The pharmacology of Andrographis paniculata

Pharmacological effects

1. Antipyretic effect:

Both Andrographolide and New Andrographolide have the effect of inhibiting and delaying the increase of body temperature caused by Streptococcus pneumoniae and hemolytic Streptococcus species, and the latter is less effective than the former. Deoxyandrographolide, andrographolide, neoandrographolide, lactone, and dehydroandrographolide in fever-induced rats caused by typhoid paratyphoid vaccine or in 2,4-dinitrophenol Certain antipyretic effects, among which dehydroandrographolide has the strongest effect. By intraperitoneal administration of deoxyandrographolide and neo-andrographolide, fever rabbits caused by subcutaneous injections of both pneumococcus and hemolytic streptococcus cultures were able to delay the increase in body temperature and reduce the increase in body temperature.

2, anti-inflammatory effects:

Using xylene, acetic acid-induced increased capillary permeability of the skin or abdominal cavity, intragastric administration of deoxyandrographolide or dehydroandrographolide can reduce capillary wall exudation, compared with the control P<0.05 or P< 0.01. Hemorrhagic necrotizing exudation caused by croton oil in rats, deoxyandrographolide has a significant inhibitory effect. Deoxy-andrographolide, andrographolide and neo-andrographolide significantly inhibited leukocyte migration in rat CMC sac at 7.5 h at high doses of 100 mg/capsule. The experiment also observed that these four andrographolide had different levels of excitatory effects on the adrenocortical function of mice, and dehydroandrographolide was the strongest. Andrographolide and new andrographolide inhibit E. coli.

3, the impact on immune function:

Andrographis decoction can increase the ability of peripheral blood leukocytes to phagocytose Staphylococcus aureus in vitro. It has been reported that oral administration of andrographolide can increase the delayed skin hypersensitivity caused by old tuberculin in tumor patients and other patients or healthy people. Andrographolide injection also enhances phagocyte function. In vitro tests of 3H-thymidine infiltration into lymphocytes showed that the water-soluble derivative of Andrographis paniculata inhibited PHA-induced 3H-thymidine infiltration. Dehydroandrographolide succinic acid hemi-ester (DAS) synthesized with andrographolide also inhibited delayed-type hypersensitivity induced by 2,4-trinitrochlorobenzene in mice. Andrographolide significantly inhibited the clearance of carbon in the venous blood. Andrographolide, a new product of Andrographis paniculata (containing esters and ketones), can increase serum lysozyme levels in mice.

4. Effect on pituitary-adrenocortical system function:

Andrographis A, B, C 4g/kg, and SB 1g/kg were intragastrically administered to the young mice and intraperitoneal injection of dehydroandrographolide semisuccinic acid ester (DAS) 63-250 mg/kg once daily for 3 consecutive times Days can make the thymus atrophy, suggesting that it has an adrenocortical function. Dehydration of andrographolide 125-250mg/kg intraperitoneal injection of 5 days, can significantly reduce the rat adrenal vitamin C content, 250mg/kg dose group rats ACTH content in the anterior pituitary slightly higher than the control group. DAS reduces the effect of vitamin C content in the adrenal glands and completely disappears after the removal of the pituitary. DAS of the juvenile rat that excised the adrenal gland cannot prolong its survival time. It suggests that DAS itself has no corticosteroid-like effects, but can excitate the anterior pituitary function, promote the synthesis and release of ACTH, thereby enhancing the adrenocortical function. After anesthesia with sodium pentobarbital in rats, DAS can still make adrenal vitamin C The content is reduced. However, on the basis of pentobarbital anesthesia, morphine, dexamethasone, chlorpromazine, etc. can completely block the DAS to reduce the content of vitamin C in the adrenal glands, indicating that the site of action of the DAS excitatory neuro-pituitary-adrenocortical system may be The subcortical center.

