{"title":"通过溶剂分馏提高Clerodendrum viscosum vent.提取物的抗癌活性：体外和硅学机理研究","authors":"","doi":"10.1016/j.procbio.2024.07.007","DOIUrl":null,"url":null,"abstract":"<div><p><em>Clerodendrum viscosum</em> Vent. is a well-known plant in Indian and Chinese traditional medicine systems. While studies showed its crude leaf extract's cytotoxicity against HT-29 and HeLa cells, various non-bioactive compounds present in crude extracts may influence overall bioactivity. This study aimed to separate the most bioactive fractions from <em>Clerodendrum viscosum</em>’s crude extracts that exhibit anticancer potential against HepG2 cells. Crude extracts were fractionated using a solvent-polarity-based process and their anticancer activity was investigated through in vitro, in silico, and network pharmacology approaches. Nonpolar leaf (CVL<sub>H</sub>) and root (CVR<sub>H</sub>) fractions showed maximum cytotoxicity in HepG2 cells without affecting noncancer-origin WRL68 cells. Both extracts induced oxidative stress, DNA damage, cell cycle arrest, and apoptosis in HepG2 cells, with CVR<sub>H</sub> exhibiting a superior effect. GC-MS analysis identified various anticancer phytochemicals differentially present in CVL<sub>H</sub> and CVR<sub>H</sub>. Network pharmacology with these phytochemicals predicted Bcl-2 as the primary target, while molecular docking confirmed lupeol, stigmasterol, alpha-amyrin, cycloartenol, and calysterol being the top five phytochemicals exhibiting strong binding against Bcl-2, androgen receptor (AR), and epidermal growth factor receptor (EGFR). Western blot confirmed an elevated Bax/Bcl-2 ratio in HepG2 cells by CVL<sub>H</sub> and CVR<sub>H</sub>. In summary, the nonpolar fractions of <em>Clerodendrum viscosum</em> leaf and root crude extracts showed enhanced anticancer activity, suggesting their potential pharmaceutical applications.</p></div>","PeriodicalId":20811,"journal":{"name":"Process Biochemistry","volume":null,"pages":null},"PeriodicalIF":3.7000,"publicationDate":"2024-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Enhancing anticancer activity of Clerodendrum viscosum vent. extracts by solvent fractionation: An in vitro and in silico mechanistic study\",\"authors\":\"\",\"doi\":\"10.1016/j.procbio.2024.07.007\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p><em>Clerodendrum viscosum</em> Vent. is a well-known plant in Indian and Chinese traditional medicine systems. While studies showed its crude leaf extract's cytotoxicity against HT-29 and HeLa cells, various non-bioactive compounds present in crude extracts may influence overall bioactivity. This study aimed to separate the most bioactive fractions from <em>Clerodendrum viscosum</em>’s crude extracts that exhibit anticancer potential against HepG2 cells. Crude extracts were fractionated using a solvent-polarity-based process and their anticancer activity was investigated through in vitro, in silico, and network pharmacology approaches. Nonpolar leaf (CVL<sub>H</sub>) and root (CVR<sub>H</sub>) fractions showed maximum cytotoxicity in HepG2 cells without affecting noncancer-origin WRL68 cells. Both extracts induced oxidative stress, DNA damage, cell cycle arrest, and apoptosis in HepG2 cells, with CVR<sub>H</sub> exhibiting a superior effect. GC-MS analysis identified various anticancer phytochemicals differentially present in CVL<sub>H</sub> and CVR<sub>H</sub>. Network pharmacology with these phytochemicals predicted Bcl-2 as the primary target, while molecular docking confirmed lupeol, stigmasterol, alpha-amyrin, cycloartenol, and calysterol being the top five phytochemicals exhibiting strong binding against Bcl-2, androgen receptor (AR), and epidermal growth factor receptor (EGFR). Western blot confirmed an elevated Bax/Bcl-2 ratio in HepG2 cells by CVL<sub>H</sub> and CVR<sub>H</sub>. In summary, the nonpolar fractions of <em>Clerodendrum viscosum</em> leaf and root crude extracts showed enhanced anticancer activity, suggesting their potential pharmaceutical applications.</p></div>\",\"PeriodicalId\":20811,\"journal\":{\"name\":\"Process Biochemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":3.7000,\"publicationDate\":\"2024-07-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Process Biochemistry\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1359511324002289\",\"RegionNum\":3,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Process Biochemistry","FirstCategoryId":"99","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1359511324002289","RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Enhancing anticancer activity of Clerodendrum viscosum vent. extracts by solvent fractionation: An in vitro and in silico mechanistic study
Clerodendrum viscosum Vent. is a well-known plant in Indian and Chinese traditional medicine systems. While studies showed its crude leaf extract's cytotoxicity against HT-29 and HeLa cells, various non-bioactive compounds present in crude extracts may influence overall bioactivity. This study aimed to separate the most bioactive fractions from Clerodendrum viscosum’s crude extracts that exhibit anticancer potential against HepG2 cells. Crude extracts were fractionated using a solvent-polarity-based process and their anticancer activity was investigated through in vitro, in silico, and network pharmacology approaches. Nonpolar leaf (CVLH) and root (CVRH) fractions showed maximum cytotoxicity in HepG2 cells without affecting noncancer-origin WRL68 cells. Both extracts induced oxidative stress, DNA damage, cell cycle arrest, and apoptosis in HepG2 cells, with CVRH exhibiting a superior effect. GC-MS analysis identified various anticancer phytochemicals differentially present in CVLH and CVRH. Network pharmacology with these phytochemicals predicted Bcl-2 as the primary target, while molecular docking confirmed lupeol, stigmasterol, alpha-amyrin, cycloartenol, and calysterol being the top five phytochemicals exhibiting strong binding against Bcl-2, androgen receptor (AR), and epidermal growth factor receptor (EGFR). Western blot confirmed an elevated Bax/Bcl-2 ratio in HepG2 cells by CVLH and CVRH. In summary, the nonpolar fractions of Clerodendrum viscosum leaf and root crude extracts showed enhanced anticancer activity, suggesting their potential pharmaceutical applications.
期刊介绍：
Process Biochemistry is an application-orientated research journal devoted to reporting advances with originality and novelty, in the science and technology of the processes involving bioactive molecules and living organisms. These processes concern the production of useful metabolites or materials, or the removal of toxic compounds using tools and methods of current biology and engineering. Its main areas of interest include novel bioprocesses and enabling technologies (such as nanobiotechnology, tissue engineering, directed evolution, metabolic engineering, systems biology, and synthetic biology) applicable in food (nutraceutical), healthcare (medical, pharmaceutical, cosmetic), energy (biofuels), environmental, and biorefinery industries and their underlying biological and engineering principles.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
