AW: Anti-leishmanial drug from Galipea logiflora

[Dr. Oliver Kayser]

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Subject: Chimanine

These simple natural quinoline derivatives 2-n-propylquinoline, chimanine B,
chimanine D, 2-n-pentylquinoline, 4-methoxy-2-phenylquinoline, and
2-(3,4-methylenedioxyphenyl)quinoline were tested for cutaneous
leishmaniasis in comparison to Nifurtimox and exhibited acitivities in the
between EC50 = 25-50 µg/mL or 150 - 300 µM (Fournet et al., 1993, Gantier et
al., 1996). Only chimanine B was active in vivo (50 mg/kg b.w., BALB/c
mice), and twice daily oral treatment resulted in a decrease of parasite
load by 95 %, at the same rate as found for the reference N-methylglucamine
antimonate (Fournet et al., 1996). No mechanism has been found yet to
explain these effects.

Attached you find the structure as an ISIS-File


Two papers dealing with the compounds are:

Fournet, A., Ferreira, M. E., Rojas De Arias, A., Torres De Ortiz, S.,
Fuentes, S., Nakayama, H., Schinini, A., Hocquemiller, R. (1996) In vivo
efficacy of oral and intralesional administration of 2-substituted
quinolines in experimental treatment of new world cutaneous leishmaniasis
caused by Leishmania amazonensis, Antimicrob. Agents Chemother., 40,
2447-2451

Gantier, J. C., Fournet, A., Munos, H. M., Hocquemiller, R. (1996) The
effect of 2-substituted quinolines isolated from Galipea longiflora on
Plasmodium vinckei petteri infected mice, Planta Med. 62, 285-286


If you need a copy, I can send it to you.

Greetings,

Dr. O. Kayser
Freie Universität Berlin
Institut für Pharmazie
Abt. Pharmazeutische Technologie & Biopharmazie und Biotechnologie
Kelchstraße 31
12169 Berlin
Deutschland/ Germany
Fax/Fon: +49-30 77 000 489
Mobile: 0177-327 1999
email: kayser at zedat.fu-berlin.de
http://www.pharmazeutische-biotechnologie.de


-----Ursprüngliche Nachricht-----
Von: leish-l at bdt.org.br [mailto:leish-l at bdt.org.br]Im Auftrag von
Jacques Mauel
Gesendet: Donnerstag, 6. Januar 2000 11:35
An: Multiple recipients of list
Betreff: Anti-leishmanial drug from Galipea logiflora


Dear colleagues,

This is a request for information regarding a potential
anti-leishmanial agent isolated from the plant Galipea longiflora
(Eventa) said to be relatively common in the Peruvian forest.
Apparently, a new drug called "chimanine", obtained from this plant,
has been patented by the "Coopératrion française"

Has anyone any further information regarding this product ? Does it
exist ? Is it actually being tested ? Are the results available ?

Thanks for your help.
Jacques Mauël
Jacques Mauel
Institute of Biochemistry
Ch. des Boveresses 155
CH-1066 EPALINGES
Switzerland
Tel ++41 21 692 57 04
Fax ++41 21 692 57 05

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