Procyanidin C1 (PCC1) 一种具有口服活性的天然多酚，可引起 DNA 损伤，细胞周期阻滞，诱导细胞凋亡。Procyanidin C1 降低肿瘤细胞中 Bcl-2 的表达，但提高 BAX、caspase 3 和 9 的表达。Procyanidin C1 具有 senotherapeutic 活性并能够延长小鼠寿命。
| 生物活性 | Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and inducesapoptosis. Procyanidin C1 decreases the level ofBcl-2, but enhancesBAX,caspase 3and 9 expression incancercells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice[1][2]. |
| IC50& Target | IC50: 31.5 μg/mL (MCF-7), 36.6 μg/mL (MDA-MB-231)[1] |
体外研究
(In Vitro) | Procyanidin C1 (6.25-100 μg/mL; 48 h) shows cytotoxic activities to MCF-7 and MDA-MB-231 cells[1].Procyanidin C1 (35 μg/mL; 48 h) affects cell cycle of MCF-7 and MDA-MB-231 cancer cells[1].Procyanidin C1 significantly up-regulates Chk 1 and Chk 2 in MCF-7 and MDA-MB-231 cancer cells[1].Procyanidin C1 (27.85 and 66.41 μL) induces significant DNA damage in MCF-7 and MDA-MB-231 cancer cells[1].Procyanidin C1 (45 μg/mL; 72 h) reduces the expression level of Bcl-2 but increases the expression level of BAX, and increases activities of caspase 3 and 9 to induces cell apoptosis of MCF-7 and MDA-MB-231 cancer cells[1].
Cell Cycle Analysis[1] | Cell Line: | MCF-7 and MDA-MB-231 cell lines | | Concentration: | 35 μg/mL | | Incubation Time: | 48 h | | Result: | Induced the cell cycle arrest at the S-phase in MCF-7 and MDA-MB-231 cell lines. |
Cell Cytotoxicity Assay[1] | Cell Line: | MCF-7 and MDA-MB-231 cell lines | | Concentration: | 6.25-100 μg/mL | | Incubation Time: | 48 h | | Result: | Inhibited cell proliferation of MCF-7 and MDA-MB-231 cells with IC50values of 31.5 and 36.6 μg/mL and showed a higher cytotoxic activity to MDA-MB-231 than tamoxifen. |
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体内研究
(In Vivo) | Procyanidin C1 (20 mg/kg; i.p.; 2 weeks after the first MIT dose and then delivered biweekly) increases tumour regression[2].Procyanidin C1 (20 mg/kg; i.p.; for 7 d) shows senolytic efficacy in mice with senescent mouse embryonic fibroblasts injection[2].Procyanidin C1 (20 mg/kg; p.o.; for 3 d) increases the lifespan of old mice[2].
| Animal Model: | Non-obese diabetes and severe combined immunodficiency mice with PSC27 and PC3 cancer cells injection, and pre-treated with mitoxantrone (MIT)[2] | | Dosage: | 20 mg/kg | | Administration: | Intraperitoneal injection; 20 mg/kg; 2 weeks after the first MIT dose and then delivered biweekly | | Result: | Remarkably enhanced tumour regression (55.2% reduction in tumour size compared with
MIT alone; 74.9% reduction in tumour volume compared with the placebo treatment) and depleted the majority of senescent cells in chemotherapy treated animals. |
| Animal Model: | 24-27 months of age mice (both sexes)[2] | | Dosage: | 20 mg/kg | | Administration: | Oral gavage; 20 mg/kg; for three consecutive days | | Result: | Enhanced the median post-treatment lifespan with 64.2% and decreased the mortality hazard than the vehicle-treated group. |
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| 来源 | - Plants
- Rosaceae
- Crataegus pinnatifidaBge.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(115.37 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.88 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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