Abstract
Gentianae Radix, the dried root and rhizoma of Gentiana lutea L. (Gentianaceae), has long been used as a remedy for liver and stomach inflammation, eye troubles, etc. In this paper, the gastroprotective effects of the methanol extract of Gentian root (GM) were studied using different gastric lesion models. In pylorus-ligated rats, administration of GM in the duodenum suppressed gastric juice secretion and total acid output in a dose-dependent manner. Oral or duodenum administration of GM showed significant protection against acute gastric ulcer induced by aspirin plus pylorus ligation, water-immersion restraint stress-induced ulcers, and gastric mucosal injury induced by ethanol. Furthermore, four secoiridoid glycosides, amarogentin (A1), gentiopicroside (A2), amaroswerin (A3), and swertiamarin (A4), were obtained from Gentian root or Swertia herb, and their protective effects against stress-induced ulcers and ethanol-induced gastric mucosal injury were evaluated. The doses required for 50% inhibition (ID50) of A1, A3, and A4 on stress-induced ulcers were calculated to be 5.76, 2.58, and 167 mg/kg respectively. The protective effect of A2 at 250 mg/kg was 26.5%. On ethanol-induced gastritis, 5.0 mg/kg of A1 and A3 showed remarkable suppressive effects (33.7 and 45.4%, respectively), and 20 mg/kg of A4 exhibited a suppressive effect (30.8%). The effects of A1, A3, and A4 on ethanol-induced gastric lesions were canceled by 5.0 mg/kg indomethacin pretreatment. These results suggest that the therapeutic effects of Gentian root on gastric lesions are associated with enhanced mucosal defensive factors via the prostaglandin pathway in the cell membrane, and that secoiridoid glycosides contribute to this activity.
Similar content being viewed by others
Abbreviations
- A1:
-
Amarogentin
- A2:
-
Gentiopicroside
- A3:
-
Amaroswerin
- A4:
-
Swertiamarin
- CMC-Na:
-
Carboxymethyl cellulose-Na
- GM:
-
Methanolic extract of Gentian root
- G1:
-
Ether soluble fraction of Gentian root
- G2:
-
EtOAc soluble fraction of Gentian root
- G3:
-
n-BuOH soluble fraction of Gentian root
- G4:
-
Water soluble residue
- UI:
-
Ulcer index
References
Kohlein F (1991) Gentians. Timber Press, Portland, pp 25–27
Namba T (1993) Wakan–Yaku Hyakka–Jiten. (The encyclopedia of Wakan–Yaku, Japanese–Chinese herbal drugs) (in Japanese). Hoikusha, Tokyo, pp 188–189
The Japanese Pharmacopoeia (English version) (2001), 14th edn, Part II. Ministry of Health, Labor and Welfare Japan, pp 925–992; Japanese Pharmacopoeia 14th Guide Book, Hirokawa Publisher, Tokyo, 2001, pp D341–D348 (in Japanese)
Hayashi T (1976) Studies on crude drugs originated from Gentianaceous plants I Determination of gentiopicroside, the bitter principle of Gentianae radix and Gentianae scabrae radix (in Japanese). Yakugaku Zasshi 96:356–361
Wagner H, Wolff P (1977) New natural products and plant drugs with pharmacological, biological or therapeutical activity. Springer, Berlin Heidelberg New York
Kondo Y, Takano F, Hojo H (1994) Suppression of chemically and immunologically induced hepatic injuries by gentiopicroside in mice. Planta Med 60:414–416
Blumberger W, Glatzel H (1968) The action of customary spices on the lysozyme activity of the saliva (in German). Dtsch Zahnarztl Z 23:666–674
Yamahara J, Konoshima T, Sawada T, Fujimura H (1978) Biologically active principles of crude drugs: pharmacological actions of Swertia japonica extracts, swertiamarin and gentianine (in Japanese). Yakugaku Zasshi 98:1446–1451
Okabe S, Takeuchi K, Ikenishi H, Ohmi F, Takaoka A (1983) Effects of SM powder, a combined herbal preparation for stomach diseases, on gastric secretion and acute gastro-duodenal lesions in rats (in Japanese). Nippon Yakurigaku Zasshi (Jpn J Pharmacol) 81:285–294
Glatzel H, Hackenberg K (1967) Roentgenological studies of the effect of bitters on digestive organs (in German). Planta Med 15:223–232
Niiho Y, Takayanagi K, Takagi K (1977) Effects of a combined stomachic and its ingredients on rabbit stomach motility in situ. Jpn J Pharmacol 27:177–179
Akamatsu K (1970) Wakan-Yaku (in Japanese). Ishiyaku Shuppan, Tokyo
Niiho Y, Mitsunaga K, Koike K, Ohmoto T (1994) Studies on the gastric antiulcer components from the woods of Picrasma quassioides (Simaroubaceae) (in Japanese). Nat Med 48:116–121
Akada Y, Kawano S, Yamagishi M, Tanase Y (1979) High-speed liquid chromatographic analysis of drugs. VI. Rapid estimation of gentiopicroside in Gentianae scabrae radix and Gentianae radix (in Japanese). Yakugaku Zasshi 99:1047–1050
Boros CA, Stermitz FR (1991) Iridoids. An updated review, part II. J Nat Prod 54:1173–1246
Shay H, Komarov SA, Fels SS, Meranze D, Gruenstein M, Siplet H (1945) A simple method for the uniform production of gastric ulceration. Gastroenterology 5:43–61
Suzuki Y, Hayashi M, Ito M, Yamagami I (1976) Anti-ulcer effects of 4′-(2-carboxyethyl) phenyl trans-4-aminomethyl cyclohexane carboxylate hydrochloride (cetraxate) on various experimental gastric ulcers in rats. Jpn J Pharmacol 26:471–480
Anson ML (1938) The estimation of pepsin, trypsin, papain and catepsin with hemoglobin. J Gen Physiol 22:78–89
Takagi K, Okabe S (1968) The effects of drugs on the production and recovery process of the stress ulcer. Jpn J Pharmacol 18:299–311
Goldenberg MM, Honkomp LJ, Burrous SE, Castellion AW (1975) Protective effect of Pepto-Bismol liquid on the gastric mucosa of rats. Gastroenterology 69:636–640
Miyoshi A (ed) (1993) Reconsideration of anti-secretory drugs in peptic ulcer. Iyaku Journal, Tokyo
Robert A (1981) Gastric cytoprotection by sodium salicylate. Prostaglandins 21(Suppl):139–146
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Niiho, Y., Yamazaki, T., Nakajima, Y. et al. Gastroprotective effects of bitter principles isolated from Gentian root and Swertia herb on experimentally-induced gastric lesions in rats. J Nat Med 60, 82–88 (2006). https://doi.org/10.1007/s11418-005-0014-2
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s11418-005-0014-2