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考布酸的遗传毒性评估,考布酸是一种存在于苦配巴油中的生物活性二萜类化合物。

Genotoxicity evaluation of kaurenoic acid, a bioactive diterpenoid present in Copaiba oil.

作者信息

Cavalcanti B C, Costa-Lotufo L V, Moraes M O, Burbano R R, Silveira E R, Cunha K M A, Rao V S N, Moura D J, Rosa R M, Henriques J A P, Pessoa C

机构信息

Department of Physiology and Pharmacology, Faculty of Medicine, Federal University of Ceará, Fortaleza, CE, Brazil.

出版信息

Food Chem Toxicol. 2006 Mar;44(3):388-92. doi: 10.1016/j.fct.2005.08.011. Epub 2005 Sep 21.

Abstract

Copaiba oil extracted from the Amazon traditional medicinal plant Copaifera langsdorffii is rich in kaurenoic acid (ent-kaur-16-en-19-oic acid), a diterpene that has been shown to exert anti-inflammatory, hypotensive, and diuretic effects in vivo and antimicrobial, smooth muscle relaxant and cytotoxic actions in vitro. This study evaluated its potential genotoxicity against Chinese hamster lung fibroblast (V79) cells in vitro, using the Comet and the micronucleus assays. Kaurenoic acid was tested at concentrations of 2.5, 5,10, 30 and 60 microg/mL. The positive control was the methylmethanesulfonate (MMS). The duration of the treatment of V79 cells with these agents was 3h. The results showed that unlike MMS, kaurenoic acid (2.5, 5, and 10 microg/mL) failed to induce significantly elevated cell DNA damage or the micronucleus frequencies in the studied tests. However, exposure of V79 cells to higher concentrations of kaurenoic acid (30 and 60 microg/mL) caused significant increases in cell damage index and frequency. The data obtained provide support to the view that the diterpene kaurenoic acid induces genotoxicity.

摘要

从亚马逊传统药用植物朗氏南美油楠中提取的古巴香脂油富含贝壳杉烯酸(对映-贝壳杉-16-烯-19-酸),这是一种二萜类化合物,已证明其在体内具有抗炎、降血压和利尿作用,在体外具有抗菌、平滑肌松弛和细胞毒性作用。本研究使用彗星试验和微核试验评估了其对中国仓鼠肺成纤维细胞(V79)的潜在遗传毒性。对贝壳杉烯酸进行了2.5、5、10、30和60μg/mL浓度的测试。阳性对照为甲磺酸甲酯(MMS)。用这些试剂处理V79细胞的持续时间为3小时。结果表明,与MMS不同,贝壳杉烯酸(2.5、5和10μg/mL)在研究的试验中未能显著诱导细胞DNA损伤或微核频率升高。然而,将V79细胞暴露于较高浓度的贝壳杉烯酸(30和60μg/mL)会导致细胞损伤指数和频率显著增加。所获得的数据支持了二萜类化合物贝壳杉烯酸具有遗传毒性这一观点。

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