Pharmacological Research - Natural Products最新文献_第4页

Antioxidant activity and identification by HPLC-DAD-MS of 3-deoxyanthocyanins in the husks of Sorghum caudatum (L.) Moench grains from Burkina Faso 布基纳法索高粱（Sorghum caudatum (L.) Moench）谷物外皮中的 3-脱氧anthocyanins的抗氧化活性和 HPLC-DAD-MS 鉴定

Pharmacological Research - Natural Products

Pub Date : 2024-09-27 DOI: 10.1016/j.prenap.2024.100096

Ousséni Sawadogo , Dominique Saga Kaboré , Mahamadi Ouedraogo , Arrounan Noba , Rémy K. Bationo , Hermine Zime Diawara , Eloi Palé

As indicated by the World Health Organisation (WHO), the resurgence of chronic diseases is projected to account for 70 % of deaths and 56 % of illnesses globally by 2030. In response, authorities are allocating resources towards prevention through the use of substances with natural or synthetic antioxidant properties. However, the safety of synthetic antioxidants is constrained by the limited number of molecules they can be derived from and the necessity for intricate and costly testing to substantiate their safety. In light of this, the scientific community has set itself the objective of identifying new potential sources of natural antioxidants with the more effective capacity in prevetion of these chronic diseases. Anthocyanins, particularly 3-deoxyanthocyanins are cited as one antioxidant molecules with preventive efficacy. The objective of this study is to contribute to the discovery of new sources of 3-deoxyanthocyanins. In order to achieve this objective, a concentrated extract of 3-deoxyanthocyanins was first prepared by maceration of the husks of Sorghum caudatum grains in acidified ethanol, followed by precipitation in acidified distilled water.The Folin-Ciocalteu and differential pH methods were then employed to determine the total phenolic compound content and the total 3-deoxyanthocyanin content of the extract, respectively. The antioxidant potential of the extract was evaluated by determining its free radical scavenging activity using the ABTS method, its reducing power of ferric ions using the FRAP method, and the percentage of hydrogen peroxide (H₂O₂) scavenging. Using physico-chemical and physical methods (PC, HPLC, UV–vis and MS), the 3-deoxyanthocyanins present in the extract from the husks of Sorghum caudatum grains were identified. The results of these analyses demonstrated that the total phenolic compound content was 237.73 ± 2.12 mg GAE/g extract, while the 3-deoxyanthocyanin content was 99.33 ± 4.16 mg EApi/g extract and 110.05 ± 4.33 mg ELt/g extract. The extract demonstrated notable antioxidant activity, with an CI₅₀ of 62.59 µg/mL as determined by the ABTS method, a content of 77.35 ± 0.17 mg TE /g extract as quantified by the FRAP method, and an H₂O₂ scavenging percentage of approximately 72.29 %. The extract was found to contain five distinct compounds, namely luteolinidin, 7-O-methylluteolinidin, 5-O-methylluteolinidin, apigeninidin and 7-O-methylapigeninidin. The grain husks of Sorghum caudatum represent a novel source of 3-deoxyanthocyanins. Consequently, they offer a promising avenue for the extraction of natural antioxidants, natural colouring agents and nutraceuticals for the food industry, thereby enhancing the economic value of agricultural waste and augmenting the profitability of Sorghum cultivation.

世界卫生组织（WHO）指出，预计到 2030 年，慢性疾病的重新抬头将占全球死亡人数的 70%，占疾病总数的 56%。为此，有关部门正在调拨资源，通过使用具有天然或合成抗氧化特性的物质来进行预防。然而，合成抗氧化剂的安全性受到限制，因为它们可以提取的分子数量有限，而且必须进行复杂而昂贵的测试才能证实其安全性。有鉴于此，科学界将目标设定为寻找新的天然抗氧化剂潜在来源，以更有效地预防这些慢性疾病。花青素，尤其是 3-脱氧花青素被认为是一种具有预防功效的抗氧化分子。本研究的目的是为发现 3-脱氧花青素的新来源做出贡献。为了实现这一目标，首先用酸化乙醇浸泡高粱谷壳，然后用酸化蒸馏水沉淀，制备 3-脱氧花青素的浓缩提取物，然后采用 Folin-Ciocalteu 和 pH 差值法分别测定提取物中的总酚类化合物含量和总 3-脱氧花青素含量。通过 ABTS 法测定自由基清除活性、FRAP 法测定铁离子还原力和过氧化氢（H2O2）清除百分比，评估了提取物的抗氧化潜力。利用物理化学和物理方法（PC、HPLC、UV-vis 和 MS）鉴定了高粱谷壳提取物中的 3-脱氧anthocyanins。分析结果表明，总酚类化合物含量为 237.73 ± 2.12 毫克 GAE/克提取物，3-脱氧花青素含量为 99.33 ± 4.16 毫克 EApi/克提取物和 110.05 ± 4.33 毫克 ELt/克提取物。该提取物具有显著的抗氧化活性，ABTS 法测定的 CI50 为 62.59 µg/mL，FRAP 法量化的 TE 含量为 77.35 ± 0.17 mg TE/g，H2O2 清除率约为 72.29 %。提取物中含有五种不同的化合物，即木犀草素、7-O-甲基木犀草素、5-O-甲基木犀草素、芹菜素和 7-O-甲基芹菜素。高粱的谷壳是 3-脱氧花青素的一种新来源。因此，它们为食品工业提取天然抗氧化剂、天然着色剂和营养保健品提供了一个前景广阔的途径，从而提高了农业废弃物的经济价值，增加了高粱种植的利润。

{"title":"Antioxidant activity and identification by HPLC-DAD-MS of 3-deoxyanthocyanins in the husks of Sorghum caudatum (L.) Moench grains from Burkina Faso","authors":"Ousséni Sawadogo , Dominique Saga Kaboré , Mahamadi Ouedraogo , Arrounan Noba , Rémy K. Bationo , Hermine Zime Diawara , Eloi Palé","doi":"10.1016/j.prenap.2024.100096","DOIUrl":"10.1016/j.prenap.2024.100096","url":null,"abstract":"<div><div>As indicated by the World Health Organisation (WHO), the resurgence of chronic diseases is projected to account for 70 % of deaths and 56 % of illnesses globally by 2030. In response, authorities are allocating resources towards prevention through the use of substances with natural or synthetic antioxidant properties. However, the safety of synthetic antioxidants is constrained by the limited number of molecules they can be derived from and the necessity for intricate and costly testing to substantiate their safety. In light of this, the scientific community has set itself the objective of identifying new potential sources of natural antioxidants with the more effective capacity in prevetion of these chronic diseases. Anthocyanins, particularly 3-deoxyanthocyanins are cited as one antioxidant molecules with preventive efficacy. The objective of this study is to contribute to the discovery of new sources of 3-deoxyanthocyanins. In order to achieve this objective, a concentrated extract of 3-deoxyanthocyanins was first prepared by maceration of the husks of <em>Sorghum caudatum</em> grains in acidified ethanol, followed by precipitation in acidified distilled water.The Folin-Ciocalteu and differential pH methods were then employed to determine the total phenolic compound content and the total 3-deoxyanthocyanin content of the extract, respectively. The antioxidant potential of the extract was evaluated by determining its free radical scavenging activity using the ABTS method, its reducing power of ferric ions using the FRAP method, and the percentage of hydrogen peroxide (H<sub>2</sub>O<sub>2</sub>) scavenging. Using physico-chemical and physical methods (PC, HPLC, UV–vis and MS), the 3-deoxyanthocyanins present in the extract from the husks of <em>Sorghum caudatum</em> grains were identified. The results of these analyses demonstrated that the total phenolic compound content was 237.73 ± 2.12 mg GAE/g extract, while the 3-deoxyanthocyanin content was 99.33 ± 4.16 mg EApi/g extract and 110.05 ± 4.33 mg ELt/g extract. The extract demonstrated notable antioxidant activity, with an CI<sub>50</sub> of 62.59 µg/mL as determined by the ABTS method, a content of 77.35 ± 0.17 mg TE /g extract as quantified by the FRAP method, and an H<sub>2</sub>O<sub>2</sub> scavenging percentage of approximately 72.29 %. The extract was found to contain five distinct compounds, namely luteolinidin, 7-<em>O</em>-methylluteolinidin, 5-<em>O</em>-methylluteolinidin, apigeninidin and 7-<em>O</em>-methylapigeninidin. The grain husks of <em>Sorghum caudatum</em> represent a novel source of 3-deoxyanthocyanins. Consequently, they offer a promising avenue for the extraction of natural antioxidants, natural colouring agents and nutraceuticals for the food industry, thereby enhancing the economic value of agricultural waste and augmenting the profitability of <em>Sorghum</em> cultivation.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100096"},"PeriodicalIF":0.0,"publicationDate":"2024-09-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142422691","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}

