Prunus persica, Cupressus sempervirens</em> and their chitosan nanoparticles and chitosan nanogels.</div></div><div><h3>Methods</h3><div><em>In vitro</em> anti-inflammatory activities of <em>M. parviflora</em> root extracts, <em>P. persica</em> and <em>C. sempervirens</em> exudates were investigated using the protein denaturation assay method. A 1% bovine albumin reaction mixture in phosphate buffer and 80% (v/v) methanol was incubated with plant extracts or exudates at 37 °C and 70 °C. Cross-linked chitosan nanoparticles loaded with plant extracts or exudates were prepared by the gelation method. The entrapment efficiency of the plants in the chitosan nanoformulation was estimated using the phenolic content of plant materials. The nanoparticles-based nanogel was formulated by suspending nanoparticles in a gel base. Inflammation was induced in Wistar rats (230 – 270 g) by subcutaneous injection of 0.1 mL of 1% (w/v) carrageenan in the plantar tissue of the right hind paw of the rats. The rats (<em>n</em> = 48) were randomly divided into two experimental groups (A and B) of 24 rats each for oral and topical administration of nanoformulations, respectively. Each group (<em>n</em> = 24) was subdivided into 6 test group (<em>n</em> = 4), where test groups 1, 2, and 3 were treated with 500 mg/kg/BW each of <em>M. parviflora, C. sempervirens</em>, and <em>P. persica</em> nanoparticle/nanogel, either orally or topically, respectively. Test groups 4, 5, and 6, respectively served as positive control, placebo nanoparticles (<em>i.e.</em>, chitosan nanoparticles), and negative control, treated orally or topically with indomethacin (50 mg/kg/BW), chitosan nanoparticle/nanogel alone (500 mg/kg/BW/100 mg/kg/BW), and saline (3 mL).</div></div><div><h3>Results</h3><div><em>P. persica</em> exudate had the highest TPC of 70.42 ± 0.53 µg of GAE/mg compared to <em>M. parviflora</em> root extract and <em>C. sempervirens</em> exudate with the 30.93 ± 1.65 µg of GAE/mg and 9.99 ± 0.65 µg of GAE/mg, respectively. <em>M. parviflora</em> root extracts had the highest <em>in vitro</em> protein denaturation (92.40%) compared to leaves and stem extracts. <em>P. persica</em> and <em>C. sempervirens</em> nanoparticles had the highest entrapment efficiencies (99.46% and 99.56%). <em>M. parviflora</em> root extract nanoparticles showed the greatest inhibition of oedema (90%) with oral administration, outperforming <em>P. persica</em> and <em>C. sempervirens</em> exudates nanoparticle","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100685"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145107940","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-09-12DOI: 10.1016/j.prmcm.2025.100689
Kingsley Chimaeze Mbara , Poloko Stephen Kheoane , Clemence Tarirai
<div><h3>Introduction</h3><div>Berberine (黄连素, huáng lián sù) is a time-honored remedy in Traditional Chinese Medicine (TCM) that is found in various medicinal herbs and used to treat diabetes mellitus (DM), infections, diarrhea, and dysentery. Berberine, the major active component of <em>Coptidis rhizome</em> (黄连, huanglian), <em>Phellodendri cortex</em> (黄柏, huangbai), and <em>Mahoniae caulis</em> (亮叶十大功劳, Gong Lao Mu), exhibits several pharmacological activities, including antioxidant, anti-inflammatory, anti-apoptotic, cardioprotective, antineoplastic, antimicrobial, and antidiabetic effects. Antidiabetic effects of berberine are partly attributed to the activation of AMP-activated protein kinase (AMPK), which is a key mechanism and a potential treatment strategy for DM and its complications. This review discusses recent studies on the significant roles of berberine in activating AMPK for treating DM and its complications.</div></div><div><h3>Method</h3><div>We have comprehensively searched online databases like Scopus, PubMed, and Google Scholar for articles published in English between 2016 and 2025 using different permutations of these keywords: “Berberine”, “AMPK”, “Diabetes Mellitus”, “Diabetic nephropathy”, “Diabetic neuropathy”, “Diabetic retinopathy”, “Diabetic cardiomyopathy”, “Diabetic hepatic steatosis,” “Diabetic bone diseases”, “Diabetic atherosclerosis”, “Diabetic cognitive dysfunction”, “Diabetic lung injury” and “Other diabetic complications” to compile this narrative review. Out of 1750 initially retrieved articles, 183 were included based on their relevance to treating DM or its complications through the AMPK signaling pathway, pharmacokinetics, and translational potential. Non-English articles and studies not focused on AMPK activation by berberine and that did not address DM and its complications were excluded.</div></div><div><h3>Results</h3><div>The literature review found that berberine consistently activates AMPK across various preclinical studies of DM. The activation of AMPK is frequently mediated by pathways involving LKB1 and CAMKKβ. Berberine's activation of AMPK positively impacts glucose uptake, insulin sensitivity, lipid metabolism, oxidative stress, and inflammatory responses. Evidence from animal models demonstrated its efficacy in ameliorating complications such as diabetic nephropathy, neuropathy, retinopathy, cardiomyopathy, hepatic steatosis, bone diseases, atherosclerosis, cognitive dysfunction, and lung injury. Clinical trials reported significant reductions in fasting blood glucose (FBG), HbA1c, and lipid levels, with minimal side effects, at standard doses.</div></div><div><h3>Discussion</h3><div>AMPK activation by berberine plays a central role in cellular energy homeostasis, modulating key processes such as gluconeogenesis, lipogenesis, oxidative stress, and inflammation, which contribute to its therapeutic efficacy in metabolic dysfunction and DM-related complications. However, challenges remain re
{"title":"Targeting AMPK signaling: The therapeutic potential of berberine in diabetes and its complications","authors":"Kingsley Chimaeze Mbara , Poloko Stephen Kheoane , Clemence Tarirai","doi":"10.1016/j.prmcm.2025.100689","DOIUrl":"10.1016/j.prmcm.2025.100689","url":null,"abstract":"<div><h3>Introduction</h3><div>Berberine (黄连素, huáng lián sù) is a time-honored remedy in Traditional Chinese Medicine (TCM) that is found in various medicinal herbs and used to treat diabetes mellitus (DM), infections, diarrhea, and dysentery. Berberine, the major active component of <em>Coptidis rhizome</em> (黄连, huanglian), <em>Phellodendri cortex</em> (黄柏, huangbai), and <em>Mahoniae caulis</em> (亮叶十大功劳, Gong Lao Mu), exhibits several pharmacological activities, including antioxidant, anti-inflammatory, anti-apoptotic, cardioprotective, antineoplastic, antimicrobial, and antidiabetic effects. Antidiabetic effects of berberine are partly attributed to the activation of AMP-activated protein kinase (AMPK), which is a key mechanism and a potential treatment strategy for DM and its complications. This review discusses recent studies on the significant roles of berberine in activating AMPK for treating DM and its complications.