Schiff bases are aldehyde-or ketone-like compounds in which the carbonyl group is replaced by an imine or azomethine group. They are widely used for industrial purposes and also exhibit a broad range of biological activities. This short review compiles examples of the most promising antimalarial, antibacterial, antifungal, and antiviral Schiff bases. An overview of synthetic methodologies used for the preparation of Schiff bases is also described.
The lack of antifungal compounds with reduced side effects highlights the importance of studying natural products for this purpose. Curcumin was a more potent antifungal than fluconazole against P. brasiliensis, the causal agent of the neglected disease paracoccidioidomycosis. Curcumin dramatically inhibited the adhesion of Candida species isolated from AIDS patients to BEC, demonstrating that curcumin is a promising lead compound that warrants further investigation into its therapeutical use in immunocompromised patients.
Nature is an inexhaustible source of natural compounds with interesting biological activities. In general, natural products are an important source of new compounds with a variety of structural arrangements and singular properties. Styryl lactones are a group of secondary metabolites ubiquitous in the genus Goniothalamus that have demonstrated to possess interesting biological properties, in particular antiproliferative activity against cancer cells. In general, the cytotoxicity of styryl lactones appears to be specific against cancer cells since insignificant effects of these compounds on normal cells are reported. A large body of evidence suggests that the antiproliferative activity of styryl lactones is associated with the induction of apoptosis in target cells. In the first part of this review we discuss the biological activities of styryl lactones focusing on cancer cells, the causal agent of Chagas' disease and the vectors for yellow fever and human lymphatic filariasis. Stru described in detail for ninety styryl lactones. The last part describes the molecular targets of styryl lactones for inducing apoptosis, as well as immunosuppressive and inflammatory processes. Overall, understanding how these compounds exert their activities in biological system is essential for future development and application of styryl lactones for human health.
Recebido em 22/2/07; aceito em 6/9/07; publicado na web em 9/4/08 GLUTATHIONE AND RELATED ENZYMES: BIOLOGICAL ROLES AND IMPORTANCE IN PATHOLOGICAL PROCESSES. Glutathione (GSH) and related enzymes are pivotal for the normal functioning of several important biological processes. In this review we discuss the biosynthesis and the catalytic cycles of glutathione as well as the major GSH-related enzymes. We also present how glutathione and enzymes are involved in cancer and the chromatographic and non-chromatographic methods used to analyze glutathione and/or its derivatives.Keywords: glutathione; oxidative stress; cancer.
INTRODUÇÃOA glutationa (GSH, 1, Figura 1), possui papel central na biotransformação e eliminação de xenobióticos e na defesa das cé-lulas contra o estresse oxidativo.1 Este tripeptídeo é encontrado intracelularmente em altas concentrações, essencialmente em todos os organismos aeróbicos. Nota-se a ligação γ-peptídica pouco usual, a presença da porção γ-glutamil e do grupo α-carboxilato livre prevenindo a hidrólise da GSH pelas peptidases celulares que degradam outros peptídeos pequenos. A GSH é o mais abundante tiol celular de baixa massa molecular; a sua concentração é ~ 2mM e mais de 10 mM em eritrócitos humanos e hepatócitos, respectivamente.1 Face à potencialidade de inibidores das enzimas relacionadas à GSH como alvo para o desenvolvimento de substâncias candidatas a fármacos, nesta revisão serão apresentados aspectos importantes do papel fisiológico da glutationa (GSH) e sua implicação em patologias. Considerando esta abordagem, ênfase especial será dada às glutationas transferase e redutase. Uma vez que a investigação do envolvimento da GSH em processos fisiopatológicos requer sua detecção e quantificação em diferentes matrizes, também serão abordados os principais métodos de análise deste tripeptídeo e derivados.Muitas das reações da GSH envolvem o grupo sulfidrila (SH), altamente polarizável, tornando-o um bom nucleófilo para reações com compostos químicos eletrofílicos. Esta habilidade de doar elé-trons a outros compostos também faz da glutationa um bom redutor. A combinação de sua abundância nos organismos aeróbicos e das propriedades químicas do grupo sulfidrila suporta a proposta de que a GSH surgiu na evolução bioquímica como uma proteção contra espécies reativas de oxigênio e compostos eletrofílicos gerados por processos oxidativos, tanto no organismo quanto no ambiente em que este vive.
BiossínteseA biossíntese da GSH ocorre no meio intracelular (exceto em células epiteliais), pela ação consecutiva de duas enzimas. Na primeira reação, é formada uma ligação peptídica entre os aminoácidos glutâmico (2, Figura 2) e cisteína (3), catalisada pela enzima γ-glutamilcisteína sintetase, levando à γ-L-glutamil-L-cisteína (4). Este dipeptídeo é então ligado à glicina pela ação da glutationa sintetase. Estas etapas requerem ATP e Mg +2 . A γ-glutamilcisteína sintetase sofre regulação pela GSH através de um feedback negativo, o que previne a produção excessiva desta ou o acúmulo do intermediário...
Calixarenes, macrocyclic compounds of phenolic units linked by methylene groups at the 2,6-positions, present some of the requirements to serve as platforms for the design and synthesis of biological active compounds. They are also interesting host molecules for chemical biology study purposes. Their basic molecular scaffold has potential ability for molecule recognition; it is promptly synthesized in large amounts, and might be easily modified for maximizing molecular interactions toward relevant guest molecules. Calixarenes present well-defined conformational properties and cavities with molecular dimensions that enable to encapsulate guest drugs. Calixarenes have been shown to have antiviral, antibacterial, antifungal, and anticancer activities (including HIV as target). We provide here an overview of the use of calixarenes either as new chemical entity of distinct biological activities or as host for bioactive guest molecules. The importance of calixarenes for drugs development is discussed. The use of Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS) techniques for the study of calixarenes as biological molecule hosts is also described.
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