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Eur J Med Chem. 2016 Nov 10;123:577-595. doi: 10.1016/j.ejmech.2016.07.070. Epub 2016 Jul 29.

Modulatory effects of silibinin in various cell signaling pathways against liver disorders and cancer - A comprehensive review.

Author information

1
State Key Laboratory of Core Technology in Innovative Chinese Medicine, Tasly Pharmaceutical Group Co., Ltd., Tianjin 300410, China; Tasly Academy, Tasly Holding Group Co., Ltd., Tianjin 300410, China.
2
State Key Laboratory of Core Technology in Innovative Chinese Medicine, Tasly Pharmaceutical Group Co., Ltd., Tianjin 300410, China; Tasly Academy, Tasly Holding Group Co., Ltd., Tianjin 300410, China; Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
3
State Key Laboratory of Core Technology in Innovative Chinese Medicine, Tasly Pharmaceutical Group Co., Ltd., Tianjin 300410, China; Tasly Holding Group Co., Ltd., Tianjin 300410, China.
4
State Key Laboratory of Core Technology in Innovative Chinese Medicine, Tasly Pharmaceutical Group Co., Ltd., Tianjin 300410, China; Tasly Academy, Tasly Holding Group Co., Ltd., Tianjin 300410, China; National Resource Center for Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China. Electronic address: Liwei_wzhy@163.com.
5
Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
6
State Key Laboratory of Core Technology in Innovative Chinese Medicine, Tasly Pharmaceutical Group Co., Ltd., Tianjin 300410, China; The State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China.

Abstract

Silibinin, a natural flavanone, derived from the milk thistle plant (Silybum marianum), was illustrated for several medicinal uses such as liver-protective, anti-oxidant, anti-cancer, anti-inflammation and many other. However, silibinin has poor absorbance and bioavailability due to low water solubility, thereby limiting its clinical applications and therapeutic efficiency. To overcome this problem, the combination of silibinin with phosphatidylcholine (PC) as a formulation was used to enhance the solubility and bioavailability. The results indicated that silibinin-PC taken orally markedly enhanced bioavailability and therapeutic efficiency. In addition, a deeper understanding of the signaling pathways modulated by silibinin is important to realize its potential in developing targeted therapies against liver disorders and cancer. Silibinin has been shown to inhibit many cell signaling pathways in preclinical models, demonstrating promising effects against liver disorders and cancer through in vitro and in vivo studies. This review summarizes the pharmacokinetic properties, bioavailability, safety data, clinical activities and modulatory effects of silibinin in different cell signaling pathways against liver disorders and cancer.

KEYWORDS:

Apoptosis; Cancer; Hepatoprotective; Milk thistle; Phosphatidyl choline; Silibinin

PMID:
27517806
DOI:
10.1016/j.ejmech.2016.07.070
[Indexed for MEDLINE]

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