Programa de Pós-Graduação em Ciências Farmacêuticas - PPGCF/ICS

URI Permanente desta comunidadehttps://repositorio.ufpa.br/handle/2011/2312

O Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF) vinculado ao Instituto de Ciências da Saúde (ICS) da Universidade Federal do Pará (UFPA) apresenta um auto-impacto de inserção regional uma vez que se trata do único PPGCF na Região Norte pelo grande potencial de utilização da biodiversidade na região amazônica. Além de favorecer a fixação e atração de profissionais qualificados na área de Ciências Farmacêuticas na Região Amazônica.

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Acesso aberto (Open Access)
Estudo da ação antinociceptiva e antiinflamátoria do 1-Nitro-2-Feniletano, principal constituinte da Aniba Canelilla
(Universidade Federal do Pará, 2008-06-26) LIMA, Anderson Bentes de; MAIA, José Guilherme Soares; http://lattes.cnpq.br/1034534634988402; SOUSA, Pergentino José da Cunha; http://lattes.cnpq.br/9909053957915090
Aniba canellila is a large size tree found in Northern region of Brazil and largely used in folk medicine. The infusate of its leaves and bark skin is believed to be a good antispasmodic, antidiarreic, anti-inflammatory, tonic agent and a good stimulant of digestive and the central nervous systems. This study was designed to evaluate the effects 1-nitro-2-phenylethane, main component of Aniba canelilla. We evaluated the antinociceptive and anti-inflammatory effects of the 1-nitro-2-phenylethane which is the main component of essential oil of Aniba canelilla. For nociception models were designed the writhing test, hot plate test and formalin test. For inflammation models were designed the croton oil-induced ear edema, rat paw edema induced by carrageenan and dextran, and leucocyte and neutrophil migration on carrageenan-induced peritonitis. In the writhing test, the 1-nitro-2-phenylethane dosed at 15, 25 and 50 mg/kg reduced the abdominal writhes in a significant manner. In the hot plate test (55 ? 0.5? C), the 1-nitro-2-phenylethane dosed at 50, 100 and 200 mg/kg did not induced alterations in the latency time when compared to the control. In the formalin test, the 1-nitro-2-phenylethane dosed at 50 and 25 mg/kg reduced in a significant manner the second phase of the algic stimulous. In addition, its antinociception was reversed by naloxone in the second phase. The 1-nitro2-phenyletahne produced inhibition of rat paw edema induced by carrageenan and dextran in a dose-dependent manner at the doses of 25 and 50 mg/kg. Doses of 25 and 50 mg/kg caused a dose-dependent inhibition of croton oil-induced ear edema in mice (with inhibition of 73% and 79%, respectively). Pretreatment (60 min) of rats with 1-nitro-2-phenylethane (25 mg/kg) significantly decreased leucocyte and neutrophil migration on carrageenan-induced peritonitis (with inhibition of 22,55% and 38,13%, respectively). Our results suggest that 1-nitro-2-phenylethane has analgesic activity which, according to the tests employed, is probably of peripheral origin. The mechanism involved is not completely understood, however these results suggest that opiod receptors are involved in the antinociceptive action of the 1-nitro-2-phenylethane. Further, our results suggest that 1-nitro-2-phenylethane has anti-inflammatory activity which, according to the tests employed, is probably of peripheral origin.
Acesso aberto (Open Access)
Avaliação da atividade antimicrobiana de plantas utilizadas na medicina popular da Amazônia
(Universidade Federal do Pará, 2008-07-24) RIBEIRO, Christian Miranda; OLIVEIRA, Davi de Jesus; http://lattes.cnpq.br/5170029508278769; VIEIRA, José Maria dos Santos; http://lattes.cnpq.br/6807452375674442
The study of medicinal plants it makes possible the discovery of new bioactive components in the search for promising drugs. The increase of infections and the appearance of the microbial resistance strengthen this research. The Objective of this study it was evaluate the antimicrobial activity of the extracts of six medicinal plants of the Amazonia: Psidium guajava (guava), Bryophyllum calycinum Salisb (pirarucu), Eleutherine plicata Herb (marupazinho), Uncaria guianensis (Cats claw), Arrabideae chica (pariri) e Mansoa alliacea (Lam.) A.H. Gentry (cipó d'alho) against ATCC strains of fungi and bacteria.The collection and the identification of the plant were performed in EMBRAPA/CPATU and the phytochemical analysis in the Laboratory of FACFAR/UFPA and CESUPA in agreement with the methodologies established in these laboratories. The crude ethanolic extract of leaves and the underground parts of marupazinho were submitted to the antimicrobial activity evaluation though the ágar disc diffusion method and determination of minimum inhibitory concentration (MIC) though microdilution in plate and ágar disc diffusion methods. The extracts were used in concentrations of 500, 250, 125, 62,5 and 31,25 mg/mL using as solvent Dimethyl Sulfoxide (DMSO). The Guava extract was effective against S. aureus, P. aeruginosa and C. albicans (MIC 125mg\mL), pirarucu was effective against S aureus (MIC= 500 mg/mL) and P. aeruginosa (MIC= 250 mg/mL), marupazinho against S.aureus (MIC= 500mg/mL) and C. albicans (MIC= 250mg/mL), Cats claw against S. aureus (MIC= 62,5mg/mL) and pariri was effective against S. aureus (MIC= 62,5 mg/mL), E. coli (MIC=250 mg/mL) and C. albicans (MIC 500 mg/mL). The fractions of U. guianensis extracts was obtained though fractioned dissolution methods and show that only the methanolic fraction presented antimicrobial activity. The results show that Amazonia medicinal plants presents antimicrobial activity and. This promissory extracts open the possibility of finding new clinically effective antimicrobial compounds.
