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Purity: ≥98%
Gambogic Acid (also called Guttatic Acid, Guttic Acid) is a naturally occurring xanthonoid isolated from the brownish or orange resin from Garcinia hanburyi. It is presently undergoing clinical trials in China and may have antitumor properties. Gambogic acid works by competitively inhibiting Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bcl-B, and Mcl-1 with IC50 values of 1.47, 1.21, 2.02, 0.66, 1.06, and 0.79 μM, respectively. Caspases are activated by gambogic acid with an EC50 range of 0.78-1.64 μM. The cytotoxic natural substance GA blocks the ability of several antiapoptotic Bcl-2 family members to suppress the release of apoptogenic proteins from mitochondria by competing for the BH3 peptide binding sites on these proteins. The proliferation of human gastric carcinoma MGC-803 cells was shown to be inhibited by GA in vitro in a dose-dependent manner. The rate of inhibition reached 89.45% after 72 hours of GA 5 mg/ml exposure to the cells.
| Targets |
Bcl-2 (Ki < 0.01 nM)
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| Cell Assay |
MTT assay is used to assess how treatments such as gambogic acid, CDDP alone, or both together, affect in vitro cell viability. In 96-well culture plates, the cells (2×104 cells per mL) are seeded. Following an overnight incubation, gambogic acid is applied to NCI-H460, A549, and NCI-H1299 cells in the following concentrations: 0.125, 0.25, 0.25, 0.5, 1, 2, and 4 μM, 0.44, 0.88, 1.75, 3.5, 7, 10.5 and 14 μM, and 0.44, 0.88, 1.75, 4, 8, 12, and 16 μM respectively. In NSCLC cells, three sequences are tested for the combined treatment: (a) Gambogic Acid followed by CDDP cells are exposed to Gambogic Acid for 48 h, and then after washout of Gambogic Acid, cells are treated with CDDP for an additional 48 h; (b) CDDP followed by Gambogic Acid cells are exposed to CDDP for 48 h, and then after washout of CDDP, cells are treated with Gambogic Acid for an additional 48 h; and (c) concurrent treatment cells are exposed to both Gambogic Acid and ADM for 48 h. The nature of the drug interaction is analysed by using the combination index (CI)[2].
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| Animal Protocol |
Mice: A549 viable cells (5×106/100 μL PBS per mouse) are subcutaneously injected into the right flank of male SCID mice that are 7 to 8 weeks old in order to assess the in vivo antitumor activity of gambogic acid combined with CDDP. The mice are randomly assigned to one of four treatment groups when the tumor volume reaches 100 mm3, including control (saline only, n=5), gambogic acid (3.0 mg/kg every two days, intravenously; n=6), CDDP (4 mg/kg every week, intravenously; n=6), and sequential combination (CDDP treatment one day before gambogic acid treatment, n=6). To help detect any additive effects of combination therapy with platinum-based agents and gambogic acid, CDDP (4 mg/kg, weekly) is typically administered at doses lower than the maximum tolerated dose. Once every two days, a caliper is used to measure the tumor's size. Once every two days, body weight is measured. The tumors are removed after 14 days, and the mice are then put to death. They are then kept at -80°C for future research.
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| References |
| Molecular Formula |
C38H44O8
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| Molecular Weight |
628.75
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| Exact Mass |
628.30362
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| Elemental Analysis |
C, 72.59; H, 7.05; O, 20.36
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| CAS # |
2752-65-0
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| Related CAS # |
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| Appearance |
Yellow solid powder
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| SMILES |
CC(=CCC[C@@]1(C=CC2=C(C3=C(C(=C2O1)CC=C(C)C)O[C@@]45[C@H]6C[C@@H](C=C4C3=O)C(=O)[C@@]5(OC6(C)C)C/C=C(/C)\C(=O)O)O)C)C
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| InChi Key |
GEZHEQNLKAOMCA-RRZNCOCZSA-N
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| InChi Code |
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
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| Chemical Name |
(Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
2% DMSO+40% PEG 300+2% Tween 80+ddH2O: 4mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5905 mL | 7.9523 mL | 15.9046 mL | |
| 5 mM | 0.3181 mL | 1.5905 mL | 3.1809 mL | |
| 10 mM | 0.1590 mL | 0.7952 mL | 1.5905 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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