2. Academic Validation
  3. Rupestonic acids B-G, NO inhibitory sesquiterpenoids from Artemisia rupestris

Rupestonic acids B-G, NO inhibitory sesquiterpenoids from Artemisia rupestris

  • Bioorg Med Chem Lett. 2014 Sep 1;24(17):4318-22. doi: 10.1016/j.bmcl.2014.07.008.
Zhang Chen 1,  Shu Wang 2,  Ke-Wu Zeng 1,  Feng-Xia Cui 3,  Hong-Wei Jin 1,  Xiao-Yu Guo 1,  Yong Jiang 4,  Peng-Fei Tu 5
Affiliations

Affiliations

  • 1 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, PR China.
  • 2 Department of Medicinal Chemistry and Pharmaceutical Analysis, Logistics College of Chinese People's Armed Police Forces, Tianjin 300162, PR China.
  • 3 Key Laboratory of Traditional Chinese Research and Development in Hebei Province, Chengde Medical University, Chengde 067000, PR China.
  • 4 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, PR China. Electronic address: yongjiang@bjmu.edu.cn.
  • 5 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, PR China. Electronic address: pengfeitu@vip.163.com.
PMID: 25127164 DOI: 10.1016/j.bmcl.2014.07.008
Abstract

Six new guaiane sesquiterpenoids, rupestonic acids B-G (1-6), have been isolated from the whole Plants of Artemisia rupestris together with six known compounds (7-12). The structures of the new isolates (1-6) were elucidated on the basis of extensive 1D and 2D NMR analysis, and the absolute configurations were established by electronic circular dichroism (ECD) in combination with density functional theory calculations. In in vitro bioassays, compounds 2 and 6 exhibited significant inhibitory effects on LPS-stimulated NO production in BV-2 microglial cells with IC50 values of 2.6 and 2.2 μM, respectively.

Keywords

Absolute configurations; Artemisia rupestris; NO inhibition; Rupestonic acids B–G; Sesquiterpenoids.

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