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1.
Anticancer Agents Med Chem ; 24(10): 798-811, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38500290

RESUMO

INTRODUCTION: Bee venom has therapeutics and pharmacological properties. Further toxicological studies on animal models are necessary due to the severe allergic reactions caused by this product. METHOD: Here, Caenorhabditis elegans was used as an in vivo toxicity model, while breast cancer cells were used to evaluate the pharmacological benefits. The bee venom utilized in this research was collected from Apis mellifera species found in Northeast Brazil. The cytotoxicity caused by bee venom was measured by MTT assay on MDA-MB-231 and J774 A.1 cells during 24 - 72 hours of exposure. C. elegans at the L4 larval stage were exposed for three hours to M9 buffer or bee venom. Survival, behavioral parameters, reproduction, DAF-16 transcription factor translocation, the expression of superoxide dismutase (SOD), and metabolomics were analyzed. Bee venom suppressed the growth of MDA-MB-231 cancer cells and exhibited cytotoxic effects on macrophages. Also, decreased C. elegans survival impacted its behaviors by decreasing C. elegans feeding behavior, movement, and reproduction. RESULTS: Bee venom did not increase the expression of SOD-3, but it enhanced DAF-16 translocation from the cytoplasm to the nucleus. C. elegans metabolites differed after bee venom exposure, primarily related to aminoacyl- tRNA biosynthesis, glycine, serine and threonine metabolism, and sphingolipid and purine metabolic pathways. Our findings indicate that exposure to bee venom resulted in harmful effects on the cells and animal models examined. CONCLUSION: Thus, due to its potential toxic effect and induction of allergic reactions, using bee venom as a therapeutic approach has been limited. The development of controlled-release drug strategies to improve this natural product's efficacy and safety should be intensified.


Assuntos
Antineoplásicos , Venenos de Abelha , Caenorhabditis elegans , Animais , Humanos , Venenos de Abelha/farmacologia , Venenos de Abelha/química , Caenorhabditis elegans/efeitos dos fármacos , Caenorhabditis elegans/metabolismo , Antineoplásicos/farmacologia , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Relação Dose-Resposta a Droga , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Neoplasias da Mama/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Relação Estrutura-Atividade , Feminino , Estrutura Molecular
2.
Anticancer Agents Med Chem ; 23(12): 1469-1481, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37032502

RESUMO

INTRODUCTION: Despite numerous scientific advances, cancer continues to be one of the main causes of death in the world. This situation has driven the search for promising molecules. Lichen substances have been widely described for their pharmacological potential. OBJECTIVE: The present study evaluated the antitumour potential of a depsidone isolated from Parmotrema concurrens- salazinic acid (SAL) - through in vitro, in vivo and in silico studies. METHODS: The molecule was isolated from the acetonic extract of the lichen and recrystallized in acetone. The macrophage J774, sarcoma-180 and MDA-MB-231 cell lines were used for the MTT cytotoxicity assay. The antitumor assay used a murine model (Swiss albino mice) with sarcoma-180. The animals were treated for seven consecutive days with doses of SAL (25 and 50 mg/kg) and 5-fluorouracil (20 mg/kg). RESULTS: Its purity was determined using high-performance liquid chromatography (94%), and its structure was confirmed by H1 and C13 nuclear magnetic resonance. SAL was not considered toxic to cancer cell lines, showing cell viability rates of 79.49 ± 4.15% and 86.88 ± 1.02% for sarcoma-180 and MDA-MB-231, respectively. The tumour inhibition rate was greater than 80% in the animals treated with SAL and 65% for those that received 5-fluorouracil. Simulations of molecular dynamics to estimate the flexibility of the interactions between human thymidylate synthase and derivatives of SAL and 5-fluorouracil revealed that SAL exhibited greater enzymatic interaction capacity, with highly favourable energy, compared to 5-fluorouracil. CONCLUSION: The present results demonstrate the potential of salazinic acid as a tumour inhibition agent.