Acesso aberto (Open Access)
Plantas medicinais utilizadas em comunidades do município de Igarapé-Miri, Pará: etnofarmácia do município de Igarapé-Miri-Pará
(Universidade Federal do Pará, 2008-08-08) PINTO, Lucianna do Nascimento; BARBOSA, Wagner Luiz Ramos; http://lattes.cnpq.br/1372405563294070
In IgarapéMiri, as well throughout the state of Pará, the use of medicinal plants to treat many illnesses is very usual. In the same way, in some states in Brazil official programs of medicinal plants have been registered and to follow the plant species used in the folk phytotherapy ethnoguided methodologies are applied mainly ethnobotany and ethnopharmacology. From the Pharmaceutical Sciences Ethopharmacy was elaborated, which has been worldwide used to approach medicinal plants and to evaluate the remedies prepared from them. The general aim of this work is to contribute for the consolidation of Ethnopharmacy and the implementation of the PNPMF in the state of Pará, bringing information collected about indication of medicinal plants, preparation and administration of vegetal remedies and problems related to the use of them. More specifically, it aims to determine the regional nosogeography, to identify and to select the used phytotherapeutical resources for the treatment of the prevalent illnesses, to know and to characterise from the pharmaceutical point of view the remedies made with vegetable base, as well as elaborating cards with information about selected vegetables, these are other objectives considered here. The tool to reach these objectives is the ethnopharmaceutical survey which associates elements of other ethnoguided methods with the content of the Pharmaceutical Care. Applied in eighty six communities of the city, at two moments, first in the year 2000 and in March/April 2008, the method supplied data which were tabulated using Excel to make tables and graphs. Thus, 91 illnesses, 236 plants species, distributed through 72 botanical families, and in 7 different forms of administration. Thirty eight adverse events could also be identified. Cards with botanical, chemical and ethnopharmaceutical information were elaborated for the four plants species with highest relative citation frequencies.
Acesso aberto (Open Access)
Determinação das concentrações plasmáticas e teciduais de itraconazol em pacientes com cromoblastomicose
(Universidade Federal do Pará, 2008-09-01) GRISÓLIA, Daniella Paternostro de Araújo; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
Chromoblastomycosis is a subcutaneous mycosis caused by deployment transcutaneous of several species of dematiaceous fungi, that is, melanized fungi. Considering the incidence of this disease in the state of Pará and the resulting morbidity of patients affected, with economic and social repercussions, it was made to the optimization of therapeutic schemes adopted, to the best knowledge of the relation dose x response. The itraconazole is one of the few drugs available for treatment, which has marked variability kinetic intra and inter individual, which compromises the establishment of the relation dose and response, as well as tissue and plasma concentrations achieved. In this sense, this work aimed at validation of analytical methodology by High Performance Liquid Chromatography and subsequent determination of itraconazole in samples of plasma and tissue in 20 patients with chromoblastomycosis, assisted in the laboratory of dermatoimmunology Dr. Marcello Candia, Marituba, Pará, who used the drug in doses of 200mg/day and 400mg/day. The technique employed was validated and proved adequate results in accordance with applicable law. Concentrations of plasma and tissue of itraconazole in the dose of 200mg/day were 121.3 87.9 ng/mL and 5.36 5.9 μg/g. The average plasma concentration of itraconazole in patients using 400mg/day was 290 234 ng/mL, and the plasma and tissue mean concentrations of itraconazole in patients who showed no clinical favourable, at doses of 200mg, making it necessary to increase to 400mg were 217 216 and 304 173 ng/mL; 14.87 12.94 e 21.80 6.62 μg/g. The average of relation between tissue and plasma concentrations in patients who had positive developments in clinical in the doses of 200mg/day was 44.29 67.12 and those that did not show positive developments in clinical in the doses of 200mg/day, making necessary to increase to 400mg/day were 68.52 59.90 and 71.71 38.26 respectively.