引用次数: 0

Biological evaluation of selected phytochemicals as a multi-targeted antitumor, antiproliferative and apoptotic agents in cancer 选定植物化学物质作为多靶点抗肿瘤、抗增殖和细胞凋亡剂对癌症的生物学评估

Pharmacological Research - Natural Products

Pub Date : 2024-09-26 DOI: 10.1016/j.prenap.2024.100097

Habiba Khan , Zeeshan Arif

Background

Cancer is one of the most challenging and complex diseases to treat. It is currently the primary cause of mortality globally. Even with the advances in modern medicine and therapies, there is no significant progress in the overall survival rate. Thus, many efforts are continued to find new strategies and preventive agents to improve efficiency in cancer therapy.

Results

Naturally occurring components isolated from plants known as phytochemicals, serve as a vital source for cancer prevention and treatment. The majority of approved anti-cancer medications are isolated from natural sources. Phytochemicals exert complementary and overlying mechanisms of action to slow down multistep carcinogenesis. The specific mechanisms of phytochemicals include an increase in reactive oxygen species (ROS), a decrease in proliferation rate, inactivation of carcinogens, induction of phase arrest in the cell cycle and apoptosis.

Conclusions

This review highlights the comprehensive therapeutic effects of phytochemicals against several forms of cancer with special focus on Rhein, Karanjin, 6-Gingerol, 10-Gingerol and their proapoptotic, antiproliferative, antimetastatic and antiangiogenic effects.

背景癌症是治疗过程中最具挑战性和最复杂的疾病之一。目前，它是导致全球死亡的主要原因。即使现代医学和疗法不断进步，癌症患者的总生存率也没有明显提高。从植物中分离出来的天然成分被称为植物化学物质，是预防和治疗癌症的重要来源。大多数获批的抗癌药物都是从天然来源中分离出来的。植物化学物质具有互补和重叠的作用机制，可减缓多步致癌过程。植物化学物质的具体作用机制包括增加活性氧（ROS）、降低增殖率、灭活致癌物质、诱导细胞周期的阶段性停滞和细胞凋亡。

{"title":"Biological evaluation of selected phytochemicals as a multi-targeted antitumor, antiproliferative and apoptotic agents in cancer","authors":"Habiba Khan , Zeeshan Arif","doi":"10.1016/j.prenap.2024.100097","DOIUrl":"10.1016/j.prenap.2024.100097","url":null,"abstract":"<div><h3>Background</h3><div>Cancer is one of the most challenging and complex diseases to treat. It is currently the primary cause of mortality globally. Even with the advances in modern medicine and therapies, there is no significant progress in the overall survival rate. Thus, many efforts are continued to find new strategies and preventive agents to improve efficiency in cancer therapy.</div></div><div><h3>Results</h3><div>Naturally occurring components isolated from plants known as phytochemicals, serve as a vital source for cancer prevention and treatment. The majority of approved anti-cancer medications are isolated from natural sources. Phytochemicals exert complementary and overlying mechanisms of action to slow down multistep carcinogenesis. The specific mechanisms of phytochemicals include an increase in reactive oxygen species (ROS), a decrease in proliferation rate, inactivation of carcinogens, induction of phase arrest in the cell cycle and apoptosis.</div></div><div><h3>Conclusions</h3><div>This review highlights the comprehensive therapeutic effects of phytochemicals against several forms of cancer with special focus on Rhein, Karanjin, 6-Gingerol, 10-Gingerol and their proapoptotic, antiproliferative, antimetastatic and antiangiogenic effects.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100097"},"PeriodicalIF":0.0,"publicationDate":"2024-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142422690","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}

引用次数: 0

Phytochemical screening, antioxidant, antibacterial, and antifungal properties of the Cymbopogon citratus methanolic extract 柠檬香蒲甲醇提取物的植物化学筛选、抗氧化、抗菌和抗真菌特性

Pharmacological Research - Natural Products

Pub Date : 2024-09-19 DOI: 10.1016/j.prenap.2024.100094

Salah Neghmouche Nacer , Lakhdari Wassima , Walid Boussebaa , Abderrezzak Abadi , Ibtissem Benyahia , Djawahir Mouhoubi , Amel Ladjal , Hamida Hammi , Hakim Bachir , Abderrahmene Dehliz , Younes Moussaoui

In this work, the aerial parts of Cymbopogon citratus, harvested in Algeria, were analyzed as potential sources of biologically active compounds. The phytochemical composition, the content of total phenols and flavonoids in the methanolic extract of this plant, as well as its antioxidant, antibacterial, and antifungal capacities, were evaluated. The methanolic extract had phenolic compounds and flavonoids, with levels of 92.82 µg GAE/mg Dry weight and 58.98 µg QE/mg Dry weight, respectively. Furthermore, the methanolic extract exhibited moderate antioxidant activity as assessed by DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2′azinobis (3-ethylbenzothiozoline-6-sulfonic acid) disodium salt radical), and β-carotene tests, while its antimicrobial activity was tested against four bacterial strains. Thus, a MBC/MIC ratio of 2 indicates that the extract exhibits bactericidal activity against Escherichia coli. Additionally, the extract exhibited antifungal activity against Thielaviopsis paradoxa, Alternaria sp., and Fusarium solani, with inhibition rates ranging from 50.59 % to 70.20 %. LC-MS analysis identified a variety of components, including chlorogenic acid (17.40 %), catechin (34.64 %), salicin (9.55 %), and curcumin (8.97 %), which are likely responsible for the observed activities. This study demonstrated that the aerial parts of Cymbopogon citratus offer a cost-effective source of natural compounds with bactericidal and antifungal activity, offering potential applications in the food and pharmaceutical industries.

