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基于结构的生物活性天然产物 rhizonin A 和 ternatin 的杂交,导致了一种针对 3T3-L1 脂肪细胞的选择性脂肪积累抑制剂。

Structure-based hybridization of the bioactive natural products rhizonin A and ternatin leading to a selective fat-accumulation inhibitor against 3T3-L1 adipocytes.

机构信息

Department of Chemistry, Graduate School of Science, Nagoya University, Furo-cho, Chikusa, Nagoya 464-8602, Japan.

出版信息

Bioorg Med Chem Lett. 2009 Feb 1;19(3):867-9. doi: 10.1016/j.bmcl.2008.11.109. Epub 2008 Dec 6.

Abstract

Based on the structural similarity between the naturally occurring cyclic heptapeptides rhizonin A and ternatin, two novel analogues were designed. The synthetic analogues were assessed with regard to their fat-accumulation inhibitory effect against 3T3-L1 adipocytes, and this led to the discovery of a potent and selective fat-accumulation inhibitor compared to the parent compound rhizonin A.

摘要

基于天然存在的环状七肽 rhizonin A 和 ternatin 之间的结构相似性,设计了两种新型类似物。评估了合成类似物对 3T3-L1 脂肪细胞的脂肪积累抑制作用,与母体化合物 rhizonin A 相比,发现了一种强效且选择性的脂肪积累抑制剂。

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