Anti-angiogenesis and immunomodulatory activities of an anti-tumor sesquiterpene bigelovin isolated from Inula helianthus-aquatica
Yue, Grace G. L.1,2; Chan, Ben C. L.1,2; Kwok, Hin-Fai1,2; Wong, Yuk-Lau1,2; Leung, Hoi-Wing1,2; Ji, Chang-Jiu4; Fung, Kwok-Pui1,2,3; Leung, Ping-Chung1,2; Tan, Ning-Hua4; Lau, Clara B. S.1,2
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2013
卷号59页码:243-252
关键词Bigelovin Inula helianthus-aquatica Angiogenesis Zebrafish HMEC-1 Cell adhesion molecules
英文摘要Bigelovin is a sesquiterpene lactone isolated from the plant Inula helianthus-aquatica which was traditionally used in cancer treatment in Yunnan, China. The potent apoptotic activities of bigelovin in human leukemia U937 cells were shown in our previous study. The present study investigated 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. Furthermore, the inhibitory activities of bigelovin on the human endothelial cell adhesion molecules (CAMs) were also examined. Our results showed that the growth of subintestinal vessels of the bigelovin-treated zebrafish embryos was significantly inhibited and the gene expressions in angiogenesis signaling pathways (e.g. Ang2 and Tie2) of the zebrafish were down-regulated after bigelovin treatment. Besides, the proliferation and Th1 cytokines productions (e.g. IFN-gamma, IL-2 and IL-12) were suppressed in bigelovin-treated PBMCs. On the other hand, bigelovin was shown to significantly inhibit the human monocyte adhesion to human endothelial cells and the gene expressions of inflammation-related CAMs (e.g. ICAM-1, VCAM-1 and E-selectin) were significantly down-regulated in bigelovin-treated human endothelial cells. In summary, our data provide the first evidence that bigelovin possesses anti-angiogenic and immunomodulatory activities, suggesting bigelovin may exert multi-target functions against cancer in animal models. (C) 2012 Elsevier Masson SAS. All rights reserved.
WOS标题词Science & Technology ; Life Sciences & Biomedicine
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]RECEPTOR TYROSINE KINASES ; IN-VITRO ; CHRONIC INFLAMMATION ; ZEBRAFISH EMBRYOS ; CANCER ; ANGIOPOIETINS ; GROWTH ; CELLS ; HUVEC ; VEGF
收录类别SCI
语种英语
WOS记录号WOS:000315554100028
内容类型期刊论文
源URL[http://ir.kib.ac.cn/handle/151853/19168]  
专题昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
作者单位1.Chinese Univ Hong Kong, Inst Chinese Med, Shatin, Hong Kong, Peoples R China
2.Chinese Univ Hong Kong, State Key Lab Phytochem & Plant Resources West Ch, Shatin, Hong Kong, Peoples R China
3.Chinese Univ Hong Kong, Sch Biomed Sci, Shatin, Hong Kong, Peoples R China
4.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China
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Yue, Grace G. L.,Chan, Ben C. L.,Kwok, Hin-Fai,et al. Anti-angiogenesis and immunomodulatory activities of an anti-tumor sesquiterpene bigelovin isolated from Inula helianthus-aquatica[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2013,59:243-252.
APA Yue, Grace G. L..,Chan, Ben C. L..,Kwok, Hin-Fai.,Wong, Yuk-Lau.,Leung, Hoi-Wing.,...&Lau, Clara B. S..(2013).Anti-angiogenesis and immunomodulatory activities of an anti-tumor sesquiterpene bigelovin isolated from Inula helianthus-aquatica.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,59,243-252.
MLA Yue, Grace G. L.,et al."Anti-angiogenesis and immunomodulatory activities of an anti-tumor sesquiterpene bigelovin isolated from Inula helianthus-aquatica".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 59(2013):243-252.
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