1、 Pharmacopoeia standard of Aconitum carmichaeli
Aconitum carmichaeli
Chuanwu
ACONITI RADIX
This product is Aconitum from RanunculaceaeAconitum carmichaelii Debx.Dried mother root of.6From the last ten days of the month to8Excavate in the first ten days of the month, remove the roots, fibrous roots and silt, and dry them in the sun.
[character] this product is irregular conical, slightly curved, and often has residual stems at the top. The middle part tends to expand on one side and is long2～7.5cm, diameter1.2～2.5cm. the surface is tan or grayish brown, wrinkled, There are traces of small tumor like lateral roots and daughter roots after detachment. The texture is solid, the section is white or light grayish yellow, and the ring pattern of the cambium is polygonal. It has slight air, spicy taste and tingling tongue.
[identification]（1）; Stone cells are occasionally seen in cortical parenchyma, scattered singly or in groups, like rectangle, square or long oval, and the cell cavity Larger; The endothelial layer is not very obvious. Sieve tube groups were scattered in phloem; Fiber bundles were occasionally seen in the medial side. Cambium is polygonal. Occasionally on the inside and outside1To several heterotypic vascular bundles. Xylem vessels are many rows, radial or slightly “V”Shape arrangement. The medulla is obvious. Parenchyma cells were filled with starch granules.
The powder is grayish yellow. The starch granules are spherical, oblong or reniform in shape, with a diameter of3～22μm; compound granules are made of2～15Granulation composition. The stone cells are nearly colorless or yellowish green, and are rectangular, square, and polygonal Shape or one side oblique tip, diameter49～117μm, long113～280μm, wall thickness4～13μm. The metazoan cortical cells are brown, and some of the walls are thickened and protrude into the cell cavity. The duct is light yellow, mainly with marginal pits, diameter29～70μmThe end is flat cut or short pointed, the perforation is located in the end wall or side wall, and some duct elements are thick and short, curved or vertically and horizontally connected.
（2）Take this product powder2g, ammonia test solution2mlWetting, adding ether20ml, sonication30Min, filtered, the filtrate evaporated, and dichloromethane was added to the residue1mlDissolve as test solution. Take another Cephaline reference, hypaconitine reference and mesaconitine reference, plus isopropanol-（1：1）The mixed solution was made into each1mlEach containing1mgAs the control solution. According to thin layer chromatography Law (General0502）Test, aspirate the above two solutions5μl, respectively, on the same silica gelGThin layer plate with n-hexane-ethyl acetate-Methanol（6.4：3.6：1）As developing agent, saturated with ammonia vapor20 Minutes in the unfolding cylinder, unfold, take out, dry, and spray with dilute bismuth potassium iodide test solution. In the chromatogram of the test sample, spots with the same color appear at the corresponding position of the chromatogram of the control sample.
[inspection] the water content shall not be too high12.0%(General0832The second method).
Total ash content shall not exceed9.0%(General2302）。
Acid insoluble ash content shall not exceed2.0%(General2302）。
[content determination] according to HPLC (general rules0512）Assay.
Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; With acetonitrile-Tetrahydrofuran（25：15）A, to0.1mol/LAmmonium acetate solution (per1000mlplus Glacial acetic acid0.5ml）B, gradient elution according to the following table; The detection wavelength was235nmThe number of theoretical plates calculated according to the peak of mesaconitine should not be less than2000。
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Time (minutes) mobile phaseA(%) mobile phaseB（％）
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0~48 15→26 85→74
48~49 26→35 74→65
49~58 35 65
58~65 35→15 65→85
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Preparation of reference solution take an appropriate amount of aconitine reference, hypaconitine reference and mesaconitine reference, weigh accurately, and add isopropanol-（1：1）The mixed solution was made into each1ml Aconitine containing50μg, hypaconitine and mesaconitine, respectively0.15mgA mixed solution of.
Preparation of test solution take the powder of this product (passing through No. 3 screen) for about2g, weigh accurately, place in a corked conical flask, and add ammonia test solution3ml, precision addition of isopropanol-（1：1）Mixed solution 50ml, weighed, sonicated (power300W, frequency40kHZ; water temperature at25℃Below)30Minutes, let cool, weigh again, and use isopropanol-（1：1）The mixed solution makes up for the lost . Precise measurement of continuous filtrate25ml，40℃The solvent was recovered to dryness under reduced pressure, and isopropanol was precisely added to the residue-（1：1）Mixed solution3mlDissolve, filter, take the continuous filtrate, Ready to get.
The determination method accurately aspirates the reference solution and the test solution respectively10μl.
This product is calculated as dry product and contains Aconitine（C34H47NO11）, hypaconitine（C33H45NO10）And mesaconitine（C33H45NO11）The total amount of should be0.050%～0.17%。
Decoction pieces
. Mash when needed.
[character], [identification], [inspection], [content determination] are the same as those of medicinal materials.
[nature, taste and meridian tropism] pungent, bitter and hot; It is highly toxic. Homing, liver, kidney and spleen meridians.
[functions and indications] dispel wind and dampness, warm meridians and relieve pain. It is used for wind cold dampness arthralgia, joint pain, cold pain in the heart and abdomen, cold hernia pain and anesthesia pain relief.
[usage and dosage] generally used after processing.
[note] it is advisable to take raw products with caution; Forbidden for pregnant women; It is not suitable to mix with Pinellia ternata, Fructus Trichosanthis, Fructus Trichosanthis, pericarpium trichosanthis, trichosanthin, Fritillaria chuanensis, Fritillaria zhejianensis, Fritillaria pingensis, Fritillaria yiensis, Fritillaria hupehensis, Cayratia japonica, white and With.
