Brazilian Journal of Pharmaceutical Sciences最新文献_第6页

Selective photodynamic effects on cervical adenocarcinoma cells provided by F127 Pluronic®-based micelles modulating hypericin delivery 基于F127 Pluronic®的胶束调节金丝桃素递送对宫颈腺癌细胞的选择性光动力作用

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-22 DOI: 10.1590/s2175-97902023e22459

K. H. Mashiba, Lucimara Rofrigues Carobeli, Maria Vítoria Felipe de Souza, Lyvia Eloiza de Freitas Meirelles, N. L. Mari, G. B. Cesar, R. S. Gonçalves, W. Caetano, Edílson Damke, V. R. S. Silva, G. M. Z. F. Damke, M. E. L. Consolaro

{"title":"Selective photodynamic effects on cervical adenocarcinoma cells provided by F127 Pluronic®-based micelles modulating hypericin delivery","authors":"K. H. Mashiba, Lucimara Rofrigues Carobeli, Maria Vítoria Felipe de Souza, Lyvia Eloiza de Freitas Meirelles, N. L. Mari, G. B. Cesar, R. S. Gonçalves, W. Caetano, Edílson Damke, V. R. S. Silva, G. M. Z. F. Damke, M. E. L. Consolaro","doi":"10.1590/s2175-97902023e22459","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22459","url":null,"abstract":"Cervical cancer is a leading cause of death among women. The endocervical adenocarcinoma (ECA) represents an aggressive and metastatic type of cancer with no effective treatment options currently available. We evaluated the antitumoral and anti-migratory effects of hypericin (HYP) encapsulated on Pluronic F127 (F127/HYP) photodynamic therapy (PDT) against a human cell line derived from invasive cervical adenocarcinoma (HeLa) compared to a human epithelial cell line (HaCaT). The phototoxicity and cytotoxicity of F127/HYP were evaluated by the following assays: colorimetric assay, MTT, cellular morphological changes by microscopy and long-term cytotoxicity by clonogenic assay. In addition, we performed fluorescence microscopy to analyze cell uptake and subcellular distribution of F127/HYP, cell death pathway and reactive oxygen species (ROS) production. The PDT mechanism was determined with sodium azide and D-mannitol and cell migration by wound-healing assay. The treatment with F127/HYP promoted a phototoxic result in the HeLa cells in a dose-dependent and selective form. Internalization of F127/HYP was observed mainly in the mitochondria, causing cell death by necrosis and ROS production especially by the type II PDT mechanism. Furthermore, F127/HYP reduced the long-term proliferation and migration capacity of HeLa cells. Overall, our results indicate a potentially application of F127/HYP micelles as a novel approach for PDT with HYP delivery to more specifically treat ECA.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67741837","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Development and clinical application of hydrogel formulations containing papain and urea for wound healing 含有木瓜蛋白酶和尿素的伤口愈合水凝胶配方的开发和临床应用

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e201090

Thais Menezes dos Santos, Danieli Silva Feijó de Sousa, Karina Chamma Di Piero, A. Todeschini, W. Dias, C. Oliveira, E. P. Santos, M. Monteiro, M. K. Gomes, Cristiano dos Reis Moura, Pedro Antônio Castelo Teixeira, E. Ricci-Júnior, Z. Freitas