这项研究分析了在阿尔及利亚收获的柠檬香蒲（Cymbopogon citratus）的气生部分，将其视为生物活性化合物的潜在来源。研究人员对该植物甲醇提取物中的植物化学成分、总酚和类黄酮含量及其抗氧化、抗菌和抗真菌能力进行了评估。甲醇提取物中的酚类化合物和类黄酮含量分别为 92.82 µg GAE/mg（干重）和 58.98 µg QE/mg（干重）。此外，通过 DPPH（2,2-二苯基-1-苦基肼）、ABTS（2,2′azinobis（3-乙基苯并硫唑啉-6-磺酸）二钠盐自由基）和 β-胡萝卜素测试，甲醇提取物显示出中等程度的抗氧化活性，而其抗菌活性则针对四种细菌菌株进行了测试。因此，MBC/MIC 比率为 2 表明该提取物对大肠杆菌具有杀菌活性。此外，萃取物还对 Thielaviopsis paradoxa、Alternaria sp.和 Fusarium solani 具有抗真菌活性，抑制率从 50.59 % 到 70.20 % 不等。LC-MS 分析确定了多种成分，包括绿原酸（17.40 %）、儿茶素（34.64 %）、水杨酸（9.55 %）和姜黄素（8.97 %），这些成分可能是导致观察到的活性的原因。这项研究表明，柠檬香蒲的气生部分是一种具有成本效益的天然化合物来源，具有杀菌和抗真菌活性，在食品和制药行业具有潜在的应用价值。

{"title":"Phytochemical screening, antioxidant, antibacterial, and antifungal properties of the Cymbopogon citratus methanolic extract","authors":"Salah Neghmouche Nacer , Lakhdari Wassima , Walid Boussebaa , Abderrezzak Abadi , Ibtissem Benyahia , Djawahir Mouhoubi , Amel Ladjal , Hamida Hammi , Hakim Bachir , Abderrahmene Dehliz , Younes Moussaoui","doi":"10.1016/j.prenap.2024.100094","DOIUrl":"10.1016/j.prenap.2024.100094","url":null,"abstract":"<div><div>In this work, the aerial parts of <em>Cymbopogon citratus</em>, harvested in Algeria, were analyzed as potential sources of biologically active compounds. The phytochemical composition, the content of total phenols and flavonoids in the methanolic extract of this plant, as well as its antioxidant, antibacterial, and antifungal capacities, were evaluated. The methanolic extract had phenolic compounds and flavonoids, with levels of 92.82 µg GAE/mg Dry weight and 58.98 µg QE/mg Dry weight, respectively. Furthermore, the methanolic extract exhibited moderate antioxidant activity as assessed by DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2′azinobis (3-ethylbenzothiozoline-6-sulfonic acid) disodium salt radical), and β-carotene tests, while its antimicrobial activity was tested against four bacterial strains. Thus, a MBC/MIC ratio of 2 indicates that the extract exhibits bactericidal activity against <em>Escherichia coli</em>. Additionally, the extract exhibited antifungal activity against <em>Thielaviopsis paradoxa</em>, <em>Alternaria</em> sp., and <em>Fusarium solani</em>, with inhibition rates ranging from 50.59 % to 70.20 %. LC-MS analysis identified a variety of components, including chlorogenic acid (17.40 %), catechin (34.64 %), salicin (9.55 %), and curcumin (8.97 %), which are likely responsible for the observed activities. This study demonstrated that the aerial parts of <em>Cymbopogon citratus</em> offer a cost-effective source of natural compounds with bactericidal and antifungal activity, offering potential applications in the food and pharmaceutical industries.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100094"},"PeriodicalIF":0.0,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142314985","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}

引用次数: 0

GC-MS profiling of the leaf extract of Garcinia pedunculata, molecular docking, ADME/drug likeness predictions and toxicity analysis 藤黄属植物叶提取物的气相色谱-质谱分析、分子对接、ADME/药物相似性预测和毒性分析

Pharmacological Research - Natural Products

Pub Date : 2024-09-19 DOI: 10.1016/j.prenap.2024.100089

Rajesh Kumar Shah , Modhumita Karmakar , Mouchurisha Deori , Leeza Das

Medicinal plants have long been valued for their efficacy, cultural acceptance and lower side effects. Amidst rising concerns about multidrug-resistant bacteria, there is an increasing push to identify novel plant-based drugs with unique mechanisms of action. Garcinia pedunculata, commonly used as food and traditional medicine among tribal communities in North Eastern India, was investigated for its potential medicinal properties. The study involved analyzing the phytoconstituents of the methanolic leaf extract using GC-MS (Gas Chromatography- Mass Spectrometry), which identified 30 compounds. These compounds were further evaluated through in silico studies, including drug-likeness assessments and molecular docking. Molecular docking results indicated that the compounds strongly interacted with Penicillin Binding Protein 4 (PBP4) of Staphylococcus aureus (S aureus), a well-known drug target. Notably, ethane-1,1-diol dipropanoate demonstrated favorable drug-like properties, meeting four out of five drug filters and exhibiting promising physiochemical characteristics, lipophilicity, solubility and pharmacokinetic profiles with minimal toxicity. This suggests its potential for development into novel antimicrobial formulations. Further research using animal models is underway to validate these findings in vivo.

长期以来，药用植物因其功效、文化认可度和较低的副作用而备受重视。随着人们对耐多药细菌的担忧日益加剧，人们越来越希望找到具有独特作用机制的新型植物药物。Garcinia pedunculata 是印度东北部部落社区常用的食物和传统药物，研究人员对其潜在的药用特性进行了调查。研究使用气相色谱-质谱法（GC-MS）分析了甲醇叶提取物中的植物成分，确定了 30 种化合物。通过药物相似性评估和分子对接等硅学研究对这些化合物进行了进一步评估。分子对接结果表明，这些化合物与金黄色葡萄球菌（S aureus）的青霉素结合蛋白 4（PBP4）（众所周知的药物靶标）有强烈的相互作用。值得注意的是，1,1-二醇二丙酸乙酯表现出了良好的类药物特性，符合五项药物筛选条件中的四项，并表现出良好的理化特性、亲脂性、溶解性和药代动力学特征，且毒性极低。这表明它具有开发新型抗菌制剂的潜力。目前正在利用动物模型开展进一步研究，以便在体内验证这些发现。

{"title":"GC-MS profiling of the leaf extract of Garcinia pedunculata, molecular docking, ADME/drug likeness predictions and toxicity analysis","authors":"Rajesh Kumar Shah , Modhumita Karmakar , Mouchurisha Deori , Leeza Das","doi":"10.1016/j.prenap.2024.100089","DOIUrl":"10.1016/j.prenap.2024.100089","url":null,"abstract":"<div><div>Medicinal plants have long been valued for their efficacy, cultural acceptance and lower side effects. Amidst rising concerns about multidrug-resistant bacteria, there is an increasing push to identify novel plant-based drugs with unique mechanisms of action. <em>Garcinia pedunculata</em>, commonly used as food and traditional medicine among tribal communities in North Eastern India, was investigated for its potential medicinal properties. The study involved analyzing the phytoconstituents of the methanolic leaf extract using GC-MS (Gas Chromatography- Mass Spectrometry), which identified 30 compounds. These compounds were further evaluated through <em>in silico</em> studies, including drug-likeness assessments and molecular docking. Molecular docking results indicated that the compounds strongly interacted with Penicillin Binding Protein 4 (PBP4) of <em>Staphylococcus aureus (S aureus)</em>, a well-known drug target. Notably, ethane-1,1-diol dipropanoate demonstrated favorable drug-like properties, meeting four out of five drug filters and exhibiting promising physiochemical characteristics, lipophilicity, solubility and pharmacokinetic profiles with minimal toxicity. This suggests its potential for development into novel antimicrobial formulations. Further research using animal models is underway to validate these findings in vivo.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100089"},"PeriodicalIF":0.0,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142311321","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}

