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Kely N. de Oliveira,Helena C. Castro,Márcia M. Souza,Plínio Cunha Sathler,Uiaran O. Magalhães,Carlos R. Rodrigues,Patrícia R. Palm,Maicon Sarda,Pablo E. Perotto,Sabrina Cezar,Monique A. de Brito,Arian 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.10
In this paper, we describe the antinociceptive activity, molecular modeling and in silico ADMET screening of a series of sulphonyl-hydrazone and sulphonamide imidobenzene derivatives. Among these compounds, the sulphonyl-hydrazones 9 and 11 showed the most potent analgesic activity (ID50 = 5.1 and 6.8 μmol/kg, respectively). Interestingly, all derivatives evaluated in this study have a better analgesic profile than the control drugs, acetyl salicylic acid and acetaminophen. Derivative 9 was the most promising compound; with a level of activity that was 24 times higher than the control drugs. Our SAR study showed a relationship among the distribution of the frontier orbital HOMO coefficients, HOMO-LUMO energy gap of these molecules and their reactivity. The best analgesic compounds (including 6, 9, 10, 11 and 12) fulfilled the Lipinski “rule-of-five”, which is theoretically important for good drug absorption and permeation.
Higuera-Rubio Jesús M.,Ibarra-Laclette Enrique,Reyes-López Miguel A.,Sandoval-Castro Eduardo,Cruz-Mendívil Abraham,Vega-García Misael O.,Calderón-Vázquez Carlos L. 한국식물생명공학회 2022 Plant biotechnology reports Vol.16 No.4
This study aims to disentangle avocado enzymatic browning by identifying and analyzing the PPO coding genes. Two avocado accessions (AVO48 and San Miguel) and the Hass cultivar with contrasting browning kinetics and enzyme activity levels were selected for gene characterization. Upon 90 min of light exposure, Hass and San Miguel showed a greater decrease in luminosity retention (closer to 40% of initial luminosity) compared to AVO48 (85% of luminosity). PPO activity in crude extracts was significantly higher (P < 0.05) in San Miguel (696 U μg-1 protein) than Hass (174 U μg-1 protein) and AVO48 (46–56 U μg-1 protein). San Miguel showed a higher Vmax Km-1 ratio (20.88 min-1), followed by Hass (14.29 min-1) and AVO48 (1.64 min-1), suggesting that San Miguel and Hass have higher substrate affinity. Four PPO coding genes: PamPPO1, PamPPO2, PamPPO3 and PamPPO4 were identified in the Hass genome, all of them containing the main features of plant PPOs, but with specific amino acid combinations in the catalytic pocket of the tyrosinase domain; suggesting that PPO1, PPO2 and PPO4 have monophenolase activity, whereas PPO3, has o-diphenolase activity. The evidence of transcription of PPO3 in fruit of the three genotypes suggests an important role for this gene in avocado pulp browning. PPO2 expression was only found in AVO48. This research provides gene candidates for selective silencing to reduce enzymatic browning.
Lopera Alex A.,Bezzon Vinicius D. N.,Ospina Victoria,Higuita-Castro Jorge L.,Ramirez Francisco J.,Ferraz Humberto G.,Orlando Marcos T. A.,Paucar Carlos G.,Robledo Sara M.,Garcia Claudia P. 한국세라믹학회 2023 한국세라믹학회지 Vol.60 No.1
Many efforts in the tissue engineering field have been devoted to producing biomedical devices with several physico-chemical properties that could promote an increase in the quality of therapeutic treatments. Thus, 3D printing is an efficient method which facilitates manufacturing high quality products to be used as medical devices. However, high-performance materials are required for obtaining products that are able to be 3D printed to attend the biomedical concerns. In this work, fused PLA-calcium phosphate-tobramycin-based filaments with antimicrobial properties were produced. X-ray powder diffraction, Fourier transform infrared spectroscopy and thermal analysis were performed to characterize the pure compounds as well as the composite filaments, revealing that the drug is preserved into the filaments by the implemented methodology, even after the hot extrusion procedure. The filaments and the printed pieces presented great antimicrobial effect and a controlled-release profile was also observed by the drug-release assays for the filaments produced, thereby indicating this material as a promising candidate to be used for implantable medical devices in the future.