Table of contents

  • Introduction to Puerarin
  • Pharmacological effects of puerarin
  • Clinical uses of puerarin
  • Indications of puerarin
  • Contraindications of puerarin
  • Adverse reactions of puerarin
  • Dosage of Puerarin

 

  • Introduction to Puerarin

Puerarin is an 8-β-D-glucopyranose-4′,7-dihydroxyisoflavone isolated from the roots of the legume Pueraria lobata (Willd) Ohwi and Pueraria thunbergiana Benth. Calculated by dry product, the content of C21H20O9 should be 98.0% to 102.0%. It is an isoflavone derivative with a crown-expanding effect. Appearance is white to slightly yellow crystalline powder, soluble in methanol, slightly soluble in ethanol, slightly soluble in water, insoluble in chloroform or ether.

CAS Number: 3681-99-0

Molecular formula: C21H20O9

Molecular weight: 416.37800

Structural formula:

Puerarin

Puerarin has antipyretic, sedative and increased coronary blood flow, and has protective effect on acute myocardial hemorrhage caused by pituitrin. Clinical use for coronary heart disease angina pectoris, hypertension, etc.

  • Pharmacological effects of puerarin

Injecting puerarin into the coronary arteries of anesthetized dogs has been shown to increase cerebral blood flow and reduce vascular resistance. Puerarin also protects against myocardial ischemia caused by neurohypophysis. Both in vivo and in vitro experiments proved that puerarin can produce competitive β-receptor antagonism on rabbit arterial smooth muscle and airway smooth muscle. Puerarin can reduce blood pressure and heart rate in spontaneously hypertensive rats, but has little effect on normal Wistar rats. Puerarin can inhibit the Na current of rat spinal nerve root center neurons against tetrodotoxin (Tetradotoxin is a sodium ion channel-specific blocker, which can block the inward Na current), and has neuroprotective effect against cerebral ischemia. And by dilating intracranial arteries, improve cerebral blood flow. This effect is dose-dependent. Puerarin also lowers blood pressure, especially renal hypertension.

The effect of puerarin on the liver system: puerarin contains saponins, which have a protective effect on immune damage to liver tissue. The C-29 hydroxyl group and the C-5″ oxygen-containing group can enhance the liver protection activity. Puerarin can be absorbed through the stomach. Protects liver damage, induces apoptosis of activated hepatic stellate cells, effectively reverses chemical-induced liver fibrosis, and also has protective effects on carbon tetrachloride-induced acute liver injury, and has various physiological activities.

The effect of puerarin on the cardiovascular system: the total flavonoids in puerarin can increase the blood flow of the brain and coronary arteries. Puerarin can significantly promote the cerebral circulation and peripheral circulation of animals and humans. The total flavonoids of puerariae have mild promoting effects in improving cerebral vascular tone, elasticity and pulsatile supply in patients with hypertension and coronary heart disease. Puerarin not only improves the normal cerebral microcirculation of the human body, but also significantly improves the microcirculation disorders, mainly manifested as the increase of the local microvascular blood flow and the range of motion. Puerarin can also improve the microcirculation of nail folds in patients with sudden deafness, which can speed up the blood flow rate of microvascular, clear blood vessel loop congestion, and improve the hearing of patients. Puerarin has a protective effect on hypoxic myocardium. Puerarin can significantly reduce the oxygen consumption of ischemic myocardium and protect the heart from ultrastructural damage caused by ischemia-reperfusion.

  1. Improve the effect of microcirculation.

Mice were pre-instilled with 0.5% puerarin to antagonize the arterial constriction, slowing of flow velocity and flow reduction caused by epinephrine (ADR). , and obtained similar results as above.

  1. Effects on Hemorheology

Puerarin can reduce “JG” value, whole blood specific viscosity, erythrocyte electrophoresis time and fibrin with no difference, and hematocrit difference.

  1. The effect of increasing cerebral blood flow

Using pulsed ultrasound Doppler and transcranial ultrasound Doppler to simultaneously measure the intracranial and extracranial blood vessels and hemodynamics in anesthetized dogs, it was observed that small doses of puerarin did not reduce blood perfusion pressure, but could slow down the brain. The flow velocity of the middle and anterior cerebral arteries increases cerebral blood flow, which is caused by intracranial pressure arterial expansion.

  1. Increase coronary blood flow to protect myocardial ischemia

Puerarin has obvious effect of dilating coronary blood vessels. Can dilate normal and spastic coronary vessels.

  1. Inhibit platelet aggregation

Puerarin can inhibit adenosine diphosphate (ADP)-induced platelet aggregation in humans and animals, and the concentration ID50 of inhibiting 50% of ADP-induced platelet aggregation in rats is 0.43 mg/ml; while the combination of 5-HT and ADP Induced platelet aggregation in rabbits and sheep was also inhibited; puerarin also significantly inhibited the release of 5-HT in platelets induced by thrombin.

  1. Antiarrhythmic effect

Puerarin has obvious preventive effect on arrhythmia induced by aconitine and barium chloride, and the effect of alcohol extract and daidzein is stronger than that of puerarin. Puerarin can also significantly shorten chloroform-adrenaline-induced arrhythmia time in rabbits, and significantly increase the threshold of ouabain-induced premature ventricular contractions and ventricular tachycardia.

  1. Antihypertensive effect

Puerarin can attenuate the hypertensive or hypotensive response of norepinephrine acetomethine in hypertensive dogs.

  • Clinical uses of puerarin

Puerarin is mainly used to dilate blood vessels and improve blood circulation; reduce myocardial oxygen consumption and inhibit cancer cells; increase coronary flow and adjust blood microcirculation; treat sudden deafness at all ages; reduce the risk of cardiovascular and cerebrovascular diseases.

  • Indications for puerarin

Puerarin is used for ischemic heart disease, such as coronary atherosclerotic heart disease, angina pectoris, myocardial infarction; fundus disease, such as retinal arteriovenous occlusion, optic atrophy; such as sudden deafness; ischemic cerebrovascular disease, Such as cerebral vasospasm, cerebral infarction, cerebral thrombosis; arrhythmia, such as ventricular premature contraction, ventricular tachycardia.

  • Contraindications for puerarin
  1. Those who are allergic to puerarin are prohibited.
  2. People with hypovolemia should use puerarin after replenishing blood volume in a short period of time.
  3. It is a vasodilator and should be used with caution in patients with obvious active bleeding and bleeding tendency.
  • Adverse reactions to puerarin

Gastrointestinal reactions such as temporary abdominal distension and nausea may occur in individual cases at the beginning of the medication, which may disappear on their own if the medication is continued. Large doses can express mental arousal. Fever, rash, and shock are rare in patients.

  • Dosage of Puerarin
  1. Add 5% glucose injection or 0.9% sodium chloride injection to 100～200mg each time, 2 times a day;
  2. Intravenous infusion: 200-400 mg of 5% glucose injection or sodium chloride injection each time, once a day.
  3. Oral: 10mg each time, 3 times a day.

 

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