858 registros encontrados - unidade Faculdade de Ciências Farmacêuticas
ARTIGO - Inglês
Assunto: Simetria
Abstract: Nature often produces compounds with a high degree of symmetry to reduce structural information and complexity. Synthesis of identical twin...
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Abstract: Nature often produces compounds with a high degree of symmetry to reduce structural information and complexity. Synthesis of identical twin drugs, through the linkage of two identical pharmacophoric entities, is a classical strategy to produce more potent and/or selective drugs. Herein, two units of the privileged core of the coumarin hymecromone were linked together using "click chemistry". Synthesis of 1-[2-(4-Methyl-7-coumarinyloxy)ethyl]-4-(5-{1-[2-(4-methyl-7-coumarinyloxy)ethyl]-1H-1,2,3-triazol-4-yl}pentyl)-1H-1,2,3-triazole was achieved by coupling of two identical units of an azido coumarin with a symmetrical alkine using copper(I)-catalyzed alkyne-azide cycloaddition reaction, in good yields and with complete regioselectivity
DOI: https://doi.org/10.3390/M894
Texto completo: https://www.mdpi.com/1422-8599/2016/2/M894
ARTIGO - Inglês
Assunto: Atividade antiproliferativa
Glioblastoma multiforme (GBM) is an aggressive cancer with very limited clinical therapies. Herein, we have designed novel mercaptobenzimidazole...
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Glioblastoma multiforme (GBM) is an aggressive cancer with very limited clinical therapies. Herein, we have designed novel mercaptobenzimidazole derivatives (1–7) as multitarget antineoplastic drugs and assessed their antiproliferative profiles on an experimental model for GBM, the C6 glioma line. The target compounds were synthesized in few steps with reasonable yields (33–90%). Compounds 1 (∼18 μM) and 4 (∼20 μM) showed dose-dependent antiproliferative effects on C6 glioma and significantly increased early apoptosis, but only 4 disrupted the cell cycle progression and did not induce autophagy. Docking simulations suggested these compounds as dual kinase and colchicine binding site inhibitors. In spite of the limited selective toxicity, 4 hold the potential to be further optimized for the treatment of GBM
ARTIGO - Inglês
Assunto: Anticâncer
A biologically relevant natural pigment, 1,6-dihydroxy-3-methyl-9,10-anthraquinone 1, widely produced by fungus from Phoma genus, has been isolated...
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A biologically relevant natural pigment, 1,6-dihydroxy-3-methyl-9,10-anthraquinone 1, widely produced by fungus from Phoma genus, has been isolated from Cassia sophera Linn. (Caesalpiniaceae) roots and subjected to detailed spectral studies, including ID-and 2D-NMR. The compound 1 inhibits the proliferation of several cancer cell lines at different extents, showing minor effects on the growth of non-tumorogenic keratinocyte cells
Texto completo: http://nopr.niscair.res.in/handle/123456789/43272
2021 : ano internacional para a eliminação do trabalho infantil
EDITORIAL - Multilíngua
Assunto: Menores - Emprego
ARTIGO - Inglês
Assunto: Artigo original
Abstract: 6-Nitrodopamine (6-ND) is a novel endogenous catecholamine that is released from the rat isolated vas deferens, and has been characterized...
