Gambogic acid - CAS 2752-65-0
Catalog number:
2752-65-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C38H44O8
Molecular Weight:
628.76
COA:
Inquire
Targets:
Hsp90 | Bcl-2 Family
Description:
Gambogic acid is a natural product inhibitor of Hsp90.
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Brife Description:
Gambogic acid is a natural product inhibitor of Hsp90.
Purity:
>95%
Appearance:
Amorphous orange solid
Synonyms:
β-Guttiferin
Solubility:
DMSO: 25 mg/ml
Storage:
3 years -20oC powder, 6 months-80oC in solvent.
MSDS:
Inquire
Quality Standard:
In-house
Quantity:
Grams-Kilos
InChIKey:
GEZHEQNLKAOMCA-RRZNCOCZSA-N
InChI:
InChI=1S/C38H44O8/c1-20(2)10-9-15-36(8)16-14-24-29(39)28-30(40)26-18-23-19-27-35(6,7)46-37(33(23)41,17-13-22(5)34(42)43)38(26,27)45-32(28)25(31(24)44-36)12-11-21(3)4/h10-11,13-14,16,18,23,27,39H,9,12,15,17,19H2,1-8H3,(H,42,43)/b22-13-/t23-,27+,36-,37+,38-/m1/s1
Canonical SMILES:
CC(=CCCC1(C=CC2=C(O1)C(=C3C(=C2O)C(=O)C4=CC5CC6C4(O3)C(C5=O)(OC6(C)C)CC=C(C)C(=O)O)CC=C(C)C)C)C
1.Protective role of gambogic acid in experimental pulmonary fibrosis in vitro and in vivo.
Qu Y1, Zhang G1, Ji Y1, Zhua H1, Lv C2, Jiang W3. Phytomedicine. 2016 Apr 15;23(4):350-8. doi: 10.1016/j.phymed.2016.01.011. Epub 2016 Feb 9.
BACKGROUND: Idiopathic pulmonary fibrosis (IPF) is a progressive disorder with poor prognosis. The treatment options for IPF are very limited. Gambogic acid (GA) has anticancer effect and anti-proliferative activity which is extracted from a dried yellow resin of the Garcinia hanburyi Hook.f. [Clusiaceae (Guttiferae)] in Southeast Asia. However, the anti-fibrotic activities of GA have not been previously investigated.
2.Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer.
Wang C1, Wang W2, Wang C2, Tang Y2, Tian H3. Oncol Lett. 2015 Oct;10(4):2063-2066. Epub 2015 Aug 12.
Although patients with non-small cell lung cancer (NSCLC) experience an initial response to the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor gefitinib, those individuals with activating mutations in EGFR develop resistance. Gambogic acid (GA), a polyprenylated xanthone, has strong antitumor activities. In the present study, the therapeutic efficacy of gefitinib with GA was evaluated in a gefitinib-resistant NSCLC model. The NCI-H1975 cell line with EGFR-T790M mutation was subcutaneously injected into immunocompromised mice. The mice were randomly assigned to receive treatment with gefitinib, GA, gefitinib plus GA, or vehicle for 4 weeks, then all mice were sacrificed and their tumor tissues were subjected to caspase activity detection and western blot analysis. Gefitinib and GA alone slightly inhibited the tumor growth of NCI-H1975. However, the combined treatment significantly enhanced their antitumor effects, without any marked adverse events.
3.[Sensitization of human colon cancer HT-29 cells to TRAIL-induced apoptosis by gambognic acid].
Ye JL, Yu YJ, Wu AL, Wang DY, Liu YC, Liu YQ. Yao Xue Xue Bao. 2015 Oct;50(10):1252-7.
To investigate the effects of gambognic acid (GA) on TRAIL-induced apoptosis of cancer cells, human colon HT-29 cancer cells were treated with GA to promote apoptosis. Inhibition of the cell proliferation was measured with MTT assay and cell apoptosis was detected with formation of DNA ladders in agarose gel electrophoresis, and activation of caspase activity. The content of cytosolic reactive oxygen species (ROS) was measured with flow cytometry. The activities of Caspase-3, -8, -9 were detected using spectrophotometric assay. The levels of c-FLIP, CHOP, DR4 and DR5 in cells were tested by Western blot. Combination of GA (1 µg · mL(-1)) and TRAIL (40 ng · mL(-1)) significantly reduced proliferation and increased apoptosis of HT-29 cells over those induced by each agent alone. Percentage of apoptotic cells was increased to 45.5%. GA markedly enhanced the intracellular ROS generation. Expression of CHOP, DR4 and DR5 was up-regulated to 7.
4.Gambogic acid induces apoptotic cell death in T98G glioma cells.
Thida M1, Kim DW2, Tran TT3, Pham MQ3, Lee H4, Kim I5, Lee JW6. Bioorg Med Chem Lett. 2016 Feb 1;26(3):1097-101. doi: 10.1016/j.bmcl.2015.11.043. Epub 2015 Nov 14.
Gambogic acid (GA), a natural product with a xanthone structure, has a broad range of anti-proliferative effects on cancer cell lines. We evaluated GA for its cytotoxic effects on T98G glioblastoma cells. GA exhibited potent anti-proliferative activity and induced apoptosis in T98G glioblastoma cells in a dose-dependent manner. Incubation of cells with GA revealed apoptotic features including increased Bax and AIF expression, cytochrome c release, and cleavage of caspase-3, -8, -9, and PARP, while Bcl-2 expression was downregulated. Furthermore, GA induced reactive oxygen species (ROS) generation in T98G cells. Our results indicate that GA increases Bax- and AIF-associated apoptotic signaling in glioblastoma cells.
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CAS 2752-65-0 Gambogic acid

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