RESUMO
Pimprinine, an extracellular alkaloid has been isolated from the culture filtrate of Streptomyces CDRIL-312. Pimprinine was subsequently purified using silica gel column chromatography and also by preparatory thin layer chromatography. Some physicochemical properties, antimicrobial activities (in-vitro) and pharmacological activities of pimprinine were studied. Pimprinine showed promising anticonvulsant activity in both minimum and maximum electric seizure threshold test in mice. Its anticonvulsant activity is very much comparable to that of phenyl hydantion sodium. Pimprinine also inhibited effectively tremorine-induced tremors and analgesia in mice.
Assuntos
Anticonvulsivantes/farmacologia , Oxazóis/metabolismo , Oxazóis/farmacologia , Fenitoína/metabolismo , Fenitoína/farmacologia , Streptomyces/metabolismo , Animais , Biotecnologia/métodos , Cromatografia em Camada Fina/métodos , Relação Dose-Resposta a Droga , Fermentação , Dose Letal Mediana , Camundongos , Camundongos Endogâmicos , Testes de Sensibilidade Microbiana , Oxazóis/isolamento & purificação , Fenitoína/isolamento & purificação , Insuficiência Respiratória/induzido quimicamente , Convulsões/tratamento farmacológico , Testes de Toxicidade , Tremor/induzido quimicamente , Tremor/tratamento farmacológico , Tremorina/toxicidadeRESUMO
HA-1-92, a new oxohexaene polyene macrolide showed significant hypolipidemic and hypoprostatic activity both in rat and rabbit models. HA-1-92 did not elicit significant effect on blood pressure or respiration in anaesthetized rat or on various isolated tissue preparation studies.
Assuntos
Antibacterianos/farmacologia , Hipolipemiantes/farmacologia , Macrolídeos , Próstata/efeitos dos fármacos , Animais , Antibacterianos/toxicidade , Hipolipemiantes/toxicidade , Lipídeos/sangue , Masculino , Tamanho do Órgão/efeitos dos fármacos , Próstata/anatomia & histologia , Coelhos , Ratos , Ratos WistarRESUMO
HA-1-92, a new polyene oxohexaene macrolide antibiotic isolated from Streptomyces CDRIL-312, was incorporated into liposomes containing phosphotidyl choline and cholesterol. The liposomal incorporated HA-1-92 considerably decreased toxicity when compared with free HA-1-92 in mice. Liposomal HA-1-92 showed improved pharmacokinetic profiles in rats. When administered to aspergillosis- and cryptococcosis-infected Balb/c mice, liposomal HA-1-92 showed increased antifungal activity, compared with free HA-1-92, with improved survival rate and decreased colony-forming units in lung, liver, spleen and kidney. These results suggest that liposomal HA-1-92 is more effective than free HA-1-92 in controlling experimental aspergillosis and cryptococcosis in Ba1b/c mice.
