Inability of 7,8 – Dihydroxy-4- Methylcoumarin antioxidant activity, to prolong longevity and to protect against stress in Caenorhabditis Elegans worms

Despite an increase in life expectancy, it is known that this factor is not necessarily accompanied by a better quality of life, which reflects in longevity. Aspects related to metabolic stress to which cells are subjected can modulate this process, which can lead to various pathologies. Coumarins are secondary metabolites found in several plants, such as guaco, and are part of the polyphenol family capable of producing up to 1300 derivatives, with potential effects against metabolic stress, in addition to being used in the cosmetics industry with the objective of improving fragrance of products. Therefore, it seems necessary to seek to elucidate molecular mechanisms that can regulate this aging process, which can be associated with the gradual loss of physiological functions of cells and tissues, increasing the number of cells in senescence that may be related to increased oxidative stress. PURPOSE: the aim of this study was to identify the influence of the use of the coumarin synthetic compound 7,8-Dihydroxy-4-methylcoumarin (DHMC) on longevity and resistance to different types of stress in vivo. METHODS: free radical scavenging (DPPH) analyzes were performed for the compound, longevity, and stress tests (H2O2, NaCl, Heat) for C. elegans worms. RESULTS: in the first analysis, the compound showed 92% of antioxidant activity already in small concentrations (25ug/ml) through DPPH analysis. In the following tests DHMC did not show antibacterial responses against Escherichia coli, and Caenorhabditis elegans worms did not show stress reduction or significant improvement in longevity with the use of the compound. CONCLUSION: therefore, the DHMC compound expresses a high antioxidant activity and presents several study potentials. However, it has no biological effects in protecting against stress or contributing to longevity in C. elegans worm

A single-step multicomponent synthesis of a quinoline derivative and the characterization of its cyclodextrin inclusion complex

Multicomponent synthesis are convergent reactions in which three or more starting materials react in a single step to form the product. In the discovery and development of new drugs, multicomponent reactions offer several advantages over traditional synthesis: shorter experiment time, less need for laboratory techniques and scalability. Thus, the objective of this work was to perform the multicomponent synthesis of a hexahydroquinoline compound whose pharmacological activity has been described previously. The synthesis product was characterized by spectroscopic techniques such as Fourier transform infrared spectrometry and 1H, 13C and HMQC nuclear magnetic resonance (NMR). The mechanism of the reaction was proposed to include a conjugated Michael addition. Subsequently, inclusion complexes (ICs) at 1:1 and 1:2 stoichiometries were prepared with the appropriate cyclodextrin to increase the aqueous solubility and bioavailability of this molecule. Kneading and lyophilization (LYO) methods were used to prepare the inclusion complexes, which were evaluated by phase solubility and 1H NMR spectroscopy, with LYO at a 1:2 stoichiometry having the best results. The ICs were then characterized by differential scanning calorimetry, near-infrared spectroscopy and in vitro dissolution tests, which verified a slower release of the compound with the potential to improve its biological properties.This work was supported by the Research Institute for Medicines (iMed-ULisboa) through FCT/MCTES (UID/DTP/04138/2019), Central de Análise e Prospecção Química (CAPQ), Fundação de Amparo à Pesquisa de Minas Gerais (FAPEMIG), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq).info:eu-repo/semantics/publishedVersio

Achyrocline satureioides (Lam.) DC extracts acting as enzyme modulators: digestion, inflammation, and hemostasis

Achyrocline satureioides is popularly known for its richness in phenolic compounds and medicinal properties (anti-inflammatory, analgesic, and hepatoprotective). The present study aimed at broadening the knowledge about the pharmacological potential exerted by the aqueous and ethanolic extracts of A. satureioides. These extracts were characterized by HPLC and tested for their modulatory action on phospholipases A2 and proteases of snake venoms. In addition, they were tested on the activities of digestive enzymes. Snake venoms were used as tools since they have enzymes with high functional and structural homology to human enzymes. The results demonstrate that the extracts of A. satureioides act as enzymatic inhibitors or potentiators, interfering in processes related to the hemostasis, such as coagulation and thrombus dissolution. In addition, the anti-genotoxic activity and inhibitions exerted on digestive enzymes suggests their potential use in the prevention and/or treatment of several pathologies. New studies could provide information on how the compounds present in the extracts and the different enzymes interact

Synthetic acylsugars and their effects on the control of arthropod pests

ABSTRACT One of the main problems facing agriculture is the loss of production as a result of the attack of agricultural pests. Alternative ways to work around this problem are being sought. There are substances called acylsugars that are naturally produced by the wild tomato species S. pennellii and affect arthropod pests. The objectives of this work were to synthesize two acylsugars and assess the biological effect of these on the arthropod pests Bemissia tabaci and Tetranycus urticae. The syntheses were performed via the reactions of glucose and sucrose (saccharose) with acetic anhydride using sodium acetate as the catalyst. The products of these reactions were sucrose octa-acetate and glucose penta-acetate, the structures of which were confirmed by spectroscopic techniques. In a resistance test against the mite, a linear correlation between the concentration of the synthesized substances, and the dislocation of the mite was obtained. A delay in the hatching of the arthropod eggs was observed, causing a mortality rate of approximately 95% in the 1st instar larvae of mites that was confirmed in adults. In the biological tests with Bemisia tabaci, there was a low rate of hatching and emergence, and the effect on the nymphs was the deformation of the emergent adults

Removal of the synthetic hormone methyltestosterone from aqueous solution using a β-cyclodextrin/silica composite

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Chemical constituents of açai berry pulp (<i>Euterpe oleracea Mart</i>.) by LC-UV-BPSU/NMR and LC-UV-SPE/NMR

The techniques LC-UV-BPSU and LC-UV-SPE/NMR were applied for the first time in the analysis of açai berry (Euterpe oleracea Mart.) pulp extracts. Those techniques allowed the identification of twenty-three metabolites: Valine (1), citric acid (2), tachioside (3), isotachioside (4), α-guaiacylglycerol (5), syringylglycerol (6), uridine (7), adenosine (8), dimethoxy-1,4-benzoquinone (9), koaburaside (10), protocatechuic acid (11), eurycorymboside B (12), 7′,8′-dihydroxy-dihydrodehydroconiferyl alcohol-9-O-β-D-glucopyranoside (13), orientin (14), homoorientin (15), dihydrokaempferol-3-glucoside (16), isolariciresinol-9′-O-β-D-glucopyranoside (17), 5′-methoxyisolariciresinol-9′-O-β-D-glucopyranoside (18), cyanidin-3-O-glucoside (19), cyandin-3-O-rutenoside (20), 9,12-octadecadienoic acid (Z,Z)-2-hydroxy-1-(hydroxymethyl) ethyl ester (21), linolenic acid (22), and 1,2-di-O-α-linolenoyl-3-O-β-D-galactopyranosyl-sn-glycerol (23). In this plant, compounds 3, 4, 5, 6, 8, 10, 12, 17, 18, 21, and 23 are reported for the first time. All the structures were determined through extensive analyses of 1D and 2D NMR data, mass spectrometry, and comparison with published data. This methodology has proven to be an efficient alternative to the analysis of complex extracts containing a large variety of compounds.</p