1、 Pharmacopoeia standard of Andrographis paniculata
This product is the dry aboveground part of Andrographis paniculata (burm.f.) nees, a plant of the family Andrographis paniculata. At the beginning of autumn, the stems and leaves are harvested and dried in the sun.
[character] the stem of this product is square columnar, multi branched, 50 ~ 70cm long, and the nodes are slightly expanded; . Simple leaves opposite, petioles short or subsessile; The leaves are shrunken and fragile. The intact ones are lanceolate or ovoid lanceolate after flattening, 3-12cm long and 2-5cm wide. The apex is gradually pointed, and the base is cuneate downward, full or wavy; The upper surface is green, the lower surface is grayish green, and both sides are smooth. The breath is slight and the taste is extremely bitter.
; There are glandular scales, and some non glandular hairs can be seen. Palisade tissue consists of 1-2 rows of cells, running through the upper part of the main vein; Spongy tissue is loosely arranged. The vascular bundle of the main vein is tough and grooved, and there are also crystal cells above the xylem.
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Laminar wavy. The lower epidermis is densely stomated, straight axis type, and the size of accessory guard cells varies greatly, and there are also indefinite types. The glandular scale has an oblate head, 4, 6 (8) cells, a diameter of 40 μ m, and a very short stalk. The non glandular hairs are 1-4 cells, about 160 μ m long, about 40 μ m in diameter at the base, and have cuticular texture on the surface.
(2) Take 0.5g of Andrographis paniculata reference medicinal material, add 30ml of ethanol, sonicate for 30 minutes, filter, and concentrate the filtrate to 5ml as the reference medicinal material solution. Then take the dehydrated andrographolide reference substance and andrographolide reference substance, add absolute ethanol to make a mixed solution containing 1mg per 1ml as the reference solution. According to the thin-layer chromatography (general rule 0502), suck 4 μ l of the test solution, the above reference medicinal material solution and the reference solution under the item of [content determination], respectively, dot them on the same silica gel gf254 thin-layer plate, use trichloromethane ethyl acetate methanol (4:3:0.4) as the developing agent, develop, take out, dry, and view under the UV light (254nm). In the chromatogram of the test sample, spots of the same color are displayed on the corresponding positions of the chromatogram of the control medicinal material and the chromatogram of the control sample respectively; Spray 2% 3,5-dinitrobenzoic acid ethanol solution -2mol/l potassium hydroxide solution (1:1) mixed solution (prepared temporarily), and immediately inspect under sunlight. In the chromatogram of the test sample, spots of the same color are displayed at the corresponding positions of the chromatogram of the control medicinal material and the chromatogram of the control sample.
[inspection] leaves shall not be less than 30%.
[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 8.0%.
[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; Methanol water (52:48) was used as mobile phase; The detection wavelength of andrographolide is 225nm, and that of dehydroandrographolide is 254nm. The number of theoretical plates should not be less than 2000 according to the peak of andrographolide and dehydroandrographolide.
Preparation of reference solution take an appropriate amount of andrographolide reference and dehydrated andrographolide reference, weigh accurately, add methanol to make a mixed solution containing 0.1mg per 1ml.
Preparation of test solution take about 0.5g of the powder (passing through No. 4 screen), accurately weigh it, place it in a corked conical flask, precisely add 25ml of 40% methanol, weigh it, soak it for 1 hour, sonicate it (power 250W, frequency 33khz) for 30 minutes, cool it, weigh it again, use 40% methanol to make up the lost weight, shake it well, and filter it. Accurately measure 10ml of the continuous filtrate, put it on a neutral alumina column (200-300 mesh, 5g, inner diameter 1.5cm), elute with 15ml of methanol, collect the eluent, put it into a 50ml volumetric flask, add methanol to the scale, shake well, and then get it.
The determination method is to precisely suck 5 μ l each of the reference solution and the test solution, inject them into the liquid chromatograph, and determine.
The total amount of andrographolide (c20h30o5) and dehydroandrographolide (c20h28o4) in this product shall not be less than 0.80% based on the dry product.
Decoction pieces
[processing] remove impurities, wash, segment and dry.
This product has irregular sections. The stem is square and columnar, and the nodes are slightly expanded. . The leaves are mostly shrunken or broken, and the intact ones are lanceolate or ovoid lanceolate after flattening. The apex is gradually pointed, and the base is cuneate and downward extended, full or wavy; The upper surface is green, the lower surface is grayish green, and both sides are smooth. The breath is slight and the taste is extremely bitter.
