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来自海洋来源真菌黄曲霉HN4-13的α-葡萄糖苷酶抑制剂

α-Glucosidase Inhibitors from the Marine-Derived Fungus Aspergillus flavipes HN4-13.

作者信息

Wang Cong, Guo Lei, Hao Jiejie, Wang Liping, Zhu Weiming

机构信息

Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China , Qingdao 266003, People's Republic of China.

Jiangsu Marine Resources Development Research Institute, School of Marine Life and Fisheries, Huaihai Institute of Technology , Lianyungang 222004, People's Republic of China.

出版信息

J Nat Prod. 2016 Nov 23;79(11):2977-2981. doi: 10.1021/acs.jnatprod.6b00766. Epub 2016 Nov 14.

Abstract

Three new butenolide derivatives, flavipesolides A-C (1-3), along with 13 known compounds (4-13, aspulvinone Q, monochlorosulochrin, and dihydrogeodin), were isolated from the marine-derived Aspergillus flavipes HN4-13 from a Lianyungang coastal sediment sample. The structures were elucidated by spectroscopic evidence. Compounds 4-6 and 9 were noncompetitive α-glucosidase inhibitors with K/IC values of 0.43/34, 2.1/37, 0.79/19, and 2.8/90 μM, respectively. Compounds 1-3, 8, 10, and 13 are mixed α-glucosidase inhibitors with K/IC values of (2.5, 19)/44, (3.4, 14)/57, (9.2, 4.7)/95, (6.3, 5.5)/55, (1.4, 0.60)/9.9, and (2.5, 7.2)/33 μM, respectively (IC 101 μM for acarbose and 79 μM for 1-deoxynojirimycin).

摘要

从连云港沿海沉积物样本中分离得到的海洋来源黄柄曲霉HN4-13中,鉴定出三种新的丁烯内酯衍生物,即黄柄曲霉内酯A-C(1-3),以及13种已知化合物(4-13,曲霉醌、一氯苏罗克菌素和二氢戈地因)。通过光谱数据对其结构进行了鉴定。化合物4-6和9为非竞争性α-葡萄糖苷酶抑制剂,其K/IC值分别为0.43/34、2.1/37、0.79/19和2.8/90 μM。化合物1-3、8、10和13为混合型α-葡萄糖苷酶抑制剂,其K/IC值分别为(2.5, 19)/44、(3.4, 14)/57、(9.2, 4.7)/95、(6.3, 5.5)/55、(1.4, 0.60)/9.9和(2.5, 7.2)/33 μM(阿卡波糖的IC为101 μM,1-脱氧野尻霉素的IC为79 μM)。

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