Tubeimosides在消炎，抗肿瘤和抗肿瘤促进作用中的构效关系。,Acta Pharmacologica Sinica

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Tubeimosides在消炎，抗肿瘤和抗肿瘤促进作用中的构效关系。
Acta Pharmacologica Sinica ( IF 6.9 ) Pub Date : 2001-12-18
T X Yu ₁ , R D Ma , L J Yu

Affiliation

目的研究从山茱Bo中分离得到的块茎苷的抗炎，抗肿瘤和促进肿瘤的构效关系。方法从中草药“土贝母”（Bulbostemma paniculatum（Maxim）Franquet（Cucurbitaceae））的块茎中分离出块茎苷I，II和III，它们具有抗炎，抗肿瘤，抗致瘤活性和急性毒性。在体内进行了研究。结果Tubeimosides I，II和III都是来自同一药用植物的齐墩果烷型三萜皂苷的天然类似物，均具有抗炎，抗肿瘤和抗肿瘤的作用。但是，厚朴素II的抗炎，抗肿瘤和抗肿瘤活性比厚朴素I更强，块茎苷II的急性毒性低于块茎苷I。Tubeimoside III的抗炎，抗肿瘤和抗致瘤活性比tubeimoside II的强，而Tubeimoside III的急性毒性也比tubeimoside II的强。结论块茎苷II的C-16羟基在增强块茎苷II的生物活性和降低其毒性中起重要作用。块茎甙III和II之间B和/或C位置的化学结构差异在增强块茎甙III的生物活性和毒性中起重要作用。因此，在抗结核药I，II和III中，抗结核菌素II可能是最有前途的癌症化学预防和化学治疗药物。杜鹃花苷III的抗肿瘤活性和抗肿瘤活性都比杜鹃花苷II强，并且杜鹃花苷III的急性毒性也比杜鹃花苷II强。结论块茎苷II的C-16羟基在增强块茎苷II的生物活性和降低其毒性中起重要作用。块茎甙III和II之间B和/或C位置的化学结构差异在增强块茎甙III的生物活性和毒性中起重要作用。因此，在抗结核药I，II和III中，抗结核菌素II可能是最有前途的癌症化学预防和化学治疗药物。杜鹃花苷III的抗肿瘤活性和抗肿瘤活性都比杜鹃花苷II强，并且杜鹃花苷III的急性毒性也比杜鹃花苷II强。结论块茎苷II的C-16羟基在增强块茎苷II的生物活性和降低其毒性中起重要作用。块茎甙III和II之间B和/或C位置的化学结构差异在增强块茎甙III的生物活性和毒性中起重要作用。因此，在抗结核药I，II和III中，抗结核菌素II可能是最有前途的癌症化学预防和化学治疗药物。结论块茎苷II的C-16羟基在增强块茎苷II的生物活性和降低其毒性中起重要作用。块茎甙III和II之间B和/或C位置的化学结构差异在增强块茎甙III的生物活性和毒性中起重要作用。因此，在抗结核药I，II和III中，抗结核菌素II可能是最有前途的癌症化学预防和化学治疗药物。结论块茎苷II的C-16羟基在增强块茎苷II的生物活性和降低其毒性中起重要作用。块茎甙III和II之间B和/或C位置的化学结构差异在增强块茎甙III的生物活性和毒性中起重要作用。因此，结核菌素II可能是结核菌素I，II和III中最有前途的癌症化学预防和化学治疗药物。

"点击查看英文标题和摘要"

Structure-activity relationship of tubeimosides in anti-inflammatory, antitumor, and antitumor-promoting effects.

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 Tubeimosides I, 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-promo ting 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 II is lower than that of tubeimoside I; the anti-inflammatory, anti-tumor, and anti-tumorigenic activities of tubeimoside III are stronger than those of tubeimoside II, and the acute toxicity of tubeimoside III is also stronger than that of tubeimoside II. 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 III and II plays an important role in enhancing biological activity and toxicity of tubeimoside III. Therefore tubeimosidre II may be the most promising agent for cancer chemoprevention and chemotherapy among tubeimosides I, II, and III.

更新日期：2019-11-01

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