Ibuprofen-Maltodextrin Interaction: Study of Enantiomeric Recognition and Complex Characterization

The interaction between ibuprofen and maltodextrins with different dextrose equivalent was studied in solution and solid state in order to investigate the effect on the solubility of ibuprofen and to determine their usefulness in terms of chiral recognition. Apparent binding constants were calculated using nuclear magnetic resonance spectroscopy experiments and solubility studies. The results showed an increase in the apparent solubility of ibuprofen in the presence of maltodextrins that depended on their ionization state. The freeze-drying method was used to prepare solid complexes, while physical mixtures were obtained by simple blending. These solid systems were characterized in the solid state using differential scanning calorimetry, thermogravimetric analysis, Fourier Transform-Infrared spectroscopy, scanning electron microscopy and X-ray diffractometry. Detailed nuclear magnetic resonance studies provided evidence of the influence of the type and concentration of the maltodextrin host on the chiral recognition of racemic ibuprofen, indicating that these linear ligands act as chiral selectors.

Molecular Modeling of Quinoline-Based Compounds as Potential Dual Inhibitors of Reverse Transcriptase and Integrase of HIV

As follow-up of our past publication?[1], we propose that quinolones (as part of the pyridinone family) are capable to increase the number of interactions with HIV reverse transcriptase (RT) or integrase (IN) by adding a halogen in position C-8 of aromatic portion of the quinolones. This addition could help with the activity of dual inhibitors of RT and IN. In this work, we add a chlorine atom with the rationale to identify in the docking simulations a halogen interaction with the oxygen in the near aminoacids in the binding pockets of RT and IN enzymes. Our docking studies started with RT and 320 structures. Later, we took 73 structures with good results in docking with RT. The structures that we choose contain ester or acids groups in C-3 due the structural similarity with groups in charge to interact with the Mg++ ions in Elvitegravir. In conclusion, we obtained 14 structures that could occupy the allosteric pocket of RT and could inhibit the catalytic activity of IN, for this reason could be dual inhibitors. A major perspective of this work is the synthesis and testing of the potential dual inhibitors designed.

Determination of sildenafil by preconcentration on surfactant coated polymeric resin followed by spectrofluorimetry

The illicit addition of phosphodiesterase type-5 （PDE-5） inhibitors like sildenafil （Viagra） in product offered as herbal medicine or dietary supplement for male erectile dysfunction has concerned authorities in recent times. In this paper, we proposed a sensitive surfactant-coated Amberlite XADTM resin for sildenafil preconcentration method with spectrofluorimetric detection. Retention capacity of micellar coated XAD resin for sildenafil was studied and the obtained eluate was measured by spectrofluorometer at excitation and emission wavelengths of 350 and 430 nm, respectively. This method allowed the detection of sildenafil at 0.15 ng/mL with linear range of 0.0003-7.0 μg/mL. The method has been successfully applied to the analysis of some local commercially available herbal medicines and urine.

Determination of Paraquat in Several Commercially Available Types of Rice

Introduction: Paraquat (1,1’-dimethyl-4,4’-bipyridine-dichloride) is a herbicide used to combat weeds and improve crop productivity. Its acute toxicity can cause fatal poisoning in humans and animals and several studies have shown a strong correlation between paraquat and Parkinson’s disease. Objective: To determine the concentration of paraquat in different types of rice in Brazil. Method: Paraquat quantification is based on a complexation reaction with sodium dithionite, which generates a blueish color compound, whose absorbance was read in a spectrophotometer at the 600 nm wavelength. Results: Five samples were found to be above the maximum allowed limit, while one sample had a concentration in the upper allowed limit. The method employed did not allow quantification of black rice. Conclusion: There is a need for identification of the type of pesticide used in each examined crop as well as their respective dates of remission in order to improve the safety of agricultural practices.

