Objective: Human health has continued to be at risk from lead exposure. This study explored the antioxidative potential of ethanol extract of ripe Musa sapientum peels to protect against lead acetate-induced neuronal insult in female wistar rats. Methods: Thirty adult female rats (120-160 g) were randomly divided into six groups (n = 5): Group 1 (control group) received 10 mL/kg of distilled water; Group 2 received 100 mg/kg lead acetate. Group 3 received 2.5 mg/kg of donepezil. Groups 4 to 6 received 100, 200, and 400 mg/kg ethanol extract of ripe M sapientum, respectively, via oral gavage. Groups 2 to 5 were co-treated with 100 mg/kg lead acetate for 21 days. Neurobehavioral parameter, biochemical and histological analyses of the hippocampus were determined. Recognition memory was evaluated using Novel Object Recognition Test. Results: There was a significant ( p < 0.05) increase in total exploration, discrimination index, and percentage alternation in the ethanol extract M sapientum-treated groups compared with the lead acetate-induced group. M sapientum ethanol extract and dopamine significantly ( p < 0.05) reduced acetylcholinesterase enzyme (AChE) and malondialdehyde (MDA) activities in a dose-dependent manner and significantly ( p < 0.05) increased superoxide dismutase activity (SOD) dose dependently, respectively. In the histopathological analysis of the hippocampal area, there were mild vacuolation (V), mild degeneration as well as mild granular cell atrophy in the treated groups, suggesting that M sapientum may have neuroprotective properties. Conclusion: Ethanol extract of ripe M sapientum peels enhanced cognitive functions and may be beneficial in preventing neurodegenerative disorders via antioxidant mechanism.
{"title":"Ripe Musa sapientum Peels Exhibit Neuroprotection Against Lead Acetate-Induced Brain Damage in Wistar Rats","authors":"Uduak Anthony Inwang, Ezekiel Etim Ben, Obinna Onwe Uchewa, Ekementeabasi Aniebo Umoh, Azubuike Raphael Nwaji","doi":"10.1177/1934578x241265192","DOIUrl":"https://doi.org/10.1177/1934578x241265192","url":null,"abstract":"Objective: Human health has continued to be at risk from lead exposure. This study explored the antioxidative potential of ethanol extract of ripe Musa sapientum peels to protect against lead acetate-induced neuronal insult in female wistar rats. Methods: Thirty adult female rats (120-160 g) were randomly divided into six groups (n = 5): Group 1 (control group) received 10 mL/kg of distilled water; Group 2 received 100 mg/kg lead acetate. Group 3 received 2.5 mg/kg of donepezil. Groups 4 to 6 received 100, 200, and 400 mg/kg ethanol extract of ripe M sapientum, respectively, via oral gavage. Groups 2 to 5 were co-treated with 100 mg/kg lead acetate for 21 days. Neurobehavioral parameter, biochemical and histological analyses of the hippocampus were determined. Recognition memory was evaluated using Novel Object Recognition Test. Results: There was a significant ( p < 0.05) increase in total exploration, discrimination index, and percentage alternation in the ethanol extract M sapientum-treated groups compared with the lead acetate-induced group. M sapientum ethanol extract and dopamine significantly ( p < 0.05) reduced acetylcholinesterase enzyme (AChE) and malondialdehyde (MDA) activities in a dose-dependent manner and significantly ( p < 0.05) increased superoxide dismutase activity (SOD) dose dependently, respectively. In the histopathological analysis of the hippocampal area, there were mild vacuolation (V), mild degeneration as well as mild granular cell atrophy in the treated groups, suggesting that M sapientum may have neuroprotective properties. Conclusion: Ethanol extract of ripe M sapientum peels enhanced cognitive functions and may be beneficial in preventing neurodegenerative disorders via antioxidant mechanism.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"31 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141778609","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-23DOI: 10.1177/1934578x241264995
Veronica James Enyiekere, Edet Effiong Asanga, Jude Efiom Okokon, Chinedum Martins Ekeleme, Martin Osita Anagboso, Ise Peter Uduak
BackgroundJusticia insularis (Acanthaceae) T. Anderson is ethnopharmacologically used in Nigeria for the treatment of diseases including malaria. Therefore, this study was designed to investigate in vivo antiplasmodial effect of J. insularis leaf in Plasmodium berghei-infected mice, characterize its constituents, and carryout in silico studies of its compounds.MethodsStandard protocols were followed in the processing of the plant leaves, extraction, fractionation, isolation, and characterization, evaluation of in vivo antiplasmodial assay, retrieval of Plasmodium falciparum serine hydroxymethyl transferase (PfSHMT) and Plasmodium falciparum erythrocyte membrane protein 1 (PfEMP-1) proteins, absorption, distribution, metabolism, excretion, and toxicity (ADMET), and docking studies. Gas chromatography-mass spectrometry (GC-MS) was employed to isolate and characterize the compounds; SWISSADME and ADMET lab 2 enhanced the evaluation of pharmacokinetic properties, PyRx for docking analysis; Biovia discovery studio for 2D visualization, and PyMol software for 3D visualization of the ligand-protein interactions.ResultsThe dichloromethane (61.59%) and ethyl acetate (73.15%) fractions had the best therapeutic indices and compared favorably with chloroquine (81.58%) in the curative antiplasmodial assay. The GC-MS analysis revealed 20 already reported antiplasmodial compounds with hexanoic acid 1,1-dimethylethyl ester, octadecanoic acid docosyl ester, and trans-β-ocimene as the lead compounds based on their binding affinities, permeation of the blood-brain-barrier, non-inhibition of metabolizing enzymes, ease of excretion, non-carcinogenicity, as well as non-violation of Lipinski's criteria.ConclusionOctadecanoic acid docosyl ester and hexanoic acid 1,1-dimethylethyl ester bonded the tetrahydrofolate-binding sites of PfSHMT, caused inhibition of DNA synthesis, and apoptosis, whereas trans-β-ocimene inhibited PfEMP-1, reversed the attachment of parasitized red blood cells to micro-vascular endothelium as their mechanism of action for parasitemia clearance. Moreover, these lead compounds reported for the first time in the dichloromethane and EtoAc fractions of this plant are responsible for the remarkable antiplasmodial activity observed in this study.
