文献类型：期刊文章

作　　者：于廷曦[1] 马润娣[2] 于立坚[2]

机构地区：[1]北京医科大学生物化学与分子生物学系,北京中国100083 [2]湛江海洋大学海洋生物研究所海洋药物研究室

出　　处：《Acta Pharmacologica Sinica》

年　　份：2001

卷　　号：22

期　　号：5

起止页码：83-88

语　　种：中文

收录情况：AJ、BDHX、BDHX2000、BIOSISPREVIEWS、CAB、CAS、CSA、CSA-PROQEUST、CSCD、CSCD2011_2012、EBSCO、EMBASE、FSTA、IC、JST、PROQUEST、PUBMED、SCI-EXPANDED(收录号：WOS:000168479200016)、SCIE、SCOPUS、WOS、ZGKJHX、核心刊

摘　　要：AIM: To study structure-activity relationship of tubeimosides isolated from Bolbostemma paniculatum for their anti-inflammatory, antitumor, and antitumor-promoting effects. METHODS: Tubeimosides Ⅰ , Ⅱ , and Ⅲ were isolated from tubers of Bolbostemma paniculatum (Maxim) Franquet ( Cucurbitaceae), a Chinese folk medicine,'Tubeimu', and their anti-inflammatory, anti-tumor, anti-tumorigenic activities, and acute toxicity were studied in vivo. RESULTS: TubeimosidesⅠ , Ⅱ , and Ⅲ are all natural analogues of oleanane type of triterpenoid saponins from the same medicinal plant, and all show anti-inflammatory, antitumor, and antitumor-promoting effects. However, the anti-inflammatory, anti-tumor, and anti-tumorigenic activities of tubeimoside Ⅱ are stronger than those of tubeimoside Ⅰ , and the acute toxicity of tubeimoside n is lower than that of tubeimoside Ⅱ ; the anti-inflammatory, anti-tumor, and anti-tumorigenic activities of tubeimoside Ⅰ are stronger than those of tubeimoside Ⅲ , and the acute toxicity of tubeimoside Ⅱ is also stronger than that of tubeimoside Ⅲ . CONCLUSION: C-16 hydroxyl group of tubeimoside Ⅱ plays an important role in enhancing biological activity of tubeimoside Ⅱ and in decreasing its toxicity. The difference of chemical structure in B and/or C position between tubeimosides Ⅲand Ⅱplays an important role in enhancing biological activity and toxicity oftubeimoside Ⅲ . Therefore tubeimosidre Ⅱ may be the most promising agent for cancer chemoprevention and chemotherapy among tubeimosides Ⅰ , Ⅱ , and Ⅲ .

关 键 词：Bolbostemma paniculatum  tubeimo- sides  SAPONINS nonsteroidal anti-inflammatory agents  phytogenic antineoplastic agents  skin neoplasms  toxici- ty  topical administration  structure-activity relationship  

分 类 号：R285[中药学类]