Effects of Andrographolide
Andrographis paniculata (scientific name: Andrographis paniculata (Burm. f.) Nees), also known as Spring Lotus and Autumn Willow, is a favorite at first sight, as well as Elephantia paniculata, gallbladder, golden herb, golden ear hook, Indian grass, bitter grass, etc. Annual herbaceous plant, 4 to 8 cm long and 1 to 2.5 cm wide. Medicinal plants have the effects of clearing heat, detoxifying, reducing inflammation, reducing swelling and analgesic.
アンドログラフォリド Distribution
It is commonly cultivated in Fujian, Guangdong, Hainan, Guangxi, and Yunnan in my country, and has also been introduced in Jiangsu and Shaanxi; its origin may be in South Asia. It is also cultivated in Australia.
Andrographolide main ingredient
The leaves contain diterpene lactone compounds: Andrographis A is deoxyandrographolide with more than 0.1%, Andrographis B is andrographolide with more than 1.5%, Andrographis C is neoandrographolide with more than 0.2%; and high andrographolide, Pennilactone. Also contains andrographol, andrographone, andrographol, β-sitosterol-D-glucoside, etc.
In addition to andrographolide, it also contains 5-hydroxy-7,8,2′,3′-tetramethoxyflavone and 5-hydroxy-7,8,2′-trimethoxyflavone. , 5,2′-dihydroxy-7,8-dimethoxyflavone, apigenin-7,4′-dimethyl ether, α-sitosterol, etc.
The whole plant still contains 14–deoxy–11–oxyandrographolide, 14–deoxy–11,12–didehydroandrographolide, and according to preliminary analysis, it also contains sterol saponins and sugars. and phenolic substances such as condensed tannins.
Three kinds of sesquiterpene lactone compounds were obtained from the callus tissue obtained from leaves, twigs, hypocotyls, roots and germs through culture and separation: eleminolide A, B and C.
アンドログラフォリド Pharmacological effects
Andrographolide antipyretic effect
Both andrographolide and neoandrographolide have the effect of inhibiting and delaying the increase in body temperature caused by pneumococci and hemolytic B streptococci, but the latter is less powerful than the former. For rabbits with fever caused by typhoid paratyphoid vaccine or rats with fever caused by 2,4-dinitrophenol, deoxyandrographolide, andrographolide, neoandrographolide, lactone, and dehydrated andrographolide are all It has a certain antipyretic effect, among which dehydrated andrographolide has the strongest effect. Intraperitoneal injection of deoxyandrographolide and neoandrographolide suspension can delay the rise in body temperature and attenuate the degree of body temperature rise in rabbits with fever caused by simultaneous subcutaneous injection of pneumococcal and hemolytic streptococcus cultures.
Andrographolide anti-inflammatory effect
The capillary permeability of the skin or abdominal cavity of mice was increased due to xylene and acetic acid, and intragastric administration of deoxyandrographolide or dehydrated andrographolide could reduce the leakage of capillary walls. Compared with the control, P<0.05 or P< 0.01. Deoxyandrographolide has a significant inhibitory effect on hemorrhagic necrotic exudation caused by croton oil in rats. Deoxyandrographolide, andrographolide and neoandrographolide had a significant inhibitory effect on the migration of leukocytes in rat CMC cysts for 7.5 hours at a large dose of 100 mg/bag. The experiment also observed that these four kinds of andrographolide have varying degrees of stimulating effects on the adrenocortical function of mice, with dehydrated andrographolide being the strongest. Andrographolide and neoandrographolide have the effect of inhibiting Escherichia coli.
Andrographolide Impact 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 oral administration of Andrographis paniculata can enhance the delayed skin hypersensitivity reaction caused by old tuberculin in tumor patients and other patients or healthy people. Andrographis A injection can also enhance phagocyte function. In vitro experiments on the penetration of 3H-thymidine into lymphocytes showed that Andrographis paniculata water-soluble derivative injection has an inhibitory effect on PHA’s promotion of 3H-thymidine penetration. Dehydrated andrographolide succinate half-ester (DAS) synthesized from andrographolide also has an inhibitory effect on delayed-type hypersensitivity in mice induced by 2,4-trinitrochlorobenzene. Andrographolide can significantly inhibit the carbon clearance rate in venous blood. Andrographis paniculata preparation Xindipin (containing esters and ketones) can increase serum lysozyme levels in mice.
Andrographolide effects on pituitary-adrenocortical system function
Andrographis A, B, C 4g/kg and Dingulin 1g/kg were administered to young mice by gavage, and dehydrated andrographolide succinate half ester (DAS) 63~250mg/kg was intraperitoneally injected once a day for 3 consecutive days. It can cause the thymus to atrophy every day, suggesting that it can enhance the function of the adrenal cortex. Intraperitoneal injection of dehydrated andrographolide 125~250mg/kg for 5 days can significantly reduce the content of vitamin C in the adrenal glands of rats. The ACTH content in the anterior pituitary gland of rats in the 250mg/kg dose group was slightly higher than that in the control group. The effect of DAS on reducing the content of vitamin C in the adrenal gland disappears completely after the pituitary gland is removed. DAS cannot prolong the survival time of young rats with adrenalectomy. It is suggested that DAS itself has no adrenocortical hormone-like effects, but it can stimulate the function of the anterior pituitary gland, promote the synthesis and release of ACTH, thereby enhancing the adrenal cortex function. After rats were anesthetized with sodium pentobarbital, DAS can still increase the amount of vitamin C in the adrenal glands. content decreased. However, based on pentobarbital anesthesia, morphine, dexamethasone, chlorpromazine, etc. can completely block DAS and reduce the content of vitamin C in the adrenal gland, indicating that the site of action of DAS on the excitatory nerve-pituitary-adrenocortical system may be in Subcortical centers.
