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环境病理学,毒理学和肿瘤学期刊
影响因子: 1.625 5年影响因子: 1.63 SJR: 0.402 SNIP: 0.613 CiteScore™: 2.3

ISSN 打印: 0731-8898
ISSN 在线: 2162-6537

环境病理学,毒理学和肿瘤学期刊

DOI: 10.1615/JEnvironPatholToxicolOncol.2013007125
pages 59-72

Effective melanoma inhibition by synthetic pentacyclic triterpenoid 2-(3-phenylprop-2-en-1-ylidene)-22β-hydroxy-3-oxoolean-12-en-28-oic acid: An in vitro and in vivo study

Navin Kumar Tailor
Department of Pharmacy, Jaypee University of Information Technology, Waknaghat 173234 India
Hong Boon Lee
Cancer Research Initiative Foundation, Drug Discovery Laboratory, 12A Jalan TP5, Taman Perindustrian UEP, 47600 Subang Jaya, Selangor Darul Ehsan Malaysia
Manu Sharma
Department of Pharmacy, Jaypee University of Information Technology, Waknaghat, Himachal Pradesh, India

ABSTRACT

The C-2 arylidene analog (compound 3) of pentacyclic triterpenoid Lantadene A (compound 1) was synthesized and evaluated by the National Cancer Institute, USA, for in vitro cytotoxicity against a panel of melanoma cancer cell lines: LOX IMVI, MALME-3M, M14, MDA-MB-435, SK-MEL-2, SK-MEL-28, SK-MEL-5, UACC-257 UACC-62 and B16F10. Compound 3 showed enhanced cytotoxicity compared with compound 1 and the standard drug cisplatin. At the same time, compound 3 showed selective toxicity toward cancer cells and was inactive (i.e., nontoxic) against normal cells (VERO). Compound 3 induced sub-G1 cell cycle arrest and apoptosis in B16F10 cells by down-regulating NF-κB, c-jun, Bcl-2, and by activating caspase-3 and Bax expression. Compound 3 also demonstrated beneficial effects in a clinically relevant B16F10 allograft mice model, with significant reduction of tumor growth/tumor weight in vivo. Compound 3 improved the survival rate in comparison to the control group and the cisplatin group. At the same time, compound 3 had a better safety profile than cisplatin in terms of hematological parameters and liver enzyme levels.


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