文献类型：期刊文献

中文题名：土贝母皂苷抗炎、抗肿瘤和抗促瘤的构效关系(英文)

英文题名：Structure-activity relationship of tubeimosides in anti-inflamma-tory, antitumor, and antitumor-promoting effects

作者：于廷曦[1];马润娣[2];于立坚[2]

机构：[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

年份：2001

卷号：22

期号：5

起止页码：83

中文期刊名：Acta Pharmacologica Sinica

外文期刊名：中国药理学报（英文版）

收录：CSTPCD、、北大核心2000、Scopus、CSCD2011_2012、北大核心、CSCD、PubMed

语种：中文

中文关键词：土贝母;土贝母苷类;皂苷类;非甾类消炎药;植物性抗肿瘤药;皮肤肿瘤;毒性;局部投药;构效关系

外文关键词：Bolbostemma paniculatum; tubeimo- sides; saponins; nonsteroidal anti-inflammatory agents; phytogenic antineoplastic agents; skin neoplasms; toxici- ty; topical administration; structure-activity relationship

中文摘要：目的:研究土贝母苷Ⅰ、Ⅱ和Ⅲ的抗炎、抗瘤和抗促瘤效果的构效关系。方法:从中药土贝母中分离土贝母苷Ⅰ、Ⅱ和Ⅲ,并研究它们的抗炎、抗瘤和抗促瘤活性及急性毒性。结果:土贝母苷Ⅰ、Ⅱ和Ⅲ是来自同一植物的齐墩果烷型三萜皂苷天然类似物。实验证实,它们都具有抗炎、抗瘤和抗促瘤效果。然而,土贝母苷Ⅱ的抗炎、抗瘤和抗促瘤效果比土贝母苷Ⅰ强,其急性毒性却比土贝母苷Ⅰ低;土贝母苷Ⅲ的抗炎、抗瘤和抗促瘤效果比土贝母苷Ⅱ高,其急性毒性也比土贝母苷Ⅱ强。结论:土贝母苷Ⅱ16位碳上的羟基对于增强土贝母苷Ⅱ的生物学活性和降低它的毒性具有重要意义;土贝母苷Ⅲ和土贝母苷Ⅱ在B和/或C位上化学结构的差异对于增强土贝母苷Ⅲ的生物活性和毒性起着重要作用。

外文摘要：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 .