引用次数: 0

Mitigating type 2 diabetes: Scientific validation of Biophytum sensitivum (L.) DC. and Mimosa pudica L. as substitutes for Cassia mimosoides L. in ayurvedic medicine 缓解 2 型糖尿病：在阿育吠陀医学中，以Biophytum sensitivum (L.) DC.和Mimosa pudica L.替代决明子的科学验证

Pharmacological Research - Natural Products

Pub Date : 2024-09-19 DOI: 10.1016/j.prenap.2024.100091

Abdul Rahim Muhammed Jasim , Sivaji Yuvaranjani , Alaganandam Kumaran

The Ayurvedic concept of 'pratinidhi dravya' (substitute drugs) offers a systematic approach to replaces scarce ingredients in traditional formulations with botanically or pharmacologically similar alternatives. This practice aims to maintain therapeutic efficacy and safety while preventing adulteration. However, scientific validation of these substitutes is essential. This study investigates the substitution of the rare species Cassia mimosoides L. (CM) with two more readily available species recommended in Ayurveda: Biophytum sensitivum (L.) DC. (BS) and Mimosa pudica L. (MP). The research focuses on their potential use in the popular antidiabetic Ayurvedic medicine Katakakhadiradi Kashayam, specifically examining their antioxidant and antidiabetic properties. Our findings revealed that the substituted species, BS and MP, exhibit a remarkable richness in phenolic and flavonoid content compared to the species CM, indicating their potent antioxidant capabilities (IC₅₀ values: CM: 19.55 μg/ml, BS: 60.38 μg/ml, MP: 39.49 μg/ml). LC-MS/MS profiling and quantification indicate a significant amount of different pharmacologically active polyphenols in the three species. Among the identified compounds, orientin (CM-EA: 44.362 mg/kg, BS-EA: 20.528 mg/kg, MP-EA: 34.094 mg/kg) and isoorientin (CM-EA: 85.022 mg/kg, BS-EA: 25.168 mg/kg, MP-EA: 45.035 mg/kg) were the major compounds present in substantial quantity in all three species. Additionally, shikimic acid and chlorogenic acid were present in higher concentrations in the BS-EA and MP-EA extracts. Furthermore, these species demonstrated significant activity against α-glucosidase in various solvent extracts, with IC₅₀ values of 16.44 μg/ml for CM, 56.65 μg/ml for MP, and 69.25 μg/ml for BS, suggesting their promising role in managing diabetes mellitus. These findings support the efficacy of BS and MP as substitutes for CM in managing diabetes and oxidative stress, emphasizing the importance of scientific validation in herbal medicine substitution and adulteration prevention.

阿育吠陀的 "pratinidhi dravya"（替代药物）概念提供了一种系统方法，用植物学或药理学上相似的替代品取代传统配方中的稀缺成分。这种做法旨在保持疗效和安全性，同时防止掺假。然而，对这些替代品进行科学验证至关重要。本研究调查了用阿育吠陀中推荐的两种更易获得的物种替代稀有物种决明子（CM）的情况：Biophytum sensitivum (L.) DC.(BS) 和 Mimosa pudica L. (MP)。研究的重点是它们在阿育吠陀常用的抗糖尿病药物 Katakakhadiradi Kashayam 中的潜在用途，特别是检查它们的抗氧化和抗糖尿病特性。我们的研究结果表明，与 CM 相比，BS 和 MP 的酚类和类黄酮含量显著丰富，这表明它们具有很强的抗氧化能力（IC50 值：CM：19.55 μg/ml；BS：60.38 μg/ml；MP：39.49 μg/ml）。LC-MS/MS 分析和定量结果表明，这三种植物中含有大量不同药理活性的多酚类化合物。在已鉴定的化合物中，荭草苷（CM-EA：44.362 毫克/千克，BS-EA：20.528 毫克/千克，MP-EA：34.094 毫克/千克）和异荭草苷（CM-EA：85.022 毫克/千克，BS-EA：25.168 毫克/千克，MP-EA：45.035 毫克/千克）是这三种植物中大量存在的主要化合物。此外，莽草酸和绿原酸在 BS-EA 和 MP-EA 提取物中含量较高。此外，在各种溶剂提取物中，这些物种对α-葡萄糖苷酶具有明显的活性，CM 的 IC50 值为 16.44 μg/ml，MP 为 56.65 μg/ml，BS 为 69.25 μg/ml，这表明它们在控制糖尿病方面具有良好的作用。这些研究结果支持 BS 和 MP 作为中药替代品在控制糖尿病和氧化应激方面的功效，强调了科学验证在中药替代和防止掺假方面的重要性。

{"title":"Mitigating type 2 diabetes: Scientific validation of Biophytum sensitivum (L.) DC. and Mimosa pudica L. as substitutes for Cassia mimosoides L. in ayurvedic medicine","authors":"Abdul Rahim Muhammed Jasim , Sivaji Yuvaranjani , Alaganandam Kumaran","doi":"10.1016/j.prenap.2024.100091","DOIUrl":"10.1016/j.prenap.2024.100091","url":null,"abstract":"<div><div>The Ayurvedic concept of 'pratinidhi dravya' (substitute drugs) offers a systematic approach to replaces scarce ingredients in traditional formulations with botanically or pharmacologically similar alternatives. This practice aims to maintain therapeutic efficacy and safety while preventing adulteration. However, scientific validation of these substitutes is essential. This study investigates the substitution of the rare species <em>Cassia mimosoides</em> L. (CM) with two more readily available species recommended in Ayurveda: <em>Biophytum sensitivum</em> (L.) DC. (BS) and <em>Mimosa pudica</em> L. (MP). The research focuses on their potential use in the popular antidiabetic Ayurvedic medicine Katakakhadiradi Kashayam, specifically examining their antioxidant and antidiabetic properties. Our findings revealed that the substituted species, BS and MP, exhibit a remarkable richness in phenolic and flavonoid content compared to the species CM, indicating their potent antioxidant capabilities (IC<sub>50</sub> values: CM: 19.55 μg/ml, BS: 60.38 μg/ml, MP: 39.49 μg/ml). LC-MS/MS profiling and quantification indicate a significant amount of different pharmacologically active polyphenols in the three species. Among the identified compounds, orientin (CM-EA: 44.362 mg/kg, BS-EA: 20.528 mg/kg, MP-EA: 34.094 mg/kg) and isoorientin (CM-EA: 85.022 mg/kg, BS-EA: 25.168 mg/kg, MP-EA: 45.035 mg/kg) were the major compounds present in substantial quantity in all three species. Additionally, shikimic acid and chlorogenic acid were present in higher concentrations in the BS-EA and MP-EA extracts. Furthermore, these species demonstrated significant activity against α-glucosidase in various solvent extracts, with IC<sub>50</sub> values of 16.44 μg/ml for CM, 56.65 μg/ml for MP, and 69.25 μg/ml for BS, suggesting their promising role in managing diabetes mellitus. These findings support the efficacy of BS and MP as substitutes for CM in managing diabetes and oxidative stress, emphasizing the importance of scientific validation in herbal medicine substitution and adulteration prevention.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100091"},"PeriodicalIF":0.0,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142311184","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}

引用次数: 0

Unveiling the therapeutical potential of Tupistra clarkei in diabetic neuropathic pain on Wistar albino rats: A Himalayan Gem 揭示 Tupistra clarkei 对 Wistar albino 大鼠糖尿病神经性疼痛的治疗潜力：喜马拉雅宝石

Pharmacological Research - Natural Products

Pub Date : 2024-09-17 DOI: 10.1016/j.prenap.2024.100092

Pramod Rai , Manodeep Chakraborty , Devid Chutia , Nihar Ranjan Bhuyan

Background and aims

Diabetic neuropathy is a long-existing painful neuronal error associated with high sugar levels, hyperalgesia, and slowed motor nerve conduction. Therefore, the study aims to investigate the efficacy of the methanolic extract of Tupistra clarkei (METC) against diabetes-inducing neuropathy in Wistar albino rats. The potential of these findings to inspire hope for improved treatment strategies for diabetic neuropathy is significant and inspiring, offering a promising outlook for the future.

