Currently, cancer is the second most common cause of death in the United States, exceeded only by heart disease. Chemotherapy traditionally suffers from a non-specific distribution, with only a small fraction of the drug reaching the tumor, in this sense, the use of dendrimers incorporating drugs non-covalently encapsulated inside the dendrimer or covalently conjugated have proven to be effectives against different cancer cell lines. However, at present the dendrimers used as drug-carriers still do not meet the necessary characteristic to be considered as an ideal dendrimer for drug delivery; high toxicity, bio-degradability, low toxicity, biodistribution characteristics, and favorable retention with appropriate specificity and bioavailability have not been fully covered by the current available dendrimers. However, the development and study of new dendrimers drug-carriers continues to be an important tool in the cancer therapy as they can be functionalized with varied ligands to reach the tumor tissue through the different body barriers in the body with minimal loss of activity in the bloodstream, have the ability to selectively kill tumor cells without affecting the normal cells and most important with a release mechanism controlling actively. Given the continuous efforts and research in this area of interest, we presented in this review the work done with a special emphasis on the development of dendrimers as a major tool in the combination with drugs, as a potential adjunctive agent in anticancer therapy.
Keeping in mind the concept of green chemistry, this research aims to synthesize and characterize new ionic liquids (ILs) derived from N-cinnamyl imidazole with different sizes of alkyl chains (1, 6, 8, and 10 carbon atoms), and evaluate their antibacterial activity against Skin and soft tissue infections (SSTIs) causative bacteria. The antibacterial screening was carried out by agar well diffusion and the Minimum Inhibitory Concentration (MIC) and Half Maximum Inhibitory Concentration (IC50) of the different ILs were determined by microdilution in broth, also Molecular dynamics simulations were performed to study the interaction mechanism between ILs and membranes. The MIC value in Gram-positive bacteria showed that as the hydrocarbon chain increases, the MIC value decreases with a dose-dependent effect. Furthermore, Gram-negative bacteria showed high MIC values, which were also evidenced in the antibacterial screening. The molecular dynamics showed an incorporation of the ILs with the longer chain (10 C), corresponding to a passive diffusion towards the membrane surface, for its part, the ILs with the shorter chain due to its lack of hydrophobicity was not incorporated into the bilayer. Finally, the new ILs synthesized could be an alternative for the treatment of Gram-positive bacteria causative of SSTIs.
17 September 2021 in International Journal of Food Science
With the continuous increase in research on lipids, technologies and the development of chemical-analytical methods associated with the characterization and monitoring of different processes that involve modifications in edible fats are increasing. The beneficial effect of lipids, especially those essential for the health of the population, is widely known. However, degradation compounds are also produced that eventually have negative effects. In this dual context, the monitoring of the changes suffered by nutritional compounds can be obtained thanks to the development of technologies and analytical methods applied to the study of lipids. The modifications that lipids undergo can be followed by a wide variety of methods, ranging from the basic ones associated with simple chemical titrations to the more complex ones associated with sophisticated laboratory equipment. These determinations involve chemical and/or physical quantification of lipids to know an initial condition on the major and minor components. In addition to technologies that allow monitoring during more complex processes such as thermal deterioration, in multiple conditions depending on the objective of the study, this review could benefit a comprehensive understanding of lipid deterioration for future developments and research in the study of fats and oils for human consumption.
A facile [3 + 2]cycloaddition/oxidation/aromatization cascade reaction for the synthesis of pyrrolo[2,1-a]isoquinolines and indolizino[8,7-b]indoles has been developed. This tandem approach was accomplished by employing tert-butyl hydroperoxide (TBHP) as the environmentally benign stoichiometric oxidant, with the catalysis of non-toxic tetrabutylammonium iodide (TBAI) and isopropanol as the green solvent. Gratifyingly, this protocol is highly versatile, as the construction of polycyclics could be tailored by readily available dipolarophiles. Only a catalytic amount of TBAI was required, as the hypervalent electrophilic iodine species (IOH) can be recovered in situ by oxidation with TBHP. Furthermore, for the first time, the mechanistic aspects and the putative intermediates associated with this cascade have been intercepted and characterized by online monitoring of the reaction by using ESI-MS/MS.
Background: Regular consumption of fruits and vegetables (e.g., tomatoes) has been shown to be beneficial in terms of reducing the incidence of cardiovascular diseases. The industrial processing of tomatoes into tomato-based products includes several thermal treatments. Very little is known on the effect of tomato industrial processing on antiaggregatory activity and phenolic profile. Methods: It was assessed the effect of tomato and by-products extracts on platelet aggregation induced by ADP, collagen, TRAP-6 and arachidonic acid. These in vitro antithrombotic properties were further supported in an in vivo model of thrombosis. A set of antiplatelet compounds has been selected for HPLC analysis in the different extracts. Results: Some natural compounds such as chlorogenic, caffeic, ferulic and p-coumaric acids were identified by HPLC in tomatoes and its products may inhibit platelet activation. Red tomatoes, tomato products (sauce, ketchup and juice) and by-products extracts inhibited platelet aggregation induced adenosine 5'-diphosphate, collagen, thrombin receptor activator peptide-6 and arachidonic acid, but to a different extent. Also, pomace extract presents antithrombotic activity. Conclusions: Processed tomatoes may have a higher content of health-benefiting compounds than fresh ones. Pomace even presents the best antiplatelet activity. Finally, tomato products may be used as a functional ingredient adding antiplatelet activities to processed foods.
5 June 2017 in Journal of Thermal Analysis and Calorimetry