Anticandida and antibiofilm activities of extract from Schinopsis brasiliensis Engl. against Candida spp

Abstract The pathogenic nature of infections caused by Candida spp. underscores the necessity for novel therapeutic agents. Extracts of Schinopsis brasilienses Engl are / a promising source of agents with antifungal effects. This study aimed to assess the antifungal potential of the leaf extract of S. brasilienses. The antifungal activity was evaluated by determining the minimum inhibitory concentrations and fungicide concentrations (MIC and MFC). The antibiofilm potential was assessed by counting colony-forming units/mL. The study examined the inhibition kinetics of fungal growth and potential synergism between gallic acid or the extract and nystatin using the Checkerboard method. Cytotoxicity was evaluated through the MTT assay. The extract exhibited antifungal effect against all tested strains, with MIC and MFC ranging from 31.25-250 μg/mL. Gallic acid, the main isolated compound, displayed a MIC of 2000 μg/mL. The extract of S. brasilienses at 31.25 μg/mL inhibited the formation of biofilm by C. albicans and significantly reduced the mass of mature biofilm after 24 and 48 h (p < 0. 05). At a concentration of 125 μg/mL, the extract demonstrated significant inhibition of fungal growth after 6 hours. The combination of gallic acid or extract with nystatin did not exhibit synergistic or antagonistic effect. Furthermore, the extract did not induce cytotoxicity to a human cell line. The extract of S. brasiliensis demonstrates antifungal activity against Candida, generally exhibiting fungicidal action and capacity to inhibit biofilm formation as well as reduce mature biofilms. Additionally, the extract showed low cytotoxicity to human cells.

Oral Medicine and Pharmacology Teleconsulting Sessions of the Telehealth Program in one Southeastern State of Brazil

ABSTRACT Objective: To evaluate questions concerning oral medicineand pharmacology-related specialties of asynchronous dental teleconsulting sessions of the Telehealth Brazil Networks Program. Material and Methods: Data were collected from secondary databases of asynchronous dental teleconsulting sessions of the telehealth centers of Minas Gerais from July 2015 to July 2017. The variables for dental underlying fields and the types of questions were evaluated. Descriptive analysis was performed with the SPSS v.22.0 program. Results: 3,920 teleconsulting sessions were referred to the telehealth centers of Minas Gerais during the study period. Regarding oral medicine-related questions (n=745), most (n=469; 62.95%) addressed diagnosis, whereas the underlying field questions mostly regarded fungal, viral, and bacterial infections (17.3%), biopsies (16.4%), developmental defects and dental abnormalities (9.9%), and soft tissue tumors (9.4%). Pharmacology-related questions (n=738) mostly addressed general approaches (n=672; 91.06%), and the most common questions were about underlying fields' prescriptions (44.7%), anesthetics (17.6%), adverse effects of medications and anesthetics (10.2%), and selection of anesthetics for patients with systemic conditions (9.8%). Conclusion: Most teleconsulting sessions regarded conditions or procedures common in primary health care and essential for diagnosis and treatment planning at all care levels, which suggests a need for more academic learning processes for healthcare professionals, especially in dentistry primary fields.

Network pharmacology and molecular docking reveal the mechanism of resveratrol in oral squamous cell carcinoma treatment / 口腔疾病防治

Objective@#To explore the molecular mechanism of resveratrol (RES) in the treatment of oral squamous cell carcinoma (OSCC) through the use of biological information methods such as network pharmacology and molecular docking and to provide a theoretical reference for the clinical application of RES in the treatment of OSCC.@*Methods@#The Swiss Target Prediction(http://www.swisstargetprediction.ch), SEA (http://sea.bkslab.org)database, and Pharm mapper database(http://lilab-ecust.cn) were used to retrieve RES-related targets, and the DISGENET (www.disgenet.org), OMIM (https://omim.org) and GeneCards (https://www.genecards.org) databases were used to screen OSCC disease targets. The intersection of drugs and disease targets was determined, and Cytoscape 3.7.2 software was used to construct a "drug-diseasetarget pathway" network. The Search Tool for the Retrieval of Interacting Genes/Proteins (STRING) database was used to construct a target protein interaction network, and the DAVID database was used for enrichment analysis of key proteins. Finally, molecular docking validation of key proteins was performed using AutoDock and PyMOL. The enrichment analysis and molecular docking results were integrated to predict the possible molecular mechanisms of RES treatment in OSCC; western blot was used to determine the effect of resveratrol at different concentrations (50, 100) μmol/L on the expression of Src tyrosine kinase (SRC), epidermal growth factor receptor (EGFR), estrogen receptor gene 1 (ESR1), and phosphatidylinositol 3 kinase/protein kinase B (PI3K/AKT) signaling pathway proteins in OSCC HSC-3 cells.@*Results@#A total of 243 targets of RES drugs and 6 094 targets of OSCC were identified. A total of 116 potential common targets were obtained by intersecting drugs with disease targets. These potential targets mainly participate in biological processes such as in vivo protein self-phosphorylation, peptide tyrosine phosphorylation, transmembrane receptor protein tyrosine kinase signaling pathway, and positive regulation of RNA polymerase Ⅱ promoter transcription, and they interfere with the PI3K/AKT signaling pathway to exert anti-OSCC effects. The docking results of resveratrol with OSCC molecules indicated that key targets, such as EGFR, ESR1, and SRC, have good binding activity. The results of cell-based experiments showed that resveratrol inhibited the protein expression of SRC, EGFR, ESR1, p-PI3K, and p-AKT in HSC-3 cells in a dose-dependent manner.@*Conclusion@#RES can inhibit the expression of its targets EGFR, ESR1, SRC, p-PI3K, and p-AKT in OSCC cells.