[identification] (except for the leaf cross section) is the same as that of medicinal materials.
[nature, taste and meridian tropism] bitter, cold. Homing, lung, large intestine, bladder meridian.
[functions and indications] it can clear away heat, detoxify, cool blood and reduce swelling. It is used for cold and fever, sore throat, sore mouth and tongue, cough and cough, diarrhea and dysentery, hot shower and pain, carbuncle and sore, snake and insect bite.
[usage and dosage] 6-9g. Suitable for external use.
[storage] put it in a dry place.

2、 Chemical constituents of Andrographis paniculata

The leaf contains diterpenoid lactones: andrographin a, i.eAndrographolide deoxygenatedMore than 0.1%, andrographin B i.eAndrographolideMore than 1.5%, Andrographis CNeoandrographolideMore than 0.2%; And andrographolide, panilactone. It also contains andrographane, andrographone, andrographsterol, β - sitosterol-d-glucoside, etc.
Eradicating the bacteria containingAndrographolideIn addition, it also contains 5-hydroxy-7,8,2 ', 3' - tetramethoxyflavone, 5-hydroxy-7,8,2 '- trimethoxyflavone, 5,2' - dihydroxy-7,8-dimethoxyflavone, apigenin-7,4 '- dimethyl ether, α - sitosterol, etc.
The whole herb also contains 14-deoxy-11-oxidized andrographolide14-deoxy-11,12-dihydroandrographolideAccording to preliminary analysis, it also contains sterol saponins, sugars, condensed tannins and other phenolic substances.
Three sesquiterpene lactones were isolated from the healed tissues obtained from leaves, twigs, hypocotyls, roots, and plumules through culture: elemene nuclide aElemene lotus lactoneB andElemene lotus lactoneC。

3、 Pharmacological effects of Andrographis paniculata
1. antipyretic effect: andrographolide and neoandrographolide have the effect of inhibiting and delaying the temperature rise caused by Diplococcus pneumoniae and hemolytic streptococcus B, while the latter is less powerful than the former. For rabbits with fever caused by typhoid and paratyphoid vaccine or rats with fever caused by 2,4-dinitrophenol, deoxyandrographolide, andrographolide, neoandrographolide, andrographolide and dehydroandrographolide have certain antipyretic effects, among which dehydroandrographolide has the strongest effect. The intraperitoneal injection of deoxyandrographolide and neoandrographolide suspension can delay the time of temperature rise and weaken the degree of temperature rise in rabbits with fever caused by simultaneous subcutaneous injection of pneumococcus and hemolytic streptococcus cultures.
2. anti inflammatory effect: the permeability of skin or abdominal capillaries in mice was increased by xylene and acetic acid. Intragastric administration of deoxyandrographolide or dehydroandrographolide could reduce the leakage of capillary walls, P < 0.05 or P < 0.01 compared with the control. Deoxyandrographolide has obvious inhibitory effect on hemorrhagic necrotic exudation induced by croton oil in rats. Deoxyandrographolide, andrographolide and neoandrographolide at a high dose of 100mg/ capsule for 7.5 hours significantly inhibited leukocyte migration in CMC capsules of rats. . Andrographolide and neoandrographolide can inhibit E. coli.
3. effect on immune function: Andrographis paniculata decoction can improve the ability of peripheral blood leukocytes to phagocytose Staphylococcus aureus in vitro. It has been reported that Andrographis paniculata can enhance the skin delayed hypersensitivity reaction caused by old tuberculin in tumor patients and other patients or healthy people. Andrographolide a injection can also enhance phagocyte function. . Dehydroandrographolide succinate (DAS), synthesized from andrographolide, also inhibited delayed type hypersensitivity induced by 2,4-trinitrochlorobenzene in mice. Andrographolide can significantly inhibit the clearance rate of carbon particles in venous blood. Andrographis paniculata preparation xindeping (containing ester and ketone) can increase the level of serum lysozyme in mice.
