Abstract
Although anticancer effect of gambogic acid (GA) and its potential mechanisms were well documented in past decades, limited information is available on the anticancer effect of gambogenic acid (GNA), another major active component of Gamboge. Here we performed a study to determine whether GNA possesses anticancer effect and find its potential mechanisms. The results suggested that GNA significantly inhibited the proliferation of several tumor cell lines in vitro and in vivo. Treatment with GNA dose and time dependently induced A549 cells apoptosis, arrested the cells to G0/G1 phase in vitro and down-regulated the expression of cyclin D1 and cyclooxygenase (COX)-2 in mRNA level. In addition, anticancer effect was further demonstrated by applying xenografts in nude mice coupled with the characteristic of apoptosis in the GNA treated group. Taken together, these observations might suggest that GNA inhibits tumor cell proliferation via apoptosis-induction and cell cycle arrest.
MeSH terms
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Adenocarcinoma / drug therapy*
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Adenocarcinoma / pathology
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Animals
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Antineoplastic Agents, Phytogenic / pharmacology*
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Antineoplastic Agents, Phytogenic / therapeutic use
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Apoptosis / drug effects*
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Cell Cycle / drug effects*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cyclin D1 / genetics
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Cyclin D1 / metabolism
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Cyclooxygenase 2 / genetics
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Cyclooxygenase 2 / metabolism
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Dose-Response Relationship, Drug
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Down-Regulation
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Female
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Garcinia / chemistry*
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Gene Expression Regulation
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Humans
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Lung Neoplasms / drug therapy*
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Lung Neoplasms / pathology
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Male
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Mice
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Mice, Inbred BALB C
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Mice, Nude
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Phytotherapy
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Plant Extracts / pharmacology*
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Plant Extracts / therapeutic use
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RNA, Messenger / metabolism
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Resins, Plant
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Terpenes / isolation & purification
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Terpenes / pharmacology
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Terpenes / therapeutic use*
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Xanthenes
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Xanthones / isolation & purification
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Xanthones / pharmacology
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Xanthones / therapeutic use*
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Xenograft Model Antitumor Assays
Substances
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Antineoplastic Agents, Phytogenic
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Plant Extracts
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RNA, Messenger
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Resins, Plant
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Terpenes
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Xanthenes
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Xanthones
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Cyclin D1
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neo-gambogic acid
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Cyclooxygenase 2