Evaluation of cryptolepine and huperzine derivatives as lead compounds towards new agents for the treatment of human African Trypanosomiasis.
Oluwafemi, A.J. Okanla, O. Camps, P. Muñoz-Torrero, D. Mackey, Z.B. Chiang, P.K. Seville, Scott Wright, Colin W.
Oluwafemi, A.J.
Okanla, O.
Camps, P.
Muñoz-Torrero, D.
Mackey, Z.B.
Chiang, P.K.
Seville, Scott
Wright, Colin W.
Publication Date
2009
End of Embargo
Supervisor
Rights
Peer-Reviewed
Yes
Open Access status
closedAccess
Accepted for publication
Institution
Department
Awarded
Embargo end date
Collections
Additional title
Abstract
The alkaloid cryptolepine (1) and eight synthetic analogues (2-8) were assessed for in vitro activities against Trypanosoma brucei. Four of the analogues were found to be highly potent with IC50 values of less than 3 nM and three of these were assessed against T. brucei brucei infection in rats. The most effective compound was 2,7-dibromocryptolepine (7); a single oral dose of 20 mg/Kg suppressed parasitaemia and increased the mean survival time to 13.6 days compared with 8.4 days for untreated controls. In addition, four huperzine derivatives (9-12) were shown to have in vitro antitrypanosomal activities with IC50 values from 303-377 nM.
Version
No full-text in the repository
Citation
Oluwafemi, A. J., Okanla, E. O., Camps, P., Muñoz-Torrerob, D., Mackey, Z. B., Chiang, P. K., Seville, S. and Wright, C. W. (2009). Evaluation of cryptolepine and huperzine derivatives as lead compounds towards new agents for the treatment of human African Trypanosomiasis. Natural Product Communications, Vol. 4, No. 2. pp.193-198.
Link to publisher’s version
Link to published version
Link to Version of Record
Type
Article