Acesso aberto (Open Access)
Caracterização farmacognóstica, química, físico-química e estudos preliminares de pré-formulação da Arrabidaea chica (Humb. & Bonpl.) B. Verlt.
(Universidade Federal do Pará, 2008-10-22) ALVES, Mauro Sérgio Marques; SILVA JÚNIOR, José Otávio Carréra; http://lattes.cnpq.br/4437885351749994
This work aimed the physical, chemical, physico-chemical and preformulations characterizing of Arrabidaea chica (Humb. & Bonpl.) B. Verlt., belonging to the family of Bignoniacae, which receives several denominations, and in the Amazon region is known popularly as pariri, that is widely used in popular medicine for the treatment of many diseases, such as skin infirmities caused by dermatitis and eczema. The use of natural products from vegetal origin requires the pharmaco-botanical quality control and pureness analysis which sets the species technical specifications. Therefore, it was made an anatomical description of the young and mature leaves of the plant from observations made at the optic microscope in histological cuts. The pharmacological tests included the determination of the granulometrical distribution of the plants powder, determination of the humidity purport and of total ashes and, about the dyeing, it was made pH, relative density and solids purport determinations, and also it was made the chemical prospection, the chromatographic profile by thin-layer chromatography (TLC) and the highperformance liquid chromatography (HPLC), besides the valuation of its microbial activity. To the powder as well as the dyeing of the A. chica observed the profiles by spectroscopy in the infrared region and thermal profiles by TGA and DTA. Some studies of preformulation were made by spectroscopy in the infrared region and thermal analysis (TGA and DTA) of the binary mixtures of the formula adjuvants suggested to spread the dye, with the purpose to evaluate possible incompatibilities between the dye and these elements. The results obtained evidenced that the A. chica dye demonstrated to adjust to the aim demanded, moreover it assured the compatibility to the tested adjuvants to constitute the proposed formula, once none clue of physical or chemical incompatibilities were observed among them. The studies provided relevant basis to the development of the proposed formula, seeking to obtain quick results with the wished accuracy.
Acesso aberto (Open Access)
Determinação das concentrações plasmáticas de amitriptilina por cromatografia líquida de alta eficiência em pacientes com hanseníase e estados reacionais
(Universidade Federal do Pará, 2008-10-24) MORAES, Tânia Mara Pires; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
Leprosy is a granulomatous disease affecting the skin and peripheral nerves caused by Mycobacterium leprae. The alterations in peripheral nerves can originate pain symptoms and deformities, with consequent reduction of patient life quality. Amitriptyline is the drug of choice for the treatment of pain symptoms in patients with leprosy. Amitriptyline had a narrow therapeutic range and a great variability in plasmatic concentrations between patients. Thus the therapeutic monitoring of the plasmatic concentrations of this drug its a important tool for therapy optimization. In this sense this work aimed the validation of an analytical procedure for determination of amitriptyline by high performance liquid chromatography, in patients with hansenic reactions using amitriptyline daily doses of 25mg or 50mg, as well make the comparison between amitriptyline plasmatic concentrations in the presence or absence of multidrug therapy and in the reactions type I and II. This study was conducted in Tropical Medicine Institute from Para Federal University. Were enrolled 21 patients, 12(57%) male and 9 (43%) female. Eight patients (38%) were in curse of multidrug therapy and 10 (47%) presented hansenic reaction type I. The medium plasmatic amitriptyline concentration in dose of 25mg was 318144ng/mL and 361182ng/mL. No statistical significance was observed between medium plasmatic amitriptyline concentrations in doses of 25mg and 50mg, as well in the presence of multidrug therapy.
