The pharmacological effects of Sophora

Pharmacological effects

1. Beauty and skin care effects: cold, heat and dampness, insecticidal effect, sophora flavescens bath can remove hot and humid under the coke, and kill insects and itching, has a good alleviation effect on skin itching, plant herbs can balance oil secretion, and clear Convergence of pores, removal of toxins from the skin, rich herbal nutrition, promote the growth and repair of damaged blood vessels and nerve cells, restore the vitality of subcutaneous capillary cells, skin to reproduce tight and smooth, play a role in skin care.

2. Antibacterial effect: Sophora flavescens Ether extract and alcohol extract have strong antibacterial effect against Staphylococcus aureus; Sophora flavescens water infusion agent against Trichophyton mentagrophytes, Trichophyton mentagrophytes, Trichophytonaceae, Audu ang Bacillus spores have inhibitory effects.

3. Anti-tumor effect: Matrine inhibits Ehrlich ascites carcinoma and sarcoma-180 in vitro and in vivo.

4. Whitening effect: Soluble total alkaloids and oxymatrine have a significant whitening effect, which has a significant therapeutic effect on leukopenia caused by cyclophosphamide, X-ray and cobalt radiation.

5. Anti-inflammatory effects: Matrine has inhibitory effects on ear swelling caused by croton oil in mice, increased peritoneal exudation caused by acetic acid, and footpad swelling in rat carrageenan.

6. Anti-arrhythmic effects: Matrine is able to counteract chloroform-adrenergic induced ventricular fibrillation in cats; it also counteracts aconitine-induced arrhythmias in rats and ouabain-induced ventricular fibrillation in guinea pigs. Inhalation of chloroform caused by ventricular fibrillation in mice, aconitine-induced rat arrhythmias, chloroform-adrenergic induced arrhythmias in rabbits have obvious antagonistic effect; Sophora Flavonoids can fight spontaneous myocardial cell mass and ouaba Abnormal rhythm due to pulsation. In addition, there is a significant diuretic effect of Sophora flavescens; alkaloids of Sophora flavescens are stable, antiasthmatic, and immunosuppressive.

Pharmacological function

Anti-tumor effect

Matrine has anti-cancer activity. The survival rate of mice in the group of 500 μg.d intraperitoneal injection for 2 months was 40%, while the control group died within 23 days. Oxymatrine has no effect on this. Matrine has the effect of reducing mouse peritoneal macrophages inhibiting the proliferation of P815 tumor cells in vitro. Sophocarpine also has anticancer activity, and it has obvious inhibitory effects on S-180, U-14.ECA, L and other tumor strains in experimental mice. Matrine, oxymatrine, sophocarpine and their mixed A, B and C bases all had different degrees of inhibition on solid tumors of S-180. The inhibitory rate of each alkaloid was 35 Above the %, when the dose of C base mixed at different ratios is 113 mg/(kg·d), the tumor inhibition rate of continuous intraperitoneal injection for 10 days is 61.38%, which is 23.5% higher than that of total alkali, compared with that of matrine alone. There was a significant difference (P<0.01). Matrine has a significant inhibitory effect on the rate of colony production of peripheral multipotential hematopoietic progenitor cells in chronic myelogenous leukemia with an inhibition rate of 0.76 and an optimal inhibitory concentration of 100 mg/L. Sophora flavescens decoction acts on human promyelocytic leukemia cells cultured in vitro. At a dose of 8 mg/ml, leukemia cells can be significantly induced to differentiate into mononuclear macrophages.

Lectin

Oxymatrine can prevent mouse leucopenia caused by MMC and cyclophosphamide. WBC or intramuscular injection of 30 mg/kg total oxymatrine and 100 mg/kg oxymatrine on peripheral blood leukocytes in normal rabbits. There was a significant elevation effect, and the peak time for the oxidative maturation of the whitening effect of normal rabbits, the duration of maintenance, and the peak white blood cell count were similar to those of the total alkaloids of Sophora flavescens, and were basically the same within 18 days after administration. The white effect is better than shark liver alcohol. In the leukopenia-induced leukopenia induced by the total amount of Sophora flavescens, oxymatrine, and matrine in rabbit X-rays, the total alkaloids in Sophora flavescens group were counted from day 5 to day 19 of leukocyte counts. It remained at above 6000/mm3, but the control group did not recover the above levels until 22 days. The titration efficiency of oxymatrine was not higher than that of total alkaloids. Matrine had no therapeutic effect. Oxymatrine induced leukopenia in rabbits after whole body irradiation with 60 Cobalt r-rays of 500 μL. The dose rate was 31 lennes/min, showing certain prevention and control effects. There was no prevention and treatment effect at a dose rate of 120 nm/min.

