Pub Date : 2026-02-02DOI: 10.1016/j.prenap.2026.100543
Dorcas Akuorkor Teiko , Patrick Amoateng , Wonder Kofi Mensah Abotsi , Eric Boakye-Gyasi , Newman Osafo
Migraine, a common neurological disorder, is marked by severe headache with associated symptoms such as light and sound sensitivity, vomiting and cutaneous allodynia. Nitroglycerin (NTG) is widely utilized to induce migraine in rodents due to its ability to replicate central and peripheral sensitization as observed in human migraine patients. The current study investigated the prophylactic and therapeutic effects of geraniin, a polyphenolic ellagitannin, on acute migraine induced with nitroglycerin (NTG) to assess mechanical and thermal hypersensitivities in Sprague Dawley rats. Migraine-like symptoms were induced by NTG (5 mg/kg, i.p.) administration. Behavioural assays including mechanical sensitivity (von Frey), cold hyperalgesia (acetone test) and thermal nociception (hot plate) were conducted. Geraniin was administered in both preventive and therapeutic protocols at 3, 10 and 30 mg/kg. The probable involvement of 5-HT1B/1D receptors in geraniin’s acute anti-migraine action was studied. Geraniin significantly reversed these responses in a dose-dependent manner in both prophylactic and therapeutic settings. Mechanistically, geraniin’s effects were reversed by the 5-HT1B/1D antagonist (GR127935), suggesting its action may be associated with the serotonergic pathway of migraine development. Geraniin demonstrates robust anti-nociceptive effects in an acute NTG-induced migraine model. It can therefore by further studied as a potential therapeutic candidate for migraine management.
{"title":"Geraniin alleviates nitroglycerine (NTG)-induced acute migraine in Sprague Dawley rats","authors":"Dorcas Akuorkor Teiko , Patrick Amoateng , Wonder Kofi Mensah Abotsi , Eric Boakye-Gyasi , Newman Osafo","doi":"10.1016/j.prenap.2026.100543","DOIUrl":"10.1016/j.prenap.2026.100543","url":null,"abstract":"<div><div>Migraine, a common neurological disorder, is marked by severe headache with associated symptoms such as light and sound sensitivity, vomiting and cutaneous allodynia. Nitroglycerin (NTG) is widely utilized to induce migraine in rodents due to its ability to replicate central and peripheral sensitization as observed in human migraine patients. The current study investigated the prophylactic and therapeutic effects of geraniin, a polyphenolic ellagitannin, on acute migraine induced with nitroglycerin (NTG) to assess mechanical and thermal hypersensitivities in Sprague Dawley rats. Migraine-like symptoms were induced by NTG (5 mg/kg, i.p.) administration. Behavioural assays including mechanical sensitivity (von Frey), cold hyperalgesia (acetone test) and thermal nociception (hot plate) were conducted. Geraniin was administered in both preventive and therapeutic protocols at 3, 10 and 30 mg/kg. The probable involvement of 5-HT<sub>1B/1D</sub> receptors in geraniin’s acute anti-migraine action was studied. Geraniin significantly reversed these responses in a dose-dependent manner in both prophylactic and therapeutic settings. Mechanistically, geraniin’s effects were reversed by the 5-HT<sub>1B/1D</sub> antagonist (GR127935), suggesting its action may be associated with the serotonergic pathway of migraine development. Geraniin demonstrates robust anti-nociceptive effects in an acute NTG-induced migraine model. It can therefore by further studied as a potential therapeutic candidate for migraine management.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100543"},"PeriodicalIF":0.0,"publicationDate":"2026-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146173583","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 : 2026-01-31DOI: 10.1016/j.prenap.2026.100532
V. Saran, A. Jeeva, G. Syamala
Polyphenols derived from Chinese herbal medicine possess a broad spectrum of pharmacological activities, including antioxidant, anti-inflammatory, anti-tumor, and cardioprotective effects. Despite their therapeutic potential, the clinical application of polyphenols is often limited by poor aqueous solubility, low membrane permeability, rapid metabolism, and limited bioavailability. These pharmacokinetic challenges significantly hinder their systemic efficacy and therapeutic outcomes. This review explores how advanced drug delivery strategies have been employed to overcome these limitations and enhance the clinical potential of polyphenolic compounds commonly used in Traditional Chinese Medicine (TCM). We focus on seven representative polyphenols curcumin, rutin, quercetin, resveratrol, kaempferol, tannins, and epigallocatechin gallate (EGCG)detailing their absorption, distribution, metabolism, and excretion (ADME) profiles and the obstacles faced in conventional administration. Innovative delivery platforms such as phytosomes, liposomes, micelles, solid lipid nanoparticles, nanoemulsions, self-microemulsifying drug delivery systems (SMEDDS), cyclodextrin complexes, dendrimers, nanocrystals, prodrug strategies, and transdermal systems are comprehensively reviewed. These systems have demonstrated considerable success in improving solubility, protecting polyphenols from premature degradation, enhancing permeability, enabling sustained release, and allowing for targeted delivery. Furthermore, we discuss how the integration of modern nanotechnology with traditional ethnopharmacological knowledge not only improves the pharmacokinetic properties of polyphenols but also supports their use in evidence-based and standardized therapies. This fusion represents a promising pathway to translate bioactive herbal components into effective clinical treatments. Ultimately, the review emphasizes the need for continued interdisciplinary research to fully unlock the potential of Chinese herbal polyphenols in modern therapeutic contexts
