The Extraction And Isolation From Grapefruits Peel And Their Antihyperlipidemic Effects

Hyperlipidemia which is a common disease can induce various cardiovascular and cerebrovascular diseases which serious threaten to people's health, especially in recent years have increasing trend. Statins, fibrates as the common drug clinical in treatment of hyperlipidemia, although the effects are obvious, there are a variety of side effects. Our country is rich in natural products resources and combined with local resources in Chongqing, we studied the lipid-lowing of grapefruits peel, which have strong significance of the development of grapefruits peel and lipid-lowing drug research.Our studies as follow:1. The extraction and preparation of compoundsThe peel as the raw material was extracted with 75% ethanol at 60℃for three times, then recrystallized with methanol and ethanol repeatedly to obtain a pure compound; then the compound was added into 2% H2SO4 to chemical cleavage for 30min, after ethyl acetate extraction and silica gel column chromatography, prepared compoundⅠand compoundⅡ.2. The identification of compoundsThrough the structural data determined by melting point, color reaction, UV, HPLC,1H NMR, 13C NMR, TLC and so on, three compounds were identified as naringin, prunin and naringenin in order.3. Effect of compounds on the activity of HMGR in vitro The inhibition of compounds to HMGR activity in vitro was detected by HPLC and further researched the structure-activity relationship among these three compounds. The results showed that all three compounds had a certain inhibition effect on HMGR, but with the increasing 7-OH glucosyl numbers, their inhibition to HMGR decreasing.4. The lipid-lowering experiment in vivoThrough the establishment of animal models of hyperlipidemia, it was found that naringin, prunin and naringenin could reduce lipid levels in vivo, meanwhile, inhibit the information of atherosclerosis and fatty liver, which were also associated with the increasing 7-OH glucosyl numbers to gradually reduce.The experiments both in vitro and in vivo found that naringin, prunin and naringenin have better effect than any compound's solo medication according to the ratio of 1:1:1 as mixed medication, indicating that there were a certain synergetic effects in lipid-lowering.