</div></div><div><h3>Method</h3><div>We have comprehensively searched online databases like Scopus, PubMed, and Google Scholar for articles published in English between 2016 and 2025 using different permutations of these keywords: “Berberine”, “AMPK”, “Diabetes Mellitus”, “Diabetic nephropathy”, “Diabetic neuropathy”, “Diabetic retinopathy”, “Diabetic cardiomyopathy”, “Diabetic hepatic steatosis,” “Diabetic bone diseases”, “Diabetic atherosclerosis”, “Diabetic cognitive dysfunction”, “Diabetic lung injury” and “Other diabetic complications” to compile this narrative review. Out of 1750 initially retrieved articles, 183 were included based on their relevance to treating DM or its complications through the AMPK signaling pathway, pharmacokinetics, and translational potential. Non-English articles and studies not focused on AMPK activation by berberine and that did not address DM and its complications were excluded.</div></div><div><h3>Results</h3><div>The literature review found that berberine consistently activates AMPK across various preclinical studies of DM. The activation of AMPK is frequently mediated by pathways involving LKB1 and CAMKKβ. Berberine's activation of AMPK positively impacts glucose uptake, insulin sensitivity, lipid metabolism, oxidative stress, and inflammatory responses. Evidence from animal models demonstrated its efficacy in ameliorating complications such as diabetic nephropathy, neuropathy, retinopathy, cardiomyopathy, hepatic steatosis, bone diseases, atherosclerosis, cognitive dysfunction, and lung injury. Clinical trials reported significant reductions in fasting blood glucose (FBG), HbA1c, and lipid levels, with minimal side effects, at standard doses.</div></div><div><h3>Discussion</h3><div>AMPK activation by berberine plays a central role in cellular energy homeostasis, modulating key processes such as gluconeogenesis, lipogenesis, oxidative stress, and inflammation, which contribute to its therapeutic efficacy in metabolic dysfunction and DM-related complications. However, challenges remain re","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100689"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145108034","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-11-25DOI: 10.1016/j.prmcm.2025.100725
Naruwat Pakdee, Ronnachai Poowanna
Introduction
Antidesma thwaitesianum (Chinese name: 小斑五月茶, Pinyin: xiǎo yè wǔ yuè chá), taxonomically associated with its synonym Antidesma puncticulatum is a fruit rich in phenolic compounds known for their health benefits as well as their antibacterial and antioxidant activities. This study aimed to analyze the phenolic compound content and antioxidant activity of A. thwaitesianum extracts, as well as to investigate their inhibitory effects on the growth of Eschrichia coli, Aeromonas hydrophila, Bacillus spp. and Proteus mirabilis.
Methods
The extracts were prepared by freshly squeezing the fruits and using 95 % ethanol as a solvent. The phenolic compound content was analyzed using the Folin - Ciocalteu method. Antioxidant activity was assessed using the DPPH assay, while antibacterial activity was evaluated using the disc diffusion method, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC).
Results
The results showed that A. thwaitesianum black fruit extract exhibited the highest total phenolic content (116.48 ± 2.8 mg GAE/g), while the strongest antioxidant activity (IC50 = 79.27 ± 1.88 mg/mL) occurred in red fruit water extract. whereas the red fruit ethanolic extract showed the strongest antibacterial activity with MIC values ranging from 0.98 - 250 µg/mL against tested bacteria.
Discussion
Ethanol extracts of A. thwaitesianum especially from black fruits, contained higher phenolic content, while red fruit water extracts showed the strongest antioxidant activity and red fruit ethanol extracts exhibited the most potent antibacterial effects. These results highlight the potential of A. thwaitesianum as a natural source of antioxidant and antibacterial agents for functional food and phytopharmaceutical applications.
{"title":"Phenolic content, antioxidant activities and antibacterial effects of Antidesma thwaitesianum Mull. Arg. extracts","authors":"Naruwat Pakdee, Ronnachai Poowanna","doi":"10.1016/j.prmcm.2025.100725","DOIUrl":"10.1016/j.prmcm.2025.100725","url":null,"abstract":"<div><h3>Introduction</h3><div><em>Antidesma thwaitesianum</em> (Chinese name: 小斑五月茶, Pinyin: xiǎo yè wǔ yuè chá), taxonomically associated with its synonym <em>Antidesma puncticulatum</em> is a fruit rich in phenolic compounds known for their health benefits as well as their antibacterial and antioxidant activities. This study aimed to analyze the phenolic compound content and antioxidant activity of <em>A. thwaitesianum</em> extracts, as well as to investigate their inhibitory effects on the growth of <em>Eschrichia coli, Aeromonas hydrophila, Bacillus</em> spp. and <em>Proteus mirabilis</em>.</div></div><div><h3>Methods</h3><div>The extracts were prepared by freshly squeezing the fruits and using 95 % ethanol as a solvent. The phenolic compound content was analyzed using the Folin - Ciocalteu method. Antioxidant activity was assessed using the DPPH assay, while antibacterial activity was evaluated using the disc diffusion method, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC).</div></div><div><h3>Results</h3><div>The results showed that <em>A. thwaitesianum</em> black fruit extract exhibited the highest total phenolic content (116.48 ± 2.8 mg GAE/g), while the strongest antioxidant activity (IC<sub>50</sub> = 79.27 ± 1.88 mg/mL) occurred in red fruit water extract. whereas the red fruit ethanolic extract showed the strongest antibacterial activity with MIC values ranging from 0.98 - 250 µg/mL against tested bacteria.</div></div><div><h3>Discussion</h3><div>Ethanol extracts of <em>A. thwaitesianum</em> especially from black fruits, contained higher phenolic content, while red fruit water extracts showed the strongest antioxidant activity and red fruit ethanol extracts exhibited the most potent antibacterial effects. These results highlight the potential of <em>A. thwaitesianum</em> as a natural source of antioxidant and antibacterial agents for functional food and phytopharmaceutical applications.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100725"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145623889","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-10-17DOI: 10.1016/j.prmcm.2025.100706
Rufaida Wasim , Sumaiya Azmi , Asad Ahmad
Introduction
: Cardiovascular diseases (CVDs) remain the leading global cause of morbidity and mortality, driven by mechanisms such as oxidative stress, endothelial dysfunction, inflammation, and lipid imbalance. Curcumin, the principal bioactive constituent of Curcuma longa (turmeric), has long been used in Traditional Chinese Medicine (TCM) to improve circulation and alleviate stasis. Modern pharmacological evidence suggests it may offer cardiovascular protection.