{"title":"Nanotechnology-enabled delivery systems to improve the bioavailability and efficacy of polyphenolic compounds","authors":"V. Saran, A. Jeeva, G. Syamala","doi":"10.1016/j.prenap.2026.100532","DOIUrl":"10.1016/j.prenap.2026.100532","url":null,"abstract":"<div><div>Polyphenols derived from Chinese herbal medicine possess a broad spectrum of pharmacological activities, including antioxidant, anti-inflammatory, anti-tumor, and cardioprotective effects. Despite their therapeutic potential, the clinical application of polyphenols is often limited by poor aqueous solubility, low membrane permeability, rapid metabolism, and limited bioavailability. These pharmacokinetic challenges significantly hinder their systemic efficacy and therapeutic outcomes. This review explores how advanced drug delivery strategies have been employed to overcome these limitations and enhance the clinical potential of polyphenolic compounds commonly used in Traditional Chinese Medicine (TCM). We focus on seven representative polyphenols curcumin, rutin, quercetin, resveratrol, kaempferol, tannins, and epigallocatechin gallate (EGCG)detailing their absorption, distribution, metabolism, and excretion (ADME) profiles and the obstacles faced in conventional administration. Innovative delivery platforms such as phytosomes, liposomes, micelles, solid lipid nanoparticles, nanoemulsions, self-microemulsifying drug delivery systems (SMEDDS), cyclodextrin complexes, dendrimers, nanocrystals, prodrug strategies, and transdermal systems are comprehensively reviewed. These systems have demonstrated considerable success in improving solubility, protecting polyphenols from premature degradation, enhancing permeability, enabling sustained release, and allowing for targeted delivery. Furthermore, we discuss how the integration of modern nanotechnology with traditional ethnopharmacological knowledge not only improves the pharmacokinetic properties of polyphenols but also supports their use in evidence-based and standardized therapies. This fusion represents a promising pathway to translate bioactive herbal components into effective clinical treatments. Ultimately, the review emphasizes the need for continued interdisciplinary research to fully unlock the potential of Chinese herbal polyphenols in modern therapeutic contexts</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100532"},"PeriodicalIF":0.0,"publicationDate":"2026-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146173528","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 : 2026-01-30DOI: 10.1016/j.prenap.2026.100539
Daniel Hassan Mhya , Asiya Muhammad Kabir , Evelyn Bulus Nkarina , Fatima Muhammad Dambam , Theophilus Tagun Dawus
Purpose
This study aimed to investigate extract mixture of Hibiscus sabdariffa and Citrus paradisi on glucose-induced cataract and glomerulopathy.
Methodology
Hibiscus sabdariffa (HPE) and Citrus paradisi (CPE) samples were collected from local farmers in Bauchi and Plateau States. The samples were air-dried and aqueous-extracted. The extracts obtained were screened for antioxidant molecules (phenolic, carotenoids, vitamin A, C and E) before re-extracted for anthocyanins from HPE and naringin from CPE, and tested for anti-cataractogenic and anti-glomerulopathic activities alone and in combination on rats' lens and glomeruli exposed to high glucose solution. Malondialdehyde and antioxidant enzymes were assayed spectrophotometrically while the morphology of the lens was analyzed microscopically.
Results
The results revealed that extracts of HPE and CPE are high in antioxidants such as phenolics, carotenoids, and vitamins A, C, and E. Lens exposed to high glucose developed cataracts, and treatment with extracts of HPE and CPE alleviated cataracts by reducing oxidative stress and preventing lens opacity. Treatment of glomeruli exposed to high glucose with the mixed extracts (HPE and CPE) enhanced its glucose absorption at 6.07 ± 1.31 mM compared to 1.87 ± 0.62 mM (negative control), antioxidant enzyme activities: CAT (µmol H₂O₂/min) 8.65 ± 0.43 against negative control (3.67 ± 0.32), SOD (U/mL) 14.75 ± 0.84 against negative control (6.12 ± 0.54), Peroxidase (μM tetraguaiacol/min) 11.89 ± 0.60 against negative control; 5.28 ± 0.48 and lower malondialdehyde (µM/L) at 3.97 ± 0.24 against negative control; 9.73 ± 0.65.
Conclusion
The study concluded that the efficacy of HPE and CPE extracts in preventing cataracts and glomerulopathy may be augmented through their combination.
