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1.
Arch Dermatol Res ; 316(8): 601, 2024 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-39225867

RESUMO

Scabies is a prevalent ectoparasitic infectious disease, caused by the mite Sarcoptes scabiei. As a consequence of the infestation, localised cutaneous inflammation, pruritus and polymorphic skin lesions develop. The primary symptoms of scabies manifest as hypersensitivity-like reactions and immune responses, the precise mechanisms of which remain poorly defined. The objective of this study was to evaluate the effects of oral ivermectin treatment in patients with scabies on the systemic immune response and the patient's quality of life (QoL). Patients admitted to the dermatology outpatient clinic and diagnosed with scabies were administered oral ivermectin treatment following diagnosis at week 0 and 2. Laboratory tests were conducted to measure complete blood count (CBC), erythrocyte sedimentation rate (ESR), and C-reactive protein (CRP) levels before treatment and at week 4. The systemic immune-inflammation index (SII) was calculated using the platelet, neutrophil and lymphocyte counts. Additionally, data pertaining to the Dermatological Life Quality Index (DLQI) were recorded. In 119 patients (51 males) diagnosed with scabies, increases in ESR, CRP, and SII values and decreases in inflammatory cell counts and DLQI scores were observed one month after treatment with oral ivermectin. The results of the study showed that the use of oral ivermectin, a scabicidal agent, triggered the inflammatory response and improved the QoL of the patients.


Assuntos
Proteína C-Reativa , Ivermectina , Qualidade de Vida , Escabiose , Humanos , Escabiose/tratamento farmacológico , Escabiose/imunologia , Ivermectina/administração & dosagem , Ivermectina/uso terapêutico , Masculino , Feminino , Pessoa de Meia-Idade , Administração Oral , Adulto , Proteína C-Reativa/análise , Proteína C-Reativa/metabolismo , Idoso , Adulto Jovem , Adolescente , Antiparasitários/administração & dosagem , Antiparasitários/uso terapêutico , Sarcoptes scabiei/efeitos dos fármacos , Sarcoptes scabiei/imunologia , Sedimentação Sanguínea , Inflamação/imunologia , Inflamação/tratamento farmacológico , Resultado do Tratamento , Animais
2.
Comp Med ; 74(3): 167-172, 2024 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-39107940

RESUMO

Murine fur mites are commonly excluded in modern research animal programs, yet infestations continue to persist due to challenges in detection and control. Because all diagnostic methods and treatment options have limitations, programs must make many operational decisions when trying to eradicate these ectoparasites. The primary aim of this study was to assess various durations of treatment time with an ivermectin-compounded diet in eliminating Radfordia affinis in mice as determined by PCR testing and pelt examination. A shorter treatment duration would be highly advantageous as compared with the current regimen of 8 wk as it would minimize cost and time for animal management programs, impediments to research, and ivermectin drug effects on infested animals. Five experimental groups of R. affinis -positive mice received dietary ivermectin for 0, 2, 4, 6, or 8 wk. A fur mite-negative, naïve mouse was added to each group every 8 wk to perpetuate the infestation and amplify any remaining populations of fur mites. At 16 wk after the respective treatment end, PCR testing was performed for all treated groups in conjunction with the positive control group (no treatment). Visual examination of pelts for mites and eggs via direct microscopy was also performed at each time point. All treated mice were free of R. affinis at 16 wk after the end of treatment as confirmed by both PCR testing and pelt examination. These findings indicate that a dietary ivermectin treatment duration of as little as 2 wk is effective in eliminating R. affinis, making successful eradication initiatives more achievable.


Assuntos
Ivermectina , Infestações por Ácaros , Animais , Ivermectina/administração & dosagem , Camundongos , Infestações por Ácaros/tratamento farmacológico , Infestações por Ácaros/veterinária , Infestações por Ácaros/prevenção & controle , Ácaros/efeitos dos fármacos , Antiparasitários/administração & dosagem , Doenças dos Roedores/tratamento farmacológico , Doenças dos Roedores/parasitologia , Doenças dos Roedores/prevenção & controle , Feminino , Fatores de Tempo , Dieta/veterinária
4.
Rev Bras Parasitol Vet ; 33(3): e003324, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39140496

