Product name: Grapefruit Extract
Plant latin name: Citrus grandis, Citrus paradisi
Product specifications: Naringin 80-98% HPLC
Appearance: Gray white or pale yellow crystal powder
CAS No .: 10236-47-2
EINECS number: 233-566-4
Molecular formula: C27H32O14
Molecular weight: 580.5346
Studies have shown that naringin from grapefruit extract can increase the activity of superoxide dismutase (SOD) and catalase (CAT) in the liver, reduce the content of mitochondrial hydrogen peroxide in the liver cells and increase the concentration of vitamin E in the plasma. Naringin can also induce the expression of antioxidant enzyme mRNA.
Naringin has a mild inhibitory effect on lipid peroxidation in the rat brain and kidney tissue homogenate. The presence of phenolic hydroxyl groups in the molecular structure is an important factor in the antioxidant effect of naringin, suggesting that the low inhibitory effect is related to a small phenolic hydroxyl number in its structure.
Reducing blood lipid
In vivo studies have shown that naringin from grapefruit extract has the effect of lowering cholesterol, which may be achieved by inhibiting the activity of cholesterol synthase (such as HMG-CoA ~ DACAT), reducing the synthesis of cholesterol in the body, promoting cholesterol breakdown, reducing low density lipoprotein (LDL).
Scientists fed male rats with high cholesterol diet and naringin, the rat plasma, liver lipid content and neutral steroid excretion are determined after 42 days, the test results show that naringin cannot significantly improve plasma triglyceride level, but can significantly reduce plasma and liver cholesterol levels, and reduce the amount of steroid excretion. The levels of HMG-CoA and ACAT in the naringin-treated group were significantly lower than the control group.
Naringin reduces the rate of cholesterol biosynthesis in the liver by inhibiting HMG-CoA, increases steroid excretion and reduces plasma cholesterol. At the same time, histopathological analysis showed that naringin could relieve the damage of vascular wall caused by high fat diet and had a certain effect on reducing the organ damage caused by high cholesterol diet.
The result of in vitro experiments with human hepatocytes HePG2, showed that HepG2 cells treated with naringin and hesperidin reduced their ability to secrete apolipoprotein B and low density lipoproteins, which promote cholesterol deposition, so naringin has the role of prevention of atherosclerosis.
Improving the bioavailability of medicines
Naringin from grapefruit extract affects the absorption of medicines by interacting with P-glycoprotein in the intestine, and also affects the activity of cytochrome P450. Thereby naringin changes the kinetics of medicines.
Simvastatin is an oral medicine to reduce plasma cholesterol by inhibiting the activity of HMG-CoA reductase. The first pass effect of simvastatin after oral administration is an important reason for its low bioavailability. Simvastatin is also a precursor drug that requires hydrolytic metabolism. In addition, simvastatin is the substrate of cytochrome P450 enzyme, which can be oxidized in the catalysis of this enzyme.
Naringin is an effective CYP450 enzyme inhibitor that interferes with the cytochrome P450 isomerase involved in the metabolism of simvastatin in liver. Related studies found that the in vivo clearance rate of simvastatin is 26.2 L · min · 106 in the rat liver cells with the presence of naringin. After the administration of naringin, the in vivo clearance rate decreased significantly, dose-dependently. When the concentration of naringin was 50 mol·L-1, the in vivo. clearance rate was 4.15 L·min·106 cells.
Scientific studies have found that naringin from grapefruit extract can reduce carcinogen-induced gastric cancer incidence in Wistar rats. MNNG (N-methyl-N-nitro-N-nitrosoguanidine) was used to induce gastric cancer in rats in the experiment. Compared with the control group, the carcinogenic rate and the level of leucopoietin (LPO)decreased significantly, the content of SOD, CAT, GPx GSH, Vitamin C, Vitamin E increased. The positive mediation of naringin is probably the main reason for the reduction in the incidence of gastric cancer.
Naringin can inhibit the metastasis of lung cancer cells and reduce the content of MMP-2 and U-PA in the treated cells. It is found that the oral administration can inhibit the metastasis of human lung adenocarcinoma (A549) and Lewis lung carcinoma (LLC).