title: Studies on anti-hepatoma activity of Annona squamosa L. pericarp extract.
abstract: This study investigated the anti-hepatoma activity of different extracts from A. squamosa pericarps, phytochemistry of the ethyl acetate (EtOAc) fraction and possible anti-hepatoma mechanism of active constituents. The anti-hepatoma activity of different extracts from A. squamosa pericarps were evaluated by MTT assay against SMMC-7721 cells in vitro and verified by using H22xenografts bearing mice. Phytochemical investigation of the active pericarp extract was carried out. The pro-apoptosis and cycle arrest effects of active constituents were observed by fluorescent microscope and flow cytometry. Western blot assay was conducted to find the possible anti-hepatoma mechanisms of active constituents. The result showed that EtOAc extract was the active fraction. Two ent-kaurane diterpenoids, named ent-kauran-16-en-19-oic acid and ent-kauran-15-en-19-oic acid, were isolated from the active EtOAc fraction. The pro-apoptosis and G1 phase arrest effects of these diterpenoids were found. Western blot assay showed that ent-kauran-16-en-19-oic acid could activate caspase-3,-8,-9, up-regulate of Bax and down-regulate of Bcl-2.
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Ya-Yun
authors.initials: YY
authors.lastname: Chen
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Yu-Zhu
authors.initials: YZ
authors.lastname: Cao
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Fu-Qiang
authors.initials: FQ
authors.lastname: Li
authors.affiliation: Nanjing University of Chinese Medicine Hanlin College, Taizhou 225300, China.
authors.forename: Xiao-Li
authors.initials: XL
authors.lastname: Zhu
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Chen-Xiao
authors.initials: CX
authors.lastname: Peng
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Jia-Hui
authors.initials: JH
authors.lastname: Lu
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Jian-Wei
authors.initials: JW
authors.lastname: Chen
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China. Electronic address: lixiang_8182@163.com.
authors.forename: Xiang
authors.initials: X
authors.lastname: Li
authors.affiliation: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China. Electronic address: achenyon@gmail.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Chen
mesh_terms: D000818:Animals; D031041:Annona / Q000737:chemistry*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D045786:Diterpenes, Kaurane / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D008099:Liver / Q000187:drug effects* / Q000473:pathology; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000473:pathology; D051379:Mice
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D045786:Diterpenes, Kaurane
keywords: Annona squamosa; Anti-hepatoma; Diterpenoid; Mechanism