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Abstract: 6-Nitrodopamine (6-ND) is a novel endogenous catecholamine that is released from the rat isolated vas deferens, and has been characterized as a major modulator of the contractility of rat isolated epididymal vas deferens (RIEVD). Drugs such as tricyclic antidepressants, a1 and ß1ß2 adrenoceptor blockers, act as selective antagonists of the 6-ND receptor in the RIEVD. In the rat isolated atria, 6-ND has a potent positive chronotropic action and causes remarkable potentiation of the positive chronotropic effects induced by dopamine, noradrenaline, and adrenaline. Here, whether 6-ND interacts with the classical catecholamines in the rat isolated vas deferens was investigated. Incubation with 6-ND (0.1 and 1 nM; 30min) caused no contractions in the RIEVD but provoked significant leftward shifts in the concentration-response curves to noradrenaline, adrenaline, and dopamine. Pre-incubation of the RIEVD with 6-ND (1 nM), potentiated the contractions induced by electric-field stimulation (EFS), whereas pre-incubation with 1 nM of dopamine, noradrenaline or adrenaline, did not affect EFS-induced contractions. In tetrodotoxin (1 µM) pre-treated (30 min) RIEVD, pre-incubation with 6-ND (0.1 nM) did not cause leftward shifts in the concentration-dependent contractions induced by noradrenaline, adrenaline, or dopamine. Pre-incubation of the RIEVD with the a2A-adrenoceptor antagonist idazoxan (30 min, 10 nM) did not affect dopamine, noradrenaline, adrenaline, and EFS-induced contractions. However, when idazoxan (10 nM) and 6-ND (0.1 nM) were simultaneously pre-incubated (30 min), a significant potentiation of the EFS-induced contractions of the RIEVD was observed. 6-nitrodopamine causes remarkable potentiation of dopamine, noradrenaline, and adrenaline contractions on the RIEVD, due to activation of adrenergic terminals, possibly via pre-synaptic adrenoceptors
PRE-PRINT - Inglês
Assunto: Atropina
Abstract: 6-Nitrodopamine (6-ND) is a novel endogenous catecholamine that is released from the rat isolated vas deferens, and has been characterized...
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Abstract: 6-Nitrodopamine (6-ND) is a novel endogenous catecholamine that is released from the rat isolated vas deferens, and has been characterized as a major modulator of the contractility of rat isolated epididymal vas deferens (RIEVD). Drugs such as tricyclic antidepressants, a1 and ß1ß2 adrenoceptor blockers, act as selective antagonists of the 6-ND receptor in the RIEVD. In the rat isolated atria, 6-ND has a potent positive chronotropic action and causes remarkable potentiation of the positive chronotropic effects induced by dopamine, noradrenaline, and adrenaline. Here, whether 6-ND interacts with the classical catecholamines in the rat isolated vas deferens was investigated. Incubation with 6-ND (0.1 and 1 nM; 30min) caused no contractions in the RIEVD but provoked significant leftward shifts in the concentration-response curves to noradrenaline, adrenaline, and dopamine. Pre-incubation of the RIEVD with 6-ND (1 nM), potentiated the contractions induced by electric-field stimulation (EFS), whereas pre-incubation with 1 nM of dopamine, noradrenaline or adrenaline, did not affect EFS-induced contractions. In tetrodotoxin (1 µM) pre-treated (30 min) RIEVD, pre-incubation with 6-ND (0.1 nM) did not cause leftward shifts in the concentration-dependent contractions induced by noradrenaline, adrenaline, or dopamine. Pre-incubation of the RIEVD with the a2A-adrenoceptor antagonist idazoxan (30 min, 10 nM) did not affect dopamine, noradrenaline, adrenaline, and EFS-induced contractions. However, when idazoxan (10 nM) and 6-ND (0.1 nM) were simultaneously pre-incubated (30 min), a significant potentiation of the EFS-induced contractions of the RIEVD was observed. 6-nitrodopamine causes remarkable potentiation of dopamine, noradrenaline, and adrenaline contractions on the RIEVD, due to activation of adrenergic terminals, possibly via pre-synaptic adrenoceptors
7,7-Dimethylaporphine and other alkaloids from the bark of guatteria friesiana
ARTIGO - Inglês
Assunto: Alcaloides
Phytochemical investigation of the bark of Guatteria friesiana afforded 12 new aporphines (1–12), along with nine known alkaloids (13–21). The...
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Phytochemical investigation of the bark of Guatteria friesiana afforded 12 new aporphines (1–12), along with nine known alkaloids (13–21). The structures of the new alkaloids were determined on the basis of spectroscopic data interpretation. The cytotoxic activity of the isolated compounds against a small panel of tumor cell lines was assessed using the Alamar blue assay
A comparison between characterization and biological properties of brazilian fresh and aged propolis
ARTIGO - Inglês
Assunto: Própolis
As propolis is a highly valued bee product, we aimed to verify the quality of aged propolis, investigating their phenolic and flavonoid composition,...
