2. Academic Validation
  3. Dinghupeptins A-D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces

Dinghupeptins A-D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces

  • J Nat Prod. 2018 Sep 28;81(9):1928-1936. doi: 10.1021/acs.jnatprod.7b01009.
Li Yang 1 2,  Hanxiang Li 1,  Ping Wu 1,  Ahmed Mahal 1,  Jinghua Xue 1,  Liangxiong Xu 1,  Xiaoyi Wei 1
Affiliations

Affiliations

  • 1 Key Laboratory of Plant Resources Conservation and Sustainable Utilization/Guangdong Provincial Key Laboratory of Applied Botany , South China Botanical Garden, Chinese Academy of Sciences , Xingke Road 723 , Tianhe District, Guangzhou 510650 , People's Republic of China.
  • 2 School of Life Sciences , University of Chinese Academy of Sciences , Yuquanlu 19A , Beijing 100049 , People's Republic of China.
PMID: 30222343 DOI: 10.1021/acs.jnatprod.7b01009
Abstract

Four new cyclodepsipeptides, dinghupeptins A-D (1-4), possessing a rare N5-(2-hydroxylethyl)glutamine moiety, were isolated from cultures of the soil-derived Streptomyces sp. SC0581. Their structures were elucidated by spectroscopic and advanced Marfey's amino acid analysis, and their 3D structures were established by theoretical conformational analysis. Compounds 1 and 2, containing a 3-amino-6-hydroxypiperidone unit, displayed selective inhibition of chymotrypsin with IC50 values of 2.1 and 1.1 μM, respectively. Enzyme kinetic analysis and molecular docking experiments revealed they are competitive inhibitors binding to the active site of chymotrypsin.

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