Korean J Med.
1998 Sep;55(3):302-309.
The Effect of DA-6034, Eupatilin Derivatives of Flavonoids, on the Rats with Trinitrobenzene Sulfonic Acid (TNBS) - Induced Colitis
- Affiliations
-
- 1Department of Internal Medicine, Liver Research Institute, Seoul National University College of Medicine, Seoul, Korea.
- 2Dong-A Pharmaceutical Research Laboratories1, Suwon, Korea.
Abstract
OBJECTIVE
In traditional medicine, Artemisia capillaris has been used for treatment of chronic diarrhea. Previously
we found Artemisia capillaris had an effect on rats with TNBS-induced colitis. Eupatilin, a kind of flavonoids, may be
a probable effective component. To evaluate the effect of a eupatilin derivative compound DA-6034 on the rat with
TNBS-induced colitis, we perfomed this study.
METHODS
Colitis was induced with 1ml of 50 mg/ml TNBS mixed with 60 % ethanol (vol/vol) in Sprague- Dawley
rats. From the next day, 1ml methylcellulose, 1 mg/kg prednisolone, 0.3 or 3 mg/kg of DA-6017 and DA-6034 were
administered through rectum once daily for 2 weeks. At 2days, 1week, and 2weeks later, we evaluated the effect by gross
damage score (0-10) and measured myeloperoxidase, PGE2, and LTB4 from the damaged mucosa.
RESULTS
The mean gross damage scores of prednisolone and 3 mg/kg of DA-6034 groups were significantly lower
than that of a placebo group at 2weeks (0.8, 0.9 vs. 4.0, p<0.05). Myeloperoxidase activities also seemed to be lower in
those effective groups but were not statistically significant. LTB4 levels were lower in prednisolone and, 0.3 and 3 mg/kg
of DA-6034 groups than in a placebo group at 2weeks (7.91, 7.23, and 7.13 vs. 13.90 ng/mg protein, p<0.05). PGE2 levels
were decreased in prednisolone and 0.3 mg/kg of DA-6034 groups at 2days. DA-6017 showed no effects.
CONCLUSIONS
Eupatilin derivative compound, DA- 6034 was effective in rats with TNBS-induced colitis. In that
LTB4 level is lowered with some decrease of PGE2 level, this agent probably has an inhibitory effect on arachidonic acid
metabolism.