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Synthesis and antioxidant activity of vitamin C analogs and vitamin E analogs

维生素C类似物和维生素E类似物的合成及其抗氧化活性

基本信息

批准号：
11672217
负责人：
MASHINO Tadahiko
金额：
$ 1.92万
依托单位：
Kyoritsu College of Pharmacy
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
1999
资助国家：
日本
起止时间：
1999 至 2000
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-11672217/
关键词：
Vitamin C Vitamin E Ascorbic acid Tocopherol Antioxidant reductic acid キサンチンオキシダーゼ痛風治療薬

项目摘要

Reactive oxygen species (ROS) and free radicals induce oxidative stress and play the important role in developing and/or progression of human diseases such as cancer. So, antioxidants are expected to be a good lead compounds for medicines. In this study, we developed excellent antioxidants based vitamin C and E.1. Vitamin E analogsWe designed and synthesized benzo[h]chroman compounds (BC) which had benzene ring fused with vitamin E skelton and examined superoxide and OH radical quenching activity by ESR spin-trapping methods. Both activities were higher than that of trolox, which is vitamin E water-soluble analog.2. Vitamin C analogsReductic acid (RA) which has a 2,3-enediol moiety conjugated with a carbonyl group in a five-membered carbon ring was synthesized. RA inhibited xanthine oxidase activity, while ascorbic acid did not.RA quenched free radicals and also decreases active oxygen production. RA is thought to be a more potent inhibitor of active oxygen toxicity than ascorbic acid.Xanthine oxidase produces uric acid, which plays a crucial role in goat. Therefore, xanthine oxidase inhibitor works as a medicine for goat. RA is thought to be a promising inhibitor for oxidative stress and remedy for goat.Our data showed that BC and RA serves as a new starting structure for the design of pharmacologically effective compounds such as cancer.

活性氧（ROS）和自由基诱导氧化应激，并在人类疾病如癌症的发生和/或进展中起重要作用。因此，抗氧化剂有望成为一种良好的药物先导化合物。在这项研究中，我们开发了基于维生素C和E.1的优秀抗氧化剂。设计并合成了苯并[h]色满类化合物（BC），用ESR自旋捕捉法研究了BC对超氧阴离子和OH自由基的猝灭活性。这两种活性均高于维生素E水溶性类似物trolox.维生素C类似物还原酸（RA）是一种在5元碳环上有一个羰基与2，3-烯醇共轭的化合物。RA抑制黄嘌呤氧化酶的活性，而抗坏血酸没有。RA淬灭自由基，并减少活性氧的产生。黄嘌呤氧化酶产生尿酸，尿酸在山羊体内起重要作用。因此，黄嘌呤氧化酶抑制剂可作为山羊的药物。RA被认为是一种很有前途的氧化应激抑制剂和山羊的治疗药物。我们的数据表明，BC和RA是一个新的起始结构，用于设计抗肿瘤的化合物，如癌症。