Andrographolide

【 English name 】Andrographolide

【 Traits 】This article is whitish crystalline; Odourless, bitter taste.

This product is dissolved in boiling ethanol, slightly soluble in methanol or ethanol, and practically insoluble in water.

【 Specifications 】25 kg / bucket

【 Pharmacological effects 】Andrographolide, the major active ingredient of the natural plant Andrographis paniculata, has the efficacy of expectorant heat detoxification, anti-inflammatory and pain relief, and is particularly effective against bacterial and viral upper respiratory infections and dysentery, and has been hailed as a natural antibiotic drug. This product is a diterpenoid lactone compound, all poorly soluble in water and usually capable of oral administration only.

1. Anti pathogen microbial effects

Animal studies showed that andrographolide and new andrographolide both inhibited and delayed the increase in body temperature caused by S. pneumoniae or S. haemolyticus group B, although andrographolide was more potent than new andrographolide.

In vitro experiments showed that Andrographis paniculata has some anti HIV effect.

2. Antipyretic effect andrographolide has different degrees of antipyretic effect on fever induced by endotoxin, pneumococcus, or hemolytic streptococcus in rabbits. The antipyretic effects of Andrographis paniculata, B, C, and D were sequentially attenuated in rabbits with fever caused by typhoid or paratyphoid vaccine, or in rats with fever induced by 2,4-dinitrophenol.

3. Anti inflammatory effects Andrographis paniculata (Andrographis paniculata), B, C, C, and d all showed various degrees of anti-inflammatory effects, and a 1 g / kg gavage inhibited the increase in skin or peritoneal capillary permeability induced by xylene or acetic acid in mice and reduced the amount of acute exudate induced by croton oil in the granulation sac of Selye but had no significant effect on granulation tissue proliferation. Was able to inhibit the development of footpad in egg white rats, but the effect disappeared after adrenalectomy. The anti-inflammatory effect of butanol was the strongest, and propranolol, alphamartin and ethidin the second.

4. Effects on immune function of the body there are reports that Andrographis may have a role in some links of cellular immunity. Its water decoction improved the phagocytosis of Staphylococcus aureus by human leukocytes in vitro, and oral administration of Andrographis paniculata enhanced human dermal delayed type hypersensitivity response to old tuberculin. The Andrographis paniculata preparation, xinzhiping (intein esters and ketones), increases serum lysozyme levels and enhances phagocytosis of peritoneal macrophages and neutrophils in mice. Continuous administration of andrographolide sulfonate to rabbits or mice significantly increased phagocytosis of pneumococcus or Staphylococcus aureus by peripheral blood phagocytes, which was also enhanced by andrographolide and camptothecin. The delayed type hypersensitivity reaction in mice induced by 2,4-dinitrochlorobenzene was also inhibited by dehydroandrographolide succinate half ester.

5. Anti fertility effects Andrographis paniculata has a significant effect of aborted pregnancy. Andrographis paniculata orally enables contraception in mice and abortion in pregnant rabbits. Intraperitoneal injection of the water decoction significantly aborted implantation, early pregnancy, middle and late pregnancy in mice at different stages. Intramuscular, subcutaneous, gavage, intraperitoneal, intravenous and intrauterine injections have all been shown to produce anti first trimester efficacy, with abdominal, intravenous and intrauterine injections having the best efficacy. Intrauterine injection, the dosage is both small and effective. Exogenous progesterone or luteinizing hormone releasing hormone (LH-RH) injected concomitantly with Andrographis paniculata prevents miscarriage, suggesting that Andrographis may act against progesterone in vivo to cause miscarriage. It has been suggested that Andrographis paniculata inhibits the growth of placental villous trophoblast cells in vitro. Studies have shown that some semisynthetic derivatives of andrographolide also have varying degrees of anti first trimester effects, and a dehydrated andrographolide derivative, perforin-4, has shown good anti first trimester effects in mice and rats and is a contraceptive drug that warrants further investigation in the context of a significant effect on placental trophoblasts, resulting in placental villous atrophy and reduced cell numbers, Syncytia and Langhan cells disappeared, interstitial edema and hemorrhage.

6. Choleretic and hepatoprotective effects Andrographis paniculata has choleretic effects on rats and can increase the liver weight of rats and shorten the sleep time induced by cyclohex - ababituo sodium. Prior administration of andrographolide to combat the hepatotoxic effects caused by carbon tetrachloride, D-galactosamine, and acetamide based phenols significantly reduced SGPT, SGOT, SALP, and HTG levels, respectively. Reported that methanol infusion of Andrographis paniculata is toxic and promotes death in rats with liver injury.

7. Antitumor effect dehydroandrographolide succinic half ester showed a certain inhibitory effect on W256 transplantable tumors. Potassium hydrogen hemisuccinate hemisuccinate of dehydroandrographolide was used to make arginine complex salt (named as perforin), which was effective on tumor cells regardless of the large, medium, or small dose, and the effect was enhanced with the increasing dose, so the tumor inhibition effect was real and stable. In vitro experiments demonstrated that Andrographis paniculata inhibited DNA synthesis in cultured breast cancer cells.

8. Other effects yansunin and pengsunin injection have obvious sedative effects, can shorten the latency period of penta - barbitura sodium to anesthesia in mice, prolong the duration of anesthesia, and can cause anesthesia by subthreshold amounts of penta - barbitura sodium.

Andrographolide increases adrenocortical function, and Andrographis alfa, B, C, C, and D can produce thymic atrophy in juvenile mice at larger doses.

【 Clinical application】

For dysentery, leptospirosis, meningitis, pneumonia, enhanced adrenocortical function, upper respiratory tract infections. In response to the demand of viral infection emergencies in the clinic, different hydrophilic groups were introduced into the lactone structure to enhance its water solubility and improve the efficacy. Since then, several kinds of needles have been developed for andrographolide, and the more widely used clinically are andrographolide needles, yansuning needles, and lianbiji needles, which are representative medicines of this class, and have been classified as one of the necessary medicines in emergency departments by the Ministry of health and the State Administration of traditional Chinese Medicine (TCM).

【 Approval No.】NMPN H51023720