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.

Effect of gastrointestinal lipase inhibitor combined with biguanides on serum estrogens in polycystic ovary syndrome with infertility / 中国生化药物杂志

Objective To investigate the effect of gastrointestinal lipase inhibitor combined with biguanides on serum estrogens in the treatment of polycystic ovary syndrome with infertility in patients.Methods 72 cases with polycystic ovary syndrome with infertility from Huangyan Hospital Affiliated to Wenzhou Medical University were selected and randomly divided into 2 groups, 36 cases of each group.The control group received conventional therapy, and the treatment group received more with orlistat, serological indicators, clinical symptoms, signs, pregnancy rate and ovulation rate were compared after the treatment.Results Compared with control group, levels of blood glucose and blood lipid index decreased in treatment group after treatment (P<0.05), the levels of luteinizing hormone (LH), follicles estrogen (FSH), estradiol (E2) and testosterone (T) decrease(P<0.05), levels of visfatin (VF) and leptin (LEP) decreased(P<0.05), adiponectin (APN) increased(P<0.05), and levels of BMI, WHR, hirsutism score and ovarian volume decreased (P<0.05).Compared with the control group(69.44%, 55.56%), the ovulation rate and pregnancy rate in the treatment (91.67%, 80.56%) were higher(P<0.05).Conclusion Gastrointestinal lipase inhibitor combined with biguanides could improve the pregnancy rate and ovulation rate in patients with polycystic ovary syndrome with infertility, reduce the levels of estrogens.

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.

Research on Chinese medicine pairs effects of Panax notoginseng and Bletilla striata before and after compatibility on contents of notoginsenosides / 中国中药杂志

To discuss the synergistic mechanism of compatible use of two medicinal herbs,Panax notoginseng and Bletilla striata, an HPLC was established to determine two ginseng saponins (20S)-ginseng saponin Rg₃ and ginseng saponin Rh₄ contained in single decoction of Panax notoginseng as well as in compound decoction of Panax notoginseng and Bletillastriata in different compatibility ratio (1∶0.5, 1∶1, 1∶2), followed by analyzing the impact of amount of notoginsenosides after compatibility. As a result, compared with the single decoction of Panax notoginseng, the contents of ginseng saponin Rg₃ and ginseng saponin Rh₄ in the compound decoction of Panax notoginseng and Bletillastriata were on the rise as the increasement of the amount of Bletillastriata. The contents of the notoginsengsaponin R₁, ginseng saponin Rg₁ and ginseng saponin Rb₁ of Panax notoginseng single decoction were significantly decreased after compatibility. Therefore, after compatibility, it was more easy to produce (20S)-ginseng saponin Rg₃ and ginseng saponin Rh₄.This study can extend to a method of preparation of (20S)-ginseng saponin Rg₃ and ginseng saponin Rh₄. Furthermore, after compatibility, two ginseng saponins which had lipase inhibitory effect were both increased significantly, indicating that the compatibility of these two herb medicines may have effect on losing weight.

Extraction and Characteristics of Anti-obesity Lipase Inhibitor from Phellinus linteus

To develop a potent anti-obesity lipase inhibitor from mushroom, the lipase inhibitory activities of various mushroom extracts were determined. Methanol extracts from Phellinus linteus fruiting body exhibited the highest lipase inhibitory activity (72.8%). The inhibitor was maximally extracted by treatment of a P. linteus fruiting body with 80% methanol at 40degrees C for 24 hr. After partial purification by systematic solvent extraction, the inhibitor was stable in the range of 40~80degrees C and pH 2.0~9.0. In addition to lipase inhibitory activity, the inhibitor showed 59.4% of superoxide dismutase-like activity and 56.3% of acetylcholinesterase inhibitory activity.