Studies On Active Ingredients For Diabetes From Momordica Charantia Linn By High Throughput Screen

Momordica charantia Linn (MC) was not only a main vegetable, but also a traditional Chinese herbal drug. Pharmacological studies showed that MC had the significant hyperglycemic effect on type II diabetes, including its fresh fruit, its water extraction and its ethanol extraction. The mechanism of its hypoglycemic was a hot research topic in recent year.Peroxisome proliferator-activated receptor (PPAR) belongs to one member of the nuclear receptor superfamily, and plays important roles in lipid and glucose homeostasis. Combining with the high throughput screening (HTS) technology, we had used the transactivation assay based on screening platform at the cellular level. Its reliability has been fully approved by the positive agonist assay control, and it is believed that the constructed screening model may find its wide applications in search for novel lead compounds against diabetes from MC. Results were as follows.1. Screening PPAR agonists from MC extracts by HTSHTS moulds of PPAR α,β /δ,γ agonist were used to screen PPAR α,β /δ,γ agonist from MC extracts and isolated products .Results were as follows.(1) 5 MC extracts including MC1,MC2,MC3,MC4 and MC5, had no activation effect on PPAR α . MC3 was an agonist of PPAR γ and PPAR β /δ , and the activity times were 1.689 and 1.995, respectively.(2) MC3-2 and MC3-4 were agonists of PPAR γ ,and the activity times were 1.769 and 1.699, respectively. MC3-2-1 and MC3-2-2 were agonists of PPAR γ,and the activity times were 1.57 and 1.69, respectively.(3) MC2-3 was an agonist of PPARα , PPAR 8 and PPAR y ,and the activity times were 1.767 ,3.773 and 1.785, respectively. The activity times for PPARa was more than positive control 2-Bro-(5uM).(4) Charantin was an agonist of PPARa , PPAR β /δ and PPAR γ ,and the activity times were 1.7218 ,1.7797 and 1.6818, respectively.MC-3, MC2-3 and Charantin would be the potential anti-diabetic ,anti-hyperlipidenmia and anti-obesity agents.2.Isolation, purification and chemical structure of MC polysaccharide.MC3 was isolated by DEAE ion-exchange cellulose (DE-52) and Sephadex G-100 gel filtrations. GC and TLC determined the components of the saccharides. Its MWs was measured by HPLC. The form of glucosidic bond was determined by IR.