1、 Pharmacopoeia standard of Gentiana macrophylla
This product is the dried roots of Gentiana macrophylla pall., Gentiana straminea maxim., Gentiana crassicaulis duthie ex burk., or Gentiana dahurica fisch., which belong to the Gentianaceae family. The first three are conventionally called "Gentiana macrophylla" and "Gentiana straminea" according to their different characters, while the latter is conventionally called "Gentiana macrophylla". ; When Gentiana macrophylla and Gentiana straminea are softened in the sun and piled with "sweating" until the surface is reddish yellow or grayish yellow, they are spread out and dried, or directly dried without "sweating"; Take advantage of fresh Gentiana macrophylla to rub off the black skin and dry it in the sun.
[character] Gentiana macrophylla is cylindrical, thick at the top and thin at the bottom, not straight and twisted, 10 ~ 30cm long and 1 ~ 3cm in diameter. Its surface is yellowish brown or grayish yellow, with longitudinal or twisted wrinkles, and there are residual stem bases and fibrous leaf sheaths at the top. It is hard and brittle, easy to break, and the section is slightly oily, with yellow or brown skin and yellow wood. It has special flavor and tastes bitter and slightly astringent.
Gentiana straminea is cone-shaped, and it is mostly expanded by several small roots, with a diameter of 7cm. The surface is brown, rough, and has cracks and reticular pores. It is brittle and easy to break, and the cross section is mostly withered.
Gentiana macrophylla is conical or cylindrical in shape, 8 ～ 15cm long and 0.2 ～ LCM in diameter. The surface is brownish yellow. The main root is usually 1, the residual stem base has fibrous leaf sheath, and the lower part has many branches. The section is yellow and white.
[identification] (1) take 0.5g of this product powder, add 10ml of methanol, sonicate for 15 minutes, filter, and take the filtrate as the test solution. In addition, take gentiopicroside reference substance and add methanol to make a solution containing 1mg per 1ml as the reference substance solution. According to the thin-layer chromatography (general rule 0502), suck 5 μ l of the test solution and 1 μ l of the control solution, respectively dot them on the same silica gel gf254 thin-layer plate, use ethyl acetate methanol water (10:2:1) as the developing agent, develop, take out, dry, and view under the UV light (254nm). In the chromatogram of the test sample, spots with the same color appear at the corresponding position of the chromatogram of the control sample.
(2) Take quercitric acid reference substance and add chloroform to make a solution containing 0.5mg per 1ml as the reference solution. Test according to thin-layer chromatography (general rule 0502), suck 5 μ l of the test solution and 1 μ l of the above reference solution under item (1) of [identification], dot them on the same silica gel G thin-layer plate respectively, use chloroform methanol formic acid (50:1:0.5) as the developing agent, develop, take out, air dry, spray 10% sulfuric acid ethanol solution, heat at 105 ℃ until the spots are clear. 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 moisture content shall not exceed 9.0% (the second method of general rule 0832).
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Acid insoluble ash content shall not exceed 3.0% (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 24.0%.
[content determination] determine according to high performance liquid chromatography (general rule 0512).
Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile-0.1% acetic acid solution (9:91); The detection wavelength was 254nm. The number of theoretical plates should not be less than 3000 according to the gentiopicrin peak.
Preparation of control solution take appropriate amount of gentiopicroside control and loganic acid control, weigh accurately, and add methanol to make a solution containing 0.5mg gentiopicroside and 0.3mg loganic acid per 1ml respectively.
Preparation of test solution take about 0.5g of powder (passing through No. 3 screen), weigh accurately, place in a corked conical flask, add 20ml of methanol precisely, sonicate (power 500W, frequency 40KHz) for 30 minutes, cool, weigh again, make up the lost weight with methanol, shake well, filter, and take the filtrate. The determination method is to precisely suck 5 ～ 10 μ l of each of the two reference solutions and the test solution, inject them into the liquid chromatograph, and determine.
The total amount of gentiopicroside (c16h20o9) and loganic acid (c16h24o10) in this product shall not be less than 2.5% according to the calculation of dry product.
Decoction pieces
[processing] remove impurities, wash, moisten, cut into thick pieces, and dry.
This product is a thick round piece. The skin is yellowish brown, grayish yellow or tan in appearance, rough, with twisted longitudinal lines or reticulated pores. The skin of the cut surface is yellow or brownish yellow, the wood is yellow, and some centers are withered. It has special flavor and tastes bitter and slightly astringent.
[extract] the same as that of medicinal materials, not less than 20.0%.
[identification], [inspection], [content determination] are the same as those of medicinal materials.
[nature, taste and meridian tropism] pungent, bitter and peaceful. It belongs to the stomach, liver and gallbladder channels.
[functions and indications] dispel wind dampness, clear damp heat, stop arthralgia, and eliminate deficiency heat. It is used for rheumatic arthralgia, stroke hemiplegia, muscle and pulse contracture, arthralgia, damp heat jaundice, bone steaming hot flushes, infantile malnutrition and fever.
[usage and dosage] 3 ～ 10g.
[storage] place in a ventilated and dry place