Caries prevention mechanism of the Xinjiang Mori Cortex based on network pharmacology and its effect on the main cariogenic bacteria / 口腔疾病防治

Objective@#To investigate the potential caries prevention mechanism of the Xinjiang Mori cortex and to analyze its effect on the main cariogenic bacteria.@*Methods@#The active components of the Xinjiang Mori cortex and the main targets were predicted and screened using the TCMSP database. The GeneCards, DisGENET and TTD databases were used to obtain caries-related targets. The common targets were derived, and core genes were screened. The enrichment analysis was performed using the DAVID data platform. Molecular docking was performed using AutoDock software. In in vitro antibacterial experiments, first, the 50% minimum inhibitory concentration (MIC50) and the minimum bactericidal concentration (MBC) of the Xinjiang Mori Cortex extract against Streptococcus mutans, Streptococcus sanguis and Actinomyces viscosus were determined and the growth curves were measured. The effects of the Xinjiang Mori Cortex extract on acid production, polysaccharide production and adhesion ability of Streptococcus mutans, Streptococcus sanguis and Actinomyces viscosus in the planktonic state were determined. The 50% minimum biofilm inhibition concentration (MBIC50) and 50% minimum biofilm reduction concentration (MBRC50) were determined by crystal violet staining, and biofilm morphology was visualized using scanning electron microscopy (SEM).@*Results@#The main active components of the Xinjiang Mori cortex included quercetin, kaempferol, and β-sitosterol. Tumor necrosis factor (TNF), interleukin-6 (IL-6), and interleukin-1beta (IL-1β) could be the most important targets of the Xinjiang Mori cortex for the prevention of dental caries. The enrichment analysis results showed that Mori cortex extract may have effects on the AGE-RAGE signaling pathway, IL-17 signaling pathway, and TNF signaling pathway. The antibacterial experiment results showed that the MIC50 values of Xinjiang Mori Cortex extract against Streptococcus mutans, Streptococcus sanguis and Actinomyces viscosus were 0.5, 0.5 and 0.25 mg/mL, respectively, and the MBCs were 4.0, 2.0 and 1.0 mg/mL, respectively. The inhibitory effect of Xinjiang Mori Cortex extract on the acid production, polysaccharide production and adhesion ability of three major cariogenic bacteria in the planktonic state was stronger than that of the control group, and the differences were statistically significant (P<0.05). The MBIC50 was 1.0, 1.0, and 0.5 mg/mL, and the MBRC50 was 4.0, 4.0, and 2.0 mg/mL. SEM observation showed that the amount of biofilm formation decreased with the drug concentration compared with the control group.@*Conclusion@#Xinjiang Mori cortex extract can prevent caries through quercetin, kaempferol, and β-sitosterol active ingredients, TNF、IL-6、IL-1β key targets and multiple pathways and inhibit the growth, acid production, polysaccharide production, and adhesion ability of three major cariogenic bacteria in the planktonic state and has some inhibitory effect on corticogenic biofilm formation.

Mechanism of Tumor T Cell Exhaustion from Perspective of ''Sanjiao-Yingwei'' Qi Transformation Malfunction / 中国实验方剂学杂志

In order to promote the innovative application of Sanjiao theory and Yingwei theory， this paper tries to apply the ''Sanjiao-Yingwei'' Qi transformation theory to the treatment of tumor diseases， integrating it with T cell exhaustion mechanism to elaborate on its scientific connotation and using network pharmacology and bioinformatics to elucidate the correlation between the anti-tumor mechanism of ''Sanjiao-Yingwei'' Qi transformation and T cell exhaustion. The ''Sanjiao-Yingwei'' Qi transformation function is closely related to the immunometabolic ability of the human body， and the ''Sanjiao-Yingwei'' Qi transformation system constitutes the immunometabolic exchange system within and outside the cellular environment. Cancer toxicity is generated by the fuzzy Sanjiao Qi， and the long-term fuzzy Sanjiao Qi is the primary factor leading to T cell exhaustion， which is related to the long-term activation of T cell receptors by the high tumor antigen load in the tumor microenvironment. Qi transformation malfunction of the Sanjiao produces phlegm and collects stasis， which contributes to T cell exhaustion and is correlated with nutrient deprivation， lipid accumulation， and high lactate levels in the immunosuppressed tumor microenvironment， as well as with the release of transforming growth factor-β and upregulated expression of programmed death receptor-1 by tumor-associated fibroblasts and platelets in the tumor microenvironment. Ying and Wei damage due to Sanjiao Qi transformation malfunction is similar to the abnormal manifestations such as progressive loss of exhausted T cell effector function and disturbance of cellular energy metabolism. Guizhi decoction， Shengming decoction， and Wendan decoction can correct T cell exhaustion and exert anti-tumor effects through multi-target and multi-pathways by regulating ''Sanjiao-Yingwei'' Qi transformation， and hypoxia inducible factor-1α （HIF-1α） may be one of the main pathways to correct T cell exhaustion. It was found that HIF-1α may be one of the important prognostic indicators in common tumors by bioinformatics. The use of the ''Sanjiao-Yingwei'' Qi transformation method may play an important part in improving the prognosis of tumor patients in clinical practice.

Mechanism of Astragaloside Ⅳ on db/db Mice with Type 2 Diabetes Mellitus and Non-alcoholic Fatty Liver Disease Based on AMPK Signaling Pathway / 中国实验方剂学杂志

