癌症预防剂。第8部分：甜菊糖苷及相关化合物的化学预防作用。

Cancer preventive agents. Part 8: Chemopreventive effects of stevioside and related compounds.

作者信息

Takasaki Midori, Konoshima Takao, Kozuka Mutsuo, Tokuda Harukuni, Takayasu Junko, Nishino Hoyoku, Miyakoshi Masazumi, Mizutani Kenji, Lee Kuo-Hsiung

机构信息

Faculty of Pharmaceutical Sciences, Chiba Institute of Science, Choshi, Chiba 288-0025, Japan.

出版信息

Bioorg Med Chem. 2009 Jan 15;17(2):600-5. doi: 10.1016/j.bmc.2008.11.077. Epub 2008 Dec 6.

DOI:10.1016/j.bmc.2008.11.077

PMID:19131254

Abstract

In a search for potential cancer chemopreventive agents from natural resources, stevioside (1), a sweetener, and six related compounds, including two aglycones steviol (6) and isosteviol (7), were screened in an in vitro assay for inhibitory effects on Epstein-Barr virus early antigen activation. Compounds 1, 6 and 7 showed significant activity in this assay and also exhibited strong inhibitory effects in a two-stage carcinogenesis test using mouse skin induced by 7,12-dimethylbenz[a]anthracene (DMBA) and 12-O-tetradecanoylphorbol-13-acetate (TPA). The inhibitory effects of these three compounds were greater than that of glycyrrhizin. Furthermore, these three compounds significantly inhibited mouse skin carcinogenesis initiated by peroxynitrite and promoted by TPA. Their activities were comparable to that of curcumin. These results suggested that 1, as well as 6 and 7, could be valuable as chemopreventive agents for chemical carcinogenesis.

摘要

在从自然资源中寻找潜在的癌症化学预防剂的过程中，对甜味剂甜菊糖苷（1）以及六种相关化合物进行了筛选，其中包括两种苷元甜菊醇（6）和异甜菊醇（7），通过体外试验检测它们对爱泼斯坦 - 巴尔病毒早期抗原激活的抑制作用。化合物1、6和7在该试验中显示出显著活性，并且在使用7,12 - 二甲基苯并[a]蒽（DMBA）和12 - O - 十四烷酰佛波醇 - 13 - 乙酸酯（TPA）诱导的小鼠皮肤两阶段致癌试验中也表现出强烈的抑制作用。这三种化合物的抑制作用大于甘草酸。此外，这三种化合物显著抑制由过氧亚硝酸盐引发并由TPA促进的小鼠皮肤癌发生。它们的活性与姜黄素相当。这些结果表明，1以及6和7作为化学致癌作用的化学预防剂可能具有重要价值。