(1) Effects on heart function:
Pueraria lobata total flavonoids and Pueraria Lobata Root Extract intravenous injection can significantly slow down the heart rate of anesthetized dogs, increase the stroke volume, decrease the total peripheral resistance, increase the aortic pressure, left ventricular end-diastolic pressure and left ventricular pressure (dp/dt ) decreased slightly, the left ventricular work decreased, and the myocardial oxygen consumption decreased. The conduction time at the atrioventricular junction was prolonged, the effective refractory period of the ventricular muscle was significantly prolonged, and the effective refractory period of the atrial muscle was slightly prolonged. Puerarin significantly prolonged the 50% and 90% repolarization process (MAPD50, MAPD90) of the monophasic action potential (MAP) in anesthetized cats, and the effective refractory period (ERP) was also significantly prolonged. Puerarin daidzein and daidzein solid dispersion (SDD) 100mg/kg orally administered, SDD can significantly lower blood pressure, slow heart rate, while daidzein has a weaker effect.
(2) Effects on myocardial metabolism:
Intravenous injection of Pueraria Lobata Root Extract 30mg/kg or Pueraria Lobata Root Extract 20mg/kg can reduce myocardial oxygen utilization rate and myocardial oxygen consumption rate in dogs, and can also reduce myocardial utilization rate of lactic acid and pyruvate. After ligation of the anterior descending coronary artery in dogs, the blood oxygen content in the coronary sinus and coronary vein decreased significantly, and the oxygen utilization rate in the normal area and the infarct area increased significantly. After intravenous injection of 30 mg/kg total flavonoids (pueraria ketone), blood oxygen content in coronary sinus and coronary vein increased significantly, and myocardial oxygen consumption in normal and infarcted areas decreased. In addition, the lactate content of arterial, coronary sinus, and coronary venous blood was reduced after ligation. Experiments have shown that intravenous injection of Gecone can reduce the elevated lactic acid content, reduce the production of lactic acid, improve myocardial oxygen metabolism, and have a beneficial effect on myocardial metabolism.
(3) Anti-myocardial ischemia effect:
Pueraria Lobata Root Extract (E21-22) has obvious protective effect on acute myocardial ischemia in rats induced by pituitrin. Pueraria total flavonoids can relieve the coronary vasospasm caused by pituitrin in acute myocardial ischemia and increase coronary blood flow. Using the canine experimental model in situ under hypothermia and external circulation, puerarin 2mg/kg was added to the perfused cold potassium cardioplegia solution, which can relieve coronary spasm, reduce myocardial energy demand, promote the recovery of left ventricular function after ischemia, and reduce lactic acid discharge , Reduce creatine phosphokinase (CPK) leakage, etc., and enhance myocardial tolerance to ischemia. Electron microscope observation also found that Pueraria Lobata Root Extract had a protective effect on ischemic myocardium, and the ultrastructure of ischemic myocardium was basically within the normal range after 140 minutes of cardiac arrest.
S86019, a component of kudzu root, exhibited a time- and concentration-dependent inhibitory effect on human acute promyelocytic leukemia HL-60 cell line, and made the cells develop from the original promyeloid stage to mature mesogranule, metamyeloid and mature Rod-shaped nuclei and segmented nuclei, indicating that S86019 is an effective inducer of HL-60 cell differentiation. The daidzein contained in kudzu root can inhibit the proliferation of leukemia cells HL-60, but the inducing effect of daidzein alone on HL-60 cells is weak. , It has obvious inhibitory and differentiation-inducing effects on the growth of HL-60 cells.