RESUMO

Cyathostomins are the largest group of parasites in horses that can be controlled by ivermectin (IVM). This study aimed to run a four-dose titration trial of IVM in 28 naturally infected Thoroughbred yearlings. The local Strongyle population had been recorded to be resistant to IVM (200 µg/kg). The parasite fecal egg count (FEC) was performed to investigate the egg reappearance period (ERP) of two and five weeks (w2pt and w5pt) after IVM treatment. FEC was > 1000 on day zero for all groups. Although 100% FEC reduction was reported at w2pt for all concentrations, the FEC at w5pt revealed < 83% efficacy. This study reports the reduction of ERP using the label dose as well as 300, and 400 µg/kg (double dose) of IVM. The protocol allowed IVM to significantly suppress FEC w2pt although not eliminating adult worms, failing to guarantee an extension of its protection period over 8 weeks. Moreover, the FEC at w5pt possibly means the infection was not cleared, and worms reestablished egg laying. We raised the possibility of withdrawing IVM of control programs when the drug has less than 80% FEC reduction at w5pt.


Assuntos
Ivermectina , Contagem de Ovos de Parasitas , Animais , Ivermectina/uso terapêutico , Ivermectina/administração & dosagem , Cavalos/parasitologia , Brasil , Doenças dos Cavalos/parasitologia , Doenças dos Cavalos/tratamento farmacológico , Doenças dos Cavalos/diagnóstico , Feminino , Antiparasitários/uso terapêutico , Antiparasitários/administração & dosagem , Infecções Equinas por Strongyloidea/tratamento farmacológico , Infecções Equinas por Strongyloidea/parasitologia , Infecções Equinas por Strongyloidea/diagnóstico , Fezes/parasitologia
5.
Curr Opin Infect Dis ; 37(5): 313-319, 2024 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-39088697

RESUMO

PURPOSE OF REVIEW: Neurocysticercosis (NCC) is still a significant contributor to neurological disease in vast regions of the world, and increasingly diagnosed in nonendemic countries because of travel and immigration from endemic settings. There is a need for clinicians in endemic and nonendemic regions to understand the complexities of its diagnosis and management. RECENT FINDINGS: Recent information on the performance and use of available imaging and immunodiagnostic tools as well as antiparasitic and anti-inflammatory therapeutic regimes were assessed. SUMMARY: Imaging and serology data should be assessed in the context of the specific type of NCC to improve diagnostic precision. In terms of therapeutic approaches, more controlled data is required on the efficacy and safety of combined antiparasitic therapy, and antiseizure and anti-inflammatory regimes should be optimized to minimize perilesional damage and reduce the risk of epilepsy.


Assuntos
Neurocisticercose , Neurocisticercose/diagnóstico , Neurocisticercose/epidemiologia , Humanos , Antiparasitários/uso terapêutico , Animais , Anti-Inflamatórios/uso terapêutico
6.
Trends Parasitol ; 40(9): 820-828, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-39107181

RESUMO

The development of new drug modalities has been facilitated recently by the introduction of boron as a component of organic compounds, and specifically within a benzoxaborale scaffold. This has enabled exploration of new chemical space and the development of effective compounds targeting a broad range of morbidities, including infections by protozoa, fungi, worms, and bacteria. Most notable is the recent demonstration of a single oral dose cure using acoziborole against African trypanosomiasis. Common and species-/structure-specific interactions between benzoxaboroles and parasite species have emerged and provide vital insights into the mechanisms of cidality, as well as potential challenges in terms of resistance and/or side effects. Here, we discuss the literature specific to benzoxaborole studies in parasitic protists and consider unanswered questions concerning this important new drug class.


Assuntos
Compostos de Boro , Animais , Compostos de Boro/farmacologia , Compostos de Boro/uso terapêutico , Antiparasitários/farmacologia , Antiparasitários/uso terapêutico , Humanos , Boro/farmacologia
7.
Theriogenology ; 227: 92-101, 2024 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-39047407

