丙炔基转移酶
土曲霉
查尔酮
预酸化
阿卡波糖
化学
立体化学
戒指(化学)
酶
生物化学
有机化学
作者
Qianqian Ran,Linlan Tao,Xiang Zhou,Shu‐Ming Li,Chun‐Mao Yuan,Song Yang,Kang Zhou
标识
DOI:10.1021/acs.jafc.2c08743
摘要
Geranylated chalcones mainly exist in plants, and many of them have attracted attention because of their diverse pharmacological and biological activities. Herein, we report geranylation of eight chalcones by the Aspergillus terreus aromatic prenyltransferase AtaPT. Ten new mono-geranylated enzyme products (1G–5G, 6G1, 6G2, 7G, 8G1, and 8G2) were obtained. Most of the products are C-geranylated products with prenyl moieties at ring B. In comparison, plant aromatic prenyltransferases usually catalyze the geranylation at ring A. Therefore, AtaPT can be used complementarily for chalcone geranylation to increase the structural diversity of small molecules. In addition, seven compounds (1G, 3G, 4G, 6G1, 7G, 8G1, and 8G2) exhibited a potential inhibitory effect on α-glucosidase with the IC50 values ranging from 45.59 ± 3.48 to 82.85 ± 2.15 μg/mL. Among them, compound 7G (45.59 ± 3.48 μg/mL) was the most potential α-glucosidase inhibitor, which is about seven times stronger than the positive control acarbose (IC50 = 346.63 ± 15.65 μg/mL).
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