Detection of Gene Dosage in Circulating Free Plasma DNA as Biomarker for Lung Cancer

The increase in the number of gene copies at specific loci is a genetic alteration frequently associated with over expression of the related protein in cancer cells. Genes whose dose is consistently augmented in cancer include those involved in cell cycle control, proliferation, apoptosis, and angiogenesis among others. In this study, gene dose of onc ogenes MYCL1, MYCN, MYC, EGFR, ERBB2 and AKT2 in DNA obtained from lung tissue and blood plasma, of patients with primary lung cancer was evaluated with respect to normal lung tissue and plasma DNA of healthy individ uals, to determine the capacity of these genes to discriminate normal and neoplastic phenotypes. The number of copies of each gene was determined using real-time (2-△△CT). The AKT2 oncogene was found to be amplified frequently in plasma DNA from patients (74% of cases). This marker showed a noticeable ability to discriminate normal and neo-plastic phenotypes, with a 76 to 89% probability of correctly recognize a plasma sample provided by a lung cancer patient or a healthy individual. For this reason, this detection could be a very useful tool to supplement the existing diagnostic methods in pulmonary cancer.

Sensory denervation with capsaicin reduces ovarian follicular development and delays the onset of puberty in guinea pigs

Introduction: It has been documented that mammalian ovaries receive sympathetic, parasympathetic and sensory nerve fibers. The aim of this work was to investigate the effects of sensory denervation with capsaicin at the first vaginal opening (FVO) on follicular development and the expression of TRPV1 receptors in ovary cells as well as in the dorsal root ganglia (DRGs) and lumbar dorsal spinal cord neurons of guinea pigs. The DRGs and lumbar dorsal spinal cord neurons serve as a nerve connection from the ovaries to the CNS. Materials and Methods: Female guinea pigs received a subcutaneous injection of capsaicin (30 mM) at 10 days of age (P10), while control animals were injected with vehicle. Using light microscopy, we counted healthy preantral follicles (HPF), healthy antral follicles (HAF), atretic preantral follicles (APF), and atretic antral follicles (AAF) in the ovaries at the FVO, and the numbers of TRPV1-positive cells were counted in the ovarian follicles, DRGs, and lumbar dorsal spinal cord (L2-L4) neurons by immunohistochemistry. Results: Guinea pigs treated with capsaicin showed a significant delay of FVO in comparison with the control animals (36 vs. 44 days). In the ovaries, the number of preantral and antral follicles decreased significantly. Additionally, the number of TRPV1-positive thecainterstitial cells of the antral follicles was reduced significantly, and the number of TRPV1-positive neurons in the DRGs and lumbar dorsal spinal cord (L2-L4) decreased. Thus, we showed that TRPV1 receptors throughout the sensory fibers modulate ovarian follicular development and the onset of puberty in guinea pigs. Conclusion: Sensory denervation decreases ovarian follicular development and delays the onset of puberty of guinea pigs. Our data support the idea that through TRPV1 receptors, ovarian afferent fibers sense local stimuli that are sent to the CNS.

Morphological and biochemical effects of weekend alcohol consumption in rats: Role of concentration and gender

AIM To examine the association between weekend alcohol consumption and the biochemical and histological alterations at two different concentrations of alcohol in both genders in rats.METHODS Wistar rats weighing 170-200 g were divided into groups as follows:(1) Control groups; and(2) weekend alcohol-consumption group: 2 d/weekly per 12 wk, at two different concentrations:(1) Group of males or females with a consumption of a solution of alcohol at 40%; and(2) group of males or females with a consumption of a solution of alcohol at 5%. At the end of the experiment, serum and liver samples were obtained. The following enzymes and metabolites were determined in serum: Alanine Aminotransferase(ALT), Aspartate Aminotransferase(AST), Lactate Dehydrogenase, and Gamma-Glutamyltransferase, and glucose, triglycerides, cholesterol, bilirubin, and albumin. Liver samples from each group were employed to analyze morphological abnormalities by light microscopy.RESULTS In all of the weekend alcohol-consumption groups, AST activity presented a significant, 10-fold rise. Regarding ALT activity, the groups with weekend alcohol consumption presented a significant increase that was six times greater. Bilirubin levels increased significantly in both groups of females. We observed a significant increase in the parameters of fatty change and inflammation due to weekend alcohol consumption. Only the group of females that consumed alcohol at 40% presented slight hepatocel ular disorganization CONCLUSION The results obtained herein provide solid evidence that weekend alcohol consumption gives rise to liver damage, demonstrated by biochemical and histological alterations, first manifested acutely, and prolonged weekend alcohol consumption can cause greater, irreversible damage.