Studies have reported that daidzein has weak anti-tumor ability, can inhibit the growth of melanoma K1735M2 cells and Swiss3T3 cells, block their cell cycle in S phase, and reduce the number of cells in G1 phase, but its efficacy is weaker than trihydroxyisoflavone. The induction of apoptosis by trihydroxyisoflavones is related to some members of caspase family and bcl-2 family. Pueraria Lobata Root Extract, daidzein and trihydroxyisoflavones as the main components of Pueraria flavonoids induce apoptosis in HL-60 cells, and the regulatory pathway is also related to some members of caspase family and bcl-2 family. The effect of pueraria flavonoids extract on HL-60 cell apoptosis was related to up-regulation of Fas, up-regulation of pro-apoptotic gene bax mRNA and protein expression levels, and down-regulation of anti-apoptotic gene bcl-2 mRNA and protein expression levels. Further studies confirmed that the treatment of HL-60 cells with Pueraria total flavonoids can up-regulate the transcription and protein translation levels of caspase-8 and caspase-3 genes, which may induce HL-60 cell apoptosis through Fas death receptors and (or) mitochondria pathways collectively mediate execution. The ability of Pueraria Lobata Root Extract and daidzein monomer to inhibit the induction of apoptosis was stronger than that of Pueraria Lobata Root Extract.
Daidzein can also significantly inhibit the proliferation of melanoma B16 cells, and the ability of B16 cells to form clones and carcinogenesis in vivo after 4 days of drug treatment is significantly reduced. The principle is that daidzein can significantly change the formation of B16 cells and induce B16 cells differentiation. In addition, Pueraria Lobata Root Extract has a certain inhibitory effect on ESC cancer, sarcoma S180 and lung cancer Lewis. Moreover, Pueraria Lobata Root Extract can produce tumor necrosis factor (TNF) in the serum of animals stimulated by OK432 or LPS. TNF has direct damage to tumor cells, and can induce the production of other cytokines to activate immune-related cells. The active ingredients in kudzu root such as daidzein, daidzin, puerarin, genistein and genistin have estrogen-like activity, which can change the topoisomerase, and have effects on hormone-dependent tumors such as breast cancer, uterine membrane, etc. Cancer, ovarian cancer, colon cancer, prostate cancer cell proliferation has inhibitory effect.
Pueraria Lobata Origin Extract has a solid anti-oxidation result, including 0.1% of linoleic acid has an impact equal to 100 × 10-6 δ-tocopherol. The antioxidant effect of puerarin in lard is more powerful than that of α-tocopherol. Pueraria Lobata Root Essence can dramatically reduce lipid peroxidation and also increase the task of superoxide dismutase (TURF) and also glutathione peroxidase (GSH-Px) in aged computer mice. The isolated and refined PG1 (GP) as well as mangoside (MF) from Pueraria origin can capture the DPPH gene, and can dramatically hinder the hemolysis of red cell brought on by oxidative damage. The development of lipid peroxidation additionally has an inhibitory result, so both GP and also MF have the antioxidant impact of recording cost-free radicals. The flavonoids rich in Pueraria lobata can properly remove -OH and also hinder the oxidative damages of erythrocyte membrane, liver, spleen and brain cells, showing that Pueraria flavonoids can be used to prevent oxidative damages of biofilm. In vitro experiments revealed that 10-1000 mg/kg of kudzu root isoflavones can considerably prevent the rise of malondialdehyde, a lipid peroxidation product, caused by mouse liver, kidney cells as well as bunny mind tissue homogenate under oscillating temperature level problems, and revealed a dosage result. relationship. Pueraria flavone is an efficient natural cost-free radical scavenger, which has obvious safety result on DNA damages, and also it is confirmed via the research of dose-effect partnership that it can successfully hinder complimentary extreme damage to DNA in the series of 0.02-1000 μg/ ml. On top of that, Pueraria Lobata Origin Remove can prevent aging degenerative conditions triggered by lipid peroxidation.
Pueraria lobata can increase the weight of the uterus of immature mice, indicating that it has an estrogen-like effect, and its active ingredient may be daidzein. Giving mice Pueraria root preparations has contraceptive effect, which may be related to the estrogen-like effect of Pueraria root isoflavones. Pueraria total isoflavones restore estrogen levels in castrated rats. Pueraria Lobata Root Extract can significantly increase the weight of the vagina and uterus of ovariectomized rats, improve uterine atrophy, increase the content of estradiol in the serum of ovariectomized rats, and reduce the content of luteinizing hormone, indicating that it has certain estrogen activity . This effect was independent of an increase in serum estradiol levels, suggesting a likely direct effect.