RESUMO
A nonvolatile and slightly water-soluble antimicrobial sulfur compound newly isolated from heated garlic extract was characterized. The compound was generated most when heated at 120°C for 30 minutes and completely disappeared after 90 minutes of heating. It has a molecular mass of 225 daltons with an elemental ratio of C6H11N1O2S3, and the interpretation of ¹H- and ¹³C-nuclear magnetic resonance and Fourier transform-infrared data showed that the compound was CH2=CH-CH2-S-S-S-CH2-CH(NH2)COOH, 3-(allyltrisulfanyl)-2-aminopropanoic acid, a derivative of cysteine, presumably derived from alliin (S-allyl-L-cysteine sulfoxide). This novel compound has comparatively potent anti-yeast activity and rather weak antibacterial activity, similar to other antimicrobial compounds in garlic.
Assuntos
Anti-Infecciosos/isolamento & purificação , Alho/química , Temperatura Alta , Compostos de Sulfidrila/isolamento & purificação , beta-Alanina/análogos & derivados , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Peso Molecular , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Compostos de Sulfidrila/química , Compostos de Sulfidrila/farmacologia , Volatilização , Água , Leveduras/efeitos dos fármacos , beta-Alanina/química , beta-Alanina/isolamento & purificação , beta-Alanina/farmacologiaRESUMO
OBJECTIVES: Clevudine has demonstrated antiviral potency in the treatment of naïve chronic hepatitis B patients in pivotal studies. The objectives of this study were to evaluate the safety and efficacy of a 1-year treatment with clevudine in chronic hepatitis B patients. METHODS: This is a post-marketing surveillance using case report forms which were submitted to the health authorities. RESULTS: Analysis of individual data showed that hepatitis B virus (HBV) DNA after a 1-year treatment was <141,500 copies/ml in 96% of hepatitis B e antigen (HBeAg)-positive and 100% of HBeAg-negative patients. The proportion of patients with HBV DNA <2,000 copies/ml after a 1-year treatment was 74%: 71% of HBeAg-positive and 93% of HBeAg-negative patients. Most of the patients with HBV DNA below the detection limit with each assay at week 24 showed sustained viral suppression up to week 48. The proportion of patients who showed normal alanine aminotransferase at week 48 was 86% in HBeAg-positive patients and 87% in HBeAg-negative patients. The rates of HBeAg-loss were 21%. Two patients showed viral breakthrough during treatment. CONCLUSION: Clevudine monotherapy demonstrates potent antiviral activity as well as biochemical and serological response with a 0.7% rate of viral breakthrough in naïve chronic hepatitis B patients.
