Institute Tecnologia em Farmacos

Rio de Janeiro, Brazil

Institute Tecnologia em Farmacos

Rio de Janeiro, Brazil
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Macedo A.L.,Federal University of Fluminense | dos Santos T.C.C.,Federal University of Fluminense | Valverde A.L.,Federal University of Fluminense | de Lima Moreira D.,Institute Tecnologia em Farmacos | Vasconcelos T.R.A.,Federal University of Fluminense
Mini-Reviews in Medicinal Chemistry | Year: 2017

Background: The genus Piper L. has the shikimic acid pathway predominantly expressed, biosynthesizing many cinnamic acid derivatives (CAD). Objective: Neolignans comprise an important class of CAD that exhibit a wide range of pharmacological properties such as antibacterial, antitumor, insecticidal, anti-inflammatory, antioxidant, smooth muscle relaxant, neuroprotective, antiprotozoal and against platelet aggregation factor. These substances have been extracted and isolated from Piper species using different technics. Results: The present review aims to summarize extraction and isolation methods and biological activities of the different types of neolignans covering the period from 1968 to January 2016. © 2017 Bentham Science Publishers.

Da Monteiro S.S.,Institute Tecnologia em Farmacos | Da Silva V.P.,Institute Tecnologia em Farmacos | Nakamura M.J.,Institute Tecnologia em Farmacos | Siani A.C.,Institute Tecnologia em Farmacos
Journal of Essential Oil Research | Year: 2010

The leaf oils from five Myrtaceae species growing in the restinga forest of Carapebus, on the southeastern Brazilian coast, were obtained by hydrodistillation and analyzed by GC/MS. Eugenia punicifolia oil contained only sesquiterpenes, with predominance of β-elemene (22.1%) followed by β-caryophyllene (8.5%) and components of the selinane (24.8%) and cadinane (14.0%) skeletal-types. Eugenia sulcata oil had the highest content of monoterpenes, among which a-pinene (12.2%), β-pinene (10.8%) and 1,8-cineole (19.6%) predominated. This profile was completed with 23.5% of caryophyllane and humulane derivatives. αa-Pinene also appeared significantly (18.8%) in Eugenia rotundifolia, followed by small amounts of α-terpineol (4.4), while limonene (4.7%) and 1,8-cineole (6.8%) were the main monoterpenes in Myrciaria floribunda. The chemical profile of Neontitranthes obscura was also dominated by selinane-type sesquiterpenes: α-cadinene (23.4%), selina-3,7(11)-diene (13.9%), β-selinene (8.5%) and α-selinene (5.5%), followed by traces of pinenes, limonene and 1,8-cineole (2.4%). Total cyclic sesquiterpene alcohols, esters and epoxides decreased from 55.5% in E. rotundifolia to 8.6% in M. floribunda. However, the latter species contained 26.9% of (E)-nerolidol in the oil composition. Traces of ketones (up to 3.1%) are present in E. punicifolia, N. obscura and M. floribunda. © 2010 Allured Business Media.

Figueiredo T.A.,Institute Tecnologia em Farmacos | De Andrade Schramm J.M.,Escola Nacional de Saude Publica Sergio Arouca | Pepe V.L.E.,Escola Nacional de Saude Publica Sergio Arouca
Cadernos de Saude Publica | Year: 2014

The World Health Organization (WHO) defines essential medicines as those that meet the population’s priority healthcare needs. Their selection aims to reflect collective needs, thus recommending the use of studies on global burden of disease. An exploratory study was performed to link the medicines from the RENAME lists to Global Burden of Disease in Brazil (1998 and 2008) and the scientific evidence. The study thus sought to verify whether the RENAME (2002 to 2012) met WHO guidelines for drug selection. Although RENAME 2010 and 2012 both adhere to Global Burden of Disease in Brazil 2008, the 2012 version includes a longer list of medicines and appears to be pressured by the growing market for new technologies. Thus, RENAME is no longer a list of essential medicines, but has become a list of financing for pharmaceutical care.

Moulton T.P.,State University of Rio de Janeiro | Magalhaes-Fraga S.A.P.,Institute Tecnologia em Farmacos | Brito E.F.,State University of Rio de Janeiro | Barbosa F.A.,Federal University of Minas Gerais
Hydrobiologia | Year: 2010