ObjectiveTo study the mechanism of astragaloside Ⅳ （AS Ⅳ） on db/db mice with type 2 diabetes mellitus （T2DM） and non-alcoholic fatty liver disease （NAFLD） based on network pharmacology and experimental validation. MethodA total of 24 db/db mice were randomly divided into four groups： model group， metformin group， and low-dose and high-dose AS Ⅳ groups. Six C57 mice were used as the blank group. The low-dose and high-dose AS Ⅳ groups were given AS Ⅳ of 0.015 and 0.030 g·kg-1 by gavage， and the metformin group was given 0.067 g·kg-1 by gavage. The blank and model groups were given equal volumes of distilled water by gavage. After intragastric administration， fasting blood glucose （FBG） was detected， and an oral glucose tolerance test was performed. Serum lipid level and liver histopathology were detected. The target and enrichment pathway of AS Ⅳ for treating T2DM and NAFLD were predicted by network pharmacology， and the main enrichment pathway was verified by molecular biology techniques. The protein expressions of AMPK， p-AMPK， sterol regulatory element-binding protein-1 （SREBP-1）， and fatty acid synthetase （FAS） in liver tissue were detected by Western blot. ResultCompared with the blank group， the levels of body mass， liver weight coefficient， fasting blood glucose， serum total cholesterol， triglyceride， and low-density lipoprotein cholesterol in mice treated with AS Ⅳ were decreased （P<0.05， P<0.01）. The pathology of liver tissue showed significant improvement in lipid accumulation， and imaging results showed that the degree of fatty liver was reduced after AS Ⅳ therapy. Network pharmacological prediction results showed that vascular endothelial growth factor α （VEGFA）， galactoagglutinin 3 （LGALS3）， serine/threonine kinase B2 （Akt2）， RHO-associated coiled-coil protein kinase 1 （ROCK1）， serine/threonine kinase B1 （Akt1）， signaling and transcriptional activator protein （STAT3）， and messtimal epidermal transformation factor （MET） were key targets in "drug-disease" network. The results from the Kyoto encyclopedia of genes and genomes （KEGG） enrichment showed that the AMP-dependent protein kinase （AMPK） signaling pathway was strongly associated with T2DM and NAFLD. Western blot results showed that compared with the blank group， the expression levels of p-AMPK/AMPK in the model group were significantly down-regulated， while those of SREBP-1 and FAS proteins were significantly up-regulated （P<0.01）. Compared with the model group， the expression levels of p-AMPK/AMPK in the metformin group and high-dose AS Ⅳ group were significantly up-regulated， while those of SREBP-1 and FAS proteins were significantly down-regulated （P<0.05， P<0.01）. ConclusionAS Ⅳ regulates the expression of lipid proteins by activating the AMPK signaling pathway， thereby improving lipid metabolism.

Determination and Mechanism Prediction of Potential Active Ingredients in Erdongtang Based on UHPLC-QqQ-MS and Network Pharmacology / 中国实验方剂学杂志

ObjectiveTo establish an ultra-high performance liquid chromatography-tandem triple quadrupole mass spectrometry（UHPLC-QqQ-MS） for determination of the active ingredients in Erdongtang， and to predict the targets and pathways of anti-insulin resistance action of this formula. MethodThe analysis was performed on an ACQUITY UPLC BEH C18 column（2.1 mm×100 mm， 1.7 μm） with the mobile phase of 0.1% formic acid aqueous solution（A）-acetonitrile（B） for gradient elution（0-3 min， 90%-87%A； 3-6 min， 87%-86%A； 6-9 min， 86%-83%A； 9-11 min， 83%-75%A； 11-18 min， 75%-70%A； 18-19 min， 70%-52%A； 19-22 min， 52%A； 22-25 min， 52%-5%A； 25-27 min， 5%-90%A； 27-30 min， 90%A）. The contents of active ingredients in Erdongtang was detected by electrospray ionization（ESI） and multiple reaction monitoring（MRM） mode under positive and negative ion modes. On this basis， network pharmacology was applied to predict the targets and pathways of Erdongtang exerting anti-insulin resistance effect. ResultThe 20 active ingredients in Erdongtang showed good linear relationships within a certain mass concentration range， and the precision， stability， repeatability and recovery rate were good. The results of determination showed that the ingredients with high content in 15 batches of samples were baicalein（1 259.39-1 635.78 mg·L-1）， baicalin（1 078.37-1 411.52 mg·L-1）， the ingredients with medium content were mangiferin（148.59-217.04 mg·L-1）， timosaponin BⅡ（245.10-604.89 mg·L-1）， quercetin-3-O-glucuronide（89.30-423.26 mg·L-1）， rutin（46.91-1 553.61 mg·L-1）， glycyrrhizic acid（55.97-391.47 mg·L-1）， neomangiferin（37.45-127.03 mg·L-1）， nuciferine（0.89-63.48 mg·L-1）， hyperoside（6.96-136.78 mg·L-1）， liquiritin（30.89-122.78 mg·L-1）， liquiritigenin（26.64-110.67 mg·L-1）， protodioscin（58.57-284.26 mg·L-1）， the ingredients with low content were wogonin（7.16-20.74 mg·L-1）， pseudoprotodioscin（5.49-22.96 mg·L-1）， ginsenoside Rb1（7.31-23.87 mg·L-1）， ginsenoside Rg1（10.78-28.33 mg·L-1）， ginsenoside Re（7.78-24.76 mg·L-1）， ophiopogonin D（2.08-4.29 mg·L-1）， methylophiopogonanone A（0.74-1.67 mg·L-1）. The results of network pharmacology indicated that the mechanism of anti-insulin resistance exerted by Erdongtang might be related to the phosphatidylinositol 3-kinase/protein kinase B（PI3K/Akt） signaling pathway. ConclusionThe established UHPLC-QqQ-MS has the advantages of simple sample processing， strong exclusivity and high sensitivity， and can simultaneously determine the contents of the main ingredients from seven herbs in Erdongtang， which can lay the foundation for the development of Erdongtang compound preparations. The results of the network pharmacology can provide a reference for the mechanism study of Erdongtang in the treatment of type 2 diabetes mellitus.

