The α-Glucosidase Inhibition Activities of Phaeochromycins D and E Isolated from Marine Streptomyces sp. FJ0218.

从海洋链霉菌 FJ0218 中分离得到的 Phaeochromycins D 和 E 的 α-葡萄糖苷酶抑制活性

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作者:Lin Pingfa, Shi Mianmian, Wang Feifei, Lin Yong, Zheng Yongbiao
Marine Streptomyces are an important source of naturally occurring active compounds. Out of 23 marine Streptomyces strains, 1 strain of Streptomyces sp. FJ0218 was selected for its high activity in inhibiting α-glucosidase. Two polyketides, phaeochromycins D (2) and E (1), were isolated from the fermentation broth of this strain using bioactivity-guided column chromatography over RP-18, Sephadex LH-20, and silica gel. Their structures were determined using NMR data, HR-EI-MS, and single-crystal X-ray crystallography. Phaeochromycins D (2) and E (1) exhibited inhibitory activity against α-glucosidase, with IC(50) values of 10 mM and 25 mM, respectively. Lineweaver-Burk plots revealed that phaeochromycin E (1) acts as an uncompetitive inhibitor, while phaeochromycin D (2) acts as a non-competitive inhibitor. These findings suggest that there is potential for the pharmacological regulation of glucose levels through the use of polyketide phaeochromycins, emphasizing their significant impact on glucose management.

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