背景Justicia insularis (Acanthaceae) T. Anderson 在尼日利亚被用于治疗包括疟疾在内的各种疾病。因此，本研究旨在调查 J. insularis 叶片对受伯格希氏疟原虫感染的小鼠的体内抗疟效果，确定其成分的特征，并对其化合物进行硅学研究。方法在植物叶片的加工、提取、分馏、分离和表征、体内抗疟试验评估、恶性疟原虫丝氨酸羟甲基转移酶（PfSHMT）和恶性疟原虫红细胞膜蛋白 1（PfEMP-1）蛋白的回收、吸收、分布、代谢、排泄和毒性（ADMET）以及对接研究等方面均遵循了标准方案。气相色谱-质谱联用仪（GC-MS）用于分离和表征化合物；SWISSADME 和 ADMET 实验室 2 增强了药代动力学特性的评估；PyRx 用于对接分析；Biovia discovery studio 用于二维可视化；PyMol 软件用于配体与蛋白质相互作用的三维可视化。结果二氯甲烷（61.59%）和乙酸乙酯（73.15%）馏分的治疗指数最高，在抗疟治疗试验中与氯喹（81.58%）相比效果更好。气相色谱-质谱分析发现了 20 种已报道的抗疟化合物，其中以己酸 1,1 二甲基乙酯、十八酸二十二烷基酯和反式-β-ocimene 为首要化合物，其依据是这些化合物的结合亲和力、血脑屏障渗透性、不抑制代谢酶、易于排泄、无致癌性以及不违反利平斯基标准。结论十八酸二十二烷基酯和十六酸 1,1-二甲基乙酯结合了 PfSHMT 的四氢叶酸结合位点，抑制了 DNA 合成并导致细胞凋亡，而反式-β-ocimene 则抑制了 PfEMP-1，逆转了寄生红细胞与微血管内皮的附着，这是它们清除寄生虫血症的作用机制。此外，在该植物的二氯甲烷和 EtoAc 馏分中首次发现的这些先导化合物是本研究中观察到的显著抗疟活性的原因。
{"title":"Fatty Acid Esters and Acyclic Monoterpenoid from Justicia insularis Leaf Fractions Attenuated Malaria Pathogenesis Through Docking with Plasmodium falciparum Serine Hydroxymethyl Transferase and Plasmodium falciparum Erythrocyte Membrane Protein 1 Proteins","authors":"Veronica James Enyiekere, Edet Effiong Asanga, Jude Efiom Okokon, Chinedum Martins Ekeleme, Martin Osita Anagboso, Ise Peter Uduak","doi":"10.1177/1934578x241264995","DOIUrl":"https://doi.org/10.1177/1934578x241264995","url":null,"abstract":"BackgroundJusticia insularis (Acanthaceae) T. Anderson is ethnopharmacologically used in Nigeria for the treatment of diseases including malaria. Therefore, this study was designed to investigate in vivo antiplasmodial effect of J. insularis leaf in Plasmodium berghei-infected mice, characterize its constituents, and carryout in silico studies of its compounds.MethodsStandard protocols were followed in the processing of the plant leaves, extraction, fractionation, isolation, and characterization, evaluation of in vivo antiplasmodial assay, retrieval of Plasmodium falciparum serine hydroxymethyl transferase (PfSHMT) and Plasmodium falciparum erythrocyte membrane protein 1 (PfEMP-1) proteins, absorption, distribution, metabolism, excretion, and toxicity (ADMET), and docking studies. Gas chromatography-mass spectrometry (GC-MS) was employed to isolate and characterize the compounds; SWISSADME and ADMET lab 2 enhanced the evaluation of pharmacokinetic properties, PyRx for docking analysis; Biovia discovery studio for 2D visualization, and PyMol software for 3D visualization of the ligand-protein interactions.ResultsThe dichloromethane (61.59%) and ethyl acetate (73.15%) fractions had the best therapeutic indices and compared favorably with chloroquine (81.58%) in the curative antiplasmodial assay. The GC-MS analysis revealed 20 already reported antiplasmodial compounds with hexanoic acid 1,1-dimethylethyl ester, octadecanoic acid docosyl ester, and trans-β-ocimene as the lead compounds based on their binding affinities, permeation of the blood-brain-barrier, non-inhibition of metabolizing enzymes, ease of excretion, non-carcinogenicity, as well as non-violation of Lipinski's criteria.ConclusionOctadecanoic acid docosyl ester and hexanoic acid 1,1-dimethylethyl ester bonded the tetrahydrofolate-binding sites of PfSHMT, caused inhibition of DNA synthesis, and apoptosis, whereas trans-β-ocimene inhibited PfEMP-1, reversed the attachment of parasitized red blood cells to micro-vascular endothelium as their mechanism of action for parasitemia clearance. Moreover, these lead compounds reported for the first time in the dichloromethane and EtoAc fractions of this plant are responsible for the remarkable antiplasmodial activity observed in this study.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"412 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141778608","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-23DOI: 10.1177/1934578x241257828
Yadong Xing, Min Wu, Shijie Zhong, Hui Zhang, Aiping Zheng
Background: Compound Scutellariae Radix Granules (CSRG) are used to treat gastrointestinal diseases, including colorectal cancer (CRC), which is the second leading cause of cancer-related deaths. Studies have demonstrated that CSRG have anti-CRC effects; however, the exact molecular mechanisms remain unclear. Methods: This study used network pharmacology and molecular docking to identify the active ingredients in CSRG and assess CRC-related genes and pathways. After that, the effect of CSRG on HT29 cells was observed in vitro. Cell Counting Kit-8 detection, Western blot, and flow cytometry with AnnexinV-FITC/PI double staining experiments were used to observe the effects of CSRG on the proliferation, apoptosis and other effects of HT-29 cells. Moreover, the effects of CSRG and IGF-I (PI3K/AKT agonist) on HT-29 cell biological behaviors were gauged. Results: Naringenin, quercetin, licochalcone A, acacetin, wogonin, baicalein, kaempferol, and isorhamnetin were the key active ingredients in CSRG, which affect CRC through five genes: mitogen-activated protein kinase 3 and 1, tumor protein 53, signal transducer and activator of transcription 3, and RELA proto-oncogene, NF-kB subunit. The