Planta Med 2012; 78 - PD83
DOI: 10.1055/s-0032-1320441

Anti-angiogenesis and immunomodulatory activities of an anti-tumor sesquiterpene bigelovin

GGL Yue 1, 2, BCL Chan 1, 2, FHF Kwok 1, 2, CJ Ji 4, KP Fung 1, 2, 3, PC Leung 1, 2, NH Tan 4, CBS Lau 1, 2
  • 1Institute of Chinese Medicine
  • 2State Key Laboratory of Phytochemistry and Plant Resources in West China (CUHK)
  • 3School of Biomedical Sciences, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong
  • 4State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China

Bigelovin is a sesquiterpene lactone isolated from the plant Inula helianthus-aquatica which was traditionally used in cancer treatment in Yunnan, China. We previously demonstrated the potent apoptotic activities of bigelovin. The objective of this study was to investigate the anti-angiogenic and immunomodulatory effects of bigelovin using transgenic zebrafish Tg(fli1a:EGFP)y1 with fluorescent blood vessels and human peripheral blood mononuclear cells (PBMCs), respectively. The growth of subintestinal vessels and gene expression in angiogenesis signaling pathways of bigelovin-treated zebrafish embryos were examined. The proliferation and cytokines production of bigelovin-treated PBMCs were also evaluated. Our results showed that bigelovin could significantly inhibit the growth of subintestinal vessels and down-regulate the expression of Ang2 and Tie2 of zebrafish embryos. Besides, bigelovin could significantly suppress the proliferation and production of Th1 cytokines (IFNγ, IL-2 and IL-12) in human PBMCs. This is the first report of the anti-angiogenic and immunomodulatory activities of bigelovin in zebrafish and human lymphocytes. Our findings suggest that bigelovin may exert multi-target function against tumor in animal model.