| Size | Price | Stock | Qty |
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| 5g |
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| 10g | |||
| Other Sizes |
Purity: ≥98%
Grape Seed Extract is a natural product isolated from whole grape seeds that have a great concentration of vitamin E, flavonoids, linoleic acid, and OPCs. It has a number of health advantages, including an anti-inflammatory effect. The fat-metabolizing enzymes lipoprotein lipase and pancreatic lipase are inhibited by grape seed extract.
| Targets |
Pancreatic lipase (IC50 = 22 μg/mL for the grape seed extract fraction rich in procyanidins) [2]
- Human colorectal carcinoma cells [3] |
|---|---|
| ln Vitro |
Grape seed extract (25-100 μg/mL; 12-48 hours) inhibits the growth of and causes the death of human colorectal cancer cells[3].
Grape seed extract (25-100 μg/mL; 12-24 hours) modulates the protein levels of molecules that control the cell cycle in HT29 and LoVo cells[3]. Grape seed extract (25-100 μg/mL; 24 hours) causes human colorectal cancer cells to undergo apoptotic cell death[3]. Inhibited pancreatic lipase activity in a concentration-dependent manner; the procyanidin-rich fraction of Grape Seed Extract showed stronger inhibitory effect than the crude extract [2] - Suppressed the proliferation of human colorectal carcinoma cell lines (HT-29, HCT-116, SW480) in a time- and concentration-dependent manner; induced cell cycle arrest at the G0/G1 phase and apoptosis in HT-29 cells; downregulated the expression of cyclin D1, cyclin E, and CDK2, while upregulated p21WAF1/CIP1 and p27KIP1; reduced the activation of PI3K/Akt and MAPK (ERK1/2, p38) signaling pathways [3] |
| ln Vivo |
Grape seed extract (200 mg/kg; i.g.; 5 days/wk; for 8 weeks) inhibits the growth of HT29 colon carcinoma tumor xenografts in athymic nude mice[3].
In tumors, grape seed extract decreases cell proliferation while increasing apoptotic cell death[3]. In tumors, grape seed extract increases poly(ADP-ribose) poly-merase cleavage and Cip1/p21 protein levels[3]. In obese or overweight individuals, daily supplementation with 1000 mg of Grape Seed Extract for 8 weeks significantly decreased serum levels of hs-CRP (a pro-inflammatory marker) and neuropeptide Y (an appetite-stimulating neuropeptide), but did not affect anthropometric measures (body weight, BMI, waist circumference) or appetite scores compared to the placebo group [1] - In nude mice xenografted with HT-29 human colorectal carcinoma cells, oral administration of Grape Seed Extract (200 mg/kg body weight, 5 days/week for 4 weeks) significantly inhibited tumor growth (tumor volume and weight reduced by ~40-50%) without causing obvious toxicity; downregulated the expression of cyclin D1, phosphorylated Akt, and phosphorylated ERK1/2 in tumor tissues [3] |
| Enzyme Assay |
Pancreatic lipase activity assay: The reaction mixture contained lipase enzyme, substrate (p-nitrophenyl butyrate), and various concentrations of Grape Seed Extract or its fractions. After incubation at 37°C for a specified time, the absorbance was measured at 405 nm to determine the enzyme activity; the inhibitory rate was calculated and IC50 value was determined by regression analysis [2]
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| Cell Assay |
Colorectal carcinoma cell proliferation assay: Cells were seeded in 96-well plates and treated with different concentrations of Grape Seed Extract (0-200 μg/mL) for 24, 48, or 72 hours. Cell viability was assessed using the MTT assay, and the proliferation rate was calculated relative to the control group [3]
- Cell cycle and apoptosis analysis: HT-29 cells were treated with Grape Seed Extract (100 μg/mL) for 48 hours. For cell cycle analysis, cells were fixed, stained with propidium iodide, and analyzed by flow cytometry. For apoptosis analysis, cells were stained with Annexin V-FITC and propidium iodide, then detected by flow cytometry [3] - Western blot analysis: HT-29 cells treated with Grape Seed Extract were lysed, and protein extracts were separated by SDS-PAGE, transferred to membranes, and probed with specific antibodies against cyclin D1, cyclin E, CDK2, p21WAF1/CIP1, p27KIP1, PI3K, Akt, ERK1/2, p38, and β-actin (loading control). The bands were visualized using chemiluminescence and quantified by densitometry [3] |
| Animal Protocol |
Athymic male nu/nu mice, with human colon carcinoma HT29 tumor xenograft[3]
200 mg/kg Oral gavage, 5 days/wk, for 8 weeks Nude mice (6-8 weeks old) were subcutaneously inoculated with HT-29 human colorectal carcinoma cells (1×106 cells/mouse) to establish xenograft tumors. When tumors reached ~100 mm3, mice were randomly divided into two groups: control group (oral gavage with vehicle) and Grape Seed Extract group (oral gavage with 200 mg/kg body weight of Grape Seed Extract dissolved in vehicle). Administration was performed 5 days/week for 4 weeks. Tumor volume was measured every 3-4 days, and mice were weighed weekly. At the end of the experiment, mice were euthanized, tumors were excised and weighed, and tumor tissues were collected for histological and molecular analysis [3] |
| Toxicity/Toxicokinetics |
In an 8-week human clinical trial, daily supplementation with 1000 mg of grape seed extract did not cause any serious adverse events; a few subjects reported mild and transient gastrointestinal symptoms (nausea, bloating), with no significant difference between the grape seed extract group and the placebo group [1]
- In a nude mouse xenograft model, oral administration of 200 mg/kg of grape seed extract daily for 4 consecutive weeks did not affect the mice's body weight, food intake, or organ weight (liver, kidney, spleen), and no obvious histological abnormalities were observed in the major organs [3] |
| References | |
| Additional Infomation |
See also: Grape seed extract (note moved to).