molecular docking experiments predicted the activity of the active ingredients in CSRG against their intended target, each of which could stably bind the corresponding CRC target. The enrichment analysis indicate that CSRG played a synergistic effect in regulating the process of apoptosis and cell proliferation, and that multiple pathways were participated in CSRG-related CRC treatment. Cell experiments results demonstrated that the PI3k–Akt pathway may be critical pathways. Besides, Tp53 was found tightly linked to apoptosis. Moreover, the suppressive effect of CSRG on HT29 cell malignant phenotypes was reversed by IGF-I. Conclusion: CSRG are an anti-colon cancer herb containing multiple components, involving multiple target genes and signaling pathways. CSRG inhibited colon cancer cell proliferation and induced apoptosis, which may be related to its inhibition of the PI3K/Akt pathway and activation of the Tp53 pathway.
{"title":"Pharmacodynamic Materials and Mechanisms of Compound Scutellariae Radix Granules for Colorectal Cancer: A Network Pharmacology, Molecular Docking and Cell Experiments Study","authors":"Yadong Xing, Min Wu, Shijie Zhong, Hui Zhang, Aiping Zheng","doi":"10.1177/1934578x241257828","DOIUrl":"https://doi.org/10.1177/1934578x241257828","url":null,"abstract":"Background: Compound Scutellariae Radix Granules (CSRG) are used to treat gastrointestinal diseases, including colorectal cancer (CRC), which is the second leading cause of cancer-related deaths. Studies have demonstrated that CSRG have anti-CRC effects; however, the exact molecular mechanisms remain unclear. Methods: This study used network pharmacology and molecular docking to identify the active ingredients in CSRG and assess CRC-related genes and pathways. After that, the effect of CSRG on HT29 cells was observed in vitro. Cell Counting Kit-8 detection, Western blot, and flow cytometry with AnnexinV-FITC/PI double staining experiments were used to observe the effects of CSRG on the proliferation, apoptosis and other effects of HT-29 cells. Moreover, the effects of CSRG and IGF-I (PI3K/AKT agonist) on HT-29 cell biological behaviors were gauged. Results: Naringenin, quercetin, licochalcone A, acacetin, wogonin, baicalein, kaempferol, and isorhamnetin were the key active ingredients in CSRG, which affect CRC through five genes: mitogen-activated protein kinase 3 and 1, tumor protein 53, signal transducer and activator of transcription 3, and RELA proto-oncogene, NF-kB subunit. The molecular docking experiments predicted the activity of the active ingredients in CSRG against their intended target, each of which could stably bind the corresponding CRC target. The enrichment analysis indicate that CSRG played a synergistic effect in regulating the process of apoptosis and cell proliferation, and that multiple pathways were participated in CSRG-related CRC treatment. Cell experiments results demonstrated that the PI3k–Akt pathway may be critical pathways. Besides, Tp53 was found tightly linked to apoptosis. Moreover, the suppressive effect of CSRG on HT29 cell malignant phenotypes was reversed by IGF-I. Conclusion: CSRG are an anti-colon cancer herb containing multiple components, involving multiple target genes and signaling pathways. CSRG inhibited colon cancer cell proliferation and induced apoptosis, which may be related to its inhibition of the PI3K/Akt pathway and activation of the Tp53 pathway.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"9 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141778612","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-23DOI: 10.1177/1934578x241264632
Taowen Ye, Yumin Ma, Jin Dong, Yanli Dong, Jie Hui, Chengniu Wang, Yang Liu, Xiaorong Wang
ObjectiveHydroxytyrosol (HT), a polyphenolic component identified in olive oil and leaves, represents one of the most extensively investigated natural phenol due to its diverse beneficial biological properties. Recent studies have shown that HT exhibits protective effects on reproductive function and can improve sperm quality. However, the precise effect and underlying mechanism of HT on oligozoospermia remain unclear. This study aims to investigate the effect and mechanism of HT across varying concentrations on oligozoospermia.MethodsOligozoospermia was induced in ICR male mice via intraperitoneal injection of busulfan (BUS, 30 mg/kg). The mice were randomly categorized into five groups as Normal, BUS, HT 10 mg/kg, HT 30 mg/kg and HT 50 mg/kg. The efficacy of HT on oligozoospermia was assessed through sperm concentration and motility using a computer-assisted sperm analysis system. Testicular and epididymal histology was examined via hematoxylin-eosin staining, while cytoskeletal integrity was evaluated by immunofluorescence. Hormone levels, along with reactive oxygen species (ROS) and malondialdehyde (MDA) were examined by ELISA kits. Differentially expressed genes were identified through RNA sequencing, and the expression levels of key genes were validated by qPCR.ResultsThe results indicated