Home
Resources
Publications
Identification of Isosilybin a From Milk Thistle Seeds as an Agonist of Peroxisome Proliferator-Activated Receptor Gamma

Identification of Isosilybin a From Milk Thistle Seeds as an Agonist of Peroxisome Proliferator-Activated Receptor Gamma

Eva-Maria Pferschy-Wenzig, Atanas G Atanasov, Clemens Malainer, Stefan M Noha, Olaf Kunert, Daniela Schuster, Elke H Heiss, Nicholas H Oberlies, Hildebert Wagner, Rudolf Bauer, Verena M Dirsch

J Nat Prod. 2014 Apr 25;77(4):842-7.

PMID: 24597776

Abstract:

Peroxisome proliferator-activated receptor gamma (PPARγ) is a key regulator of glucose and lipid metabolism. Agonists of this nuclear receptor are used in the treatment of type 2 diabetes and are also studied as a potential treatment of other metabolic diseases, including nonalcoholic fatty liver disease. Silymarin, a concentrated phenolic mixture from milk thistle (Silybum marianum) seeds, is used widely as a supportive agent in the treatment of a variety of liver diseases. In this study, the PPARγ activation potential of silymarin and its main constituents was investigated. Isosilybin A (3) caused transactivation of a PPARγ-dependent luciferase reporter in a concentration-dependent manner. This effect could be reversed upon co-treatment with the PPARγ antagonist T0070907. In silico docking studies suggested a binding mode for 3 distinct from that of the inactive silymarin constituents, with one additional hydrogen bond to Ser342 in the entrance region of the ligand-binding domain of the receptor. Hence, isosilybin A (3) has been identified as the first flavonolignan PPARγ agonist, suggesting its further investigation as a modulator of this nuclear receptor.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP142796212	Isosilybin A		142796-21-2	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: