1、 Pharmacopoeia standard of Corydalis yanhusuo
Corydalis yanhusuo
Yanhusuo
CORYDALIS RHIZOMA
This product is the dried tuber of Corydalis yanhusuo W.T.WANG, a plant in the poppy family. .Yanhusuo
CORYDALIS RHIZOMA
[properties] the product is irregular oblate, with a diameter of 0.5 ~ 1.5cm. The surface is yellow or yellowish brown, with irregular reticular wrinkles. There are slightly concave stem marks at the top and pimple like protrusions at the bottom. It is hard and brittle, with yellow section, horny like and waxy luster. The breath is slight and the taste is bitter.
[identification] (1) the powder of this product is green and yellow. Gelatinized starch pellets are yellowish or nearly colorless. The thick walled cells of the lower epidermis are greenish yellow, and the cells are polygonal, square like or long strip-shaped. The walls are slightly curved, lignified, and some become bead like thickened, with fine pits. The diameter of threaded conduit is 16 ~ 32 µ M.
(2) Take 1g of the product powder, add 50ml of methanol, sonicate for 30 minutes, filter, evaporate the filtrate, add 10ml of water to dissolve the residue, add concentrated ammonia to adjust the test solution to alkaline, shake and extract three times with ether, 10ml each time, combine the ether solution, evaporate to dryness, add 1ml of methanol to dissolve the residue, and use it as the test solution. Another 1g of Corydalis Corydalis reference medicinal material was prepared into the reference medicinal material solution by the same method. Then take the tetrahydropalmatine reference substance and add methanol to make a solution containing 0.5mg per 1ml as the reference solution. According to the test of thin-layer chromatography (general rule 0502), absorb 2-3 µ l of each of the above three solutions, respectively dot them on the same silica gel G thin-layer plate prepared with 1% sodium hydroxide solution, use toluene acetone (9:2) as the developing agent, develop, take out, dry, put in an iodine tank for about 3 minutes, take out, volatilize the iodine adsorbed on the plate, and check under the ultraviolet light (365nm). In the chromatogram of the test sample, fluorescent spots of the same color appear at the positions corresponding to the chromatogram of the control medicinal material and the chromatogram of the control sample.
[check] moisture .
Total ash Not more than 4.0% (general rule 2302).
[extract] according to the hot leaching method under the alcohol soluble extract determination method (general rule 2201), using dilute ethanol as solvent, it shall not be less than 13.0%.
[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 (triethylamine adjusted to pH 6.0) (55:45); The detection wavelength was 280nm. The number of theoretical plates should not be less than 3000 according to the tetrahydropalmatine peak.
Preparation of reference solution Take an appropriate amount of tetrahydropalmatine reference substance, accurately weigh it, add methanol to make a solution containing 46 µ g per 1ml.
Preparation of test solution Take about 0.5g of this product powder (passing through No. 3 screen), weigh it accurately, place it in a flat bottomed flask, add 50ml of concentrated ammonia test solution methanol (1:20) mixed solution precisely, weigh it, soak it in cold for 1 hour, heat it to reflux for 1 hour, cool it, weigh it again, use concentrated ammonia test solution methanol (1:20) mixed solution to make up the weight lost, shake it well, and filter it. Accurately measure 25ml of the secondary filtrate, evaporate to dryness, add methanol to dissolve the residue, transfer to a 5ml volumetric flask, dilute to the scale, shake well, filter, and take the secondary filtrate.
Assay Precisely suck 10 µ l of the control solution and 10 µ l of the test solution respectively, inject them into the liquid chromatograph, and determine.
This product is calculated as dry product, and the content of tetrahydropalmatine (c21h25no4) shall not be less than 0.050%.
Decoction pieces
[processing] Corydalis yanhusuo .
This product is irregular round thick film. The outer skin is yellow or yellowish brown, with irregular fine wrinkles. The cut surface is yellow, horny and waxy. The breath is slight and the taste is bitter.
[content determination] the content of tetrahydropalmatine (c21h25no4) in the same medicinal material shall not be less than 0.040%.
[identification], [inspection], [extract] are the same as that of medicinal materials.
Vinegar Corydalis yanhusuo Remove the Rhizoma Corydalis, fry it according to the vinegar roasting method (general rule 0213), or boil it according to the vinegar boiling method (general rule 0213) until the vinegar is absorbed, cut it into thick pieces or mash it when used.
This product is shaped like Corydalis yanhusuo or tablet, with yellowish brown surface and cut surface and relatively hard quality. It has a slight vinegar aroma.
[content determination] the content of tetrahydropalmatine (c21h25no4) in the same medicinal material shall not be less than 0.040%.
[identification], [inspection], [extract] are the same as that of medicinal materials.
