研究动态
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草豆蔻根中的生物碱及其抗肿瘤活性。

Alkaloids from the roots of Sophora flavescens and their anti-tumor activity.

发表日期:2023 Sep 22
作者: Yang Xu, Xiuli Wang, Kuiru Sa, Hua Li, Lixia Chen
来源: Cellular & Molecular Immunology

摘要:

苦参属于豆科中的苦参属。其根部被作为中药使用。在我们对苦参根部的研究中,发现了3种新的和19种已知的生物碱,其中包括8种阿洛哌啶型和14种马钦型生物碱。这些化合物的平面构型通过光谱数据确定,新化合物1、2和4的绝对构型由吡啶溶剂效应、ECD和斯纳兹克方法分别确定。所有化合物均对MCF-7细胞生长的抑制活性进行了测试,其中化合物12在浓度为20μM、处理24小时后对MCF-7细胞的生长具有一定的抑制效果,抑制率为31.28%。通过靶点筛选和分子对接,人类Rho GTP酶激活蛋白5变体和人类花生四烯酸12-脂氧合酶(12S型)可能是化合物12发挥抗肿瘤活性的重要靶点。版权所有 © 2023,由Elsevier B.V.出版。
Sophora flavescens belongs to Sophora genus of Leguminosae. Its roots are used as a traditional Chinese medicine. In our study on Sophora flavescens roots, 3 new and 19 known alkaloids have been found, including 8 aloperine-type and 14 matrine-type alkaloids. The planar configurations of these compounds were determined by the spectral data, and the absolute configurations of new compounds 1, 2 and 4 were determined by pyridine solvent effect, ECD and snatzke methods, respectively. All compounds were tested for their inhibitory activity on MCF-7 cell growth, and compound 12 exhibited certain inhibitory effects on the growth of MCF-7 cells after 24 h of treatment at a concentration of 20 μM, with inhibition rates of 31.28%. Through target screening and molecular docking, human Rho GTPase activating protein 5 variant and human arachidonate 12-lipoxygenase (12S-type) might be important targets for compound 12 to exert anti-tumor activity.Copyright © 2023. Published by Elsevier B.V.