Methods
: This review synthesises findings from preclinical models, clinical studies, and molecular investigations of curcumin in CVD, alongside traditional perspectives from TCM for integrative context.
Results
: Experimental studies reveal that curcumin reduces oxidative stress, downregulates NF-κB and pro-inflammatory cytokines, enhances nitric oxide bioavailability, and inhibits vascular smooth muscle proliferation. In animal models, it decreases myocardial infarct size, attenuates hypertrophy, and improves ventricular function. Clinical trials report improvements in blood pressure, endothelial function, lipid regulation, and inflammatory biomarkers among individuals at cardiovascular risk. However, outcomes remain inconsistent due to variability in study design, small sample sizes, heterogeneous formulations, and limited duration of follow-up. TCM perspectives on promoting blood flow and reducing stasis align with curcumin’s observed effects on vascular remodeling and atherosclerosis.
Discussion
: Curcumin is a safe, pleiotropic compound with growing evidence for adjunctive use in CVD management. Its poor oral bioavailability remains a key limitation, highlighting the need for novel formulations. Well-designed, larger clinical trials are essential to establish efficacy and bridge traditional knowledge with modern cardiovascular therapeutics.
{"title":"Integrating traditional chinese medicine and modern pharmacology: The role of Jiang Huang (curcumin) in cardiovascular health","authors":"Rufaida Wasim , Sumaiya Azmi , Asad Ahmad","doi":"10.1016/j.prmcm.2025.100706","DOIUrl":"10.1016/j.prmcm.2025.100706","url":null,"abstract":"<div><h3>Introduction</h3><div><strong>:</strong> Cardiovascular diseases (CVDs) remain the leading global cause of morbidity and mortality, driven by mechanisms such as oxidative stress, endothelial dysfunction, inflammation, and lipid imbalance. Curcumin, the principal bioactive constituent of <em>Curcuma longa</em> (turmeric), has long been used in Traditional Chinese Medicine (TCM) to improve circulation and alleviate stasis. Modern pharmacological evidence suggests it may offer cardiovascular protection.</div></div><div><h3>Methods</h3><div><strong>:</strong> This review synthesises findings from preclinical models, clinical studies, and molecular investigations of curcumin in CVD, alongside traditional perspectives from TCM for integrative context.</div></div><div><h3>Results</h3><div><strong>:</strong> Experimental studies reveal that curcumin reduces oxidative stress, downregulates NF-κB and pro-inflammatory cytokines, enhances nitric oxide bioavailability, and inhibits vascular smooth muscle proliferation. In animal models, it decreases myocardial infarct size, attenuates hypertrophy, and improves ventricular function. Clinical trials report improvements in blood pressure, endothelial function, lipid regulation, and inflammatory biomarkers among individuals at cardiovascular risk. However, outcomes remain inconsistent due to variability in study design, small sample sizes, heterogeneous formulations, and limited duration of follow-up. TCM perspectives on promoting blood flow and reducing stasis align with curcumin’s observed effects on vascular remodeling and atherosclerosis.</div></div><div><h3>Discussion</h3><div><strong>:</strong> Curcumin is a safe, pleiotropic compound with growing evidence for adjunctive use in CVD management. Its poor oral bioavailability remains a key limitation, highlighting the need for novel formulations. Well-designed, larger clinical trials are essential to establish efficacy and bridge traditional knowledge with modern cardiovascular therapeutics.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100706"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145363237","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-09-12DOI: 10.1016/j.prmcm.2025.100692
Y. Yan , X. Liu , Y. Sun, H. Wang
Introduction
Gambogic acid (GA), a caged xanthone derived from the resin of Garcinia hanburyi (known as Téng Huáng in traditional Chinese medicine), has been historically utilized in TCM for its properties of “combating toxins, eroding sores, dispelling blood stasis, and resolving masses” in the treatment of abscesses, boils, and refractory skin diseases. In recent decades, GA has gained significant attention as a promising multi-target anticancer agent. This review aims to synthesize current preclinical evidence regarding GA’s antitumor mechanisms, its efficacy in combination therapies, and strategies to overcome its pharmacological limitations.
Methods
A systematic literature search was conducted across electronic databases including PubMed, Web of Science, and CNKI to identify relevant preclinical studies investigating the anticancer mechanisms and delivery strategies of GA. Articles were selected based on their relevance to GA’s molecular targets, efficacy in mono- and combination therapy, and novel formulation approaches.
Results
Preclinical studies demonstrate that GA exerts broad-spectrum antitumor effects through multiple mechanisms: induction of apoptosis via mitochondrial and death receptor pathways; cell cycle arrest at G0/G1 or G2/M phases; inhibition of angiogenesis via HIF-1α/VEGF/MMPs suppression; and reduction of metastasis through downregulation of MMPs. GA modulates key oncogenic pathways including NF-κB, PI3K/Akt/mTOR, and MAPKs. It overcomes drug resistance by targeting P-glycoprotein, Bcr-Abl, and SHH pathways. Notably, GA induces immunogenic pyroptosis via caspase-3/GSDME activation and reprograms tumor-associated macrophages by suppressing extracellular vesicle-mediated miR-21 transfer. Synergistic effects are observed when GA is combined with chemotherapy, targeted agents (e.g., bortezomib, gefitinib), radiotherapy, or photothermal therapy. However, GA’s clinical application is limited by poor solubility and bioavailability. Nanocarrier systems—such as polymeric nanoparticles, protein-based carriers, biomimetic designs, and stimuli-responsive formulations—have significantly improved GA’s stability, tumor targeting, and therapeutic index.
Discussion
GA represents a multi-mechanistic anticancer agent derived from TCM with high translational potential. Despite compelling preclinical results, further well-designed clinical trials are essential to validate its efficacy and safety in humans. The integration of GA with modern drug delivery technologies, especially nanotechnology, provides a promising approach to overcoming its physicochemical limitations. Future research should focus on context-dependent pathway modulation, immune microenvironment interactions, and clinical translation of advanced GA formulations.