that HT (50 mg/kg) significantly increased sperm concentration, promoted morphological recovery of testicular tissue, heightened the levels of serum testosterone, follicle-stimulating hormone, luteinizing hormone, as well as decreased the accumulation of ROS and MDA in mice with oligozoospermia. RNA sequencing analysis and RT-qPCR results revealed that HT could restore spermatogenesis and ameliorate oligozoospermia by up-regulating genes related to cilium organization, microtubule-based movement, and spermatid differentiation and development.ConclusionsHT demonstrates therapeutic efficacy against busulfan-induced oligozoospermia. The mechanism of HT on oligozoospermia may be related to its influence on cilium and microtubule-based movement, along with the differentiation and development of spermatids. HT shows potential as a prospective therapeutic intervention for the treatment of oligozoospermia.
{"title":"Hydroxytyrosol Ameliorates Busulfan-Induced Oligozoospermia in a Mouse Model","authors":"Taowen Ye, Yumin Ma, Jin Dong, Yanli Dong, Jie Hui, Chengniu Wang, Yang Liu, Xiaorong Wang","doi":"10.1177/1934578x241264632","DOIUrl":"https://doi.org/10.1177/1934578x241264632","url":null,"abstract":"ObjectiveHydroxytyrosol (HT), a polyphenolic component identified in olive oil and leaves, represents one of the most extensively investigated natural phenol due to its diverse beneficial biological properties. Recent studies have shown that HT exhibits protective effects on reproductive function and can improve sperm quality. However, the precise effect and underlying mechanism of HT on oligozoospermia remain unclear. This study aims to investigate the effect and mechanism of HT across varying concentrations on oligozoospermia.MethodsOligozoospermia was induced in ICR male mice via intraperitoneal injection of busulfan (BUS, 30 mg/kg). The mice were randomly categorized into five groups as Normal, BUS, HT 10 mg/kg, HT 30 mg/kg and HT 50 mg/kg. The efficacy of HT on oligozoospermia was assessed through sperm concentration and motility using a computer-assisted sperm analysis system. Testicular and epididymal histology was examined via hematoxylin-eosin staining, while cytoskeletal integrity was evaluated by immunofluorescence. Hormone levels, along with reactive oxygen species (ROS) and malondialdehyde (MDA) were examined by ELISA kits. Differentially expressed genes were identified through RNA sequencing, and the expression levels of key genes were validated by qPCR.ResultsThe results indicated that HT (50 mg/kg) significantly increased sperm concentration, promoted morphological recovery of testicular tissue, heightened the levels of serum testosterone, follicle-stimulating hormone, luteinizing hormone, as well as decreased the accumulation of ROS and MDA in mice with oligozoospermia. RNA sequencing analysis and RT-qPCR results revealed that HT could restore spermatogenesis and ameliorate oligozoospermia by up-regulating genes related to cilium organization, microtubule-based movement, and spermatid differentiation and development.ConclusionsHT demonstrates therapeutic efficacy against busulfan-induced oligozoospermia. The mechanism of HT on oligozoospermia may be related to its influence on cilium and microtubule-based movement, along with the differentiation and development of spermatids. HT shows potential as a prospective therapeutic intervention for the treatment of oligozoospermia.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"42 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141778607","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-29DOI: 10.1177/1934578x241257080
Akanji A. Murtala, Abidemi J. Akindele, Ibrahim A. Oreagba
ObjectivesTo investigate the safety profile of subchronic oral administration of hydroethanol leaf extract of Newbouldia laevis (NL) in rats.MethodsNL was administered orally (20, 100, and 500 mg/kg) to groups of rats for 90 days. Distilled water served as control. Some rats were spared for an extra 30 days with no extract administration (reversibility study). Blood, urine and selected vital organs were collected for analyses.ResultsIn male rats, NL (20, 500 mg/kg) irreversibly increased ( P˂.05) bodyweight and feeding pattern with opposite trend of results in females. NL (20 mg/kg) elicited irreversible decrease ( P˂0.05) in RBC in male rats; a reversible decrease in RBC and Hb, and an irreversible increase (500 mg/kg) in WBC and neutrophils in females. In male rats, NL irreversibly decreased ( P˂.01) HDL-c and increased uric acid; in female rats, it elicited a reversible increase ( P˂.05, 500 mg/kg) in AST. NL (500 mg/kg) irreversibly decreased ( P˂.05) sperm motility and count, and produced an irreversible increase ( P˂.01) in testosterone levels in male rats (100 mg/kg). It reversibly decreased (20-500 mg/kg) luteinizing hormone levels (both sexes).ConclusionsNL is fairly safe at lower doses. However, it could cause anemia at lower doses, infertility (both sexes), liver and kidney injuries at high doses.
