世界科学技术-中医药现代化
世界科學技術-中醫藥現代化
세계과학기술-중의약현대화
WORLD SCIENCE AND TECHNOLOGY-MODERNIZATION OF TRADITIONAL CHINESE MEDICINE
2014年
4期
869-875
,共7页
杜洪飞%曾瑶波%张毅%刘晓玲
杜洪飛%曾瑤波%張毅%劉曉玲
두홍비%증요파%장의%류효령
斑蝥素%去甲斑蝥素%Diels-Alder反应%磷酸酯酶抑制活性%结构修饰
斑蝥素%去甲斑蝥素%Diels-Alder反應%燐痠酯酶抑製活性%結構脩飾
반모소%거갑반모소%Diels-Alder반응%린산지매억제활성%결구수식
Cantharidin%norcantharidin%Diels -Alder reaction%phosphatase inhibitory activity%structure modification
本文概述了三大经典代表斑蝥类化合物的来源和物化性质,综述了其合成策略和基本合成路线。随后着重综述了斑蝥素和去甲斑蝥素及其衍生物的基本概况,及其近年来在抗肿瘤方面的研究进展,特别是其与抗癌机理密切相关的特异性结合酶,丝/苏氨酸蛋白磷酸酯酶(PP)中PP1、PP2A和PP2B的抑制活性和选择性的构效关系。总结了斑蝥类新型生物活性小分子的设计和发展方向。
本文概述瞭三大經典代錶斑蝥類化閤物的來源和物化性質,綜述瞭其閤成策略和基本閤成路線。隨後著重綜述瞭斑蝥素和去甲斑蝥素及其衍生物的基本概況,及其近年來在抗腫瘤方麵的研究進展,特彆是其與抗癌機理密切相關的特異性結閤酶,絲/囌氨痠蛋白燐痠酯酶(PP)中PP1、PP2A和PP2B的抑製活性和選擇性的構效關繫。總結瞭斑蝥類新型生物活性小分子的設計和髮展方嚮。
본문개술료삼대경전대표반모류화합물적래원화물화성질,종술료기합성책략화기본합성로선。수후착중종술료반모소화거갑반모소급기연생물적기본개황,급기근년래재항종류방면적연구진전,특별시기여항암궤리밀절상관적특이성결합매,사/소안산단백린산지매(PP)중PP1、PP2A화PP2B적억제활성화선택성적구효관계。총결료반모류신형생물활성소분자적설계화발전방향。
This study was aimed to summarize main-bone structure of cantharidin-based small molecules and facts about three typical candidates including its origin, physical-chemical properties and general synthetic approaches. Basic chemical and pharmacological information as well as development of anti-cancer activities, which were related to cantharidin, norcantharidin and their analogues were reviewed, especially the relationship between the structures and their inhibitory activity and selectivity of serine-threonine protein phosphatases PP1, PP2A and PP2B in cancer treatment. The designs and developments of new biological cantharidin-based small molecules were also reviewed.