[Effects of gambogic acid on the regulation of steroid receptor coactivator-3 in A549 cells].
OBJECTIVE
To investigate the effects of gambogic acid (GA) on the proliferation inhibition and apoptosis induction in Human lung adenocarcinoma A549 cells in vitro, as well as the regulation of steroid receptor coactivator-3 (SRC-3) to explore the relationship between them.


METHODS
The effect of GA on the growth of A549 cells was studied by MTT assay. Apoptosis was detected by Hoechst 33258 staining. The localization of SRC-3 was determined by confocal laser scanning microscopy. Western blot and RT-PCR technique were applied to assess the expression of SRC-3.


RESULTS
GA presented a striking proliferation inhibition potency on A549 cells in vitro, as well as apoptosis induction activity in a time- and dose-dependent manner. The IC(50) value for 24 h was (3.17 +/- 0.13) micromol/L. Overexpression of SRC-3 was found in A549 cells, whereas the SRC-3 protein and mRNA expression levels were significantly downregulated in A549 cells induced by GA in a dose-dependent manner. The location of SRC-3 was situated mainly in the cell nuclei.


CONCLUSIONS
GA exhibits a potent proliferation inhibition and apoptosis induction in human lung adenocarcinoma A549 cells, which might correspond to the downregulation of the expression of SRC-3. Thus, it promises to be a new target drug for lung cancer treatment.
Department of Hematology, Huazhong Science and Technology University, Wuhan 430022, China.
Rui
R
Li
Yan
Y
Chen
Fei
F
Zhao
Yuan
Y
Liu
Lu
L
Wen
Ling-lan
LL
Zeng
D000230:Adenocarcinoma / Q000378:metabolism / Q000473:pathology; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D002467:Cell Nucleus / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation; D006801:Humans; D008175:Lung Neoplasms / Q000378:metabolism / Q000473:pathology; D056921:Nuclear Receptor Coactivator 3 / Q000235:genetics / Q000378:metabolism*; D012333:RNA, Messenger / Q000378:metabolism; D044004:Xanthones / Q000008:administration & dosage / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D012333:RNA, Messenger; D044004:Xanthones; C052659:gambogic acid; C538866:NCOA3 protein, human; D056921:Nuclear Receptor Coactivator 3