Author Topic: Analgesic Indole alkaloids.....  (Read 5901 times)

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Analgesic Indole alkaloids.....
« on: August 23, 2004, 06:32:00 AM »
Note:I checked under 52 916 2004 in TFSE and not listed , so I assume it may be of interest and not posted

Chemistry and Pharmacology of Analgesic Indole Alkaloids
from the Rubiaceous Plant, Mitragyna speciosa

Hiromitsu TAKAYAMA

Chem. Pharm. Bull. 52(8) 916—928 (2004)

The leaves of a tropical plant, Mitragyna speciosa KORTH (Rubiaceae), have been traditionally used as a substitute
for opium. Phytochemical studies of the constituents of the plant growing in Thailand and Malaysia have
led to the isolation of several 9-methoxy-Corynanthe-type monoterpenoid indole alkaloids, including new natural
products. The structures of the new compounds were elucidated by spectroscopic and/or synthetic methods. The
potent opioid agonistic activities of mitragynine, the major constituent of this plant, and its analogues were
found in in vitro and in vivo experiments and the mechanisms underlying the analgesic activity were clarified.
The essential structural features of mitragynines, which differ from those of morphine and are responsible for
the analgesic activity, were elucidated by pharmacological evaluation of the natural and synthetic derivatives.
Among the mitragynine derivatives, 7-hydroxymitragynine, a minor constituent of M. speciosa, was found to exhibit
potent antinociceptive activity in mice.