{"title":"Development and clinical application of hydrogel formulations containing papain and urea for wound healing","authors":"Thais Menezes dos Santos, Danieli Silva Feijó de Sousa, Karina Chamma Di Piero, A. Todeschini, W. Dias, C. Oliveira, E. P. Santos, M. Monteiro, M. K. Gomes, Cristiano dos Reis Moura, Pedro Antônio Castelo Teixeira, E. Ricci-Júnior, Z. Freitas","doi":"10.1590/s2175-97902023e201090","DOIUrl":"https://doi.org/10.1590/s2175-97902023e201090","url":null,"abstract":"Hydrogels are used for wound treatment, as they may contain one or more active components and protect the wound bed. Papain is one of the active substances that have been used with this purpose, alongside urea. In this paper, carboxypolymethylene hydrogels containing papain (2% and 10% concentrations) and urea (5% concentration) were produced. Physical-chemical stability was performed at 0, 7, 15 and 30 days at 2-8ºC, 25ºC and 40ºC, as well as the rheological aspects and proteolytic activity of papain by gel electrophoresis. Clinical efficacy of the formulations in patients with lower limb ulcers was also evaluated in a prospective, single-center, randomized, double-blind and comparative clinical trial. The results showed 7-day stability for the formulations under 25ºC, in addition to approximately 100% and 15% of protein activity for 10% and 2% papain hydrogel, respectively. The rheological profile was non-Newtonian for the 10% papain hydrogel tested. There were no significant differences regarding the mean time for healing of the lesions, although 10% papain presented a better approach to be used in all types of tissue present in the wound bed.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67737254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Applicability of [18F]FDG/PET for investigating rosmarinic acid preconditioning efficacy in a global stroke model in mice [18F]FDG/PET对小鼠脑卒中模型迷迭香酸预处理效果的适用性

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e21555

E. V. Santos, B. G. A. Schirmer, Jousie Michel Pereira, N. V. S. Cardoso, C. Malamut, Mércia Liane de Oliveira

{"title":"Applicability of [18F]FDG/PET for investigating rosmarinic acid preconditioning efficacy in a global stroke model in mice","authors":"E. V. Santos, B. G. A. Schirmer, Jousie Michel Pereira, N. V. S. Cardoso, C. Malamut, Mércia Liane de Oliveira","doi":"10.1590/s2175-97902023e21555","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21555","url":null,"abstract":"Positron emission tomography (PET) is a non-invasive nuclear imaging technique that uses radiotracers to track cell activity. The radiopharmaceutical 18F-fluoro-2-deoxyglucose ([ 18 F] FDG) is most commonly used in nuclear medicine for the diagnosis of various diseases, including stroke. A stroke is a serious condition with high mortality and morbidity rates. Rosmarinic acid (RA) is a promising therapeutic agent that exerts neuroprotective effects against various neurological diseases. Therefore, this study aimed to evaluate the applicability of [ 18 F]FDG/ PET for investigating the neuroprotective effects of RA in case of a global stroke model in mice. The [ 18 F]FDG/PET technique facilitates the observation of ischemia and reperfusion injuries in the brain. Moreover, the recovery of glucose metabolism in three specific brain regions, the striatum, superior colliculus, and inferior colliculus, was observed after preconditioning with RA. It was concluded that the [ 18 F]FDG/PET technique may be useful for stroke diagnosis and the assessment of treatment response. In addition, a long-term longitudinal study using biochemical analysis in conjunction with functional imaging may provide further conclusive results regarding the effect of RA on cerebral ischemia.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67740956","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Development of metformin HCl granules using brown flaxseed mucilage as a retardant polymer: effects of polymer and drug ratio 棕色亚麻籽胶浆作为阻燃聚合物制备盐酸二甲双胍颗粒：聚合物和药物配比的影响

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e22320

L. O. Rodrigues, D. Falcão, S. Mourão

{"title":"Development of metformin HCl granules using brown flaxseed mucilage as a retardant polymer: effects of polymer and drug ratio","authors":"L. O. Rodrigues, D. Falcão, S. Mourão","doi":"10.1590/s2175-97902023e22320","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22320","url":null,"abstract":"Flaxseed ( Linum usitatissimum L.) is the seed of a multipurpose plant of pharmaceutical interest, as its mucilage can be used as a natural matrix to develop extended-release dosage forms and potentially replace synthetic polymers. In this study, a 3² factorial design with two replicates of the central point was applied to optimize the development of extended-release granules of metformin HCl. The total fiber content of the mucilage as well as the friability and dissolution of the formulations were evaluated. The lyophilized mucilage presented a high total fiber content (42.63%), which suggests a high efficiency extraction process. Higher concentrations of the mucilage and metformin HCl yielded less friable granules. In addition, lower concentrations of metformin HCl and higher concentrations of the mucilage resulted in slower drug release during the dissolution assays. The release kinetics for most formulations were better represented by the Hixson-Crowell model, while formulations containing a higher concentration of the mucilage were represented by the Korsmeyer-Peppas model. Nonetheless, five formulations showed a longer release than the reference HPMC formulation. More desirable results were obtained with a higher concentration of the mucilage (13–18%) and a lower concentration of metformin (40%).","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742077","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