RESUMO

Fluazuron is a novel veterinary pour-on antitick formulation which can be applied simultaneously with bovine reproduction management strategies. Considering the economic importance of the livestock industry in many countries, it is important to know whether antiparasitics such as fluazuron may cause embryonic loss. The aim of this study was to evaluate the toxicological effect of fluazuron on bovine oocytes during in vitro maturation. The best fluazuron concentrations were determined in a preliminary experiment on Chinese hamster ovary (CHO)-K1 cells and further used to compare fluazuron toxicity in both study models. Results of the annexin V and alkaline single cell gel electrophoresis assays demonstrated that fluazuron caused cytotoxicity and genotoxicity in bovine cumulus cells at all the concentrations tested (50, 75 and 100 µg fluazuron/mL). The evaluation of cortical granules and mitochondria distribution showed that cytoplasmic maturation was not affected by fluazuron treatment. However, a decrease in metaphase II + polar body, degenerate oocytes as well as disorganized chromatin in polar body were observed at all concentrations tested. Whereas the fertilization process was not altered by 50 µg/mL fluazuron, the embryo development rate decreased significantly. No significant differences were observed in any of the oxidative stress parameters assessed. This study contributes to a better understanding of fluazuron in bovines, suggesting that the antiparasitic may affect bovine reproduction and might cause embryo loss.


Assuntos
Técnicas de Maturação in Vitro de Oócitos , Oócitos , Compostos de Fenilureia , Animais , Bovinos , Oócitos/efeitos dos fármacos , Compostos de Fenilureia/farmacologia , Técnicas de Maturação in Vitro de Oócitos/veterinária , Técnicas de Maturação in Vitro de Oócitos/métodos , Células CHO , Cricetulus , Antiparasitários/farmacologia , Antiparasitários/toxicidade , Feminino
8.
J Infect Dis ; 230(1): 263-270, 2024 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-39052743

RESUMO

Pathogens such as Plasmodium, Babesia, and Theileria invade and multiply within host red blood cells, leading to the pathological consequences of malaria, babesiosis, and theileriosis. Establishing continuous in vitro culture systems and suitable animal models is crucial for studying these pathogens. This review spotlights the Babesia duncani in culture-in mouse (ICIM) model as a promising resource for advancing research on the biology, pathogenicity, and virulence of intraerythrocytic parasites. The model offers practical benefits, encompassing well-defined culture conditions, ease of manipulation, and a well-annotated genome. Moreover, B. duncani serves as a surrogate system for drug discovery, facilitating the evaluation of new antiparasitic drugs in vitro and in animals, elucidating their modes of action, and uncovering potential resistance mechanisms. The B. duncani ICIM model thus emerges as a multifaceted tool with profound implications, promising advancements in our understanding of parasitic biology and shaping the development of future therapies.


Assuntos
Babesia , Babesiose , Modelos Animais de Doenças , Eritrócitos , Animais , Babesia/efeitos dos fármacos , Babesia/genética , Eritrócitos/parasitologia , Camundongos , Babesiose/tratamento farmacológico , Babesiose/parasitologia , Antiparasitários/uso terapêutico , Antiparasitários/farmacologia , Humanos , Virulência
9.
Environ Sci Pollut Res Int ; 31(32): 45425-45440, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38965109

RESUMO

Ivermectin (IVM) is a widely used antiparasitic. Concerns have been raised about its environmental effects in the wetlands of Río de la Plata basin where cattle have been treated with IVM for years. This study investigated the sublethal effects of environmentally relevant IVM concentrations in sediments on the Neotropical fish Prochilodus lineatus. Juvenile P. lineatus were exposed to IVM-spiked sediments (2 and 20 µg/Kg) for 14 days, alongside a control sediment treatment without IVM. Biochemical and oxidative stress responses were assessed in brain, gills, and liver tissues, including lipid damage, glutathione levels, enzyme activities, and antioxidant competence. Muscle and brain acetylcholinesterase activity (AChE) and stable isotopes of 13C and 15N in muscle were also measured. The lowest IVM treatment resulted in an increase in brain lipid peroxidation, as measured by thiobarbituric acid reactive substances (TBARs), decreased levels of reduced glutathione (GSH) in gills and liver, increased catalase activity (CAT) in the liver, and decreased antioxidant capacity against peroxyl radicals (ACAP) in gills and liver. The highest IVM treatment significantly reduced GSH in the liver. Muscle (AChE) was decreased in both treatments. Multivariate analysis showed significant overall effects in the liver tissue, followed by gills and brain. These findings demonstrate the sublethal effects of IVM in P. lineatus, emphasizing the importance of considering sediment contamination and trophic habits in realistic exposure scenarios.


