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A critical overview of computational approaches employed for COVID-19 drug discovery
(2021) Muratov, Eugene; Amaro, Rommie E.; Andrade, Carolina Horta; Brown, Nathan; Ekins, Sean; Isayev, Olexandr; Fourches, Denis; Kozakov, Dima; Franco, José Luis Medina; Merz, Kenneth Malcolm; Oprea, Tudor I.
COVID-19 has resulted in huge numbers of infections and deaths worldwide and brought the most severe disruptions to societies and economies since the Great Depression. Massive experimental and computational research effort to understand and characterize the disease and rapidly develop diagnostics, vaccines, and drugs has emerged in response to this devastating pandemic and more than 130 000 COVID-19-related research papers have been published in peer-reviewed journals or deposited in preprint servers. Much of the research effort has focused on the discovery of novel drug candidates or repurposing of existing drugs against COVID-19, and many such projects have been either exclusively computational or computer-aided experimental studies. Herein, we provide an expert overview of the key computational methods and their applications for the discovery of COVID-19 small-molecule therapeutics that have been reported in the research literature. We further outline that, after the first year the COVID-19 pandemic, it appears that drug repurposing has not produced rapid and global solutions. However, several known drugs have been used in the clinic to cure COVID-19 patients, and a few repurposed drugs continue to be considered in clinical trials, along with several novel clinical candidates. We posit that truly impactful computational tools must deliver actionable, experimentally testable hypotheses enabling the discovery of novel drugs and drug combinations, and that open science and rapid sharing of research results are critical to accelerate the development of novel, much needed therapeutics for COVID-19.
A diarylamine derived from anthranilic acid inhibits ZIKV replication
(2019) Silva, Suely da; Shimizu, Jacqueline Farinha; Oliveira, Débora Moraes; Assis, Leticia Ribeiro de; Oliva, Cíntia Bittar; Mottin, Melina; Sousa, Bruna Katiele de Paula; Mesquita, Nathalya Cristina de Moraes Roso; Regasini, Luis Octávio; Rahal, Paula; Andrade, Carolina Horta
Zika virus (ZIKV) is a mosquito-transmitted Flavivirus, originally identified in Uganda in 1947 and recently associated with a large outbreak in South America. Despite extensive efforts there are currently no approved antiviral compounds for treatment of ZIKV infection. Here we describe the antiviral activity of diarylamines derived from anthranilic acid (FAMs) against ZIKV. A synthetic FAM (E3) demonstrated anti-ZIKV potential by reducing viral replication up to 86%. We analyzed the possible mechanisms of action of FAM E3 by evaluating the intercalation of this compound into the viral dsRNA and its interaction with the RNA polymerase of bacteriophage SP6. However, FAM E3 did not act by these mechanisms. In silico results predicted that FAM E3 might bind to the ZIKV NS3 helicase suggesting that this protein could be one possible target of this compound. To test this, the thermal stability and the ATPase activity of the ZIKV NS3 helicase domain (NS3Hel) were investigated in vitro and we demonstrated that FAM E3 could indeed bind to and stabilize NS3Hel.
A evolução da química medicinal no Brasil: avanços nos 40 anos da Sociedade Brasileira de Química
(2017) Amaral, Antonia Tavares do; Andrade, Carolina Horta; Kummerle, Arthur Eugen; Guido, Rafael Victorio Carvalho
MEDICINAL CHEMISTRY PROGRESS IN BRAZIL: ADVANCES IN THE 40 YEARS OF THE BRAZILIAN CHEMICAL SOCIETY. Medicinal Chemistry includes the invention, discovery, design, identification, and interpretation of the molecular mechanism of action of biologically active compounds. In addition to the discovery of bioactive molecules, Medicinal Chemistry investigates drug metabolism and the relationships between chemical structure and biological activity. The advances achieved in the 20th century have significantly contributed to the better understanding of pathophysiological processes as well as the development of new, safer and more effective drugs for many diseases. In this article, we review the evolution of Medicinal Chemistry in Brazil during the last 40 years and evaluate the impact of the Brazilian contributions in the international context. The analyzed data revealed that Medicinal Chemistry research in Brazil has increased exponentially in the last two decades, the research groups became more well-distributed across the Brazilian regions and our scientific contributions have significant impact in the main journals of the field. Therefore, aiming at evolving steadily and striving for excellence in drug discovery and development, we shall focus on national and international collaborations and investment in translational research, as well.