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As propolis is a highly valued bee product, we aimed to verify the quality of aged propolis, investigating their phenolic and flavonoid composition, levels of toxic metals, radical scavenging and antimicrobial activities. Material and Methods. Samples of
DOI: https://doi.org/10.1155/2014/257617
Texto completo: https://www.hindawi.com/journals/bmri/2014/257617
ARTIGO - Inglês
Assunto: Melipona
The geopropolis is a unique type of propolis produced by some stingless bee species. This product is known in folk medicine for its pharmacological...
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The geopropolis is a unique type of propolis produced by some stingless bee species. This product is known in folk medicine for its pharmacological properties, mainly antimicrobial and antioxidant, but there are few scientific studies that prove these properties. The objective of this study was to evaluate the phenolic composition and the antimicrobial, antioxidant and antiproliferative activities of Melipona quadrifasciata geopropolis. The phenolic characterization of the geopropolis ethanolic extract was evaluated by LC-ESI-QTOF-MS. The antimicrobial activity was carried out against Gram-positive (including multiresistant microorganisms), negative and yeast. The synergistic effect was evaluated in association with Sulfamethoxazole + Trimethoprim. DPPH, ABTS, FRAP, ORAC and HPLC on-line were used to evaluate the antioxidant activity. Antiproliferative activity was assessed by the sulforhodamine B assay. Flavonoids and phenolic acids were identified in the extract, which showed promising antimicrobial activity, partially synergistic effect and antioxidant activity
A critical overview about cosmetic labeling claims
ARTIGO - Inglês
Assunto: Controle social formal
Abstract: In several countries, still there is no standardized regulation on the use of claims. However, there are some guideline materials and...
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Abstract: In several countries, still there is no standardized regulation on the use of claims. However, there are some guideline materials and content that are used by regulatory agencies. Objective: The goal of this manuscript is to provide an approach to the understanding of the thematic of cosmetic claims to dermatologists and general practice physicians. The objective is to discuss the definition, regulatory framework and tips to help them on how to use this knowledge to guarantee an assertive indication. Results: Knowing the appropriate tests for the substantiation of claims allows the physician to indicate the most appropriate dermocosmetic for the skin condition of each patient. Conclusion: For a more critical and assertive indication or suggestion, it is recommended that the physician observe the product packaging and know how to understand and interpret the terms on the product label
DOI: https://doi.org/10.2174/0126667797256475231004105550
Texto completo: https://www.eurekaselect.com/article/135414
Dados de pesquisa: https://doi.org/10.25824/redu/5AFMTP
ARTIGO - Multilíngua
Assunto: Revisão sistemática
ARTIGO - Inglês
Assunto: Novas substâncias psicoativas
Abstract: New psychoactive substances (NPS) are a broad category of drugs that pose public health risks and have poorly characterized pharmacological...
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Abstract: New psychoactive substances (NPS) are a broad category of drugs that pose public health risks and have poorly characterized pharmacological properties. Further studies are critical for risk assessment, toxicological profiling, and intoxication management. Human evaluations are limited by ethical and safety constraints, making animal models essential. Among in vivo models, zebrafish (Danio rerio) deserves emphasis in the study of NPS due to neurobehavioral, metabolic, and toxicological alterations. Considering some advantages, such as high genetic and neurochemical homology to humans, small body size, external fertilization, and embryo-larval transparency, zebrafish is well-suited for high-throughput screening of NPS. Their central nervous system shares key neurotransmitter pathways with mammals, supporting neurobehavioral assays. Also, a conserved cytochrome P450 system allows metabolism studies. Zebrafish have been successfully used to investigate NPS effects, with embryo-larval models offering practical advantages for acute toxicity and high-throughput behavioral screening. Adults, in turn, are more appropriate for complex behaviors and long-term or chronic exposure protocols. This review synthesizes for the first time behavior, toxicology, and metabolism data from zebrafish studies with a range of NPS classes within a unifying framework, to deliver a comprehensive understanding of their in vivo activity. By focusing on the translational value of zebrafish research, this review bridges experimental toxicology and clinical and forensic applications, thus filling a significant gap in current knowledge and demonstrating how zebrafish models can uniquely accelerate NPS toxicity profiling by providing mechanistic and behavioral information with high translational value
ARTIGO - Inglês
Assunto: Artigo original
Abstract: Liquid-phase microextraction (LPME) is a simple, low-cost, and eco-friendly technique that enables the detection of trace concentrations of...
