BREVISCAPINE

Description

Breviscapine is extracted from Erigeron breviscapus, the main component of which is scutellarin. It is the herb of Erigeron breviscapus (Vant.) Hand.-Mazz, distributed in Yunnan, Guangxi province, and other places, especially in Yunnan. Erigeron breviscapus was first contained in Southern Yunnan Materia Medica: “Erigeron breviscapus is mainly used for bruises, with the effects of dispelling cold and antagonizing inflammation.” Erigeron breviscapus is also widely distributed in ethnic minority areas, so it becomes a folk herb in many nations.

Physical properties

Appearance: yellow powder, with a certain hygroscopicity, odorless, tasteless, or slightly salty. Solubility: soluble in methanol and pyridine and diluted alkali solution, slightly soluble in hot water (ethanol and ethyl acetate), almost insoluble in water (ether, chloroform, benzene, and acetone). It has a maximum absorption at 284±2?nm and 335±2?nm wavelengths.

History

A 90-year old senior herbalist doctor from Qiubei County of Wenshan Zhuang and Miao Autonomous Prefecture said that Erigeron breviscapus could be used for the treatment of cerebral hemiplegia. The clinical trial demonstrates that the extract of Erigeron breviscapus has a significant effect on cerebral hemiplegia, coronary heart disease, cerebral thrombosis, cerebral hemorrhage, cerebral embolism, microcirculation, and other diseases . Since then, Erigeron breviscapus gradually gets into the vision of researchers. At present the preferred method to improve solubility at abroad is modifying chemical structure of the compound, such as esterification, benzyl esterification, and hydroxyacetamide, so as to improve the pharmacokinetic properties, esterifying the carboxyl group with polyethylene glycol (PEG) to improve the water solubility of scutellarin and hydrolyzing glucuronic acid to improve the fat-soluble scutellarin and its oral absorption .

Indications

Breviscapine is recorded in the Pharmacopoeia of the People’s Republic of China (2015). Tablets: 20?mg/tablet, 40?mg/tablet; Injection: 5?mg/ml. Ischemic cerebrovascular disease, such as cerebral thrombosis, cerebral embolism, and so on.

Pharmacology

Since 1979, breviscapine has been made into injection and tablets used in clinical, but the further research on pharmacological effects and large-scale development of breviscapine began until the late 1980s. The study found that breviscapine has a good pharmacological activity in the treatment of cardiovascular and cerebrovascular diseases. Breviscapine can be used for patients with coronary heart disease angina pectoris by inhibiting the aggregation of platelet and erythrocyte, increasing blood flow, dilating blood vessels, and improving microcirculation. It can antagonize heart failure by blocking the β-receptor, inhibiting Ca2+ influx and K+ efflux. The mechanism of breviscapine is not clear; on one hand, it may be due to the inhibition of intracellular calcium release and, on the other hand, may be stimulating the baroreceptors of blood vessel walls, so as to increase the incoming of parasympathetic impulses, directly activate the central parasympathetic nucleus and acetylcholine receptors, and then increase the activity of parasympathetic nerve. At the same time, the sympathetic impulse reduces because of the sensitization of baroreceptor, so that the sympathetic activity and blood pressure decreases. In addition, a large number of studies have shown that breviscapine can inhibit cardiomyocyte hypertrophy, hyperplasia, and reverse vascular remodeling . In addition to cardiovascular system, breviscapine also plays a critical role in the dilation of cerebral blood vessels. It can reduce cerebral vascular resistance and has a protective effect on the brain with ischemia reperfusion injury, which is mainly through upregulating the Nrf2/HO-1 pathway . Breviscapine also has a certain role in diabetic neuropathy .

Clinical Use

Breviscapine is a cerebrovascular dilator, with effects of increasing cerebral blood flow, reducing cerebrovascular resistance, and improving microcirculation. It is used clinically for the treatment of ischemic cerebrovascular disease such as cerebral thrombosis. Breviscapine has less adverse reactions, which occasionally can cause high fever, chills, and other infusion reactions.

Side effects

Individual patients may have rash, dry mouth, fatigue, and other symptoms, disappearing after withdrawal. Breviscapine injection added with low molecular weight dextran had caused acute gastrointestinal bleeding; therefore, the elderly or patients with a history of upper gastrointestinal bleeding should use cautiously .