Coarse particulate organic matter is often broken down by specialist shredder invertebrates in temperate streams. In some tropical streams, larger, non-specialist, omnivorous fauna, (macroconsumers), particularly decapod shrimps and crabs, have been found to process coarse particulate matter. Larger shrimps and fish may also prey on or inhibit smaller invertebrates. Depending on the relative importance of larger and smaller fauna in leaf processing and in predatory interactions, we could expect that exclusion of larger fauna could either result in a decrease in leaf processing (if they were important in shredding or bioturbation) or increase in leaf processing if they negatively affected smaller shredders. We tested this by excluding fauna of different sizes from leaf peaks using bags with different sizes of mesh -0.2 mm (exclusion of most fauna), 2 mm (exclusion of larger fauna), and 10 mm (access to most fauna). Bag effect on leaf processing was minimized by constructing the bags of the same, fine, material, and sewing a relatively small window of the required mesh size. The experiment was conducted on two occasions in three streams of the urban forest of Parque Estadual da Pedra Branca, city of Rio de Janeiro. The three streams differed in larger fauna of shrimps (Macrobrachium potiuna), crabs, tadpoles, and fish. Packs were incubated for six time intervals and the rate of leaf processing calculated as the exponential rate of loss of leaf material. Rate of leaf processing was faster in bags with the largest mesh size; the rates in the other two mesh sizes were not statistically different. Rates varied between experiments and among streams. We could not attribute the faster leaf processing to any particular component of the larger fauna; the patterns of differences among streams and between experiments were not associated with particular taxa. There was no general trend of fewer smaller fauna in the presence of macroconsumers; the few smaller taxa that were different between mesh sizes were variously less and more abundant in the 10-mm mesh bags compared to the 2-mm. Known shredders were rare in the smaller fauna; the mining chironomid Stenochironomus was common, but was apparently not affected by larger fauna and apparently did not increase leaf processing. We conclude that macroconsumers and not smaller fauna had a positive effect on leaf processing, and this confirms a pattern observed in some other coastal Neotropical streams. © Springer Science+Business Media B.V. 2009.

Siani A.C.,Institute Tecnologia em Farmacos | Souza M.C.,Institute Tecnologia em Farmacos | Henriques M.G.M.O.,Institute Tecnologia em Farmacos | Ramos M.F.S.,Institute Tecnologia em Farmacos | Ramos M.F.S.,Federal University of Rio de Janeiro
Pharmaceutical Biology | Year: 2013

Context: Despite the many biological activities reported for essential oils, their anti-inflammatory ability is relatively underexplored considering the wide variation in plant sources and in their volatile composition. Oils from Syzygium cumini Skells (SC) and Psidium guajava L. (PG) (Myrtaceae) have been described as having diverse pharmacological activities. Objective: The current study seeks to evaluate the anti-inflammatory activity of the essential oils from the leaves of SC and PG, as well as some of their terpene-enriched fractions (+V = more volatile and -V = less volatile) obtained by vacuum distillation. Both the pharmacological responses and chemical compositions were correlated. Materials and methods: The relative contents of the oils and their fractions were evaluated by gas chromatography. Individual constituents in the oils were characterized by gas chromatography coupled to mass spectrometry. Anti-inflammatory activity was accessed in the lipopolysaccharide-induced pleurisy model, by measuring the inhibition of total leukocyte, neutrophil and eosinophil migration in the mice pleural lavage, after oil treatment with the oils at 100 mg/kg. Results: Eosinophil migration was inhibited by SC (67%), SC (+V) (63%), PG (76%), PG (+V) (67%) and PG (-V) (74%). This efficacy was correlated with the presence of β-pinene and β-caryophyllene in the oils, a result that was reinforced by evaluating both these pure components (38 and 50% inhibition, respectively). Synergistic effects associated with the presence of α-pinene were speculated. Discussion and conclusion: Essential oils from SC and PG may be useful to treat inflammatory diseases by mechanisms that include the inhibition of eosinophil migration. © 2013 Informa Healthcare USA, Inc.

Soares D.C.,Federal University of Rio de Janeiro | Portella N.A.,Federal University of Rio de Janeiro | Ramos M.F.D.S.,Federal University of Rio de Janeiro | Siani A.C.,Institute Tecnologia em Farmacos | Saraiva E.M.,Federal University of Rio de Janeiro
Evidence-based Complementary and Alternative Medicine | Year: 2013

This study investigated the leishmanicidal activity against Leishmania amazonensis of four commercial oils from Copaifera spp. named as C1, C2, C3, and C4, the sesquiterpene and diterpene pools obtained from distilling C4, and isolated β-caryophyllene (CAR). Copaiba oils chemical compositions were analyzed by gas chromatography and correlated with biological activities. Diterpenes-rich oils C2 and C3 showed antipromastigote activity. Sesquiterpenes-rich C1 and C4, and isolated CAR presented a dose-dependent activity against intracellular amastigotes, with ICof 2.9 μg/mL, 2.3 μg/mL, and 1.3 μg/mL (6.4 μM), respectively. Based on the highest antiamastigote activity and the low toxicity to the host cells, C4 was steamdistillated to separate pools of sesquiterpenes and diterpenes. Both pools were less active against L. amazonensis and more toxic for the macrophages than the whole C4 oil. The leishmanicidal activity of C3 and C4 oils, as well as C4 fractions and CAR, appears to be independent of nitric oxide production by macrophages. This study pointed out β-caryophyllene as an effective antileishmanial compound and also to its role as potential chemical marker in copaiba oils or fractions derived thereof, aiming further development of this rainforest raw material for leishmaniasis therapy. © 2013 Deivid C. Soares et al.

