Yang, Li and Li, Hanxiang and Wu, Ping and Mahal, Ahmed and Xue, Jinghua and Xu, Liangxiong and Wei, Xiaoyi (2018) Dinghupeptins A–D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces. Journal of Natural Products, 81 (9). pp. 1928-1936. ISSN 1520-6025 (online)
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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.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Cyclodepsipeptides, Dinghupeptins, Streptomyces, Chymotrypsin inhibition, Molecular docking |
| Subjects: | Q Science > QD Chemistry Q Science > QK Botany R Medicine > RM Therapeutics. Pharmacology |
| Divisions: | Department of Medical Biochemical Analysis > Research papers |
| Depositing User: | ePrints Depositor |
| Date Deposited: | 14 Aug 2025 05:56 |
| Last Modified: | 14 Aug 2025 05:56 |
| URI: | https://eprints.cihanuniversity.edu.iq/id/eprint/4748 |
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