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      Anti-proliferation activity of terpenoids isolated from Euphorbia kansui in human cancer cells and their structure-activity relationship

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          Abstract

          Euphorbia kansui is a commonly used traditional Chinese medicine for the treatment of edema, pleural effusion, and asthma, etc. According to the previous researches, terpenoids in E. kansui possess various biological activities, e.g., anti-virus, anti-allergy, antitumor effects. In this work, twenty five terpenoids were isolated from E. kansui, including thirteen ingenane- and eight jatrophane-type diterpenoids (with two new compounds, kansuinin P and Q) and four triterpenoids. Eighteen of them were analyzed by MTS assay for in vitro anticancer activity in five human cancer cell lines. Structure-activity relationship for 12 ingenane-type diterpenoids in colorectal cancer Colo205 cells were preliminary studied. Significant anti-proliferation activities were observed in human melanoma cells breast cancer MDA-MB-435 cells and Colo205 cells. More than half of the isolated ingenane-type diterpenoids showed inhibitory activities in MDA-MB-435 cells. Eight ingenane- and one jatrophane-type diterpenoids possessed much lower IC 50 values in MDA-MB-435 cells than positive control staurosporine. Preliminary structure-activity relationship analysis showed that substituent on position 20 was important for the activity of ingenane-type diterpenoids in Colo205 cells and substituent on position 3 contributed more significant biological activity of the compounds than that on position 5 in both MDA-MB-435 and Colo205 cells.

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          Antitumor Agents, 119. Kansuiphorins A and B, Two Novel Antileukemic Diterpene Esters from Euphorbia kansui

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            Author and article information

            Journal
            CJNM
            Chinese Journal of Natural Medicines
            Elsevier
            1875-5364
            20 October 2017
            : 15
            : 10
            : 766-774
            Affiliations
            1Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Haike Road 501, Shanghai 201203, China
            Author notes
            *Corresponding author: WU Wan-Ying, E-mail: wanyingwu@ 123456simm.ac.cn ; GUO De-An, E-mail: daguo@ 123456simm.ac.cn

            ΔThese authors contributed to the work equally.

            These authors have no conflict of interest to declare.

            Article
            S1875-5364(17)30108-5
            10.1016/S1875-5364(17)30108-5
            29103462
            Copyright © 2017 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.
            Funding
            Funded by: National Natural Science Foundation of China
            Award ID: 81073026
            This work was supported by the National Natural Science Foundation of China (No. 81073026).

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