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Release Date:2017/12/5 13:59:13
Erigeron breviscapus
1、 Pharmacopoeia standard of Erigeron breviscapus
Erigeron breviscapus (Erigeron breviscapus)
Dengzhanxixin
ERIGERONTIS HERBA
      This product is the dried whole grass of Erigeron breviscapus (vant.) hand.-mazz., a composite plant. Excavate in summer and autumn, remove impurities and dry in the sun.
      [properties] the product is 15 ~ 25cm long, 1 ~ 3cm long rhizome, 0.2 ~ 0.5cm in diameter; the surface is uneven, with many cylindrical fine roots, about 0.1cm in diameter, light brown to yellowish brown. The stem is cylindrical, 14 ~ 22cm long and 0.1 ~ 0.2cm in diameter; it is yellowish green to light brown, with fine longitudinal edges and white pubescence; It is brittle in texture, yellowish white in cross section, medullary or hollow. The basal leaves are shrunken and broken, and the intact ones are flattened to be obovate lanceolate, spoon shaped, broad lanceolate or broad obovate, 1.5-9cm long and 0.5-1.3cm wide; yellowish green, blunt and round at the apex, with short tips, base tapering, and entire; The cauline leaves are alternate, lanceolate, and the base holds the stem. Capitulum terminal. Achene oblate obovate. .
      . Non glandular hairs are 1-8 cells, about 180-560 µ m in length. The head of glandular hairs is 1-4 cells, and the stalk is 1-multicellular.
      (2) Take this product and test it according to the method under [content determination]. The chromatogram of the test sample should present a chromatographic peak consistent with the chromatographic retention time of the control sample.
      [check] moisture   .
      Total ash   Not more than 15.0% (general rule 2302).
      ; Not more than 8.0% (general rule 2302).
      [extract] according to the hot leaching method under the determination method of alcohol soluble extract (general rule 2201), the use of ethanol as solvent shall not be less than 7.0%.
      [content determination] determine according to HPLC (general rule 0512).
      ; Octadecylsilane bonded silica gel was used as filler; The mobile phase was methanol-0.1% phosphoric acid solution (40:60); The detection wavelength was 335nm. The number of theoretical plates should not be less than 5000 according to the peak of scutellarin.
      Preparation of reference solution   Take an appropriate amount of scutellarin reference substance, accurately weigh it, add methanol to make a solution containing 0.1mg per 1ml.
      ; Take about 0.5g of crude powder of this product, weigh accurately, put it in Soxhlet extractor, add appropriate amount of chloroform, heat and reflux until the extraction solution is green, discard the chloroform solution, volatilize the solvent from the drug residue, and transfer it together with the filter paper cylinder into a corked conical bottle, add 50ml of methanol precisely, close the plug, weigh the weight, place for 1 hour, heat and reflux in water bath for 1 hour, cool down, weigh again, use methanol to make up the lost weight, shake well, and filter. Accurately measure 25ml of the secondary filtrate, recover the solvent to dryness, dissolve the residue with methanol and transfer it to a 10ml volumetric flask, add methanol to the scale, shake well, filter, and take the secondary filtrate.
      Assay   Precisely suck 5 ~ lo µ l of the reference solution and test solution respectively, inject them into the liquid chromatograph, and determine.
      According to the dry product, the content of scutellarin (c21h18o12) in this product shall not be less than 0.30%.
      [nature, taste and meridian tropism] pungent, slightly bitter, warm. .
      [functions and indications] activating blood circulation, dredging collaterals and relieving pain, dispelling wind and dispersing cold. For stroke hemiplegia, chest pain, rheumatism pain, headache, toothache.
      [usage and dosage] 9-15g, fried or ground steamed egg. .
      [storage] put it in a dry place.