Crystal Structure, Synthesis and Biological Activity of Ether and Ester <i>Trans</i>-Ferulic Acid Derivatives

The structures of methoxymethyl (E)-3-(4-hydroxy-3-methoxyphenyl)acrylate, 2;(E)-3-(3-methoxy-4-(methoxymethoxy)phenyl)acrylic acid, 3;methyl (E)- 3-(4-(benzyloxy)-3-methoxyphenyl)acrylate, 4;benzyl (E)-3-(4-(benzyloxy)- 3-methoxyphenyl)acrylate, 6;and (E)-3-(4-(benzyloxy)-3-methoxyphenyl)- acrylic acid, 7;were established by spectroscopic and X-ray diffraction studies. Structure 2 is a new com-pound. Compounds with free phenolic hydroxyls v.gr. methyl (E)-3-(4-hydroxy-3-methoxyphenyl)acrylate 1, 2 and ben-zyl(E)-3-(4-hydroxy-3-methoxyphenyl)acrylate 5, showed scavenging free- radical and antioxidant activity while moderate scavenging free-radical was observed in compound 3. Moderate inhibition of lipid peroxidation was observed for 7. Compound 5 exerted significant inhibition of cell growth in PC-3, K562 tumor cell lines and 4 exhibited the largest cytotoxic effect upon the K562 cell line.

Molecular Modeling of Potential Dual Inhibitors of HIV Reverse Transcriptase and Integrase

With the goal of suggesting dual inhibitors of HIV reverse transcriptase (RT) and integrase (IN), herein we report the molecular docking of an initial set of 556 compounds related to the pyridinone class. Docking with multiple crystallographic structures of HIV-1 RT led to 160 potential binders of RT interacting with key amino acid residues at the enzyme’s allosteric site. Compounds selected from the docking with RT were further docked with a crystallographic structure of HIV-1 IN. A total of 31 structures had the potential to make contacts with Mg2+ ions located in a small space between DNA and IN. Interactions with Mg2+ ions are relevant because they participate in the stabilization of the IN-DNA complex. In conclusion, 31 compounds synthetically accessible are proposed as dual inhibitors of RT and IN. It is hypothesized that the suggested compounds will inhibit RT by occupying the allosteric site for NNRTIs and will inhibit the catalytic activity of IN by destabilizing the IN-DNA complex. The main perspective of this work is the synthesis and biological testing of the candidate molecules.

Protective Effect of Phenolic-Rich Extracts from Different Parts of <i>Opuntia joconostle</i>Fruit against Carbon Tetrachloride-Induced Oxidative Stress in Mice

Opuntia joconostle fruit is a rich source of biocompounds such as polyphenols including gallic, vanilic, 4-hidroxybenzoic, cafeic, and syringic acids, catechin, epicatechin, rutin, and vanillin, besides betalains. The objective of this research was to evaluate the effect of supplementation polyphenols-rich extracts from different parts of Opuntia joconostle against carbon tetrachloride-induced oxidative stress in a mouse model. The animals were treated orally with polyphenols-rich extracts at 50, 100 and 200 mg/kg BW for 30 consecutive days. On day 30th the mice received carbon tetrachloride (CCl4) as hepatoxic agent. Biochemical evaluations were carried out 24 h after induction of the oxidative stress. Data showed that methanolic extracts from different parts of Opuntia joconostle exerting protective effect against the CCl4-induced oxidative stress in mice. Histology examination revealed that the damage decreased in groups treated with polyphenols-rich extracts compared to the group that did not receive any treatment. Opuntia joconostle fruit contains many phenolic compounds, flavonoids and betalains. The protective effect of extracts may be related to the phenolic composition and also by a counteraction with other compounds, such as betalains and flavonoids that increase their antioxidant effect.