Acesso aberto (Open Access)
Avaliação da atividade antinociceptiva e antiinflamatória do óleo essencial de Hyptis crenata (Pohl) ex Benth
(Universidade Federal do Pará, 2008-11-07) BRAVIM, Luciana Silva; MAIA, José Guilherme Soares; http://lattes.cnpq.br/1034534634988402; SOUSA, Pergentino José da Cunha; http://lattes.cnpq.br/9909053957915090
Hyptis crenata (Pohl) ex Benth. is a herbaceous aromatic and medicinal plant, belongs to Lamiaceae, popularly known as salva-do-marajó, malva-do-marajó and hortelã-bravo. This plant is distributed since the mouth of Amazonas River, Marajó Island, Pantanal, and extending up to the states of Minas Gerais. Its essential oil is characterized by presence of monoterpenes and sesquiterpenes. The leaf tea is used as sudorific, tonic, stimulant, as well as to treat the eyes and throat inflammation, constipation and arthritis. Based in these information, we decided to evaluate the antinociceptive and anti-inflammatory activity of the oil (HcEO) of Hyptis crenata in mouse throught the following tests: abdominal constriction, hot plate, formalin, croton oil-induced ear edema, rat paw edema induced by dextran and carrageenan, carrageenan-induced peritonitis. The statistical method used in this study was ANOVA followed by multiple comparison (Student-Newman-Keuls test or Student t test). The essential oil was extracted by hydrodistillation, yield was 0,6% and their main components were monoterpenes (94,5%). The lethal dose (DL50) was 5000 mg/kg. In the abdominal constriction test, at doses of 250, 350 and 500 mg/kg, the HcEO inhibited the abdominal constrictions in 22,56%, 60,76% and 75,53%, respectively, in a dose-dependent manner when compared to the control group. The DE50 calculated was 364,22 mg/kg with a correlation coefficient of 0,9341. The oil not changed significantly the time of latency in the hot plate test. HcEO (364,22 mg/kg) caused an inhibition of the phase I in 26,42% and an inhibition of the phase II in 43,86% of the formalin test. Naloxone, an antagonist of opioid receptor, reverted the analgesic effect of EOHc. HcEO reduced croton oil-induced ear edema in 44,26%. In rat paw edema induced by dextran, HcEO produced inhibition at the dose of 364,22 mg/kg, but the rat paw edema induced by carrageenan this inhibition was not observed. In carrageenan-induced peritonitis, HcEo significantly decreased the leucocyte and neutrophil migration in 47,55% e 66,47%, respectively. Based on the results we are suggesting that the essential oil of H. crenata has an antinociceptive activity.It is probably as consequence of direct action on the nociceptive fiber, as well as the opioid system is involved in this effect. Further, our results suggest that anti-inflammatory activity of HcEO is probably of peripheral origin. It can be suggested, too, that the possible components responsible for these actions are the compounds monoterpenes presents in HcEO.
Acesso aberto (Open Access)
Caracterização química e físico-química e estudos preliminares de planejamento da formulação fitoterápica semi-sólida contendo tintura de Calendula officinalis L.
(Universidade Federal do Pará, 2008-12-29) NUNES, Kariane Mendes; SILVA JÚNIOR, José Otávio Carréra; http://lattes.cnpq.br/4437885351749994
The phytotherapy is a form of medicinal therapy that has been grown noticeably over the years, however, despite the broad use of phytomedicines, the quality of these drugs is often poor and questionable. Among the several medicinal plants used as herbal medicine, the Calendula officinalis L. is known for its anti-inflammatory, antiseptic and healing effects. Thus, this present study aimed to enhance and consolidate the use of methods of pharmaceutical technology in the development of phytotherapeutic agents, through the completion of preliminary studies of the planning of a semi-solid formulation phytotherapic containing tincture of Calendula officinalis L., for the quality control of the stages of their development. In the physical characterization and physical chemistry of the dust and tincture of calendula were obtained farmacognóstics specifications consistent with the literature, and to establish the identity of the plant material through the detection of the chemical marker rutin by Thin-Layer Chromatography (TLC). Through the validation of the method, that presented parameters recommended by existing legislation, was given 463 μg/mL of rutin in tincture. The infrared (IR) spectra showed characteristics of rutin in the lyophilised extract, in addition to demonstrate the permanence of these bands after mixing with the excipients of the formulation. The thermoanalytic techniques confirmed the compatibility between the excipients and lyophilisate of calendula extract. In the preliminary assessment of the stability of the gel formulation remained stable during the cycles in greenhouse (45 ± 2 0C) and temperature (25 ± 2 0C). In the preliminary study of the gel, permeation tended to favor the permeation of total flavonoids as rutin for receiving phase. These results demonstrate the importance of employment of protocols for quality control of raw materials plant, besides the establishment of technological methods for the production of phytotherapic.
