2. Academic Validation
  3. Structurally Diverse Diterpenoids from Isodon scoparius and Their Bioactivity

Structurally Diverse Diterpenoids from Isodon scoparius and Their Bioactivity

  • J Nat Prod. 2017 Jul 28;80(7):2026-2036. doi: 10.1021/acs.jnatprod.7b00163.
Hua-Yi Jiang 1 2 3,  Wei-Guang Wang 1,  Jian-Wei Tang 1,  Miao Liu 1,  Xing-Ren Li 1,  Kun Hu 1,  Xue Du 1,  Xiao-Nian Li 1,  Hong-Bin Zhang 3,  Jian-Xin Pu 1,  Han-Dong Sun 1
Affiliations

Affiliations

  • 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, and Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming Institute of Botany, Chinese Academy of Sciences , Kunming 650201, People's Republic of China.
  • 2 University of Chinese Academy of Sciences , Beijing 100049, People's Republic of China.
  • 3 Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University , Kunming 650091, People's Republic of China.
PMID: 28654256 DOI: 10.1021/acs.jnatprod.7b00163
Abstract

Fourteen new Diterpenoids (1-14) based on four skeletal types and two known analogues (15 and 16) were isolated from the aerial parts of Isodon scoparius. Compound 2 is the first ent-kaurane diterpenoid featuring a 1,11-ether bridge, and the structures of these new compounds were established mainly by NMR and MS methods. The absolute configurations of 1 and 5 and the relative configuration of 3 were determined using single-crystal X-ray diffraction. The absolute configuration of 14 was determined by comparison of the experimental and calculated electronic circular dichroism spectra. Compounds 1, 4, and 15 were active against five human tumor cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW-480), and they also inhibited NO production in LPS-stimulated RAW264.7 cells, with IC50 values of 1.0, 3.1, and 1.8 μM, respectively.

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