medigraphic.com
SPANISH

Revista Latinoamericana de Microbiología

Revista Latinoamericana de Microbiología
  • Contents
  • View Archive
  • Information
    • General Information        
    • Directory
  • Publish
    • Instructions for authors        
  • medigraphic.com
    • Home
    • Journals index            
    • Register / Login
  • Mi perfil

2001, Number 1

Next >>

Microbiología 2001; 43 (1)

Trypanocidal activity of 4 isopropyl salicylaldehyde and 4-isopropyl salicylic acid on Trypanosoma cruzi

Nogueda-Torres B, Rodríguez-Páez L, Baeza RI, Wong RC
Full text How to cite this article

Language: English
References: 27
Page: 1-6
PDF size: 80.40 Kb.


Key words:

Trypanosoma cruzi, drogas tripanosomicidas, 4-isopropil salicilaldeído, ácido 4-isopropil salicílico.

ABSTRACT

We synthesized and study the possible trypanocidal activity of 4-isopropyl salicylaldehyde and 4-isopropyl salicylic acid, these compounds were chemical derivatives of gossypol, a drug that inhibits the growth of T. cruzi in culture. These derivatives were tested in two T. cruzi strains with different in vitro susceptibility to benznidazole and nifurtimox, used as a reference drugs. It was found that they were better inhibitors of T. cruzi a-hydroxyacid dehydrogenase than gossypol, in both strains. The in vitro and in vivo pharmacological tests were performed and in both test, the gossypol derivatives showed a higher and better trypanocidal effect than gossypol, and a higher and much better trypanocidal effect than nifurtimox and benznidazole in the two studied T. cruzi strains. The trypanocidal effect was higher in the NINOA strain than in the MIGUZ strain.


REFERENCES

  1. Aronov, A. M., C. L. Verlinde, W. G. Hol, and M. H. Gelb. 1998. Selective tight binding inhibitors of trypanosomnal glyceraldehyde-3-phosphate dehydrogenase via structure-based drug design. J. Med. Chem. 41:4790-4799.

  2. Andrade, S. G., J.B. Magalhanes, and A. L. Pontes. 1985. Evaluation of chemotherapy with benznidazole and nifurtimox in mice infected with T. cruzi strains of different type. Bull. WHO. 62:721-726.

  3. Bakker, B. M., H. V. Westerhoff, F. R. Opperdoes, and P. A. M. Michels. 2000. Metabolic control analysis of glycolysis in trypanosomes as an approach to improve selectivity and effectiveness of drugs. Mol. Biochem. Pharmacol. 106:1-10.

  4. Blanco, A., A. Aoki, E. E. Montamat, and L. E. Rovai. 1983. Effect of gossypol upon motility and ultrastructure of Trypanosome cruzi. J. Protozool. 30:648-651.

  5. Blanco, A. 1990. Functional significance of the testis and sperm-specific lactate dehydrogenase isozyme (LDH-C4). Acad. Nac. Cienc. Argentina. Misc. 84:1-31.

  6. Brener, Z. 1962. Therapeutic activity and criterion of cure in mice experimentally infected with Trypanosoma cruzi. Rev. Inst. Med. Trop. Sao Paulo. 4:389- 396.

  7. Brenner, Z. 1984. Recent advances in the chemotherapy od Chagas disease. Mem. Inst. Oswaldo Cruz. 79:149-155.

  8. Coronel C., L. E. Rovai, N. M. Gerez de Burgos, C. Burgos, and A. Blanco. 1981. Properties of ahydroxyacid dehydrogenase from isozymes from Trypanosome cruzi. Mol. Biochem. Parasitol. 4:29-38.

  9. Coronel, C. E., N. M. Gerez de Burgos, C. Burgos, L. E. Rovai, and A. Blanco, A. 1984. Effect of temperature upon catalytic properties of a-hydroxyacid dehydrogenase from Trypanosome cruzi. Mol. Biochem. Parasitol. 10:185-193.