Acesso aberto (Open Access)
Isoeleuterol e isoeleuterina: potenciais marcadores químicos da tintura de Eleutherine plicata Herb (Iridaceae) e atividades microbiológica e antioxidante
(Universidade Federal do Pará, 2008-12-30) MALHEIROS, Luiz Claudio da Silva; VIEIRA, José Maria dos Santos; http://lattes.cnpq.br/6807452375674442; BARBOSA, Wagner Luiz Ramos; http://lattes.cnpq.br/1372405563294070
Eleutherine plicata Herb. is an Iridaceae, popularly known as marupazinho, widely used by people to treat diarrhea. With the bulb of the plant is about a cup of tea, which is used to treat infestations caused by amoeba. The plant material used in this study was collected in Belém do Pará and their identification by comparison of botany was deposited in exsiccates Paraense Emilio Goeldi Museum under nº 10543. The ethanol extract was prepared by percolation from the bulb previously dried and crushed. After drying the ethanol extract was suspended in a solution hydroalcoholic (1:1) and subjected to partition with solvents of increasing polarity. With the ethanol extract and the fractions were performed eighteen tests to detect classes of secondary metabolites. The ethanol extract and the fractions hexanic and chloroform, showed a positive result for naphthoquinones, anthraquinones and steroids and triperpenoids. The analysis by thin-layer chromatography fractions of ethanol extract and hexane and chloroform, showed areas susceptible to methanolic solution of KOH 10%, indicating the presence of quinones in these samples. The evaluation of the antimicrobial activity of ethanol extract and fractions hexanic and chloroform with strains of C. albicans, S. aureus, E. coli and P. aeruginosa, showed that the chloroform fraction is the most active, presenting the largest halos of inhibition of microbial growth, possibly containing a higher concentration of active constituents. The chemical constituents isoeleutherol and isoeleutherine were isolated from chloroform fraction, and were characterized chemically using RMN 1H e 13C, compared with the literature. The ethanol extract, isoeleutherol and isoeleutherine were submitted to evaluation of their antioxidant activies, and showed weak activity when compared with BHT.
Acesso aberto (Open Access)
Isolamento e quantificação de flavonóides e abordagem das atividades antioxidante e antimicrobiana de Jatropha gossypiifolia L.
(Universidade Federal do Pará, 2008-12-30) VEIGA, Andrex Augusto Silva da; BARBOSA, Wagner Luiz Ramos; http://lattes.cnpq.br/1372405563294070
Jatropha gossypiifolia L (Euphobeaceae), known in Pará as “Pião roxo” is used for treatment of hemorroids, burns, stomach pains among other diseases, the importance of this plant to this region has led to its research in order to improve its phytotherapeutic development. During the analysis, the chromatographic profiles of its Crude Ethanolic Extract (CEE)was determined using Thin Layer chromatography (TLC) and High Performance Liquid Chromatography (HPLC) methods. The total and isolated flavonoids quantities were determined. Antimicrobial activity essays of the crude ethanolic extract were also conducted and the fractions obtained (hexanic, chloroform, ethyl acetate and residual fractions). The antioxidant activities of the extract and the fractions were also characterized. The plant materials were collected from EMBRAPA medicinal plants garden in the east Amazon and then extracted through percolation to obtain crude ethanolic extract. The dry extract was obtained using low pressure rotative evaporator followed by liquid-liquid partition with hexane, chloroform and ethyl acetate successively. The fractions obtained were also concentrated at low pressure, The ethyl acetate fractions were re-fractioned, giving rise to acetone fraction (ActF-II), a new ethyl acetate (AF-II), methanolic fraction (MF-II) and a solid residue (SR-II). ActF-II was submitted to liquid chromatography at average pressure, resulting in sub-fractions like Fr ActS-II and Fr ActS3-II called Jg1 and Jg2, respectively. Chemical prospection of the Extract and the metabolite fractions were conducted in triplicates, leading to the observation of the presence of the following polyphenols: Catechines, Tannins and flavonoids. The analysis by thin Layer Chromatography (TLC) was conducted using eluent of ethyl acetate/formic acid/glacial acetic acid/water at (100:11:11:26) on a normal phase silica gel, showing the retention factors in the following zones:0.65, 0.72, and 0.77 in reaction to Fecl3 solution . The HPLC chromatogram of ethanolic crude extract presented three significant peaks with average values of RT: 13.2 min, 15.02 min, and 16.00 min whose spectra are characteristics of flavonoids. On calculating the flavonoid quantity using the average absorbance reading (A=0.874), 2.02% flavonoid was found. The concentrations for each isolated substances was 340ug for Jg1 and 406 ug for Jg2 per milliliter of extract solution. Regarding the biological activity tested AF-1 and Fr-1 inhibited growths of S. aureus and C.albicans and also manifested a great antioxidant potential. These results provide adequate polyphenol parameters for quality control serving as chemical markers and their possible quantities.
Acesso aberto (Open Access)
Caracterização fitoquímica e avaliação da atividade anti-inflamatória e antinociceptiva do óleo fixo de Euterpe oleracea Mart.