黄曲霉酸（GA）是一种笼状的山酮，从黄曲霉的树脂中提取（在中医中称为黄曲霉Huáng），因其具有“抗毒素、腐蚀疮、化瘀、化块”的功效，在中医中一直被用于治疗脓肿、疖子和难治性皮肤病。近几十年来，GA作为一种有前景的多靶点抗癌药物受到了广泛的关注。本综述旨在综合目前关于GA抗肿瘤机制的临床前证据，其在联合治疗中的疗效，以及克服其药理学局限性的策略。方法系统检索PubMed、Web of Science、中国知网等电子数据库，收集GA抗癌机制和给药策略的相关临床前研究。文章的选择是基于它们与GA的分子靶点的相关性，单一和联合治疗的疗效，以及新的配方方法。结果临床前期研究表明，GA可通过多种机制发挥广谱抗肿瘤作用：通过线粒体和死亡受体途径诱导细胞凋亡；细胞周期阻滞于G0/G1或G2/M期；通过抑制HIF-1α/VEGF/MMPs抑制血管生成；并通过下调MMPs来减少转移。GA调节NF-κB、PI3K/Akt/mTOR和MAPKs等关键的致癌途径。它通过靶向p -糖蛋白、Bcr-Abl和SHH通路来克服耐药性。值得注意的是，GA通过caspase-3/GSDME激活诱导免疫原性焦亡，并通过抑制细胞外囊泡介导的miR-21转移对肿瘤相关巨噬细胞进行重编程。当GA与化疗、靶向药物（如硼替佐米、吉非替尼）、放疗或光热疗法联合使用时，可以观察到协同效应。然而，GA的临床应用受到溶解度和生物利用度差的限制。纳米载体系统，如聚合纳米颗粒、蛋白质载体、仿生设计和刺激反应配方，显著提高了GA的稳定性、肿瘤靶向性和治疗指数。ga是一种来自中药的多机制抗癌药物，具有很高的转化潜力。尽管有令人信服的临床前结果，但进一步精心设计的临床试验对于验证其在人体中的有效性和安全性至关重要。遗传基因与现代药物传递技术，特别是纳米技术的结合，为克服其物理化学局限性提供了一条有前途的途径。未来的研究应集中在上下文依赖性通路调节、免疫微环境相互作用和高级GA配方的临床翻译上。
{"title":"Gambogic acid: A review of its pharmacological mechanisms against cancer","authors":"Y. Yan , X. Liu , Y. Sun, H. Wang","doi":"10.1016/j.prmcm.2025.100692","DOIUrl":"10.1016/j.prmcm.2025.100692","url":null,"abstract":"<div><h3>Introduction</h3><div>Gambogic acid (GA), a caged xanthone derived from the resin of Garcinia hanburyi (known as <em>Téng Huáng</em> in traditional Chinese medicine), has been historically utilized in TCM for its properties of “combating toxins, eroding sores, dispelling blood stasis, and resolving masses” in the treatment of abscesses, boils, and refractory skin diseases. In recent decades, GA has gained significant attention as a promising multi-target anticancer agent. This review aims to synthesize current preclinical evidence regarding GA’s antitumor mechanisms, its efficacy in combination therapies, and strategies to overcome its pharmacological limitations.</div></div><div><h3>Methods</h3><div>A systematic literature search was conducted across electronic databases including PubMed, Web of Science, and CNKI to identify relevant preclinical studies investigating the anticancer mechanisms and delivery strategies of GA. Articles were selected based on their relevance to GA’s molecular targets, efficacy in mono- and combination therapy, and novel formulation approaches.</div></div><div><h3>Results</h3><div>Preclinical studies demonstrate that GA exerts broad-spectrum antitumor effects through multiple mechanisms: induction of apoptosis via mitochondrial and death receptor pathways; cell cycle arrest at G0/G1 or G2/M phases; inhibition of angiogenesis via HIF-1α/VEGF/MMPs suppression; and reduction of metastasis through downregulation of MMPs. GA modulates key oncogenic pathways including NF-κB, PI3K/Akt/mTOR, and MAPKs. It overcomes drug resistance by targeting P-glycoprotein, Bcr-Abl, and SHH pathways. Notably, GA induces immunogenic pyroptosis via caspase-3/GSDME activation and reprograms tumor-associated macrophages by suppressing extracellular vesicle-mediated miR-21 transfer. Synergistic effects are observed when GA is combined with chemotherapy, targeted agents (<em>e.g.</em>, bortezomib, gefitinib), radiotherapy, or photothermal therapy. However, GA’s clinical application is limited by poor solubility and bioavailability. Nanocarrier systems—such as polymeric nanoparticles, protein-based carriers, biomimetic designs, and stimuli-responsive formulations—have significantly improved GA’s stability, tumor targeting, and therapeutic index.</div></div><div><h3>Discussion</h3><div>GA represents a multi-mechanistic anticancer agent derived from TCM with high translational potential. Despite compelling preclinical results, further well-designed clinical trials are essential to validate its efficacy and safety in humans. The integration of GA with modern drug delivery technologies, especially nanotechnology, provides a promising approach to overcoming its physicochemical limitations. Future research should focus on context-dependent pathway modulation, immune microenvironment interactions, and clinical translation of advanced GA formulations.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100692"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145107937","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-11-19DOI: 10.1016/j.prmcm.2025.100722
Muhammad Tariq Saeed , Jinghao Zhao , Hassan Mohamed , Tahira Naz , Bushra Iqbal , Asmaa S. Ramadan , Hafiz Muhammad Saleem Akhtar , Molalign Assefa , Hina Khalid , Yuanda Song , Wenlong Sun
Introduction
Tamarix chinensis Lour (TCL) is a known arid plant belonging to the family Tamaricaceae, widely distributed near the Yellow River Delta, northeastern Shandong Province of China. The researchers have mainly focused on heat and salt alkaline resistance properties of TCL, but recently, it has gained significant attention for its wide range of pharmacological and therapeutically bioactive ingredients. The flavonoids, phenolics, terpenoids, volatiles, and other miscellaneous compounds are vital bioactive substances that demonstrate hepatoprotective, antioxidant, anti-inflammatory, cardio-protective, lung protection, anticancer, anti-complement, antidiabetic, neurological protection, and other bioactivities. This comprehensive review summarized the traditional medicinal uses, phytochemistry, therapeutic potential, and mechanistic insights, consolidating the current research on the medicinal potential of TCL.