{"title":"Impact of combining Hibiscus sabdariffa and Citrus paradisi extracts on glucose-induced cataracts and glomerulopathy","authors":"Daniel Hassan Mhya , Asiya Muhammad Kabir , Evelyn Bulus Nkarina , Fatima Muhammad Dambam , Theophilus Tagun Dawus","doi":"10.1016/j.prenap.2026.100539","DOIUrl":"10.1016/j.prenap.2026.100539","url":null,"abstract":"<div><h3>Purpose</h3><div>This study aimed to investigate extract mixture of <em>Hibiscus sabdariffa</em> and <em>Citrus paradisi</em> on glucose-induced cataract and glomerulopathy.</div></div><div><h3>Methodology</h3><div><em>Hibiscus sabdariffa</em> (HPE) and <em>Citrus paradisi</em> (CPE) samples were collected from local farmers in Bauchi and Plateau States. The samples were air-dried and aqueous-extracted. The extracts obtained were screened for antioxidant molecules (phenolic, carotenoids, vitamin A, C and E) before re-extracted for anthocyanins from HPE and naringin from CPE, and tested for anti-cataractogenic and anti-glomerulopathic activities alone and in combination on rats' lens and glomeruli exposed to high glucose solution. Malondialdehyde and antioxidant enzymes were assayed spectrophotometrically while the morphology of the lens was analyzed microscopically.</div></div><div><h3>Results</h3><div>The results revealed that extracts of HPE and CPE are high in antioxidants such as phenolics, carotenoids, and vitamins A, C, and E. Lens exposed to high glucose developed cataracts, and treatment with extracts of HPE and CPE alleviated cataracts by reducing oxidative stress and preventing lens opacity. Treatment of glomeruli exposed to high glucose with the mixed extracts (HPE and CPE) enhanced its glucose absorption at 6.07 ± 1.31 mM compared to 1.87 ± 0.62 mM (negative control), antioxidant enzyme activities: CAT (µmol H₂O₂/min) 8.65 ± 0.43 against negative control (3.67 ± 0.32), SOD (U/mL) 14.75 ± 0.84 against negative control (6.12 ± 0.54), Peroxidase (μM tetraguaiacol/min) 11.89 ± 0.60 against negative control; 5.28 ± 0.48 and lower malondialdehyde (µM/L) at 3.97 ± 0.24 against negative control; 9.73 ± 0.65.</div></div><div><h3>Conclusion</h3><div>The study concluded that the efficacy of HPE and CPE extracts in preventing cataracts and glomerulopathy may be augmented through their combination.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100539"},"PeriodicalIF":0.0,"publicationDate":"2026-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146173587","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 : 2026-01-30DOI: 10.1016/j.prenap.2026.100542
Supriya Sharma , Divya Sharma , Chetan Paul Singh , Yogesh P. Bharitkar , Mahaveer Dhobi
Background
This investigation is driven by the traditional use of Maytenus emarginata in ancient medicinal practices for its alleged anti-inflammatory properties, which have yet to be thoroughly validated through scientific research.
Purpose
The study aims to identify the phytochemical profiling of Maytenus emarginata crude extract and investigate its anti-inflammatory activity through in vitro and in vivo approaches.
Methods
The methanol extract (ME) and its bioactive n-hexane fraction (HME) from Maytenus emarginata were evaluated for their anti-inflammatory action through ELISA and flow cytometric analysis. Bioassay-guided fractionation followed by column chromatography was used to isolate bioactive compounds. Furthermore, in vivo studies used the rat paw edema model, which induces inflammation with carrageenan, to evaluate the anti-inflammatory action of Maytenus emarginata.
Results
ME and its bioactive fraction (HME) demonstrated significant anti-inflammatory activity in both models. Among all tested fractions, HME effectively inhibits the release of TNF-α and IL-6, primarily by decreasing the levels of NF-κB in LPS-stimulated macrophages. This inhibitory effect was further supported by flow cytometric analysis. Subsequent phytochemical analysis of HME resulted in the characterization of three compounds: lupeol, stigmasterol, and β-amyrin. The in vivo model further confirmed the anti-inflammatory activity of HME, with 50 mg/kg showing the greatest edema reduction in the rat model.
Conclusion
Maytenus emarginata (Willd.) Ding Hou demonstrated notable anti-inflammatory effects, reflected by decreased levels of pro-inflammatory cytokines and changes associated with NF-κB signalling.
{"title":"Potential benefits of Maytenus emarginata (Willd.) Ding Hou against inflammation via suppression of pro-inflammatory cytokines","authors":"Supriya Sharma , Divya Sharma , Chetan Paul Singh , Yogesh P. Bharitkar , Mahaveer Dhobi","doi":"10.1016/j.prenap.2026.100542","DOIUrl":"10.1016/j.prenap.2026.100542","url":null,"abstract":"<div><h3>Background</h3><div>This investigation is driven by the traditional use of <em>Maytenus emarginata</em> in ancient medicinal practices for its alleged anti-inflammatory properties, which have yet to be thoroughly validated through scientific research.</div></div><div><h3>Purpose</h3><div>The study aims to identify the phytochemical profiling of <em>Maytenus emarginata</em> crude extract and investigate its anti-inflammatory activity through <em>in vitro</em> and <em>in vivo</em> approaches.</div></div><div><h3>Methods</h3><div>The methanol extract (ME) and its bioactive n-hexane fraction (HME) from <em>Maytenus emarginata</em> were evaluated for their anti-inflammatory action through ELISA and flow cytometric analysis. Bioassay-guided fractionation followed by column chromatography was used to isolate bioactive compounds. Furthermore, <em>in vivo</em> studies used the rat paw edema model, which induces inflammation with carrageenan, to evaluate the anti-inflammatory action of <em>Maytenus emarginata</em>.</div></div><div><h3>Results</h3><div>ME and its bioactive fraction (HME) demonstrated significant anti-inflammatory activity in both models. Among all tested fractions, HME effectively inhibits the release of TNF-α and IL-6, primarily by decreasing the levels of NF-κB in LPS-stimulated macrophages. This inhibitory effect was further supported by flow cytometric analysis. Subsequent phytochemical analysis of HME resulted in the characterization of three compounds: lupeol, stigmasterol, and β-amyrin. The <em>in vivo</em> model further confirmed the anti-inflammatory activity of HME, with 50 mg/kg showing the greatest edema reduction in the rat model.</div></div><div><h3>Conclusion</h3><div><em>Maytenus emarginata</em> (Willd.) Ding Hou demonstrated notable anti-inflammatory effects, reflected by decreased levels of pro-inflammatory cytokines and changes associated with NF-κB signalling.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100542"},"PeriodicalIF":0.0,"publicationDate":"2026-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146173534","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 : 2026-01-30DOI: 10.1016/j.prenap.2026.100541