[nature, taste and meridian tropism] pungent, bitter and warm. Return to the liver and spleen meridians.
[functions and indications] activating blood circulation, activating qi and relieving pain. For chest and flank pain, abdominal pain, chest pain, dysmenorrhea, postpartum blood stasis, tumescent pain.
[usage and dosage] 3 ~ 10g; swallow the powder, 1.5 ~ 3G at a time.
[storage] store in a dry place to prevent moths.
2、 Chemical constituents of Corydalis yanhusuo
1. a total of more than 10 alkaloids have been proposed from the tubers of Corydalis yanhusuo, among which the identified ones areCorydalis a(Corydaline)、Tetrahydropalmatine(Tetrahydropalmatine)、Protoopioid(Protopine)、L tetrahydroberberineL-tetrahy-drocoptisine, l-tetrahy-drocolumbamine, corybulbine, β - homoche lidonine, l-tetrahy-drocoptisine, l-tetrahy-drocolumbamine, l-tetrahy-drocoptisine, l-tetrahy-drocoptisine, l-tetrahy-drocolumbamine, l-tetrahy-drocoptisine, l-tetrahy-drocoptisine, l-tetrahy-drocolumbamine, l-tetrahy-drocolumbamine, l-tetrahy-drocoptisine, l-tetraBerberine(Coptisine)、Dehydrocorydine(De-hydrocorydaline), alsoCordieramine baseCorydalmine (corydalmine), dehydrocoryndamine.
. It also contains protoopioid base. The tuber of Rhizoma Corydalis contains protoberberine alkaloids, including Corydaline and dehydrocoryzanine. Corydaline, corypalmine, l-tetrahydroberberine and coptisine. It also contains protoopioid alkaloids protoopioid and β - homochelerythrine. It also contains irritating volatile oil.
3. the tuber of Euphorbia tuberosa contains protoopioid, l-tetrahydroberberine, bicuculline, Cymene a (c23h23o7n, MP 205 ℃), Cymene B (c18h19o6n, MP 191-192 ℃). Corydalisbulbosavar.canonical. (c.remotamaxim.) from North Korea contains protoberberine alkaloids: berberine, hydrogenated berberine, tetrahydroberberine, berberine, tetrahydrocorysamine, tetrahydrotetrandrine and sculerine; ; And protoopioid alkaloids: protoopioid, β - homochelerythrine (or α - allocryptopine). It also contains hydroxystreptomycin, stigmasterol, oleic acid, linoleic acid, linolenic acid, etc.
3、 Pharmacological action of Corydalis yanhusuo
1. effects on the central nervous system: 1.1. analgesic effect: the method of electrically stimulating mouse tail proved that Ig Corydalis powder has analgesic effect, its potency is 1/10 that of opioid, and the effect lasts for 2 hours. The hot plate method in mice proved that both Corydalis A and ugly element had significant analgesic effects. Rabbit b-heat stimulation and electrical summation stimulation proved that IV B 15-20mg/kg, ugly 10-15mg/kg or a 30-40mg/kg had analgesic effect. And B element and ugly element are the strongest, followed by a element. The analgesic effect of SC B 50mg/kg or ugly B 40mg/kg in rats was similar to that in rabbits. The analgesic effect of propolin on writhing reaction induced by intraperitoneal injection of acetic acid in mice and the analgesic test of electrical stimulation was also obvious, but weaker than that of morphine. ; The experiment also showed that B was not found to be addictive.
2.1. hypnotic, sedative and sedative effects: a large dose of tetrahydropalmatine has obvious hypnotic effects in rabbits, rats, dogs, monkeys and other tests. B could significantly reduce the spontaneous and passive activities of mice, but could not eliminate the righting reflex, showing no anesthetic effect. B can antagonize the central excitatory effects of caffeine and amphetamine and the convulsions caused by pentylenetetramine, but it can sensitize the convulsions caused by tudining. . Similar to chlorpromazine and reserpine. The sedative effect of ugly and caprine is weaker than that of B. the central action principle of B is that it can inhibit the electrical activity of cerebral cortex and subcortical, especially the cortical motor area is more sensitive. However, in the experiments of applying the drug solution directly on the cortex or isolated cortex, it has been proved that B does not directly affect the cortex. Injection of the drug solution into the brain ventricle can produce analgesic and sedative effects in large doses. B can significantly inhibit the wake-up reaction caused by stimulating the skin, and block the ascending activating system and descending sexual function of the reticular formation. All these prove that B has a certain selective effect on subcortical structures. B has a wide range of action sites, unlike morphine, which has a specific action site. Although its analgesic effect is not as powerful as morphine, it has a better sedative and sedative effect. The effects of optical isomers of B are also different. L-ethyl has analgesic and sedative effects, and larger doses have tremor in monkeys; On the contrary, dextrosomes have short-term excitatory effects. Both the left and right-handed bodies have the effect of sensitizing strychnine convulsion, but the right-handed body is more obvious. .