Assuntos
Antiparasitários , Ivermectina , Poluentes Químicos da Água , Animais , Ivermectina/toxicidade , Antiparasitários/toxicidade , Poluentes Químicos da Água/toxicidade , Gado , América do Sul , Estresse Oxidativo/efeitos dos fármacos , Sedimentos Geológicos/química , Brânquias/efeitos dos fármacos , Brânquias/metabolismo
11.
Vet Rec ; 195(1): 46, 2024 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-38967199

RESUMO

Did you spot BVA President Anna Judson on BBC's Springwatch last month, talking about the measures vets can take to help minimise the impact of parasiticides on the environment?


Assuntos
Antiparasitários , Animais , Humanos , Reino Unido , Antiparasitários/uso terapêutico , Doenças Parasitárias em Animais/prevenção & controle , Sociedades Veterinárias
12.
Spectrochim Acta A Mol Biomol Spectrosc ; 321: 124757, 2024 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-38959688

RESUMO

With the developing resistance to traditional antiparasitic medications, the purpose of this study was to efficiently develop a series of six noble flavanoidal tetrazinane-6'-one derivatives by a one-pot reaction pathway. FT-IR, 1HNMR, 13CNMR, and Mass spectra were employed for the structural elucidation of the synthesized compounds (7-12). Clinostomum complanatum, a parasite infection model that has been well-established, demonstrated that all the synthesized compounds are potent antiparasitic agents. DNA is the main target for various medicinal compounds. As a result, thestudy of how small molecules attach to DNA has received a lot of attention. In the present study, we have performed various biophysical techniques to determine the mode of binding of synthesized compounds (7-12) with calf thymus DNA (ct-DNA). It was observed from the UV-visible absorbance and fluorescence spectra that all synthesized compounds (7-12) form complexes with the ct-DNA. The value of binding constant (Kb) was obtained to be in the range of 4.36---24.50 × 103 M - 1 at 298 K. Competitive displacement assay with ethidium bromide (EB), CD spectral analysis, viscosity measurements, and in silico molecular docking confirmed that ligands (7-12) incorporate with ct-DNA through groove binding only. Molecular docking studies were performed for all synthesized compounds with the calf thymus DNA and it was found that all the newly synthesized compounds strongly bind with the chain B of DNA in the minor groove with the value of binding energy in the range of -8.54 to -9.04 kcal per mole and several hydrogen bonding interactions.


Assuntos
DNA , Simulação de Acoplamento Molecular , Espectrometria de Fluorescência , DNA/metabolismo , DNA/química , Animais , Bovinos , Antiparasitários/farmacologia , Antiparasitários/química , Antiparasitários/síntese química , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Modelos Moleculares , Flavonoides/farmacologia , Flavonoides/química , Flavonoides/metabolismo , Flavonoides/síntese química , Dicroísmo Circular
13.
Eur J Med Chem ; 276: 116641, 2024 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-38971047

RESUMO

Chagas disease is caused by the parasite Trypanosoma cruzi and affects over 7 million people worldwide. The two actual treatments, Benznidazole (Bzn) and Nifurtimox, cause serious side effects due to their high toxicity leading to treatment abandonment by the patients. In this work, we propose DNA G-quadruplexes (G4) as potential therapeutic targets for this infectious disease. We have found 174 PQS per 100,000 nucleotides in the genome of T. cruzi and confirmed G4 formation of three frequent motifs. We synthesized a family of 14 quadruplex ligands based in the dithienylethene (DTE) scaffold and demonstrated their binding to these identified G4 sequences. Several DTE derivatives exhibited micromolar activity against epimastigotes of four different strains of T. cruzi, in the same concentration range as Bzn. Compounds L3 and L4 presented remarkable activity against trypomastigotes, the active form in blood, of T. cruzi SOL strain (IC50 = 1.5-3.3 µM, SI = 25-40.9), being around 40 times more active than Bzn and displaying much better selectivity indexes.


Assuntos
Doença de Chagas , Quadruplex G , Tripanossomicidas , Trypanosoma cruzi , Trypanosoma cruzi/efeitos dos fármacos , Quadruplex G/efeitos dos fármacos , Ligantes , Doença de Chagas/tratamento farmacológico , Tripanossomicidas/farmacologia , Tripanossomicidas/química , Tripanossomicidas/síntese química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Relação Dose-Resposta a Droga , Testes de Sensibilidade Parasitária , Antiparasitários/farmacologia , Antiparasitários/química , Antiparasitários/síntese química
14.
PLoS One ; 19(7): e0305667, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39028725