Method and results

Phytochemical and acute toxicity screening were carried out using METC. Then, Streptozotocin induces hyperglycaemia followed by neuropathy was carried out in five groups of animals such as the normal control (NC), Diabetic control (DC), The standard control (Std), The low-dose (100 mg/kg), the high-dose group (200 mg/kg). After regular observation of motor nerve conduction, neuropathic assays, and inflammatory mediators for the 8th week, animals were sacrificed using ketamine hydrochloride. The sciatic nerve was isolated, then subjected to histopathological analysis using an Olympus binocular microscope at 45X, and subjected to antioxidant study. METC reported the presence of alkaloids, carbohydrates, flavonoids, saponins, and steroids. The results of the LC-MS analysis of the METC samples detected at peak m/z 371.1100 could be responsible for the antidiabetic property of Tupistra clarkei. In addition, the results indicate significant restoration of oxidative stress, nerve conduction, inflammatory pain, elevated blood glucose levels related to hyperalgesia, motor nerve conduction, and reversible curing of cellular injury.

Conclusion

METC controls and prevents diabetes-induced neuropathic pain and related complications such as nerve conduction, raised temperature threshold, and extended latency in hyperalgesia.

背景和目的糖尿病神经病变是一种长期存在的疼痛性神经元错误，与高血糖、痛觉减退和运动神经传导减慢有关。因此，本研究旨在探讨蟾酥甲醇提取物（METC）对 Wistar 白化大鼠糖尿病神经病变的疗效。这些研究结果为改善糖尿病神经病变的治疗策略带来了希望，具有重要的启发意义，为未来提供了一个充满希望的前景。方法和结果使用 METC 进行了植物化学和急性毒性筛选。然后，对正常对照组（NC）、糖尿病对照组（DC）、标准对照组（std）、低剂量组（100 mg/kg）和高剂量组（200 mg/kg）等五组动物进行链脲佐菌素诱导高血糖继发神经病变的实验。第 8 周定期观察运动神经传导、神经病理性检测和炎症介质后，使用盐酸氯胺酮处死动物。分离坐骨神经，然后使用奥林巴斯双目显微镜在 45 倍显微镜下进行组织病理学分析，并进行抗氧化研究。METC 报告了生物碱、碳水化合物、黄酮类、皂苷和类固醇的存在。对 METC 样品进行 LC-MS 分析的结果显示，在 m/z 371.1100 峰上检测到的物质可能是 Tupistra clarkei 具有抗糖尿病特性的原因。此外，研究结果表明，METC 对氧化应激、神经传导、炎症性疼痛、与痛觉减退相关的血糖水平升高、运动神经传导以及细胞损伤的可逆性治愈有明显的恢复作用。

{"title":"Unveiling the therapeutical potential of Tupistra clarkei in diabetic neuropathic pain on Wistar albino rats: A Himalayan Gem","authors":"Pramod Rai , Manodeep Chakraborty , Devid Chutia , Nihar Ranjan Bhuyan","doi":"10.1016/j.prenap.2024.100092","DOIUrl":"10.1016/j.prenap.2024.100092","url":null,"abstract":"<div><h3>Background and aims</h3><p>Diabetic neuropathy is a long-existing painful neuronal error associated with high sugar levels, hyperalgesia, and slowed motor nerve conduction. Therefore, the study aims to investigate the efficacy of the methanolic extract of <em>Tupistra clarkei</em> (METC) against diabetes-inducing neuropathy in Wistar albino rats. The potential of these findings to inspire hope for improved treatment strategies for diabetic neuropathy is significant and inspiring, offering a promising outlook for the future.</p></div><div><h3>Method and results</h3><p>Phytochemical and acute toxicity screening were carried out using METC. Then, Streptozotocin induces hyperglycaemia followed by neuropathy was carried out in five groups of animals such as the normal control (NC), Diabetic control (DC), The standard control (Std), The low-dose (100 mg/kg), the high-dose group (200 mg/kg). After regular observation of motor nerve conduction, neuropathic assays, and inflammatory mediators for the 8th week, animals were sacrificed using ketamine hydrochloride. The sciatic nerve was isolated, then subjected to histopathological analysis using an Olympus binocular microscope at 45X, and subjected to antioxidant study. METC reported the presence of alkaloids, carbohydrates, flavonoids, saponins, and steroids. The results of the LC-MS analysis of the METC samples detected at peak <em>m/z</em> 371.1100 could be responsible for the antidiabetic property of <em>Tupistra clarkei</em>. In addition, the results indicate significant restoration of oxidative stress, nerve conduction, inflammatory pain, elevated blood glucose levels related to hyperalgesia, motor nerve conduction, and reversible curing of cellular injury.</p></div><div><h3>Conclusion</h3><p>METC controls and prevents diabetes-induced neuropathic pain and related complications such as nerve conduction, raised temperature threshold, and extended latency in hyperalgesia.</p></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100092"},"PeriodicalIF":0.0,"publicationDate":"2024-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142274822","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}

引用次数: 0

Anxiolytic-like effect of daidzin possibly through GABAA receptor α2 and α3 subunits interaction pathway: In vivo and in silico studies daidzin可能通过GABAA受体α2和α3亚基相互作用途径产生抗焦虑样效应：体内和硅学研究

Pharmacological Research - Natural Products

Pub Date : 2024-09-16 DOI: 10.1016/j.prenap.2024.100090

Md. Torequl Islam , Abdullah Al Shamsh Prottay , Md. Showkot Akbor , Md. Shimul Bhuia , Md. Amirul Islam , Md. Saifiuzzaman

The soy plant-derived isoflavone daidzin (DZN) has diverse biological activities, including neuroprotective (e.g., memory-enhancing and antiepileptic) effects. This study emphasizes evaluating the anxiolytic effect of DZN on mice. Additionally, in silico investigations were also carried out to check the potential molecular mechanisms for the anxiolytic effect of DZN. For this, adult male Swiss albino mice were intraperitoneally (i.p.) treated with DZN (5, 10, and 20 mg/kg) with or without the standard GABAergic agonist drug diazepam (DZP: 2 mg/kg) and/or antagonist drug flumazenil (FLU: 0.1 mg/kg) and checked for different locomotor behaviors using various mouse models. The molecular docking study of DZN was conducted against GABA_A receptor subunits. Findings suggest that DZN dose-dependently and significantly (p <0.05) increased locomotor activities such as the number of field crosses, hole crosses, swings, grooming, and light residence time while decreasing the rearing of the animals. With DZP, it significantly (p <0.05) reduced the test parameters, while altering these parameters with FLU. Our molecular docking studies demonstrate that DZN has a strong binding affinity of −7.4 and −6.9 kcal/mol for α2 and α3 subunits of the GABA_A receptor, respectively, whereas the standard drugs DZP and FLU showed binding affinities between −6.0 and −6.7 kcal/mol for these subunits. Taken together, DZN augmented the anxiolytic effect of DZP while reducing the effect of FLU in mice. We suppose that DZN may show anxiolytic-like effects on Swiss mice, possibly through α2 and α3 subunits of the GABA_A receptor interaction pathway.

