title: A potential antitumor ellagitannin, davidiin, inhibited hepatocellular tumor growth by targeting EZH2.
abstract: Hepatocellular carcinoma (HCC) is the fifth most common cancer worldwide and is the third most common cause of cancer-related deaths. Currently available treatment options for HCC patients are scarce resulting in an urgent need to develop a novel effective cure. Polygonum capitatum is a medicinal herb which has been used to treat inflammatory diseases in Miao nationality of China. We recently isolated a pure compound davidiin from P. capitatum extract. Four HCC cell lines were treated with davidiin. Cell viability was recorded by MTT assay. siRNAs targeting enhancer of zeste homolog 2 (EZH2) were applied to modulate the expression of EZH2. Established xenograft mice models of HCC were applied to evaluate the in vivo anticancer activity of davidiin. We investigated the anticancer activity and the underlying mechanism of davidiin. The compound inhibited HCC cell growth and also suppressed tumor growth in xenografted HCC mouse. Such inhibition was facilitated by specifically downregulation on EZH2. The compound possesses anticancer activity both in vitro and in vivo which warrants further clinical investigation as a potential anti-HCC agent.
authors.affiliation: State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, 100050, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.forename: Jingyi
authors.initials: J
authors.lastname: Ma
authors.forename: Sheung Ching
authors.initials: SC
authors.lastname: Chow
authors.forename: Chi Han
authors.initials: CH
authors.lastname: Li
authors.forename: Zhangang
authors.initials: Z
authors.lastname: Xiao
authors.forename: Ru
authors.initials: R
authors.lastname: Feng
authors.forename: Jie
authors.initials: J
authors.lastname: Fu
authors.forename: Yangchao
authors.initials: Y
authors.lastname: Chen
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D006528:Carcinoma, Hepatocellular / Q000235:genetics* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004195:Disease Models, Animal; D019008:Drug Resistance, Neoplasm / Q000235:genetics; D000071221:Enhancer of Zeste Homolog 2 Protein; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects*; D055785:Gene Knockdown Techniques; D006801:Humans; D047348:Hydrolyzable Tannins / Q000737:chemistry / Q000494:pharmacology*; D008113:Liver Neoplasms / Q000235:genetics* / Q000473:pathology; D008297:Male; D051379:Mice; D063151:Polycomb Repressive Complex 2 / Q000235:genetics*; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D013634:Tannins / Q000737:chemistry / Q000494:pharmacology*; D047368:Tumor Burden / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D047348:Hydrolyzable Tannins; D013634:Tannins; C576705:davidiin; C013515:ellagitannin; C498409:EZH2 protein, human; D000071221:Enhancer of Zeste Homolog 2 Protein; D063151:Polycomb Repressive Complex 2; D046988:Proteasome Endopeptidase Complex
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