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Abstract: Liquid-phase microextraction (LPME) is a simple, low-cost, and eco-friendly technique that enables the detection of trace concentrations of organic contaminants in water samples. In this work, a novel customized microextraction device was developed for the LPME extraction and preconcentration of nine illicit drugs in surface water and influent and effluent wastewater samples, followed by analysis by GC-MS without derivatization. The customized device was semi-automated by coupling it with a peristaltic pump to perform the collection of the upper layer of the organic phase. The extraction parameters affecting the LPME efficiency were optimized. The optimized conditions were: 100 µL of a toluene/DCM/EtAc mixture as extractor solvent; 30 min of extraction time under vortex agitation (500 rpm) and a solution pH of 11.6. The limits of detection and quantification ranged from 10.5 ng L-1 (ethylone) to 22.0 ng L-1 (methylone), and from 34.9 ng L-1 to 73.3 ng L-1 for these same compounds, respectively. The enrichment factors ranged from 39.7 (MDMA) to 117 (cocaethylene) and the relative recoveries ranged from 80.4 % (N-ethylpentylone) to 120 % (cocaine and cocaine-d3). The method was applied to real surface water, effluent, and influent wastewater samples collected in Salvador City, Bahia, Brazil. Cocaine was the main drug detected and quantified in wastewater samples, and its concentration ranged from 312 ng L-1 to 1,847 ng L-1. Finally, the AGREE metrics were applied to verify the greenness of the proposed method, and an overall score of 0.56 was achieved, which was considered environmentally friendly
A highly active triterpene derivative capable of biofilm damage to control cryptococcus spp.
ARTIGO - Inglês
Assunto: Triterpenos
Cryptococcus neoformans is an encapsulated yeast responsible for more than 180,000 deaths per year. The standard therapeutic approach against...
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Cryptococcus neoformans is an encapsulated yeast responsible for more than 180,000 deaths per year. The standard therapeutic approach against cryptococcosis is a combination of amphotericin B with flucytosine. In countries where cryptococcosis is most prevalent, 5-fluorocytosine is rarely available, and amphotericin B requires intravenous administration. C. neoformans biofilm formation is related to increased drug resistance, which is an important outcome for hospitalized patients. Here, we describe new molecules with anti-cryptococcal activity. A collection of 66 semisynthetic derivatives of ursolic acid and betulinic acid was tested against mature biofilms of C. neoformans at 25 mu M. Out of these, eight derivatives including terpenes, benzazoles, flavonoids, and quinolines were able to cause damage and eradicate mature biofilms. Four terpene compounds demonstrated significative growth inhibition of C. neoformans. Our study identified a pentacyclic triterpenoid derived from betulinic acid (LAFIS13) as a potential drug for anti-cryptococcal treatment. This compound appears to be highly active with low toxicity at minimal inhibitory concentration and capable of biofilm eradication
DOI: https://doi.org/10.3390/biom9120831
Texto completo: https://www.mdpi.com/2218-273X/9/12/831
ARTIGO - Inglês
Assunto: Zika virus
Recent outbreaks of Zika virus in Oceania and Latin America, accompanied by unexpected clinical complications, made this infection a global public...
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Recent outbreaks of Zika virus in Oceania and Latin America, accompanied by unexpected clinical complications, made this infection a global public health concern. This virus has tropism to neural tissue, leading to microcephaly in newborns in a significant proportion of infected mothers. The clinical relevance of this infection, the difficulty to perform accurate diagnosis and the small amount of data in literature indicate the necessity of studies on Zika infection in order to characterize new biomarkers of this infection and to establish new targets for viral control in vertebrates and invertebrate vectors. Thus, this study aims at establishing a lipidomics profile of infected mosquito cells compared to a control group to define potential targets for viral control in mosquitoes. Thirteen lipids were elected as specific markers for Zika virus infection (Brazilian strain), which were identified as putatively linked to the intracellular mechanism of viral replication and/or cell recognition. Our findings bring biochemical information that may translate into useful targets for breaking the transmission cycle
ARTIGO - Inglês
Assunto: Zika virus
Abstract: Recent Zika outbreaks in South America, accompanied by unexpectedly severe clinical complications have brought much interest in fast and...
