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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。
Objective: To study the structure-activity relationship of anti-inflammatory, anti-tumor, and anti-tumor effects of flavone glycosides I, II, and III. METHODS: Fritillaria I, II and III were isolated from Fritillaria citri, and their anti-inflammatory, anti-tumor and antitumor activities and acute toxicity were studied. Results: Tetrilobone I, II and III are natural oleanane-type triterpene saponins from the same plant. Experiments confirmed that they all have anti-inflammatory, anti-tumor and anti-tumor effects. However, the anti-inflammatory, anti-tumor, and anti-tumor effects of temelobine II are stronger than that of terpene glucoside I, its acute toxicity is lower than that of temerine I, and its anti-inflammatory and anti-tumor effects The anti-tumor effect is higher than that of lobeglobulin II, and its acute toxicity is also stronger than that of lobebenin II. Conclusion: The hydroxyl group at the 16-position carbon of terpene glucoside II is of great significance for enhancing the biological activity and reducing the toxicity of terpene glucoside II; melphalan III and terpene glycoside II are in the B and/or C position. The difference in chemical structure plays an important role in enhancing the biological activity and toxicity of terpene glycoside III.