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1.
J Inorg Biochem ; 115: 13-9, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22922288

RESUMO

A series of novel platinum(II) complexes derived from N-alkyl-ethanediamine and N-alkyl-propanediamine ligands were prepared and characterized. These complexes contain a long chain aliphatic diamine where the carbon length is variable and present a hydroxyl group in two different positions. The complexes with the ethanediamine derivatives were prepared from K(2)PtCl(4). Interestingly, the propanediamine derivatives did not react well with this platinum salt under the experimental conditions normally employed and could only be obtained from the more reactive K(2)PtI(4). A theoretical molecular modeling study was performed to understand this difference in reactivity and it showed that the conformation around the diamine plays an important role in the ring closure step of complex formation. The complexes had their cytotoxicity investigated in B16F1, CT26, B16F10, and MDA cell lines. Some of them demonstrated superior activity when compared to cisplatin and carboplatin. We were also able to confirm a structure-activity relationship between cytotoxicity and carbon chain length.


Assuntos
Antineoplásicos/síntese química , Citotoxinas/síntese química , Compostos Organoplatínicos/síntese química , Platina/química , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Citotoxinas/química , Citotoxinas/farmacologia , Etilenodiaminas/química , Humanos , Camundongos , Compostos Organoplatínicos/química , Compostos Organoplatínicos/farmacologia
2.
J Ind Microbiol Biotechnol ; 36(8): 1023-7, 2009 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19437056

RESUMO

The biotransformation of 1R-(-)-camphorquinone, achieved by growing cells of four fungi species isolated from soil (Mucor plumbeus, Lecanicillium muscarium, Thamnostylum sp. and Syncephalastrum racemosum), was investigated in optimized culture media for each species. Fungi were grown aerobically under shaking and their activities with respect to camphorquinone were monitored for 20 days by gas chromatography coupled to mass spectrometry (GCMS). Camphorquinone was found to be stable in control flasks throughout the experiment. The most interesting results were found for M. plumbeus, which was only able to perform monoreduction of camphorquinone when cultivated on a glucose-peptone-yeast extract medium. Large-scale experiments were set up and the camphorquinone biotransformation products formed by M. plumbeus were purified by column chromatography and identified by (1)H and (13)C nuclear magnetic resonance (NMR). Theoretical calculations were employed as a complementary technique to unambiguously identify the biotransformation products. These findings suggest that M. plumbeus could be of great use for the selective reduction of camphorquinone and related compounds.


Assuntos
Proteínas Fúngicas/metabolismo , Mucorales/enzimologia , Oxirredutases/metabolismo , Terpenos/metabolismo , Aerobiose , Biotransformação , Meios de Cultura/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Espectroscopia de Ressonância Magnética/métodos , Mucorales/isolamento & purificação , Mucorales/metabolismo , Microbiologia do Solo , Especificidade por Substrato
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