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狗牙花提取物的细胞毒性、羟基自由基清除及拓扑异构酶抑制活性研究

Studies on cytotoxic, hydroxyl radical scavenging and topoisomerase inhibitory activities of extracts of Tabernaemontana divaricata (L.) R.Br. ex Roem. and Schult.

作者信息

Thind Tarunpreet Singh, Agrawal Satyam Kumar, Saxena A K, Arora Saroj

机构信息

Department of Botanical and Environmental Sciences, Guru Nanak Dev University, Amritsar 143005, Punjab, India.

出版信息

Food Chem Toxicol. 2008 Aug;46(8):2922-7. doi: 10.1016/j.fct.2008.05.036. Epub 2008 Jun 6.

DOI:10.1016/j.fct.2008.05.036
PMID:18577413
Abstract

In the present investigation, the cytotoxic, hydroxyl radical scavenging and topoisomerase inhibition activities of Tabernaemontana divaricata (Apocynaceae) were evaluated. The extracts from leaves of the plant were prepared with different solvents viz. chloroform, methanol, ethyl acetate and hexane. In, in vitro cytotoxicity assay, with cell lines viz HCT-15 (Colon), HT-29 (Colon), 502713 (Colon), MCF-7 (Breast), PC- 3 (Prostrate), it was observed that the ethyl acetate extract was effective against only one colon cell line (502713) at the lowest dose i.e. 10 micro g/ml, whereas the chloroform extract was effective against all the three colon cancer cell lines, at 30 microg/ ml. In order to evaluate the mechanism of cytotoxicity of these extracts, they were assessed for their ability to scavenge hydroxyl radicals in plasmid nicking assay with pBR322. It was observed that all the extracts effectively inhibited the unwinding of supercoiled DNA except hexane extract, which showed the least effect. Since the expression of topo enzymes is linked with cell proliferation so the extracts were also checked for topo I and topo II inhibitory activities. It was noticed that ethyl acetate extract selectively showed inhibition of topo II in topoisomerase II relaxation assay.

摘要

在本研究中,对狗牙花(夹竹桃科)的细胞毒性、羟自由基清除能力和拓扑异构酶抑制活性进行了评估。用不同溶剂即氯仿、甲醇、乙酸乙酯和己烷制备了该植物叶片的提取物。在体外细胞毒性试验中,使用了HCT-15(结肠)、HT-29(结肠)、502713(结肠)、MCF-7(乳腺)、PC-3(前列腺)等细胞系,观察到乙酸乙酯提取物仅在最低剂量即10微克/毫升时对一种结肠癌细胞系(502713)有效,而氯仿提取物在30微克/毫升时对所有三种结肠癌细胞系均有效。为了评估这些提取物的细胞毒性机制,在使用pBR322的质粒切口试验中评估了它们清除羟自由基的能力。观察到除己烷提取物显示出最小作用外,所有提取物均有效抑制了超螺旋DNA的解旋。由于拓扑异构酶的表达与细胞增殖相关,因此还检查了提取物对拓扑异构酶I和拓扑异构酶II的抑制活性。注意到在拓扑异构酶II松弛试验中,乙酸乙酯提取物选择性地显示出对拓扑异构酶II的抑制作用。

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