New insights into the mechanism of action of the anti-inflammatory triterpene lupeol

Abstract

The pentacyclic triterpene lupeol has been studied for its inhibitory effects on murine models of inflammation and peritoneal macrophage functions in-vitro. Lupeol (0.5 and 1 mg/ear) administered topically suppressed the mouse ear oedema induced by 12-0-tetradecanoyl-phorbol acetate (TPA), being less effective on ear oedema induced by arachidonic acid. Quantitation of the neutrophil specific marker myeloperoxidase demonstrated that its topical activity was associated with reduction in cell infiltration into inflamed tissues. When tested in-vitro, lupeol significantly reduced prostaglandin E2 (PGE2) production from A23187-stimulated macrophages, but failed to affect leukotriene C4 release. It was a weak inhibitor of nitrite release, but dose-dependently suppressed PGE2. Cytokine production (tumour necrosis factor-alpha and interleukin-1beta) was inhibited in the range 10-100 microM in lipopolysaccharide-treated macrophages. This study demonstrated that lupeol possessed anti-inflammatory activity which was likely to depend on its ability to prevent the production of some pro-inflammatory mediators.

Anti-Inflammatory and Chemopreventive Effects of Triterpene Cinnamates and Acetates from Shea Fat

“…The inhibitory effects on EBV-EA activation induced by TPA were examined as a preliminary evaluation of the potential antitumor-promoting activities 12,13 for compounds 1a-4a and 1c-4c. The results are shown in Table 1, together with comparable data for retinoic acid, one of the reti- 19 , these compounds may have potential as antitumor agents.…”

“…We have recently determined the contents and composition of triterpene alcohol fractions of the non-saponifinable lipids NSL along with fatty acid composition of the kernel fats n-hexane extracts of the shea tree for 36 nut samples from seven subSaharan countries 10 . Since naturally occurring triterpene alcohols and their derivatives exhibit a variety of biological activities including anti-inflammatory, antitumor, chemopreventive, and antimycobacterial activities [11][12][13][14][15] , we were especially interested to undertake investigation of the trit-erpene ester constituents of shea fat in order to evaluate their further pharmacological potential. We now report, in this paper, the isolation of four triterpene acetates 1a-4a and four triterpene cinnamates 1c-4c from shea fat and the evaluation of their inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate TPA induced inflammation in mice, and on the Epstein-Barr virus early antigen EBV-EA activation induced by TPA.…”

In vitro free radical scavenging activity of Ixora coccinea L

“…Literature reviews about the plant also confirm the presence of terpinoids group. Many naturally occurring triterpinoids exhibited a good antiinflammatory activity have been isolated from various plants (Fernandez et al, 2001;Ismaili et al, 2002). Pentacyclic triterpinoids have a wide spectrum of biological activities and some of them may be useful in medicine.…”

Targeted inhibition of tumor proliferation, survival, and metastasis by pentacyclic triterpenoids: Potential role in prevention and therapy of cancer

“…For example, Lupeol was shown to suppress cisplatin induced NF-jB activation and inhibited the orthotopically implanted head and neck squamous cell carcinoma in nude mice and skin cancer in CD-1 mice [134,135]. Lupeol has been shown to inhibit several pro-inflammatory mediators and oncogenic kinases pathways such as PI3K/AKT dependent pathway [136], and pro-inflammatory molecules such as prostaglandin E2/ TNF-a/IL-1b [137]. In addition, the beneficial and pre-clinical studies using lupeol has been recently reviewed [138].…”