Polyphenolic Compounds as Pancreatic Lipase Inhibitors

Abstract

Obesity and its associated diseases such as diabetes mellitus and coronary heart diseases are a major challenge for our society. An important target for the treatment of obesity includes the development of inhibitors of nutrient digestion and absorption. Inhibition of pancreatic lipase and the associated reduction of lipid absorption is an attractive approach for the discovery of potent agents. Currently, the only clinically approved pharmacologic agent as pancreatic lipase inhibitor is Orlistat. However, its usage is compromised by unpleasant gastrointestinal adverse reactions (oily stools, oily spotting, flatulence). The use of botanical materials as a potential source of new drugs is of increasing importance and application. Natural products that are interesting for obesity treatment are generally considered to have less toxic and side effects than totally synthetic drugs. One of the most important sources of potential pancreatic lipase inhibitors represents the class of polyphenols. This article summarizes most studied subclasses of polyphenols including flavonoids, hydroxycinnamic acids, hydroxybenzoic acids and lignans with pancreatic lipase inhibitory effects. A structural comparison of potent inhibitors shows an increased inhibitory effect depending on number and position of phenolic hydroxyl groups, degree of polymerization and elimination of glycosylation during digestion.

Phytochemical and biological evaluations of Arum hygrophilum boiss. (Araceae)

“…The importance of polyphenolic substances as potential inhibitors of PL were discussed recently by Buchholz and Melzig. [31] Several flavonoids, as the largest class of polyphenolic substances, have been evaluated and the studies indicated that the flavonoids having hydroxyl or methoxy groups at C3’ and C4’ in ring B as well as C-glycosidic flavones favor the PL inhibition. [313233] Additionally, the efficacy of phenolic acids, namely caffeic-, rosmarinic-, and ferulic acids, as PL inhibitors are well described.…”

“…[31] Several flavonoids, as the largest class of polyphenolic substances, have been evaluated and the studies indicated that the flavonoids having hydroxyl or methoxy groups at C3’ and C4’ in ring B as well as C-glycosidic flavones favor the PL inhibition. [313233] Additionally, the efficacy of phenolic acids, namely caffeic-, rosmarinic-, and ferulic acids, as PL inhibitors are well described. [3435] In effect, the results of the present study indicate that the PL inhibitory efficacy of A. hygrophilum may be attributable to their multiple phenolic components acting additively or synergistically.…”

A Synthetic-Biology-Inspired Therapeutic Strategy for Targeting and Treating Hepatogenous Diabetes

“…56,57 As a natural triterpenoid widely found in several dietary and medicinal plants (e.g., Olea europaea, Viscum album L., or Aralia chinensis L.), OA has been used in Chinese medicine for the treatment of liver disorders for over 20 years, and commercial OA tablets are available as OTC drugs in Chinese pharmacies for the treatment of acute and chronic hepatitis infections. 30,58 Although they are slow-acting, herbal medicines and medical nutrition therapies are recommended for liver disease patients over pharmacotherapies that utilize chemically synthesized drugs, because the former elicit milder metabolic burdens on a defective liver during the unavoidable hepatic first pass of xenobiotics.…”

Inhibitory Activity of Chalcone Moeties on Pancreatic Lipase Enzyme: A Review

“…Tina Buchholz, Matthias F. Melzig [21] Obesity and its associated diseases such as diabetes mellitus and coronary heart diseases are a major challenge for our society. Billington CJ, Epstein LH [22] More than half of adult Americans are overweight or obese, and public health recommendations call for weight loss in those who are overweight with associated medical conditions or who are obese.…”