3D-QSARpy: Combining variable selection strategies and machine learning techniques to build QSAR models 3D QSARpy：结合变量选择策略和机器学习技术构建QSAR模型

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e22373

Priscilla S. de S. N. Silverio, J. O. Viana, E. Barbosa

{"title":"3D-QSARpy: Combining variable selection strategies and machine learning techniques to build QSAR models","authors":"Priscilla S. de S. N. Silverio, J. O. Viana, E. Barbosa","doi":"10.1590/s2175-97902023e22373","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22373","url":null,"abstract":"Quantitative Structure-Activity Relationship (QSAR) is a computer-aided technology in the field of medicinal chemistry that seeks to clarify the relationships between molecular structures and their biological activities. Such technologies allow for the acceleration of the development of new compounds by reducing the costs of drug design. This work presents 3D-QSARpy, a flexible, user-friendly and robust tool, freely available without registration, to support the generation of QSAR 3D models in an automated way. The user only needs to provide aligned molecular structures and the respective dependent variable. The current version was developed using Python with packages such as scikit-learn and includes various techniques of machine learning for regression. The diverse techniques employed by the tool is a differential compared to known methodologies, such as CoMFA and CoMSIA, because it expands the search space of possible solutions, and in this way increases the chances of obtaining relevant models. Additionally, approaches for select variables (dimension reduction) were implemented in the tool. To evaluate its potentials, experiments were carried out to compare results obtained from the proposed 3D-QSARpy tool with the results from already published works. The results demonstrated that 3D-QSARpy is extremely useful in the field due to its expressive results.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67742175","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Antioxidant, Antidiabetic and Lipid Profiling of Spermadicyton Suaveolens in Streptozotocin (STZ) Induced Diabetic Rats 链脲佐菌素(STZ)诱导的糖尿病大鼠精原细胞抗氧化、降糖及脂质谱分析

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e21820

Pratik P. Maske, P. Kumbhar, Ashok Gurulingappa Wali, J. Disouza, M. Sharma

{"title":"Antioxidant, Antidiabetic and Lipid Profiling of Spermadicyton Suaveolens in Streptozotocin (STZ) Induced Diabetic Rats","authors":"Pratik P. Maske, P. Kumbhar, Ashok Gurulingappa Wali, J. Disouza, M. Sharma","doi":"10.1590/s2175-97902023e21820","DOIUrl":"https://doi.org/10.1590/s2175-97902023e21820","url":null,"abstract":"Diabetes is a life-threatening disease, and currently available synthetic medicines for treating diabetes are associated with various side effects. Therefore, there is an unmet need to develop herbal remedies against diabetes as an alternative to synthetic medicines. Although local healers use the roots of Spermadicyton suaveolens (SS) to manage diabetes, there is negligible research to validate its antidiabetic properties. The present investigation aims to the assess the antioxidant, antidiabetic, and antihyperlipidemic potential of the ethanolic extract of S. Suaveolen’s roots (EESS) on streptozotocin (STZ) induced diabetic rats. The extract was screened for in vitro antioxidant and antidiabetic activity. The in vivo antidiabetic potential of EESS (at 200 and 400 mg/kg) was studied on STZ-induced diabetic rats for 20 days. The EESS displayed significant (p<0.05) antidiabetic and antioxidant properties. The administration of 200 mg/kg and 400 mg/kg EESS in STZ-induced diabetic rats significantly reduced hyperglycemia, and restored antioxidant enzymes and lipid profile–a high density lipoprotein (HDL) increased by the administration of a single dose of streptozotocin. Thus, EESS could be a promising herbal medicine in the treatment of diabetes and hyperlipidemia.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67741535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Protective Effect of Combined Metoprolol and Atractylenolide I in Rats with Acute Myocardial Infarction via Modulation of the SIRT3/β-CATENIN/PPAR-γ Signaling Pathway 美托洛尔联合苍术内酯I通过调节SIRT3/β-CATENIN/PPAR-γ信号通路对急性心肌梗死大鼠的保护作用

