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葛根提取物的一部分,富含抗氧化化合物,可缓解去卵巢诱导的大鼠骨质疏松症,并抑制乳腺癌和卵巢癌细胞的生长。

A fraction of Pueraria tuberosa extract, rich in antioxidant compounds, alleviates ovariectomized-induced osteoporosis in rats and inhibits growth of breast and ovarian cancer cells.

机构信息

Institute of Pharmacy, Guru Ghasidas University, Bilaspur, CG, India.

Department of Pharmaceutical & Biomedical Sciences, College of Pharmacy, California Health Sciences University, Clovis, California, United States of America.

出版信息

PLoS One. 2021 Jan 14;16(1):e0240068. doi: 10.1371/journal.pone.0240068. eCollection 2021.

DOI:10.1371/journal.pone.0240068
PMID:33444328
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7808586/
Abstract

Pueraria tuberosa (Roxb. ex Willd.) DC., known as Indian Kudzu belongs to family Fabaceae and it is solicited as "Rasayana" drugs in Ayurveda. In the present study, we analyzed the efficacy of an ethyl acetate fraction from the tuber extract of Pueraria tuberosa (fraction rich in antioxidant compounds, FRAC) against menopausal osteoporosis, and breast and ovarian cancer cells. The FRAC from Pueraria tuberosa was characterized for its phenolic composition (total phenolic and flavonoid amount). Antioxidant property (in vitro assays) of the FRAC was also carried out followed by the analysis of the FRAC for its antiosteoporotic and anticancer potentials. The antiosteoporotic activity of FRAC was investigated in ovariectomy-induced osteoporosis in rats. The cytotoxicity effect was determined in breast and ovarian cancer cells. Gas chromatography/mass spectrometry (GC/MS) analysis of the FRAC was performed to determine its various phytoconstituents. Docking analysis was performed to verify the interaction of bioactive molecules with estrogen receptors (ERs). The FRAC significantly improved various biomechanical and biochemical parameters in a dose-dependent manner in the ovariectomized rats. FRAC also controlled the increased body weight and decreased uterus weight following ovariectomy in rats. Histopathology of the femur demonstrated the restoration of typical bone structure and trabecular width in ovariectomized animals after treatment with FRAC and raloxifene. The FRAC also exhibited in vitro cytotoxicity in the breast (MCF-7 and MDA-MB-231) and ovarian (SKOV-3) cancer cells. Furthermore, genistein and daidzein exhibited a high affinity towards both estrogen receptors (α and β) in the docking study revealing the probable mechanism of the antiosteoporotic activity. GC/MS analysis confirmed the presence of other bioactive molecules such as stigmasterol, β-sitosterol, and stigmasta-3,5-dien-7-one. The FRAC from Pueraria tuberosa has potential for treatment of menopausal osteoporosis. Also, the FRAC possesses anticancer activity.

摘要

野葛(Roxb. ex Willd.)DC.,又称印度葛藤,属于豆科,在阿育吠陀中被视为“延年益寿”药物。在本研究中,我们分析了野葛块根提取物的乙酸乙酯部分(富含抗氧化化合物的部分,FRAC)对绝经后骨质疏松症、乳腺癌和卵巢癌细胞的疗效。对野葛 FRAC 的酚类成分(总酚和类黄酮含量)进行了表征。还进行了 FRAC 的抗氧化特性(体外测定),然后分析了 FRAC 的抗骨质疏松症和抗癌潜力。在去卵巢诱导的骨质疏松症大鼠中研究了 FRAC 的抗骨质疏松症活性。在乳腺癌和卵巢癌细胞中测定细胞毒性作用。对 FRAC 进行气相色谱/质谱(GC/MS)分析,以确定其各种植物成分。进行对接分析以验证生物活性分子与雌激素受体(ERs)的相互作用。FRAC 以剂量依赖性方式显著改善了去卵巢大鼠的各种生物力学和生化参数。FRAC 还控制了去卵巢大鼠体重增加和子宫重量减轻。股骨组织病理学显示,在用 FRAC 和雷洛昔芬治疗后,去卵巢动物的典型骨结构和小梁宽度得到恢复。FRAC 还在体外对乳腺癌(MCF-7 和 MDA-MB-231)和卵巢(SKOV-3)癌细胞具有细胞毒性。此外,在对接研究中,染料木素和大豆苷元对两种雌激素受体(α和β)均表现出高亲和力,揭示了其抗骨质疏松活性的可能机制。GC/MS 分析证实存在其他生物活性分子,如豆甾醇、β-谷甾醇和豆甾烷-3,5-二烯-7-酮。野葛的 FRAC 具有治疗绝经后骨质疏松症的潜力。此外,FRAC 具有抗癌活性。

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