Sanjib Bhattacharya
The nanotechnology-based combined novel delivery of extant cancer chemotherapeutic agents with dietary phytochemicals has been found to be remarkably more efficacious and viable than monotherapy or combinations thereof in conventional pharmaceutical dosage forms to counteract cancer. The present review attempts to furnish an evidence-based account on relevant pre-clinical studies corroborating the fact of improved compliance through such combinatorial interventions, overcoming the admitted limitations against cancer. Nanoemulsion, nanosponge, nanosuspension, solid lipid nanoparticles (SLN), polymeric nanoparticles, metallic nanoparticles, carbon nanotubes (CWT), nanoliposomes, hybrid nanoparticles and nanostructured lipid carriers (NLC) were such novel nanocarriers. Breast cancer, gastric cancer, lung cancer, liver cancer, ovarian cancer, cervical cancer, brain cancer, colon cancer, and prostate cancer were thus counteracted as cell lines in vitro or in vivo in experimental animals. Curcumin was shown to be the most prevalent dietary phytochemical used effectively followed by resveratrol, quercetin, berberine and others. Lipid-based nanocarriers, polymeric nanoparticles, liposomes and micelles were found to be the most used nanoplatforms. However, there are a number of gaps that need to be addressed in pre-clinical and clinical stages, including optimization of drug combination, scalable manufacturing, physiological barriers, complexity of interactions, understanding tumor and multi-drug antitumor mechanisms, long-term stability of novel combinatorial nanoformulations, safety concerns and food/drug regulatory matters. Future investigations with the promising candidates in this direction may open a new window in cancer chemotherapy to achieve optimal effects in humans.
{"title":"Harnessing cancer chemotherapy with dietary phytochemicals by nanotechnology","authors":"Sanjib Bhattacharya","doi":"10.1016/j.prenap.2026.100541","DOIUrl":"10.1016/j.prenap.2026.100541","url":null,"abstract":"<div><div>The nanotechnology-based combined novel delivery of extant cancer chemotherapeutic agents with dietary phytochemicals has been found to be remarkably more efficacious and viable than monotherapy or combinations thereof in conventional pharmaceutical dosage forms to counteract cancer. The present review attempts to furnish an evidence-based account on relevant pre-clinical studies corroborating the fact of improved compliance through such combinatorial interventions, overcoming the admitted limitations against cancer. Nanoemulsion, nanosponge, nanosuspension, solid lipid nanoparticles (SLN), polymeric nanoparticles, metallic nanoparticles, carbon nanotubes (CWT), nanoliposomes, hybrid nanoparticles and nanostructured lipid carriers (NLC) were such novel nanocarriers. Breast cancer, gastric cancer, lung cancer, liver cancer, ovarian cancer, cervical cancer, brain cancer, colon cancer, and prostate cancer were thus counteracted as cell lines <em>in vitro</em> or <em>in vivo</em> in experimental animals. Curcumin was shown to be the most prevalent dietary phytochemical used effectively followed by resveratrol, quercetin, berberine and others. Lipid-based nanocarriers, polymeric nanoparticles, liposomes and micelles were found to be the most used nanoplatforms. However, there are a number of gaps that need to be addressed in pre-clinical and clinical stages, including optimization of drug combination, scalable manufacturing, physiological barriers, complexity of interactions, understanding tumor and multi-drug antitumor mechanisms, long-term stability of novel combinatorial nanoformulations, safety concerns and food/drug regulatory matters. Future investigations with the promising candidates in this direction may open a new window in cancer chemotherapy to achieve optimal effects in humans.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100541"},"PeriodicalIF":0.0,"publicationDate":"2026-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146173535","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 : 2026-01-29DOI: 10.1016/j.prenap.2026.100524
Mahalakshmi Devaraji , Punniyakoti Veeraveedu Thanikachalam , H. Mohamed Ishaq , D. Vidhya Varshini , Karthika Ramesh , Kannan R. Ramaswamy
Objective
The aim of the present study was to evaluate the anticancer effects of Moringa oleifera fruit extracts and their bioactive polyphenols, specifically quercetin and kaempferol, against colorectal cancer cell lines, and to validate their molecular interactions with relevant target proteins through in silico and in vitro approaches.
Materials and methods
Preliminary phytochemical screening and GC-MS analysis were conducted to identify the phytochemical composition of Moringa oleifera. Anticancer activity was evaluated using MTT assay against HCT-116 colorectal cancer cells, microscopy, and AO/EtBr staining. Additionally, molecular docking, ADMET analysis, and molecular dynamics (MD) simulations were performed to assess the binding affinity and stability of major phytoconstituents against BRAF V600E—a mutation in the BRAF gene implicated in colorectal cancer.