Genetic Structure of Cartagena de Indias Population Using Hypervariable Markers of Y Chromosome

Ethnicity has been associated with the incidence of diseases and consequently it is a cornerstone in medical genetic studies. It is mainly important in admixture populations, where the population stratification can produce spurious results that lead to erroneous conclusions. Consequently, population stratification has become one of the most important confounding factors in population-based genetic association studies, especially in Latino populations. Cartagena de Indias is a cosmopolitan city with dissimilar ancestry proportions due to recent miscegenation. This population mainly exhibits African and Amerindian matrilineal ancestries. Nevertheless, important asymmetries in the paternal genetic history related to the complex patterns of migration in the colonial period increase the male genetic diversity in this population. As a result of this recent admixture, population stratification has arisen, where each subpopulation is not equally represented. Consequently, the allele differences between cases and controls could be related with different frequencies among different population strata rather than the association of the genes with the disease. In order to define the patrilineal substructure of the Cartagena’s population, a total of 130 unrelated men were ancestrally studied using 15 Y-STR loci routinely employed in anthropological, forensic and population genetics. Our results show that Cartagena is an admixture population consisting of European (80%), Amerindian (10%) and African ancestries (10%), which are represented by haplogroups R1b and I2a (xI2a1), Q-M242/Q-M3, and E1b1a/E1b1b, respectively. Complex genetic patterns found in Cartagena’s population emphasize the importance to know the genetic variation in order to diminish the inconsistence for future genetic association studies. In addition, our findings illustrate the complex genetic background of Cartagena population and reinforce the need to encompass more geographic regions to generate more robust data for anthropological and forensic applications.

Effectiveness of the Experimental Fosfatriclaben in Comparison with Two Commercial Fasciolicides in Cattle

The aim of the present study was to compare the fasciolicidal efficacy in cattle of an experimental water-soluble compound, named fosfatriclaben, a prodrug of triclabendazole, with two commercial fasciolicides. For this, twenty-four cross mixed milking cows, aged between 1 to 3 years, naturally infected with Fasciola hepatica, were used. To apply the treatment, animals were divided into 4 groups of 6 animals each being ranked according to their fecal fluke-egg count from the highest to the lowest number of eggs. The compounds were administered in the groups with a single dose. Group 1 (G1) was treated with 6 mg/kg/IM of fosfatriclaben, G2 was treated with triclabendazole at 12 mg/kg/PO;G3 was treated with 5% closantel at 10 mg/kg/SC and G4 was administered with 5 mL/IM of deionized water and served as untreated control. Fecal samples were analyzed on days—8, 0 (treatment day), 7, 14, 21 and 28 to count the number of fasciola eggs before and after the treatment using the sedimentation test. The efficacy was assessed as the percentage of fluke-egg reduction on treated groups relative to the untreated control. The resulting data were analyzed by the Kruskal-Wallis non-parametric test, using the statistical IBM SPSS 24.0 (2016) program. Results indicated a fluke-egg reduction of 100% for fosfatriclaben along the study;triclabendazole showed an efficacy of 99.7% - 100% from day 7 to day 28. In the case of closantel, values from 98.8% to 99.6% were recorded from day 7 to day 28. No statistical differences between treatments were observed (P < 0.05). It was concluded that the experimental fosfatriclaben administered at 6 mg/kg/IM to naturally infected cattle exerted a fasciolicidal efficacy similar to the drugs of choice for the treatment of fasciolosis (triclabendazole) when administered at 12 mg/kg/ PO, and closantel injected at 10 mg/kg/SC.