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Abstract: Recent Zika outbreaks in South America, accompanied by unexpectedly severe clinical complications have brought much interest in fast and reliable screening methods for ZIKV (Zika virus) identification. Reverse-transcriptase polymerase chain reaction (RT-PCR) is currently the method of choice to detect ZIKV in biological samples. This approach, nonetheless, demands a considerable amount of time and resources such as kits and reagents that, in endemic areas, may result in a substantial financial burden over affected individuals and health services veering away from RT-PCR analysis. This study presents a powerful combination of high-resolution mass spectrometry and a machine-learning prediction model for data analysis to assess the existence of ZIKV infection across a series of patients that bear similar symptomatic conditions, but not necessarily are infected with the disease. By using mass spectrometric data that are inputted with the developed decision-making algorithm, we were able to provide a set of features that work as a "fingerprint" for this specific pathophysiological condition, even after the acute phase of infection. Since both mass spectrometry and machine learning approaches are well-established and have largely utilized tools within their respective fields, this combination of methods emerges as a distinct alternative for clinical applications, providing a diagnostic screening—faster and more accurate—with improved cost-effectiveness when compared to existing technologies
ARTIGO - Inglês
Assunto: Liofilização
A great number of patients have difficulty swallowing or needle fear. Therefore, buccal and orodispersible dosage forms (ODFs) represent an important...
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A great number of patients have difficulty swallowing or needle fear. Therefore, buccal and orodispersible dosage forms (ODFs) represent an important strategy to enhance patient compliance. Besides not requiring water intake, swallowing or needles, these dosage forms allow drug release modulation. ODFs include oral lyophilizates or wafers, which present even faster disintegration than its compressed counterparts. Lyophilization can also produce buccal wafers that adhere to mucosa for sustained drug release. Due to the subject relevance and recent research growth, this review focused on oral lyophilizate production technology, formulation features, and therapy gains. It includes Critical Quality Attributes (CQA) and Critical Process Parameters (CPP) and discusses commercial and experimental examples. In sum, the available commercial products promote immediate drug release mainly based on biopolymeric matrixes and two production technologies. Therapy gains include substitution of traditional treatments depending on parenteral administration and patient preference over classical therapies. Experimental wafers show promising advantages as controlled release and drug enhanced stability. All compiled findings encourage the development of new wafers for several diseases and drug molecules
A Model system to study the lignification process in Eucalyptus globulus
ARTIGO - Inglês
Assunto: Lignina
Recalcitrance of plant biomass is closely related to the presence of the phenolic heteropolymer lignin in secondary cell walls, which has a negative...
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Resumo
Recalcitrance of plant biomass is closely related to the presence of the phenolic heteropolymer lignin in secondary cell walls, which has a negative effect on forage digestibility, biomass‐to‐biofuels conversion and chemical pulping. The genus Eucalyptus
PRE-PRINT - Inglês
Assunto: Produtos biológicos
Abstract: Synthetic cannabinoids are still a growing trend among drug users and consist of a group of hundreds of highly potent compounds. To...
