Cancer chemopreventive activity of diversin from Ferula diversivittata in vitro and in vivo
Cancer chemopreventive activity of diversin from Ferula diversivittata in vitro and in vivo
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DOI：
10.1016/j.phymed.2009.05.020
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发表时间：
2010-03-01
期刊：
影响因子：
7.9
通讯作者：
Tokuda, H.
中科院分区：
文献类型：
--
作者：
Iranshahi, M.;Sahebkar, A.;Tokuda, H.
研究了从 Ferula diversivittata 根中分离出的异戊二烯化香豆素 (diversin, 1) 以及四种新型倍半萜内酯 (diversolides A、D、F 和 G, 2-5) 对 12-O-tetradecanoylphorbol-13-acetate (TPA) 诱导的 Epstein-Barr 病毒早期抗原 (EBV-EA) 激活的可能抑制作用。所有测试的化合物均具有抗 EBV-EA 激活的活性。其中 Diversin (IC(50): 7.7) 表现出最强的抑制作用，被选来研究其对 7,12-二甲基苯并[a]蒽 (DMBA) 作为引发剂、TPA 作为促进剂诱导的体内两阶段小鼠皮肤癌发生的影响。用化合物 1 (85 nmol) 与 DMBA/TPA 一起治疗可抑制乳头状瘤形成直至第 7 周，第 20 周时乳头状瘤携带者的百分比约为 93.3%。即使在第 20 周，每只小鼠形成的乳头状瘤平均数量也仅为 5.5 个。本研究结果表明 Diversin 可能作为一种有效的癌症化学预防剂有价值，其效力与姜黄素和姜黄素相当。槲皮素，两种著名的癌症化学预防剂。 (C) 2009 爱思唯尔有限公司。版权所有。
A prenylated coumarin (diversin, 1) together with four new sesquiterpene lactones (diversolides A, D, F and G, 2-5) isolated from the roots of Ferula diversivittata were studied for their possible inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). All of the tested compounds were active against EBV-EA activation. Among these compounds diversin (IC(50): 7.7) exhibited the strongest inhibitory effect and was selected to examine its effects on in vivo two-stage mouse skin carcinogenesis induced by 7,12-dimethylbenz[a]anthracene (DMBA) as initiator and TPA as promoter. Treatment with compound 1 (85 nmol) along with DMBA/TPA inhibited papilloma formation up to week 7 and the percentage of papilloma bearers was approximately 93.3% at week 20. The average number of papillomas formed per mouse was only 5.5 even at week 20. The results of the present investigation indicated that diversin might be valuable as a potent cancer chemopreventive agent and its potency was comparable with those of curcumin and quercetin, two well-known cancer chemopreventive agents. (C) 2009 Elsevier GmbH. All rights reserved.