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Drug Information

[product name] hypericin

[English name] Hyperoside

[alias] hyperin, quercetin 3-galactoside, quercetin-3-o-galactoside

[molecular formula] c21h20o12

[molecular weight] 464.3763

[C a s No.] 482-36-0

[chemical classification] flavonoids

[source] Hypericum perforatum L

[Specification] > 98%

[Safety terminology] 1. Do not breathe dust. 2.In case of accident or discomfort, seek medical attention immediately (show its label if possible).

[Pharmacological efficacy] Hypericin is widely distributed. It is an important natural product with a variety of physiological activities, such as anti-inflammatory, antispasmodic, diuretic, cough relieving, blood pressure reducing, cholesterol lowering, protein assimilation, local and central analgesia, and protective effects on heart and cerebral vessels.

[Physical and chemical properties] Light yellow acicular crystal. The melting point is 227 ~ 229 ℃, and the optical rotation is – 83 ° (C = 0.2, pyridine). It is easily soluble in ethanol, methanol, acetone and pyridine and is stable under normal conditions. It reacts with hydrochloric acid magnesium powder to produce cherry red, and ferric chloride reacts green, α- Naphthol reaction was positive.

[Risk terminology] Harmful if swallowed.

Pharmacological Action

1. Hypericin has significant local analgesic effect, which is weaker than morphine, stronger than aspirin, and has no dependence. Hypericin is a new type of local analgesic At the same time,
2. Hypericin has a good protective effect on myocardial ischemia-reperfusion, cerebral ischemia-reperfusion and cerebral infarction.
3. Hypericin has obvious anti-inflammatory effect: after implantation of wool ball, rats were intraperitoneally injected with 20mg / kg every day for 7 days, which significantly inhibited the inflammatory process.
4. It has strong antitussive effect.
5. Assimilation.
6. Strong inhibition of aldose reductase may be beneficial to prevent diabetic cataract.

Protective effect on myocardial ischemia
Hypericin can reduce the apoptosis rate of cardiomyocytes caused by hypoxia reoxygenation, inhibit the release of lactate dehydrogenase, improve the activity of myocardial superoxide dismutase (SOD) in rats with myocardial ischemia-reperfusion injury, reduce the production of malondialdehyde (MDA), inhibit the increase of myocardial phosphokinase (CPK) in serum, and reduce the formation of oxygen free radical and nitric oxide free radical, So as to protect myocardium and reduce cardiomyocyte injury and cardiomyocyte apoptosis caused by ischemia-reperfusion.

Protective effect on cerebral ischemia
Hypericin can effectively inhibit the decrease of formazan content in cerebral slices after hypoxia glucose deprivation reperfusion injury, increase the number of surviving neurons in cortex and striatum of cerebral slices in ischemic area, and make the morphology of neurons complete and well distributed. Inhibit the decrease of neuronal activity induced by hypoxia glucose deprivation reperfusion injury. Inhibit the decrease of SOD, LDH and glutathione peroxidase (GSHPx) activities. Its mechanism may be related to free radical scavenging, inhibition of Ca2 influx and anti lipid peroxide formation.

Protective effect on liver and gastric mucosa
Hypericin has obvious protective effect on liver tissue and gastric mucosa. Its mechanism is related to antioxidant effect, promoting the return of N0 level to normal and increasing SOD activity.

Antispasmodic analgesic effect
The study found that the analgesic effect of hypericin is produced by reducing Ca 2 in painful nerve endings. At the same time, hypericin can inhibit Ca 2 influx induced by high potassium, indicating that hypericin also blocks Ca channel in nerve tissue. It is further proposed that hypericin may be a blocker of Ca 2 channel. Clinical observation shows that hypericin injection is similar to atropine in the treatment of primary dysmenorrhea. Except for a few drowsy side effects, it has no common adverse reactions such as tachycardia, mydriasis and burning sensation. It is an ideal antispasmodic and analgesic.

