鱼腥草内生放线菌Streptomyces sanglieri GZWMJZ-725次级代谢产物及其α-葡萄糖苷酶抑制活性研究  

Secondary metabolites and theirα-glucosidase inhibitory activity from Streptomyces sanglieri GZWMJZ-725,an endophytic actinomyces from Houttuynia cordata Thunb.

作　　者：李明星 王立平 许言超 吴耽 王冬阳 朱伟明 Li Mingxing;Wang Liping;Xu Yanchao;Wu Dan;Wang Dongyang;Zhu Weiming(State Key Laborataory of Functions and Applications of Medicinal Plants,Guizhou Medical University,Guiyang 550014;Natural Products Research Center of Guizhou Province,Guiyang 550014;School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003)

机构地区：[1]省部共建药用植物功效与利用国家重点实验室贵州医科大学,贵阳550014 [2]贵州省天然产物研究中心,贵阳550014 [3]中国海洋大学医药学院,青岛266003

出　　处：《中国抗生素杂志》2025年第2期194-199,共6页Chinese Journal of Antibiotics

基　　金：贵州省“百人领军人才”计划,中国科学院西部青年学者(院外);博士引进启动基金(No.天产自J字[2022]02号)。

摘　　要：目的 对鱼腥草内生链霉菌Streptomyces sanglieri GZWMJZ-725的次级代谢产物及α-葡萄糖苷酶抑制活性进行研究。方法 采用大米固体培养基对菌株进行发酵;采用有机溶剂对发酵产物进行提取;利用正反相柱色谱手段对提取物进行分离纯化;综合运用高分辨质谱、核磁共振波谱、紫外、红外等现代波谱技术对化合物平面结构进行解析;采用计算圆二色谱法确定化合物的立体构型;采用pNPG法测试化合物的α-葡萄糖苷酶抑制活性。结果 从S. sanglieri GZWMJZ-725发酵产物中分离到3个化合物,其中化合物1和2鉴定为新的protoasukamycin类似物,化合物3为protoasukamycin。化合物1~3对α-葡萄糖苷酶的半数抑制浓度(IC50)分别为(10.08±0.09)、(10.71±0.18)和(11.14±0.18)μg/mL,阳性对照阿卡波糖的IC50为(140.78±1.98)μg/mL。结论 鱼腥草内生链霉菌S. sanglieri GZWMJZ-725可产生结构新颖且具有α-葡萄糖苷酶抑制活性的protoasukamycin类化合物。Objective To investigate the secondary metabolites of endophytic Streptomyces sanglieri GZWMJZ-725 from Houttuynia cordata Thunb and theirα-glucosidase inhibition activity.Methods Rice solid culture medium was used to ferment the strains.Organic solvents were used to extract the fermentation products,and the fermentation products were separated and purified using normal and reverse-phase silica gel column chromatography.Modern spectroscopic techniques such as high-resolution mass spectrometry,nuclear magnetic resonance spectroscopy,ultraviolet spectroscopy,and infrared spectroscopy were comprehensively applied to analyze the planar structures of the compounds.Experimental and calculated electronic circular dichroism spectroscopy was employed to determine the stereo-configuration of the compound.The inhibitory activities againstα-glucosidase were assayed by the p-nitrophenyl-β-glucopyranoside method.Results Three compounds were isolated from the fermentation products of S.sanglieri GZWMJZ-725,among which compounds 1 and 2 were identified as new protoasukamycin analogues,while compound 3 was identified as protoasukamycin.Compounds 1~3 showed significant inhibitory activities againstα-glucosidase,with half inhibitory concentration(IC50)values of 10.08±0.09,(10.71±0.18),and(11.14±0.18)μg/mL,respectively.The IC50 value of acarbose was found to be 140.78±1.98μg/mL.Conclusion The endophytic S.sanglieri GZWMJZ-725 isolated from Houttuynia cordata Thunb.can produce structurally novel protoasukamycin analogs withα-glucosidase inhibitory activity.

关 键 词：内生放线菌 次级代谢产物 结构鉴定 Α-葡萄糖苷酶 

分 类 号：R978.1[医药卫生—药品]