A perspective and a new integrated computational strategy for skin sensitization assessment
(2018) Alves, Vinícius de Medeiros; Capuzzi, Stephen J.; Braga, Rodolpho de Campos; Borba, Joyce Villa Verde Bastos; Silva, Arthur de Carvalho e; Luechtefeld, Thomas; Andrade, Carolina Horta; Muratov, Eugene; Tropsha, Alexander
Traditionally, the skin sensitization potential of chemicals has been assessed using animal models. Due to growing ethical, political, and financial concerns, sustainable alternatives to animal testing need to be developed. As publicly available skin sensitization data continues to grow, computational approaches, such as alert-based systems, read-across, and QSAR models, are expected to reduce or replace animal testing for the prediction of human skin sensitization potential. Herein, we discuss current computational approaches to predicting skin sensitization and provide future perspectives of the field. As a proof-of-concept study, we have compiled the largest skin sensitization data set in the public domain and benchmarked several methods for building skin sensitization models. We propose a new comprehensive approach, which integrates multiple QSAR models developed with in vitro, in chemico, animal, and human data, and a Naive Bayes model for predicting human skin sensitization. Both the data sets and the KNIME implementation of the model allowing skin sensitization prediction for molecules of interest have been made freely available.
A structure-based approach for the discovery of inhibitors against methylcitrate synthase of Paracoccidioides lutzii
(2021) Lima, Raisa Melo; Silva, Kleber Santiago Freitas e; Silva, Lívia do Carmo; Ribeiro, Jean Francisco Rosa; Neves, Bruno Junior; Brock, Matthias; Soares, Célia Maria de Almeida; Silva, Roosevelt Alves da; Pereira, Maristela
Paracoccidioidomycosis (PCM) is a systemic mycosis, endemic in Latin America, caused by fungi of the genus Paracoccidioides. The treatment of PCM is complex, requiring a long treatment period, which often results in serious side effects. The aim of this study was to screen for inhibitors of a specific target of the fungus that is absent in humans. Methylcitrate synthase (MCS) is a unique enzyme of microorganisms and is responsible for the synthesis of methylcitrate at the beginning of the propionate degradation pathway. This pathway is essential for several microorganisms, since the accumulation of propionyl-CoA can impair virulence and prevent the development of the pathogen. We performed the modeling and molecular dynamics of the structure of Paracoccidioides lutzii MCS (PlMCS) and performed a virtual screening on 89,415 compounds against the active site of the enzyme. The compounds were selected according to the affinity and efficiency criteria of in vitro tests. Six compounds were able to inhibit the enzymatic activity of recombinant PlMCS but only the compound ZINC08964784 showed fungistatic and fungicidal activity against Paracoccidioides spp. cells. The analysis of the interaction profile of this compound with PlMCS showed its effectiveness in terms of specificity and stability when compared to the substrate (propionyl-CoA) of the enzyme. In addition, this compound did not show cytotoxicity in mammalian cells, with an excellent selectivity index. Our results suggest that the compound ZINC08964784 may become a promising alternative antifungal against Paracoccidioides spp.
Uma abordagem sobre métodos analíticos para determinação da atividade antioxidante em produtos naturais
(2011) Borges, Leonardo Luiz; Lúcio, Tathiana Carvalho; Gil, Eric de Souza; Barbosa, Eduardo Fernandes
Antioxidants have been placing a highlighted position in the pharmaceutical industry, becoming the systematic research of these compounds important, for their ability to neutralize harmful agents in biological systems such as free radicals. In this work were evaluated some methodologies to determine the antioxidant capacity of some complex systems, as plant extracts, food, wine, among others. The detection of antioxidants was based on three categories of methods: electrochemical, colorimetric (DPPH e ABTS), and biological. Besides these, other instrumental techniques were pointed out, showing the versatility of the mechanisms that can be use to unveil the concentration of these substances. The HPLC (High Performance Liquid Chromatography) is a very useful tool in the identification and quantification of these compounds and can be coupled to the DPPH method. Each analytical method cited here has advantages and limitations, and the approach presented in this work ranges within these two parameters.
