A gel can be considered to be a two-phase (liquid and solid) system, which lacks flow once it reaches a stationary state. The solid phase is usually a tridimensional polymeric mesh, while the liquid phase is usually found in three forms: contained in great cavities, retained in the capillary pores between micelles, or adsorbed on the surface of a micelle. The influence of the use of gels in crystal growth is diverse and depends on the type of gel being used. A decrease in solubility of any solute in the liquid may occur if the solvent interacts extensively with the polymeric section, hence, the nucleation in gels in these cases apparently occurs at relatively low supersaturations. However, if the pore size is small enough, there is a possibility that a higher supersaturation is needed, due to the compartmentalization of solvents. Finally, this may also represent an effect in the diffusion of substances. This review is divided into three main parts; the first evaluates the theory and practice used for the obtainment of polymorphs. The second part describes the use of gels into crystallogenesis of different substances. The last part is related to the particularities of protein crystal polymorphism, as well as modern trends in gel growth for high-resolution X-ray crystallography.
Giardiasis is a worldwide parasitic disease that affects mainly children and immunosuppressed people. Side effects and the emergence of resistance over current used drugs make imperative looking for new antiparasitics through discovering of new biological targets and designing of novel drugs. Recently, it has determined that gastric proton-pump inhibitors (PPI) have anti-giardiasic activity. The glycolytic enzyme, triosephosphate isomerase (GlTIM), is one of its potential targets. Therefore, we employed the scaffold of PPI to design new compounds aimed to increase their antigiardial capacity by inactivating GlTIM. Here we demonstrated that two novel PPI-derivatives (BHO2 and BHO3), have better anti-giardiasic activity than omeprazole in concentrations around 120–130 µM, without cytotoxic effect on mammal cell cultures. The derivatives inactivated GlTIM through the chemical modification of Cys222 promoting local structural changes in the enzyme. Furthermore, derivatives forms adducts linked to Cys residues through a C-S bond. We demonstrated that PPI can be used as scaffolds to design better antiparasitic molecules; we also are proposing a molecular mechanism of reaction for these novel derivatives.
A new anacardic acid, 6-[16′Z-nonadecenyl]-salicylic acid (1), along with seven known compounds, 6-[8′Z-pentadecenyl] salicylic acid (15:1 anacardic acid) (2), 6-nonadecenyl salicylic acid (anacardic acid 19:0) (3), 6-pentadecyl salicylic acid (anacardic acid 15:0) (4), masticadienonic acid (5), 3α-hydroxymasticadienonic acid (6), 3-epi-oleanolic acid (7) and β-sitosterol, were isolated from the bark of Amphipterygium adstringens using a bioassay-guided fractionation method. The structure of the new compound (1) was elucidated by spectroscopic data interpretation. The known compounds (2–7) were identified by comparison of their spectroscopic data with reported values in the literature. Compounds 1–4 exhibited antibacterial activity against Streptococcus mutans and Porphyromonas gingivalis with minimum inhibitory concentrations ranging from 7 to 104 µg mL and from 12 to 126 µg mL, respectively.