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.
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| http://dx.doi.org/10.1021/np400943b | DOI Listing |
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Article Synopsis
- Silymarin, a flavonoid from milk thistle, shows promising effects like antioxidant and anti-inflammatory properties, particularly in cancer research.
- In a study on SPC212 human mesothelioma cells, silymarin was found to have a dose-dependent cytotoxic effect, with a half-maximal inhibitory concentration (IC) of about 187.5 µM.
- The compound induced signs of apoptosis, such as cell shrinkage and nuclear changes, suggesting its potential as an anti-cancer agent that needs further investigation.
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