RESUMO

In eastern India, the tubers of Pueraria tuberosa (Willd.) DC. are used by the ethnic communities for its wide range of medicinal and nutritional value, especially to rejuvenate livestock health and to treat helminthiasis. The study is aimed to evaluate the ethnoveterinary medicinal importance of P. tuberosa as anthelmintic, to verify its nontoxic nature and identify the most potent phytoconstituents aided by in silico molecular docking technique. Ethnomedicinal data collected from 185 informants were quantitatively analyzed employing eight quantitative indices to highlight the use diversity and most frequently used part of the plant. High scores of certain indices employed, such as Use Value (UV = 0.52), Fidelity Level (FL = 68.42%) and Tissue Importance Value (TIV = 1) clearly illustrate an ethnomedicinal lead regarding medico-nutritional benefits of the tuber part used against intestinal helminthic diseases of veterinary animals. Based on this ethno-guided lead, root tuber has been investigated for its chemical profiling by the estimation of total phenolics, flavonoids, tannins and alkaloids, along with HPLC and GC-MS analyses. Anthelmintic property was evaluated with the tuber extracts by in vitro studies on some helminths of livestock and poultry birds, and it showed promising results against the tested parasites namely Cotylophoron cotylophorum, Raillietina tetragona and Setaria cervi. Toxicity assessments of tuber extract through in vitro and in vivo methods were performed using Vero cells and BALB/c mice. Nontoxic nature of the studied tuber extract was observed even in higher experimental doses. Out of 12 phytocompounds identified by GC-MS analysis, one compound [Morphinan-4,5-epoxy-3,6-di-ol,6- (7-nitrobenzofurazan-4-yl) amino-] exhibited the best binding conformations in cost of the lowest binding energy values with six target proteins that include one anti-inflammatory, one antioxidant, and four anthelmintic proteins. The findings of our study are found very encouraging to evaluate this tuber drug furthermore intensively towards the development of anthelmintic veterinary medicine.


Assuntos
Gado , Extratos Vegetais , Pueraria , Animais , Pueraria/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Gado/parasitologia , Camundongos , Tubérculos/química , Simulação de Acoplamento Molecular , Etnofarmacologia , Humanos , Anti-Helmínticos/farmacologia , Chlorocebus aethiops , Células Vero , Antiparasitários/farmacologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Feminino , Masculino , Índia
16.
PLoS Negl Trop Dis ; 18(6): e0012232, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38843299

RESUMO

BACKGROUND: Ocular toxoplasmosis (OT) is the most common cause of infectious uveitis worldwide, including Thailand. This study describes the clinical presentation, visual acuity (VA) outcomes, and factors associated with VA loss in patients with active OT following antiparasitic treatment. METHODOLOGY/PRINCIPAL FINDINGS: A retrospective chart review of patients with active OT treated with antiparasitic drugs between 2010 and 2020 was performed. Outcome measures included clinical characteristics, interval VA, and predictive factors associated with loss of VA ≤ 20/50 at 6 months post-treatment. Ninety-two patients (95 eyes) were enrolled. The median follow-up time was 10.9 months (IQR 4.9-31.8 months). The median age at presentation was 35.9 years, 51% were male, and 92.4% had unilateral OT. Eleven patients (12%) were immunocompromised (HIV infection, eight patients; receiving immunosuppressive agents, three patients). Patients mainly presented with primary retinitis without previous scar (62%), posterior pole lesion (56%), and lesion size of ≤ 2-disc area (75%). Immunocompromised patients showed a significantly larger size of retinitis than immunocompetent patients. Oral trimethoprim/sulfamethoxazole monotherapy was the primary short-term antiparasitic drug prescribed (85%). At the final visit, 21% of all affected eyes suffered VA ≤ 20/200. The cumulative incidence of recurrent OT at three years was 33.9% (95% CI, 19.7%-54.2%). Immunocompromised patients [adjusted odds ratio (aOR) 4.9, p = 0.041], macular lesion (aOR 5.4, p = 0.032), and initial VA ≤ 20/200 (aOR 9.1, p = 0.014) were predictive of having VA ≤ 20/50 at 6 months post-treatment. CONCLUSIONS: Ocular toxoplasmosis mainly presents as unilateral primary retinitis within the posterior pole. Severe VA loss was observed in one-fifth of eyes following treatment with lesion resolution. Immunocompromised patients, eyes with macular lesions, and poor initial VA were associated with poor VA outcomes.