Hypolipidemic effect
Hypericin can significantly reduce serum TC and increase HDL / TC ratio in high-fat mice, indicating that hypericin can reduce cholesterol, regulate blood lipid, and improve the activity of HDL and serum SOD in mice. This effect can significantly reduce the damage of superoxide free radical to vascular endothelium in hyperlipidemia, and is conducive to the decomposition and metabolism of lipid peroxide to protect vascular endothelium.

Enhance immune function
Hypericin at doses of 300 mg / kg and 150 mg / kg in vivo could significantly inhibit the thymus index, the proliferation of spleen T and B lymphocytes and the phagocytosis of peritoneal macrophages; At 59 mg / kg, it significantly enhanced the proliferation of spleen T and B lymphocytes and the phagocytosis of peritoneal macrophages. Hypericin at the dose of 50 ~ 6.25 ml in vitro can significantly promote the proliferation of spleen T and B lymphocytes and enhance the ability of T lymphocytes to produce IL-2; Hypericin at 6.25 g / ml significantly increased the ability of mouse peritoneal macrophages to phagocytize neutrophils, ranging from 12.5 to 3.12 μ G / ml significantly increased the ability of mouse peritoneal macrophages to release No.

Antidepressant effect
Hypothalamic pituitary adrenal (HPA) activation is a common biological change in patients with severe depression, which is characterized by excessive secretion of adrenocorticotropic hormone (ACTH) and cortisol. Hypericin can regulate the function of HPA axis and reduce the levels of ACTH and corticosterone, so as to play an antidepressant role.

Finished Drug

Ciwujia capsule
Acanthopanax senticosus capsule is a preparation with Acanthopanax senticosus stem and leaf extract as raw material. The main component is flavonoids, in which hypericin is the main active component of Acanthopanax senticosus leaves.
Main indications: promoting blood circulation and removing blood stasis. It is used for chest arthralgia and heart disease caused by blood stasis. Symptoms include chest pain, chest tightness, palpitation, hypertension, etc. it belongs to deficiency of spleen and kidney and blood stasis and Yin.

Xinan capsule
It is a preparation made of hawthorn leaf extract, which is rich in flavonoids, in which hypericin is one of the main components.
Main indications: expand coronary cardiovascular system, improve myocardial blood supply and reduce blood lipid. It is used to treat coronary heart disease, angina pectoris, chest tightness, palpitation, hypertension, etc.

Qiyue Jiangzhi tablet
Qiyue Jiangzhi tablet is a pure traditional Chinese medicine lipid-lowering drug prepared by extracting the effective parts of traditional Chinese medicine such as hawthorn (enucleated) and Astragalus membranaceus. One of the main effective components of hawthorn is flavonoids, in which hypericin content is high.
Main indications: reduce blood lipid and soften blood vessels. It is used to enhance coronary blood circulation and fight arrhythmia and hyperlipidemia.

Xinxuening tablet
Xinxuening tablet is a compound preparation made of traditional Chinese medicine such as hawthorn and pueraria. Hawthorn is the official medicine of our party. It contains ursolic acid, Vitexin rhamnoside, hypericin, citric acid, etc., of which hypericin is the main component.
Main indications: promoting blood circulation and removing blood stasis, dredging collaterals and relieving pain. It is used for chest arthralgia and vertigo caused by heart blood stasis and brain collaterals, as well as coronary heart disease, hypertension, angina pectoris and hyperlipidemia.

Yukexin capsule
Yukexin capsule is a traditional Chinese medicine preparation developed from an ancient prescription, which is composed of Hypericum perforatum, wild jujube kernel, Albizzia bark, Gladiolus and other traditional Chinese medicines. It mainly contains hypericin, quercetin, quercetin, chlorogenic acid, caffeic acid, yimaning, hypericin and other components.
Main indications: mental depression caused by restlessness of liver qi and poor mood.