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Esterification improves antiarthritic effectiveness of lupeol
Author(s) -
KweifioOkai George,
Field Barry,
Rumble Baden A.,
Macrides Theodore A.,
De Munk Fred
Publication year - 1995
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430350304
Subject(s) - lupeol , chemistry , medicine , biochemistry
Adult male Wistar rats were made arthritic by the subplantar injection of complete Freund's adjuvant. Oral treatment with the triterpenes lupeol, luepol palmitate, or lupeol linoleate (66 mg/kg BW every 2 days) from days 24 to 32 reduced synovial granulomatous growth (proximal interphalangeal foot joints) and its invasion of the synovial cavity and reduced the destruction of articular cartilage and subchondral bone (lupeol linoleate > lupeol palmitate > lupeol). Rats treated with the lupeol esters showed reduced periosteal bone erosion with bone repair in the form of periosteal new bone formation. Arthritic rat blood lymphocytes and serum levels of the joint degradative product, hyaluronate, which increased by 73% and 51%, respectively, were reduced by the triterpenes (lupeol linoleate > lupeol palmitate > lupeol) with lupeol linoleate restoring them to normal values. The antiarthritic effectiveness of lupeol was therefore increased by esterification with the long‐chain fatty acids. © 1995 Wiley‐Liss, Inc.