Journal
PLANTA MEDICA
Volume 67, Issue 2, Pages 114-117Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-2001-11512
Keywords
Incarvillea sinensis Lam.; Bignoniaceae; incarvillateine; antinociceptive activity; monoterpene alkaloid; phenylpropanoid; cyclobutane ring; formalin-induced pain model
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Incarvillateine (1), a new monoterpene alkaloid carrying a characteristic cyclobutane ring, has been found to shaw significant antinociceptive activity in a formalin-induced pain model in mice. To investigate the correlation between its structure and antinociceptive activity, and especially to study whether a cyclobutane ring is necessary or not for expression of activity, we evaluated the antinociceptive activity of two constructive units of incarvillateine, such as a monoterpene unit (incarvilline, 3) and a phenylpropanoid unit (ferulic acid, 2) in the formalin test, and compared activity of the units with that of incarvillateine. Furthermore, in order to obtain more information about the structure-activity relationships, monoterpene alkaloid derivatives, such as incarvine C (5, a precursor of incarvillateine), incarvine A (4, an ester compound comprised of two monoterpene alkaloids and a monoterpene) and 3,3'-demethoxy-4,4'-dehydroxyincarvillateine (6, a synthetic new compound), were examined. The antinociceptive effect of 3,3'-demethoxy-4,4'-dehydroxyincarvillateine was equal to that of incarvillateine. Meanwhile, the other compounds exhibited no or weak activity. These results suggested that the cyclobutane moiety of incarvillateine plays an important role in expression of antinociceptive action.
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