(Universidade Federal do Pará, 2009) FAVACHO, Hugo Alexandre Silva; SOUSA, Pergentino José da Cunha; http://lattes.cnpq.br/9909053957915090; CARVALHO, José Carlos Tavares; http://lattes.cnpq.br/4251174810000113
Euterpe oleracea Mart. Is a typical palm tree from the Amazon, growing spontaneously in Pará and Amapá States, appreciated for its attractive beauty and for nutritional purposes. The fruit of Euterpe oleracea, commonly known as açaí, has been demonstrated to exhibit significantly high antioxidant capacity in vitro, and, therefore, may have possible health benefits. Phytochemical studies have revealed the presence of fatty acids, anthocyanins and steroids. The aim of this work was study the fatty oil of this species (OEO) on inflammatory and hyperalgesic models in vivo, in order to detect the possible involvement of its compounds on the inflammatory and algesic responses. The following experimental models were used: writing test in mouse, rat paw edema, granulomas testing rat, vascular permeability in rat, migration test in rats and ear erythema by croton oil in mice. The oral doses of 500, 1000 and 1500 mg/kg of OEO inhibited the number of writhes by 33,67%, 45,88% and 55,58%, respectively. The OEO produced dose-dependent effect, and the median effective dose (ED50) was 1226,8mg/kg, the OEO inhibited the inflammatory process by 29,18% on the 4 hour of the assay (edema peak) when compared to the untreated control. The daily administration of OEO for 6 days inhibited the granulomatous tissue formation in 36,66%. In the ear erythema by croton oil, the OEO, provoked the significant inhibitory effect of 37.9%. In the vascular permeability test, the OEO inhibited the vascular permeability in 54.5%. Pretreatment (60min) of rats with OEO significantly decreased neutrophil migration on carrageenan-induced peritonitis (with inhibition of 80.14%). The results suggest that OEO shows anti-inflammatory activity in both acute and chronic inflammatory processes, and analgesic activity, probably of peripheral origin.
Acesso aberto (Open Access)
Planejamento de novos derivados da Edaravona
(Universidade Federal do Pará, 2009-06-30) QUEIROZ, Auriekson Noronha; BORGES, Rosivaldo dos Santos; http://lattes.cnpq.br/4783661132100859
A detailed theoretical study of the edaravone was carried out by DFT method using B3LYP/6-31G* basis set, with the objective to clarify the scavenging mechanism and influence of edaravone tautomerism under acid condition, which will be helpful to elucidate the radical-scavenging mechanisms in the ischemic process. Previous theoretical studies, tautomerization, solvent effects, and electron abstraction no were considered. In this work, the stability and reactivity were determined through geometric and energetic parameters were realized in gas phase and PCM methods in water and methanol. The acid or basic conditions were considered by bond dissociation or protonation energies may undergo anion or cation products, respectively. The antioxidant properties were calculated through HOMO, ionization potential (IP), and bond dissociation energies (BDE). HOMO and IP values showed that N-H tautomer is better antioxidant by electron abstraction, while BDE values showed that O-H tautomer is better antioxidant by hydrogen abstraction. The protonation is thermodynamically more favored than deprotonation. Furthermore, the protonation energy explain, theoretical, the reduced difference between N and O protonation. The protonation is thermodynamically more favored than deprotonation. The solvent effect decreased energies barriers to isomerization in O-H or N-H tautomers. In addition, three pyrazolone derivatives were evaluated its antioxidant activities comparated to edaravone, in an effort to develop the evaluated and pharmacophore antioxidant identification. The antioxidant activity of antypirine, dypirone, phenylbuthazone and edaravone was determined measuring the inhibition of two stables free radical DPPH and ABTS. Edaravone and phenylbuthazone exhibited more potent inhibition of DPPH and ABTS radical scavenging than dypirone, while antypirine not shown activity in all concentrations analyzed. Simultaneously, the DFT method can provide an antioxidant potential value to explain the structure-activity relationship (SAR). Furthermore, was evaluated their antioxidant activities and the ionization potential, HOMO, BDE X-H, and stabilization energies (DEiso) of the compounds have been calculated using the density functional theory (DFT) method at the B3LYP level, employing the 6-31G(d) basis set, to explore the SAR. All calculations have been performed by using the Gaussian 03 program, Hyperchem 7.5, and ChemOffice 2005. The results showed that derivatives with C-H in 4-position increased electron or hydrogen abstraction. Finality, the general strategy employed to design the target compounds was based on the studies of eighteen derivatives of edaravone. The SAR studies supported the three groups, such as more active, active and less active. Nine compounds were design with successful based in the structure of more active.