Correspondence amongst the PENO Test Battery Cognitive Results and Hippocampal Lesions in Alzheimer’s Disease

Alzheimer’s disease (AD) is characterized by a decline of cognitive functions. Distinctive histopathological hallmarks are neuritic plaques, neurofibrillary tangles, and synaptic alterations. Abnormally enlarged synaptic structures called “Meganeurite clusters” have been linked to plasticity changes. The aims of this study were to determine if cognitive impairment was related to specific neuritic and synaptic degeneration processes in patients with AD, and if the results of a cognitive test could be correlated with the histopathological damage. The neuropsychological evaluation obtained by the Protocole d’evaluation neuropsychologique optimal (PENO) test battery was used in live AD and control individuals. The histopathological evaluation of their brain after their death was carried out with specific polyclonal and monoclonal antibodies to Aβ, pTau protein, synaptophysin, and GAP-43. Images were obtained by confocal microscopy. The results showed a significant difference between healthy controls and Alzheimer’s patients in neuropsychological evaluation and histopathological hallmarks expression. The most significant positive correlation in AD patients was between memory and language results with the PENO test and the presence of Aβ +pTau+ plaques in the hippocampus. An interesting negative correlation was between cognitive impairment and the presence of Meganeuritic clusters, considered as “plasticity” markers. These results strongly supported the use of the PENO battery test to evaluate the progression of cognitive impairment in AD prone individuals and patients due to the strong correlation of the test results with histopathological brain lesions characteristic of Alzheimer’s disease.

Solubility and thermodynamics of lamotrigine in ternary mixtures of ionic liquids([OMIm][Br]+[HMIm][Br]+water)at different temperatures

Experimental mole fraction solubility of lamotrigine(LTG)in ternary aqueous mixtures of two ionic liquids(ILs),1-hexyl and 1-octyl-3-methylimidazolium bromide,[HMIm][Br]and[OMIm][Br]were reported at several temperatures T=(293.15 to 313.15)K.The van’t Hoff and(Jouyban-Acree-van’t Hoff,E-Jouyban-Acree-van’t Hoff,e-NRTL,UNIQUAC and Wilson)models were used to correlate the solubility data.The comparison of the models with temperature and solvent composition dependencies shows that the Wilson model has the minimum ARD which are relatively close to those obtained from Jouyban-Acree-van’t Hoff and E-Jouyban-Acree-van’t Hoff models and maximum ARD belonged to the UNIQUAC model.The order of ARDs for these models is:Wilson b Jouyban-Acree-van’t Hoff,E-Jouyban-Acree-van’t Hoff b e-NRTL b UNIQUAC.Moreover,the apparent thermodynamic functions,Gibbs free energy,enthalpy and entropy of dissolution and mixing were calculated based on the van’t Hoff and Gibbs free energy equations.The strong LTG-ILs interactions and enthalpic contribution of the dissolution process resulted from the calculated thermodynamic functions.

Resveratrol effects on neural connectivity during aging

Aging has been considered a natural process of any living being.The rate of aging depends on many factors,including genetic and environmental factors.For this reason,many researchers in this field suggest that aging is an epigenetic process.Nowadays,the age groups have undergone a change.

Nanoencapsulation of Human Adipose Mesenchymal Stem Cells: Experimental Factors Role to Successfully Preserve Viability and Functionality of Cells

Cell nanoencapsulation is a novel delivery system based on a self-assembly technique mediated by electrostatic interactions called Layer-by-Layer (LbL) deposition, without an increase in volume implant because of the nanometric thickness of its layers. LbL coats the entire surface of individual cells, providing mechanical resistance to cells against manipulation and storage conditions prior to implantation in the patient. In this work, single-cell nanocapsule formation using human adipose-derived mesenchymal stem cells (ADSC) given their potentiality in regenerative medicine was assessed by fluorescence microscopy and Zeta potential assays. Both methodologies were conclusive in showing layer-by-layer nanocapsule formation of every single ADSC. Significant differences in terms of viability and cell functionality preservation were observed depending on the polycation used. Using a combination of fluorescence microscopy and fluorimetric assays, we found that cell survival after nanocapsulation was only efficient when chitosan was added to cells. These results were consistent with other cell types used in this study. Other polycations such as poly(allylamine hydrochloride) (PAH), poly(diallyldimethylammonium chloride) (PDADMAC) and poly-L-lysine (PLL) markedly decreased cell viability (22%, 11% and 15%, respectively). In addition, the use of potassium-enriched saline solutions, such as Hanks and Ringer’s solution, during the nanoencapsulation process on ADSCs was harmful on cell viability compared to standard media (36% vs 79%, respectively). The addition of a mixture of polyanions such as hyaluronic acid and chondroitin sulfate did not affect cell viability (79% and 81%). The combination of chitosan/hyaluronic acid and chondroitin sulfate was also effective in preserving the cell functionality of ADSCs, including the proliferation and differentiation of these cells as assessed by MTT assay and microscopy, respectively. Taken together, these results indicate that ADSCs can be successfully nanoencapsulated using a first layer of chitosan and a second layer of a combination of hyaluronic acid and chondroitin sulfate with a standard potassium concentration in the culture medium.