Results
The hydroalcoholic fruit extract confirmed the presence of key secondary metabolites. GC-MS identified 26 bioactive compounds, with (E)-9-Octadecenoic acid ethyl ester and cis-Vaccenic acid in high quantities. The extract showed concentration-dependent cytotoxicity in MTT assays against HCT-116 colorectal cancer cells, with an IC₅₀ of 13.076 ± 3.288 µg/ml. Apoptotic effects were evident through AO/EtBr staining and phase-contrast microscopy, with outcomes comparable to Paclitaxel. In silico, 10 major phytoconstituents were docked with BRAF V600E kinase (PDB ID: 6XFP), an oncogenic target in colorectal cancer. Quercetin and Kaempferol showed stronger binding affinities (-11.1685 and −10.4259 kcal/mol) than Encorafenib (-10.0141 kcal/mol). MD simulations confirmed the stability of the Quercetin–BRAF complex, while Kaempferol showed lower stability.
Conclusions
This is the first report on the anticancer effects of Moringa oleifera fruit extract against colorectal cancer via BRAF targeting. Quercetin emerged as a promising natural BRAF inhibitor, meriting further in vivo validation.
{"title":"GC-MS profiling, anticancer activity of Moringa oleifera Lam. hydroalcoholic fruit extract against colorectal cancer cells, and In Silico targeting of BRAF in the serrated pathway","authors":"Mahalakshmi Devaraji , Punniyakoti Veeraveedu Thanikachalam , H. Mohamed Ishaq , D. Vidhya Varshini , Karthika Ramesh , Kannan R. Ramaswamy","doi":"10.1016/j.prenap.2026.100524","DOIUrl":"10.1016/j.prenap.2026.100524","url":null,"abstract":"<div><h3>Objective</h3><div>The aim of the present study was to evaluate the anticancer effects of Moringa oleifera fruit extracts and their bioactive polyphenols, specifically quercetin and kaempferol, against colorectal cancer cell lines, and to validate their molecular interactions with relevant target proteins through in silico and in vitro approaches.</div></div><div><h3>Materials and methods</h3><div>Preliminary phytochemical screening and GC-MS analysis were conducted to identify the phytochemical composition of <em>Moringa oleifera</em>. Anticancer activity was evaluated using MTT assay against HCT-116 colorectal cancer cells, microscopy, and AO/EtBr staining. Additionally, molecular docking, ADMET analysis, and molecular dynamics (MD) simulations were performed to assess the binding affinity and stability of major phytoconstituents against BRAF V600E—a mutation in the BRAF gene implicated in colorectal cancer.</div></div><div><h3>Results</h3><div>The hydroalcoholic fruit extract confirmed the presence of key secondary metabolites. GC-MS identified 26 bioactive compounds, with (<em>E</em>)-9-Octadecenoic acid ethyl ester and cis-Vaccenic acid in high quantities. The extract showed concentration-dependent cytotoxicity in MTT assays against HCT-116 colorectal cancer cells, with an IC₅₀ of 13.076 ± 3.288 µg/ml. Apoptotic effects were evident through AO/EtBr staining and phase-contrast microscopy, with outcomes comparable to Paclitaxel. In silico, 10 major phytoconstituents were docked with BRAF V600E kinase (PDB ID: 6XFP), an oncogenic target in colorectal cancer. Quercetin and Kaempferol showed stronger binding affinities (-11.1685 and −10.4259 kcal/mol) than Encorafenib (-10.0141 kcal/mol). MD simulations confirmed the stability of the Quercetin–BRAF complex, while Kaempferol showed lower stability.</div></div><div><h3>Conclusions</h3><div>This is the first report on the anticancer effects of <em>Moringa oleifera</em> fruit extract against colorectal cancer via BRAF targeting. Quercetin emerged as a promising natural BRAF inhibitor, meriting further in vivo validation.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100524"},"PeriodicalIF":0.0,"publicationDate":"2026-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146077649","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 : 2026-01-28DOI: 10.1016/j.prenap.2026.100537
Cláudia Bernadete de Souza Lira, Janaína Vital de Albuquerque, Thâmarah de Albuquerque Lima, Leydianne Leite de Siqueira Patriota, Thiago Henrique Napoleão
This review analyzed and synthesized current evidence on the therapeutic effects of Erythrina velutina Willd. extracts, with a particular focus on their application in the treatment of nervous system diseases and disorders. The objective was to identify the biological activities of these extracts and their relevance in managing conditions such as anxiety, depression, and other neurological pathologies. A comprehensive literature search was conducted across PubMed, Web of Science, ScienceDirect and Scopus databases, with no temporal restrictions. After applying relevant search terms and exclusion criteria, 12 studies were selected: 11 were conducted in vivo (two of which included complementary in vitro analysis and one also incorporating ex vivo experiments), and 1 was performed exclusively in vitro. Notably, E. velutina extracts demonstrated anxiolytic and neuroprotective properties, along with beneficial effects on sleep regulation, memory, and motor function. Several studies also explored their potential roles in pain modulation and in experimental models of neurodegenerative diseases such as Alzheimer’s and Parkinson’s, as well as psychiatric disorders including schizophrenia. Despite methodological differences across studies, the findings consistently support the therapeutic potential of E. velutina, particularly in relation to central nervous system depression, cognitive enhancement, and antioxidant activity. However, a significant gap remains in the chemical characterization of the extracts. In conclusion, E. velutina emerges as a promising candidate for further research and development of safer, more effective therapeutic agents, while also contributing to the validation of its traditional medicinal uses.
