RESUMEN
Reaction of BiCl3 with 2-(2-hydroxy-3-methoxyphenyl)benzimidazole (HL) in tetrahydrofuran (THF) under reflux gave mononuclear complex of formula [Bi(HL)2Cl3·H2O]. The binding interaction of the complex with bovine serum albumin (BSA) was investigated using the fluorescence quenching method. The experimental results showed that the complex could bind to BSA in the proportion of about 1:1. The binding reaction was spontaneous and hydrophobic force played major role in the reaction. The binding of the complex to BSA could change the microenvironment and conformation of BSA.
Asunto(s)
Bencimidazoles/química , Bismuto/química , Complejos de Coordinación/química , Animales , Bencimidazoles/síntesis química , Bencimidazoles/metabolismo , Bismuto/metabolismo , Bovinos , Complejos de Coordinación/síntesis química , Complejos de Coordinación/metabolismo , Cristalografía por Rayos X , Interacciones Hidrofóbicas e Hidrofílicas , Ligandos , Modelos Moleculares , Unión Proteica , Albúmina Sérica Bovina/química , Albúmina Sérica Bovina/metabolismo , Espectrometría de Fluorescencia , TermodinámicaRESUMEN
Nordihydroguaiaretic acid (NDGA) and its synthetic analogues are potentially useful in treating diseases related to cancers, diabetes, viral and bacterial infections, and inflammation. In this paper, we report the optimal synthetic methods and the bioactivity study of terameprocol 2, NDGA derivative 3, and its cyclized analogue 4. The IC50 of these three compounds 2, 3 and 4 on the growth metabolism of Schizosacchromyces pombe and K562 cell lines were determined by microcalorimetry. The preliminary results showed that the compounds 2, 3 and 4 possessed good inhibition activities on S. pombe and K562 cell lines, and exhibited bidirectional biological effect and Hormesis effect. In particular, terameprocol 2 was found to possess the most potent inhibitory effect on K562 cell lines.
Asunto(s)
Antifúngicos/farmacología , Masoprocol/farmacología , Schizosaccharomyces/efectos de los fármacos , Antifúngicos/síntesis química , Antifúngicos/química , Relación Dosis-Respuesta a Droga , Humanos , Células K562 , Masoprocol/síntesis química , Masoprocol/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad , Células Tumorales CultivadasRESUMEN
This paper reports the synthesis of a new bioactive complex, 8-hydroxyquinolinato-bis-(salicylato) yttrium (III) (HSAY), whose composition and structure were characterized by elemental analysis, IR spectra, thermogravimetric analysis, and X-ray diffraction. The power-time curves of the compounds HSAY, C(7)H(6)O(3), C(9)H(7)NO, and YCl(3)·6H(2)O on the growth metabolism of Schizosaccharomyces pombe (S. pombe) were determined at 32.00°C, respectively. The corresponding thermokinetics parameters, which include the microbial growth rate constant (κ), inhibition ratio (I), and half inhibition concentration (IC(50)), were also derived. The results showed that the generation time was 168.2 min, and all the compounds HSAY, C(7)H(6)O(3), C(9)H(7)NO, and YCl(3)·6H(2)O possessed good bioactivities on the growth metabolism of S. pombe, with the values of IC(50) being 0.055, 3.57, 0.057, and 1.35 mmol L(-1), respectively. The inhibition ability of these compounds above on the growth of the S. pombe has been observed to decrease in the order HSAY>C(9)H(7)NO>YCl(3)·6H(2)O>C(7)H(6)O(3).