Non-related contact lens coinfection with Acanthamoeba and Fusarium

Rationale: Microbial keratitis caused by coinfection with more than one species of pathogens is a severe condition with an unfavorable prognosis. Patient concerns: An immunocompetent Nepali woman complained of pain in the left eye, redness, watering and decreased vision for 5 months. Interventions: The patient was discarded and accurately diagnosed with coinfection with Fusarium sp. and Acanthamoeba sp. The habit of washing the eyes with tap water from a domestic storage tank was the most likely source of infection since it was found to be contaminated with cysts of Acanthamoeba sp. The woman received eye drops of fluconazole and natamycin(5%), cefazoline(50 mg/m L), atropine, and tablets of itraconazole(100 mg), which were later switched to eye drops of clotrimazole(1%), natamycin(5%) and voriconazole(1%), and tablets of itraconazole. A full thickness penetrating keratoplasty was performed followed by treatment with eye drops of voriconazole(1%), natamet(5%), ofloxacin, atropine and carboxymethylcellulose for one week.Outcomes: After treatment, the condition of the patient significantly improved and was discharged one week after keratoplasty. Lessons: This is the first report of Acanthamoeba keratitis in Nepal and the first report of coinfection with Fusarium in this country and highlights the importance of early diagnosis of microbial keratitis both in single microorganism infections and coinfections, even in no contact lens wearers.

Morphology and Chemical Phenotype of the Ovarian Intrinsic Neurons in Neonate and Sexually Mature Reproductive Guinea Pig

Introduction: The existence of ovarian intrinsic neurons is well established. However, the morphology and chemical phenotype are not completely characterized and are even unknown for some species used in medical research. The purpose of this work was to determine the morphology and chemical phenotype of intrinsic neurons of the guinea pig ovary at two ages: neonates (0 days old) and sexually mature reproductive animals (90 days old). Materials and Methods: For the morphological analysis, we employed the modified Golgi-Cox impregnation technique. For the chemical phenotype, we used immunohistochemistry and the following antibodies;tyrosine hydroxylase (TH), calcitonin gene-related peptide (CGRP), transient receptor potential type 1 (TRPV1), neuron-specific nuclear protein (NeuN) and proto-oncogene product of the cFos gene (cFos). We also used enzyme histochemistry for NADPH-diaphorase detection. Results: The number of intrinsic neurons in the neonate ovary was low in comparison to the adult guinea pig ovary. The intrinsic neurons were located in the cortex and the ovarian medulla;some were isolated or clustered, forming ganglia, and others were interconnected and formed networks. The neurons were small, medium or large. In the cortex of neonate vs adult ovaries, the small and medium neurons comprised 23% vs 36% and 5.2% vs 11.6%, respectively. In the medulla, the percent of the same neurons was 10.1% vs 10.1% and 1.1% vs 2.2% in the neonate and adult, respectively. In both cortex and medulla < 1% were large neurons at two ages. Also, the neurons were rounded, fusiform or multipolar. In the cortex, they were 12.7% vs 20.9%, 14.9% vs 24.2% and 1.1% vs 3.0%, respectively. In the medulla, the percent of small vs medium neurons was 6% vs 7.1% and 4.1% vs 4.8% in the neonate and adult ovary, respectively, and <1% were large neurons at both ages. The chemical phenotypes were in the neonate and adult: TH/NeuN-positive neurons, 16.3% vs 26.5%;CGRP/NeuN, 13.5% vs 35.8%;TRPV1/NeuN, 10.2% vs 38.6%;and cFos/NeuN, 4.6% vs 5.4%, respectively.The percent of NADPHd-positive cells in the cortex was 9.5% vs 25.1% and 3.2% vs 62.2% in the medulla in the neonate and adult, respectively. Conclusion: Altogether, these data showed that the number of ovarian intrinsic neurons was low at birth and increased in the sexually mature reproductive guinea pig. The chemical phenotype was rich and peptidergic, catecholaminergic and nitrergic in nature and positive for cFos immunoreactivity. Therefore, intrinsic neurons can be chemical sensors inside of the gonad and transmit signal to the central nervous system.

