Evaluation of In Vitro Activity of Aurones and Related Compounds against Cryptosporidium parvum

Abstract

The efficacy of a series of aurones, auronols and 4-methoxy-α-pyrones has been screened for the ability to inhibit the intracellular growth of the parasitic protist Cryptosporidium parvum using an in vitro enzyme linked immunosorbent assay (ELISA). All aurones of this series were active at 25 to 100 μM. 10 of 19 aurones inhibited the intracellular growth of C. parvum by > 90 % with moderate to no toxicity. The most active of these was 3′,4′,6-trihydroxy-2-[phenylmethylene]-3(2H)-benzofuranone.

Key words

Aurones - Cryptosporidium - ELISA assay - protist chemotherapy - drug testing

References

• 1 Laing R B. Nosocomial infections in patients with HIV disease.  Journal of Hospital Infection. 1999;  43 179-85
• 2 Ramratnam B, Flanigan T P. Cryptosporidiosis in persons with HIV infection.  Postgraduate Medicine. 1997;  73 713-6
• 3 Das P. Cryptosporidium related diarrhoea.  Indian Journal of Medicinal Research. 1996;  104 86-95
• 4 Woods K M, Nesterenko M V, Upton S J. Efficacy of 101 antimicrobials and other agents on the development of Cryptosporidium parvum in vitro .  Annals of Tropical Medicine and Parasitology. 1996;  90 603-15
• 5 Sharma P, Sharma J D. Plants showing antiplasmodial activity - from crude extracts to isolated compounds.  Indian Journal of Malariology. 1998;  35 57-110
• 6 van Agtmael M A, Eggelte T a, van Boxtel C J. Artemisinin drugs in the treatment of Malaria: From medicinal herb to registered medication.  Trends in Pharmacological Sciences. 1999;  20 199-205
• 7 Sepúvelda-Boza S, Cassels B K. Plant metabolites active against Trypanosoma cruzi .  Planta Medica. 1996;  62 98-105
• 8 Bley K. Darstellung einiger Auronole (= 2-Benzoylcumaranone-(3)) und analytischer Vergleich mit entsprechend substituierten Flavonolen. PhD Dissertation 1970 Freie Universität Berlin;
• 9 Woods K M, Nesterenko M V, Upton S J. Development of a microtiter ELISA to quantify development of Cryptosporidium parvum in vitro .  FEMS Microbiology Letters. 1995;  128 89-93
• 10 Upton S J. In vitro cultivation. In R. Fayer, (ed.) Cryptosporidium and Cryptosporidiosis, 1st ed. CRC Press Boca Raton, Fl.; 1997: p. 181-207
• 11 Upton S J, Tilley M, Brillhart D B. Effects of select medium supplements on in vitro development of Cryptosporidium parvum in HCT-8 cells.  Journal of Clinical Microbiology. 1995;  33 371-5