从大豆中提取的异黄酮大豆异黄酮（DZN）具有多种生物活性，包括神经保护（如增强记忆和抗癫痫）作用。本研究重点评估了 DZN 对小鼠的抗焦虑作用。此外，研究人员还进行了硅学研究，以检查 DZN 抗焦虑作用的潜在分子机制。为此，对成年雄性瑞士白化小鼠腹腔注射（i.p.）DZN（5、10 和 20 毫克/千克），同时注射或不注射标准 GABA 能激动剂药物地西泮（DZP：2 毫克/千克）和/或拮抗剂药物氟马西尼（FLU：0.1 毫克/千克），并使用各种小鼠模型检查不同的运动行为。DZN 与 GABAA 受体亚基进行了分子对接研究。研究结果表明，DZN剂量依赖性地显著（p <0.05）增加了小鼠的运动活动，如田间穿越次数、洞穴穿越次数、摆动次数、梳理次数和光照停留时间，同时减少了动物的饲养。DZP能显著（p <0.05）降低测试参数，而FLU则能改变这些参数。我们的分子对接研究表明，DZN与GABAA受体α2和α3亚基的结合亲和力分别为-7.4和-6.9 kcal/mol，而标准药物DZP和FLU与这些亚基的结合亲和力介于-6.0和-6.7 kcal/mol之间。综上所述，DZN增强了DZP的抗焦虑作用，同时降低了FLU对小鼠的作用。我们推测，DZN可能通过GABAA受体相互作用途径的α2和α3亚基对瑞士小鼠产生类似抗焦虑的作用。

{"title":"Anxiolytic-like effect of daidzin possibly through GABAA receptor α2 and α3 subunits interaction pathway: In vivo and in silico studies","authors":"Md. Torequl Islam , Abdullah Al Shamsh Prottay , Md. Showkot Akbor , Md. Shimul Bhuia , Md. Amirul Islam , Md. Saifiuzzaman","doi":"10.1016/j.prenap.2024.100090","DOIUrl":"10.1016/j.prenap.2024.100090","url":null,"abstract":"<div><p>The soy plant-derived isoflavone daidzin (DZN) has diverse biological activities, including neuroprotective (e.g., memory-enhancing and antiepileptic) effects. This study emphasizes evaluating the anxiolytic effect of DZN on mice. Additionally, <em>in silico</em> investigations were also carried out to check the potential molecular mechanisms for the anxiolytic effect of DZN. For this, adult male <em>Swiss</em> albino mice were intraperitoneally (i.p.) treated with DZN (5, 10, and 20 mg/kg) with or without the standard GABAergic agonist drug diazepam (DZP: 2 mg/kg) and/or antagonist drug flumazenil (FLU: 0.1 mg/kg) and checked for different locomotor behaviors using various mouse models. The molecular docking study of DZN was conducted against GABA<sub>A</sub> receptor subunits. Findings suggest that DZN dose-dependently and significantly (<em>p</em> <0.05) increased locomotor activities such as the number of field crosses, hole crosses, swings, grooming, and light residence time while decreasing the rearing of the animals. With DZP, it significantly (<em>p</em> <0.05) reduced the test parameters, while altering these parameters with FLU. Our molecular docking studies demonstrate that DZN has a strong binding affinity of −7.4 and −6.9 kcal/mol for α2 and α3 subunits of the GABA<sub>A</sub> receptor, respectively, whereas the standard drugs DZP and FLU showed binding affinities between −6.0 and −6.7 kcal/mol for these subunits. Taken together, DZN augmented the anxiolytic effect of DZP while reducing the effect of FLU in mice. We suppose that DZN may show anxiolytic-<em>like</em> effects on <em>Swiss</em> mice, possibly through α2 and α3 subunits of the GABA<sub>A</sub> receptor interaction pathway.</p></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100090"},"PeriodicalIF":0.0,"publicationDate":"2024-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142240769","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}

引用次数: 0

Revisiting the application and efficacy of phytochemicals of medicinal plants for the treatment of COVID-19 重新审视药用植物的植物化学成分在治疗 COVID-19 中的应用和疗效

Pharmacological Research - Natural Products

Pub Date : 2024-09-12 DOI: 10.1016/j.prenap.2024.100087

Sahar Naveed , Abiodun Oladipo , Peter Olusakin Oladoye , Mahak Naveed , Mohammed Kadhom , Adewale Akanni Tella Taleat , Naveed Anjum

The paucity of targeted medications and vaccines, coupled with the coronaviruses (COVID-19) outbreak brought by SARS-CoV-19, forced scientists to look for novel antiviral formulations. The absence of a specific treatment for COVID-19, designing new drugs and considering the use of plant-based products is crucial in the search for an effective remedy to target this deadly virus. Phytochemical medicines are faster and more cost-effective compared to conventional treatment methods. The potential use of plant extracts in the prevention and treatment of COVID-19 may have its start with the abundance of naturally occurring chemicals obtained from plants. Coronavirus enzymes, which are necessary for virus infection and replication, can be inhibited by antiviral polyphenolic medications. Flavonoids, alkaloids, terpenes and terpenoids and many more are categorized as naturally occurring compounds that may be important in the development of antiviral treatments that block viral proteases. In this review, we presented up-to-date studies with special attention on challenges and side effects of medication and traditional plant-based therapies for respiratory problems. It also highlights the importance of plant-based antiviral compounds, particularly in the development of a broad-spectrum medication against coronaviruses like SARS-CoV-2.

由于缺乏有针对性的药物和疫苗，再加上 SARS-CoV-19 带来的冠状病毒（COVID-19）爆发，科学家们不得不寻找新型抗病毒制剂。由于没有针对 COVID-19 的特效疗法，因此设计新药和考虑使用植物产品对于寻找针对这种致命病毒的有效疗法至关重要。与传统治疗方法相比，植物化学药物更快、更具成本效益。植物提取物在预防和治疗 COVID-19 方面的潜在用途可能始于从植物中获取的大量天然化学物质。抗病毒多酚药物可抑制病毒感染和复制所必需的冠状病毒酶。黄酮类、生物碱类、萜类和萜类等天然化合物可能对开发阻断病毒蛋白酶的抗病毒疗法非常重要。在这篇综述中，我们介绍了最新的研究，特别关注了药物和传统植物疗法在治疗呼吸系统问题方面所面临的挑战和副作用。它还强调了植物抗病毒化合物的重要性，特别是在开发针对冠状病毒（如 SARS-CoV-2）的广谱药物方面。