Ação do óleo essencial de Syzygium aromaticum (L.) Merr. & L.M.Perry sobre as hifas de alguns fungos fitopatogênicos
(2011) Costa, A. R. T.; Amaral, M. F. Z. J.; Martins, P. M.; Paula, J. A. M.; Fiuza, Tatiana de Sousa; Tresvenzol, Leonice Manrique Faustino; Paula, José Realino de; Bara, Maria Teresa Freitas
Currently, the use of alternative methods to control diseases and pests in agriculture has been a recognized and necessary practice to minimize damages to the environment and public health. This study aimed to investigate the action of clove [Syzygium aromaticum (L.) Merr. & L.M.Perry] essential oil on the in vitro mycelial growth of the phytopathogenic fungi Rhizoctonia solani, Fusarium solani, Fusarium oxysporum and Macrophomina phaseolina. Analysis by gas chromatography-mass spectrometry allowed the identification of eugenol (83.6%), eugenyl acetate (11.6%) and caryophyllene (4.2%). Microscopic evaluation of mycelia showed several morphological changes such as presence of vacuoles, cell content disorganization, decreased cell wall clearness, intense fragmentation and lower turgescence of hyphae. Clove essential oil showed fungicidal activity at 0.15% on the growth of R. solani, F. oxysporum and F. solani, but not for M. phaseolina. These results indicate favorable perspectives for future use of clove essential oil to control these phytopathogens in agriculture.
Acetaminophen treatment evokes anticontractile effects in rat aorta by blocking L-type calcium channels
(2022) Correia, Mikaelle Costa; Santos, Eder S. A.; Neves, Bruno Junior; Rocha, Matheus Lavorenti
Background Acetaminophen (APAP) is the most widely used analgesic and antipyretic in the world. However, in high or continuous doses, it can cause serious side effects including blood pressure variability and cardiovascular injuries, which are barely explored. This study aimed to evaluate the acute effect of APAP treatment on vascular tone focused on the blocking of Ca2+ channels. Methods Rats were treated with APAP orally by gavage (500 mg/kg/single dose). After 12 h, the aorta was isolated for vascular reactivity studies in an isolated organ bath. Vascular contraction and relaxation were measured after different stimuli. Moreover, molecular docking studies were performed to evaluate the action of NAPQI (APAP metabolite) on L-type calcium channels. Results Phenylephrine-induced maximal vascular contraction was reduced in the APAP group (138.4 ± 9.2%) compared to the control group (172.2 ± 11.1%). APAP treatment significantly reduced contraction induced by Ca2+ influx stimulated with phenylephrine or KCl and reduced contraction mediated by Ca2+ released from the sarcoplasmic reticulum induced by caffeine. There was no difference in vascular relaxation induced by acetylcholine or sodium nitroprusside. Computational molecular docking demonstrated that NAPQI is capable of blocking L-type Ca2+ channels (Cav1.2), which would limit the influx of Ca2+. Conclusion These results suggest that APAP treatment causes an anticontractile effect in rat aorta, possibly by blocking the influx of Ca2+ through L-type channels (Cav1.2).
Alarms about structural alerts
(2016) Alves, Vinícius de Medeiros; Muratov, Eugene; Capuzzi, Stephen J.; Polit, Regina; Yen, Sia Low; Braga, Rodolpho de Campos; Zakharov, Alexey V.; Sedykh, Alexander; Mokshyna, Elena; Farag, Sherif; Andrade, Carolona Horta
Structural alerts are widely accepted in chemical toxicology and regulatory decision support as a simple and transparent means to flag potential chemical hazards or group compounds into categories for read-across. However, there has been a growing concern that alerts disproportionally flag chemicals as toxic, which questions their reliability as toxicity markers. Conversely, rigorously developed and properly validated statistical QSAR models can accurately and reliably predict the toxicity of a chemical; however, their use in regulatory toxicology has been hampered by a lack of transparency and interpretability. We demonstrate that contrary to the common perception of QSAR models as “black boxes” they can be used to identify statistically significant chemical substructures (QSAR-based alerts) that influence toxicity. We show through several case studies, however, that the mere presence of structural alerts in a chemical, irrespective of the derivation method (expert-based or QSAR-based), should be perceived only as hypotheses of possible toxicological effect. We propose a new approach that synergistically integrates structural alerts and rigorously validated QSAR models for a more transparent and accurate safety assessment of new chemicals.