{"title":"Ninety-Day Toxicological Assessment of Preparation of the Medicinal Plant Newbouldia laevis (P. Beauv.) Seem. (Bignoniaceae) in Rats","authors":"Akanji A. Murtala, Abidemi J. Akindele, Ibrahim A. Oreagba","doi":"10.1177/1934578x241257080","DOIUrl":"https://doi.org/10.1177/1934578x241257080","url":null,"abstract":"ObjectivesTo investigate the safety profile of subchronic oral administration of hydroethanol leaf extract of Newbouldia laevis (NL) in rats.MethodsNL was administered orally (20, 100, and 500 mg/kg) to groups of rats for 90 days. Distilled water served as control. Some rats were spared for an extra 30 days with no extract administration (reversibility study). Blood, urine and selected vital organs were collected for analyses.ResultsIn male rats, NL (20, 500 mg/kg) irreversibly increased ( P˂.05) bodyweight and feeding pattern with opposite trend of results in females. NL (20 mg/kg) elicited irreversible decrease ( P˂0.05) in RBC in male rats; a reversible decrease in RBC and Hb, and an irreversible increase (500 mg/kg) in WBC and neutrophils in females. In male rats, NL irreversibly decreased ( P˂.01) HDL-c and increased uric acid; in female rats, it elicited a reversible increase ( P˂.05, 500 mg/kg) in AST. NL (500 mg/kg) irreversibly decreased ( P˂.05) sperm motility and count, and produced an irreversible increase ( P˂.01) in testosterone levels in male rats (100 mg/kg). It reversibly decreased (20-500 mg/kg) luteinizing hormone levels (both sexes).ConclusionsNL is fairly safe at lower doses. However, it could cause anemia at lower doses, infertility (both sexes), liver and kidney injuries at high doses.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"25 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141195590","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-29DOI: 10.1177/1934578x241258568
Leonel Tarcisio da Cristina Bungala, Bao Van Nguyen, Chanung Park, Ramaraj Sathasivam, Gwonjeong Bok, Jong Seok Park, Sang Un Park
Objective: Brassica rapa is an important source of phytochemicals essential for plant defense and human health. To better understand their metabolic characteristics, this study aimed to investigate the glucosinolates and phenolic content from sprouts of 7 B. rapa subspecies. Methods: Glucosinolates and phenolic compounds were extracted using previously reported procedures, with slight modifications. Glucosinolates were identified based on their high-performance liquid chromatography peak area ratios and quantified based on the peak areas, retention time, and response factor and phenolic compounds were identified based on retention times and spiking tests and quantified concerning a corresponding calibration curve. Results: Statistical analysis showed that Choy sum (31.82 ± 2.3 mg/g DW) and Bok choy (31.73 ± 1.49 mg/g DW) presented the highest total glucosinolates content, and the lowest content was observed in Turnip rape (21.75 ± 1.67 mg/g DW). Between the contents of individual glucosinolates, progoitrin presented the highest content in Bok choy (17.84 ± 1.24 mg/g DW). The highest concentration of total phenolic compounds was found in the sprouts of Chinese cabbage (2.7 ± 0.05 mg/g DW), whereas the lowest concentration was found in Choy sum sprouts (2.17 ± 0.05 mg/g DW). The highest individual phenolic content was observed for benzoic acid (0.96 ± 0.03 mg/g DW) and rutin (0.85 ± 0.03 mg/g DW), which were highest in mizuna and Chinese cabbage, respectively. Conclusion: Subspecies may influence the levels of glucosinolates and polyphenols in vegetables. The results of our study showed the distinctive metabolic signatures embedded in the 7 B. rapa subspecies.
