Hochuli E, Kupfer E, Maurer R, Meister W, Mercadal Y, Schmidt K
Central Research Units, F. Hoffmann-La Roche & Co., Ltd., Basel, Switzerland.
J Antibiot (Tokyo). 1987 Aug;40(8):1086-91. doi: 10.7164/antibiotics.40.1086.
The structure of a new pancreatic lipase inhibitor, lipstatin, produced by Streptomyces toxytricini was determined as (2S,3S,5S,7Z,10Z)-5-[(S)-2-formamido-4-methylpentanoyloxy ]-2-hexyl-3- hydroxy-7,10-hexadecadienoic lactone by spectroscopic and chemical methods. Structurally lipstatin is closely related to the known esterase inhibitor esterastin. It contains a N-formyl-L-leucine side chain instead of the N-acetyl-L-asparagine in esterastin.
通过光谱和化学方法确定了由产毒链霉菌产生的新型胰脂肪酶抑制剂利普司他汀的结构为(2S,3S,5S,7Z,10Z)-5-[(S)-2-甲酰胺基-4-甲基戊酰氧基]-2-己基-3-羟基-7,10-十六碳二烯酸内酯。从结构上看，利普司他汀与已知的酯酶抑制剂酯抑素密切相关。它含有一个N-甲酰基-L-亮氨酸侧链，而不是酯抑素中的N-乙酰基-L-天冬酰胺。
