Rhaponiticin（155-58-8）

Pharmacology: active hypoglycemic effect: rhubarb extract is often used to weaken metabolic abnormalities such as diabetes, high blood cholesterol, platelet aggregation, etc. The experiment shows that [14]: the 70% ethanol extract of rhubarb can significantly reduce the blood glucose concentration of streptozotocin induced diabetes mice. The extract was separated by XAD-4 column chromatography, and its 60%, 80% and 100% methanol elution enhanced insulin sensitivity and inhibited α- Glucose activity. The active substances such as levantin and rhein were further separated. Among them, lefangtin enhanced insulin-induced glucose absorption and triglyceride accumulation in 3T3-L1 adipocytes, and its effect was similar to that of pyrrolidone, a thiazolidinedione drug, suggesting that lefangtin might be PPAR- γ To reduce the blood sugar concentration and achieve the effect of treating diabetes. Antioxidant effect: 10 kinds of stilbene compounds isolated from rhubarb, including lefatine, have antioxidant activity. Kinetic studies show that these compounds compete with linoleic acid to inhibit the active sites of lipoxygenase, with IC50 values of 6.7~74.1 μ 50. In addition, it also has a significant scavenging effect on ABTS+free radicals (TEAC=1.16~4.64). Some studies have also shown that lefatine has a scavenging effect on ROS, DPPH free radicals and H2O2 in cells. Further study of its mechanism found that lefatine can prevent the oxidation of lung fibroblasts V94-7 by improving the antioxidant activity of cells and regulating the cell signal transduction pathway (enhancing the phosphorylation of extracellular ERK and inhibiting the activity of AP-1). Anti-thrombotic and platelet aggregation: both in vivo and in vitro experiments of ADP and collagen-induced platelet aggregation in mice confirmed that Lefatine and its 8-O- β- D-glucose derivatives have antiplatelet aggregation effects, with IC50 values of 4 mg • L-1 and 70 mg • L-1 respectively, which are better than aspirin, and the latter can significantly reduce the death caused by pulmonary thromboembolism in mice. Congestion is a series of symptoms caused by blood stasis or inflammation. Rheum is commonly used in traditional Chinese medicine to treat stasis. Studies by Japanese scholars have shown that the mechanism of action is the inhibition of the production of NO in LPS-active macrophages by diphenyl compounds such as lefatine and the protective effect of D-galactosamine/LPS-induced liver injury. Anti-allergic effect: Lefatine is converted into 8-O under the action of human intestinal flora- β- D-glucose derivative, research table: this derivative has inhibitory effect on a histamine-hydrohyaluronidase released by mast cells and anaphylaxis (PCA), and its effect is better than that of non-glucocorticoid anti-inflammatory agent - sodium cromolynate. Therefore, Lefentine can be developed as a prodrug of antiallergic drugs. Other studies have shown that Lefatin 8-O- β- D-glucose derivatives have good inhibitory effects on anaphylaxis at 25mg • L-1 and 50mg • mL-1, with inhibition rates of 48% and 85% respectively. The anti-inflammatory effect of Lefangting orally is better than that of intravenous injection. Anti-tumor effect: Ryu et al. [19] showed that several stilbene compounds, including lefatine, have anti-tumor activity in vitro and have inhibitory effect on five human cancer cell lines - A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT15. Vasodilatory effect: Yoo et al. [20] showed that the methanol extract of Rhubarb undulata can stretch the rat thoracic artery of 0.3 µ mol • L-1 contracted by adrenaline, with an EC50 value of 5.8 µ g • mL-1. The extract was further isolated to obtain seven functional compounds, including lefatine, whose mechanism of action may be related to NO signal transduction pathway. Inhibition of apoptosis: β The accumulation of amyloid 1-42 is an important reason for the formation of Alzheimer's disease. Studies have shown that lefatine has an effect on the IMR-32 system of human neuroblastoma cells β Amyloid 1-42 has resistance to maintain cell viability and protect mitochondria. The mechanism of action is related to the expression of bcl-2 gene family, β Amyloid protein 1-42 induces up-regulation of bax and down-regulation of bcl-2, which leads to neurotoxicity. However, Lepidotide leads to down-regulation of bax and up-regulation of bcl-2, thus inhibiting the formation of Alzheimer's disease. Whitening: The research shows that Lefentine has a whitening function because of its strong percutaneous absorption ability and can inhibit the formation of melanin. Its whitening ability is in a dose-effect relationship with the content of Lefentine (0.0001%~10%). Anti-alcoholic effect: The research shows that Lefatine can reduce the metabolism of alcohol to aldehyde by inhibiting the effect of alcohol dehydrogenase, thereby reducing the symptoms of cytotoxicity and hangover, so as to achieve the anti-alcoholic effect. Estrogen-like effect: diethylstilbestrol is the prototype of synthetic hormone. Among the natural stilbene compounds, only lefentine has estrogen effect and can be used for the development of contraceptives.