Mechanism of Qizhenziyin mixture in the treatment of hypogonadism based on network pharmacology analysis and molecular docking / 药学实践杂志

Objective To investigate the mechanism of Qizhenziyin mixture in the treatment of hypogonadism by using the network pharmacology approach. Methods The active components of Qizhenziyin mixture were obtained by searching TCMSP ，TCMID and HIT databases.The related targets of candidate compounds were obtained by searching STITCH databases. The potential targets of Qizhenziyin mixture in the treatment of hypogonadism were obtained by mapping the disease genes of hypogonadism with Genecards and DisGeNet databases. The protein interaction platform database (STRING) was used to construct the interaction relationship between action targets. The target protein interaction （PPI） network was constructed by introducing Cytoscape software. The mechanism of Qizhenziyin mixture in the treatment of hypogonadism was explained through the enrichment analysis of GO, KEGG and molecular docking technology. Results A total of 148 drug-disease chemical compounds, 96 drug-disease intersection targets, 1085 disease targets were obtained；the components for treating diseases are: quercetin，kaempferol, luteolin, etc; enrichment analysis of GO revealed 1792 biological processes （BP）, 31 cellular components (CC) and 79 molecular functions (MF)；the results of KEGG pathway enrichment analysis indicated such as FOXO signaling pathway, prostate cancer, AGE-RAGE signaling pathway in diabetic complications, HIF-1 signaling pathway, etc.The results of molecular docking showed that kaempferol and LEP had the best and stable binding energy. Conclusion The active components of Qizhenziyin mixture may play a role of the treatment of hypogonadism by improving insulin resistance and the expression of testosterone synthetase of Leydig cells.

Analysis of Antidepressant Quality Markers of Bupleuri Radix Before and After Vinegar-processing Based on UPLC-Q-TOF-MS and Network Pharmacology / 中国实验方剂学杂志

ObjectiveTo analyze the antidepressant quality markers（Q-Marker） of Bupleuri Radix（BP） before and after vinegar-processing by ultra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry（UPLC-Q-TOF-MS）， multivariate statistical analysis and network pharmacology. MethodUPLC-Q-TOF-MS was used to analyze the chemical basis of raw and vinegar-processed products of BP， and principal component analysis（PCA） orthogonal partial least squares-discriminant analysis（OPLS-DA） were used to identify the differential components in BP that changed significantly before and after vinegar-processing， which were regarded as candidate quality markers（Q-Marker）. Then the disease-drug-component-target network related to antidepressant effect of BP was constructed by network pharmacology， and the antidepressant Q-Marker of raw and vinegar-processed products of BP was determined. Rats were randomly divided into blank group， model group， fluoxetine group（2.67 mg·kg-1） and total saponin group（0.72 mg·kg-1）， except the blank group， rats in the other groups were subjected to chronic unpredictable mild stress（CUMS）. Three weeks after the start of modeling， rats in each administration group were given the corresponding dose of drugs once a day for 4 weeks， and rats in the blank and model groups were given normal saline with dose of 10 mL·kg-1. At 1 day before modeling， 21 days and 28 days after administration， body mass weighing， sucrose preference test and open field test were performed on each group . After 28 days of administration， real-time fluorescence quantitative polymerase chain reaction（Real-time PCR） was used to detect the mRNA expression levels of phosphatidylinositol 3-kinase（PI3K）， protein kinase B（Akt）， mammalian target of rapamycin（mTOR）， glycogen synthase kinase-3β（GSK-3β）， forkhead box transcription factor O3a（FoxO3a） and β-catenin in hippocampal tissues of rats in each group， while protein expression levels of PI3K， Akt， mTOR and FoxO3a in hippocampal tissues of rats in each group were detected by Western blot. ResultThere were 19 components in BP showed significant changes before and after vinegar-processing， and 9 components such as saikosaponin A， saikosaponin B1， saikosaponin B2， saikosaponin C and saikosaponin D were identified as potential Q-Marker through S-plot differential marker screening. Combined with the disease-drug-component-target network， saikosaponin A， saikosaponin B1， saikosaponin B2 and saikosaponin D were identified as antidepressant Q-Marker of raw and vinegar-processed products of BP. According to the results of pharmacodynamic tests， after 28 d of administration， compared with the blank group， the body mass， sucrose preference index and open field total score of rats in model group， fluoxetine group and total saponin group decreased significantly（P<0.01）. Compared with the model group， the body mass， sucrose preference index and open field total score in total saponin group increased significantly（P<0.01）. Compared with the blank group， mRNA expression levels of PI3K， Akt， mTOR and β-catenin in hippocampus of rats in the model group decreased significantly（P<0.05）， while mRNA expression levels of GSK-3β and FoxO3a increased significantly（P<0.05）. Compared with the model group， mRNA expression levels of PI3K， Akt， mTOR and β-catenin in hippocampus of rats in the total saponin group were increased significantly（P<0.05）， while mRNA expression levels of GSK-3β and FoxO3a decreased significantly（P<0.05）. Compared with the blank group， the protein expression levels of Akt and mTOR in hippocampus of the model group decreased significantly（P<0.01）， while the protein expression levels of PI3K and FoxO3a increased significantly（P<0.01）. Compared with the model group， the expression level of Akt in hippocampus of the total saponin group increased significantly（P<0.01）， the mTOR expression level was increased but not statistically significant， while the protein expression levels of PI3K and FoxO3a decreased significantly（P<0.01）. ConclusionThe chemical constituents of BP changed greatly after vinegar-processing， and the antidepressant Q-Marker of raw and vinegar-processed products of BP was determined by chemical basis， pharmacodynamics， network pharmacology and signaling pathway， which provided a reference for further research on quality control， pharmacodynamic substance basis and processing mechanism of BP.

