RESUMEN
Asiaticoside, a plant glycoside with rhamnose as end sugar and having microbicidal properties was tested against Mycobacterium leprae and Mycobacterium tuberculosis both in vivo and in vitro. As rhamnose is reported to have no tissue specificity, corchorusin D having glucose as end sugar was used for targeting with an equimolar proportion of asiaticoside in liposomal form for testing the drug value. Results showed that liposomal asiaticoside had better microbicidal property against M. leprae and M. tuberculosis when compared to that of free asiaticoside whereas liposomes containing asiaticoside and corchorusin D were found to be equally or more active in comparison to liposomal asiaticoside alone. It is inferred that appropriate glycosides, if used in liposomal form (incorporated or covalently grafted) have enhanced drug efficacy and such glycoside bearing liposomes as targeted delivery systems could be used for chemotherapeutic control of several other diseases.
Asunto(s)
Animales , Portadores de Fármacos , Femenino , Lepra/tratamiento farmacológico , Liposomas , Macrófagos/efectos de los fármacos , Masculino , Ratones , Mycobacterium leprae , Mycobacterium tuberculosis , Triterpenos/administración & dosificación , Tuberculosis/tratamiento farmacológicoRESUMEN
The active principle, isolated from the funicles of A. auriculiformis, consisted of two triterpenoid saponins, acaciaside A and acaciaside B which killed in vitro 97% microfilaria of Setaria cervi in 100 min at 4mg/ml concentration and 100% of adults in 35 min. The drug, when administered orally at 100 mg/kg on rats, in which S. cervi adults were implanted intra-peritoneally, increased the blood mf count by 1.5-fold after the first phase of treatment for 10 days. Following the third phase of treatment and thereafter, the mf density was reduced by more than 80%. No toxic effect of the saponins was observed in rats. The rise in mf count indicated that the drug induced a very high physiological stress on the adult worms which increased the rate of discharge of the mf before impending death. The treated rats on autopsy did not show any adult worms.