Structure of Procyanidin C1
CAS No.: 37064-30-5
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Procyanidin C1 is a natural polyphenol with anti-tumor and antioxidant properties. It induces cell cycle arrest and apoptosis, showing significant efficacy in various cancer models.
Synonyms: PCC1; Proanthocyanidin C1; Procyanidol C1
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CAS No. : | 37064-30-5 |
Formula : | C45H38O18 |
M.W : | 866.77 |
SMILES Code : | O[C@H]1[C@@H](C2=CC=C(O)C(O)=C2)OC3=C(C(O)=CC(O)=C3)[C@@H]1C4=C(O)C=C(O)C5=C4O[C@H](C6=CC=C(O)C(O)=C6)[C@H](O)[C@H]5C7=C(O)C=C(O)C8=C7O[C@H](C9=CC=C(O)C(O)=C9)[C@H](O)C8 |
Synonyms : |
PCC1; Proanthocyanidin C1; Procyanidol C1
|
MDL No. : | MFCD01682743 |
InChI Key : | MOJZMWJRUKIQGL-XILRTYJMSA-N |
Pubchem ID : | 169853 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319 |
Precautionary Statements: | P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
MSCs | 100 µM | 3 days | PCC1 selectively eliminates senescent cells by inducing apoptosis. | Nat Metab. 2021 Dec;3(12):1706-1726 |
HUVECs | 100 µM | 3 days | PCC1 selectively eliminates senescent cells by inducing apoptosis. | Nat Metab. 2021 Dec;3(12):1706-1726 |
HT22 cells | 5 and 10 µM | 12 hours | To evaluate the preventive effect of PC-1 against glutamate-induced apoptosis in HT22 cells. Results showed that PC-1 significantly reduced glutamate-induced chromatin condensation and the number of annexin V-positive cells. | Int J Mol Sci. 2019 Jan 2;20(1):142 |
RAW 264.7 macrophages | 10 and 100 µM | 2 hours pretreatment followed by 24 hours LPS stimulation | To evaluate the inhibitory effect of Procyanidin C1 on LPS-induced inflammatory responses. Results showed that Procyanidin C1 significantly inhibited LPS-induced NO production and the expression of iNOS and COX-2. | Molecules. 2023 Mar 20;28(6):2813 |
Human nucleus pulposus cells | 10, 20, 40 µM | 24 hours | PCC1 pretreatment significantly improved cell viability and reversed acidic pH stress-induced changes in extracellular matrix metabolism. | J Transl Med. 2024 Nov 27;22(1):1071 |
RAW 264.7 macrophage cell line | 50 µM | 24 hours | To evaluate the senolytic and anti-inflammatory effects of PCC1 on senescent cells. Results showed that PCC1 significantly reduced β-galactosidase-positive cells, decreased TNF-α and IL-6 levels, and induced apoptosis in senescent cells. | NPJ Aging. 2025 May 2;11(1):31 |
HT22 cells | 5 and 10 µM | 24 hours | To assess the neuroprotective effects of PC-1 against glutamate-induced HT22 cell death. Results showed that PC-1 significantly reduced glutamate-induced cell death. | Int J Mol Sci. 2019 Jan 2;20(1):142 |
Whipworm (Trichuris trichiura) larvae | 50.4 µg/mL (41.0–62.9) | 24 hours | Evaluate the anthelmintic activity of Procyanidin C1 against whipworm larvae, showing significant activity in the unfermented state. | Front Pharmacol. 2024 Jul 22;15:1390500 |
HCT116 | 5 µM and 10 µM | 24, 48, and 72 hours | PCC1 inhibited CRC cell proliferation, migration, and invasion by suppressing miR-501-3p and upregulating HIGD1A expression | J Adv Res. 2024 Jun;60:215-231 |
DLD1 | 5 µM and 10 µM | 24, 48, and 72 hours | PCC1 inhibited CRC cell proliferation, migration, and invasion by suppressing miR-501-3p and upregulating HIGD1A expression | J Adv Res. 2024 Jun;60:215-231 |
WI38 cells | 100 µM | 3 days | PCC1 selectively eliminates senescent cells by inducing apoptosis. | Nat Metab. 2021 Dec;3(12):1706-1726 |
PSC27 cells | 50 µM | 3 days | PCC1 selectively eliminates senescent cells by inducing apoptosis and exacerbating mitochondrial stress. | Nat Metab. 2021 Dec;3(12):1706-1726 |
INS-1 cells | 12.5–50 µM | 48 hours | Procyanidin C1 dose-dependently increased cell viability and decreased ROS accumulation in H2O2-treated β-cells. | Acta Pharmacol Sin. 2016 Aug;37(8):1083-90 |
HT22 cells | 5 and 10 µM | 6 hours | To evaluate the effect of PC-1 on Nrf2 nuclear translocation and HO-1 expression. Results showed that PC-1 significantly increased nuclear translocation of Nrf2 and expression of HO-1. | Int J Mol Sci. 2019 Jan 2;20(1):142 |