Antibacterial Activity of <i>Bougainvillea Glabra, Eucalyptus Globulus, Gnaphalium Attenuatum</i>, and Propolis Collected in Mexico

Bougainvillea glabra C., Eucalyptus globules Labill., and Gnaphalium attenuatum DC., as well as propolis, have been used in Mexican traditional medicine as a remedy to treat respiratory illnesses. There are few biological reports of such material collected in Mexico, despite the high demand for them as raw material for popular and industrial uses. The antibacterial activity of the plants and propolis studied here were evaluated against a panel of bacteria using three different methodologies: agar disc diffusion, macro and micro dilution methods. E. globules and G. attenuatum extracts showed the strongest active values (P > 0.05) in the agar disc diffusion method with a range of 8 - 22 mm inhibition zone, MIC values ranging from 25 - 250g/mL, and MBC values of 25 - 500g/mL obtained by macro and micro dilution methods. B. glabra extracts were active against E. coli, S. typhi, K. pneumoniae, S. aureus and S. agalactiae, with 8 - 13 mm inhibition zone, MICs ranging from 500 - 3000g/mL, and MBCs of 1000 - 3000g/mL. The propolis extract turned out to be active against E. coli, K. pneumoniae, S. aureus and S. agalactiae, with values of 7 - 12 mm, MICs of 1000 - 2000g/mL, and MBCs of 2000 - 2500g/mL. E. globules and G. attenuatum extracts were the most active in the three methodologies assayed. This is also the first time that the antibacterial activity of G. attenuatum has been experimentally demonstrated. The microdilution method showed to be more sensitive, less expensive and minor time-consuming technique compared with the other two.

Facile Preparation of 1,2-Diols from Chalcones: An NMR Spectroscopy and X-Ray Crystallography Study

Structures of 2-(naphthalen-2-ylmethyl)-2,3-dihydro-1H-indene-1,2-diol (C20H18O2), compound 1 and 1-(3,4-dimethoxyphenyl)-3-methoxy-3-(4-nitrophenyl)propane-1,2-diol chloroform (C18H21NO7·CHCl3) compound 2 were established by spectral and X-ray diffraction studies. Compound 1 crystallizes in the orthorhombic space group P212121 with unit cell parameters a = 5.2177 (6), b = 13.903 (2), c = 21.121 (2) A, Z = 4. Compound 2 crystallizes in the triclinic space group P-1 with unit cell parameters a = 9.238 (1), b = 9.879 (1), c = 12.636 (1) A, α = 102.004 (1), β = 92.356 (1), γ = 90.779 (1)o, Z = 2. These two new molecules arise from a facile preparation of 1,2-diols from chalcones and have been fully characterized. Based on the crystallographic information obtained for compound 1, the relative configuration for the chiral centers is 1S and 2S. In structure 1, both hydroxyl groups adopt an anti-conformation with a torsion angle O1-C1-C2-O2 value of 93.1 (2)o [in molecule 2, both hydroxyl groups adopt a trans-conformation with a torsion angle O1-C1-C2-O2 value of -171.0 (2)。]. In both structures, the molecules in the crystal are linked by intermolecular hydrogen bonds O-H···O and C-H···O interactions and adjacent molecules are interconnected by intermolecular weak C-H···π and C-H···Cl interactions which give additional support to molecular packing stability.