2、 Chemical constituents of Gentiana macrophylla

1. the root of Gentiana macrophylla contains gentianine a, gentianine B, gentianine C,Gentiopicroside，SwertiamarinIt is also reported that the root of Gentiana macrophylla mainly containsGentiopicroside, when extracting and separating,GentiopicrosideIt can be converted into alkaloids such as longcholine and Gentiana alkaloid C by the action of ammonia. Recently, it has been reported that Gentiana macrophylla root containsGentiopicroside, lignitic acid), methyl lignonate,Quercitric acid， α - geraniol,β - sitosterol, β - sitosterol - β - D-glucoside β.

2. crude Gentiana macrophylla root containsGentiopicroside，Swertide，Swertiamarin, longcholine, Gentiana base C.

3. Gentiana straminea root containsGentiopicroside，Swertide，Swertiamarin, longcholine, Gentiana base C.

4. the root of Gentiana dahurica containsGentiopicroside，Swertiamarin, longcholine, Gentiana base C.

; The roots of Gentiana straminea in Tibet contain longcholine. Orocholine, isoorocholine, Tibetan orocholine; The root of Gentiana straminea var. tubulosa contains longcholine and Gentiana base C.

3、 Pharmacological effects of Gentiana macrophylla

1. anti inflammatory effect Gentiana alkaloid a can reduce formaldehyde induced arthritis in rats and accelerate the resolution of swelling. Daily intraperitoneal injection of 90mg/kg for 10 consecutive days can basically restore the swelling of the foot to normal, and its effect is equivalent to sodium salicylate 200mg/kg. If pre injected with Gentiana alkaloid a, it can also reduce and reduce the swelling of egg white induced foot swelling in rats. Its intensity of action is similar to chloroquine, corticosterone and Gentiana neutral ethanol extract, but slightly stronger than sodium salicylate. The anti-inflammatory effect principle of Gentiana alkaloid A is achieved by exciting the adrenal cortex, but it is different from corticotropin. It does not directly excite the adrenal cortex, and but through the nervous system to stimulate the pituitary gland, promote the secretion of adrenal cortical hormone to increase and achieve its anti-inflammatory effect. It is worth noting that the dihydrogen compound of Gentiana alkaloid a (the double bond on the side chain is saturated with hydrogen) has no anti-inflammatory effect, so the existence of the double bond is a necessary condition for anti-inflammatory. In addition, Gentiana alkaloid a can significantly reduce the increase of capillary permeability caused by egg white injection.

2. effects on the central system Gentiana base a has sedative effect on rats and mice at low doses, and can also enhance the hypnotic effect of pentobarbital sodium, but it has central excitatory effect at higher doses, and finally leads to paralysis and death. When injected at a small dose, it can inhibit the reflex intestinal fluid secretion caused by the infusion of mercurous chloride in dogs with intestinal flaccidity, that is, it inhibits the nervous system of dogs, and this inhibitory effect is strengthened with the increase of the dose. The experiment of photothermal stimulation showed that Gentiana base a could increase the pain threshold of rats, but the effect was short, and disappeared after 40 minutes. The hot plate test showed that Gentiana alkaloid a had analgesic effect on mice.

3. effects on cardiovascular system Gentiana alkaloid a can reduce the blood pressure of guinea pigs, and also has obvious and temporary blood pressure lowering effects on anesthetized dogs and rabbits. It can always slow down the heart rate without rapid tolerance. Intravenous injection of atropine and transection of both sides of the vagus nerve could not block its lowering effect. In addition, it had an inhibitory effect on isolated frog heart, slowing down the heart rate, accompanied by cardiac diastolic insufficiency and reduced cardiac output, which proved that its hypotensive effect was not related to the vagus nerve, and may be the result of direct inhibition of the heart.

. While increasing blood glucose, liver glycogen was significantly reduced. Its effect increases with increasing dose. Since this effect disappears after adrenalectomy or the use of epinephrine blocking drugs (diphenyl chloroethylamine), the principle of the effect of increasing blood glucose is through the release of the adrenal gland.

5. anti anaphylactic shock and antihistamine effects Gentiana alkaloid a can significantly alleviate asthma and convulsions caused by histamine spray in guinea pigs, and also has a significant protective effect on egg white anaphylactic shock in rabbits, and can significantly reduce capillary permeability in rats.

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. The dog artificial gastric flaccidity test showed that gentiopicroside could promote the secretion of gastric juice and free hydrochloric acid.