RESUMEN
Two novel Ru(ii) polypyridyl complexes bearing imidazo-phenanthroline conjugated hydroxybenzoic acid groups were designed to enhance the tumor targeting ability as photosensitizers for photodynamic therapy. [Ru(bpy)2(phcpip)] (ClO4)2 (Ru-1) and [Ru(bpy)2(ohcpip)] (ClO4)2 (Ru-2) (bpy = 2,2'-bipyridine; phcpip = 2-(3-carboxyl-4-hydroxyphenyl) imidazo [4,5-f]phenanthroline; ohcpip = 2-(2-hydroxyl-3-carboxyphenyl) imidazo [4,5-f] [1,10] phenanthroline) were synthesized and their photodynamic antitumor activities were investigated. Both complexes displayed high photocytotoxicity toward cancerous cell lines HepG2, A549, MCF-7, and MDA-MB-231, but low photocytotoxicity toward normal cell lines GES-1 and Huvec. They were mainly localized at the nucleus of HepG2 cells after 24 h incubation, arrested the cell cycle at the G2/M phase and induced cancer cell apoptosis through reactive oxygen species (ROS) mediated pathways. Tumor targeting of the complexes is attributed to stronger molecular binding to DNA.
Asunto(s)
Antineoplásicos/farmacología , Complejos de Coordinación/farmacología , Fotoquimioterapia , Fármacos Fotosensibilizantes/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Línea Celular , Proliferación Celular/efectos de los fármacos , Complejos de Coordinación/síntesis química , Complejos de Coordinación/química , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacología , Imidazoles/química , Imidazoles/farmacología , Ensayo de Materiales , Conformación Molecular , Simulación del Acoplamiento Molecular , Fenantrolinas/química , Fenantrolinas/farmacología , Fármacos Fotosensibilizantes/síntesis química , Fármacos Fotosensibilizantes/química , Especies Reactivas de Oxígeno/análisis , Especies Reactivas de Oxígeno/metabolismo , Rutenio/química , Rutenio/farmacologíaRESUMEN
Two GFPPS linked (+)-thalianatriene (1) and (-)-retigeranin B (2) sesterterpene synthase genes were identified from the genome of Arabidopsis thaliana. 1 possesses an unprecedented 11-6-5 tricyclic ring system, while 2 contains a characteristic 5-5-5-6-5 pentacyclic ring system. Their structures were determined by extensive NMR spectroscopy, chemical derivatization, and X-ray crystallography. The variable-temp NMR measurement of 3, a diepoxy-bearing derivative of 1, enables us to completely assign the NMR signals of the two conformers as 3a (67%, UUU) and 3b (33%, UUD). A plausible biosynthesis mechanism of 1 was proposed.
Asunto(s)
Arabidopsis , Cristalografía por Rayos X , Espectroscopía de Resonancia Magnética , Estructura Molecular , SesterterpenosRESUMEN
Based on the statistical theory, the paper collected routine monitoring data for 3 years of 11 municipal wastewater treatment plants with secondary treatment or enhanced secondary treatment in a northern city in China, and analysis of the discharge concentration distribution of COD showed a Delta-lognormal distribution. On this basis, referring to the formulation methods of water pollutant discharge limits used in the USA, the paper studied and assessed the discharge status of COD of the municipal wastewater treatment plants in the city, including the daily maximum and the monthly average discharge status, and came to the conclusion that the daily maximum discharge status met the first grade A class discharge standard (50 mg · L(-1)) required by the Discharge Standard of Pollutants for Municipal Wastewater Treatment Plant (GB 18918-2002). Meanwhile, the assessment conclusion was obtained for the monthly average discharge status, and the conclusions were discussed. The assessment method and the conclusions in this paper might provide reference for formulation and revision of water discharge standards.
