1. Academic Validation
  2. Cafestol-Type Diterpenoids from the Twigs of Tricalysia fruticosa with Potential Anti-inflammatory Activity

Cafestol-Type Diterpenoids from the Twigs of Tricalysia fruticosa with Potential Anti-inflammatory Activity

  • J Nat Prod. 2015 Jun 26;78(6):1322-9. doi: 10.1021/acs.jnatprod.5b00165.
Chuan-Pu Shen 1 Jian-Guang Luo 1 Ming-Hua Yang 1 Ling-Yi Kong 1
Affiliations

Affiliation

  • 1 State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
Abstract

Eight new cafestol-type Diterpenoids, tricalysins A-H (1-8), along with five known analogues (9-13), were isolated from the twigs of Tricalysia fruticosa. The structures of 1-8 were elucidated by the application of spectroscopic methods. Inhibitory effects of the isolates on nitric oxide (NO) production in lipopolysaccaride-activated RAW 264.7 macrophages were evaluated, and compound 8 exhibited the most potent bioactivity, with an IC50 value of 6.6 ± 0.4 μM. It was shown further that compound 8 inhibits inflammatory responses via suppression of the expression of iNOS and reduction of the production of the pro-inflammatory cytokines IL-6 and TNF-α, resulting from activation of nuclear factor-kappaB (NF-κB) and phosphorylation of MAPKs (ERK, JNK, and p38).

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