Lima A.M.B.,Institute Tecnologia Em Farmacos | D'Avila L.A.,Federal University of Rio de Janeiro | Siani A.C.,Institute Tecnologia Em Farmacos
Chromatographia | Year: 2014

This study details a method to characterize the triterpene acid-rich extract obtained from the defatted leaves of Eugenia brasiliensis (Myrtaceae) via extraction with 2 % NaOH in ethanol at room temperature. The crude extract (yield 2.35 %) was submitted to analysis by gas chromatography coupled to mass spectrometry (GC-MS) confirming ursolic acid as its major compound. The optimal conditions for the separation of oleanolic, betulinic and ursolic acids were assayed by GC with flame ionization detection (GC-FID) using two different columns (DB-5 and DB-17HT) and by applying two distinct derivatizing protocols. The use of a DB-17HT column led to the best results, with a shorter runtime and a better resolution (Rs) between the oleanolic and betulinic signals for both the bis-trimethylsilyl (Rs 2.84) and methyl ester derivatives (Rs 2.47). A DB-5 column also gave satisfactory results for the TMS ester, with a runtime of 30 min and Rs 2.14. Ursolic acid in the crude extract was quantified by comparison to two individual standard curves determined using commercial ursolic as its TMS derivative on the DB-5 column and its methyl ester on the DB-17HT column. Good linearity was achieved in both cases (r2 = 0.9776 and 0.9953, respectively), and the amounts of ursolic acid in the extracts were calculated to be 144.7 and 147.9 mg·g-1, respectively. These results showed no significant differences when compared using Tukey's HSD test. Total triterpene acids amounted to 0.52 % in E. brasiliensis dry leaves. © 2014 Springer-Verlag.

Reis D.C.,Federal University of Minas Gerais | Pinto M.C.X.,Federal University of Minas Gerais | Souza-Fagundes E.M.,Federal University of Minas Gerais | Wardell S.M.S.V.,Institute Tecnologia em Farmacos | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2010

The antimony(III) complexes [Sb(2Bz4DH)Cl 2] (1), [Sb(H2Bz4M)Cl 3]·2H 2O (2) and [Sb(2Bz4Ph)Cl 2] (3) were obtained with 2-benzoylpyridine thiosemicarbazone (H2Bz4DH) and its N(4)-methyl (H2Bz4M) and N(4)-phenyl (H2Bz4Ph) derivatives. H2Bz4DH, H2Bz4Ph and complexes (1-3) exhibited high cytotoxic activity against HL-60 and Jurkat human leukemia cell lines. When these compounds were tested against HL-60 cells with ectopic expression of BcrAbl, Bcl-2 or Bcl-X L, which confer resistance to apoptosis against a variety of death-inducing agents, the cytotoxicity was much lower, indicating apoptosis to be part of their mechanism of action. The cytotoxic activity of complexes 2 and 3 against HL-60 and Jurkat cells was significantly higher than that of the corresponding thiosemicarbazones, suggesting coordination to be an interesting strategy of cytotoxic dose reduction. [Sb(2Bz4DH)Cl 2] (1), [Sb(H2Bz4M)Cl 3] (2) and [Sb(2Bz4Ph)Cl 2] (3) were obtained with 2-benzoylpyridine thiosemicarbazone (H2Bz4DH) and its N(4)-methyl (H2Bz4M) and N(4)-phenyl (H2Bz4Ph) derivatives. H2Bz4DH, H2Bz4Ph and 1-3 were highly cytotoxic to leukemia cells. © 2010 Elsevier Masson SAS. All rights reserved.

Boechat N.,Institute Tecnologia em Farmacos | Pinheiro L.C.S.,Institute Tecnologia em Farmacos | Santos-Filho O.A.,Institute Tecnologia em Farmacos | Silva I.C.,Institute Tecnologia em Farmacos
Molecules | Year: 2011

A rational approach was used to synthesize a new set of 15 1H-1,2,4-triazol-3-yl benzenesulfonamide derivatives with the aim of developing new antimalarial lead compounds. These derivatives were prepared in yields between 50% and 62%, and their structures were elucidated using IR, 1H-, 13C-, 19F-NMR, MS and elemental analysis. A docking study based on sulfonamides previously used against malaria identified trifluoromethyl-substituted derivatives to be the best lead compounds for new antimalarial drug development. © 2011 by The Authors.

Prado L.D.,Institute Tecnologia em Farmacos | Rocha H.V.A.,Institute Tecnologia em Farmacos
Revista Virtual de Quimica | Year: 2015

Most marketed pharmaceuticals consist of molecular crystals due to reasons of stability and ease handling during the development. Pharmaceutical solids can exist in the different forms. The arrangement of the molecules in a crystal determines its physical properties, influences the formulation, as well as dissolution rate and stability. Several examples are reported to demonstrate the importance of polymorphism in properties that can change the quality of the final product. A thorough understanding of the relationships between physical structures and the properties of pharmaceutical solids is therefore important in selecting the most suitable form. In this review, the different crystal forms of pharmaceuticals, the commonly used solid-state analytical techniques and advantages and disadvantages of each technique are discussed. In more detail, here is exposed the impact of solid forms in a galenic level.

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