王智颖,孙坤来.浒苔来源真菌Aspergillus versicolor ZJOU-SKL-02次级代谢产物及其活性研究[J].中国海洋药物,2020,39(4):16-22. |
浒苔来源真菌Aspergillus versicolor ZJOU-SKL-02次级代谢产物及其活性研究 |
Studies on the Secondary Metabolites of Aspergillus versicolor ZJOU-SKL-02 and Their Activities |
投稿时间:2020-02-19 修订日期:2020-04-27 |
DOI: |
中文关键词: Aspergillus versicolor 次生代谢产物 结构鉴定 抑菌活性 α-葡萄糖苷酶抑制活性 |
English Keywords:Aspergillus versicolor secondary metabolites structural identification antibacterial activity α-glucosidase inhibitory activity |
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中文摘要: |
目的 研究真菌Aspergillus versicolor ZJOU-SKL-02的次级代谢产物及其生物活性。方法 利用硅胶柱色谱、TLC、HPLC等方法对Aspergillus versicolor ZJOU-SKL-02发酵液进行分离纯化;通过ESI-MS、NMR、比旋光、化学合成等手段,并结合文献数据,确定了其产生的化合物结构及绝对构型。对分离得到的化合物进行了抑菌活性和α-葡萄糖苷酶抑制活性的测试。结果 分离得到6个二苯醚类化合物Diorcinol B(1)、Diorcinol C(2)、Diorcinol E(3)、Diorcinol J(4)、Diorcinol(5)和methyl diorcinol-4-carboxylate(6)。其中化合物5对铜绿假单胞菌有较强的抑菌活性,MIC值为4 μg/mL;化合物6显示出对铜绿假单胞菌和光滑念珠菌有较强的抑菌活性,MIC值分别为4和8 μg/mL。化合物3和化合物4具有强的α-葡萄糖苷酶抑制活性,IC50值分别为117.3和237.4 μM,优于阳性对照阿卡波糖的IC50 255.3 μM。结论 以上活性化合物可以为抗生素的发现和糖尿病的预防和治疗用药提供活性先导化合物资源。 |
English Summary: |
Objective To study the secondary metabolites of Aspergillus versicolor ZJOU-SKL-02 and their biological activities. Methods Aspergillus versicolor ZJOU-SKL-02 fermentation broth was separated and purified by silica gel column chromatography, TLC, HPLC, etc .; ESI-MS, NMR, specific rotation, chemical synthesis and other methods were combined with literature data to determine the structure and absolute configuration of the resulting compound. The isolated compounds were tested for antibacterial activity and α-glucosidase inhibitory activity. Results Six diphenyl ether compounds Diorcinol B (1), Diorcinol C (2), Diorcinol E (3), Diorcinol J (4), Diorcinol (5) and methyl diorcinol-4-carboxylate (6) were isolated. . Compound 5 showed strong antibacterial activity against P. aeruginosa with a MIC value of 4 μg / mL; Compound 6 showed strong antibacterial activity against Pseudomonas aeruginosa and Candida glabrata, respectively. 4 and 8 μg / mL. Compounds 3 and 4 had strong α-glucosidase inhibitory activities, with IC50 values of 117.3 and 237.4 μM, respectively, which are better than the IC50 of positive control acarbose 255.3 μM. Conclusion The above active compounds can provide active lead compound resources for the discovery of antibiotics and the prevention and treatment of diabetes. |
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