Alterações teciduais agudas induzidas em ratos wistar por trypanosoma cruzi
(Marize Campos Valadares, 2007-06) Oliveira, Kleber Mirallia de; Souza Júnior, Nozelmar Borges de; Mata, Fabiana Ribeiro da; Sabóia-Morais, Simone Maria Teixeira; Aversi-Ferreira, Tales Alexandre; Mata, João Roberto da
The Chagas disease, described in 1909, has a behavior that partially depends on the Trypanosoma cruzi isolate. In this work, the parasitemy curve and the alterations in the tissues of the encephalus, heart, tongue, esophagus, lungs, stomach, small and large intestines, kidneys and bladder of Wistar rats infected with Trypanosoma cruzi isolated from a patient carrying the cardiac and digestive form of the disease, were analyzed. Forty rats (ten groups of four animals each) were utilized. Two groups that were inoculated at 15 days and the other two at 60 days with 10 x 103 or 10 x 104 trypomastigotes/animal, were submitted to an evaluation of parasitemy at alternate days starting from the third day after inoculation. The organs listed were processed using the routine histological technique, and then microscope slides were confectioned and stained with hematoxillin and eosin. The animals inoculated at 60 days presented peaks of parasitemy ranging from 24,710 forms/mL of blood in inoculates of 10 x 103 forms/animal to 28,240 forms/mL in inoculates of 10 x 104 forms/animal. The animals inoculated at 15 days with 10 x 103 forms, presented a peak of 116,490 forms/mL, while the ones inoculated at 15 days with 10 x 104 forms had a peak of 229,450 forms/mL. The parasitemy peak occurred between the 21st and 23rd day after inoculation in the groups evaluated, whereas the animals inoculated at 15 days of age presented, for both inoculates, higher values of parasitemy than the animals inoculated at 60 days. The histological analysis demonstrated tropism in the heart, with tissue alterations such as: focal and diffuse inflammatory process, perivascular infiltrate and parasite nests both intact and breached. Such processes presented cells such as macrophages, lymphocytes, polymorph nuclear cells, plasmocytes and fibroblasts. The remaining organs evaluated presented histological aspects similar to those of the control animals. There were greater alterations in the cardiac tissue of the younger animals (15 days), submitted to the greater inoculum.
Análise da atividade antimicrobiana das folhas de Davilla elliptica St.-Hil. (Dilleniaceae)
(2009) Soares, M. L.; Bustamante, K. G. L.; Echalar, Adda Daniela Lima Figueiredo; Pimenta, Fabiana Cristina; Fiuza, Tatiane de Sousa; Bara, Maria Teresa Freitas; Tresvenzol, Leonice Manrique Faustino; Paula, José Realino de
Análise da glicemia em jejum em pacientes provenientes do município de Terezópolis (Goiás-Brasil) associada com hipertensão arterial, circunferência abdominal e uso de medicamentos
(Marize Campos Valadares, 2007-06) Sousa, Rafael Lopes Pena de; Santos, Hebert Humberto Dutra dos; Campos, Claudio; Aversi-Ferreira, Tales Alexandre
The hypertension is one important complication associated with diabetes mellitus (DM) type 2, and the micro vessel alterations a result that evidence the high glycemy of these patients. The DM II has taking epidemics proportions because the amplified aging of population associated to sedentary custom, and the cardiovascular complications one important risk factor, indeed is associated by specialized literature that hypertension and DM was associated. Is known that mortality of DM patients is larger than population in general, and this fact is consequence of cardiovascular diseases. With main of available retrospectively that glycemy alterations that use hypoglycemic medicines and/or hypotensor 65 persons, between 2005 december and 2006 april interview, residents on Terezópolis of Goiás city (Brazil) were distribute in 4 different groups (health, hypertensions, hyperglycemis and hypertensions and hyperglycemics), all submitted to clinics examination that are capillary glycemy fasting, arterial pressure evaluation and anthropometrics data colleted. The evaluation of the this study permit verified that that DM II patients diagnosed present high glycemy levels same with concomitant hypoglycemic medicines use, and that the patients with booth DM and hypertension have larger glycemy level, and that women with DM present larger IMC than men. These data are indicators of need of more care with patients with diseases derivate of metabolic syndrome, better medicines adequate to treatment controls and more care with fatty persons and olds, mainly with hypertension, and more attention to fatty women with hyperglycemia.
