2. Academic Validation
  3. Clerodane diterpenoids with in-vitro anti-neuroinflammatory activity from the tuberous root of Tinospora sagittata (Menispermaceae)

Clerodane diterpenoids with in-vitro anti-neuroinflammatory activity from the tuberous root of Tinospora sagittata (Menispermaceae)

  • Phytochemistry. 2024 Feb:218:113932. doi: 10.1016/j.phytochem.2023.113932.
Jia-Qi Song 1,  Kai-Cheng Yang 1,  Xian-Zhe Fan 1,  Li Deng 1,  Yang-Li Zhu 1,  Hong Zhou 2,  Ya-Si Huang 2,  Xiang-Qian Kong 3,  Li-Jun Zhang 4,  Hai-Bing Liao 5
Affiliations

Affiliations

  • 1 State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin, 541004, China.
  • 2 Key Laboratory of Basic Pharmacology of Ministry of Education and Joint International Research Laboratory of Ethnomedicine of Ministry of Education, Zunyi Medical University, Zunyi, 563000, China.
  • 3 GuangZhou Institutes of Biomedicine and Health, Chinese Academy of Science, Guangzhou, 510530, China.
  • 4 State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin, 541004, China. Electronic address: [email protected].
  • 5 State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin, 541004, China. Electronic address: [email protected].
PMID: 38056516 DOI: 10.1016/j.phytochem.2023.113932
Abstract

Twenty-six clerodane Diterpenoids have been isolated from T. sagittata, a plant species of traditional Chinese medicine Radix Tinosporae, also named as "Jin Guo Lan". Among them, there are eight previously undescribed clerodane Diterpenoids (tinotanoids A-H: 1-8), and 18 known Diterpenoids (9-26). The absolute configurations of compounds 1, 2, 5, 8, 13, 17 and 20 were determined by single-crystal X-ray diffraction. Compound 1 is the first example of rotameric clerodane diterpenoid with a γ-lactone ring which is constructed between C-11 and C-17; meanwhile, compounds 3 and 4 are two pairs of inseparable epimers. Compounds 2, 12 and 17 demonstrated excellent inhibitory activity on NO production against LPS-stimulated BV-2 cells with IC50 values of 9.56 ± 0.69, 9.11 ± 0.53 and 11.12 ± 0.70 μM, respectively. These activities were significantly higher than that of the positive control minocycline (IC50 = 23.57 ± 0.92 μM). Moreover, compounds 2, 12 and 17 dramatically reduced the LPS-induced upregulation of iNOS and COX-2 expression. Compounds 2 and 12 significantly inhibited the levels of pro-inflammatory cytokines TNF-α, IL-1β and IL-6 that were increased by LPS stimulation.

Keywords

BV-2 cells; COX-2; Clerodane diterpenoids; IL-6; Jin guo lan; Menispermaceae; Tinospora sagittata; iNOS.

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