Network Pharmacology in Research on Efficacy of Traditional Chinese Medicine and Compound Prescriptions / 中国实验方剂学杂志

The efficacy of traditional Chinese medicine （TCM） and compound prescriptions is confirmed based on practical experience. It is a highly generalized expression of the clinical characteristics and scope of prescriptions and a unique expression of the medical effects of TCM. Network pharmacology， as a cross-disciplinary field based on the theory of systems biology and multi-level analysis of biological systems， has become a common virtual screening tool in TCM research and gradually developed with the progress in big data and artificial intelligence. In the context of modern medicine， the efficacy of TCM compound prescriptions has a vague concept and lacks scientific evidence. Elucidating the connotation of TCM efficacy and guiding TCM theoretical research has become one of the hotspots and difficulties in TCM research. This article explores the feasibility of using network pharmacology for the research on the efficacy of TCM compound prescriptions and investigates whether the research results can represent part of the efficacy of prescriptions. Furthermore， the research platforms and algorithms in this field are summarized. The research ideas and existing problems in this field are proposed from the aspects of efficacy concept embodiment， target screening， result verification， efficacy network building， and homogenization avoiding of network pharmacology research results. Finally， the future development directions are prospected. This article is expected to provide a reference for exploring the modern biological basis of the efficacy of TCM and compound prescriptions and for the clinical application and theoretical research of TCM.

Propriedades Químicas e Farmacológicas do Gênero Copaifera no Tratamento de Lesões/feridas: Revisão Integrativa / Chemical and Pharmacological Properties of the Genus Copaifera in the Treatment of Injuries/wounds: Integrative Review / Propiedades Químicas y Farmacológicas del Género Copaifera en el Tratamiento de Lesiones/heridas: Revisión Integradora

Objetivo:Identificar propriedades químicas e farmacológicas do gênero Copaifera no tratamento de lesões e feridas. Método: Revisão integrativa da literatura realizada nas bases de dados LILACS, MEDLINE, PubMed, Taylor & Francis e Scopus, em janeiro de 2022, por meio da estratégia de busca: "Chemical Properties" AND "Copaifera" AND "Wounds and Injuries" e "Pharmacology" AND "Copaifera" AND "Wounds and Injuries". Foram incluídos artigos originais, de texto completo, identificados de acordo nível de evidência, redigidos em português, inglês ou espanhol. Resultados: Na busca primária foram encontrados 261 artigos. Após a seleção sistematizada, 12 estudos foram selecionados para análise qualitativa. Espécies do gênero Copaifera apresentam propriedades farmacológicas favoráveis ao tratamento de feridas: controle da dor inflamatória, diminuição da reação inflamatória, reepitelização e reparo tecidual, angiogênese, retração da ferida e remodelagem de cicatrizes. Dentre as propriedades químicas associadas ao tratamento de lesões, destacam-se presença de compostos bioativos: diterpenos, 3-hidroxi-copálico, sesquiterpenos, éster kolavic-15-metílico. Entre os diterpenos testados, o caurenoico e os ácidos copálicos mostraram atividades hemolíticas significativas. Apenas o ácido copálico e o ácido hardwíckiico inibiram a produção de óxido nítrico em macrófagos ativados por lipopolissacarídeos. Conclusão: As plantas do gênero Copaifera apresentam propriedades químicas e farmacológicas favoráveis ao tratamento de lesões e feridas

Objective:To identify chemical and pharmacological properties of Copaifera in the treatment of injuries and wounds. Method: Integrative literature review conducted in the LILACS, MEDLINE, PubMed, Taylor & Francis and Scopus databases in January 2022, using the search strategy: "Chemical Properties" AND "Copaifera" AND "Wounds and Injuries" and "Pharmacology" AND "Copaifera" AND "Wounds and Injuries." Original articles, full text, identified according to level of evidence, written in Portuguese, English or Spanish, were included. Results: In the primary search 261 articles were found. After systematized selection, 12 studies were selected for qualitative analysis. Species of the genus Copaifera have pharmacological properties favorable for wound treatment: control of inflammatory pain, reduction of inflammatory reaction, tissue reepithelialization and repair, angiogenesis, wound retraction and scar remodeling. Among the chemical properties associated with the treatment of injuries, the presence of bioactive compounds stand out: diterpenes, 3-hydroxy-copalic, sesquiterpenes, kolavic-15-methyl ester. Among the tested diterpenes, kaurenoic and copalic acids showed significant hemolytic activities. Only copalic acid and hardwickiic acid inhibited nitric oxide production in lipopolysaccharide-activated macrophages. Conclusion: Plants of the genus Copaifera have chemical and pharmacological properties favorable for the treatment of injuries and wounds.

Objetivo:Identificar las propiedades químicas y farmacológicas del género Copaifera en el tratamiento de lesiones y heridas. Método: Revisión integradora de la literatura realizada en las bases de datos LILACS, MEDLINE, PubMed, Taylor & Francis y Scopus, en enero de 2022, mediante la estrategia de búsqueda: "Chemical Properties" AND "Copaifera" AND "Wounds and Injuries" e "Pharmacology" AND "Copaifera" AND "Wounds and Injuries". Se incluyeron artículos originales, a texto completo, identificados según el nivel de evidencia, escritos en portugués, inglés o español. Resultados: En la búsqueda primaria se encontraron 261 artículos. Tras una selección sistematizada, se seleccionaron 12 estudios para el análisis cualitativo. Las especies del género Copaifera presentan propiedades farmacológicas favorables para el tratamiento de las enfermedades: control del dolor inflamatorio, disminución de la reacción inflamatoria, reepitelización y reparación tecidual, angiogénesis, retracción de la piel y remodelación de las cicatrices. Entre las propiedades químicas asociadas al tratamiento de las lesiones, destaca la presencia de compuestos bioactivos: diterpenos, 3-hidroxicopálico, sesquiterpenos, éster kolavico-15-metilo. Entre los diterpenos probados, los ácidos kaurenoico y copálico mostraron actividades hemolíticas significativas. Sólo el ácido copálico y el ácido hardwickiico inhibieron la producción de óxido nítrico en macrófagos activados por lipopolisacáridos. Conclusión: Las plantas del género Copaifera presentan propiedades químicas y farmacológicas favorables para el tratamiento de lesiones y heridas.