Análise da publicidade de medicamentos veiculada em Goiás - Brasil
(Marize Campos Valadares, 2005-12) Freitas, Johnathan Santana de; Zampiere, Ana Lúcia Teixeira de Carvalho; Aquino, Aline Teixeira de; Lobo, Lina Monteiro de Castro; Montes, Patrícia Regina; Soares, Arthur; Silva, Érica T. da; A. Neto, João da C.; Araújo, Mariana de Paiva; Tresvenzol, Leonice Manrique Faustino; Prudente, Luciana Resende; Lima, Dione Marçal
Medicines are special products, whose advertisement inserts require different care relating to their ethic and moral aspects, once they have highly specific characteristics and their use is based on a precise diagnosis of a situation that causes risk to health. In this regarding, regulatory agencies established a specific legislation (RDC n° 102/00), set in legal parameters to medicines advertisements. The aim of this work was to evaluate the advertisements of medicines in Goias-Brazil based on the current legislation. The captation of irregular medicine advertisement inserts was performed between November/2004 and September/2005. The analysis followed the guideline “Roteiro de Verificação de Conformidades das Publicidades e Propagandas de Medicamentos”, present in the “Manual de Monitoramento de Propaganda de Produtos Sujeitos à Vigilância Sanitária” (MS, 2005). The results showed most of advertisements were related to over the counter medicines (OTC) (88,63%), followed by medicine prescription (8,33%) and controlled prescription (3,04%). The advertisement flyers were identified as the principal responsible for the propagation of irregular inserts (81,06%), followed by TV (14,40%) and radio (4,54%). In the 132 inserts analysed were detected many non-conformities with legislation and the absence of information about cares and warnings was observed in the majority of them. The present work demonstrated the importance of the medicines advertisements build based on the current legislation, assuring the defense of the population´s health.
Análise de prescrições médicas para tratamento de câncer de mama em um hospital universitário do estado de São Paulo
(2014) Bózoli, Luís Felipe Beloni; Ribeiro, Camila Milani; Zoccal, Polyana Lara de Mello; Ferreira, Iahel Manon de Lima; Fernandes, Rodrigo Marangoni; Sakamoto, Luiz Maçao; Abramovicius, Alexandra Cruz; Andrade, Jurandyr Moreira de; Dewulf, Nathalie de Lourdes Souza; Ungari, Andrea Queiróz
This article focuses on the analysis of prescriptions for the treatment of breast cancer in patients followed up in a university hospital in the state of São Paulo. The study analyzed 408 prescriptions between September and December 2012, with 201 in Chemotherapy Center and 207 in Chemotherapy Pharmacy in this teaching hospital. The main results were: (a) from 201 prescriptions analyzed in Chemotherapy Center, only 123 (61.2%) had weight, 89 (44.3%) height and 113 (56.2%) of the body surface patient; (b) 100% of prescriptions in Chemotherapy Center and 48.3% in the Chemotherapy Pharmacy showed abbreviations; (c) the trade name of the drug was present in 54.7% of prescriptions in Chemotherapy Center; (d) high rates of absence of information about the pharmaceutical form of the drug; (e) 05 (1.2%) prescriptions with illegible name of the patient and 04 (1%) prescriptions with illegible name of the drug. Data analysis shows the absence of complete information necessary for the safe use of anticancer drugs, if not evidencing compliance with current legislation. Thus, we highlight the importance of continuous training of physicians about the importance of a clear and complete prescription, as well as greater participation of clinical pharmacists and suggest also the implementation of the electronic prescription. These actions can improve the quality of prescriptions and promote the safe and rational use of medicines.
