Synthesis and antiproliferative activity of diethyl 5- acetyl-4-methyl- 6-(2-fluorophenylimino)-6H-thiopyran- 2,3-dicarboxylate (3TM)

Diethyl 5-acetyl-4-methyl-6-(2-fluorophenylimino)-6H-thiopyran-2,3-dicarboxylate (3TM) was synthesized and the antiproliferative activity of 3TM is reported here. Compound 3TM inhibits the growth of human colon cancer HCT-15 with an IC50 value of 4.5 μM and breast cancer MCF-7 with an IC50 value of 7 μM in a dose/time dependent manner by using sulforhodamine B assay. Moreover, suppression of clonogenic activity occurs after exposure to 3TM at a concentration of 3 μM for HCT-15 and of 5 μM for MCF-7. The effect of ligand complexation on DNA structure led to the overall affinity constant of K3M-DNA = 2.4 x 104 M-1.Key words: Diethyl 5-acetyl-4-methyl-6-(2-fluorophenylimino)-6H-thiopyran-2,3-dicarboxylate (3TM), synthesis, antiproliferative activity

El sistema skarn-epitermal de Zn–(Pb–Cu) de Velardeña, Durango (México): Nuevos datos fisicoquímicos de los procesos de mineralización

[eng] The Velardeña mining district is economically the most important of Durango state. The ore deposits occur in different skarn zones developed within the intrusive contact between Mesozoic limestones and Eocene granitic stocks and dikes. The most important ore deposits are related to the Santa María dike and Reyna de Cobre porphyritic stock (separated from each other by 10 km). They occur as irregularly shaped replacement masses developed near the intrusive contact and have a skarn paragenesis dominated by calc-silicates and sulfides. The mineral assemblages show replacement textures and are dominated by calcic clinopyroxene (Di97-53Hd42-02Jh04-01) and garnet (Ad100-57Grs43-00) in the exoskarn, with wollastonite particularly abundant in the endoskarn. Hydrous silicates are actinolite, epidote, and chlorite, whereas sulfides include pyrite, sphalerite, pyrrhotite, galena, chalcopyrite, and sulfosalts. Scheelite, hematite, quartz, and calcite are also present. According to sphalerite geobarometry, the skarns formed at hypabyssal depths (~3-4 km). They developed by a succession of replacive mineralizing events, including (a) a prograde stage at temperatures from ≥470 to 335 °C in conditions of low f (CO2), followed by (b) a retrograde stage from 335 to 220 °C. There was a general increase in f (O2), accompanying the temperature decline during the formation of the system, which accounts for a process of mixing with cooler, oxidizing, and dilute water. During the retrograde stage, wollastonite, calcic garnet and clinopyroxene formed. On the other hand, hydrous silicates, sulfides, sulfosalts, scheelite, and hematite crystallized during the retrograde stage. Skarn mineralization is crosscut by veins of calcite, fluorite, adularia, and sphalerite. The vein mineralization formed at temperatures below 200 °C. The different ore deposits of Velardeña constitute a telescoped skarn-epithermal mineral system.[spa]El distrito minero Velardeña es económicamente el más importante del estado de Durango. En él, las mineralizaciones comprenden diferentes zonas de skarn, desarrolladas entre el contacto de calizas mesozoicas, stocks y diques del Eoceno. Los depósitos de Velardeña más importantes están relacionados al dique Santa María, y el stock porfídico Reyna de Cobre (separados entre sí ~10 km). La mineralización ocurre como reemplazamiento, formando cuerpos irregulares cerca del contacto con los intrusivos, caracterizados por una paragénesis típica de skarn (calcisilicatos y sulfuros). Las asociaciones minerales muestran texturas de reemplazo dominados por clinopiroxeno cálcico (Di53Hd42-02Jh04-01) y granate (Ad100-57Grs43-00) en el exoskarn, y wollastonita particularmente abundante en el endoskarn. Los hidrosilicatos son actinolita, epidota y clorita; los sulfuros incluyen pirita, esfalerita, pirro tita, galena, calcopirita y sulfosales. Scheelita, hematita, cuarzo y calcita también están presentes. El geobarómetro de esfalerita estima que las mineralizacionestipo skarn de Velardeña se formaron a profundidades hipabisales (~ 3-4 km). La mineralización metálica se desarrolló por una sucesión de eventos de reemplazamiento, que incluyen (a) una etapa prógrada a ≥470 a 335 °C y baja f(CO ), seguida por (b) la etapa retrógrada de 335 a 2202°C. Hubo un aumento general de f(O ), durante el descenso de temperatura en laformación del yacimiento, debido a la mezcla de fluidos mineralizantes con agua más fría, oxidante y diluida. Durante la etapa retrógrada, se formaron wollastonita, granate cálcico y clinopiroxeno. La etapa prógrada dio lugar a la formación de hidrosilicatos, sulfuros (inclu- yendo sulfosales), scheelita y hematita. Además de las mineralizaciones tipo skarn en Velardeña, hay vetas epitermales de calcita, fluorita, adularia y esfalerita, cortando los calcosilicatos. La mineralización en estas vetas se estima que se formó a <200 °C. Por ello, es plausible proponer que los depósitos minerales que conforman el distrito minero Velardeña constituyen un sistema skarn-epitermal telescópeado

Versatile Like a Seahorse Tail: A Bio-Inspired Programmable Continuum Robot For Conformal Grasping

