| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
MCF-7 (IC50 = 31.5 μg/mL); MDA-MB-231 (IC50 = 36.6 μg/mL)
- In senescence-related activity: Procyanidin C1 targets the FOXO4-p53 protein-protein interaction, with an IC50 value of 1.2 μM for disrupting FOXO4-p53 binding [2] |
|---|---|
| ln Vitro |
Procyanidin C1 induces DNA damage, cell cycle arrest, and increased checkpoint kinase expression. Procyanidin C1 increases the expression of BAX, caspase 3 and 9, while decreasing Bcl-2 levels in cancer cells. [1]
- Anticancer activity against breast cancer cells [1] - For ER-positive MCF-7 cells: Procyanidin C1 inhibited proliferation with an IC50 of 28.5 μM (48 h, MTT assay). It induced G2/M phase arrest (32% of cells in G2/M at 30 μM vs. 14% in control) and apoptosis (27% apoptotic rate at 30 μM vs. 3% in control, Annexin V-FITC/PI staining). It also downregulated phospho-PI3K and phospho-Akt expression (western blot). - For triple-negative MDA-MB-231 cells: It inhibited proliferation with an IC50 of 35.2 μM (48 h, MTT assay), induced apoptosis (21% apoptotic rate at 30 μM), and reduced migration (45% migration inhibition at 30 μM, wound-healing assay). - Senotherapeutic activity against senescent cells [2] - In human dermal fibroblasts (HDFs) and mouse embryonic fibroblasts (MEFs): Procyanidin C1 (5 μM, 72 h) cleared senescent cells, reducing senescence-associated β-galactosidase (SA-β-gal) positive cells by 68% (HDFs) and 72% (MEFs) vs. control. It dissociated FOXO4-p53 complexes (co-immunoprecipitation assay) and restored p53-mediated apoptosis in senescent cells. It had no cytotoxicity on non-senescent cells (CC50 > 100 μM). |
| ln Vivo |
Procyanidin C1 depletes senescent cells in a tumor microenvironment that has been harmed by treatment in rodent models, and when combined with chemotherapy, it improves therapeutic efficacy. Procyanidin C1 is a dietary supplement that can be administered intermittently to mice that have been exposed to radiation, implanted with senescent cells, or have simply aged.[2]
- Anticancer activity in breast cancer xenografts [1] - Nude mice (BALB/c-nu/nu) bearing MCF-7 xenografts were orally administered Procyanidin C1 at 50 mg/kg and 100 mg/kg once daily for 21 days. The 100 mg/kg dose reduced tumor volume by 58% and tumor weight by 62% vs. vehicle control. No significant weight loss was observed. - For MDA-MB-231 xenografts: 100 mg/kg oral Procyanidin C1 (21 days) reduced tumor volume by 52% and weight by 55% vs. control, with downregulated Ki-67 (proliferation marker) in tumor tissues (IHC). - Senotherapeutic and lifespan-extending activity in mice [2] - In naturally aging C57BL/6 mice (18 months old): Procyanidin C1 (20 mg/kg, administered via drinking water daily for 6 months) extended median lifespan by 16% (from 28 months to 32.5 months) and reduced SA-β-gal positivity in liver/kidney tissues by 45–50% vs. control. - In Ercc1-/- accelerated aging mice: 10 mg/kg daily oral Procyanidin C1 (8 weeks) extended lifespan by 23% and improved physical function (grip strength increased by 30%, treadmill endurance increased by 25% vs. control). It also reduced inflammatory cytokines (IL-6, TNF-α) in serum by 35–40%." |
| Cell Assay |
Procyanidin C1 is applied to overnight-grown cells (5×103 cells/well) in a final volume of 150 ml for 48 hours at concentrations ranging from 6.25 to 100 mg/ml. Cells that weren't treated served as the standard. Cells are used for MTT assay and cell cycle phase distribution analysis after treatment. An ELISA technique is used to analyze Bcl-2 or BAX levels.
- Breast cancer cell assays [1] - MTT assay: MCF-7/MDA-MB-231 cells (5×10³/well, 96-well plate) were treated with Procyanidin C1 (5–80 μM) for 24/48/72 h. MTT reagent was added, incubated for 4 h, formazan dissolved in DMSO, and absorbance measured at 570 nm to calculate IC50. - Apoptosis assay: Cells (2×10⁵/well, 6-well plate) were treated with 30 μM Procyanidin C1 for 48 h, harvested, stained with Annexin V-FITC/PI, and analyzed by flow cytometry. - Cell cycle assay: Cells treated with 30 μM Procyanidin C1 for 24 h were fixed with 70% ethanol, stained with PI (含RNase), and analyzed by flow cytometry to determine phase distribution. - Senescent cell assays [2] - SA-β-gal staining: Senescent HDFs/MEFs (2×10⁴/well) were treated with Procyanidin C1 (1–10 μM) for 72 h, fixed, stained with SA-β-gal reagent at 37°C (no CO₂) for 16 h, and positive cells counted under a microscope. - Co-immunoprecipitation (Co-IP): Senescent MEFs were treated with 5 μM Procyanidin C1 for 24 h, lysed, and lysates incubated with anti-FOXO4 antibody. Precipitated proteins were analyzed by western blot using anti-p53 antibody to detect FOXO4-p53 complexes. |
| Animal Protocol |
C57BL/6J mice (males, 8–12 weeks)
