title: Antitumor activity of 4-O-(2″-O-acetyl-6″-O-p-coumaroyl-β-D-glucopyranosyl)-p-coumaric acid against lung cancers via mitochondrial-mediated apoptosis.
abstract: This study was aimed to investigate antitumor activity of 4-O-(2″-O-acetyl-6″-O-p-coumaroyl-β-D-glucopyranosyl)-p-coumaric acid (4-ACGC) against lung cancer and its mechanisms. The anti-proliferative effects of 4-ACGC on lung cancer cell lines including A549, NCI-H1299, HCC827 were evaluated by MTT method and the IC50 values were calculated, and subsequently a mice xenograft model of A549 was established to investigate the antitumor effect of 4-ACGC in vivo. Furthermore, the apoptosis of the A549 cells was determined by fluorescence microscope by staining with Hoechst 33324 and flow cytometer by staining with FITC conjugated Annexin V/PI, and the further mechanisms were investigated by Western blotting. Our results demonstrated that 4-ACGC possessed notable anti-tumor activity on lung cancer in vivo and in vitro; the mechanisms were involved in inducing mitochondria-mediated apoptosis via up-regulations of caspase-3, caspase-9, Bad and Bax, and down-regulation of Bcl-2. Collectively, our results indicated that the 4-ACGC could be treated as a new candidate for treatment of lung cancer in the future.
authors.affiliation: College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Peng
authors.affiliation: Academy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou 350108, PR China.
authors.forename: Jian-Guo
authors.initials: JG
authors.lastname: Wu
authors.affiliation: College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China.
authors.forename: Yun-Bin
authors.initials: YB
authors.lastname: Jiang
authors.affiliation: College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China.
authors.forename: Yu-Jie
authors.initials: YJ
authors.lastname: Liu
authors.affiliation: College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China.
authors.forename: Tao
authors.initials: T
authors.lastname: Sun
authors.affiliation: College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China.
authors.forename: Na
authors.initials: N
authors.lastname: Wu
authors.affiliation: College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China. Electronic address: wucjcdtcm@163.com.
authors.forename: Chun-Jie
authors.initials: CJ
authors.lastname: Wu
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D019659:Asteraceae / Q000737:chemistry; D053148:Caspase 3 / Q000378:metabolism; D053453:Caspase 9 / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003373:Coumaric Acids / Q000737:chemistry / Q000494:pharmacology*; D015536:Down-Regulation / Q000187:drug effects; D005960:Glucosides / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008168:Lung / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008928:Mitochondria / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D011422:Propionates; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003373:Coumaric Acids; D005960:Glucosides; D011422:Propionates; D019253:Proto-Oncogene Proteins c-bcl-2; D051028:bcl-2-Associated X Protein; D053148:Caspase 3; D053453:Caspase 9; C495469:p-coumaric acid
keywords: 4-O-(2″-O-acetyl-6″-O-p-coumaroyl-β-d-glucopyranosyl)-p-coumaric acid; A549; Apoptosis; Lung cancers