本文分析和综合了目前国内外关于绒赤藓的治疗作用。提取物,特别关注其在治疗神经系统疾病和失调中的应用。目的是确定这些提取物的生物活性及其在治疗诸如焦虑、抑郁和其他神经系统疾病方面的相关性。在PubMed、Web of Science、ScienceDirect和Scopus数据库中进行了全面的文献检索,没有时间限制。应用相关检索词和排除标准后,共筛选出12项研究,其中11项为体内实验(其中2项为体外互补实验,1项为体外实验),1项为纯体外实验。值得注意的是,白芦巴提取物显示出抗焦虑和神经保护特性,以及对睡眠调节、记忆和运动功能的有益作用。一些研究还探索了它们在疼痛调节和神经退行性疾病(如阿尔茨海默病和帕金森病)以及精神疾病(包括精神分裂症)的实验模型中的潜在作用。尽管不同研究的方法存在差异,但研究结果一致支持绒皮草的治疗潜力,特别是在中枢神经系统抑郁、认知增强和抗氧化活性方面。然而,在提取物的化学表征方面仍有很大的差距。综上所述,胡芦巴为进一步研究和开发更安全、更有效的治疗药物提供了一个有希望的候选药物,同时也有助于验证其传统药用价值。
{"title":"Neurotherapeutic effects of Erythrina velutina Willd. extracts: A systematic review","authors":"Cláudia Bernadete de Souza Lira, Janaína Vital de Albuquerque, Thâmarah de Albuquerque Lima, Leydianne Leite de Siqueira Patriota, Thiago Henrique Napoleão","doi":"10.1016/j.prenap.2026.100537","DOIUrl":"10.1016/j.prenap.2026.100537","url":null,"abstract":"<div><div>This review analyzed and synthesized current evidence on the therapeutic effects of <em>Erythrina velutina</em> Willd. extracts, with a particular focus on their application in the treatment of nervous system diseases and disorders. The objective was to identify the biological activities of these extracts and their relevance in managing conditions such as anxiety, depression, and other neurological pathologies. A comprehensive literature search was conducted across PubMed, Web of Science, ScienceDirect and Scopus databases, with no temporal restrictions. After applying relevant search terms and exclusion criteria, 12 studies were selected: 11 were conducted <em>in vivo</em> (two of which included complementary <em>in vitro</em> analysis and one also incorporating <em>ex vivo</em> experiments), and 1 was performed exclusively <em>in vitro</em>. Notably, <em>E. velutina</em> extracts demonstrated anxiolytic and neuroprotective properties, along with beneficial effects on sleep regulation, memory, and motor function. Several studies also explored their potential roles in pain modulation and in experimental models of neurodegenerative diseases such as Alzheimer’s and Parkinson’s, as well as psychiatric disorders including schizophrenia. Despite methodological differences across studies, the findings consistently support the therapeutic potential of <em>E. velutina</em>, particularly in relation to central nervous system depression, cognitive enhancement, and antioxidant activity. However, a significant gap remains in the chemical characterization of the extracts. In conclusion, <em>E. velutina</em> emerges as a promising candidate for further research and development of safer, more effective therapeutic agents, while also contributing to the validation of its traditional medicinal uses.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100537"},"PeriodicalIF":0.0,"publicationDate":"2026-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146077652","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}
The genus Flemingia Roxb. ex W.T. Aiton (Leguminosae) comprises approximately 48 species and two varieties, widely distributed across tropical and subtropical regions. Various Flemingia species hold significant ethnopharmacological relevance, particularly in Asia and Africa, where different plant parts are traditionally used to treat inflammatory disorders, rheumatism, gastrointestinal ailments, reproductive health issues, and infectious diseases. Beyond medicinal applications, Flemingia species contribute to agroforestry and natural dye production, with compounds like flemingin used in silk dyeing. Phytochemical investigations reveal a diverse array of bioactive compounds, including flavonoids such as genistein and auriculasin, chalcones, terpenoids, and anthraquinones, which contribute to their pharmacological activities. Scientific studies have demonstrated their antioxidant, antimicrobial, antidiabetic, hepatoprotective, neuroprotective, immunomodulatory, and anti-inflammatory properties. Certain species, such as F. vestita, F. macrophylla, and F. philippinensis exhibit potent anthelmintic, estrogenic, and anti-photoaging effects, while inhibitory activities against key enzymes like tyrosinase, neuraminidase, and xanthine oxidase suggest potential applications in metabolic disorders, dermatology, and infectious diseases. Despite the promising pharmacological potential, the toxicological profile of most Flemingia species remains largely unexplored, and clinical validation is limited. Further studies focusing on bioassay-guided isolation, mechanistic pathways, pharmacokinetics, and comprehensive safety evaluations are essential to advance their therapeutic applications and ensure their sustainable utilization. This review consolidates existing knowledge on the botanical, ethnopharmacological, phytochemical, pharmacological, and toxicological aspects of Flemingia species, highlighting research gaps and future directions in drug discovery.
