Natural and artificial pollination of white-fleshed pitaya.

To produce pitaya (Hylocereus spp.), it is essential that pollination occur, either artificially or by pollinating agents. This study evaluated the viability of self-pollination, cross-pollination, and natural pollination, as well as pollen viability, stigma receptivity and ideal pollination window in pitaya flowers (Hylocereus spp.). An experiment was conducted with a randomized block design consisting of four treatments: T1: manual self-pollination; T2: nocturnal open pollination; T3: diurnal open pollination; and T4: manual cross-pollination - red-fleshed pitaya [ Hylocereus polyrhizus] pollen placed on white-fleshed pitaya [ Hylocereus undatus] stigma. The experiment had four replicates, with two plants per replicate (two flowers per plant), totaling 16 flowers per treatment. The analyzed variables were fruit weight, length, diameter, titratable acidity, pH, soluble solids, and SS/TA ratio; the germination percentage of pollen grains; and the receptivity of stigmas. Artificial pollination (self- and cross-pollination) of white-fleshed pitaya (Hylocereus undatus) is viable, resulting in larger fruits than natural pollination, with cross-pollination being the most recommended. Throughout the floral opening period, the pitaya flower (Hylocereus spp.) has receptive stigma capable of receiving pollen. The flowers exhibit the highest pollen germination rate at 7 p.m, which is the ideal pollination window for pitaya.

Synthesis, biological evaluation and molecular modeling studies of novel 1,2,3-triazole-linked menadione-furan derivatives as P2X7 inhibitors.

The P2X7 receptor (P2X7R) is an ion channel that promotes the passage of ions through the membrane through brief stimulation once activated by ATP, its endogenous opener. However, prolonged stimulation with ATP, which occurs in pathological processes, opens a nonselective pore in the plasma membrane, allowing the passage of large molecules and leading to cytokine release or even cell death. In this sense, the search for new inhibitors for this receptor has attracted a great deal of attention in recent years. Considering the booming of biomass upgrading reactions in recent years and the continued efforts to synthesize biologically active molecules containing the 1,2,3-triazole ring, in the present work, we aimed to investigate whether triazole-linked menadione-furan derivatives could present P2X7R inhibitory activity. The novel compounds were tested for their inhibitory activity on ATP-induced dye uptake in peritoneal macrophages. Some have shown promising results, having displayed IC50 values lower than that of the P2X7R inhibitor BBG. Molecular docking studies also indicated that the active compounds bind to an allosteric site on P2X7R, presenting potential P2X7R inhibition.

An Update on the Synthesis and Applications of Bis(Naphthoquinones): An Important Class of Molecules against Infectious Diseases and other Conditions.

Naphthoquinones are important molecules belonging to the general class of quinones, and many of these compounds have become drugs that are in the pharmaceutical market for the treatment of several diseases. A special subclass of compounds is that of the bis(naphthoquinones), which have two linked naphthoquinone units. In the last few years, several synthetic approaches toward such valuable compounds have been described, as well as their evaluation against numerous important biological targets. In this review, we provide a thorough discussion on the various synthetic methods reported for the synthesis of bis(naphthoquinone) analogues, also highlighting the biological activities of these substances.

Bioactive 1,2,3-Triazoles: An Account on their Synthesis, Structural Diversity and Biological Applications.

The triazole heterocycle is a privileged scaffold in medicinal chemistry, since its structure is present in a large number of biologically active molecules, including several drugs currently in the market. Due to their vast applications, a wide variety of methods are described for their preparation, such as the 1,3-dipolar cycloaddition and processes involving diazo compounds and diazo transfer reactions. Considering the significant number of contributions from our research group to this chemistry in recent decades, in this account we discuss both the development of new methods for the synthesis of 1,2,3-triazoles and the preparation of new triazole-functionalized biologically active molecules using classical approaches.

Quinone-Based Drugs: An Important Class of Molecules in Medicinal Chemistry.

BACKGROUND: Several quinones are on the pharmaceutical market as drugs for the treatment of several diseases. OBJECTIVE: The aim of this review was to provide an overview of the quinones that have become drugs for several therapeutic applications. METHODS: We have comprehensively and critically discussed all the information available in the literature about quinone-based drugs. RESULTS: In this review, the various aspects of the chemistry and biochemistry of these drugs are highlighted, including their repositioning, drug combination and their new uses. CONCLUSION: A number of studies related to quinone drugs for different pharmaceutical uses show that the interest in new applications is still increasing in recent years.

Drug repurposing for the treatment of COVID-19: Pharmacological aspects and synthetic approaches.

In December 2019, a new variant of SARS-CoV emerged, the so-called acute severe respiratory syndrome coronavirus 2 (SARS-CoV-2). This virus causes the new coronavirus disease (COVID-19) and has been plaguing the world owing to its unprecedented spread efficiency, which has resulted in a huge death toll. In this sense, the repositioning of approved drugs is the fastest way to an effective response to a pandemic outbreak of this scale. Considering these facts, in this review we provide a comprehensive and critical discussion on the chemical aspects surrounding the drugs currently being studied as candidates for COVID-19 therapy. We intend to provide the general chemical community with an overview on the synthetic/biosynthetic pathways related to such molecules, as well as their mechanisms of action against the evaluated viruses and some insights on the pharmacological interactions involved in each case. Overall, the review aims to present the chemical aspects of the main bioactive molecules being considered to be repositioned for effective treatment of COVID-19 in all phases, from the mildest to the most severe.

Recent Synthetic Approaches towards Small Molecule Reactivators of p53.

