Hostname: page-component-78c5997874-xbtfd Total loading time: 0 Render date: 2024-11-18T09:13:57.212Z Has data issue: false hasContentIssue false

Synergistic antimalarial activity of ketones with rufigallol and vitamin C

Published online by Cambridge University Press:  28 June 2005

S. S. MAHAJAN
Affiliation:
C.U. Shah College of Pharmacy, S.N.D.T. Women's University, Sir Vithaldas Vidya Vihar, Santacruz (West), Mumbai-400 049, India
V. R. KAMATH
Affiliation:
Haffkine Institute, Parel, Mumbai-400 012, India
S. S. GHATPANDE
Affiliation:
A-33, Tribhuvan, Ninety Feet Road, Mulund (East), Mumbai-400 081, India

Abstract

Malaria remains a major cause of human morbidity and mortality worldwide. Plasmodium falciparum, the most virulent of the 4 human Plasmodium species causing malaria, is potentially life threatening, is increasing in prevalence and is becoming even more resistant to in-use drugs. In light of the growing problem of multi-drug resistance to malarial parasites, the development of new drugs or the use of a combination therapy is of primary importance. A previous report describes a remarkable synergistic antimalarial interaction between 2 structurally similar compounds, rufigallol, an anthraquinone derivative and exifone, a benzophenone derivative, in vitro. The synergistic antimalarial activity of exifone and vitamin C was also reported. To extend the same analogy to other ketones, we carried out antimalarial testing of 20 benzophenone derivatives, individually, in combination with rufigallol, and also in combination with vitamin C, in mice infected with Plasmodium berghei. Five ketones, out of 20, showed good antimalarial activity, in vivo, when tested individually. Nine ketones, out of 20, showed good antimalarial activity, in vivo, when tested in combination with rufigallol, indicating the synergism between them. However, synergism between ketones and vitamin C was not satisfactory since only 2 ketones showed good antimalarial activity when tested in combination with vitamin C.

Type
Research Article
Copyright
© 2005 Cambridge University Press

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

References

REFERENCES

Grimshaw, J. and Haworth, R. ( 1956). Flavogallol. Journal of the Chemical Society, 42254232.CrossRefGoogle Scholar
Osdene, T. S., Russel, P. B. and Rane, L. ( 1967). 2,4,7-Triamino-6-ortho-substituted arylpteridines. Journal of Medicinal Chemistry 10, 431434.CrossRefGoogle Scholar
Sachs, J. and Maloney, P. ( 2002). The economic and social burden of malaria. Nature, London 415, 680685.CrossRefGoogle Scholar
Segui, L. ( 1934). Preparation of some derivatives of anthracene. Chemical Abstracts 28, 7257.Google Scholar
Winter, R. W., Cornell, K. A., Johnson, L. L. and Riscoe, M. K. ( 1995). Hydroxyanthaquinones as antimalarial agents. Bioorganic and Medicinal Chemistry Letters 5, 19271932.CrossRefGoogle Scholar
Winter, R. W., Ignatushchenko, M. K., Cornell, A., Johnson, L. L., Hinrichs, D. J. and Riscoe M. K. ( 1996). Potentiation of the antimalarial agent, rufigallol. Antimicrobial Agents and Chemotherapy 40, 14081411.Google Scholar
Winter, R. W., Ignatushchenko, M., Olumide, A. T., Cornell, K. A., Johnson, L. L., Hinrichs, D. J. and Riscoe, M. K. ( 1997). Potentiation of an oxidant drug. Antimicrobial Agents and Chemotherapy 41, 14491454.Google Scholar