Screening, identification and activity evaluation of pancreatic lipase inhibition in Prunella vulgaris / 中国中药杂志

Pancreatic lipase (PL) inhibitors were firstly screened from Prunella vulgaris with PL immobilized on carboxylic acid-terminated magnetic nanoparticles, then these possible inhibitors were identified by LC-MS/MS and mixed standards. Finally, their inhibitory effects and types on PL were tested by p-nitrophenol method. The results showed that four PL inhibitors were screened out from P. vulgaris and confirmed by LC-MS/MS and mixed standards. The IC₅₈ and inhibition types were as follows: caffeic acid [(252.3±3.6) mg·L⁻¹, anti-competitive inhibition], rutin [(91.2±1.6)mg·L⁻¹, competitive inhibition], hesperidin [(31.5±4.4) mg·L⁻¹, competitive inhibition] and ursolic acid [(41.3±2.2) mg·L⁻¹, competitive inhibition]. Their inhibitive types and abilities on PL were related to their molecular size, hydrophobicity and the number of hydrogen bond with PL triplet.

Pancreatic Lipase Inhibitor from Food Plant: Potential Molecule for Development of Safe Anti-obesity Drug.

Obesity is a global health concern, widely recognized as the largest and fastest growing public health problem in the developed and developing countries associated with high morbidity and mortality. It is a multifactorial disease resulting in significant impairment of health. The strategies used for the treatment of obesity generally comprise of prescription of drugs and surgery. Number of basic mechanisms has been considered for obesity management but these entail serious complexities. In recent year’s pancreatic lipase, a principal lipolytic enzyme secreted by the pancreas has gained importance as -obesity target. As the PL acts in the duodenum it has least involvement with the blood or brain, avoiding a lot of drug related side effects. Although PL has been considered as good target for obesity management, the drug discovery and development in this section is not abundantly explored. Numerous natural molecules have been established for pancreatic lipase inhibitory activity but only orlistat (tetrahydrolipstatin), a saturated derivative of lipstatin designed to inhibit the action of gastrointestinal lipase approved by Food and Drug Administration (FDA) for longterm usage. However, it has severe side effects. Therefore, the possible treatment of obesity using natural products is an extensive field to be explored. Several plant derived molecules including medicinal plants have been reported for their pancreatic lipase inhibitory activity. In particular pancreatic lipase inhibitor from food plants can be considered as a good source for the discovery of a safe anti-obesity agent due to possible active principle as edible component. Present review mainly focuses on the pancreatic lipase inhibitor from food plants and its potential in the development of safe anti-obesity drug.

Synthesis and evaluation of benzylisoquinoline derivatives for their inhibition on pancreatic lipase and preadipocyte proliferation / 中国天然药物

The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, (1)H NMR and (13)C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nucifera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.