{"title":"Analysis of Glucosinolates and Phenolic Content in Sprouts of 7 Brassica rapa Subspecies","authors":"Leonel Tarcisio da Cristina Bungala, Bao Van Nguyen, Chanung Park, Ramaraj Sathasivam, Gwonjeong Bok, Jong Seok Park, Sang Un Park","doi":"10.1177/1934578x241258568","DOIUrl":"https://doi.org/10.1177/1934578x241258568","url":null,"abstract":"Objective: Brassica rapa is an important source of phytochemicals essential for plant defense and human health. To better understand their metabolic characteristics, this study aimed to investigate the glucosinolates and phenolic content from sprouts of 7 B. rapa subspecies. Methods: Glucosinolates and phenolic compounds were extracted using previously reported procedures, with slight modifications. Glucosinolates were identified based on their high-performance liquid chromatography peak area ratios and quantified based on the peak areas, retention time, and response factor and phenolic compounds were identified based on retention times and spiking tests and quantified concerning a corresponding calibration curve. Results: Statistical analysis showed that Choy sum (31.82 ± 2.3 mg/g DW) and Bok choy (31.73 ± 1.49 mg/g DW) presented the highest total glucosinolates content, and the lowest content was observed in Turnip rape (21.75 ± 1.67 mg/g DW). Between the contents of individual glucosinolates, progoitrin presented the highest content in Bok choy (17.84 ± 1.24 mg/g DW). The highest concentration of total phenolic compounds was found in the sprouts of Chinese cabbage (2.7 ± 0.05 mg/g DW), whereas the lowest concentration was found in Choy sum sprouts (2.17 ± 0.05 mg/g DW). The highest individual phenolic content was observed for benzoic acid (0.96 ± 0.03 mg/g DW) and rutin (0.85 ± 0.03 mg/g DW), which were highest in mizuna and Chinese cabbage, respectively. Conclusion: Subspecies may influence the levels of glucosinolates and polyphenols in vegetables. The results of our study showed the distinctive metabolic signatures embedded in the 7 B. rapa subspecies.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"31 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141195595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-29DOI: 10.1177/1934578x241257127
Syeda Nishat Fathima, Sayed Mohammed Firdous, Sourav Pal, Hesham S. Ghazzawy, Mostafa M. Gouda
ObjectivesThe objective of this research was to investigate the potential anti-inflammatory properties of the Cucurbita pepo fruit. Given the adverse effects associated with long-term use or excessive doses of conventional anti-inflammatory medications, exploring herbal therapies as alternatives has become increasingly important.MethodsVarious preliminary tests and antioxidant assays, both enzymatic and non-enzymatic, were conducted on the C . pepo fruit. Bioactive substances present in the fruit, including alkaloids, carbohydrates, flavonoids, tannins, amino acids, triterpenoids, and saponin glycosides, were identified through early analysis. Different extraction solvents, such as chloroform, methanol, and water, were utilized to extract samples. The methanolic extract was subjected to further testing for its in vitro anti-inflammatory characteristics. This involved evaluating their ability to stabilize RBC membranes, inhibit protein denaturation, and suppress proteinase activity using two concentrations (150 µg/ml and 300 µg/ml) of the extract.ResultsThe methanolic extract of the C. pepo fruit exhibited strong free radical scavenging activity in both DPPH and H2O2 assays. Moreover, it demonstrated the dose-dependent stabilization of RBC membranes, resulting in reduced hemolysis, protein denaturation, and proteinase activity. These findings suggest potent anti-inflammatory effects of the methanolic extract.ConclusionThis research study has found that the C. pepo fruit methanolic extract significantly reduced inflammation. This demonstrates the promise of natural chemicals as less risky substitutes for traditional anti-inflammatory medications. Potentially safe and efficient treatments for inflammatory illnesses could be found in herbal remedies such as the C. pepo fruit. Therefore, this study highlights the significance of exploring herbal remedies as a potential treatment option for inflammation-related diseases.
{"title":"Assessment of In Vitro Antioxidant and Anti-Inflammatory Activities of Pumpkin (Cucurbita pepo) Natural Plant","authors":"Syeda Nishat Fathima, Sayed Mohammed Firdous, Sourav Pal, Hesham S. Ghazzawy, Mostafa M. Gouda","doi":"10.1177/1934578x241257127","DOIUrl":"https://doi.org/10.1177/1934578x241257127","url":null,"abstract":"ObjectivesThe objective of this research was to investigate the potential anti-inflammatory properties of the Cucurbita pepo fruit. Given the adverse effects associated with long-term use or excessive doses of conventional anti-inflammatory medications, exploring herbal therapies as alternatives has become increasingly important.MethodsVarious preliminary tests and antioxidant assays, both enzymatic and non-enzymatic, were conducted on the C . pepo fruit. Bioactive substances present in the fruit, including alkaloids, carbohydrates, flavonoids, tannins, amino acids, triterpenoids, and saponin glycosides, were identified through early analysis. Different extraction solvents, such as chloroform, methanol, and water, were utilized to extract samples. The methanolic extract was subjected to further testing for its in vitro anti-inflammatory characteristics. This involved evaluating their ability to stabilize RBC membranes, inhibit protein denaturation, and suppress proteinase activity using two concentrations (150 µg/ml and 300 µg/ml) of the extract.ResultsThe methanolic extract of the C. pepo fruit exhibited strong free radical scavenging activity in both DPPH and H<jats:sub>2</jats:sub>O<jats:sub>2</jats:sub> assays. Moreover, it demonstrated the dose-dependent stabilization of RBC membranes, resulting in reduced hemolysis, protein denaturation, and proteinase activity. These findings suggest potent anti-inflammatory effects of the methanolic extract.ConclusionThis research study has found that the C. pepo fruit methanolic extract significantly reduced inflammation. This demonstrates the promise of natural chemicals as less risky substitutes for traditional anti-inflammatory medications. Potentially safe and efficient treatments for inflammatory illnesses could be found in herbal remedies such as the C. pepo fruit. Therefore, this study highlights the significance of exploring herbal remedies as a potential treatment option for inflammation-related diseases.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"120 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141198291","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-27DOI: 10.1177/1934578x241257377