Effects on the cardiovascular system

Intravenous injection of 1/4 LD50 of matrine and oxymatrine significantly inhibited arrhythmia induced by aconitine and chloroform-adrenergic in rats; intraperitoneal injection significantly combated ventricular fibrillation induced by chloroform in mice, and also increased aconitum The amount of alkali-induced arrhythmias required in rats against alum-induced arrhythmias in rats and arrhythmia induced by ligation of the coronary artery in rats with ligation. Intravenous injection of 30 mg/kg oxymatrine to rabbits shortened the recovery time of arrhythmia induced by epinephrine, and the treatment administration was shortened by an average of 43%, and the preventive administration was shortened by an average of 22%. Intravenous injection of 42 mg/kg sophocarpine can fight calcium chloride-induced ventricular arrhythmias and aconitine-induced arrhythmias in rats; intravenous injection of l6 mg/kg can increase ouabain-induced premature beats and cardiac arrest. Dosage, but also can resist coronary obstruction - reperfusion induced canine arrhythmia, but can not fight calcium chloride - acetylcholine-induced mouse atrial fibrillation (flutter) and chloroform - adrenaline-induced arrhythmias in rabbits. Intravenous injection of 1/5 LD50 of sophoridine (11 mg/kg) can prevent or treat aconitine-induced rat arrhythmia. It can also increase the tolerance of guinea pigs to ouabain-induced arrhythmias and prevent chlorine. Induction of arrhythmias in rats by phlegm and calcium chloride. The 1/10 LD50 dose (5 mg/kg) significantly shortened the arrhythmia time induced by epinephrine, and the duration of action was much longer than that of quinidine. It can also increase the left ventricular electrical fibrillation threshold in rabbits and increase with the dose of intravenous injection. It can also dose-dependently reduce the rate of ventricular fibrillation induced by chloroform or carbon tetrachloride in mice, as well as against carbon tetrachloride-adrenaline. Caused arrhythmia in rabbits. Matrine alkaloids have dilated blood vessels and protective effects against acute myocardial ischemia. Anesthetized rabbits can cause significant antihypertensive effect, usually about 20mmHg, and return to normal for 2-3 minutes; it can cause immediate expansion of isolated rabbit ear blood vessels and last for about 10 minutes; it can extend the acute hemorrhagic heart. The pause time was extended for about 7 minutes; it had a significant protective effect on acute myocardial ischemia induced by pituitrin. Oxymatrine increased rabbit atrial contractility with a good dose-effect relationship, 9 μm did not affect myocardial excitability, but shortened the functional refractory period; decreased epinephrine-induced threshold concentration of left atrial autoregulation; slowed right atrium Autonomous rhythm and reduced the positive frequency effect of CaCl2 on the right atrium. Poisoning (360 μm) reduces myocardial contractility and excitability. Oxymatrine 50μmol/L can antagonize the positive frequency effect of isoproterenol. Oxymatrine (100 μmol/L), at a lower (high) concentration of cultured cardiomyocytes, could produce negative (positive) frequency mediated by α(β) receptors. Matrine can reduce the right atrium frequency in guinea pigs, increase right atrial contractility and reduce left atrium MDF (maximum driving frequency) in a dose-dependent manner; its negative frequency, positive inotropic and negative MDF effects were presented Straight line related. Matrine can inhibit athelin-induced left atrium in rats or prolong the incubation period of aconitine-induced automatic rhythm and slow down the initial frequency; can also increase ouabain-induced guinea pig right atrial arrhythmias and adrenaline injection The threshold concentration of autonomic self-discipline in guinea pigs was induced, and the positive inotropic effect of ouabain was enhanced. Matrine was significantly inhibited by verapamil (1 μmol/l), a Ca2+ channel blocker, and inhibited the smooth muscle more than the myocardium, suggesting that the positive inotropic effect of matrine may be related to the activation of Ca2+ channels. Matrine can increase the plasma cAMP level and decrease the cMP level in rats, but it has no significant effect on the content of cAMP and cGMP in myocardial tissue. Sophoridine can increase cAMP level in plasma and cAMP content in myocardial tissue. Oxymatrine 50μmol/L and 250μmol/L significantly inhibited the increase of lactate dehydrogenase activity induced by mitomycin C in cultured cardiomyocytes in vitro, and could alleviate the myocardium caused by hypoxia and hypoxia. Damage, but no protection against myocardial damage caused by chlorpromazine. Intramuscular injection of oxymatrine significantly prolonged the survival of mice with allogeneic free-graft myocardial survival, and its effect increased with increasing dose. When Sophora flavescens total flavonoids were 125-250 μg/ml, the frequency of spontaneous beats in cultured neonatal rat cardiomyocytes was reduced, and spontaneous beats and ouabain-induced beating rhythm disorders were counteracted. Flavonoids flavonoids have significant antagonistic effects on ventricular fibrillation induced by inhalation of chloroform in mice, with a LD50 of 23.9±1.1 g/kg and a therapeutic index of 3.56. Intravenous injection of total flavonoids of Sophora flavescens 8g and 30g/kg was given to rabbits. After 30-60 minutes, it could obviously fight the arrhythmia induced by chloroform-adrenaline. The complete confrontation rates were 40% and 70% respectively. Intravenous injection of total flavonoids of Sophora flavescens 20-40g/kg has obvious therapeutic effects on arrhythmia induced by intravenous aconitine in rats. The first treatment was effective at 63%, and the second treatment was 84%. Intravenous injection of matrine in rats significantly inhibited arrhythmias caused by aconitine, strontium chloride, and ligating coronary arteries. Intravenous injection of total flavonoids of Sophora flavescens 30g/kg and 60g/kg was given to anesthetized rats, showing significant negative effects. Self-discipline, negative frequency effect and negative conduction. These effects increase with increasing dose.