{"title":"Exploring Flemingia: A comprehensive review of botanical, phytochemical, and therapeutic insights","authors":"N.M. Sindhikar , S.K. Gavade , M.M. Lekhak , U.B. Jagtap , V.A. Bapat","doi":"10.1016/j.prenap.2026.100535","DOIUrl":"10.1016/j.prenap.2026.100535","url":null,"abstract":"<div><div>The genus <em>Flemingia</em> Roxb. ex W.T. Aiton (Leguminosae) comprises approximately 48 species and two varieties, widely distributed across tropical and subtropical regions. Various <em>Flemingia</em> species hold significant ethnopharmacological relevance, particularly in Asia and Africa, where different plant parts are traditionally used to treat inflammatory disorders, rheumatism, gastrointestinal ailments, reproductive health issues, and infectious diseases. Beyond medicinal applications, <em>Flemingia</em> species contribute to agroforestry and natural dye production, with compounds like flemingin used in silk dyeing. Phytochemical investigations reveal a diverse array of bioactive compounds, including flavonoids such as genistein and auriculasin, chalcones, terpenoids, and anthraquinones, which contribute to their pharmacological activities. Scientific studies have demonstrated their antioxidant, antimicrobial, antidiabetic, hepatoprotective, neuroprotective, immunomodulatory, and anti-inflammatory properties. Certain species, such as <em>F. vestita</em>, <em>F. macrophylla</em>, and <em>F. philippinensis</em> exhibit potent anthelmintic, estrogenic, and anti-photoaging effects, while inhibitory activities against key enzymes like tyrosinase, neuraminidase, and xanthine oxidase suggest potential applications in metabolic disorders, dermatology, and infectious diseases. Despite the promising pharmacological potential, the toxicological profile of most <em>Flemingia</em> species remains largely unexplored, and clinical validation is limited. Further studies focusing on bioassay-guided isolation, mechanistic pathways, pharmacokinetics, and comprehensive safety evaluations are essential to advance their therapeutic applications and ensure their sustainable utilization. This review consolidates existing knowledge on the botanical, ethnopharmacological, phytochemical, pharmacological, and toxicological aspects of <em>Flemingia</em> species, highlighting research gaps and future directions in drug discovery.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100535"},"PeriodicalIF":0.0,"publicationDate":"2026-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146173536","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 : 2026-01-27DOI: 10.1016/j.prenap.2026.100538
Hamid Rehman , Nida Gul , Khurshid Ahmad , Mazhar Iqbal , Aqib Hassan Ali Khan , Rehan Naeem
This study investigated the protective role of Curcuma longa L. extract (curcumin, CMN) against cypermethrin (CYP)-induced hepatic and renal injury in male albino rabbits. Animals were divided into four groups: control, CYP (25 mg kg⁻¹), CMN (50 mg kg⁻¹), and combined CYP + CMN, treated orally for 45 days. CYP administration markedly reduced hepatic and renal antioxidant enzymes, including SOD (47 %), CAT (39 %), and GPx (42 %), while elevating lipid peroxidation (61 %) and serum markers of liver (ALT 2.6-fold, AST 2.3-fold, ALP 2.1-fold) and kidney dysfunction was also increased (urea 58 %, creatinine 52 %). Co-treatment with CMN significantly restored antioxidant enzyme activities toward control levels (p < 0.01), normalized lipid profile indices, and improved histopathological architecture of hepatic and renal tissues. To complement experimental results, a computational regression model was trained on data to identify major predictors of CYP-induced oxidative stress. Binary classification model was developed to distinguish CYP-exposed (toxic) from CMN-protected (non-toxic) conditions using the same biochemical and enzymatic feature set. The classifier achieved outstanding performance, with overall accuracy of 100 %, area under the ROC curve (AUC = 1.0), precision (0.96), and recall (0.94), confirming a clear separation between the two physiological states. The Random forest model showed high predictive accuracy (R² = 0.98, RMSE = 29.20, MAPE = 1.1 %) The most discriminative predictors included SOD, GPX, and VLDL, of liver which consistently ranked among the top features in both regression and classification analyses. These results reinforce the experimental observations that hepatic antioxidant enzymes and lipid-associated parameters serve as reliable biomarkers for distinguishing oxidative injury from curcumin-mediated protection.
