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1.
Vasiliy S. Koval Albert F. Arutyunyan Victor L. Salyanov Regina R. Klimova Alla A. Kushch Ekaterina Yu. Rybalkina Olga Yu. Susova Alexei L. Zhuze 《Bioorganic & medicinal chemistry》2018,26(9):2302-2309
A series of DNA minor groove binding fluorescent dimeric bisbenzimidazoles DBA(n) bearing linkers of various length were synthesized and their biochemical and antiviral activities were evaluated. Their antiviral activity was assessed in model cell systems infected with human herpes simplex virus (HSV-1) and cytomegalovirus (CMV). Compounds DBA(1) and DBA(7) demonstrated in vitro inhibitory properties towards HSV-1, and DBA(7) completely blocked the viral infection. Compound DBA(11) displayed the in vitro therapeutic activity towards both HSV-1 and CMV. All of the DBA(n) could fluoresce, were well soluble in water, not cytotoxic to a concentration of 240?µM, penetrated well into cell nuclei by binding to DNA and could inhibit topo-I at low micromolecular concentrations. 相似文献
2.
Ricardo Iván González-Vega José Luis Cárdenas-López José Antonio López-Elías Saúl Ruiz-Cruz Aline Reyes-Díaz Liliana Maribel Perez-Perez Francisco Javier Cinco-Moroyoqui Ramón Enrique Robles-Zepeda Jesús Borboa-Flores Carmen Lizette Del-Toro-Sánchez 《Saudi Journal of Biological Sciences》2021,28(2):1401-1416
Navicula incerta is a marine microalga distributed in Baja California, México, commonly used in aquaculture nutrition, and has been extended to human food, biomedical, and pharmaceutical industries due to its high biological activity. Therefore, the study aimed to optimize culture conditions to produce antioxidant pigments. A central composite experimental design and response surface methodology (RSM) was employed to analyze the best culture conditions. The medium (nitrogen-deficient concentrations), salinity (PSU = Practical Salinity Unity [g/kg]), age of culture (days), and solvent extraction (ethanol, methanol, and acetone) were the factors used for the experiment. Chlorophyll a (Chl a) and total carotenoids (T-Car), determined spectroscopically, were used as the response variables. The antioxidant capacity was evaluated by DPPH? and ABTS?+ radical inhibition, FRAP, and anti-hemolytic activity. According to the overlay plots, the optimum growth conditions for Chl a and T-Car production were the following conditions: medium = 0.44 mol·L-1 of NaNO3, salinity = 40 PSU, age of culture: 3.5 days, and solvent = methanol. The pigment extracts obtained in these optimized conditions had high antioxidant activity in ABTS?+ (86.2–92.1% of inhibition) and anti-hemolytic activity (81.8–96.7% of hemolysis inhibition). Low inhibition (33–35%) was observed in DPPH?. The highest value of FRAP (766.03 ± 16.62 μmol TE/g) was observed in the acetonic extract. The results demonstrated that RSM could obtain an extract with high antioxidant capacity with potential applications in the biomedical and pharmaceutical industry, which encourages the use of natural resources for chemoprevention of chronic-degenerative pathologies. 相似文献