BREVISCAPINE Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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.
Physikalische Eigenschaften
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.
Pharmakologie
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.
Nebenwirkungen
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 .
BREVISCAPINE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