Estilos y enfoques de aprendizaje en estudiantes de Estomatología y relación con el rendimiento académico en Farmacología

Fundamento: los estilos y enfoques de aprendizaje permiten conocer cómo el estudiante enfrenta este proceso y el modo en que procesa la información que debe ser asimilada. Objetivo: identificar los estilos y enfoques de aprendizaje que utilizan estudiantes de Estomatología y su relación con el rendimiento académico en la disciplina Farmacología. Métodos: estudio descriptivo-transversal, con enfoque cualicuantitativo, realizado de noviembre 2021 a enero 2022. La muestra, no probabilística, fue de 28 estudiantes (90,3 %) de segundo año de la carrera de Estomatología impartida en la Facultad de Estomatología de La Habana. A los participantes se les aplicaron dos instrumentos: cuestionario Honey y Alonso sobre estilos de aprendizaje y cuestionario Enfoques e Inventario de Habilidades de Estudio de los Estudiantes. Las dimensiones del rendimiento académico fueron excelente, bueno, y regular. Resultados: predominó la preferencia muy alta/alta en el estilo teórico (67,86 %) y la preferencia moderada en el reflexivo (67,86 %). Se encontró relación significativa entre la cantidad de estilos de aprendizaje de preferencia muy alta/alta y el rendimiento académico (p=0,044), y entre el estilo reflexivo y el rendimiento académico (p=0,024). También, se encontró relación significativa entre el rendimiento académico y el enfoque de aprendizaje estratégico (p=0,008) y la preferencia por la transmisión de la información (p=0,028). Conclusiones: en los estudiantes existen estilos y enfoques de aprendizaje que se relacionan con el rendimiento académico en Farmacología; se muestran aspectos que se deben considerar para el mejoramiento del proceso docente de esta disciplina en Estomatología.

Foundation: the learning styles and approaches allow us to know how the student faces this process and the way in which they process the information that must be assimilated. Objective: to identify the learning styles and approaches used by Dentistry students and their relationship with academic performance in the Pharmacology discipline. Methods: a descriptive-cross-sectional study, with a qualitative-quantitative approach, carried out from November 2021 to January 2022. The non-probabilistic sample consisted of 28 students (90.3%) in the second year of the Dentistry course taught at the Havana Dentistry Faculty. Two instruments were applied to the participants: the Honey and Alonso questionnaire on learning styles and the Approaches and Inventory of Student Study Skills questionnaire. The dimensions of academic performance were excellent, good, and regular. Results: the very high/high preference predominated in the theoretical style (67.86%) and the moderate preference in the reflective style (67.86%). A significant relationship was found between the number of very high/high preference learning styles and academic performance (p=0.044), and between the reflective style and academic performance (p=0.024). Also, a significant relationship was found between academic performance and the strategic learning approach (p=0.008) and the preference for the transmission of information (p=0.028). Conclusions: there are learning styles and approaches among students that are related to academic performance in Pharmacology; Aspects that should be considered for the improvement of the teaching process of this discipline in Dentistry are shown.

Impacto do uso sistêmico de estatinas e de bisfosfonatos nos tecidos periodontais: revisão narrativa / Impact of the systemic use of statins and bisphosphonates in the periodontal tissues: narrative review

Introdução: A literatura tem apontado uma possível relação entre diversas condições sistêmicas e as doenças periodontais. Dentro das doenças sistêmicas que podem gerar o uso crônico de medicamentos, com potencial associação com as doenças periodontais, destacam-se a hipercolesterolemia e o uso de estatinas; e as doenças do metabolismo ósseo e o uso de bisfosfonatos. Objetivo: Dessa maneira, o presente estudo objetivou revisar a literatura sobre o efeito das estatinas e dos bisfosfonatos nos parâmetros clínicos e radiográficos periodontais de indivíduos adultos. Resultados: Apenas estudos observacionais em humanos foram incluídos. Um estudo mostrou que, em pacientes que apresentam doença periodontal e usam estatina, houve 37% menos bolsas periodontais (profundidade de sondagem ≥4mm) quando comparadas aos que não utilizam a medicação, além de apresentarem menor índice de carga inflamatória e menor perda de inserção clínica. Em relação aos bisfosfonatos em indivíduos com doenças que envolvem o metabolismo ósseo, sugere-se que a utilização do fármaco tem obtido resultados positivos nos parâmetros periodontais, como menores sinais clínicos de inflamação gengival, menor profundidade de sondagem, menor perda de inserção clínica e maior nível de osso alveolar, quando comparados aos que nunca realizam essa terapia. Conclusão: Dessa forma, as estatinas e os bisfosfonatos apresentam efeitos promissores, em pacientes sob tratamento para suas respectivas condições sistêmicas, na melhoria dos parâmetros periodontais, porém é importante salientar que são necessários mais estudos sobre o assunto para melhor entender os reais efeitos a longo prazo do uso desses fármacos.(AU)

Introduction: The literature showed a possible relationship between several systemic conditions and periodontal diseases. Within the systemic diseases that can generate the chronic use of these drugs, potentially related with periodontal diseases, it may be cited the hypercholesterolemia and the use of statins; and bone metabolism diseases and the use of bisphosphonates. Objective: In this sense, the present study aimed to review the literature about the effect of statins and bisphosphonates in the periodontal parameters of adults individuals. Results: Only observational studies in humans were included. A study showed that, in patients with periodontal disease and users of statins, there 37% fewer periodontal pockets (probing depth ≥4mm) when compared to those who do not use the medication, as well as having a lower rate of inflammatory burden and less loss of clinical insertion. Regarding the bisphosphonates in individuals diagnosed with diseases involving bone metabolism, it was suggested that the use of the drug has obtained positive results in periodontal parameters, such as a greater absence of plaque, less clinical signs of gingival inflammation, less probing depth, lower level of clinical insertion and higher level of alveolar bone when compared to those who never undergo this therapy. Conclusion: Thus, statins and bisphosphonates have promising effects in patients under treatment for their respective systemic condition in improving periodontal parameters, but it is important to emphasize that further studies on the subject are needed to better understand the long-term effects of the use of these drugs.(AU)

