1. Academic Validation
  2. Dolabrane-Type Diterpenoids with Immunosuppressive Activity from Koilodepas hainanense

Dolabrane-Type Diterpenoids with Immunosuppressive Activity from Koilodepas hainanense

  • J Nat Prod. 2022 Jun 24;85(6):1581-1590. doi: 10.1021/acs.jnatprod.2c00204.
Yu Ren 1 2 Xiao Tong 1 2 Ye Zhao 3 2 Shi-Jun He 2 Yao-Yue Fan 2 4 Jian-Min Yue 1 2 4
Affiliations

Affiliations

  • 1 University of Chinese Academy of Science, No. 19A Yuquan Road, Beijing 100049, People's Republic of China.
  • 2 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • 3 School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, People's Republic of China.
  • 4 Research Units of Discovery of New Drug Lead Molecules, Chinese Academy of Medical Sciences, Shanghai 201203, China.
Abstract

Thirteen new dolabrane-type Diterpenoids, koilodenoids A-M (1-13), including a chlorinated congener (2), along with six known analogues, were isolated from Koilodepas hainanense. The structures were determined by analysis of spectroscopic data, ECD spectra, and X-ray crystallographic studies. The absolute configuration of C-15 in the 15,16-diol unit of compounds 4 and 5 was established by using the dimolybdenum tetraacetate [Mo2(AcO)4]-induced ECD method. Compounds 4, 7, 16, 17, and 19 showed moderate to significant immunosuppressive activities against the proliferation of T and B lymphocytes in vitro, with compound 16 being the most potent (IC50 0.86 and 0.29 μM, respectively).

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