2. Academic Validation
  3. Asymmetric total synthesis and antifibrotic agents evaluation of fornicin A and its derivatives

Asymmetric total synthesis and antifibrotic agents evaluation of fornicin A and its derivatives

  • Bioorg Med Chem. 2025 Sep 24:131:118413. doi: 10.1016/j.bmc.2025.118413.
Muralikrishna Katta 1,  Sheng-Hong Li 1,  Danling Huang 1,  Yong-Xian Cheng 2
Affiliations

Affiliations

  • 1 Guangdong Provincial Key Laboratory of Chinese Medicine Ingredients and Gut Microbiomics Institute for Inheritance-Based Innovation of Chinese Medicine, Marshall Laboratory of Biomedical Engineering, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, Shenzhen 518060, China; Guangdong Key Laboratory for Biomedical Measurements and Ultrasound Imaging, School of Biomedical Engineering, Shenzhen University Medical School, Shenzhen 518060, China.
  • 2 Guangdong Provincial Key Laboratory of Chinese Medicine Ingredients and Gut Microbiomics Institute for Inheritance-Based Innovation of Chinese Medicine, Marshall Laboratory of Biomedical Engineering, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, Shenzhen 518060, China; Guangdong Key Laboratory for Biomedical Measurements and Ultrasound Imaging, School of Biomedical Engineering, Shenzhen University Medical School, Shenzhen 518060, China. Electronic address: yxcheng@szu.edu.cn.
PMID: 41066959 DOI: 10.1016/j.bmc.2025.118413
Abstract

A concise, efficient enantioselective total synthesis of (-) - fornicin A and derivatives were achieved and this route provides practical access derivatives as a general method for constructing γ-butenolide skeleton. The originally proposed approach employed by Sharpless dihydroxylation, Heck coupling, alkylation and Corey-Winter reductive olefination. This strategy achieved enantioselective syntheses of Fornicin A within five steps and in 17%, overall yield. Furthermore, a Wittig reaction produced stable derivatives and evaluated for their anti-fibrotic activities, in which FA7-9 & FA11 possessed potent anti-fibrotic activity by inhibiting the expression of fibronectin, Collagen I, and α-SMA.

Keywords

Antifibrotic agents; Enantioselectivity; Ganoderma; Meroterpenoids; γ-butenolide.

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