2. effect on digestive system: yanhusuo extract has excitatory effect on isolated intestine of guinea pig (1:1000-1:10000), but has no significant effect on isolated intestine of rabbit and rat. At the concentration of 1:2 × 10, ethoxylate could inhibit the activity of isolated rabbit intestine and block the excitatory effect of acetylcholine, barium chloride, pituitrin and 5-HT on intestinal muscle. B can antagonize the contraction induced by 5-HT in isolated rat stomach and colon. However, in whole animals, such as dogs with Pavlovian stomachs, 20-40mg/kg of B has no obvious effect on gastric juice secretion and gastric acid. When a large dose (80mg/kg) is applied, the secretion of gastric juice is significantly inhibited, and the acidity and digestibility of gastric juice are also weakened. Dehydrocyanhusol a can protect the experimental ulcer disease in rats caused by starvation or drugs (cortisone, lixueping), reduce the secretion of gastric juice, the amount of gastric acid and pepsin, and still have anti secretory effect after cutting the vagus nerve, so it can be seen that it has no blocking effect on the parasympathetic nerve. After IV of racemic tetrahydropalmatine on anesthetized open chest dogs, LVSP, dp/dtmax and VCE ± dp/dtmax showed obvious bidirectional effects of excitation first and then inhibition, and DL tetrahydropalmatine had anti arrhythmia effect.
3. effects on cardiovascular system: Corydalis Corydalis alcohol extract can significantly expand the coronary vessels of isolated rabbit hearts and in vivo cat hearts, reduce coronary resistance and increase blood flow. It has the most obvious dilation effect on the coronary artery of anesthetized dogs, followed by the internal carotid artery. It also has a certain dilating effect on the femoral artery, and its dilating effect may be one of the reasons for relieving pain. The ethanol extract of Corydalis can also increase cardiac output, reduce blood pressure and total peripheral resistance in anesthetized dogs, and has no obvious effect on left ventricular pressure and left ventricular dp/dtmax. It is suggested that Corydalis Corydalis does not enhance the contractility of the myocardium, and the increase in cardiac output may be due to the expansion of peripheral blood vessels. IP administration in mice could significantly increase the myocardial uptake of 86Rb. The total alkaloid of Corydalis yanhusuo (5 or 10mg/kgiv) can antagonize the abnormal electrocardiogram of guinea pigs caused by pituitrin. . It may have some preventive and therapeutic effects on myocardial infarction. The ethanol extract of Corydalis yanhusuo IP in mice can significantly improve the tolerance of animals to normobaric or hypobaric hypoxia. Total alkaloids of Corydalis yanhusuo have obvious therapeutic effect on aconitine induced arrhythmia in rats. The insoluble part of total alkali in water was significantly more than that in the same dose of total alkali treatment group, indicating that the components of aconitine arrhythmia exist in the water insoluble part, which may belong to the tertiary amine base part.
4. effect on the function of pituitary adrenal cortex system: after sc tetrahydropalmatine 50 or 70mg/kg (effective analgesic and diazepam dose) was given to rats, the content of vitamin C in adrenal gland decreased significantly, indicating that tetrahydropalmatine has the effect of exciting pituitary adrenal system. Injection of tetrahydropalmatine into hypophysectomized rats did not cause the decrease of adrenal vitamin C content, indicating that the effect of tetrahydropalmatine on stimulating the pituitary adrenal system is to cause the secretion of pituitary adrenocorticotropic hormone, rather than directly exciting the adrenal cortex. After injection of sodium pentobarbital 40mg/kg or prednisolone 15mg/kg into rats, the effect of tetrahydropalmatine on the release of pituitary adrenocorticotropic hormone disappeared, indicating that the site of action of tetrahydropalmatine may be in the hypothalamus. The rats were injected with tetrahydropalmatine 70mg/kg daily for 6 consecutive times, which significantly inhibited ACTH release induced by hypothermia (8 ℃ or 4 ℃).
5. relaxation effect on muscle the experiments of methyl tetrahydropalmatine and tetrahydropalmatine bromide on rabbits and guinea pigs in vitro showed that they had relaxation effect on their muscles.
6. pharmacological effects of processed products the analgesic effects of Corydalis yanhusuo made from vinegar and traditional vinegar were determined by mouse writhing method and hot plate method. The results showed that the analgesic effect of Corydalis yanhusuo made from vinegar was stronger than that of traditional vinegar (Table 9, table 10). The LD50 of Ig in mice were 135.765g/kg (traditional vinegar products); .