{"title":"An integrated binary classification and machine learning approach to decode curcumin's mitigation of cypermethrin-induced hepatorenal injury: Experimental and computational analysis","authors":"Hamid Rehman , Nida Gul , Khurshid Ahmad , Mazhar Iqbal , Aqib Hassan Ali Khan , Rehan Naeem","doi":"10.1016/j.prenap.2026.100538","DOIUrl":"10.1016/j.prenap.2026.100538","url":null,"abstract":"<div><div>This study investigated the protective role of <em>Curcuma longa</em> L. extract (curcumin, CMN) against cypermethrin (CYP)-induced hepatic and renal injury in male albino rabbits. Animals were divided into four groups: control, CYP (25 mg kg⁻¹), CMN (50 mg kg⁻¹), and combined CYP + CMN, treated orally for 45 days. CYP administration markedly reduced hepatic and renal antioxidant enzymes, including SOD (47 %), CAT (39 %), and GPx (42 %), while elevating lipid peroxidation (61 %) and serum markers of liver (ALT 2.6-fold, AST 2.3-fold, ALP 2.1-fold) and kidney dysfunction was also increased (urea 58 %, creatinine 52 %). Co-treatment with CMN significantly restored antioxidant enzyme activities toward control levels (p < 0.01), normalized lipid profile indices, and improved histopathological architecture of hepatic and renal tissues. To complement experimental results, a computational regression model was trained on data to identify major predictors of CYP-induced oxidative stress. Binary classification model was developed to distinguish CYP-exposed (toxic) from CMN-protected (non-toxic) conditions using the same biochemical and enzymatic feature set. The classifier achieved outstanding performance, with overall accuracy of 100 %<strong>,</strong> area under the ROC curve <strong>(</strong>AUC = 1.0<strong>),</strong> precision <strong>(</strong>0.96<strong>),</strong> and recall <strong>(</strong>0.94<strong>),</strong> confirming a clear separation between the two physiological states. The Random forest model showed high predictive accuracy (R² = 0.98, RMSE = 29.20, MAPE = 1.1 %) The most discriminative predictors included SOD<strong>,</strong> GPX<strong>,</strong> and VLDL<strong>,</strong> of liver which consistently ranked among the top features in both regression and classification analyses. These results reinforce the experimental observations that hepatic antioxidant enzymes and lipid-associated parameters serve as reliable biomarkers for distinguishing oxidative injury from curcumin-mediated protection.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100538"},"PeriodicalIF":0.0,"publicationDate":"2026-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146077650","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 : 2026-01-26DOI: 10.1016/j.prenap.2026.100536
Prity Lather, Dinesh Dhingra
Autism spectrum disorder (ASD) is a neurodevelopmental disorder. Two FDA approved drugs such as risperidone and aripiprazole have been reported to treat some symptoms of ASD in children and adolescents. But both these drugs have side effects. Therefore, it is worthwhile to explore safer alternatives such as medicinal plants and bioactive compounds for management of autism. Abietic acid, a resin present in various species of Pinus. It exhibits anti-depressant, memory improving, anti-inflammatory and antioxidant activities, suggesting its potential to ameliorate autism–like symptoms. The current study investigated the effect of abietic acid on sodium valproate- induced autism in male and female rat pups to assess sex- specific responses. For inducing autism, 400 mg/kg of sodium valproate was injected subcutaneously to pregnant female rats on 12th day of gestation. Abietic acid (7.5, 15, 30 mg/kg, p.o.) and standard drugs (diazepam, fluoxetine, and donepezil, i.p.) were given to separate groups of autistic pups from 26th to 40th postnatal days. Behavioural assessments revealed that autistic pups were depressed; showed repetitive and anxious behaviours; showed impairment of learning and memory; and impairment of social interaction; and increased locomotion. Biochemical analysis showed increased brain oxidative stress parameters, acetylcholinesterase activity, neuro-inflammation and apoptosis along with decreased mitochondrial complexes activities. Abietic acid (15, 30 mg/kg) remarkably reversed these behavioural deficits and restored biochemical parameters towards normal in both male and female autistic pups. These findings indicated that abietic acid produced significant neuro-protective effects in autistic pups, possibly through inhibition of acetylcholinesterase activity, amelioration of neuro-inflammation, oxidative stress, mitochondrial dysfunction, and apoptosis. Overall, this study highlights the potential of abietic acid as a natural intervention for management of autism-like behaviours.
{"title":"Neuroprotective effect of abietic acid against sodium valproate induced autism in male and female rat pups","authors":"Prity Lather, Dinesh Dhingra","doi":"10.1016/j.prenap.2026.100536","DOIUrl":"10.1016/j.prenap.2026.100536","url":null,"abstract":"<div><div>Autism spectrum disorder (ASD) is a neurodevelopmental disorder. Two FDA approved drugs such as risperidone and aripiprazole have been reported to treat some symptoms of ASD in children and adolescents. But both these drugs have side effects. Therefore, it is worthwhile to explore safer alternatives such as medicinal plants and bioactive compounds for management of autism. Abietic acid, a resin present in various species of <em>Pinus</em>. It exhibits anti-depressant, memory improving, anti-inflammatory and antioxidant activities, suggesting its potential to ameliorate autism–like symptoms. The current study investigated the effect of abietic acid on sodium valproate- induced autism in male and female rat pups to assess sex- specific responses. For inducing autism, 400 mg/kg of sodium valproate was injected subcutaneously to pregnant female rats on 12th day of gestation. Abietic acid (7.5, 15, 30 mg/kg, p.o.) and standard drugs (diazepam, fluoxetine, and donepezil, i.p.) were given to separate groups of autistic pups from 26th to 40th postnatal days. Behavioural assessments revealed that autistic pups were depressed; showed repetitive and anxious behaviours; showed impairment of learning and memory; and impairment of social interaction; and increased locomotion. Biochemical analysis showed increased brain oxidative stress parameters, acetylcholinesterase activity, neuro-inflammation and apoptosis along with decreased mitochondrial complexes activities. Abietic acid (15, 30 mg/kg) remarkably reversed these behavioural deficits and restored biochemical parameters towards normal in both male and female autistic pups. These findings indicated that abietic acid produced significant neuro-protective effects in autistic pups, possibly through inhibition of acetylcholinesterase activity, amelioration of neuro-inflammation, oxidative stress, mitochondrial dysfunction, and apoptosis. Overall, this study highlights the potential of abietic acid as a natural intervention for management of autism-like behaviours.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100536"},"PeriodicalIF":0.0,"publicationDate":"2026-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146077784","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}