Anti-rheumatoid arthritis effect of the Kochia scoparia fruits and activity comparison of momordin lc, its prosapogenin and sapogenin.
MeOH extract of Kochia scoparia was fractionated into CHCl3-, EtOAc- and BuOH extracts and the last fraction were hydrolyzed by 3%-NaOH (MeOH-H2O) to compare the bioactivities on antinociceptive and anti-inflammatory effects. Silica gel column chromatography of BuOH fraction afforded a large amount of 3-O-beta-D-xylopyranosyl (1-->3)-beta-D-glucuronopyranosyl oleanolic acid (momordin lc, 4) and that of acid hydrolysate of BuOH fraction gave 3-O-beta-D-glucuronopyranosyl oleanolic acid (momordin lb, 3), its 6'-O-methyl ester (2) and oleanolic acid (1). Silica gel column chromatography of alkaline hydrolysate afforded a large amount of 4. MeOH extract and both EtOAc- and BuOH fractions were active in the rheumatoidal rat induced Freund's complete adjuvant reagent (FCA) whereas CHCl3 fraction was inactive. Compound 1 and 4 showed significant activities in the same assay but oleanolic acid 3-O-glucuronopyranoside (3) showed no activity. These fashions were also observed in carrageenan-induced edema of the rat and in the antinociceptive activity tests undertaken in hot plate- and writhing methods. These results suggest that momordin lc and its aglycone, oleanolic acid, could be active principles for rheumatoid arthritis.
College of Pharmacy, Kyungsung University, Pusan, Korea.
Jongwon
J
Choi
Kyung-Tae
KT
Lee
Hyunju
H
Jung
Hee-Sun
HS
Park
Hee-Juhn
HJ
Park
D019342:Acetic Acid; D000818:Animals; D001169:Arthritis, Experimental / Q000188:drug therapy*; D002351:Carrageenan; D019663:Chenopodiaceae / Q000737:chemistry*; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005638:Fruit / Q000737:chemistry*; D006868:Hydrolysis; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D010147:Pain Measurement / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012502:Sapogenins / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D010936:Plant Extracts; D012502:Sapogenins; C408362:momordin I (Oleanolic Acid); D009828:Oleanolic Acid; D002351:Carrageenan; D019342:Acetic Acid