Acesso aberto (Open Access)
Análises cromatográficas por CLAE-DAD, termogravimétricas e morfo-anatômicas de amostras comerciais de Echinodorus macrophyllus (Kunth) Micheli (Chapéu-de-couro)
(Universidade Federal do Pará, 2010) FREITAS, Cristian Barbosa de; BORGES, Fernanda Iikiu; BARBOSA, Wagner Luiz Ramos; http://lattes.cnpq.br/1372405563294070
For quality control of the commercial sample of Echinodorus macrophyllus were analyzed with botanical, pharmacognostic and physical-chemical properties. To achieve the anatomical cuts was rehydrated, sectioned with steel blade and fixed on slides semi-permanent. The sections were cleared in 20% NaClO and stained with astra blue-to-follow basic fuchsin. In cross section the epidermis is uniseriate with cells of rectangular shapes, heterodimensional, smooth and thin cuticle. For realization of thermogravimetry was used both drugs as solids at a heating rate of 5, 10 and 15 degrees Celsius. The chromatography was performed in HPLC and sample was obtained from column chromatography and eluted by gradient with methanol and acidic water. The palisade tissue consists of two layers of cells. The parenchyma spongy cells have thin walls, heterodimensional, different formats and well-developed intercellular spaces. The vascular bundles are collateral. The leaf is amphistomatic with stomata paracytic. Petiole in cross section, has a triangular to hexagonal. The epidermis is uniseriate with cells of polygonal shape, smooth walls, large amounts of aerenchyma which sometimes occur diaphragms. Samples of the leaf have characteristics of the species E. macrophyllus, but the anatomy of the petiole showed different structures from those described for the species, which belong to the genus Echinodorus, however suggests possible contamination of the material supplied with other plant species. Thermogravimetric analysis contributed significantly to establish parameters and characterize the sample.
Acesso aberto (Open Access)
Concentrações plasmáticas de primaquina e metemoglobinemia em pacientes com malária por Plasmodium vivax
(Universidade Federal do Pará, 2010) FERREIRA, Michelli Erica Souza; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
The vivax malaria is a disease that effects around 40% of the world, to treat it, chloroquine (150 mg) and primaquine (15 mg). This is an 8-aminoquinoline with tissue schizonticide action. Among the adverse effects enhance the capacity to hemoglobin oxidation, dose-dependent, which is exacerbated in individuals with glucose-6-phosphate dehydrogenase deficiency. When considering the lack of studies concerning the methemoglobin levels and its correlation with primaquine concentrations plasma in patients with vivax malaria, is justified this study using as tools to monitor the plasma primaquine concentrations and its correlation with methemoglobin levels. In this sense, it was followed up clinically and laboratory findings of 20 patients with vivax malaria before (D0) and after three (D3), seven (D7) and fourteen (D14) days starting the treatment, as well as validation of the method for primaquine determination by high performance liquid chromatography (HPLC). Methemoglobinemia was evaluated using the method of Hegesh et al. (1970) and glucose-6-phosphate dehydrogenase by colorimetric method of Brewer et al. (1962 ). The methodology validated was demonstrated efficient for primaquine determination, whose average levels at D3, D7 and D14 were 227 ± 106 ng / mL, 191 ± 97 ng / mL and 160 ± 128 ng/mL. In the analysis according to gender was not observed differences significant in the drug levels in several days of study. The average methemoglobin levels in D0, D3, D7 and D14 were 1.15 ± 0.9%, 4.1 ± 2%, 5.7 ± 2% and 3 ± 1.4%, respectively. There was an increase in the methemoglobin level after drug administration, without difference by gender. There was not significant correlation between the methemoglobin levels and primaquine concentrations plasma in both sexes. The coefficients of Pearson correlation for males and females were 0.8296 and 0.8137, respectively. We observed impaired expression of the enzyme glucose-6-phosphate dehydrogenase in six male patients without differences between the methemoglobin levels and primaquine concentrations plasma, compared with patients with expression normal of the enzyme.
Acesso aberto (Open Access)
Estudo teórico do mecanismo redox de derivados quinolínicos na atividade antimalárica
(Universidade Federal do Pará, 2010) SCALERCIO, Sarah Raphaella Rocha de Azevedo; BORGES, Rosivaldo dos Santos; http://lattes.cnpq.br/4783661132100859
Malaria is a serious public health problem worldwide, causing socioeconomic deficits and contributing to subdevelopment in affected countries. In this context is important to study electronic properties, quinoline derivatives antioxidant potential and antimalarial activity relationship to design effective antimalariais prototypes. In this dissertation are used molecular modeling methods to study antioxidant and antimalarial structure-activity relationships selecting moieties and eletronic and conformacional parameters to improve farmacological activity and decrease derivatives toxicity. The HOMO and PI values analysis indicates that imino-tautomer is, probably, better antioxidant than amino-tautomer. It also observed that tautomers equilibrium is favored to amino-quinoline in the gas phase, and in water and chloroform using PCM method, with energy barriers values to 10.78 Kcal/mol, 21.65 Kcal/mol and 22.04 Kcal/mol, respectively. Then, may be noted that in quinoline analogues derivatives the electron-donor groups decrease the ionization potential, as exemple of the amino group at 8-position replaced by an alkylamine group. In 4- 8- amino-quinoline derivatives association observed that presence of quinoline moiety second nitrogen decrease its antioxidant activity, except in the 5-position, representing the most prominent group in the reduction of ionization potential and probably high antioxidant activity.