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Abstract: Synthetic cannabinoids are still a growing trend among drug users and consist of a group of hundreds of highly potent compounds. To investigate the use of such substances, sample preparation of biological matrices is a crucial step prior to instrumental analysis. Although different efficient extraction techniques have been proposed for that aim, they usually do not fit eco-friendly guidelines that have been gaining popularity in recent years, such as Green Analytical Toxicology. This work uses describes for the first time the use of switchable hydrophilicity solvent-based homogenous liquid-liquid microextraction (SHS-HLLME) for synthetic cannabinoids. This is a green technique that replaces highly toxic organic reagents for switchable hydrophilicity solvents (SHS), substances that can be either water-miscible or immiscible depending on their protonation. Thus, by simply adjusting the pH of the system, these SHS can be used as extraction solvents. A full optimization study including type of SHS, volume of protonated SHS, volume of NaOH, salting-out effect, and extraction time was perfomed. The optimized procedure consisted of precipitating the proteins of 300 ?L of plasma with 300 ?L of acetonitrile followed by centrifugation; evaporation of the organic solvent under N2 stream; addition of 500 ?L of the protonated DPA, DPA-HCl (6 M) (1:1, v/v); addition of 500 ?L of NaOH (10 M); and finally centrifugation and evaporation. Validation results showed determination coefficients ? 0.99 for the 0.1-10 ng/mL linear range; 0.01-0.08 ng/mL as limit of detection; 0.1 ng/mL as limit of quantitation; accuracy and imprecision were within acceptable ranges; matrix effect, recovery, and process efficiency ranged from -55.6% to 185.9%, 36% to 56.7%, and 18.5% to 148.4%, respectively. The SHS-HLLME herein described was fully optimized providing satisfactory recoveries of 31 synthetic cannabinoids at low concentrations requiring only 300 ?L of plasma. In addition, the validation results showed that the technique is a reliable eco-friendly alternative for clinical and toxicological analysis
ARTIGO - Inglês
Assunto: Produtos biológicos
Abstract: Synthetic cannabinoids are still a growing trend among drug users and consist of a group of hundreds of highly potent compounds. To...
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Resumo
Abstract: Synthetic cannabinoids are still a growing trend among drug users and consist of a group of hundreds of highly potent compounds. To investigate the use of such substances, sample preparation of biological matrices is a crucial step prior to instrumental analysis. Although different efficient extraction techniques have been proposed for that aim, they usually do not fit eco-friendly guidelines that have been gaining popularity in recent years, such as Green Analytical Toxicology. This work uses describes for the first time the use of switchable hydrophilicity solvent-based homogenous liquid-liquid microextraction (SHS-HLLME) for synthetic cannabinoids. This is a green technique that replaces highly toxic organic reagents for switchable hydrophilicity solvents (SHS), substances that can be either water-miscible or immiscible depending on their protonation. Thus, by simply adjusting the pH of the system, these SHS can be used as extraction solvents. A full optimization study including type of SHS, volume of protonated SHS, volume of NaOH, salting-out effect, and extraction time was perfomed. The optimized procedure consisted of precipitating the proteins of 300 ?L of plasma with 300 ?L of acetonitrile followed by centrifugation; evaporation of the organic solvent under N2 stream; addition of 500 ?L of the protonated DPA, DPA-HCl (6 M) (1:1, v/v); addition of 500 ?L of NaOH (10 M); and finally centrifugation and evaporation. Validation results showed determination coefficients ? 0.99 for the 0.1-10 ng/mL linear range; 0.01-0.08 ng/mL as limit of detection; 0.1 ng/mL as limit of quantitation; accuracy and imprecision were within acceptable ranges; matrix effect, recovery, and process efficiency ranged from -55.6% to 185.9%, 36% to 56.7%, and 18.5% to 148.4%, respectively. The SHS-HLLME herein described was fully optimized providing satisfactory recoveries of 31 synthetic cannabinoids at low concentrations requiring only 300 ?L of plasma. In addition, the validation results showed that the technique is a reliable eco-friendly alternative for clinical and toxicological analysis
ARTIGO - Inglês
Assunto: Ibuprofeno
This work describes the synthesis, characterization and antibacterial activities of a palladium(II) complex with ibuprofen (ibu). Elemental and mass...