Grape seed extract is a natural product rich in proanthocyanidins, which are considered to be the main components responsible for its bioactivity [2, 3]. - In overweight/obese individuals, grape seed extract can reduce the levels of high-sensitivity C-reactive protein (hs-CRP) and neuropeptide Y, suggesting potential anti-inflammatory and appetite-regulating effects, but further research is needed to confirm its role in weight management [1]. - The in vitro and in vivo anti-colorectal cancer effects of grape seed extract are associated with the regulation of cell cycle progression, apoptosis, and key signaling pathways (PI3K/Akt, MAPK), suggesting its potential as an adjunct to the prevention or treatment of colorectal cancer [3]. |
| Molecular Formula |
C₃₀H₁₂O₆
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|---|---|---|
| Molecular Weight |
468.42
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| Exact Mass |
590.178
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| CAS # |
84929-27-1
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| Related CAS # |
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| PubChem CID |
78577443
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| Appearance |
Brown to reddish brown solid
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
43
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| Complexity |
970
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC1=CC(=C(C2=C1C[C@@]([C@H](O2)C3=CC(=C(C=C3)O)O)(C)O)[C@H]4[C@@H]([C@H](OC5=CC(=CC(=C45)O)O)C6=CC(=C(C=C6)O)O)O)O
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| InChi Key |
VWKAFYWVDIOMSL-PMFFMQSYSA-N
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| InChi Code |
InChI=1S/C32H30O11/c1-13-7-22(38)26(30-17(13)12-32(2,41)31(43-30)15-4-6-19(35)21(37)9-15)27-25-23(39)10-16(33)11-24(25)42-29(28(27)40)14-3-5-18(34)20(36)8-14/h3-11,27-29,31,33-41H,12H2,1-2H3/t27-,28-,29+,31+,32+/m0/s1
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| Chemical Name |
(2R,3S,4S)-2-(3,4-dihydroxyphenyl)-4-[(2R,3R)-2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-3,5-dimethyl-2,4-dihydrochromen-8-yl]-3,4-dihydro-2H-chromene-3,5,7-triol
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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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) |
Solubility in Formulation 1: ≥ 0.6 mg/mL (Infinity 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 6.0 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: ≥ 0.6 mg/mL (Infinity 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), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 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 | 2.1348 mL | 10.6742 mL | 21.3484 mL | |
| 5 mM | 0.4270 mL | 2.1348 mL | 4.2697 mL | |
| 10 mM | 0.2135 mL | 1.0674 mL | 2.1348 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03087903 | Active Recruiting |
Dietary Supplement: Grape Seed Extract |
Prostate Cancer | University of Colorado, Denver |
January 18, 2018 | Not Applicable |
| NCT00713167 | Active Recruiting |
Drug: Grape Seed Extract (Vitagrape) Drug: Placebo of Grape Seed Extract |
Hyperlipidemia | Shahid Beheshti University of Medical Sciences |
July 2008 | Phase 2 Phase 3 |
| NCT01185067 | Completed | Drug: grape seed extract | Hypertension Oxidative Stress |
University of Michigan | October 2010 | Phase 1 |
| NCT04136639 | Completed | Other: Miswak Other: fluoride |
Dental Caries | Al-Azhar University | June 1, 2019 | Not Applicable |
| NCT01820299 | Completed | Drug: Grape Seed Extract Drug: Vitamin D |
Solid Cancers | Medical University of South Carolina |
March 2013 | Phase 1 |
Products are for research use only; We do not sell to patients
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