Methods
The information about TCL was collected from different reliable scholarly resources, like Chinese digital library, Google Scholar, Science Direct, and PubMed. Molecular docking was used to predict the interaction between six major compounds (Ellagic acid, Gallic acid, Isorhamnetin, Kaempferol, Quercetin, and Tamarixetin) and four target proteins, tumor necrosis factor (TNF-α), interleukin 6 (IL-6), nuclear factor erythroid 2-related factor 2 (Nrf2), and peroxisome proliferator-activated receptor alpha (PPARα).
Results
These compounds demonstrated a significant binding affinity to TNF-alpha and ellagic acid showed bonding with IL-6 and showed the potential effects as antitumor and anti-inflammatory.
Conclusion
There is a critical need to deepen the understanding of the mechanisms of therapeutic properties underlying TCL efficacy and to establish robust quality standards and regulatory frameworks that ensure safety comparable to that of Western pharmaceuticals. The current evidence on the pharmacological properties of this plant explores that this plant could be a hopeful contender for drug development.
{"title":"Unveiling the pharmacological promise of Tamarix chinensis Lour: An integrative review of phytochemical constituents, therapeutic potentials, and mechanistic pathways","authors":"Muhammad Tariq Saeed , Jinghao Zhao , Hassan Mohamed , Tahira Naz , Bushra Iqbal , Asmaa S. Ramadan , Hafiz Muhammad Saleem Akhtar , Molalign Assefa , Hina Khalid , Yuanda Song , Wenlong Sun","doi":"10.1016/j.prmcm.2025.100722","DOIUrl":"10.1016/j.prmcm.2025.100722","url":null,"abstract":"<div><h3>Introduction</h3><div><em>Tamarix chinensis</em> Lour (TCL) is a known arid plant belonging to the family <em>Tamaricaceae,</em> widely distributed near the Yellow River Delta, northeastern Shandong Province of China. The researchers have mainly focused on heat and salt alkaline resistance properties of TCL, but recently, it has gained significant attention for its wide range of pharmacological and therapeutically bioactive ingredients. The flavonoids, phenolics, terpenoids, volatiles, and other miscellaneous compounds are vital bioactive substances that demonstrate hepatoprotective, antioxidant, anti-inflammatory, cardio-protective, lung protection, anticancer, anti-complement, antidiabetic, neurological protection, and other bioactivities. This comprehensive review summarized the traditional medicinal uses, phytochemistry, therapeutic potential, and mechanistic insights, consolidating the current research on the medicinal potential of TCL<em>.</em></div></div><div><h3>Methods</h3><div>The information about TCL was collected from different reliable scholarly resources, like Chinese digital library, Google Scholar, Science Direct, and PubMed. Molecular docking was used to predict the interaction between six major compounds (Ellagic acid, Gallic acid, Isorhamnetin, Kaempferol, Quercetin, and Tamarixetin) and four target proteins, <span><span>tumor necrosis factor</span><svg><path></path></svg></span> (TNF-α), <span><span>interleukin 6</span><svg><path></path></svg></span> (IL-6), nuclear factor erythroid 2-related factor 2 (Nrf2), and peroxisome proliferator-activated receptor alpha (PPARα).</div></div><div><h3>Results</h3><div>These compounds demonstrated a significant binding affinity to TNF-alpha and ellagic acid showed bonding with IL-6 and showed the potential effects as antitumor and anti-inflammatory.</div></div><div><h3>Conclusion</h3><div>There is a critical need to deepen the understanding of the mechanisms of therapeutic properties underlying TCL efficacy and to establish robust quality standards and regulatory frameworks that ensure safety comparable to that of Western pharmaceuticals. The current evidence on the pharmacological properties of this plant explores that this plant could be a hopeful contender for drug development.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100722"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145623891","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-11-01DOI: 10.1016/j.prmcm.2025.100714
Sourav Pal , Arghya Panda , Biprojit Bhowmick , Khokan Bera
Introduction
Crithmum maritimum(sea fennel, Chinese: 海茴香 [hǎi huí xiāng]) is an edible halophyte traditionally valued in both Mediterranean diets and Traditional Chinese Medicine (TCM), where it is prescribed for “dissolving masses,” regulating qi, and resolving damp-heat/toxins—concepts aligned with anti-inflammatory, antimicrobial, and anticancer effects. Rich in phenolic acids, flavonoids, essential oils, fatty acids, vitamins, and minerals, it shows potential against gastrointestinal tract (GIT) cancers, a growing global health burden.
Methods
A systematic literature search was conducted in PubMed, Scopus, Web of Science, and Google Scholar for studies published between 2010 and 2025, limited to English language studies, using keywords “Crithmum maritimum,” “sea fennel,” “gastrointestinal cancer,” “anticancer,” “polyphenols,” “essential oils,” and “bioactive compounds.” of 167 retrieved records, 138 met the inclusion criteria: original in vitro, in vivo, or clinical research evaluating C. maritimum or its constituents for anticancer activity in GIT malignancies. Exclusion criteria removed reviews without new data, unrelated species, and studies lacking mechanistic outcomes.
Results
C. maritimum exhibits preclinical efficacy against GIT cancers via modulation of p53, NRF2, and Wnt/β-catenin pathways, aligning with its traditional TCM uses. Studies identified chlorogenic acid (30–50 % of total polyphenol), gallic acid (15–20 % of terpene), limonene, sabinene, α-pinene, γ-terpinene, fatty acids, and vitamin C as key anticancer agents that promote apoptosis, inhibit angiogenesis, and attenuate oxidative and inflammatory signaling in GIT cancer models.
Conclusion
C. maritimum exhibits a broad phytochemical spectrum with multitargeted preclinical efficacy against GIT cancers, consistent with its historical TCM applications. Standardization, mechanistic validation, and clinical trials are required to advance its therapeutic integration.
Significance Statement
This review unites TCM tradition with modern biomedical evidence, highlighting C. maritimum as a promising natural agent for GIT cancer prevention and management, with mechanistic breadth well-suited to the multifactorial nature of these malignancies.