 

2、 Chemical constituents of Erigeron breviscapus
Whole grass containsPyromellitic acid(pyromeconic acid),erigeroside Erigeroside [4,5,6,7-tetrahydroxyflavone-7-o - β - d-gluconopyranoside methyl ester],Apigenin(apigenin),High baicalein(scutellarein),Daphnetin(cosmosiin),Apigenin-7-o-glucuronide(breviscapine) (apigenin-7-o-gluconide),Plantain(plantaginin) and scutellarein-7-o-gluconide, in which the former is predominant and the mixture containing a small amount of apigenin-7-o-gluconide is namedBreviscapine(breviscapine)[4]。

3、
1. effects on cardiovascular system scutellarin extract 0.25mg/ml.smg/ml can significantly enhance the coronary flow of isolated guinea pig heart [1]. The water-soluble fraction of Erigeron breviscapus 4mg (extract) / ml can relax the isolated porcine coronary arteries contracted by 15 methylprostaglandin FZ α [2]. Erigeron breviscapus can significantly reduce the myocardial infarction range of canine myocardial infarction model. . The observation of coronary vascular tree casts showed that Erigeron breviscapus injection may promote the opening of coronary collateral circulation. Anesthetic bolus injection of Erigeron breviscapus injection 10mg/kg has the effects of slowing down heart rate, reducing myocardial contractility, reducing myocardial oxygen consumption and work [3]. In the rat model of whole heart hypoxia and reoxygenation, the release of creatine phosphokinase was significantly decreased in the 100mg/l perfusion group of total flavonoids of Erigeron breviscapus; After reoxygenation, the release amplitude of Erigeron breviscapus was also significantly lower than that of the control group, suggesting that Erigeron breviscapus has a protective effect on cardiac cell membrane. After simple hypoxia perfusion for 50min, the myocardium in the administration group showed higher activities of superoxide dismutase and glutathione peroxidase. . Erigeron breviscapus flavone decreased aortic blood flow and heart rate in rabbits, but had no obvious effect on blood pressure [5]. Clinical application of Dengzhanxixin capsules in the treatment of coronary heart disease angina pectoris, the total effective rate is higher than that of Salvia miltiorrhiza. Patients had 24.1% stroke [19]. Cardiac function indexes such as stroke volume, stroke volume per minute and cardiac index were improved [6]. Erigeron breviscapus also has an antagonistic effect on myocardial ischemia and hypoxic ECG changes [7].
2. Anticoagulant, antithrombotic and fibrinolytic activity of Erigeron breviscapus at a concentration of 23mg/ml has an inhibitory rate of 56.5% on rabbit platelet aggregation in vitro [1]. Erigeron breviscapus injection (containing erigeron breviscapus flavone SMG / L) was administered intravenously to rabbits at 8ml / kg, and the peripheral platelet count decreased and the platelet aggregation function decreased at 1H and zh after administration, with substantial changes [18]. The drug action peaked at zh after administration. . LH after injection, plasma fibrinogen decreased, globulin dissolution time decreased, and serum fibrinogen degradation products increased, suggesting that Erigeron breviscapus has the effect of promoting fibrinolytic activity. After intravenous administration of ZH in rabbits, the time of thrombosis in vitro was prolonged, the length of examination was shortened, and the wet child and dry weight of thrombus were reduced, suggesting that Erigeron breviscapus can inhibit thrombosis in vitro, and the effect of ZH after administration was the strongest [8]. Intravenous injection of breviscapine at 140mg / kg and 350mg / G can significantly reduce the weight of thrombus and inhibit the formation of thrombus in aortic thrombosis model rabbits. This cultivation is positively correlated with the dose. Breviscapine also reduces the degree of platelet rupture and inhibits the enhancement of serotonin release response. Thromboxane B2 (TXB2), a metabolite of arachidonic acid with fine platelet and vascular endothelium, and 6-keto-pgf1 α water did not change significantly in the administration group, but significantly increased in the control group [9]. .