Assuntos
Antineoplásicos , Líquens , Sarcoma , Humanos , Animais , Camundongos , Antineoplásicos/farmacologia , Fluoruracila/farmacologia , Salicilatos , Líquens/química
3.
Can Oncol Nurs J ; 32(2): 162-171, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35582247

RESUMO

Objective: To evaluate the quality of life (QOL) of patients with breast cancer undergoing radiotherapy treatment. Methods: The current study is a descriptive quantitative approach that seeks to identify the QOL of breast cancer patients during their radiotherapy treatment. A convenience sample of 30 women undergoing radiotherapy for breast cancer completed the EORTC QLQC30 questionnaire on Day 1 and Day 28. Results: Results showed significant differences in QOL between the two sessions. Decreases in overall health (88.33 to 61.67) and functional health (76.45 to 67.77) were noted in parallel to an increase in the scale of symptoms (13.85 for 24.62). Conclusions: The radiotherapeutic treatment impacts the QOL of patients with breast cancer. It is crucial for the nursing team to work together with a multi-professional team to adequately manage the treatment of these patients adequately.

5.
AAPS PharmSciTech ; 22(3): 104, 2021 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-33718986

RESUMO

Pain is a phenomenon present in the majority of the population, affecting, among others, the elderly, overweight people, and especially recently operated patients, analgesia being necessary. In the specific case of relief of postoperative pain, different kinds of anesthetics are being used, among them bupivacaine, a widely used drug which promotes long-lasting analgesic effects. However, cardiotoxicity and neurotoxicity are related to its repetitive use. To overcome these shortcomings, Novabupi® (a racemic mixture) was developed and is marketed as an injectable solution. This formulation contains an enantiomeric excess of the levogyre isomer, which has reduced toxicity effects. Seeking to rationalize its use by extending the duration of effect and reducing the number of applications, the objectives of this work were to develop and evaluate liposomes containing Novabupi (LBPV), followed by incorporation into thermogel. Liposomes were prepared using the lipid hydration method, followed by size reduction using sonication, and the developed formulations were characterized by hydrodynamic diameter, polydispersity index (PDI), surface zeta potential, and encapsulation efficiency. The selected optimal liposomal formulation was successfully incorporated into a thermogel without loss of thermoresponsive properties, being suitable for administration as a subcutaneous injection. In the ex vivo permeation studies with fresh rodent skin, the thermogel with liposomes loaded with 0.5% LBPV (T-gel formulation 3) showed higher permeation rates compared to the starting formulation, thermogel with 0.5% LBPV (T-Gel 1), which will probably translate into better therapeutic benefits for treatment of postoperative analgesia, especially with regard to the number of doses applied.


Assuntos
Analgesia/métodos , Levobupivacaína/administração & dosagem , Levobupivacaína/farmacocinética , Dor/tratamento farmacológico , Dor/metabolismo , Animais , Bovinos , Galinhas , Membrana Corioalantoide/efeitos dos fármacos , Membrana Corioalantoide/metabolismo , Géis , Humanos , Lipossomos , Masculino , Camundongos , Células NIH 3T3 , Técnicas de Cultura de Órgãos , Ratos , Ratos Wistar , Pele/efeitos dos fármacos , Pele/metabolismo , Absorção Cutânea/efeitos dos fármacos , Absorção Cutânea/fisiologia
6.
Curr Drug Deliv ; 18(5): 583-595, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32860358

RESUMO

In response to the global outbreak caused by SARS-CoV-2, this article aims to propose the development of nanosystems for the delivery of hydroxychloroquine in the respiratory system to the treatment of COVID-19. A descriptive literature review was conducted, using the descriptors "COVID-19", "Nanotechnology", "Respiratory Syndrome" and "Hydroxychloroquine", in the PubMed, ScienceDirect and SciElo databases. After analyzing the articles according to the inclusion and exclusion criteria, they were divided into 3 sessions: Coronavirus: definitions, classifications and epidemiology, pharmacological aspects of hydroxychloroquine and pharmaceutical nanotechnology in targeting of drugs. We used 131 articles published until July 18, 2020. Hydroxychloroquine seems to promote a reduction in viral load, in vivo studies, preventing the entry of SARS-CoV-2 into lung cells, and the safety of its administration is questioned due to the toxic effects that it can develop, such as retinopathy, hypoglycemia and even cardiotoxicity. Nanosystems for the delivery of drugs in the respiratory system may be a viable alternative for the administration of hydroxychloroquine, which may enhance the therapeutic effect of the drug with a consequent decrease in its toxicity, providing greater safety for implementation in the clinic in the treatment of COVID-19.


Assuntos
Antivirais/administração & dosagem , Tratamento Farmacológico da COVID-19 , Portadores de Fármacos/química , Hidroxicloroquina , Sistema Respiratório , Humanos , Hidroxicloroquina/administração & dosagem , Nanopartículas
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