Análisis del programa de Farmacología Clínica en el plan de estudio E para la carrera de Medicina / Analysis of the program of Clinical Pharmacology in the E plan study for the Medicine career i: en

Introducción: En Cuba han existido varias concepciones sobre planes de estudio. La necesidad de revisar y proponer cambios que aseguren los niveles de calidad deseados en el proceso de formación integral de los futuros profesionales motivó a investigar los elementos teóricos y metodológicos que regulan y orientan el proceso de enseñanza-aprendizaje en la asignatura Farmacología Clínica. Objetivo: Analizar el programa de Farmacología Clínica del plan de estudio E para la carrera de Medicina desde un enfoque crítico y sistematizado. Métodos: Se realizó un estudio cualitativo del programa de estudio de la asignatura Farmacología Clínica según el plan E, vigente en la Universidad de Ciencias Médicas de Santiago de Cuba, durante el 2022, para lo cual se utilizaron los métodos de revisión documental, los documentos rectores del proceso docente en la educación superior y la metodología propuesta por algunos autores. Resultados: Varios temas enunciaban un número excesivo de objetivos específicos sin tener en cuenta el nivel de asimilación; la forma de organización de la enseñanza más utilizada fue la conferencia. En las evaluaciones frecuentes no se tuvo en cuenta el trabajo investigativo independiente; en tanto, la bibliografía básica correspondió a una edición del 2002. Conclusiones: El programa no requirió trasformaciones temáticas, pero desde el punto de vista didáctico deben modificarse componentes del proceso de enseñanza-aprendizaje y, además, se debe actualizar la bibliografía básica pertinente.

Introduction: In Cuba several conceptions have existed on the study plans. The necessity to revise and propose changes that assure the levels of quality wanted in the process of integral formation of the future professionals motivated to investigate the theoretical and methodological elements that regulate and guide the teaching-learning process in the Clinical Pharmacology subject. Objective: To analyze the program of Clinical Pharmacology of the E plan study for the medicine career, from a critical and systematized approach. Methods: A qualitative study of the study program in the Clinical Pharmacology subject was carried out according to the E plan, effective in the University of Medical Sciences in Santiago de Cuba, during 2022, for which the methods of documental review, the rector documents of the teaching process in higher education and the methodology proposed by some authors were used. Results: Several topics enunciated an excessive number of specific objectives without taking into account the level of assimilation; the form of organization most used in teaching was the conference. Independent investigative work was not taken into account in frequent evaluations; meanwhile, the basic bibliography corresponded to an edition from 2002. Conclusions: The program did not require of thematic transformations, but from the didactic point of view components of the teaching-learning process should be modified, besides updating the pertinent basic literature.

The potential of the antiplatelet agent ticagrelor as a new antibacterial agent

The number of deaths caused by drug-resistant bacteria is expected to increase in the future, and there is a need to develop new antimicrobial agents. Recently, the antiplatelet drug ticagrelor has been reported to have promising antibacterial properties. The purpose of this review is to analyze articles and case reports that describe the antimicrobial action of ticagrelor. Ticagrelor was found to have antibacterial reactions against Gram-positive bacteria, including drug-resistant and spore-forming bacteria, while no effect was observed against Gram-negative bacteria. In this paper we discuss a new potential antimicrobial agent, ticagrelor.

Flipped classrooms in teaching pharmacology for medical undergraduate students – A comparative study

Background: The new competency-based medical education curriculum envisages the need to adopt newer teaching-learning methods. There is a growing concern about the effective dissemination of knowledge to a large group of students through conventional didactic lectures. Flipped classroom teaching has evolved as an innovative method and is a systematic approach to improving the student learning experience. Aims and Objectives: The present study was undertaken (1) to compare the effectiveness of flipped classroom methods with that of the lecture as a teaching learning method in pharmacology for undergraduate medical students and (2) evaluate the students’ perception of the flipped method. Materials and Methods: This study was done in the Department of Pharmacology in a tertiary care teaching hospital in Kerala after ethics committee approval. Two groups of students enrolled using the convenient sampling method, received three flipped classes and three lectures on the topics after crossover. Feedback was collected using a validated structured questionnaire and a common evaluation after each topic was done with a pre-validated multiple choice questions questionnaire. Results: This study has examined the perceptions of students about flipped teaching method using various teaching materials on a Likert 5-point scale. The findings indicate that flipped classroom was a better teaching method. The mean scores of flipped classrooms were high and it was found to be significant (P < 0.05). Conclusion: The results of the study indicate that flipped classroom is more effective for students when compared to lectures. An implication of this is the possibility that it can be used as an adjunctive method in the new curriculum.

A step toward revamping MD pharmacology curriculum by National Medical Commission: An envisioned transition from bench-side training to bedside training

With a vision to meet the changing trends and recent developments in the field of pharmacology and therapeutics, the postgraduate medical education board of the national medical commission has put forth amendments to the existing guidelines for the MD pharmacology course. Major changes include introducing a district residency-based program for 3 months apart from the clinical postings and more focus is given to the areas of rational prescribing, pharmacovigilance, and ethical aspects of research. These amendments come as a new ray of hope in developing the postgraduate student as a complete professional equipped to meet the increasing standards in the workplace be it a hospital or a research arena. Including the simulation-based approaches for training as a lesson learned from the pandemic and adopting patient-oriented learning during the course are some of the key changes in the new guidelines. This review focuses on highlighting these amendments and correlating the same with the current scenario and discusses the future areas that can be improved for comprehensive development in the pharmacology curriculum.

