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目的:研究淡紫青霉菌对纤细薯蓣皂苷的生物转化,分离鉴定转化产物并进行药理活性探讨。方法:使用硅胶柱色谱和半制备液相色谱分离转化产物,依据质谱(MS)、核磁共振(NMR)波谱分析进行结构鉴定,并对产物进行了体外抗炎活性的研究。结果:从转化粗提物中分离得到三个依次脱糖基产物,分别为5R-spirost-5-ene-3-ol-O-β-D-Glucopyranoside-(1→3)-β-D-Glucopyranosyl(1),延龄草苷(2)和薯蓣皂苷元(3),转化率分别为1%,1%,45%;体外抗炎活性研究表明三种转化产物对LPS刺激巨噬细胞分泌NO,IL-6和MCP-1具有不同程度的抑制作用,其抗炎活性随着糖链的逐步水解有所增加,以终产物薯蓣皂苷元的抗炎活性最强。结论:淡紫青霉菌转化纤细薯蓣皂苷得到薯蓣皂苷元的产率较高,糖基的数量对甾体皂苷类化合物抗炎活性有着一定的影响。
OBJECTIVE: To study the bioconversion of silage of Penicillium lippii to the separation and identification of the transformation products and to explore the pharmacological activities. Methods: The products were separated by silica gel column chromatography and semi-preparative liquid chromatography. Their structures were identified by mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy. The anti-inflammatory activity of the product was also studied. Results: Three consecutive deglycosylated products were isolated from the crude extracts, which were 5R-spirost-5-ene-3-ol-O-β-D-Glucopyranoside- Glucopyranosyl (1), Trillium glycoside (2) and Diosgenin (3), the conversion rates were 1%, 1%, 45% respectively. In vitro anti-inflammatory activity studies showed that the three conversion products stimulate LPS to stimulate the secretion of macrophages The anti-inflammatory activity of NO, IL-6 and MCP-1 were inhibited to some extent. The anti-inflammatory activity increased with the gradual hydrolysis of the sugar chain, and the end product diosgenin showed the strongest anti-inflammatory activity. Conclusion: The yield of diosgenin obtained from Penicillium lactiferus transformed with diosgenin is high, and the amount of glycosyl group has certain influence on the anti-inflammatory activity of steroidal saponins.