The tumor suppressor protein p53 is often called "the genome guardian" and controls the cell cycle and the integrity of DNA, as well as other important cellular functions. Its main function is to trigger the process of apoptosis in tumor cells, and approximately 50% of all cancers are related to the inactivation of the p53 protein through mutations in the TP53 gene. Due to the association of mutant p53 with cancer therapy resistance, different forms of restoration of p53 have been subject of intense research in recent years. In this sense, this review focus on the main currently adopted approaches for activation and reactivation of p53 tumor suppressor function, focusing on the synthetic approaches that are involved in the development and preparation of such small molecules.

Graphitic Carbon Nitride-Based Materials as Catalysts for the Upgrading of Lignocellulosic Biomass-Derived Molecules.

The use of graphitic carbon nitride (g-C3N4)-based catalysts in the upgrading of lignocellulosic biomass significantly contributes to the greener production of biofuels, polymer precursors, and building blocks. In recent years, several catalysts based on g-C3N4 have been developed and applied in both photocatalyzed and non-photocatalyzed (thermal) reactions. This Review provides an overview on the upgrading of lignocellulosic biomass deploying several compositions of g-C3N4-based catalysts.

Angelica Lactones: From Biomass-Derived Platform Chemicals to Value-Added Products.

The upgrading of biomass-derived compounds has arisen in recent years as a very promising research field in both academia and industry. In this sense, a lot of new processes and products have been developed, often involving levulinic acid as a starting material or intermediate. In the last few years, though, other scaffolds have been receiving growing attention, especially, angelica lactones. Considering these facts and the emergent applications of said molecules, in this review we will discuss their preparation and applications; the use of these frameworks as starting materials in organic synthesis to produce potential bioactive compounds will be covered, as will their use as a foundation to highly regarded compounds such as liquid alkanes with prospective use as fuels and polymers.

Temporospatial and kinetic gait variables of Doberman Pinschers with and without cervical spondylomyelopathy.

OBJECTIVE: To characterize and compare gait variables in Doberman Pinschers with and without cervical spondylomyelopathy (CSM). ANIMALS: 18 Doberman Pinschers (9 clinically normal dogs and 9 CSM-affected dogs). PROCEDURES: A neurologic examination was performed on all dogs. The diagnosis of CSM was confirmed with MRI. Temporospatial and kinetic gait variables were measured by use of a pressure-sensitive walkway. Temporospatial variables evaluated included stance phase duration, swing phase duration, gait cycle duration, stride length, and gait velocity. Kinetic variables evaluated included peak vertical force and vertical impulse. Random-effects linear regression was used to determine the difference between CSM-affected and clinically normal dogs for each of the 7 variables. RESULTS: Values for temporospatial variables were significantly smaller in the thoracic limbs of CSM-affected dogs, compared with values for the thoracic limbs of clinically normal dogs. For the kinetic variables, peak vertical force was significantly higher in the thoracic limbs than the pelvic limbs for all dogs. Vertical impulse values were higher in the thoracic limbs than the pelvic limbs. There were significant differences in mean vertical impulse between the thoracic and pelvic limbs for both groups. CONCLUSIONS AND CLINICAL RELEVANCE: In this study, significant differences in temporospatial variables were identified between the thoracic limbs of clinically normal and CSM-affected dogs, with the values being smaller for the CSM-affected dogs than for the clinically normal dogs. A pressure-sensitive walkway may provide a valid, practical option for rapid, objective assessment of gait and response to treatment in dogs with CSM.

Correction: Emerging approaches for the synthesis of triazoles: beyond metal-catalyzed and strain-promoted azide-alkyne cycloaddition.

Correction for 'Emerging approaches for the synthesis of triazoles: beyond metal-catalyzed and strain-promoted azide-alkyne cycloaddition' by Carolina G. S. Lima et al., Chem. Commun., 2015, 51, 10784-10796.

Emerging approaches for the synthesis of triazoles: beyond metal-catalyzed and strain-promoted azide-alkyne cycloaddition.

Metal-free 1,3-dipolar cycloaddition reactions have proven to be a powerful tool for the assembly of key heterocycles, in particular diversely functionalized 1,2,3-triazoles. A number of metal-free (3+2)-cycloaddition approaches have been developed up to date with the aim to circumvent the use of metal catalysts allowing these reactions to take place in biological systems without perturbation of the naturally occurring processes. This feature article specifically provides an overview of emerging metal-free synthetic routes, and their mechanistic features, in the formation of functionalized 1,2,3-triazoles.

Standardization of histological procedures for the detection of toxic substances by immunohistochemistry in Dipteran larvae of forensic importance.

Immunohistochemistry (IHC) technique is an alternative toxicological analysis to detect drugs in insects of forensic importance, but it requires thorough histological procedures. In this study, we tested different fixatives--phosphate-buffered paraformaldehyde 4% (PP), Carnoy's fluid (CF), Kahle's solution (KS), ethanol in different concentrations, and ethanol associated to PP and CF, time of fixation and histological processes for dipteran larvae's tissue, aiming to develop a sample preparation protocol for IHC application. A suitable fixation was achieved using PP for 12 and 24 h, CF for 3 h, 70% ethanol for 19 days, and 70% ethanol/CF for 2 h/3 h. Postfixation using negative pressure, two immersions in xylene for 30 min each, and one in xylene plus paraffin for 45 min increased tissue preservation. An immunohistochemical test for cocaine detection was performed using monoclonal benzoylecgonine antibody from mouse, peroxidase-conjugated anti-mouse IgG and visualized by 3,3'-diaminobenzidine method showed these histological procedures didn't compromise antigenicity.