Current trends and future prospects of lipstatin: a lipase inhibitor and pro-drug for obesity

Abstract

A review of the implications and causes of obesity, the status of antiobesity drugs, the mechanism of inhibition of pancreatic lipases, the biosynthesis of lipstatin and the present status of lipstatin production.

Exploring Aurone Derivatives as Potential Human Pancreatic Lipase Inhibitors through Molecular Docking and Molecular Dynamics Simulations

“…Considerable effort in recent years has been devoted to the discovery of new pancreatic lipase inhibitors. Natural plant-derived compounds (alkaloids, saponins, carotenoids, glycosides, polyphenols, polysaccharides, and terpenoids) and microorganism-derived compounds (lipstatin, valilactone, and panclicins) have been isolated and reported to inhibit in vitro and in vivo pancreatic lipase [ 16 , 17 , 18 ]. Synthetic compounds with diverse structures have been prepared and screened for pancreatic lipase inhibitory activity [ 19 , 20 , 21 , 22 ].…”

Implication of mutagenesis and precursor supplementation towards the enhancement of lipstatin (an antiobesity agent) biosynthesis through submerged fermentation using Streptomyces toxytricini

“…It is estimated that market of antiobesity medicines will hike to $2.6 billion up to 2019 and orlistat will dominate the market (Kumar and Dubey 2015). Increasing occurrences of obesity and high cost treatment are exacerbating the situation.…”

“…To enhance the lipstatin production from S. toxytricini, researchers performed optimization of culture conditions and medium modifications which enhanced production of lipstatin to 3290 mg/L (Luthra et al 2013b), 4208 mg/L (Zhu et al 2014) and 2262.63 mg/L (Kumar and Dubey 2016). Moreover, it was also suggested that further improvement in lipstatin production may be performed by metabolic engineering and strain improvement approaches (Kumar and Dubey 2015).…”

Rh-Catalyzed Conjugate Addition of Aryl and Alkenyl Boronic Acids to α-Methylene-β-lactones: Stereoselective Synthesis of trans-3,4-Disubstituted β-Lactones

“…1 They have been explored for anti-obesity, 2 anticancer, 3 and antibacterial 4 applications and have been utilized as probes in activity-based protein profiling (ABPP). 1b,5,6 β-Lactones are also versatile intermediates in organic synthesis with a broad range of reactivities.…”