Assuntos
Centros de Atenção Terciária , Toxoplasmose Ocular , Acuidade Visual , Humanos , Toxoplasmose Ocular/tratamento farmacológico , Toxoplasmose Ocular/fisiopatologia , Toxoplasmose Ocular/complicações , Toxoplasmose Ocular/epidemiologia , Masculino , Estudos Retrospectivos , Adulto , Feminino , Tailândia/epidemiologia , Pessoa de Meia-Idade , Centros de Atenção Terciária/estatística & dados numéricos , Adulto Jovem , Hospedeiro Imunocomprometido , Antiparasitários/uso terapêutico , Combinação Trimetoprima e Sulfametoxazol/uso terapêutico , Adolescente , Resultado do Tratamento , População do Sudeste Asiático
17.
Artigo em Inglês | MEDLINE | ID: mdl-38889874

RESUMO

Tizoxanide (TZX) is an active metabolite of nitazoxanide (NTZ) originally developed as an antiparasitic agent, and is predominantly metabolized into TZX glucuronide. In the present study, TZX glucuronidation by the liver and intestinal microsomes of humans, monkeys, dogs, rats, and mice, and recombinant human UDP-glucuronosyltransferase (UGT) were examined. The kinetics of TZX glucuronidation by the liver and intestinal microsomes followed the Michaelis-Menten or biphasic model, with species-specific variations in the intrinsic clearance (CLint). Rats and mice exhibited the highest CLint values for liver microsomes, while mice and rats were the highest for intestinal microsomes. Among human UGTs, UGT1A1 and UGT1A8 demonstrated significant glucuronidation activity. Estradiol and emodin inhibited TZX glucuronidation activities in the human liver and intestinal microsomes in a dose-dependent manner, with emodin showing stronger inhibition in the intestinal microsomes. These results suggest that the roles of UGT enzymes in TZX glucuronidation in the liver and small intestine differ extensively across species and that UGT1A1 and/or UGT1A8 mainly contribute to the metabolism and elimination of TZX in humans. This study presents the relevant and novel-appreciative report on TZX metabolism catalyzed by UGT enzymes, which may aid in the assessment of the antiparasitic, antibacterial, and antiviral activities of NTZ for the treatment of various infections.


Assuntos
Glucuronídeos , Glucuronosiltransferase , Intestino Delgado , Fígado , Nitrocompostos , Especificidade da Espécie , Tiazóis , Animais , Glucuronosiltransferase/metabolismo , Humanos , Cães , Tiazóis/metabolismo , Intestino Delgado/metabolismo , Intestino Delgado/enzimologia , Intestino Delgado/efeitos dos fármacos , Camundongos , Ratos , Nitrocompostos/metabolismo , Fígado/metabolismo , Fígado/enzimologia , Fígado/efeitos dos fármacos , Masculino , Glucuronídeos/metabolismo , Macaca fascicularis , Microssomos Hepáticos/metabolismo , Antiparasitários/metabolismo , Feminino , Microssomos/metabolismo , Microssomos/enzimologia , Ratos Sprague-Dawley , Isoenzimas/metabolismo
18.
Anal Methods ; 16(25): 4136-4142, 2024 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-38860551

RESUMO

The ivermectin (IVM), as a broad-spectrum antiparasitic drug, was widely prescribed to treat COVID-19 during the pandemic, despite lacking proven efficacy in combating this disease. Therefore, it is important to establish affordable devices in laboratories with minimal infrastructure. The laser engraving technology has been revolutionary in sensor manufacturing, primarily attributed to the diversity of substrates that can be employed and the freedom it provides in creating sensor models. In this work, electrochemical sensors based on graphene were developed using the laser engraving technology for IVM sensing. Through, the studies that used the techniques of cyclic voltammetry and differential pulse voltammetry, following parameter optimization, for the laser-induced graphene electrode demonstrated a mass transport governed by adsorption of the species and exhibited a linear working range of 10-100 (µmol L-1), a limit of detection (LOD) of 1.6 × 10-6 (mol L-1), a limit of quantification (LOQ) of 4.8 × 10-6 (mol L-1), and a sensitivity of 0.139 (µA µmol L-1). The developed method was successfully applied to direct analysis of pharmaceutical tablets, tap water (recovery of 94%) and synthetic urine samples (recovery between 97% and 113%). These results demonstrate the feasibility of the method for routine analyses involving environmental samples.