5. Effects on cardiovascular and blood systems:

According to reports, experimental coronary thrombotic myocardial infarction dogs intravenous injection of total flavonoids 4g/kg (a considerable crude drug 4g), can significantly improve the epicardial electrocardiogram. Pathological examination showed no thrombosis in the coronary arteries. Intimal shedding of the damaged coronary artery showed only intimal shedding and a little platelet aggregation, as well as adhesion of red and white blood cells. Most of the animal's myocardial sections were normal, and there was no significant change in CK-MB. Intravenous injection of total flavonoids (4g/kg) in dogs with myocardial infarction also reduced platelet aggregation induced by ADP, shortened the dissolution time of euglobulin, and decreased the TXB2 content in blood. The level of 6-keto-PGF1a was significantly increased, and platelet cAMP was also increased. Increased, suggesting that total flavonoids inhibit platelet aggregation and thrombosis and inhibit the production of TxA2, promote the formation and release of endothelial vascular endothelial PGI2, stimulate platelet cAMP increase and promote fibrinolysis. In vitro experiments, total flavonoids 0.125mg/ml can significantly inhibit ADP-induced human platelet aggregation, in the range of 0.125-1.0mg/ml dose strength was positively correlated with the dose. 0.1-5.0 mg/ml also significantly shortens the dissolution time of euglobulin. The total flavonoids of Andrographis paniculata can also significantly reduce the myocardial uptake rate in rats, and it has a protective effect on isoprenaline-induced myocardial injury and experimental ischemic infarct injury.

6, anti-venom and muscarinic effects:

The 50 or 100 mg water-soluble fraction of the ethanol extract of Andrographis in mice was able to prolong the time of respiratory failure and death caused by cobra venom poisoning in mice. This extract can cause blood pressure drop in dogs and physostigmine can be obtained. This effect was enhanced, while atropine was blocked, and both antihistamines and -blockers had no effect; extracts inhibited heart frogs, but this effect was also blocked by atropine. The extract also caused guinea pig ileum contraction, physostigmine enhanced its effect, atropine also blocked its effect, and antihistamines had no significant effect. The extract does not have any effect on the frog rectus muscle. It showed that the extract of Andrographis paniculata had no effect on nicotinic receptor activity, but showed obvious muscarinic effects, which may be the mechanism of its anti-venom effect.

7, stop pregnancy effect:

Mice were intraperitoneally injected with 10g (crude drug)/kg of Andrographis decoction daily for 2 consecutive days, with significant anti-implantation and early, middle and late pregnancy effects; daily intramuscular injection (12.5 g/kg), subcutaneous injection ( 12.5g/kg), gavage (25g/kg), intravenous injection (6.25g/kg), 2 days or intrauterine injection (2.5g/kg) can also terminate early pregnancy, including intraperitoneal injection, The effect of intravenous injection is best; the effect of intrauterine administration is also good, and the amount is small. It has the same effect on early pregnancy rabbits. Intravenous injection of andrographolide 625 mg/kg intravenously in early pregnant mice once daily for 2 consecutive days can also cause miscarriage. Exogenous progesterone and luteinizing hormone-releasing hormone have protective effects on early abortion caused by andrographis paniculata. Dehydration of andrographolide derivative -4 has a good anti-pregnancy effect in both mice and rats.

8, liver and gallbladder effects:

Andrographis has a beneficial effect on rats and can increase liver weight in rats. Intraperitoneal injection of andrographolide can significantly increase bile flow in rats. The physical properties of the bile that it secretes also change. Andrographolide also prevented liver toxicity caused by CCl4, D-galactosamine (800 mg/kg) and acetaminophen (3 g/kg, orally), and significantly reduced the levels of SGPT, SGOT, SALP, and HTG.

9, anti-tumor effect:

Dehydrated andrographolide succinic acid half ester has a certain inhibitory effect on W256 transplanted tumors. The arginine double salt (OASKARG) made from the dehydroabietide and potassium hydrogen ester of disuccinic acid disuccinic acid may inhibit the DNA synthesis of cultured breast cancer cells.

10, other roles:

Andrographolide and its derivatives have inhibitory effects on human gastric cancer cell KATO-lll. The n-hexane extract of Andrographis paniculata has a certain inhibitory effect on aldose reductase in bovine eye lens. Andrographis has a beneficial effect on the gallbladder in rats, and can increase the liver weight of rats and shorten the sleep time caused by ringworm exposure to barbiturates. Ethanol extracts are antagonistic to diarrhea caused by E. coli enterotoxins. Andrographis can increase the function of the adrenal cortex. Andrographine A, B, C, and D can make thymus atrophy in young mice at higher doses.

The intraperitoneal injection of ethanol extract of Andrographis can significantly prolong the time of respiratory failure and death caused by cobra venom poisoning in mice. Physostigmine enhances this effect, and atropine blocks this effect. Antihistamines and beta-blockers have no effect on this effect. Andrographis showed obvious muscarinic effects, but had no effect on nicotinic receptor activity.


Acesulfame K

Acesulfame K,Sweeteners In Food,Acesulfame Potassium,Acesulfame K Sweetener

CHANGZHOU GUANGHUI FOOD INGREDIENTS CO.,LTD , https://www.gsweetfood.com