2. Academic Validation
  3. Hypothemycin-Type Resorcylic Acid Lactones with Immunosuppressive Activities from a Podospora sp

Hypothemycin-Type Resorcylic Acid Lactones with Immunosuppressive Activities from a Podospora sp

  • J Nat Prod. 2021 Feb 26;84(2):483-494. doi: 10.1021/acs.jnatprod.0c01344.
Ying Gao 1,  Fang-Fang Duan 1,  Lin Liu 1,  Xiao-Gang Peng 1,  Xiang-Gao Meng 2,  Han-Li Ruan 1
Affiliations

Affiliations

  • 1 Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, People's Republic of China.
  • 2 College of Chemistry, Central China Normal University, Wuhan 430079, People's Republic of China.
PMID: 33544615 DOI: 10.1021/acs.jnatprod.0c01344
Abstract

Twelve new hypothemycin-type resorcylic acid lactones, three 10-membered (1-3) and nine 14-membered (4-12), together with seven known analogues (13-19), were obtained from the solid rice-based culture of Podospora sp. G214. Their structures were elucidated utilizing spectroscopic analysis, and the absolute configurations were determined by modified Mosher's method, Mo2(OAc)4-induced electronic circular dichroism experiments, and single-crystal X-ray diffraction. Compounds 1, 5, 10, and 12-19 exhibited potent immunosuppressive activities against concanavalin A-induced T cell proliferation with IC50 values ranging from 6.0 to 25.1 μM and lipopolysaccharide-induced B cell proliferation with IC50 values ranging from 6.2 to 29.1 μM. Further studies revealed that 1 induced Apoptosis in activated T cells through the JNK-mediated mitochondrial pathway.

Figures