Asthma

Matrine is mainly produced by stimulating β-receptors, especially the excitatory central β-receptors, releasing bronchospasm and inhibiting the release of antibodies and slow-responsive substances. Matrine in the presence of calcium or calcium-free Klinefelter's nutrient solution was able to combat the effects of acetylcholine chloride chloride on isolated guinea pigs, rat trachea and intestine. The anti-asthmatic effect of Sophora flavescens and oxymatrine on histamine-induced asthmatic guinea pigs was similar to that of ammonia tea base. The asthma rate was above 90% for one hour, and about 15% for the control group; Aminophylline has an asthma relief rate of 55% at 6 hours and total matrine at 80%. Sophora Ach is more potent than aminophylline, and its antiasthmatic effect may be through the activation of the β-receptors in the midbrain. The phenol red excretion method proved that the total amount of flavonoids and total flavonoids in mice was 0.8 g/kg.

Stability

Sophora flavescens total alkaloids 50-100mg/kg can significantly inhibit the free movement of mice; 400mg/kg can significantly inhibit the passive activity of mice; 100-200mg/kg can inhibit the Oudou aggressive behavior of lone mice; Sophora flavescens 25 -40mg/kg in combination with Dongmulin (5mg/kg) can cause the mice to correct righting reflex, 100-200mg/kg total alkaloids of Sophora flavescens can significantly strengthen the inhibitory effect of 0.5mg/kg reserpine on spontaneous activity of mice Sophora flavescens total base 50-200mg/kg and intraperitoneal injection of subthreshold dose of pentobarbital 20-25mg/kg, can cause mice to fall asleep; with thiopental (intraperitoneal injection, 40mg/kg), Combined use of chloral hydrate (intraperitoneal injection, 200 mg/kg) can significantly enhance central inhibition. Can also significantly counteract the psychomotor excitement caused by the central stimulants amphetamines (ip, 4-6mg/kg) and caffeine (50mg/kg); somatostatin to strychnine and pentetrazole-induced convulsions Not only does it have no antagonistic effect, but it increases its convulsions and increases its animal deaths. Sophora flavescens alone has mild analgesia, and combined with a threshold dose of morphine can significantly increase its percentage of analgesia.

Anti-allergic effects

Matrine can reduce the release of allergic mediators and is an immunosuppressive agent. The concentration of inhibiting 50% T cell proliferation is 0.55-0.56 mg/ml; the concentration of inhibiting IL-2 production is 0.1 mg/kg.

Immunosuppression

Matrine and oxymatrine inhibited the immune function of mice at 1/5 LD50 dose. Intramuscular injection of oxymatrine 150 mg/kg or 100 mg/kg in rabbits and rats had a significant inhibitory effect on passive or active cutaneous anaphylaxis and inhibited rabbit serum IgE antibody formation significantly. Intraperitoneal injection of oxymatrine 200 mg/kg·d for 21 days protected the mice from immediate allergy induced death.

Other effects

Intramuscular injection of oxymatrine can significantly counteract the exudative inflammation induced by croton oil, carrageenan (rats) and glacial acetic acid (mouse). Rabbit gavage, subcutaneous injection, intravenous injection, intraperitoneal injection and intramuscular injection of Sophora flavescens decoction, Kushen injection and matrine have diuretic effect, and urinary sodium chloride significantly increased. Sophora flavescens 50% methanol extract has the effect of anti-hydrochloric acid-induced ulceration, and its active ingredient is kurinone. In addition, matrine has an antibacterial effect both in vivo and in vitro, and the strength of action in vivo is comparable to that of chloramphenicol. The alcohol extract has an anti-trichomonal action in vitro, and its strength is similar to that of hops.


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