4. effect on the function of pituitary adrenal cortex system: Andrographis paniculata a, B, C 4g/kg and butyrin 1g/kg were given to young mice by gavage, and dehydrated andrographolide succinate half ester (DAS) 63-250mg/kg was injected intraperitoneally, once a day, for 3 consecutive days, all of which could make the thymus atrophy, suggesting the role of enhancing adrenal cortex function. . The effect of Das on reducing the content of vitamin C in the adrenal gland completely disappeared after the removal of pituitary gland. Das could not prolong the survival time of young rats with adrenalectomy. It is suggested that Das has no adrenocortical hormone like effect, but it can stimulate the function of anterior pituitary, promote the synthesis and release of ACTH, and thus enhance the function of adrenal cortex. After rats were anesthetized with sodium pentobarbital, DAS can still reduce the content of vitamin C in adrenal gland. However, on the basis of pentobarbital anesthesia, morphine, dexamethasone, chlorpromazine, etc. can completely block Das to reduce the content of vitamin C in the adrenal gland, indicating that the action site of Das to excite the nerve pituitary adrenal cortical system may be in the subcortical center.
5. effects on cardiovascular and blood system: it is reported that intravenous injection of total flavonoids 4g/kg (equivalent to 4G of crude drug) in dogs with experimental coronary thrombotic myocardial infarction can significantly improve epicardial ECG. According to pathological examination, no thrombosis was found in the coronary artery. Only intimal detachment, a few platelet aggregation and red and white blood cell adhesion were seen in the damaged coronary artery intima. Most animal myocardial sections were normal, and CK-MB did not change significantly. Intravenous injection of total flavonoids 4g/kg in dogs with myocardial infarction could also reduce ADP induced platelet aggregation, shorten the time of euglobulin dissolution, reduce the content of TXB2 in blood, significantly increase 6-Keto-PGF1a, and increase platelet camp, suggesting that the effect of total flavonoids on inhibiting platelet aggregation and thrombosis is related to inhibiting the production of TXA2, promoting the production of vascular endothelial PGI2, releasing, stimulating the increase of platelet camp, and promoting fibrinolysis. In vitro, total flavonoids 0.125mg/ml could significantly inhibit ADP induced human platelet aggregation, and the intensity of action was positively correlated with the dose in the range of 0.125-1.0mg/ml. 0.1-5.0mg/ml can also significantly shorten the dissolution time of euglobulin. The total flavonoids of Andrographis paniculata root can also significantly reduce the uptake rate of ytterbium in rat myocardium, and has a certain protective effect on myocardial injury caused by isoproterenol and experimental myocardial infarction ischemic injury.
6. anti snake venom and muscarinic effect: intraperitoneal injection of 50 or 100mg of the water-soluble part of Andrographis paniculata alcohol extract in mice can significantly prolong the time of respiratory failure and death in mice caused by cobra venom poisoning. This extract can cause the blood pressure of dogs to drop. Physostigmine can enhance this effect, while atropine can block it, and antihistamine and - receptor blockers have no effect; . The extract can also make the ileum of guinea pigs contract. Physostigmine can enhance its effect, atropine can also block its effect, and antihistamines have no obvious effect. The extract had no effect on frog rectus abdominis. The results showed that Andrographis paniculata extract had no effect on nicotinic receptor activity, but showed obvious muscarinic effect, which may be the mechanism of its antivenom effect.
7. pregnancy termination effect: mice were injected intraperitoneally with Andrographis paniculata Decoction 10g (crude drug) /kg daily for 2 consecutive days, which had significant anti implantation and early, middle and late pregnancy termination effects; Daily intramuscular injection (12.5g/kg), subcutaneous injection (12.5g/kg), gavage (25g/kg), intravenous injection (6.25g/kg), continuous 2 days or intrauterine injection (2.5g/kg) once can also terminate early pregnancy, among which intraperitoneal injection and intravenous injection are the best; The effect of intrauterine administration is also good, and the dosage is small. It has the same effect on early pregnant rabbits. Early pregnant mice were also induced to miscarry by intravenous injection of andrographolide 625mg/kg once a day for 2 consecutive days. Exogenous progesterone and luteinizing hormone releasing hormone have protective effects on Andrographis paniculata induced early abortion. .
8. hepatoprotective and choleretic effect: Andrographis paniculata has choleretic effect on rats and can increase the liver weight of rats. Intraperitoneal injection of andrographolide significantly increased bile flow in rats. The physical properties of the bile secreted by it have also changed. .
9. anti tumor effect: anhydroandrographolide succinate half ester has certain inhibitory effect on W256 transplanted tumor. .
10. other effects: andrographolide and its derivatives have inhibitory effects on human gastric tumor cell Kato lll. The n-hexane extract of Andrographis paniculata has a certain inhibitory effect on aldose reductase in bovine lens. Andrographis paniculata has cholagogic effect on rats, increases liver weight and shortens sleep time caused by cyclohexylbarbital. .