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Pharmacological action of glycyrrhetinic acid

    1. Adrenocorticoid-like effects
      (1) salocorticoid-like effect
      Glycyrrhetinic acid can promote sodium retention, water retention and potassium excretion in healthy people and animals, showing a deoxycorticosterone-like effect. When 40mg of hydrocortisone daily intramuscular maintenance therapy was used in patients with bilateral adrenal resection, a synergistic effect and electrolyte balance were achieved by adding glycyrrhetinic acid to 4g daily subcutaneous injection. However, if hydrocortisone is stopped and only glycyrrhetinic acid is given, the loss of sodium storage capacity occurs, and Addison’s crisis occurs.
      (2) glucocorticoid-like effect
      Glycyrrhetinic acids are chemically similar to corticosterols. Glycyrrhetinic acid can still produce sodium retention and antidiuretic and anti-inflammatory effects in animals with adrenocorticectomy and pituitary resection. The effect of 25mg glycyrrhetinic acid on water and sodium retention in rats was stronger than that of 1mg deoxycorticosterone. Therefore, it is thought that the desoxycorticosterone-like effect of glycyrrhetinic acid is not produced by endogenous desoxycorticosterone and aldosterone, but may be a direct effect. Some people also think that it is an indirect effect, that is, glycyrrhetinic acid inhibits the destruction of adrenal corticosterols in the body, so the content of corticosteroids in the blood increases correspondingly, and the adrenal corticosteroid effect is more obvious. It has also been reported that glycyrrhetinic acid has an effect on people whose adrenal cortex function is weakened without complete failure.
    2. Anti-inflammatory and anti-immune effects
      Glycyrrhetinic acid has an anti-inflammatory effect like butazone or hydrocortisone. Glycyrrhetinic acid can inhibit cotton ball granuloma, formaldehyde foot swelling and subcutaneous granulomatous inflammation in rats, and its anti-inflammatory titer is about 1/10 of cortisone or hydrocortisone. Glycyrrhetinic acid can inhibit experimental arthritis in rats and allergic reactions in guinea pigs caused by horse serum or egg white. Its anti-inflammation, anti-allergic response may be related to inhibition of capillary permeability, antihistamine, or reduced cell responsiveness to stimuli.
      Glycyrrhetinic acid has an inhibitory effect on a variety of acute inflammation, and its anti-inflammatory effect is not dependent on the pituitary-adrenal cortex system, but is related to the inhibition of PgE2 production in inflammatory tissues and the antagonism of inflammatory mediators histamine and 5-hydroxytryptamine. Sodium glycyrrhetinate can inhibit the production of malondialdehyde (MDA), a peroxide degradation product in Pg of protein-induced inflammatory mice, which can be antagonized by exogenous arachidonic acid. Sodium glycyrrhetinate can also enhance the non-specific cellular immune function. 18-β glycyrrhetinic acid has immunomodulatory effect on acute serum disease in rabbits. Fifty rabbits were randomly divided into experimental group and control group. Bovine serum protein (BSA) was used as antigen to create transient acute serum disease model. 18-β glycyrrhetinic acid was dissolved in olive oil (150mg/ml), and 200mg/kg 18-β glycyrrhetinic acid was injected into the muscles of the experimental animals on the 3rd, 5th, 7th and 9th days after BSA injection. Control group was intramuscularly injected with olive oil. Results The anti-BSA-1GG antibody in serum of the control group and the experimental group was detected on the 6th day after BSA immunization and reached the highest level on the 12th day, and the experimental group was significantly higher than the control group. The specific BSA-anti-BSA complex in circulation in both groups was significantly higher than before immunization, but there was no statistical difference between the two groups. The blood complement value in experimental group was significantly higher than that in control group. 18-β glycyrrhetinic acid had no effect on the formation of CIC.
    3. Effect on digestive system
      Glycyrrhetinic acid can reduce blood bilirubin and increase urine bilirubin excretion in rabbits and rats with total bile duct ligation, and this effect is stronger than that of glucuronolactone or methionine. It has good anti-ulcer effect on pyloric ligation rats. Its therapeutic index is higher.
    4. Antitussive and expectorant effect
      Choline salt of glycyrrhetinic acid has obvious antitussive effect on cough caused by chemical stimulation (inhalation of ammonia) and electrical stimulation of upper laryngeal nerve in cats. Therefore, it is believed that its antitussive effect is related to the center.
    5. Anti-tumor effect
      It can inhibit the growth of transplanted Oberling-gnerin myeloma in rats, and can slightly inhibit the growth of FAC and sarcoma-45 cells in mice at the maximum tolerated dose of sodium salt.
    6. Antidiuretic effect
      Glycyrrhetinic acid and its salts have obvious antidiuretic effect. It can enhance the reabsorption of sodium chloride by renal tubules and show antidiuretic effect. Its mode of action is different from desoxycorticosterone, which may be due to its direct effect on the renal tubules.
    7. Influence on the auditory function of the inner ear
      Auditory electrophysiology method showed that the action potential response threshold of auditory nerve of guinea pigs decreased after 100mg/kg intramuscularily injected glycyrrhetinic acid, indicating that glycyrrhetinic acid can improve the auditory function of the inner ear of guinea pigs.
    8. Inhibition of acetylcholinesterase
      Glycyrrhetinic acid is used at a concentration of 4×10-2mg/ml. The inhibitory effect on acetylcholinesterase was significantly increased with the increase of drug concentration in this dose range. The drug concentration at 50% inhibition rate was 21.8±1.1mg/L. The inhibition of glycyrrhetinic acid on acetylcholinesterase was a combination of competitive and non-competitive inhibition, which was similar to neostigmine.
    9. Scavenging effect on oxygen free radicals
      18-β glycyrrhetinic acid 0.3mmol/L had a significant scavenging effect on the oxygen free radicals released by human polykaryotic leukocytes (PMN), but had no effect on the oxygen consumption of PMN. 18-β glycyrrhetinic acid has obvious scavenging effect on O-2 and -OH produced in aqueous solution. The chemiluminescence produced by PMN was significantly inhibited by 30mol/L. The results show that 18-β glycyrrhetinic acid can directly trap oxygen free radicals.
    10. Other functions
      (1) The effect on estrogen
      Glycyrrhetinic acid can inhibit the growth of estrogen in the uterus of juvenile animals, and it still has the same effect after excision of adrenal gland or ovary.
      (2) Antibacterial and antiviral effects
      Glycyrrhetinic acid can enhance the inhibitory effect of berberine on staphylococcus aureus and neutralize the toxicity of tetanus toxin in vitro.
      (3) Effect on active oxygen generation and intracellular free Ca2+ concentration of neutrophils
      Rat experiments showed that sodium 18-β glycyrrhetinate could selectively inhibit Neu (neutrophil) reactive oxygen species induced by A-23187(calcium ionophorets) by 0.8 ~ 12.7mmol/L. 25.4-203mmol /L stimulated Neu to produce reactive oxygen species, and enhanced f-MLP to produce reactive oxygen species. Sodium 18-β glycyrrhetinate inhibited the increase of Neu(Ca2+) induced by A-23187 or f-MLP at 25.5-203 or 6.3 to 50.7mmol/L, and also increased Neu(Ca2+) above 101.5mmol/L.
      (4) The effect of hypoxia on mice
      Sodium ip,14mg/kg,21mg/kg can significantly prolong the survival time of mice under normal and decompression conditions, and enhance the tolerance of mice to tissue hypoxia caused by potassium cyanide and sodium nitrite and brain circulation hypoxia caused by common carotid artery ligation.
      (5) Influence on myocardial ischemia
      It can obviously counteract the electrocardiogram changes of acute myocardial ischemia caused by pituitrin in rats.

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