Andrographolide effects on the cardiovascular and blood systems
It is reported that intravenous injection of 4g/kg total flavonoids (equivalent to 4g crude drug) in dogs with experimental coronary thrombosis myocardial infarction can significantly improve the epicardial electrocardiogram. Pathological examination showed no thrombosis in the coronary arteries. Only intima detachment and a little platelet aggregation and red and white blood cell adhesion were seen in the damaged coronary intima. The myocardial sections of most animals were normal, and no obvious changes were found in CK-MB. Intravenous injection of total flavonoids 4g/kg in dogs with myocardial infarction can also reduce ADP-induced platelet aggregation, shorten euglobulin dissolution time, reduce blood TXB2 content, significantly increase 6-keto-PGF1a, and platelet cAMP also increased, suggesting that the inhibitory effect of total flavonoids on platelet aggregation and thrombosis is related to inhibiting the production of TxA2, promoting the production and release of PGI2 in the endothelium of the blood vessel wall, stimulating the increase in platelet cAMP, and promoting fibrinolysis. In vitro experiments show that total flavonoids at 0.125mg/ml can significantly inhibit ADP-induced human platelet aggregation, and the intensity of the effect is positively correlated with dose within the range of 0.125~1.0mg/ml. 0.1~5.0mg/ml can also significantly shorten the euglobulin dissolution time. The total flavonoids of Andrographis paniculata root can also significantly reduce the myocardial ytterbium uptake rate in rats, and have a certain protective effect on myocardial damage caused by isoproterenol and experimental myocardial infarction ischemic damage.
Andrographolide antivenom and muscarinic effects
Intraperitoneal injection of 50 or 100 mg/mouse of the water-soluble part of Andrographis paniculata alcohol extract can significantly prolong the respiratory failure and death time of mice caused by cobra venom poisoning. This extract can cause a decrease in blood pressure in dogs, and physostigmine can Enhance this effect, while atropine can block it, antihistamines and receptor blockers have no effect; the extract can inhibit the frog heart in vivo, but this effect can also be blocked by atropine. The extract can also cause guinea pig ileum contraction, physostigmine can enhance its effect, atropine can also block its effect, and antihistamines have no obvious effect. The extract had no effect on the frog rectus abdominis muscle. It shows that Andrographis paniculata extract has no effect on nicotinic receptor activity, but shows obvious muscarinic effects, which may be the mechanism of its antivenom effect.
Andrographolide termination of pregnancy
Mice were intraperitoneally injected with Andrographis paniculata decoction 10g (crude drug)/kg daily for 2 consecutive days, which had significant anti-implantation and aborted early, middle and late pregnancy effects; daily intramuscular injection (12.5g/kg), subcutaneous injection (12.5g/kg), intragastric administration (25g/kg), intravenous injection (6.25g/kg) for 2 consecutive days or intrauterine injection (2.5g/kg) once can also terminate early pregnancy, among which intraperitoneal injection , intravenous injection has the best effect; intrauterine administration also has good effect, and the dosage is small. It has the same effect on early pregnancy rabbits. Intravenous injection of Andrographis paniculata 625 mg/kg once a day for 2 consecutive days in early pregnant mice can also cause miscarriage. Exogenous progesterone and luteinizing hormone-releasing hormone have protective effects on early abortion caused by Andrographis paniculata. Dehydrated andrographolide derivative–Pan–4 has good anti-early pregnancy effects on mice and rats.
Hepatoprotective and choleretic effect
Andrographis paniculata has a choleretic effect in rats and increases liver weight in rats. Intraperitoneal injection of andrographolide can significantly increase bile flow in rats. The physical properties of the bile secreted by it also change. Andrographolide can also resist the hepatotoxic effects caused by CCl4, D-galactosamine (800mg/kg) and acetaminophen (3g/kg, oral), and significantly reduce the levels of SGPT, SGOT, SALP and HTG.
アンドログラフォリド anti-tumor effect
Dehydrated andrographolide succinate half-ester has a certain inhibitory effect on W256 transplanted tumors. The arginine double salt (OASKARG) made from dehydrated andrographolide disuccinate half-ester potassium hydrogen may have an inhibitory effect on DNA synthesis in cultured breast cancer cells.
Andrographolide other functions
Andrographolide and its derivatives have inhibitory effects on human gastric tumor cells KATO-llll. The n-hexane extract of Andrographis paniculata has a certain inhibitory effect on aldose reductase in the bovine lens. Andrographis paniculata has a choleretic effect in rats, and can increase rat liver weight and shorten cyclohexobarbital-induced sleep time. Ethanol extract has an antagonistic effect on diarrhea caused by Escherichia coli enterotoxin.
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