Assuntos
Técnicas Eletroquímicas , Grafite , Ivermectina , Lasers , Ivermectina/análise , Ivermectina/química , Técnicas Eletroquímicas/métodos , Técnicas Eletroquímicas/instrumentação , Grafite/química , Humanos , Limite de Detecção , Antiparasitários/urina , Antiparasitários/análise , Antiparasitários/química , Eletrodos , COVID-19 , SARS-CoV-2
19.
Artigo em Inglês | MEDLINE | ID: mdl-38885750

RESUMO

Ivermectin (IVM) is a broad-spectrum veterinary antiparasitic used worldwide in cattle breeding. The aim of this study was to evaluate the lethal effects of the active ingredient and a commercial formulation of IVM (1 % active ingredient) in the embryonic stage (S. 4-6) and larval stage (S. 25) of the South American amphibian Rhinella arenarum through chronic standardized bioassays. Also, behavior analysis and oxidative stress and cholinergic effects biomarkers were analyzed at 1, 10 and 100 µg IVM/L concentrations. For the embryonic stage, the active ingredient (96 h- LC50: 15900 µg/L) was more toxic than the commercial formulation (96 h-LC50: 51230 µg/L) during the acute period, while at chronic exposure the commercial formulation was more toxic (504 h-LC50: 10.25 µg/L), compared to the active ingredient (504 h-LC50: 312.80 µg/L). For the larval stage, in acute exposure, the active ingredient (96 h-LC50: 800 µg/L) was more toxic than the commercial formulation (96 h-LC50: 1550 µg/L). In the chronic exposure, the commercial formulation (504 h-LC50: 77.33 µg/L) was more toxic than the active ingredient (504 h-LC50: 195.25 µg/L). Overall, larvae exhibited greater sensitivity to both the active ingredient and the commercial formulation. However, during chronic exposure, embryos were more sensitive to the commercial formulation than larvae. The commercial formulation primarily induced oxidative stress, and both forms of the compound affected behavior and cholinergic effect biomarkers, even at low environmentally relevant concentrations (1 µg/L). These results highlight the potential impact of IVM on aquatic ecosystems.


Assuntos
Ivermectina , Larva , Estresse Oxidativo , Poluentes Químicos da Água , Animais , Ivermectina/toxicidade , Poluentes Químicos da Água/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Larva/efeitos dos fármacos , Antiparasitários/toxicidade , Bufonidae , Dose Letal Mediana , Ecotoxicologia , Embrião não Mamífero/efeitos dos fármacos
20.
Fish Shellfish Immunol ; 151: 109717, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38914179

RESUMO

Aquaculture is one of the fastest growing sectors in global food production, recognized as a significant contributor to poverty alleviation, food security, and income generation. However, the frequent occurrence of diseases caused by pathogen infections result in reduced yields and economic losses, posing a substantial constraint to the sustainable development of aquaculture. Here, our study identified that four catechol compounds, quercetin, luteolin, caffeic acid, and chlorogenic acid, exhibited potent antiparasitic effects against Ichthyophthirius multifiliis in both, in vitro and in vivo. The parasite is recognized as one of the most pathogenic to fish worldwide. Using a combination of in silico methods, the dipeptidyl peptidase (DPP) was identified as a critical target for catechol compounds. The two hydroxyl radicals of the catechol group were essential for its binding to and interacting with the DPP protein. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses indicated that catechol compounds disrupt pathways associated with the metabolism and growth of I. multifiliis, thereby exerting antiparasitic effects. Furthermore, these compounds attenuated the expression of proinflammatory cytokines in vivo in fish and promoted macrophage polarization toward M2 phenotype by inhibiting the STAT1 signaling pathway. The dual activity of catechol compounds, acting as both direct antiparasitic and anti-inflammatory agents in fish, offers a promising therapeutic approach for combating I. multifiliis infections in aquaculture.


Assuntos
Catecóis , Infecções por Cilióforos , Doenças dos Peixes , Hymenostomatida , Animais , Doenças dos Peixes/imunologia , Doenças dos Peixes/parasitologia , Doenças dos Peixes/prevenção & controle , Hymenostomatida/efeitos dos fármacos , Catecóis/farmacologia , Infecções por Cilióforos/veterinária , Infecções por Cilióforos/imunologia , Infecções por Cilióforos/parasitologia , Infecções por Cilióforos/prevenção & controle , Antiparasitários/farmacologia
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