title: Oblongifolin C and guttiferone K extracted from Garcinia yunnanensis fruit synergistically induce apoptosis in human colorectal cancer cells in vitro.
abstract: Oblongifolin C (OC) and guttiferone K (GUTK) are two anticancer compounds extracted from Garcinia yunnanensis Hu, but they act by different mechanisms. In this study we investigated whether a combination of OC and GUTK (1:1 molar ratio) could produce synergistic anticancer effects against human colorectal cancer cells in vitro. For comparison, we also examined the anticancer efficacy of ethanol extracts from G yunnanensis fruit, which contain OC and GUTK up to 5%. Compared to OC and GUTK alone, the combination of OC and GUTK as well as the ethanol extracts more potently inhibited the cancer cell growth with IC50values of 3.4 μmol/L and 3.85 μg/mL, respectively. Furthermore, OC and GUTK displayed synergistic inhibition on HCT116 cells: co-treatment with OC and GUTK induced more prominent apoptosis than treatment with either drug alone. Moreover, the combination of OC and GUTK markedly increased cleavage of casapse-3 and PARP, and enhanced cellular ROS production and increased JNK protein phosphorylation. In addition, the combination of OC and GUTK exerted stronger effects under nutrient-deprived conditions than in complete medium, suggesting that autophagy played an essential role in regulating OC- and GUTK-mediated cell death. OC and GUTK are the main components that contribute to the anticancer activity of G yunnanensis and the compounds have apoptosis-inducing effects in HCT116 cells in vitro.
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Xiao-Xiao
authors.initials: XX
authors.lastname: Meng
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Li
authors.initials: L
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Bao-Jun
authors.initials: BJ
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Xin-Yu
authors.initials: XY
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Wen-Wei
authors.initials: WW
authors.lastname: Fu
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Hong-Sheng
authors.initials: HS
authors.lastname: Tan
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Yuan-Zhi
authors.initials: YZ
authors.lastname: Lao
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.|Engineering Research Center of Shanghai Colleges for TCM New Drug Discovery, Shanghai 201203, China.
authors.forename: Hong-Xi
authors.initials: HX
authors.lastname: Xu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D001577:Benzophenones / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004357:Drug Synergism; D005638:Fruit / Q000737:chemistry; D029760:Garcinia / Q000737:chemistry*; D006801:Humans; D048031:JNK Mitogen-Activated Protein Kinases / Q000378:metabolism; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D013729:Terpenes / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D001577:Benzophenones; D010936:Plant Extracts; D013729:Terpenes; C519762:guttiferone K; C575447:oblongifolin C; D048031:JNK Mitogen-Activated Protein Kinases