  10. Eid, J. E., H. Ueno, C. C. Wang, and J. E. Donelson. 1988. Gossypol-induced death of African trypanosomes. Exp. Parasitol. 66:140-142.

  11. Filardi L. S. and Z. Brener. 1984. A rapid method for testing in vivo the susceptibility of different strains of Trypanosoma cruzi to active chemotherapeutic agents. Mem. Inst. Oswa ldo Cruz 79:221-225.

  12. Gerez de Burgos, N. M., C. Burgos, A. Blanco, I. Paulone, and E. S. Segura. 1976. Actividad de a-hidroxiácido dehidrogenasa en Trypanosoma cruzi. Acta Physiol. Latinoam. 26:10-19.

  13. Gerez de Burgos, N. N., C. Burgos, E. E. Montamat, L. E. Rovai, and A. Blanco, A. 1984. Inhibition by gossypol of oxidorreductases from Trypanosoma cruzi. Biochem. Pharmacol. 33:955-959.

  14. Liu, G. Z., K. C. Lyle, and J. Cao. 1987. Clinical trial of gossypol as a male contraceptive drug. Part I. Efficacy study. Fert. Steril. 48:459-461.

  15. Montamat, E. E., C. Burgos, N. M. Gerez de Burgos, L. E. Rovai, and A. Blanco. 1982. Inhibitory action of gossypol on enzymes and growth of Trypanosoma cruzi. Science 218:188-189.

  16. Morello, A. 1988. The biochemistry of the mode of action of drugs and the detoxication mechanism in Trypanosoma cruzi. Rev. Infect. Dis. 6:223-238.

  17. Murta, S. M., R. T. Gazzinelli, Z. Brener, and A. J. Romanha. 1998. Molecular characterization of susceptible and naturally resistant strain of Trypanosoma cruzi to benznidazole and nifurtimox. Mol. Biochem. Parasitol. 93:203-214.

  18. Ozaki, T., J. C. Engel, and J. A. Dvorak. 1996. Cellular and molecular biological analyses to nifurtimox resistance in Trypanosoma cruzi. Am. J. Trop. Med. Hyg. 55:111-117.

  19. Olds-Clarke, P. 1996. How does poor motility alter sperm fertilizing ability. J. Androl. 17:183-186.

  20. Pays, J. F. 1998. American human trypanosomiasis 90 years after its discovery by Carlos Chagas. I. Epidemiology and control. Med. Trop. 58:391-402.

  21. Rodríguez-Páez, L., O. A. Pérez, I. Baeza R., and C. Wong R. 1998. El gosipol inhibe a la LDH-C4 debido a la presencia del 4-isopropil salicilaldehído en su estructura molecular. Ann. Esc. Nac. Cienc. Biol., Méx. 44:71-80.

  22. Rovai, L. E., A. Aoki, N. M. Gerez de Burgos, and A. Blanco. 1990. Effect of gossypol on trypomastigotes and amastigotes of Trypanosoma cruzi. J. Protozool. 37:280-286.

  23. Tsuhako, M. H., M. J. Alves, W. Colli, L. S. Filardi, Z. Brener, and O. Augusto. 1991. Comparative studies of nifurtimox uptake and metabolism by drug-resistant and susceptible strain of Trypanosoma cruzi. Comp. Biochem. Physiol. 99:317-321.

  24. Turrens, J. F. 1986. The potential of antispermatogenic drugs against trypanosomatids. Parasitol. Today 2:351-352.

  25. Vogel, A. 1981. Vogels Practical organic chemistry. 4thed. Longman London & N.Y. pp 756, 790.

  26. Vyas, R. K., and N. R. Kalla. 1990. Effect of optical isomers of gossypol analog on human sperm motility. Contraception 39:687-697.

  27. World Health Organization. 1991. Chagas desease: Tenth program report. Geneva, W.H.O. Technical report No. 811. p 95.




2020     |     www.medigraphic.com

Mi perfil

C?MO CITAR (Vancouver)

Microbiología. 2001;43