{"title":"Crithmum maritimum: Phytoconstituents composition, and potential anticancer activity in gastrointestinal cancer mechanisms and prospects","authors":"Sourav Pal , Arghya Panda , Biprojit Bhowmick , Khokan Bera","doi":"10.1016/j.prmcm.2025.100714","DOIUrl":"10.1016/j.prmcm.2025.100714","url":null,"abstract":"<div><h3>Introduction</h3><div><em>Crithmum maritimum</em>(sea fennel, Chinese: 海茴香 [hǎi huí xiāng]) is an edible halophyte traditionally valued in both Mediterranean diets and Traditional Chinese Medicine (TCM), where it is prescribed for “dissolving masses,” regulating qi, and resolving damp-heat/toxins—concepts aligned with anti-inflammatory, antimicrobial, and anticancer effects. Rich in phenolic acids, flavonoids, essential oils, fatty acids, vitamins, and minerals, it shows potential against gastrointestinal tract (GIT) cancers, a growing global health burden.</div></div><div><h3>Methods</h3><div>A systematic literature search was conducted in PubMed, Scopus, Web of Science, and Google Scholar for studies published between 2010 and 2025, limited to English language studies, using keywords “Crithmum maritimum,” “sea fennel,” “gastrointestinal cancer,” “anticancer,” “polyphenols,” “essential oils,” and “bioactive compounds.” of 167 retrieved records, 138 met the inclusion criteria: original in vitro, in vivo, or clinical research evaluating <em>C. maritimum</em> or its constituents for anticancer activity in GIT malignancies. Exclusion criteria removed reviews without new data, unrelated species, and studies lacking mechanistic outcomes.</div></div><div><h3>Results</h3><div><em>C. maritimum</em> exhibits preclinical efficacy against GIT cancers via modulation of p53, NRF2, and Wnt/β-catenin pathways, aligning with its traditional TCM uses. Studies identified chlorogenic acid (30–50 % of total polyphenol), gallic acid (15–20 % of terpene), limonene, sabinene, α-pinene, γ-terpinene, fatty acids, and vitamin C as key anticancer agents that promote apoptosis, inhibit angiogenesis, and attenuate oxidative and inflammatory signaling in GIT cancer models.</div></div><div><h3>Conclusion</h3><div><em>C. maritimum</em> exhibits a broad phytochemical spectrum with multitargeted preclinical efficacy against GIT cancers, consistent with its historical TCM applications. Standardization, mechanistic validation, and clinical trials are required to advance its therapeutic integration.</div></div><div><h3>Significance Statement</h3><div>This review unites TCM tradition with modern biomedical evidence, highlighting <em>C. maritimum</em> as a promising natural agent for GIT cancer prevention and management, with mechanistic breadth well-suited to the multifactorial nature of these malignancies.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100714"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145466300","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-11-21DOI: 10.1016/j.prmcm.2025.100723
Anggit Listyacahyani Sunarwidhi , Agung Endro Nugroho , Sri Widyastuti , Ekowati Chasanah , Ari Hernawan , Eka Sunarwidhi Prasedya
Background
Cutaneous melanoma remains a global health issue. While lipid-rich oils have long been used in Traditional Chinese Medicine (TCM) for cancer therapy, brown macroalgae Sargassum also provide lipid derivative compounds with therapeutic potential, including in the modulation of skin diseases. However, the molecular mechanisms of fatty oil compounds from Sargassum species, such as Sargassum polycystum, in relation to cutaneous melanoma remain unexplored.
Methods
UHPLC-HRMS-based untargeted metabolomics was performed to identify the compounds in Sargassum polycystum hexane oil extract (HOE). Identified compounds were then subjected to computational analysis, including network pharmacology analysis, followed by molecular docking (Autodock Vina), molecular dynamics (GROMACS), and GO/KEGG enrichment analysis (DAVID and KEGG mapper). Finally, in vitro anti-oxidant analysis using DPPH assay and B16-F10 melanoma cytotoxic analysis using Resazurin assay were also performed.
Results
Untargeted metabolomics identified 62 drug-like compounds predicted to interact with cutaneous melanoma-related targets. Computational analysis identified Dormatinone, a sterol with strong affinity for PTPN11, an essential oncogenic gene and immune regulator in cutaneous melanoma. Enrichment analysis revealed the role of Sargassum polycystum HOE compounds in oncogenic signaling and immune regulation, while in vitro assays confirmed the extract’s anti-oxidant (IC50 = 0.847 ± 0.02mg/mL) and B16-F10 melanoma cytotoxic activity (IC50 = 0.480 ± 0.0014mg/mL).
Conclusion
These findings indicate the potential of Sargassum polycystum HOE as a sterol-rich extract with anti-cutaneous melanoma activity, providing a basis for further drug development.
{"title":"Mechanistic insights of Sargassum polycystum fatty oil compounds in cutaneous melanoma: in vitro, metabolomics guided-network pharmacology, molecular docking and dynamics approach","authors":"Anggit Listyacahyani Sunarwidhi , Agung Endro Nugroho , Sri Widyastuti , Ekowati Chasanah , Ari Hernawan , Eka Sunarwidhi Prasedya","doi":"10.1016/j.prmcm.2025.100723","DOIUrl":"10.1016/j.prmcm.2025.100723","url":null,"abstract":"<div><h3>Background</h3><div>Cutaneous melanoma remains a global health issue. While lipid-rich oils have long been used in Traditional Chinese Medicine (TCM) for cancer therapy, brown macroalgae Sargassum also provide lipid derivative compounds with therapeutic potential, including in the modulation of skin diseases. However, the molecular mechanisms of fatty oil compounds from Sargassum species, such as <em>Sargassum polycystum</em>, in relation to cutaneous melanoma remain unexplored.</div></div><div><h3>Methods</h3><div>UHPLC-HRMS-based untargeted metabolomics was performed to identify the compounds in <em>Sargassum polycystum</em> hexane oil extract (HOE). Identified compounds were then subjected to computational analysis, including network pharmacology analysis, followed by molecular docking (Autodock Vina), molecular dynamics (GROMACS), and GO/KEGG enrichment analysis (DAVID and KEGG mapper). Finally, in vitro anti-oxidant analysis using DPPH assay and B16-F10 melanoma cytotoxic analysis using Resazurin assay were also performed.</div></div><div><h3>Results</h3><div>Untargeted metabolomics identified 62 drug-like compounds predicted to interact with cutaneous melanoma-related targets. Computational analysis identified Dormatinone, a sterol with strong affinity for PTPN11, an essential oncogenic gene and immune regulator in cutaneous melanoma. Enrichment analysis revealed the role of <em>Sargassum polycystum</em> HOE compounds in oncogenic signaling and immune regulation, while in vitro assays confirmed the extract’s anti-oxidant (IC<sub>50</sub> = 0.847 ± 0.02mg/mL) and B16-F10 melanoma cytotoxic activity (IC<sub>50</sub> = 0.480 ± 0.0014mg/mL).</div></div><div><h3>Conclusion</h3><div>These findings indicate the potential <em>of Sargassum polycystum</em> HOE as a sterol-rich extract with anti-cutaneous melanoma activity, providing a basis for further drug development.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100723"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145693359","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-11-29DOI: 10.1016/j.prmcm.2025.100728