{"title":"Revisiting the application and efficacy of phytochemicals of medicinal plants for the treatment of COVID-19","authors":"Sahar Naveed , Abiodun Oladipo , Peter Olusakin Oladoye , Mahak Naveed , Mohammed Kadhom , Adewale Akanni Tella Taleat , Naveed Anjum","doi":"10.1016/j.prenap.2024.100087","DOIUrl":"10.1016/j.prenap.2024.100087","url":null,"abstract":"<div><p>The paucity of targeted medications and vaccines, coupled with the coronaviruses (COVID-19) outbreak brought by SARS-CoV-19, forced scientists to look for novel antiviral formulations. The absence of a specific treatment for COVID-19, designing new drugs and considering the use of plant-based products is crucial in the search for an effective remedy to target this deadly virus. Phytochemical medicines are faster and more cost-effective compared to conventional treatment methods. The potential use of plant extracts in the prevention and treatment of COVID-19 may have its start with the abundance of naturally occurring chemicals obtained from plants. Coronavirus enzymes, which are necessary for virus infection and replication, can be inhibited by antiviral polyphenolic medications. Flavonoids, alkaloids, terpenes and terpenoids and many more are categorized as naturally occurring compounds that may be important in the development of antiviral treatments that block viral proteases. In this review, we presented up-to-date studies with special attention on challenges and side effects of medication and traditional plant-based therapies for respiratory problems. It also highlights the importance of plant-based antiviral compounds, particularly in the development of a broad-spectrum medication against coronaviruses like SARS-CoV-2.</p></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100087"},"PeriodicalIF":0.0,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142240767","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}

引用次数: 0

Mitigation of methylglyoxal-induced hepatotoxicity by Boerhavia diffusa L. aerial extract: Insights from cellular and animal models 白花蛇舌草叶提取物缓解甲基乙二醛诱导的肝毒性：细胞和动物模型的启示

Pharmacological Research - Natural Products

Pub Date : 2024-09-12 DOI: 10.1016/j.prenap.2024.100088

Debrupa Dutta , Nikita Khandelwal , Ashutosh Behera , Snehal Dongare , Bireswar Bhattacharya , Soumi Sukla

Background

Boerhavia diffusa (Punarnava), is a perennial herb with a long-standing reputation for its antioxidative and anti-inflammatory properties, dating back to ancient times. Methylglyoxal is an advanced glycation end-product, known to be toxic in liver cell line as well as in mice model. Our objective is to illustrate the protective action of punarnava aerial extracts in methylglyoxal-induced hepatotoxicity in cell line and mice model.

Methods

Punarnava aerial parts were collected and different solvent extracts were prepared in methanol, dichloromethane and hexane by maceration followed by their LCMS/MS characterization, determination of total phenolic, total flavonoid contents and antioxidant activity by DPPH reagent. Cell viability of the extracts and methylglyoxal was assessed using different cell lines. In vitro protective effect of punarnava methanolic extract (PME) against methylglyoxal was evaluated by cell migration assay, NO and ROS production assays and Oil Red O staining in HepG2 cell line. BALB/c mice were pretreated with Punarnava methanolic extract (200 mg/kg and 400 mg/kg) for seven days followed by 290 mg/kg methylglyoxal administration for 6 hrs to induce hepatotoxicity. Serum glucose, AST, ALT, ALP and GSH level were checked and liver histopathological damages were identified.

Results

Among the three Punarnava extracts, PME possessed maximum antioxidant, total phenolic and flavonoid content as well as least cytotoxic to liver cell line. Methylglyoxal showed maximum toxicity in HepG2 cells with IC₅₀ (50 % inhibitory concentration) 3 µM. PME confers protection against methylglyoxal-induced cytotoxicity by decreasing ROS, promoting cell migration and preventing loss of cell viability. No significant change was observed in NO production and Oil Red O staining. PME-treated mice showed decrease in liver ALP levels and glucose with intact cellular morphology compared to hepatocyte steatosis and nuclear degeneration in methylglyoxal-treated group.

Discussions

Indigenous herb Punarnava is effective in protecting liver cells from damage induced by the glycolytic byproduct, methylglyoxal.

背景Boerhavia diffusa（Punarnava）是一种多年生草本植物，因其抗氧化和抗炎特性而久负盛名，其历史可追溯到古代。甲基乙二醛是一种高级糖化终产物，在肝细胞系和小鼠模型中都具有毒性。我们的目的是说明 punarnava 植物萃取物对细胞系和小鼠模型中由甲基乙二醛诱导的肝毒性的保护作用。方法收集 punarnava 植物部分，通过浸渍法在甲醇、二氯甲烷和正己烷中制备不同溶剂的萃取物，然后进行 LCMS/MS 表征，用 DPPH 试剂测定总酚、总黄酮含量和抗氧化活性。使用不同的细胞系对提取物和甲基乙二醛的细胞活力进行了评估。在 HepG2 细胞系中，通过细胞迁移试验、NO 和 ROS 生成试验以及油红 O 染色，评估了 punarnava 代谢提取物（PME）对甲基乙二醛的体外保护作用。用 Punarnava 代谢提取物（200 毫克/千克和 400 毫克/千克）对 BALB/c 小鼠进行为期七天的预处理，然后用 290 毫克/千克的甲基乙二醛诱导小鼠肝中毒 6 小时。结果在三种 Punarnava 提取物中，PME 的抗氧化剂、总酚和类黄酮含量最高，对肝细胞系的细胞毒性最小。甲基乙二酸对 HepG2 细胞的毒性最大，IC50（50% 抑制浓度）为 3 µM。PME 可通过减少 ROS、促进细胞迁移和防止细胞活力丧失来抵御甲基乙二醛诱导的细胞毒性。在 NO 生成和油红 O 染色方面未观察到明显变化。与甲基乙二醛处理组的肝细胞脂肪变性和核变性相比，PME 处理组的小鼠肝脏 ALP 水平和葡萄糖含量下降，细胞形态完好。

{"title":"Mitigation of methylglyoxal-induced hepatotoxicity by Boerhavia diffusa L. aerial extract: Insights from cellular and animal models","authors":"Debrupa Dutta , Nikita Khandelwal , Ashutosh Behera , Snehal Dongare , Bireswar Bhattacharya , Soumi Sukla","doi":"10.1016/j.prenap.2024.100088","DOIUrl":"10.1016/j.prenap.2024.100088","url":null,"abstract":"<div><h3>Background</h3><p><em>Boerhavia diffusa</em> (Punarnava), is a perennial herb with a long-standing reputation for its antioxidative and anti-inflammatory properties, dating back to ancient times. Methylglyoxal is an advanced glycation end-product, known to be toxic in liver cell line as well as in mice model. Our objective is to illustrate the protective action of punarnava aerial extracts in methylglyoxal-induced hepatotoxicity in cell line and mice model.</p></div><div><h3>Methods</h3><p>Punarnava aerial parts were collected and different solvent extracts were prepared in methanol, dichloromethane and hexane by maceration followed by their LCMS/MS characterization, determination of total phenolic, total flavonoid contents and antioxidant activity by DPPH reagent. Cell viability of the extracts and methylglyoxal was assessed using different cell lines. <em>In vitro</em> protective effect of punarnava methanolic extract (PME) against methylglyoxal was evaluated by cell migration assay, NO and ROS production assays and Oil Red O staining in HepG2 cell line. BALB/c mice were pretreated with Punarnava methanolic extract (200 mg/kg and 400 mg/kg) for seven days followed by 290 mg/kg methylglyoxal administration for 6 hrs to induce hepatotoxicity. Serum glucose, AST, ALT, ALP and GSH level were checked and liver histopathological damages were identified.</p></div><div><h3>Results</h3><p>Among the three Punarnava extracts, PME possessed maximum antioxidant, total phenolic and flavonoid content as well as least cytotoxic to liver cell line. Methylglyoxal showed maximum toxicity in HepG2 cells with IC<sub>50</sub> (50 % inhibitory concentration) 3 µM. PME confers protection against methylglyoxal-induced cytotoxicity by decreasing ROS, promoting cell migration and preventing loss of cell viability. No significant change was observed in NO production and Oil Red O staining. PME-treated mice showed decrease in liver ALP levels and glucose with intact cellular morphology compared to hepatocyte steatosis and nuclear degeneration in methylglyoxal-treated group.</p></div><div><h3>Discussions</h3><p>Indigenous herb Punarnava is effective in protecting liver cells from damage induced by the glycolytic byproduct, methylglyoxal.</p></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100088"},"PeriodicalIF":0.0,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142240894","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}