[storage] store in a ventilated and dry place to prevent moths.
Tuberous root (parent root) containsAconitine（aconitine），Hypaconitine（hypaconitine），Mesoaconitine（mesaconitine），Talamine（talatisamine）， Demethylcoclaurine, isotalatizidine, neoline,Aconitine Junggar（songorine），Aconitine（fuziline）， Salsolinol, isodelphinine,Benzoyl ZhongwuBenzoylmesaconitine,Aconitine Polygonum（karakoline）， Senbusine a, senbusine B, 14 acetyltalatisamine, lipoaconitine, lipohypaconitine, lipodeoxyaconitine, lipomesaconine, beiwutine, chuanfunine,3-deoxyaconitine（3-deoxyaconitine）， Ignavine, hokbusine A and B, uracil, aconitan a, B, C, D.
3、 Pharmacological effects of Radix Aconiti
1. effects on the heart. Aconitine initially slowed down the heart rate of isolated and eutopic frog hearts (which could be blocked by atropine), then due to the high stimulation of the myocardium, the heart rate suddenly increased, the cardiac contractility strengthened, and soon the heart rhythm disorder appeared, the cardiac contractility weakened, the cardiac contraction was mulberry like, and finally the heart stopped. Its therapeutic dose can slow down the heart rate, make the pulse soft and weak, and reduce the blood pressure slightly (excite the vagal Center);
1.1 fibrillation: aconitine poisoning is very easy to produce ventricular fibrillation, which is believed to be caused by increased myocardial excitability, membrane destruction polarization, high-frequency ectopic rhythm of the myocardium, etc., which can be inhibited by high concentration of calcium. It is believed that under the influence of cholinergic factors, the result of impulse wave multi-source reentry. .
1.2 cardiotonic effect: aconitine itself has no cardiotonic effect and is extremely toxic to the heart; The toxicity of aconine, the hydrolysate of aconitine, is only 1 / 2000-1 / 4000 of aconitine. It is said to have cardiotonic effect. It can resist aconitine induced arrhythmia in isolated frog heart
2. effects on blood pressure and blood vessels. Aconitine can reduce blood pressure. Chinese Aconitum and Chuanfu (cooked aconite tablets) Decoction can cause rapid and temporary hypotension in anesthetized dogs or cats. At this time, there is no obvious change in the heart, and the hypotension can be eliminated by a large amount of atropine or diphenhydramine. The device for measuring the terminal resistance showed that the decoction of cooked aconite tablets could cause significant dilation of blood vessels in the lower limbs, and could also dilate coronary vessels (independent of blood pressure and heart rate). It is said that the first aid Huiyang Decoction (aconite, camphor, ginseng, musk) has a pressor effect. Sini Decoction (aconite, dried ginger, licorice) also increases blood pressure in dogs with acute blood loss. However, Fugui decoction can reduce blood pressure in rats with nephrocutaneous hypertension (partial adrenal burn) and enhance the activity of the adrenal gland on the burned side (1-c14-sodium acetate incorporation test).
3. anti inflammatory effect and its relationship with adrenal cortex. The decoction of cooked aconite tablet (white aconite tablet) or black aconite tablet has obvious anti-inflammatory effect on formaldehyde and egg white ankle swelling by intraperitoneal injection or oral administration. . The alkaloid fraction isolated from Aconitum chinense and pure aconitine also had the effect of reducing ascorbic acid in adrenal gland, but the non alkaloid fraction was ineffective; In addition, the decoction of cooked aconite tablets can also increase the excretion of 17 ketosterol in the urine of rats and reduce the number of eosinophils in the peripheral blood of rats, so it has an excitatory effect on the pituitary adrenal cortex system. The histochemical method (mouse) study also proved that Aconite Decoction can reduce the content of cholesterol in adrenal cortex (indicating that adrenal cortical hormone secretion is exuberant), enhance phosphatase activity (indicating that adrenal cortical hormone enhances the metabolism of sugar, protein and fat) and promote the increase of liver glycogen. However, the content of ascorbic acid in adrenal gland of rats could not be reduced by oral administration of 1 g /100 g of heifu tablet Decoction (5 times larger than the dose reported above), once or for six consecutive times.
. Aconitine 0.1-0.2mg/kg could damage the electric defensive pole climbing conditioned reflex in rats, and the unconditioned reflex was also slightly damaged, and the ammonia content in all parts of the brain decreased sharply; Injection of 0.002 μ g/kg into the fourth ventricle of rabbits can cause anesthesia. It was proved that aconitine has certain analgesic effect by electrical stimulation of mouse tail, and scopolamine can enhance its efficacy. Aconitum in traditional Chinese medicine anesthesia compound, its analgesic effect can cooperate with the Flos Daturae, and can antagonize the accelerated heart rate and dry mouth caused by Flos Daturae. Chinese Aconitum decoction can increase the electric convulsion threshold of rabbits, but it can not prevent the maximum electric shock attack of rats.
5. other functions. Aconitine can inhibit the respiratory center and slow the respiration; The sensory nerve endings of local skin and mucosa were excited, itched and burned first, followed by paralysis and loss of consciousness; It can reflexively cause hypersecretion of saliva, so that fever and normal animal body temperature can be reduced. . It can inhibit bacteria in the test tube. Wuji powder can excite the uterine accessory ligament, vagina, uterus and duodenum. The crude extract of aconite or total sterols had no obvious effect on the body weight, levator ani muscle or kidney weight of rats and mice, indicating no assimilation and androgen like effects.