Aishwarya R. Chavan , Omkar S. Ghatge , Roshan R. Kamble , Manish S. Kondawar
<div><h3>Background</h3><div><em>Laurus nobilis Linn. (Lauraceae),</em> commonly known as Bay Laurel and referred to as Yue Gui Ye in Traditional Chinese Medicine (TCM), has been used for centuries as a culinary spice and a therapeutic herb. It is reputed for its carminative, antiseptic, and anti-inflammatory actions and for promoting digestion and circulation of Qi. Despite widespread usage, the systematic chemical profiling of its non-polar (petroleum ether) extracts remains limited, which constrains standardization efforts and pharmacological validation. Previous studies have largely focused on essential oils obtained by steam distillation, leaving a knowledge gap regarding semi-volatile components uniquely extractable in petroleum ether.</div></div><div><h3>Objective</h3><div>To establish chromatographic fingerprints and to identify major volatile and semi-volatile compounds in the petroleum ether extract of L. nobilis leaves, thereby supporting its quality control and ethnopharmacological relevance. Additionally, to compare the detected compounds with previous literature to identify newly reported and previously confirmed phytoconstituents.</div></div><div><h3>Methods</h3><div>Fresh L. nobilis leaves were collected, authenticated, and extracted using petroleum ether (40–60°C) via Soxhlet apparatus. The extract was analyzed by HPTLC using silica gel 60 F₂₅₄ plates and scanned at 366 nm, and by GC–MS using a Shimadzu TQ-8050 HS20 system. Compounds were identified using NIST 2020 library data. Literature between 2010–2024 was systematically reviewed using PubMed, Scopus, and Google Scholar to determine the novelty or previously reported nature of each compound.</div></div><div><h3>Results</h3><div>The HPTLC fingerprint displayed eight major peaks, confirming chemical diversity. GC–MS analysis identified twenty-nine volatile compounds dominated by α-pinene (32.38%), o-cymene (20.06%), γ-terpinene (9.83%), and β-myrcene (7.94%). Comparison with earlier studies revealed that key monoterpenes including α-pinene, β-myrcene, limonene, linalool, and γ-terpinene have been consistently reported in essential oils and organic extracts. However, six detected semi-volatile compounds (tetradecane, hexadecane, pentadecene isomer, benzaldehyde derivative, phytol acetate, and a minor sesquiterpene oxide) appear newly reported for petroleum ether extracts, indicating chemotype broadening beyond essential-oil profiles. Replicate analysis showed less than 2% RSD, confirming analytical consistency.</div></div><div><h3>Conclusion</h3><div>A chemical fingerprint of Yue Gui Ye was established using GC–MS and HPTLC. The findings confirm the predominance of α-pinene and o-cymene reported extensively in earlier literature, while also highlighting several newly detected constituents unique to petroleum ether extraction. This comparative profiling enhances the understanding of L. nobilis phytochemical diversity and provides reference data for herbal standardization in Trad
{"title":"Gas chromatography–mass spectrometry (GC–MS) analysis and high-performance thin-layer chromatography (HPTLC) fingerprinting profile of petroleum ether extract of Laurus nobilis Linn. (Yue Gui Ye) leaves","authors":"Aishwarya R. Chavan , Omkar S. Ghatge , Roshan R. Kamble , Manish S. Kondawar","doi":"10.1016/j.prmcm.2025.100728","DOIUrl":"10.1016/j.prmcm.2025.100728","url":null,"abstract":"<div><h3>Background</h3><div><em>Laurus nobilis Linn. (Lauraceae),</em> commonly known as Bay Laurel and referred to as Yue Gui Ye in Traditional Chinese Medicine (TCM), has been used for centuries as a culinary spice and a therapeutic herb. It is reputed for its carminative, antiseptic, and anti-inflammatory actions and for promoting digestion and circulation of Qi. Despite widespread usage, the systematic chemical profiling of its non-polar (petroleum ether) extracts remains limited, which constrains standardization efforts and pharmacological validation. Previous studies have largely focused on essential oils obtained by steam distillation, leaving a knowledge gap regarding semi-volatile components uniquely extractable in petroleum ether.</div></div><div><h3>Objective</h3><div>To establish chromatographic fingerprints and to identify major volatile and semi-volatile compounds in the petroleum ether extract of L. nobilis leaves, thereby supporting its quality control and ethnopharmacological relevance. Additionally, to compare the detected compounds with previous literature to identify newly reported and previously confirmed phytoconstituents.</div></div><div><h3>Methods</h3><div>Fresh L. nobilis leaves were collected, authenticated, and extracted using petroleum ether (40–60°C) via Soxhlet apparatus. The extract was analyzed by HPTLC using silica gel 60 F₂₅₄ plates and scanned at 366 nm, and by GC–MS using a Shimadzu TQ-8050 HS20 system. Compounds were identified using NIST 2020 library data. Literature between 2010–2024 was systematically reviewed using PubMed, Scopus, and Google Scholar to determine the novelty or previously reported nature of each compound.</div></div><div><h3>Results</h3><div>The HPTLC fingerprint displayed eight major peaks, confirming chemical diversity. GC–MS analysis identified twenty-nine volatile compounds dominated by α-pinene (32.38%), o-cymene (20.06%), γ-terpinene (9.83%), and β-myrcene (7.94%). Comparison with earlier studies revealed that key monoterpenes including α-pinene, β-myrcene, limonene, linalool, and γ-terpinene have been consistently reported in essential oils and organic extracts. However, six detected semi-volatile compounds (tetradecane, hexadecane, pentadecene isomer, benzaldehyde derivative, phytol acetate, and a minor sesquiterpene oxide) appear newly reported for petroleum ether extracts, indicating chemotype broadening beyond essential-oil profiles. Replicate analysis showed less than 2% RSD, confirming analytical consistency.</div></div><div><h3>Conclusion</h3><div>A chemical fingerprint of Yue Gui Ye was established using GC–MS and HPTLC. The findings confirm the predominance of α-pinene and o-cymene reported extensively in earlier literature, while also highlighting several newly detected constituents unique to petroleum ether extraction. This comparative profiling enhances the understanding of L. nobilis phytochemical diversity and provides reference data for herbal standardization in Trad","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100728"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145693358","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-12-01Epub Date: 2025-09-11DOI: 10.1016/j.prmcm.2025.100690
Kiren Mustafa , Noreen Akhtar , Hina Khalid , Madiha Younas , Muhammad Tariq Saeed , Yuanda Song , Zhihe Li , Hassan Mohamed
Background
Ficus carica (无花果 wúhuāguǒ) is valued in traditional Chinese medicine (TCM) and nutrition for its rich phytochemical content. Our prior research showed a crude fig extract (FLA) selectively fought liver cancer cells (HepG2) in vitro while sparing normal cells.
