2. Academic Validation
  3. Precursor-Directed Biosynthesis of Neoantimycin Derivatives with Selective Cytotoxicity

Precursor-Directed Biosynthesis of Neoantimycin Derivatives with Selective Cytotoxicity

  • J Nat Prod. 2024 May 24;87(5):1376-1383. doi: 10.1021/acs.jnatprod.4c00013.
Zhengyuan Li 1,  Ling Chai 2,  Zhenzhou Tang 1,  Hongrui Zhu 3,  Peiying Xue 1,  Fan Sun 3,  Houwen Lin 3,  Yongjun Zhou 3,  Xiao Lin 1
Affiliations

Affiliations

  • 1 Institute of Marine Drugs, Guangxi Key Laboratory of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, People's Republic of China.
  • 2 Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Chinese Medicine and Pharmaceutical Science, Nanning 530022, People's Republic of China.
  • 3 Research Center for Marine Drugs, Department of Pharmacy, Ren Ji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, People's Republic of China.
PMID: 38662398 DOI: 10.1021/acs.jnatprod.4c00013
Abstract

A precursor-directed biosynthesis approach led to the accumulation of seven new neoantimycin derivatives (1-7) from Streptomyces conglobatus RJ2. Structure elucidation was conducted using NMR and HRESIMS analysis, and the absolute configuration was determined by advanced Marfey's method, Mosher's analysis, and ECD analysis. The obtained compounds revealed selective and significant cytotoxicity, specifically against colorectal Cancer cells bearing the K-Ras mutation, with IC50 values ranging from 40 nM to 3.5 μM.

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