引用次数: 0

Antiparasitary potential of Sarcomphalus joazeiro (Mart.) Hauenschild (Rhamnaceae) Sarcomphalus joazeiro (Mart.) Hauenschild（鼠李科）的抗寄生虫潜力

Pharmacological Research - Natural Products

Pub Date : 2024-09-12 DOI: 10.1016/j.prenap.2024.100085

Camila Aparecida P. Silva , Nara Juliana S. Araújo , Ana Raquel P. da Silva , Maria do Socorro Costa , Juliete B. Soares , Yedda Maria L.S. de Matos , José Weverton A. Bezerra , Viviane B. da Silva , Erlânio O. de Souza , Maria Celeste V. Gomez , Míriam Rolóm , Cathia Coronel , Jaime Ribeiro-Filho , José Maria Barbosa Filho , Davi Antas e Silva , Lucia Raquel de Lima , Irwin R.A. Menezes , Henrique D.M. Coutinho , Jacqueline C. Andrade-Pinheiro

Leishmaniasis and American trypanosomiasis are part of a set of diseases characterized by the World Health Organization as neglected diseases caused by infectious and parasitic agents in populations in situations of poverty and poor sanitation. Pharmaceutical industries neglect such diseases, which have limited treatments, mainly due to few drug options and significant toxicity. Therefore, it is essential to search for new substances that have the potential to replace these medications. In this context, this study aimed to evaluate the leishmanicidal and trypanocidal activity of the ethanolic extract of the leaves and bark of Sarcomphalus joazeiro (Mart.) Hauenschild. These extracts were prepared by maceration with cold extraction. When carrying out the susceptibility tests, the extracts were tested in four different concentrations against the epimastigote forms of the CL-B5 parasite strains of Trypanosoma cruzi and promastigote forms of Leishmania braziliensis and Leishmania infantum, both tests were carried out "in vitro" in plates 96-well microdilution system, with nifurtimox and metronidazole as reference medicine. The cytotoxicity assay was performed with mammalian fibroblast lines from the NCTC 929 clone. The results indicate that the ethanolic extract of the bark of the stem of S. joazeiro (EBSJ) presented a more significant antiparasitic effect when compared to the ethanolic extract of the leaves of Sarcomphalus joazeiro (ELSJ) particularly against L. braziliensis and L. infantum. Regarding cytotoxicity, EBSJ and ELSJ presented moderate and low degrees, respectively. Based on the data obtained, further investigations into the properties of the bark extract are necessary, mainly due to its leishmanicidal potential.

利什曼病和美洲锥虫病是被世界卫生组织定性为被忽视的疾病的一部分，这些疾病由传染病和寄生虫病引起，多发于贫困和卫生条件差的人群。制药业忽视这类疾病，其主要原因是可供选择的药物很少，而且毒性很大，因此治疗效果有限。因此，必须寻找有可能替代这些药物的新物质。在此背景下，本研究旨在评估 Sarcomphalus joazeiro (Mart.) Hauenschild 树叶和树皮乙醇提取物的杀利什曼和杀锥虫活性。这些提取物是通过浸渍和冷提取制备的。在进行药敏试验时，以四种不同浓度的萃取物对克鲁斯锥虫 CL-B5 寄生虫菌株的表皮原虫型以及巴西利什曼原虫型和婴儿利什曼原虫型进行了试验，这两种试验都是在 96 孔微量稀释系统平板中进行的 "体外 "试验，并以硝呋太尔制霉素和甲硝唑作为参考药物。细胞毒性试验是用 NCTC 929 克隆哺乳动物成纤维细胞系进行的。结果表明，茎皮乙醇提取物（EBSJ）与叶乙醇提取物（ELSJ）相比，具有更显著的抗寄生虫效果，尤其是对巴西蝇和幼蝇。在细胞毒性方面，EBSJ 和 ELSJ 分别表现出中等程度和较低程度。根据所获得的数据，有必要对树皮提取物的特性进行进一步研究，这主要是因为它具有杀利什曼的潜力。

{"title":"Antiparasitary potential of Sarcomphalus joazeiro (Mart.) Hauenschild (Rhamnaceae)","authors":"Camila Aparecida P. Silva , Nara Juliana S. Araújo , Ana Raquel P. da Silva , Maria do Socorro Costa , Juliete B. Soares , Yedda Maria L.S. de Matos , José Weverton A. Bezerra , Viviane B. da Silva , Erlânio O. de Souza , Maria Celeste V. Gomez , Míriam Rolóm , Cathia Coronel , Jaime Ribeiro-Filho , José Maria Barbosa Filho , Davi Antas e Silva , Lucia Raquel de Lima , Irwin R.A. Menezes , Henrique D.M. Coutinho , Jacqueline C. Andrade-Pinheiro","doi":"10.1016/j.prenap.2024.100085","DOIUrl":"10.1016/j.prenap.2024.100085","url":null,"abstract":"<div><p>Leishmaniasis and American trypanosomiasis are part of a set of diseases characterized by the World Health Organization as neglected diseases caused by infectious and parasitic agents in populations in situations of poverty and poor sanitation. Pharmaceutical industries neglect such diseases, which have limited treatments, mainly due to few drug options and significant toxicity. Therefore, it is essential to search for new substances that have the potential to replace these medications. In this context, this study aimed to evaluate the leishmanicidal and trypanocidal activity of the ethanolic extract of the leaves and bark of <em>Sarcomphalus joazeiro</em> (Mart.) Hauenschild. These extracts were prepared by maceration with cold extraction. When carrying out the susceptibility tests, the extracts were tested in four different concentrations against the epimastigote forms of the CL-B5 parasite strains of <em>Trypanosoma cruzi</em> and promastigote forms of <em>Leishmania braziliensis</em> and <em>Leishmania infantum</em>, both tests were carried out \"in vitro\" in plates 96-well microdilution system, with nifurtimox and metronidazole as reference medicine. The cytotoxicity assay was performed with mammalian fibroblast lines from the NCTC 929 clone. The results indicate that the ethanolic extract of the bark of the stem of <em>S. joazeiro</em> (EBSJ) presented a more significant antiparasitic effect when compared to the ethanolic extract of the leaves of <em>Sarcomphalus joazeiro</em> (ELSJ) particularly against <em>L. braziliensis</em> and <em>L. infantum</em>. Regarding cytotoxicity, EBSJ and ELSJ presented moderate and low degrees, respectively. Based on the data obtained, further investigations into the properties of the bark extract are necessary, mainly due to its leishmanicidal potential.</p></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100085"},"PeriodicalIF":0.0,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142240768","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}

引用次数: 0