Assuntos
Inibidores da Protease de HIV/farmacologia , HIV-1/efeitos dos fármacos , Sulfonas/farmacologia , Administração Oral , Animais , Disponibilidade Biológica , Cães , Inibidores da Protease de HIV/química , Inibidores da Protease de HIV/farmacocinética , Masculino , Relação Estrutura-AtividadeRESUMO
Oxidation of (+) camphor by cytochrome P-450soy-enriched intact cells of Streptomyces griseus resulted in the formation of one major and several minor metabolites. The minor metabolites were identified as 3-endo-hydroxycamphor (2%), 5-endo-hydroxycamphor (7%), 5-exo-hydroxycamphor (9%), 2,5-diketobornane (2%), and camphorquinone (3%). The major metabolite was isolated and conclusively identified as 6-endo-hydroxycamphor (60%). When supplemented with NADPH, spinach ferredoxin:NADP oxidoreductase and spinach ferredoxin, homogeneous preparations of cytochrome P-450soy oxidized camphor to a mixture of 3-endo-, 5-endo-, 5-exo-and 6-endo-hydroxycamphor. The data presented indicates that cytochrome P-450soy resembles its mammalian counterparts in its lack of regio- and stereospecificity in camphor oxidation.
Assuntos
Cânfora/metabolismo , Streptomyces griseus/metabolismo , Sistema Enzimático do Citocromo P-450/metabolismo , Farinha , Oxirredução , Oxirredutases/metabolismo , Glycine max/enzimologia , Estereoisomerismo , Streptomyces griseus/enzimologia , Streptomyces griseus/crescimento & desenvolvimentoRESUMO
Various species of "Streptomyces," "Aspergillus," "Rhodotorula," "Brevilegnia," "Syncephalastrum," and "Stysanus" were found to transform precocene II to three major metabolites. These major biotransformation products were isolated from a preparative-scale incubation of precocene II with Streptomyces griseus and were conclusively identified as (-)cis- and (+)trans-precocene II-3,4-dihydrodiols and (+)-3-chromenol. 18O2 incorporation studies indicated the involvement of a monooxygenase enzyme system in precocene II transformation by S. griseus. A mechanism is proposed for the formation of (+)-3-chromenol.
Assuntos
Benzopiranos/metabolismo , Inseticidas/metabolismo , Plantas , Streptomyces griseus/metabolismo , Biotransformação , Cromatografia em Camada Fina , Cromatografia Gasosa-Espectrometria de Massas , OxirreduçãoRESUMO
Gilvocarcins are antitumor agents that have been reported to damage DNA upon activation by visible light. This activation is dependent on interaction with DNA. Here it is shown that gilvocarcin V and its synthetic aglycone analogue can both introduce single-strand scission into plasmid DNA. Light irradiation is required for the reaction. The binding of gilvocarcin V to plasmid DNA in the absence of light decreased the DNA linking number in a fashion similar to known intercalating agents such as ethidium bromide. The use of oligonucleotides as substrates for gilvocarcin V demonstrated that one of the steps of the reaction following binding of gilvocarcin V to DNA involves covalent modification at thymidine and to a lesser extent, cytosine residues.
