A5015128651- Malaria Research and Control
- Computational Drug Discovery Methods
- Synthesis and biological activity
- Mosquito-borne diseases and control
- Synthesis and Characterization of Heterocyclic Compounds
- Marine Sponges and Natural Products
- Click Chemistry and Applications
- HIV/AIDS drug development and treatment
- Trypanosoma species research and implications
- Bioactive Compounds and Antitumor Agents
- Synthesis and bioactivity of alkaloids
- Cancer Diagnosis and Treatment
- Synthesis and Catalytic Reactions
- Synthesis and Biological Evaluation
- Research on Leishmaniasis Studies
- Traditional and Medicinal Uses of Annonaceae
- Cancer therapeutics and mechanisms
- Insect Pest Control Strategies
- Drug-Induced Hepatotoxicity and Protection
- Synthesis of Organic Compounds
- Essential Oils and Antimicrobial Activity
- Ion Transport and Channel Regulation
- Phytochemical compounds biological activities
- Science and Education Research
- Drug Transport and Resistance Mechanisms
Federal University of São João del-Rei
2015-2024
University of Lusaka
2013
Universidade Federal de Minas Gerais
2008-2012
Fundação Oswaldo Cruz
2006-2009
Universidade de São Paulo
2000-2003
Polygala boliviensis is found in the Brazilian semiarid region. This specie little chemically and biologically studied. spp. have different metabolites, especially coumarins. Studies indicate that coumarins antimalarial potential, denoting importance of researching new active compounds from plants, since resistance Plasmodium strains to conventional therapy has increased. The present study aimed evaluate antiplasmodial activity auraptene poligalen against a chloroquine-resistant strain...
A new synthetic antimalarial drug, a salt derived from two molecules, mefloquine (MQ) and artesunate (AS), here named MEFAS, has been tested for its pharmacological activity. Combinations of AS plus MQ hydrochloride are currently being used in areas with drug-resistant Plasmodium falciparum parasites; although clears parasitemia shorter time periods than any other it does not cure infected patients; addition, causes side effects is rather expensive, important problems considering that...
Psidium guajava L. has extensive use in folk medicine. The aim of this study was to quantify the levels phenolic, flavonoids, antioxidant activity, leathality assay and antibacterial antitumoral activities extract P. guajava. In dry guava there were high phenolics (766.08 ± 14.52 mg/g), flavonoids (118.90 5.47 mg/g) activity (87.65%). LD50 185.15 μg/ml. MIC value 250 μg/ml for Streptococcus mutans, mitis oralis. IC50 tested HeLa, RKO Wi cell lines 15.6 0.8 μg/ml, 21.2 1.1 68.9 1.5...
Cardiotonic steroids are used to treat heart failure and arrhythmia have promising anticancer effects. The prototypic cardiotonic steroid ouabain may also be a hormone that modulates epithelial cell adhesion. consist of nucleus lactone ring, their biological effects depend on the binding receptor, Na,K-ATPase, through which, they inhibit Na+ K+ ion transport activate several intracellular signaling pathways. In this study, we added styrene group ring digoxin, obtain 21-benzylidene digoxin...
In antimalarial research there are no standard procedures to determine the toxicity of a drug candidate. Among alternatives available, in vitro cytotoxicity assays most widely used predict toxic effects future therapeutic products. They have advantage over vivo assays, that they offer possibility restrain number experimental variables. The objective present study was compare cytotoxic methods by testing various compounds currently treat malaria against different cell lines. Neutral red (NR)...
Owing to increased spending on pharmaceuticals since 2010, discussions about rising costs for the development of new medical technologies have been focused pharmaceutical industry. Computational techniques developed reduce associated with drug development. Among these techniques, virtual high-throughput screening (vHTS) can contribute discovery process by providing tools search drugs ability bind a specific molecular target.In this context, Brazilian malaria targets (BraMMT) was generated...
Extracts from Holostylis reniformis were tested in vivo against Plasmodium berghei and vitro a chloroquine-resistant strain of falciparum. The hexane extract the roots was most active, causing 67% reduction parasitemia vivo. From this extract, six lignans, including new (7'R,8S,8'S)-3',4'-methylenedioxy-4,5-dimethoxy-2,7'-cyclolignan-7-one, isolated P. three active lignans showed 50% inhibitor concentrations < or =0.32 microM. An evaluation minimum lethal dose (30%) values low toxicity for...
A series of new chalcones substituted with azide/triazole groups were designed and synthesized, their cytotoxic activity was evaluated in vitro against the HeLa cell line. O-Alkylation, Claisen-Schmidt condensation Cu(I)-catalyzed cycloaddition azides terminal alkynes applied key steps. Fifteen compounds tested cells. Compound 8c most active molecule, an IC50 value 13.03 µM, similar to cisplatin (7.37 µM).
Herein, we report the antimalarial activity of nine 4-methoxychalcone derivatives 1a-i and an initial analysis their ADMET properties. All compounds showed potent against P. falciparum chloroquine-resistant clone W2, with IC50 values ranging from 1.96 µM to 10.99 µM, moderate or low cytotoxicity HeLa cell line. The compound 1a (IC50 = 2.06 µM) had best selectivity index (9.0). sulfonamide 4-metychalcone synthesized cLogP between 2 5 (mean value 3.79) molecular weights (MWs) below 500....
Clinical and epidemiological studies have indicated that breastfeeding has a protective effect on breast cancer risk. Protein-based drugs, including antibodies, are being developed to attain better forms of therapy. Secretory IgA (SIgA) is the antibody class in human milk, its activity can be linked breastfeeding. The aim this study was investigate polyethylene glycol (PEG) microspheres with adsorbed SIgA MCF-7 cells.The PEG were characterized by flow cytometry fluorescence microscopy. cells...
ABSTRACT Malaria is a disease of global tropical distribution, being endemic in more than 90 countries and responsible for about 212 million cases worldwide 2016. To date, the strategies used to eradicate this have been ineffective, without specific preventive measures such as vaccines. Currently, existing therapeutic arsenal limited has become ineffective against expansion artemisinin-resistant Plasmodium, demonstrating need studies that would allow development new compounds disease. In...
Cancer continues to be one of the most important health problems worldwide, and identification novel drugs treatments address this disease is urgent. During recent years, marine organisms have proven a promising source new compounds with action against tumoral cell lines. Here, we describe synthesis anticancer activity eight 3-alkylpyridine alkaloid (3-APA) analogs in four steps good yields. The key step for these Williamson etherification under phase-transfer conditions. We investigated...
We herein report the synthesis of hybrid kauranoid molecules type 1,2,3-triazole-1,4disubstituted aiming to improve antimalarial activity kaurenoic and xylopic acids.The Cu I -catalyzed cycloaddition azides terminal alkynes was explored as a hybridization strategy.Kauranoid were prepared from acids that isolated Wedelia paludosa D. C. (Asteraceae) Xylopia frutescens Aubl.(Annonaceae).A total 15 derivatives, including nine new triazoles, obtained five out these more active than original...