中文名 | 胡椒碱 |
英文名 | Piperine |
中文别名 | 胡椒酰胺 |
英文别名 | - |
来源 | 卡瓦胡椒Piper methysticum Forst |
化合物类型 | 生物碱(Alkaloids)>哌啶类生物碱 |
化学式 | C17H19NO3 |
分子量 | 285.34 |
CAS号 | 94-62-2 |
纯度 | 98%, HPLC |
溶剂/溶解度 | DMSO: 50 mg/ml (175.23 mM) |
溶液配制 | 5mg加入1.75ml DMSO,或者每2.85mg加入1ml DMSO,配制成10mM溶液。 |
产品描述 | Piperine, a natural alkaloid isolated from Piper nigrum L, inhibits P-glycoprotein and CYP3A4 activities with an IC50 value of 61.94±0.054 μg/ml in HeLa cell. | ||||
信号通路 | - | ||||
靶点 | P-glycoprotein | CYP3A4 | - | - | - |
IC50 | 61.94±0.054 μg/ml | 61.94±0.054 μg/ml | - | - | - |
体外研究 | Piperine has shown to possess in vitro cytotoxic activity and in silico studies. The IC50 value is found to be 61.94±0.054 μg/ml and in silico studies, it has more number of hydrogen bonds with minimum binding and docking energy and may be considered as inhibitor of EGFR tyrosine kinase. Piperine has been found to have immunomodulatory, anti-oxidant, anti-asthmatic, anti-carcinogenic, anti-inflammatory, anti-ulcer, and anti-amoebic properties. Piperine could enhance the bioavailabilities of other drugs including rosuvastatin, peurarin and docetaxel (DOX) via inhibition of CYP3A and P-glycoprotein activity. | ||||
体内研究 | At the dose of 3.5 mg/kg, the bioavailability of piperine is calculated to be 25.36%. Its AUC0→t is unproportionally increased with doses, indicating a potential non-linear pharmacokinetics profile of piperine. It is found that the AUC0→t and C0 of docetaxel and t1/2of piperine are significantly increased after their combination use, suggesting potential enhanced bioavailability of not only docetaxel but also piperine, which may lead to the overall enhanced pharmacological effects. The phosphorylation of I-κB, p65, p38, ERK, and JNK is inhibited by piperine in a dose-dependent manner, indicating that piperine may be a potential anti-inflammatory drug both in endometritis and in other S. aureus-induced diseases. | ||||
临床实验 | NCT01383694: Deglutition Disorders, Phase 1|Phase 2; NCT02598726: Bladder Spasm|Malignant Neoplasm|Pain|Urinary Urgency, Phase 1. |
1.Paarakh PM, et al. In Silico Pharmacol. 2015,3(1):9.
2.Meghwal M,et al. Phytother Res. 2013,27(8):1121-30.
3.Li C, et al. J Pharm Biomed Anal. 2016,128:286-93.
4.Zhai WJ, et al. Evid Based Complement Alternat Med. 2016:8597208.
包装清单:产品编号 | 产品名称 | 包装 |
SM4064-10mM | 胡椒碱(98%, HPLC) | 10mM×0.2ml |
SM4064-25mg | 胡椒碱(98%, HPLC) | 25mg |
SM4064-100mg | 胡椒碱(98%, HPLC) | 100mg |
- | 说明书 | 1份 |
-20℃保存,至少一年有效。固体粉末4℃保存,至少一个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:本产品可能对人体有一定的毒害作用,请注意适当防护,以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
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