3. effects on microcirculation and hemorheology in the rabbit model of cerebral microcirculation disorder caused by high molecular dextran and the guinea pig model of pial microcirculation disorder, intravenous injection of Erigeron breviscapus extract can significantly restore the cerebral cortex EEG of rabbits, improve the pial microvascular flow pattern of guinea pigs, have obvious depolymerization effect on guinea pig red blood cells, and resist the vasoconstriction effect of norepinephrine [1-12]. For the disturbance of mesenteric microcirculation caused by dextran in rats, pre intravenous injection of Erigeron breviscapus extract, or administration with the same dose and method after modeling, can significantly promote microvascular opening and improve microcirculation, and they can also resist the vasoconstriction of epinephrine [10, 13]. Injection of Erigeron breviscapus 10ml / kg intravenously can improve the microcirculation of rabbits with microcirculation disorder caused by high molecular meglumine, which shows that capillary or venule flow is restored and the flow rate is accelerated. In addition, the whole blood (specific) viscosity, plasma (specific) viscosity, red fine electrophoresis and platelet electrophoresis were restored [14]. The whole blood viscosity of rabbits was significantly decreased after intravenous injection of 20mg / kg Erigeron breviscapus injection; After intramuscular injection of 10mg / kg daily for 14 days, the whole blood viscosity was also significantly decreased at 3D and 7d after injection. However, there was no significant change in plasma viscosity [15].
4. cerebral vasodilation rabbits were intravenously injected with 5% breviscapine infusion lg/kg, and the cerebral vascular tension, peripheral vascular resistance, and peripheral blood pressure of rabbits were significantly decreased [1]. Breviscapine flavone 5x10 - g / ml had a significant tensile effect on isolated canine middle cerebral artery, and significantly inhibited the contraction of basilar artery by serotonin and middle cerebral artery by 15 methylprostaglandin F2a. Erigeron breviscapus has no obvious effect on vertebral artery flow in anesthetized dogs [5].
5. other effects mice received intraperitoneal injection of breviscapine 20mg/kg, the plasma cAMP content gradually increased in smin, reached the peak at 20min, and showed a dose-response relationship in the dose range of lmy/kg ~ 20my/kg, with mg/kg as the maximum effect dose [16]. Intragastric administration of 20% aqueous solution of Erigeron breviscapus extract 60g (crude drug) / kg to mice significantly prolonged the survival time of mice under normobaric hypoxia [1]. Baicalein has inhibitory effect on protein kinase C (PKC), with an IC50 of 48pmol / L. baicalein has shown inhibitory effect on PKC at A2 ± concentration of 10-2 to 10-7mol / L. this effect is not reversed by increasing the concentration of dioleoylglyceride or substrate histone, suggesting that the inhibitory effect of baicalein and other elements belongs to non competitive inhibition [17]. Erigeron breviscapus preparation can also improve the permeability of blood-brain barrier, resist platelet aggregation caused by adenosine diphosphate and improve the phagocytic immune function of macrophages [18].
6. in vivo process after intravenous injection of 3H scutellarin 10mg / kg in mice, the 3H content in blood showed a rapid downward trend within 60min. ; At 4h, there was more radioactivity in gallbladder, small intestine, liver and myocardium, and the distribution in brain was also significantly increased. After 24h, there was still some radioactivity distribution in gallbladder, small intestine and brain. After 3H scutellarin was intravenously injected into mice, the total amount of 24h excretion from urine was 19.1% of the injected amount, and the total amount of 24h excretion from feces was 24.l% of the injected amount [19].
7. toxic 20% aqueous solution of Erigeron breviscapus extract 0.4ml/kg (equivalent to crude drug 80g / kg) was given to male mice by gavage, and no death was observed for 3 days. Male mice were intraperitoneally injected with 5% Erigeron breviscapus extract solution, and LD50 was measured according to the simplified probability unit method. It was 13.14 ± 5.42g / kg, and the LD50 of i.v. It is 10.02 soil 1.55g / kg[1]. Subacute toxicity test proved that breviscapine had no effect on hemogram, liver and kidney functions, and no substantial changes in internal organs [18].
 
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