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| 10mg |
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Purity: ≥98%
Ginsenoside Rh2, a naturally occurring steroid glycoside and an aldose reductase inhibitor, is isolated from the root of ginseng and has a variety of biological effects. Caspase-8 and Caspase-9 activation can be induced by ginsenoside Rh2. Ginsenoside Rh2 induces apoptosis in cancer cells via multiple pathways. In Alzheimer's disease models, it also lowers amyloid-β levels, induces β -cell proliferation, and inhibits osteoclastogenesis by stifling RANKL-induced osteoclast differentiation.
| Targets |
Caspase-8; Caspase-9; Apoptosis
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|---|---|
| ln Vitro |
Ginsenoside Rh2 induces the activation of two initiator caspases, caspase-8 and caspase-9 in human cancer cells. Ginsenoside Rh2 is a promising candidate for the development of anti-tumor medications since it induces cancer cells to die via multiple pathways. Ginsenoside Rh2 initiates p53-dependent Fas expression, which leads to the activation of caspase-8 and p53-independent caspase-9-mediated intrinsic pathway, ultimately leading to cancer cell death. The human tumor cell lines HeLa, SK-HEP-1, SW480, and PC-3 are used to determine Ginsenoside Rh2's cytotoxic activity. SK-HEP-1 and SW480 cells are less sensitive to Ginsenoside Rh2, with IC50 values of 3.15 g/mL and 4.06 μg/mL, respectively, while HeLa cells are significantly inhibited in their ability to divide, with an IC50 value of 2.52 μg/mL. With an IC50 value of 7.85 μg/mL, 3-fold higher than HeLa cells, PC-3 cells are the least susceptible to Ginsenoside Rh2[1].
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| ln Vivo |
Tumor sizes from the three groups that are tumor-bearing are measured 15 days after B16-F10 cells were injected. In comparison to the tumor group, the tumor sizes in the G-L and G-H groups (where G-L and G-H denote a low or high dose of ginsenoside Rh2 injection, respectively) are smaller (P<0.05). The Ginsenoside Rh2 treated groups outlive the tumor group that is not receiving treatment, and the effect is dose-dependent (P<0.05), according to the survival analysis [2].
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| Enzyme Assay |
Ginsenoside Rh2 (7.5 μg/mL) is applied to HeLa, SK-HEP-1, SW480, and PC-3 cells in serum-free media for the indicated times before the cells are harvested. 50 micrograms of cell lysates are incubated with 200 nM Ac-DEVD-AFC, Ac-IETD-AFC, and Ac-LEHD-AFC for 1 hour at 37°C in a reaction buffer containing 20 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM DTT, 0.1% CHAPS, and 10% sucrose. Fluorescence emission at 535 nm and excitation at 405 nm are used to monitor the reaction[1].
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| Cell Assay |
Determination of cell viability is performed by using MTT assay, which is used to calculate the growth inhibition induced by increasing concentrations of drug. In a 96-well plate, 1104 HeLa, SK-HEP-1, SW480, and PC-3 cells that are exponentially growing are seeded in triplicate. Cells are treated with increasing concentrations of ginsenoside Rh2 (1, 2.5, 5, 7.5, and 10 μg/mL) in serum-free media for 48 hours after 24 hours of incubation. Each well receives 20 μL of MTT (5 mg/mL) at the conclusion of the treatment, which is then incubated for an additional 4 hours. The DMSO is used to solubilize the formazan grains produced by viable cells, and an ELISA reader is used to measure the color intensity at 550 nm[1].
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| Animal Protocol |
Mice: In 4 groups of 80 mice each, the Tumor group, G-L group, G-H group, and Control group of male C57BL6 mice (3–4 weeks old) are randomly assigned. A low or high dose of ginsenoside Rh2 is referred to as G-L or G-H. The B16-F10 cell line is administered to the mice in the tumor group, G-L group, and G-H group. These 3 groups develop into cancer-bearing groups. The identical volume of PBS is injected in the control group in place of the drug. In the G-L and G-H groups of mice, ginsenoside Rh2 is injected into the left back. After day 5, the dose for the G-H group is 0.5 mg/kg or 0.2 mg/kg for the G-L group. PBS is injected into the tumor and control groups at the same time points.
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| References |
| Molecular Formula |
C36H62O8
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|---|---|
| Molecular Weight |
622.8727
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| Exact Mass |
622.4445
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| Elemental Analysis |
C, 69.42; H, 10.03; O, 20.55
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| CAS # |
78214-33-2
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| Related CAS # |
78214-33-2
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| Appearance |
Solid powder
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| SMILES |
CC(=CCC[C@@](C)([C@H]1CC[C@@]2([C@@H]1[C@@H](C[C@H]3[C@]2(CC[C@@H]4[C@@]3(CC[C@@H](C4(C)C)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O)C)C)O)C)O)C
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| InChi Key |
CKUVNOCSBYYHIS-IRFFNABBSA-N
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| InChi Code |
InChI=1S/C36H62O8/c1-20(2)10-9-14-36(8,42)21-11-16-35(7)27(21)22(38)18-25-33(5)15-13-26(32(3,4)24(33)12-17-34(25,35)6)44-31-30(41)29(40)28(39)23(19-37)43-31/h10,21-31,37-42H,9,11-19H2,1-8H3/t21-,22+,23+,24-,25+,26-,27-,28+,29-,30+,31-,33-,34+,35+,36-/m0/s1
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| Chemical Name |
(2R,3R,4S,5S,6R)-2-[[(3S,5R,8R,9R,10R,12R,13R,14R,17S)-12-hydroxy-17-[(2S)-2-hydroxy-6-methylhept-5-en-2-yl]-4,4,8,10,14-pentamethyl-2,3,5,6,7,9,11,12,13,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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| Synonyms |
20(S)-Ginsenoside Rh2; 20(S)-Rh2; Ginsenoside-Rh2;AR-1A4936; AR1A4936; AR 1A4936
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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 |
| 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) |
DMSO: 50~100 mg/mL (80.3~160.6 mM)
Ethanol: ~100 mg/mL (~160.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6055 mL | 8.0274 mL | 16.0547 mL | |
| 5 mM | 0.3211 mL | 1.6055 mL | 3.2109 mL | |
| 10 mM | 0.1605 mL | 0.8027 mL | 1.6055 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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