Md. Abdus Samadd, Md. Rifaet Hossain, Mohammad Abdullah Taher, Mohammad Mahmudul Hasan, Shariful Haque, Mashruf Islam Rafid, Md. Solaiman Hossain, Md. Ashraful Islam, Mala Khan
Objective: This study aimed to comprehensively evaluate the chemico-pharmacological properties of methanolic extractives derived from Cyanometra ramiflora leaves, encompassing a spectrum of activities including cytotoxic, thrombolytic, membrane-stabilizing, antioxidant, antidiarrheal, hypoglycemic, and analgesic effects. Methods: Phytomolecules were identified using Gas Chromatography-Mass Spectrometry (GC-MS), while antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and total phenolic content tests. Cytotoxicity was determined through the brine shrimp bioassay, while thrombolytic activity was evaluated via clot lysis assays, and membrane-stabilizing effects were investigated for potential anti-inflammatory properties. In-vivo experiments using mice were conducted solely with the methanolic extract to assess central and peripheral analgesic, hypoglycemic, and antidiarrheal properties. Results: The presence of 47 compounds in the methanolic extract, with tetratriacontyl pentafluoropropionate (9.25%), pentatriacontane (8.75%), and 2-methylhexacosane (5.9%) being predominant. The dichloromethane-soluble fraction exhibited the highest cytotoxicity, with a 50% lethal concentration (LC50) of 11.05 µg/mL. Both petroleum-ether and methanol-soluble fractions demonstrated more than 50% lysis in thrombolytic activity assays. Under hypotonic and heat-induced conditions, the ethyl acetate and dichloromethane-soluble fractions of C. ramiflora significantly reduced erythrocyte hemolysis. Notably, the methanol-soluble fraction exhibited significant antioxidant potential with 50% inhibitory concentration (IC50) of 17.71 μg/mL compared to the standard EDTA (IC50 = 75.94 μg/mL). The hypoglycemic investigation revealed a 63.73% reduction at 90 min with a 600 mg/kg dose, while mild antidiarrheal activity was observed with a 37.5% reduction in diarrhea at 4 h intervals. Significant analgesic effects were demonstrated in both central and peripheral tests, with a 68.53% reduction in writhing during the peripheral test and an average tail immersion time of 5.38 s at 90 min. Conclusion: C. ramiflora leaves show promise as natural sources for various pharmacological activities, including cytotoxicity, thrombosis, inflammation, antioxidant, hypoglycemic, and analgesic effects. However, further comprehensive research is recommended to elucidate the precise mechanisms of action and analyze the phytochemical composition of C. ramiflora plants.
{"title":"Multifaceted Chemico-Pharmacological Insights into Cynometra ramiflora L.: Unveiling its GC-MS, Cytotoxic, Thrombolytic, Anti-Inflammatory, Antioxidant, Anti-Diarrheal, Hypoglycemic, and Analgesic Potentials","authors":"Md. Abdus Samadd, Md. Rifaet Hossain, Mohammad Abdullah Taher, Mohammad Mahmudul Hasan, Shariful Haque, Mashruf Islam Rafid, Md. Solaiman Hossain, Md. Ashraful Islam, Mala Khan","doi":"10.1177/1934578x241257377","DOIUrl":"https://doi.org/10.1177/1934578x241257377","url":null,"abstract":"Objective: This study aimed to comprehensively evaluate the chemico-pharmacological properties of methanolic extractives derived from Cyanometra ramiflora leaves, encompassing a spectrum of activities including cytotoxic, thrombolytic, membrane-stabilizing, antioxidant, antidiarrheal, hypoglycemic, and analgesic effects. Methods: Phytomolecules were identified using Gas Chromatography-Mass Spectrometry (GC-MS), while antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and total phenolic content tests. Cytotoxicity was determined through the brine shrimp bioassay, while thrombolytic activity was evaluated via clot lysis assays, and membrane-stabilizing effects were investigated for potential anti-inflammatory properties. In-vivo experiments using mice were conducted solely with the methanolic extract to assess central and peripheral analgesic, hypoglycemic, and antidiarrheal properties. Results: The presence of 47 compounds in the methanolic extract, with tetratriacontyl pentafluoropropionate (9.25%), pentatriacontane (8.75%), and 2-methylhexacosane (5.9%) being predominant. The dichloromethane-soluble fraction exhibited the highest cytotoxicity, with a 50% lethal concentration (LC<jats:sub>50</jats:sub>) of 11.05 µg/mL. Both petroleum-ether and methanol-soluble fractions demonstrated more than 50% lysis in thrombolytic activity assays. Under hypotonic and heat-induced conditions, the ethyl acetate and dichloromethane-soluble fractions of C. ramiflora significantly reduced erythrocyte hemolysis. Notably, the methanol-soluble fraction exhibited significant antioxidant potential with 50% inhibitory concentration (IC<jats:sub>50</jats:sub>) of 17.71 μg/mL compared to the standard EDTA (IC<jats:sub>50 </jats:sub>= 75.94 μg/mL). The hypoglycemic investigation revealed a 63.73% reduction at 90 min with a 600 mg/kg dose, while mild antidiarrheal activity was observed with a 37.5% reduction in diarrhea at 4 h intervals. Significant analgesic effects were demonstrated in both central and peripheral tests, with a 68.53% reduction in writhing during the peripheral test and an average tail immersion time of 5.38 s at 90 min. Conclusion: C. ramiflora leaves show promise as natural sources for various pharmacological activities, including cytotoxicity, thrombosis, inflammation, antioxidant, hypoglycemic, and analgesic effects. However, further comprehensive research is recommended to elucidate the precise mechanisms of action and analyze the phytochemical composition of C. ramiflora plants.","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"6 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141168378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-25DOI: 10.1177/1934578x241252727