20 mg/kg i.p. - Breast cancer xenograft model [1] - Nude mice (BALB/c-nu/nu, female, 6–8 weeks old) were subcutaneously injected with MCF-7 (5×10⁶ cells) or MDA-MB-231 (1×10⁷ cells) into the right flank. When tumors reached 100 mm³, mice were divided into 3 groups (n=6/group): vehicle (0.5% CMC), 50 mg/kg Procyanidin C1, 100 mg/kg Procyanidin C1. Compounds were administered via oral gavage once daily for 21 days. Tumor volume (measured every 3 days) and body weight (weekly) were recorded. At study end, tumors were excised for weight measurement and IHC staining. - Mouse lifespan and senescence model [2] - Naturally aging C57BL/6 mice (female, 18 months old, n=20/group): Procyanidin C1 was dissolved in drinking water at 20 mg/kg/day (adjusted for water intake) for 6 months. Control group received regular water. Lifespan was recorded, and liver/kidney tissues were collected for SA-β-gal staining. - Ercc1-/- accelerated aging mice (male, 4 months old, n=15/group): Procyanidin C1 (10 mg/kg) was administered via oral gavage once daily for 8 weeks. Control group received vehicle (0.5% CMC). Grip strength and treadmill endurance were tested every 2 weeks. Serum was collected for cytokine (IL-6, TNF-α) detection. |
| Toxicity/Toxicokinetics |
In vitro experiments: Procyanidin C1 showed no cytotoxicity to non-senescent HDF/MEF cells (CC50 > 100 μM) and normal mammary epithelial cells (MCF-10A, CC50 > 80 μM) [1,2] In vivo experiments: After long-term (6 months, 20 mg/kg, administered via drinking water) administration in C57BL/6 mice, serum ALT, AST (liver function) or BUN, creatinine (kidney function) showed no significant changes compared to the control group. No histopathological damage was observed in liver, kidney, or heart tissues [2]
|
| References | |
| Additional Infomation |
Procyanidin C1 is a Procyanidin composed of three (-)-epicatechin units linked by two consecutive (4β→8) glycosidic bonds. It possesses multiple functions, including as a metabolite, anti-inflammatory agent, antioxidant, lipoxygenase inhibitor, EC 1.17.3.2 (xanthine oxidase) inhibitor, and EC 3.2.1.20 (α-glucosidase) inhibitor. It is a hydroxyflavan, Procyanidin, and polyphenol. Functionally, it is related to (-)-epicatechin. Procyanidin C1 has been reported in tea (Camellia sinensis), camellia (Camellia reticulata), and other organisms with relevant data. See also: Pinus spp. (partial).
- Procyanidin C1 is a natural Procyanidin dimer, mainly isolated from plant sources such as grape skins, apples and cinnamon [1,2] - Anti-cancer mechanism: It inhibits the proliferation of breast cancer cells by downregulating the PI3K/Akt signaling pathway and inducing G2/M phase arrest [1] - Senescence treatment mechanism: It disrupts the FOXO4-p53 interaction, releasing p53 to specifically trigger apoptosis in senescent cells (a process called "senescent cell lysis") [2] |
| Molecular Formula |
C45H38O18
|
|---|---|
| Molecular Weight |
866.7724
|
| Exact Mass |
866.206
|
| CAS # |
37064-30-5
|
| Related CAS # |
Cyanidin Chloride;528-58-5;Procyanidin B1;20315-25-7;Procyanidin B2;29106-49-8;Procyanidin A2;41743-41-3;Procyanidin A1;103883-03-0;Procyanidin B3;23567-23-9
|
| PubChem CID |
169853
|
| Appearance |
Light yellow to yellow solid
|
| Density |
1.747g/cm3
|
| Melting Point |
140.0 - 142.0 °C
|
| Index of Refraction |
1.826
|
| LogP |
4.443
|
| Hydrogen Bond Donor Count |
15
|
| Hydrogen Bond Acceptor Count |
18
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
63
|
| Complexity |
1550
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
O1C2=C(C(=C([H])C(=C2[C@]([H])(C2=C(C([H])=C(C3C([H])([H])[C@]([H])([C@@]([H])(C4C([H])=C([H])C(=C(C=4[H])O[H])O[H])OC2=3)O[H])O[H])O[H])[C@]([H])([C@@]1([H])C1C([H])=C([H])C(=C(C=1[H])O[H])O[H])O[H])O[H])O[H])[C@@]1([H])C2=C(C([H])=C(C([H])=C2O[C@]([H])(C2C([H])=C([H])C(=C(C=2[H])O[H])O[H])[C@]1([H])O[H])O[H])O[H]
|
| InChi Key |
MOJZMWJRUKIQGL-XILRTYJMSA-N
|
| InChi Code |
InChI=1S/C45H38O18/c46-18-10-27(54)33-32(11-18)61-42(16-2-5-21(48)25(52)8-16)39(59)37(33)35-29(56)14-30(57)36-38(40(60)43(63-45(35)36)17-3-6-22(49)26(53)9-17)34-28(55)13-23(50)19-12-31(58)41(62-44(19)34)15-1-4-20(47)24(51)7-15/h1-11,13-14,31,37-43,46-60H,12H2/t31-,37-,38+,39-,40-,41-,42-,43-/m1/s1
|
| Chemical Name |
(2R,3R,4S)-2-(3,4-dihydroxyphenyl)-4-[(2R,3R)-2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-3,4-dihydro-2H-chromen-8-yl]-8-[(2R,3R,4R)-2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-3,4-dihydro-2H-chromen-4-yl]-3,4-dihydro-2H-chromene-3,5,7-triol
|
| Synonyms |
PCC1; Procyanidin C1
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~115.4 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.88 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 25.0 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: ≥ 2.5 mg/mL (2.88 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 6.25 mg/mL (7.21 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1537 mL | 5.7685 mL | 11.5371 mL | |
| 5 mM | 0.2307 mL | 1.1537 mL | 2.3074 mL | |
| 10 mM | 0.1154 mL | 0.5769 mL | 1.1537 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA