Long Dan Cao

Radix Gentianae, Gentiana Root

Dosage

Decoction 3-6g or pill can be orally taken.

Toxicity

LD50 (mice/gentianine): 460mg/kg (endogastric perfusion) 350mg/kg (abdominal injection), greater than 500mg/kg (subcutaneous injection), and 250~300mg/kg (IV injection). LD50 (mice/gentianidine): 1.25g/kg (endogastric perfusion).

Chemical Composition

Gentiopicroside; Swertiamarin; Sweroside; Amarogentin; Amaroswerin; Glycosides; Gentianine; Gentioflavine; Trifloroside; Gentianine; Gentianidine; Gentianal; b-sitosterol; Suberol; N-30-alkanol; Carrot glycoside; a-spinasterol; Caffeic acid; Quercetin; Clove acid; 5, 8-dihydroxy-7, 3', 4', trimethoflavone. (1) , (2) , (3)

Precautions

Contraindication: Spleen and stomach deficiencies.

Pharmacology

Protecting the liver

Administered to mice by abdominal injection at 30mg/kg, Long Dan juice can alleviate CCl4-induced cytomorphosis and tissue necrosis, and increase the content of hepatic glycogen. Administered to mice by abdominal injection at 240mg/kg, twice a day, for two days, gentiopicroside can counteract CCl4- or GALN-induced liver damages. Gentiopicroside can also significantly reduce liver lipid peroxidation in hungry mice. Sweroside can significantly counteract CCl4- or GALN-induced acute liver damages in both mice and rats, reduce ALT, AST, and ALP, and prevent splenomegaly caused by GALN poisoning. (4) , (5) , (6)

Cholagogic effects

Administered to dogs by IV injection, Long Dan juice can significantly increase the bile flow. Specifically, the bile flow peaks at the 5-minute and 20-minute marks, the former due to gallbladder contraction, while the latter due to an increase in bile secretion. Administered by intraduodenal injection to healthy rats or rats with live damages, Long Dan juice has a significant cholagogic effect, increasing bile secretion, and promoting gallbladder contraction. (7)

Stomach-strengthening effect

Direct perfusion of gentiopicroside through gastric fistula to the stomach of dogs can increase the secretion of gastric juice and free acid. Administering by rubbing it onto the underside of the tongue or through intravenous injection, however, does not have this effect, suggesting that the effect is due to direct action on the stomach. Swertiamarin can significantly alleviate spasm in isolated small intestine of rabbits, guinea pigs, or rats, and can antagonize the stimulatory effect of acetylcholine, histamine, and barium chloride on isolated small intestine of guinea pigs. (8)

Anti-inflammatory and anti-allergic effect

Gentiopicroside can inhibit carrageenin from causing edema in rat paws. Intra-abdominal injection of gentianine has a significant inhibitory effect on egg white and formaldehyde-induced edema in rats. Gentian also has a significant anti-allergic effect. Experiments show that gentiopicroside has a significant protective effect on histamine-induced shock in guinea pigs and on egg white-induced allergic shock in rats. It can also significantly reduce capillary permeability in rats. If gentian water-extract is given before allergy was induced or before and after an allergic reaction attack, it can, like cortical hormone, significantly inhibit picryl chloride-induced DTH in mice. (9)

Effect on the central nervous system

Gentianine has significant sedative and anti-convulsion effects, and it can significantly reduce body temperature. Experiments show that gentianine can significantly reduce spontaneous activity in animals, strengthen the anesthetic effect of barbital and chloral hydrate on the central nervous system, and inhibit strychnine-induced convulsion. It does not inhibit cardiazol-induced convulsion, however, and it can aggravate nicotine-induced convulsion. Intra-abdominal injection of swertiamarin can also inhibit mice’s spontaneous activity, and prolong the duration of sodium pentothal’s anesthetic effect. Hot plate and body torsion experiments on mice show that intra-abdominal injection of swertiamarin has a significant analgesic effect. At 600mg/kg, its analgesic effect is about the same as that of morphine at 10mg/kg. (10)

Anti-pathogenic effects

In vitro experiments show that Long Dan decoction can inhibit Pseudomonas aeruginosa, Bacillus proteus, typhoid bacillus, Staphylococcus aureus, Trichophyton gypseum, and Nocardia asteroides. The decoction has a strong paralytic effect on Ascaris suis. Fed to cats at 75-200mg/kg, gentianine can expel ascaris. (11) , (12)

Effect on the activity of steroid 4-reductase

Gentian root can significantly inhibit the activivity of 4-reductase of steroid, a key enzyme for the decomposition and metabolism of cortisol in the liver of rats with hyperthyroidism, thus reducing the degradation of cortisol and significantly decreasing the excretion of 17-hydroxy corticosteroid. (13)

Inhibitory effect on reductase of crystal aldose

Gentian root has a significant inhibitory effect on reductase (AR) of crystal aldose in rats. (14)

References

  1. Editorial Committee of Chinese Materia Medica. State Drug Administration of China. Chinese Materia Medica. Shanghai: Science and Technology Press; 1998.
  2. Xu Li Ping, et al. The chemical composition of Long Dan Cao (I). Journal of Materia Medica. China. 1998;23(5):293-295.
  3. Xu Li Ping, et al. The chemical composition of Long Dan Cao (II). Journal of Materia Medica. China. 1998;23(9):552-553.
  4. Zhang Yong. Advances in pharmacological research on gentiopicroside. Yunan Journal of Medicine. 1991;12(5):304.
  5. Hu Ruo Qi, et al. The effect of sweroside on the spleen volume of mice with GALN-induced acute liver damages. Journal of Yunan College of TCM. 1989;12(2):8.
  6. Hu Ruo Qi, et al. The effect of sweroside on the plasma cAMP content of mice of experimental liver damages. Journal of TCM pharmacology and application. 1989;5(4):31.
  7. Central Lab of Hubei College of TCM Hospital. Collections of Experiments in Integrated traditional Chinese and Western medicine. 1979:96.
  8. Lei Wei ya, et al. Herbs for treating stomachache in children. Yunan Journal of Medicine and Herbs. 1982;(2):92.
  9. Xu Qiang, et al. Long Dan Cao’s inhibitory effect on delayed allergic reaction. Journal of Pharmacology and Clinical Application of TCM. 1993;9(5):25.
  10. Lei Wei Ya, et al. Swertiamarin’s central inhibitory effects. Journal of Chinese Materia Medica. 1982;13(8):368.
  11. Wang Yu Sheng, et al. TCM Pharmacology and Application. Beijing: People’s Health Press; 1983.
  12. Parasite Research Group. Tianjin Medical College. Preliminary experiments on 49 herbs’ in vitro inhibitory effects on ascaris. Journal of Modern Medicine and Pharmacy. 1974;(2):31.
  13. Xue Hui Juan, et al. Long Dan Cao's inhibitory effect on the activity of steroid 4-reductase. China Journal of Integrated Medicine. 1992;12(4):230-231.
  14. Zhang Jia Qing, et al. Selected herbs’ inhibitory effect on reductase of crystal aldose in mice. China Journal of Chinese Medicine. 1989;14(9):557-559.