Student’s perception on teaching and learning methods in pharmacology and changes recommended

Background: Understanding the changing trends in medical education technology helps to improve the teaching learning methods for medical graduates which can further help to improve the quality of health-care system. Apart from the conventional methods, several new methods of teaching are being introduced according to the changing medical curriculum. Most of these techniques are well accepted by the medical students. Aim and Objectives: The aim of the study was to collect feedback from the students to understand their perception on teaching and learning methods in the subject of pharmacology. Materials and Methods: This observational, cross-sectional, and questionnaire-based study was conducted in the Department of Pharmacology at Government Medical College, Thrissur, during the period 2017–2018. Pre-validated questionnaire was distributed among 2nd-year MBBS students, attending pharmacology classes and responses were collected and analyzed using a 5-point Likert scale. Results: Major responses from students perspective regarding teaching and learning methods in Pharmacology subject were that learning pharmacology is very important before going to clinics (96.5%), brief description about the clinical scenario is essential before discussing about the drugs (95.5%), knowledge of pharmacy and drug dispensing methods are necessary for patient care (94.5%). Pharmacology should be taught along with clinical subjects (93%) and also problem-based learning and prescriptions are extremely useful in clinics (90.5%). Conclusion: Regular and systematic feedback from the learners side can significantly improve the quality of medical education and health-care system. Clinically oriented teaching methods can impart more interest in studying Pharmacology.

Comparative study between academic performances of traditional versus competency-based medical education M.B.B.S. curriculum students in Pharmacology

Background: The new competency-based undergraduate curriculum (CBME) was implemented in India from the academic year 2019. However, there has been no clear-cut comparison on its effect on the academic performance of the students. Aim and Objective: This study aims to find the comparison between students of traditional and CBME curriculum in the subject of pharmacology based on their academic parameters. It also aims to establish comparison and correlation of academic performance with gender, home place area, and mode of learning used. We also aim to determine whether objective parameters like multiple choice question (MCQ) section of preliminary examination show any correlation with final university examination performance. Materials and Methods: This is a cross-sectional type of study. Seventy-seven students from traditional old curriculum and 98 students from CBME new curriculum batches participated with informed consent. The data for analysis between old and new curriculum batches were done using the mark obtained in final university examination in the subject of pharmacology. Quantitative parameters, that is, total marks overall, total theory marks, total marks in practical and oral viva combined, total marks in internal assessment and MCQ marks of preliminary examination, and qualitative variables such as gender of the student, home place area, that is, rural or urban and mode of learning used (physical or physical and digital) were obtained from the participants. IBM-SPSS version 25 software was used to perform descriptive statistics, independent t-tests, and Pearson’s correlation. Results: The results clearly demonstrate that the old curriculum batch of 2018 performed better than 2019 in overall as well as practical aspects of the subject. Pearson’s correlation between all the quantitative parameters, that is, total marks overall, total theory marks, total marks in practical and oral viva combined, total marks in internal assessment, and MCQ marks of prelims for the batch of 2019 showed positive correlation with each other. Conclusions: This study concludes that the old curriculum batch performed better than new curriculum batch in the subject of pharmacology. MCQ examination held in offline mode helps in better correlation with final university results as compared to online mode.

Validación de una estrategia didáctica para las relaciones interdisciplinarias entre Farmacología y asignaturas clínicas estomatológicas

Introducción: La validación de estrategias didácticas para favorecer las relaciones interdisciplinarias en el proceso enseñanza aprendizaje, resulta necesaria para su posterior aplicación en la práctica pedagógica y posible generalización. Objetivo: Validar una estrategia didáctica para las relaciones interdisciplinarias en el proceso enseñanza aprendizaje de las asignaturas clínicas, con la Farmacología en la carrera Estomatología. Métodos: Se realizó una investigación educativa entre enero y junio de 2022. Se asumieron métodos teóricos (analítico-sintético, inductivo-deductivo y sistematización), empíricos (consulta a expertos) y matemáticos-estadísticos (estadística descriptiva). Se seleccionó a los expertos según el nivel de competencia. Se elaboró y aplicó un cuestionario para valorar 16 aspectos de la estrategia en términos de: muy adecuado, bastante adecuado, adecuado, poco adecuado y no adecuado. Los criterios valorativos emitidos por los expertos se procesaron mediante el modelo matemático de Torgerson y se determinó el nivel de consenso de los expertos mediante el cálculo del coeficiente de concordancia de Kendall. Resultados: El coeficiente de competencia promedio de los expertos fue alto. De los 16 aspectos valorados, uno resultó "bastante adecuado" y el resto, "muy adecuado". Se estimó concordancia significativa entre los expertos consultados. Conclusiones: Los resultados de la consulta a expertos apuntan al reconocimiento del valor científico, teórico y práctico, de la estrategia didáctica diseñada para favorecer las relaciones interdisciplinarias en el proceso enseñanza aprendizaje de las asignaturas clínicas, con la Farmacología en la carrera Estomatología y le otorgan validez.

Introduction: The validation of didactic strategies to favor interdisciplinary relationships in the teaching-learning process is necessary for their subsequent application in pedagogical practice and possible generalization. Objective: To validate a didactic strategy for interdisciplinary relationships in the teaching-learning process of clinical subjects, with Pharmacology in the Stomatology career. Methods: Educational research was carried out, between January and June, 2022. Theoretical methods (analytical-synthetic, inductive-deductive and systematization), empirical (consultation to experts) and mathematical-statisticians (descriptive statistics). The experts were selected according to the level of competence. A questionnaire was developed and applied to assess 16 aspects of the strategy, in terms of: very suitable, quite suitable, suitable, not very suitable and not suitable. The evaluative criteria issued by the experts were processed using the Torgerson mathematical model and the level of consensus of the experts was determined by calculating the Kendall concordance coefficient. Results: The average competence coefficient of the experts turned out to be high. Of the 16 aspects assessed, one was "fairly adequate" and the rest, "very adequate". Significant agreement was estimated between the experts consulted Conclusions: The results of the expert consultation point to the recognition of the scientific, theoretical and practical value of the didactic strategy designed to favor interdisciplinary relationships in the teaching-learning process of clinical subjects with Pharmacology in the Stomatology career, and give validity to the same.