Purpose
We aimed to isolate an active compound from FLA and analyze the potent bioactivities, particularly anticancer potential, through in vitro and computational studies.
Method
An innovative strategy combined fractionation by vacuum liquid chromatography (VLC) on silica gel (using six non-polar to polar solvent gradients) with thin layer chromatography (TLC) and bioactivity screening on liver (HepG2) and gastric (SGC-7901) cancer cell lines, and antimicrobial assay. The active Fraction 2 (Fr-2) was repeatedly sub-fractionated using Sephadex LH-20 column chromatography and TLC to isolate psoralen. Its mechanism of action against key cancer markers was evaluated via RT-qPCR, molecular docking, and ADMET pharmacokinetic analysis, with silymarin as a comparator.
Results
Fractionation of FLA yielded Fr- 2 (Hexane: Ethyl acetate, 50:50) with the IC50 (mg/mL) against HepG2 (0.31 ± 0.1) and SGC-7901 (0.124 ± 0.05) among the six tested fractions. It also exhibited antimicrobial activity, showing maximum inhibition zones (mm) against Aspergillus flavus FL (18± 0.4 mm), Penicillium chrysogenum FL (20 ± 0.7 mm), and Pseudomonas aeruginosa (17 ± 0.8 mm). Sub-fractionation of Fr- 2 led to the identification of psoralen, which decreased the genetic expression of tumor suppressor Tp53, anti-apoptotic (Bcl2) and Cell cycle kinases (CDK1 and CDK5). Molecular interaction via molecular docking against critical cancer regulators: Tp53, oncoproteins MDM2 and Bcl2, and CDK1/CDK5 also revealed the strong binding affinity of Psoralen. Psoralen demonstrates a novel mechanism of action by dual targeting of the MDM2-p53 axis: it binds p53′s N-TAD (Arg23, -8.8 kcal/mol) to reduce ubiquitination, while competitively inhibiting MDM2 (-5.8 kcal/mol) to stabilize Tp53 and induce apoptosis. Comparative ADMET analysis revealed psoralen's superior water solubility and oral bioavailability (96.67 % absorption) versus silymarin.
Conclusion
The active Fr-2, featuring psoralen, demonstrates broad antimicrobial and anticancer activity by potentially inhibiting the MDM2-p53 pathway to induce apoptosis, and it exhibits a superior ADMET profile compared to silymarin.
{"title":"Psoralen from Ficus carica: Fractionation, bioactivity, and toxicological-pharmacokinetic comparison with silymarin","authors":"Kiren Mustafa , Noreen Akhtar , Hina Khalid , Madiha Younas , Muhammad Tariq Saeed , Yuanda Song , Zhihe Li , Hassan Mohamed","doi":"10.1016/j.prmcm.2025.100690","DOIUrl":"10.1016/j.prmcm.2025.100690","url":null,"abstract":"<div><h3>Background</h3><div><em>Ficus carica</em> (无花果 <em>wúhuāguǒ</em>) is valued in traditional Chinese medicine (TCM) and nutrition for its rich phytochemical content. Our prior research showed a crude fig extract (FLA) selectively fought liver cancer cells (HepG2) in vitro while sparing normal cells.</div></div><div><h3>Purpose</h3><div>We aimed to isolate an active compound from FLA and analyze the potent bioactivities, particularly anticancer potential, through in vitro and computational studies.</div></div><div><h3>Method</h3><div>An innovative strategy combined fractionation by vacuum liquid chromatography (VLC) on silica gel (using six non-polar to polar solvent gradients) with thin layer chromatography (TLC) and bioactivity screening on liver (HepG2) and gastric (SGC-7901) cancer cell lines, and antimicrobial assay. The active Fraction 2 (Fr-2) was repeatedly sub-fractionated using Sephadex LH-20 column chromatography and TLC to isolate psoralen. Its mechanism of action against key cancer markers was evaluated via RT-qPCR, molecular docking, and ADMET pharmacokinetic analysis, with silymarin as a comparator.</div></div><div><h3>Results</h3><div>Fractionation of FLA yielded Fr- 2 (Hexane: Ethyl acetate, 50:50) with the IC50 (mg/mL) against HepG2 (0.31 ± 0.1) and SGC-7901 (0.124 ± 0.05) among the six tested fractions. It also exhibited antimicrobial activity, showing maximum inhibition zones (mm) against <em>Aspergillus flavus</em> FL (18± 0.4 mm), <em>Penicillium chrysogenum</em> FL (20 ± 0.7 mm), and <em>Pseudomonas aeruginosa</em> (17 ± 0.8 mm). Sub-fractionation of Fr- 2 led to the identification of psoralen, which decreased the genetic expression of tumor suppressor Tp53, anti-apoptotic (Bcl2) and Cell cycle kinases (CDK1 and CDK5). Molecular interaction via molecular docking against critical cancer regulators: Tp53, oncoproteins MDM2 and Bcl2, and CDK1/CDK5 also revealed the strong binding affinity of Psoralen. Psoralen demonstrates a novel mechanism of action by dual targeting of the MDM2-p53 axis: it binds p53′s N-TAD (Arg23, -8.8 kcal/mol) to reduce ubiquitination, while competitively inhibiting MDM2 (-5.8 kcal/mol) to stabilize Tp53 and induce apoptosis. Comparative ADMET analysis revealed psoralen's superior water solubility and oral bioavailability (96.67 % absorption) versus silymarin.</div></div><div><h3>Conclusion</h3><div>The active Fr-2, featuring psoralen, demonstrates broad antimicrobial and anticancer activity by potentially inhibiting the MDM2-p53 pathway to induce apoptosis, and it exhibits a superior ADMET profile compared to silymarin.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"17 ","pages":"Article 100690"},"PeriodicalIF":0.0,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145107938","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：