Análise farmacognóstica do pó e avaliação do efeito do extrato etanólico das flores da calendula officinalis l. cultivadas no Brasil no sistema imunológico
(Marize Campos Valadares, 2004-12) Parente, Leila Maria Leal; Matos, l. G.; Cunha, Luiz Carlos da; Leão, A. R.; Paula, José Realino de; V. Júnior, G.; Silveira, Nusa de Almeida
Calendula officinalis L. (Asteraceae) is an annual herbaceous from Mediterranean area and it was adapted in Brazil. Lots of factors related to cultivation, can affect in a significant way the quality and the quantity of the active principles produced by the plants. In this work, pharmacognostic evaluation of the flowers of C. officinalis from Brazil (Paraná), was accomplish for the quality control of the botanical material. The plant, well known a long time ago, has anti-inflammatory and healing activities and several other effects. It is present in many commercialized therapeutic formulations. In this work, an ethanolic extract of the flowers of the cultivated C. officinalis (EEC) in Brazil was gotten and was become an evaluation of the effect of the EEC in the immunologic system, verifying if the extract also gotten it would present the same immunomodulatory activity for isolated fractions of the plant cultivated in the Europe and Asia.
Análise microbiológica de matérias primas e formulações farmacêuticas magistrais
(Marize Campos Valadares, 2005-12) Andrade, Flávia R. O.; Souza, Aline A.; Arantes, Maria do Carmo Batista; Paula, José Realino de; Bara, Maria Teresa Freitas
In agreement with Good Manufacturing Practice, pharmaceutical products must have a quality according to specifications set by official compendia assuring their use. The microbiological quality of raw material employed in pharmaceutical and cosmetic formulations is very important to achieve efficacy and safety. In this work it was done the heterotrophic bacteria count, the total viable aerobic count, yeasts and moulds count, detection of pathogenic bacteria in samples of purified water, plant raw materials, natural products and in formula base of creams, lotions and gels. The applied methods and the specifications were based on Pharmacopeas or World Health Organization.The results showed that 86.3% of analysed samples were according to the parameters. The microbiological quality of deionizated water demonstrated a problem to pharmacies and it was verified that 65% of them were above the specifications. It was found that 97.17% of the formulations were with microbial counts in the permited limit. The plant raw materials and natural products showed values of 3.51% and 10.5%, respectively in disagreement with the specifications. The obtained data demonstrated that the Good Manufacturing Practice applied to pharmacies contribute to microbiological quality of the pharmaceutical products, however, critical points must be solved, as the quality of the deionizated water used must be improved.