Raja Shekhar Nunavath, Krishnaveni Nagappan
{"title":"Identification of Synthetic Impurities and Their Significance in Natural Products Quality Control","authors":"Raja Shekhar Nunavath, Krishnaveni Nagappan","doi":"10.1177/1934578x241252727","DOIUrl":"https://doi.org/10.1177/1934578x241252727","url":null,"abstract":"","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"89 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-05-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141148103","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-25DOI: 10.1177/1934578x241255508
Edet Effiong Asanga, Akaninyene Joseph, EkementeAbasi Aniebo Umoh, Chinedum Martins Ekeleme, Henshaw Uchechi Okoroiwu, Uwem Okon Edet, Nikita Elkanah Umoafia, Olorunfemi Abraham Eseyin, Ani Nkang, Jude Efiom Okokon, Samuel Essang, Glory Chimzi, Daniel Nkereuwem Okpo, Patrick Bassey Ephraim, Vivian Augustine Otogwu
BackgroundInflammations, oxidative stress, and pains underlie the pathogenesis of non-communicable diseases (NCDs) like respiratory disorders and cancer; however, they are scientifically treated with Curcuma longa. Therefore, the pharmacological screening (antioxidant, anti-inflammatory, and analgesic) of the plant's rhizome, isolation and characterization of its compounds, as well as their in silico profiling with cyclooxygenases, phosphodiesterase, superoxide dismutase, glutathione peroxidase, and catalase could yield lead compounds with better benefit-to-risk ratio against oxidative stress and inflammation.MethodsThe collection of the plant's rhizomes , extract preparation, anti-inflammatory, analgesic, and antioxidant studies, retrieval of target proteins, GC-MS, ADME, and docking analyses were done using standard protocols.ResultsCurcuma longa's percentage edema inhibition and analgesic potentials were better than aspirin in both acute and sub-acute inflammations as well as chemical and thermal-induced pains; moreover, its antioxidant activities were better than vitamin C. Moreover, twenty compounds with anti-inflammatory, analgesic, and antioxidant activities were unraveled from the GC-MS analysis. Ar-tumerone, curcumin, γ-sitosterol, α-tocopherol, isocurcumenol, adamantane, and curdione were the lead compounds based on their binding affinities (for PDE-4B, COX-1, COX-2, SOD, CAT, GPx), lower molecular weights, non-permeation of blood brain barrier, bioavailability profiles, non-inhibition of metabolizing enzymes, faster renal clearance, and non-violation of Lipinski's rules.ConclusionAdamantane, α-tocopherol, and γ-sitosterol reported for the first time in the plant's rhizome could mitigate oxidative stress and inflammation as mediators of apoptosis, cytotoxic impaired autophagy, DNA damages, and mitochondrial dysfunction that contributes to the progression of non-communicable diseases (NCDs).
{"title":"New Perspectives on the Therapeutic Potentials of Bioactive Compounds from Curcuma longa: Targeting COX-1 & 2, PDE-4B, and Antioxidant Enzymes to Counteract Oxidative Stress and Inflammation","authors":"Edet Effiong Asanga, Akaninyene Joseph, EkementeAbasi Aniebo Umoh, Chinedum Martins Ekeleme, Henshaw Uchechi Okoroiwu, Uwem Okon Edet, Nikita Elkanah Umoafia, Olorunfemi Abraham Eseyin, Ani Nkang, Jude Efiom Okokon, Samuel Essang, Glory Chimzi, Daniel Nkereuwem Okpo, Patrick Bassey Ephraim, Vivian Augustine Otogwu","doi":"10.1177/1934578x241255508","DOIUrl":"https://doi.org/10.1177/1934578x241255508","url":null,"abstract":"BackgroundInflammations, oxidative stress, and pains underlie the pathogenesis of non-communicable diseases (NCDs) like respiratory disorders and cancer; however, they are scientifically treated with Curcuma longa. Therefore, the pharmacological screening (antioxidant, anti-inflammatory, and analgesic) of the plant's rhizome, isolation and characterization of its compounds, as well as their in silico profiling with cyclooxygenases, phosphodiesterase, superoxide dismutase, glutathione peroxidase, and catalase could yield lead compounds with better benefit-to-risk ratio against oxidative stress and inflammation.MethodsThe collection of the plant's rhizomes , extract preparation, anti-inflammatory, analgesic, and antioxidant studies, retrieval of target proteins, GC-MS, ADME, and docking analyses were done using standard protocols.ResultsCurcuma longa's percentage edema inhibition and analgesic potentials were better than aspirin in both acute and sub-acute inflammations as well as chemical and thermal-induced pains; moreover, its antioxidant activities were better than vitamin C. Moreover, twenty compounds with anti-inflammatory, analgesic, and antioxidant activities were unraveled from the GC-MS analysis. Ar-tumerone, curcumin, γ-sitosterol, α-tocopherol, isocurcumenol, adamantane, and curdione were the lead compounds based on their binding affinities (for PDE-4B, COX-1, COX-2, SOD, CAT, GPx), lower molecular weights, non-permeation of blood brain barrier, bioavailability profiles, non-inhibition of metabolizing enzymes, faster renal clearance, and non-violation of Lipinski's rules.ConclusionAdamantane, α-tocopherol, and γ-sitosterol reported for the first time in the plant's rhizome could mitigate oxidative stress and inflammation as mediators of apoptosis, cytotoxic impaired autophagy, DNA damages, and mitochondrial dysfunction that contributes to the progression of non-communicable diseases (NCDs).","PeriodicalId":19019,"journal":{"name":"Natural Product Communications","volume":"22 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-05-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141148139","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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