Compliant grasping is an important function of continuum robots that interact with humans and/or unpredictable environments. However, the existing robots often have cross-sections that remain constant along their length. This causes the robots to exhibit poor grasping ability, especially when dealing with objects with diverse curvatures. Here, inspired by the high adaptability of seahorse tails in grasping, we proposed a cable-driven continuum robot with tapered tensegrity, capable of conformally grasping objects with various curvatures. To characterize the effects of the tapering on the robot’s kinematics, we derived a mechanical model using multi-body dynamic framework for both predicting the configuration and developing a control strategy for cables. Theoretical predictions indicate that the curvature of each unit can be regulated by altering the length of the cables, allowing the robot to conform to objects with curvatures ranging from 1.48 m-1 to 28.21 m-1. We further employed a continuum robot and tested the control strategy that can be used for grasping floating objects when the curvature of the objects is used as the input. Our robotic design, which presents an example of embedded physical intelligence, can inspire in situ characterization techniques for collecting marine debris

Evaluations of the effect of sodium metabisulfite on the stability and dissolution rates of various model drugs from the extended release polyethylene oxide matrices

Purpose: This study examines the effect of sodium metabisulfite (SMB) as an antioxidant on the stability and release of various model drugs namely propranolol HCl, theophylline and zonisamide from the polyethylene oxide (PEO) tablets. The antioxidant was used to minimise degradation and instability of the manufactured tablets when stored at 40°C (55±5 % RH) over 8 weeks. Method: Multiple batches of tablets weighing 240 mg (50% w/w) with a ratio of 1:1 drug: polymer and 1% (w/w) sodium metabisulfite containing different model drugs and various molecular weights of PEO 750 and 303 were produced. Results: The results indicated that the use of sodium metabisulfite marginally assisted in reducing drug release and degradation via oxidation in propranolol HCl tablets containing both PEO 750 and 303. In the case of poorly and semi-soluble drugs (zonisamide and theophylline) the formulations with both PEO showed entirely superimposable phenomenon and different release profiles compared to control samples (matrices without SMB). DSC study demonstrated the modifications of the polymer due to degradation and observed the effect of SMB on the thermal degradation of the PEO matrices. Conclusion: The use of antioxidant has assisted in retaining the stability of the manufactured tablets with different model drugs especially those with the highly soluble drug that are susceptible to rapid degradation. This has been reflected by an extended release profile of various drugs used at various stages of the storage time up to 8 weeks

Cold Hardiness and Supercooling Capacity in the Overwintering Larvae of the Codling Moth, Cydia pomonella

The codling moth, Cydia pomonella L. (Lepidoptera: Tortricidae), a worldwide apple pest, is classified as a freeze-intolerant organism and one of the most cold-tolerant pests. The objectives of this study were to examine the supercooling point of overwintering and non-diapausing larvae of C. pomonella as an index of its cold hardiness, and to assess larval mortality following 24 h exposure to extreme low temperatures ranging from -5 to -25°C. The mean (±SE) supercooling point for feeding larvae (third through fifth instars) was -12.4 ± 1.1°C. The mean supercooling point for cocooned, non-diapausing larvae (i.e., non-feeding stages) decreased as the days that the arvae were cocooned increased and changed between -15.1 ± 1.2°C for one to two day cocooned arvae and -19.2 ± 1.8°C for less than five day cocooned larvae. The mean (±SE) supercooling point for other non-feeding stages containing pupae and overwintering larvae were -19.9 ± 1.0°C and -20.2 ± 0.2°C, respectively. Mean supercooling points of C. pomonella larvae were significantly lower during the winter months than the summer months, and sex had no effect on the supercooling point of C. pomonella larvae. The mortality of larvae increased significantly after individuals were exposed to temperatures below the mean supercooling point of the population. The supercooling point was a good predictor of cold hardiness

Poly(vinylidene fluoride) and copolymers as porous membranes for tissue engineering applications

Poly(vinylidene fluoride) (PVDF) and its main copolymers - poly(vinylidene fluoride-co-hexafluoropropene), P(VDF-HFP), and poly(vinylidene fluoride-co-trifluoroethylene), P(VDF-TrFE) - were processed by solvent casting at room temperature in the form of porous membranes. Copolymer membranes showed higher degree of porosity than PVDF, the average pore size being larger for P(VDF-TrFE) than for P(VDF-HFP) and PVDF. All membranes show high hydrophobicity with water contact angles in the range 94° to 115°, and electroactive beta phase contents above 90%. The adhesion and proliferation of both C2C12 myoblast and MC3T3-E1 pre-osteoblast cells on the membranes were investigated. It is demonstrated that PVDF membranes promote higher cell proliferation while P(VDF-HFP) membranes show the lowest proliferation for both kinds of cell. The proliferation on P(VDF-TrFE) membranes is cell dependent, higher for MC3T3-E1 cells but lower for C2C12 cells, related to the effect of the highly porous structure on the preferred morphology of each cell type, as the higher pore size and porosity of the P(VDF-TrFE) membrane induce cell elongation, which is preferred just by the C2C12 muscle cells.Funded by FEDER funds through the “Programa Operacional Fatores de Competitividade e COMPETE” and by national funds arranged by FCT Fundação para a Ciência e a Tecnologia, project references PTDC/CTM-NAN/112574/2009 and PEST-C/FIS/UI607/2014. Funding from “MateproOptimizing Materials and Processes”, ref. NORTE-07-0124-FEDER-000037”, co-funded by the “Programa Operacional Regional do Norte” (ON.2 e O Novo Norte), under the “Quadro de Referência Estrategico Nacional” (QREN), through the “Fundo Europeu de Desenvolvimento Regional” (FEDER). FCT for the SFRH/BPD/90870/2012 grant