Natural antibiotic - Andrographolide
10/22/2025 14:14:47
Introduction to Andrographolide
Andrographolide is an organic substance with molecular formula C20H30O5, white square prism or flaky crystals. It is the main active ingredient of the natural plant Andrographis paniculata, which has the effects of removing heat and detoxification, anti-inflammatory and analgesic, and has special effects on bacterial and viral upper respiratory tract infections and dysentery. It is known as a natural antibiotic drug. This product is a diterpenoid lactone compound, which is difficult to dissolve in water and can usually only be administered orally.
Physical properties
Properties: White square prism or flaky crystals (ethanol or methanol), odorless, bitter. Powdered into white powder, 80 mesh.
Solubility: Soluble in boiling ethanol, slightly soluble in methanol or ethanol, very slightly soluble in chloroform, almost insoluble in water or ether.
Melting point: 230～231℃,
Optical rotation: (α)17D -126.6±2° (glacial acetic acid), [α]D –112.7 (c, 0.53, MeOH),
Color reaction: purple-red with alkaline 2% 3,5-dinitrobenzoic acid reagent; positive reaction with hydroxamic acid iron.
Density: (21℃) 1.2317g/cm3.
UV: λEtOHmax nm (ε), 223(12300);
IR: vKBrmax cm-1: 3448, 3390～?279(OH), 1828, 1647, 906 (C=CH2), 1727 (α, β-unsaturated γ-lactone), 1672 (co-C=C); 13CNMR.
Plant source
The whole herb or leaves of Andrographis Paniculata (Burm.f) Ness, a plant of the Acanthaceae family.
1.Anti-pathogenic microbial effects
Animal experiments show that both andrographolide and neoandrographolide can inhibit and delay the increase in body temperature caused by pneumococcus or hemolytic group B streptococcus, but andrographolide is more effective than neoandrographolide.In vitro experiments show that Andrographis paniculata has a certain anti-HIV effect.
2.Antipyretic effect
Andrographolide has different degrees of antipyretic effect on endotoxin fever in rabbits, fever caused by pneumococcus or hemolytic streptococcus. The antipyretic effects of andrographolide A, B, C, and D on fever rabbits caused by typhoid and paratyphoid vaccines or fever rats caused by 2,4-dinitrophenol are weakened in turn.
3.Anti-inflammatory effect
Andrographis paniculata A, B, C, and D all have different degrees of anti-inflammatory effects. 1g/kg oral administration can inhibit the increase in the permeability of mouse skin or peritoneal capillaries caused by xylene or acetic acid, and reduce the amount of acute exudate caused by croton oil in Selye granuloma, but has no significant effect on the proliferation of granulation tissue. It can inhibit the development of egg white rat foot swelling, but the effect disappears after adrenalectomy. D has the strongest anti-inflammatory effect, followed by C, A, and B.
4.Effects on the body's immune function
It has been reported that Andrographis paniculata may have an effect on certain aspects of cellular immunity. Its decoction can improve the ability of human leukocytes to phagocytose Staphylococcus aureus in vitro, and oral administration of Andrographis paniculata can enhance the delayed hypersensitivity reaction of the skin caused by old tuberculin. The Andrographis paniculata preparation Xinyandeping (containing esters and ketones) can increase the level of serum lysozyme in mice and enhance the phagocytic ability of peritoneal macrophages and neutrophils. Continuous administration of andrographolide sulfonate to rabbits or mice can significantly increase the phagocytic ability of peripheral blood phagocytes against pneumococcus or Staphylococcus aureus. Andrographolide A injection and Xiyanping injection can also enhance the function of phagocytes. Dehydrated andrographolide succinate half ester also has an inhibitory effect on delayed-type hypersensitivity reactions in mice caused by 2,4-dinitrochlorobenzene.
5. Anti-fertility effect
Andrographis paniculata has a significant effect of aborting pregnancy. Oral administration of Andrographis paniculata can cause contraception in mice and abortion in pregnant rabbits. Intraperitoneal injection of the decoction has a significant aborting effect on implantation, early pregnancy, mid-pregnancy, and late pregnancy in mice. Intramuscular injection, subcutaneous injection, oral administration, intraperitoneal injection, intravenous injection and intrauterine injection can all produce anti-early pregnancy effects, among which intraperitoneal, intravenous and intrauterine injections have the best effects. Intrauterine injection has a small dosage and good effect. If exogenous progesterone or luteinizing hormone releasing hormone (LH-RH) is injected at the same time as Andrographis paniculata, it can prevent miscarriage, which suggests that Andrographis paniculata may have an effect against progesterone in the body, thereby causing miscarriage. Some people believe that Andrographis paniculata has a certain inhibitory effect on the growth of placental villous trophoblast cells cultured in vitro. Studies have shown that some semi-synthetic derivatives of andrographolide also have different degrees of anti-early pregnancy effects. The dehydrated andrographolide derivative-穿-4 has a good anti-early pregnancy effect on mice and rats. It is a new contraceptive drug worthy of further study. The drug has a significant effect on placental trophoblast cells, which can cause placental villi to atrophy, reduce the number of cells, disappear syncytial cells and Langhans cells, and cause interstitial edema and bleeding.
6.Choleretic and hepatoprotective effects
Andrographis paniculata has a choleretic effect on rats, and can increase the liver weight of rats and shorten the sleep time caused by sodium cyclohexylbarbital. Pre-administration of andrographolide can counteract the hepatotoxic effects caused by carbon tetrachloride, D-galactosamine and acetaminophen, and can significantly reduce the levels of SGPT, SGOT, SALP and HTG respectively. It has been reported that the methanol extract of andrographis paniculata is toxic and can promote the death of rats with liver damage.
7.Anti-tumor effect
Dehydroandrographolide succinate half ester has a certain inhibitory effect on W256 transplanted tumors. Dehydroandrographolide disuccinate half ester potassium hydrogen is made into arginine complex salt (abbreviated as andrographolide), which has an inhibitory effect on tumor cells regardless of large, medium or small doses, and the effect increases with the increase of dose. The tumor inhibition effect is real and stable. In vitro experiments have shown that andrographis paniculata has an inhibitory effect on DNA synthesis of cultured breast cancer cells.
8.Other effects
Yanhuning and Chuanhuning injections have obvious sedative effects, can shorten the incubation period of sodium pentobarbital anesthesia in mice, prolong the anesthesia time, and can cause subthreshold sodium pentobarbital to induce anesthesia. Andrographolide can increase adrenal cortical function, and Andrographolide A, B, C, and D can cause thymus atrophy in young mice at higher doses.
