The Durk Pearson & Sandy Shaw®
Life Extension NewsTM
Volume 18 No. 8 • December 2015


Phenolic Acids in Plants Suppress Lipolysis in Adipocytes (fat cells) Via Activation of the Niacin Receptor GRP109A (also called HM74a/PUMA-G)

The phenolic acids (including the important polyphenols you get in your diet and probably also take in supplement form), found ubiquitously in the plant kingdom, have been reported in a recent paper (Ren, 2009) to suppress lipolysis via activation of the same receptor by which niacin also suppresses lipolysis, one of the major protective effects of niacin against cardiovascular disease.

The phenolic acids tested and reported (Ren, 2009) to inhibit adipocyte lipolysis were shown in Table 1 and included (showing the dose that inhibits lipolysis by 50%, the IC50): niacin (nicotinic acid) at 0.2, caffeic acid at 14, gallic acid at 30 and others less well known, such as protocatechulc acid at 20. Note that niacin is much more effective at inhibiting lipolysis, but keep in mind that the dose of niacin being reported here is the pharmacological dose used in conventional therapy for reducing LDL cholesterol and increasing HDL cholesterol and is far higher than the physiological amount of niacin found in a good diet. The other compounds are presumably reported at doses closer to the physiological amounts one can get in a diet.

The authors explained how they became interested in the possible activity of phenolic acids at the niacin receptor: “ ...both phenolic acids and nicotinic acid are small carboxylic acids with close structural similarity. We also note that application of certain phenolic acids, such as benzoic acid, also induces a flushing response and prostaglandin D2 release in a manner similar to that of nicotinic acid treatment. We thus asked whether phenolic acids could act as GPR109A agonists [activators].”

The authors conclude in their paper’s abstract: “Activation of GPR109A by phenolic acids may thus contribute to a cardiovascular benefit of these plant-derived products.” They also note in the text of the paper that, “while considered on an individual basis, the amount of a given phenolic acid may be low, and a combined phenolic acid content could be quite high.” They give as an example of combining different phenolic acids, “...addition of 80 mm of trans-cinnamic acid, p-coumaric acid, or benzoic acid alone led to a suppression of lipolysis by 17, 26, and 3%, respectively. However, when the same concentrations of these three compounds were combined, a suppression of 53% was observed.”

References

  • Ren, Kaplan, Hernandez, Cheng, et al. Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G). J Lipid Res. 50:908-14 (2009).

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