Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, Institution of South China Sea Ecology and Environmental Engineering , South China Sea Institute of Oceanology, Chinese Academy of Sciences , 164 West Xingang Road , Guangzhou 510301 , China.
University of Chinese Academy of Sciences , Beijing 100049 , China.
Org Lett. 2020 Feb 7;22(3):1062-1066. doi: 10.1021/acs.orglett.9b04597. Epub 2020 Jan 23.
The heterologous expression of the lobophorin biosynthetic gene cluster from marine-derived SCSIO 02999 has led to the discovery of new analogues that carry d-kijanose (or its variants with a 3-amino or hydroxyl group) at C-9. The identification of intermediates resulting from the inactivation of (encoding C-17 kijanosyltransferase) and (encoding C-9 digitoxosyltransferase) demonstrates the substrate flexibility of LobG3 to also accept d-kijanose and its variants. Notably, two lobophorins with d-kijanose at C-9 show improved bioactivities.
海洋来源的 SCSIO 02999 的 lobophorin 生物合成基因簇的异源表达导致了新类似物的发现,这些类似物在 C-9 位带有 d-kijanose(或带有 3-氨基或羟基的变体)。失活 (编码 C-17 kijanosyltransferase)和 (编码 C-9 digitoxosyltransferase)的中间产物的鉴定表明 LobG3 的底物灵活性也可以接受 d-kijanose 及其变体。值得注意的是,两个在 C-9 位带有 d-kijanose 的 lobophorin 表现出改善的生物活性。