Análise tecidual e celular das brânquias de Oreochromis niloticus L. tratadas com extrato etanólico bruto e frações das folhas da pitanga (Eugenia uniflora L.) - Myrtaceae
(2011) Fiuza, Tatiana de Sousa; Silva, P. C.; Paula, José Realino de; Tresvenzol, Leonice Manrique Faustino; Souto, M. E. D; Saboia-Morais, Simone Maria Teixeira de
Eugenia uniflora L. (Myrtaceae) is a plant found in the Cerrado biome and traditionally used in the treatment of diarrheas, inflammations, hyperglycemia and hypertension. Previous studies have revealed in vitro antimicrobial activity of E. uniflora. Considering its popular use, this study aimed to assess possible systemic cellular and tissue activities of the crude extract and the fractions from the leaves of this plant on Oreochromis niloticus L. (Nile tilapia) gill. Thus, ethanol extract and fractions from the leaves of this plant were orally administered to the fish in their rations. After 24 hours, the fish were sacrificed and the second gill arch of each fish was dissected, fixed in neutral formalin, dehydrated, embedded in paraffin and sectioned. Masson’s trichome and hematoxylin and eosin (HE) were used in the histological analyses. Qualitative analyses using a light microscope led to the conclusion that the crude ethanol extract and the fractions from E. uniflora leaves presented systemic effect on Nile tilapias, affecting the gills. Toxic actions such as respiratory epithelium detachment and lifting, and hyperplasia of interlamellar epithelial cells were more pronounced in the tilapias that ingested higher concentrations. This study helped to identify the vasodilator effect of this plant and contributed to the definition of the Nile tilapia as a model system for testing plant active principles. These tests are expected to make feasible not only the use of plants as fish medication but also the maintenance of the health of animals in intensive and extensive cultures through the possible use of alternatives to synthetic medication
Análises preliminares de substâncias viscosas em espectrômetro de infravermelho utilizando suporte alternativo
(Marize Campos Valadares, 2006) Soares, Lillian Amélia; Gil, Eric de Soza; Rezende, Kênnia Rocha
Infrared spectroscopy is a very used technique for structural elucidation of organic compounds. However, some accessories used on sample preparation are somehow expensive. In this work, it was investigated an alternative procedure for qualitative analysis of viscous substances using PVC film like support. Analysis of lanolin anhydrous and vitamin E were realized in KBr discs and PVC film comparatively to literature. The main advantages of this method rely on running samples spending less time, at low-cost support cell obtaining confident spectra.
Analogues of marine guanidine alkaloids are in vitro effective against Trypanosoma cruzi and selectively eliminate leishmania ( l .) infantum intracellular amastigotes
(2016) Martins, Ligia F.; Mesquita, Juliana Tonini; Pinto, Erika Gracielle; Silva, Thais Alves da Costa; Borborema, Samanta Etel Treiger; Galisteo Junior, Andrés Jimenez; Neves, Bruno Junior; Andrade, Carolina Horta; Shuhaib, Zainab Al; Bennett, Elliot Leon
Synthetic analogues of marine sponge guanidine alkaloids showed in vitro antiparasitic activity against Leishmania (L.) infantum and Trypanosoma cruzi. Guanidines 10 and 11 presented the highest selectivity index when tested against Leishmania. The antiparasitic activity of 10 and 11 was investigated in host cells and in parasites. Both compounds induced depolarization of mitochondrial membrane potential, upregulation of reactive oxygen species levels, and increased plasma membrane permeability in Leishmania parasites. Immunomodulatory assays suggested an NO-independent effect of guanidines 10 and 11 on macrophages. The same compounds also promoted anti-inflammatory activity in L. (L.) infantum-infected macrophages cocultived with splenocytes, reducing the production of cytokines MCP-1 and IFN-γ. Guanidines 10 and 11 affect the bioenergetic metabolism of Leishmania, with selective elimination of parasites via a host-independent mechanism.
Angiogenic activity of Calendula officinalis flowers L. in rats
(2011) Parente, Leila Maria Leal; Andrade, Maria Auxiliadora; Brito, Luiz Augusto Batista; Moura, Veridiana Maria Brianezi Dignani de; Miguel, Marina Pacheco; Lino Júnior, Ruy de Souza; Tresvenzol, Leonice Faustino Manrique; Paula, José Realino de; Paulo, Neusa Margarida
Purpose: In this work, angiogenic activity of Calendula officinalis L. (Asteraceae) ethanolic extract and dichloromethane and hexanic fractions were evaluated, considering medicinal properties, especially healing activity, are attributed to this plant. Methods: Models using 36 rats and 90 embryonated eggs were used to evaluate healing and angiogenic activities of extracts and fractions of the plant, through the induction of skin wounds and the chorioallantoic membrane, respectively. The effect of vascular proliferation was also tested from the study to verify the intensity of expression of vascular endothelial growth factor (VEGF) in cutaneous wounds in rats. Results: The angiogenic activity of the extract and the fractions was evidenced in both experimental models. It was verified that this effect is not directly related to the expression of VEGF and it could be associated to other pro-angiogenic factors. Conclusion: The healing activity referred to C. officinalis is related, among other factors, to its positive effect on angiogenesis, characterized by the induction of neovascularization

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