Na+,K+-ATPase | 4.5 µM | 6 minutes | To investigate the inhibitory effect of Procyanidin C1 on Na+,K+-ATPase, results showed an IC50 of 4.5 µM. | Sci Rep. 2022 Apr 29;12(1):7011 |
Caenorhabditis elegans (L4) | 170 µg/mL (196.2 µM) | 72 hours | Evaluate the anthelmintic activity of Procyanidin C1 against C. elegans, showing significantly reduced activity after fermentation. | Front Pharmacol. 2024 Jul 22;15:1390500 |
Hookworm larvae | 60.9 µg/mL (46.7–80.6) | 72 hours | Evaluate the anthelmintic activity of Procyanidin C1 against hookworm larvae, showing significant activity in the unfermented state. | Front Pharmacol. 2024 Jul 22;15:1390500 |
HT22 cells | 5 and 10 µM | 8 hours | To assess the effect of PC-1 on glutamate-induced MAPK activation. Results showed that PC-1 significantly reduced phosphorylation of ERK1/2 and p38. | Int J Mol Sci. 2019 Jan 2;20(1):142 |
HT22 cells | 5 and 10 µM | 8 hours | To assess the effect of PC-1 on glutamate-induced intracellular ROS accumulation. Results showed that PC-1 almost completely blocked the glutamate-induced increase in ROS. | Int J Mol Sci. 2019 Jan 2;20(1):142 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
NSG mice | Peritoneal metastasis model | Intraperitoneal injection | 20 mg/kg | Every 2 days for 60 days | Evaluate the inhibitory effect of Procyanidin C1 combined with 5-FU on peritoneal metastasis, results showed combined treatment significantly inhibited peritoneal metastasis and prolonged survival | Clin Transl Med. 2023 Nov;13(11):e1481 |
Mice | NOD-SCID mice | Intraperitoneal injection | 20 mg/kg | Biweekly for 8 weeks | PCC1 significantly reduces tumor size and prolongs survival by clearing senescent cells and inhibiting SASP expression. | Nat Metab. 2021 Dec;3(12):1706-1726 |
NOD-SCID gamma (NSG) mice | Breast cancer and gastric cancer models | Intraperitoneal injection | 20 mg/kg | Once daily for 20 days | Evaluate the inhibitory effect of PCC1 on matCAF and its impact on tumor growth | Clin Transl Med. 2023 Dec;13(12):e1516 |
BALB/c nude mice | CRC cell xenograft model | Intraperitoneal injection | 20 mg/kg and 40 mg/kg | Once every 3 days | PCC1 significantly inhibited tumor growth and metastasis by modulating the miR-501-3p/HIGD1A axis | J Adv Res. 2024 Jun;60:215-231 |
Zebrafish | Parkinson's disease model | Water bath | 25 µM | 4 days | To evaluate the protective effect of Procyanidin C1 on the zebrafish Parkinson's disease model. The results showed that 25 μM Procyanidin C1 significantly improved the exercise capacity of zebrafish, reduced the damage to dopaminergic neurons, and upregulated the expression of Nrf2, NQO1, and HO-1 genes. | Molecules. 2022 Aug 6;27(15):5007 |
C57BL/6J male mice | Aged mouse model | Oral | 3.2 mg/kg/day | Once daily for 4 months | To assess the geroprotective effects of PCC1 on the hematopoietic immune system in aged mice. Results demonstrated that PCC1 significantly improved grip strength, reduced senescent cell burden, suppressed inflammatory responses, and restored immune homeostasis. | NPJ Aging. 2025 May 2;11(1):31 |
Mice | Natural aging model (18-20 months old) | Oral (diet mixture) | 8 mg/kg (mixed in standard diet) | Continued for 4 months | PCC1 reversed structural and functional decline in aged retina by clearing senescent cells and inhibiting SASP | Proc Natl Acad Sci U S A. 2024 Apr 30;121(18):e2311028121 |
Sprague-Dawley rats | Tail disc degeneration model | Intraperitoneal injection | 8 mg/kg/day | Once daily for 8 weeks | PCC1 treatment significantly alleviated histopathological changes of intervertebral disc degeneration and preserved the extracellular matrix of nucleus pulposus cells. | J Transl Med. 2024 Nov 27;22(1):1071 |
Bio Calculators | ||||
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1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.15mL 0.23mL 0.12mL |
5.77mL 1.15mL 0.58mL |
11.54mL 2.31mL 1.15mL |
Tags: Procyanidin C1 | PCC1 | Procyanidin C 1 | Procyanidin C-1 | PCC 1 | PCC-1 | Apoptosis | tamoxifen | DNA damage | caspase | BAX | Bcl-2 | senotherapeutic | SASP | polyphenol | mitoxantrone | MIT | inhibitor | 37064-30-5 |
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