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e21639

Weijian Zhou, Jing Liu, Zhongli Sun, Yongpeng Dong, Meiming Zhu, Li Li

引用次数: 0

Applicability of an HPLC method for analysis of alcoholic and glycolic Brazilian green-propolis extracts 高效液相色谱法分析巴西绿蜂胶醇和乙醇提取物的适用性

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e21972

C. F. Vecchi, R. Santos, M. Bruschi

引用次数: 1

Encapsulation of benznidazole in nanostructured lipid carriers and increased trypanocidal activity in a resistant Trypanosoma cruzi strain 纳米结构脂质载体包封苯并硝唑增强抗克氏锥虫的杀虫活性

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e22111

Flávia Lidiane Oliveira da Silva, M. B. Marques, M. Yoshida, W. Mussel, J. Silveira, P. R. Barroso, K. C. Kato, H. R. Martins, Guilherme Carneiro

引用次数: 2

Propyl (E)-3-(furan-2-yl) Acrylate: a synthetic antifungal potential with a regulatory effect on the biosynthesis of ergosterol in Candida Albicans 丙基(E)-3-(呋喃-2-基)丙烯酸酯:对白色念珠菌麦角甾醇的生物合成具有调节作用的合成抗真菌潜力

IF 1.3 4区医学

Brazilian Journal of Pharmaceutical Sciences Pub Date : 2023-05-15 DOI: 10.1590/s2175-97902023e22045

Paulo César Trindade da Costa, Thales Luciano Bezerra Santos, Jaqueline Ferreira Ramos, J. A. M. Santos, F. Medeiros, J. Freitas, W. Oliveira

{"title":"Propyl (E)-3-(furan-2-yl) Acrylate: a synthetic antifungal potential with a regulatory effect on the biosynthesis of ergosterol in Candida Albicans","authors":"Paulo César Trindade da Costa, Thales Luciano Bezerra Santos, Jaqueline Ferreira Ramos, J. A. M. Santos, F. Medeiros, J. Freitas, W. Oliveira","doi":"10.1590/s2175-97902023e22045","DOIUrl":"https://doi.org/10.1590/s2175-97902023e22045","url":null,"abstract":"The genus Candida represents the main cause of infections of fungal origin. Some species stand out as disease promoters in humans, such as C. albicans , C. glabrata , C. parapsilosis, and C. tropicalis . This study evaluated the antifungal effects of propyl (E) -3- (furan-2-yl) acrylate. The minimum inhibitory concentration of the synthetic compound, amphotericin B and fluconazole alone against four species of Candida ranged from 64 to 512 μg/mL, 1 to 2 μg/mL, and 32 to 256 μg/mL, respectively. The synergistic effect of the test substance was observed when associated with fluconazole against C. glabrata , there was no antagonism between the substances against any of the tested strains. The potential drug promoted morphological changes in C. albicans , decreasing the amount of resistance, virulence, and reproduction structures, such as the formation of pseudohyphae, blastoconidia, and chlamydospores, ensuring the antifungal potential of this substance. It was also possible to identify the fungicidal profile of the test substance through the study of the growth kinetics of C. albicans . Finally, it was observed that the test compound inhibited the ergosterol biosynthesis by yeast.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":1.3,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67741970","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0