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This work describes the synthesis, characterization and antibacterial activities of a palladium(II) complex with ibuprofen (ibu). Elemental and mass spectrometric data (ESI-QTOF-MS) suggest a 1:2 metal/ligand composition with the minimal formula PdC26H34O4. Infrared (IR) and nuclear magnetic resonance (NMR) spectroscopic measurements indicate ligand coordination to palladium(II) by the carboxylate group in a bidentate mode. Thermal analysis shows that decomposition of the Pd-ibu complex starts at 130 degrees C and occurs in three exothermic stages. The steps are consistent with the loss of two ibuprofen molecules, with the formation of the final residue of the thermal treatment at 850 degrees C. DFT calculations (LANL2DZ basis set), supported by the spectroscopic data, led to an optimized dimeric structure for the complex, where two palladium(II) centers are interconnected by four carboxylates in a cage-like structure. The palladium(II) complex with ibuprofen (Pd-ibu) is soluble in dimethylsulfoxide (DMSO) and hexane and is slightly soluble in ethanol and acetonitrile. The complex exhibited antibacterial activities against Grampositive (Staphylococcus aureus and Enterococcus faecalis) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacterial strains, which is noteworthy in the search of new antibacterial agents. Strong interactions were evidenced with biomolecules such as deoxyribonucleic acid (DNA) and bovine serum albumin (BSA) using agarose gel electrophoresis and fluorescence assays, respectively, which suggests that such molecules are possible targets for the complex in biological medium
ARTIGO - Inglês
Assunto: Saliva
Abstract: Synthetic Cannabinoid Receptor Agonists (SCRAs) are a class of Novel Psychoactive Substances (NPS) that interact with the same receptors...
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Abstract: Synthetic Cannabinoid Receptor Agonists (SCRAs) are a class of Novel Psychoactive Substances (NPS) that interact with the same receptors (CB1 and CB2) as delta-9-tetrahydrocannabinol (THC). The identification of SCRAs, such as AB-CHMINACA and MDMB-4en-PINACA, is of significant forensic and toxicological interest due to their widespread consumption in several countries and their potential involvement in overdose cases resulting from their high potency, posing a serious public health and safety concern. Currently, no standardized screening methods exist for the detection of SCRAs in forensic and toxicological contexts. This study introduces a novel electroanalytical method that combines laboratory-fabricated boron-doped diamond screen-printed electrodes (SP/BDDE) with square-wave adsorptive stripping voltammetry (SWAdSV) for the detection of AB-CHMINACA and MDMB-4en-PINACA in e-cigarette samples and real biological matrices. For the first time, the electrochemical behavior of these SCRAs is comprehensively investigated, and all their redox processes (Pc1/Pa2 and Pa3) are utilized for selective and accurate identification. The proposed method exhibited a wide linear range (20–100 µM for AB-CHMINACA and 20–70 µM for MDMB-4en-PINACA) with a low detection limit of 0.282 µM, making it highly suitable for forensic applications involving seized samples and toxicological analyses of biological specimens. The stability of the electrochemical response was assessed, with SP/BDDE showing relative standard deviations (RSD) below 10 % for Ep and Ip. Interference studies confirmed the high selectivity of the method for SCRA detection. AB-CHMINACA and MDMB-4en-PINACA were successfully identified in e-cigarette and biological samples, with recovery rates approaching 100 %, indicating minimal matrix effects in these complex samples. Therefore, the proposed method proves to be a promising, rapid, and selective screening approach for the detection of SCRAs in forensic and toxicological scenarios, as a screening test
ARTIGO - Inglês
A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
ARTIGO - Inglês
Assunto: Tetracaína
Abstract: Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in...
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Abstract: Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers (NLC) may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loading 4% TTC. Structural properties and encapsulation efficiency (%EE > 63%) guided the selection of three pre-formulations of different lipid composition, through a 23 factorial design of experiments (DOE). DLS and TEM analyses revealed average sizes (193–220 nm), polydispersity (< 0.2), zeta potential |- 21.8 to - 30.1 mV| and spherical shape of the nanoparticles, while FTIR-ATR, NTA, DSC, XRD and SANS provided details on their structure and physicochemical stability over time. Interestingly, one optimized pre-formulation (CP-TRANS/TTC) showed phase-separation after 4 months, as predicted by Raman imaging that detected lack of miscibility between its solid (cetyl palmitate) and liquid (Transcutol) lipids. SANS analyses identified lamellar arrangements inside such nanoparticles, the thickness of the lamellae been decreased by TTC. As a result of this combined approach (DOE and biophysical techniques) two optimized pre-formulations were rationally selected, both with great potential as drug delivery systems, extending the release of the anesthetic (> 48 h) and reducing TTC cytotoxicity against Balb/c 3T3 cells