Acesso aberto (Open Access)
Avaliação da atividade antiplasmódica in vitro dos óleos de Andiroba (Carapa guianensis Aubl.) e Pimenta-de-macaco (Piper aduncum L)
(Universidade Federal do Pará, 2010) MIRANDA JUNIOR, Raimundo Nonato Cardoso; DOLABELA, Maria Fâni; http://lattes.cnpq.br/0458080121943649; MAIA, José Guilherme Soares; http://lattes.cnpq.br/1034534634988402
In search of new antimalarial drugs, two typical species of the Amazon region and a fraction rich limonoids were the object of this study: Carapa guianensis Aubl. (Meliaceae), known popularly as andiroba traditionally used as an insecticide and fighting malaria, the species Piper aduncum L. (Piperaceae), known popularly as the pimento-de-macaco, used to treat inflammatory diseases and the fraction rich limonoids obtained from Carapa guianensis. Crude oil and fraction were tested in vitro using methods described by Rieckman and col. (1980) modified by Carvalho (1990) with Plasmodium falciparum clones W2 and Dd2. These studies showed that the oils had antiplasmodial activity, with a concentration of 0.82ng/mL and 8.2mg/mL andiroba oil showed an inhibition he W2 clone was 100% and Dd2 to 71% (IC50 9.4 μg/ml) after 72h of exposure respectively. For the fraction at a concentration of 3.1mg/mL, clone W2, was 100% and Dd2 to 82% (IC50 0.4 μg/ml), after 72h of exposure. The pimento-de-macaco oil overalls had a concentration of 1.30ng/mL for the W2 clone inhibition of 100% and the Dd2 to 77% after 72h of exposure to a concentration of 10.3mg/mL. The results with the chili oil overalls at a concentration of 1.30ng/ml the inhibition was 100% in clone W2 and Dd2 clone at a concentration of 10.3mg/mL, inhibition was 77% after 72h of exposure.
Acesso aberto (Open Access)
Estudos de pré-formulação e formulação de Heliotropium indicum (L.) DC (Boraginaceae)
(Universidade Federal do Pará, 2010-01-14) COSTA, Russany Silva da; SILVA JÚNIOR, José Otávio Carréra; http://lattes.cnpq.br/4437885351749994
Heliotropium indicum L. (Boraginaceae) is a shrub, reaches up to 70 cm high. It is known as “fedegoso” in the north and northeast of Brazil. Because of the biological potential of this species, this work aims to determine the quality parameters of the vegetable drug to the final product and evaluate the antimicrobial activity of the leaves of H. indicum L. The purpose of obtaining a phytotherapic formulation semisolid, we used the parameters of quality control physical, chemical and physicalchemical described in the Brazilian Pharmacopoeia and others literature. The vegetable drug was classified as coarse powder, showed values of loss on drying and total ash of 12.88% and 17.14%, respectively. The thermogravimetric analysis of the powder and the extract showed that both had good physical stability up to 180 °C. The spectra in the region IR showed an increase in the intensity of the absorption bands of the extract, which may relates to the extraction of chemical constituents of the cellular matrix. The prospecting chemical extract confirmed the presence of classes of secondary metabolites already reported in literature. The chloroform fraction suggests the presence of alkaloids by precipitation test with Dragendorff reagent. The TLC and HPLC showed a possible presence of the same substance in the alkaloidal and hexane fractions. The crude extract inhibited the growth of Staphylococcus aureus with halos of 12.5 mm ± 0.707 and 10.5 ± 0.707 mm for concentrations of 500 and 250 mg / mL, respectively. The physical mixtures of the extract with adjuvant pharmaceutical used to develop the phytotherapic formulation showed no physical incompatibility and no significant changes in the absorption profile of the compounds analyzed. The phytotherapic formulation semi-solid has a good stability after the preparation, after the submission of the gel by centripetal force and after the action of heat stress.
Acesso aberto (Open Access)
Estudos de pré-formulação e formulação de Vismia guianensis (Aubl.) Choisy
(Universidade Federal do Pará, 2010-01-15) CAMELO, Sarah Regina Pereira; VASCONCELOS, Flávio; http://lattes.cnpq.br/3695753129639448; SILVA JÚNIOR, José Otávio Carréra; http://lattes.cnpq.br/4437885351749994
The obtention and evaluation of a new herbal formulation from Vismia guianensis (Aubl.) Choisy was determined by parameters of quality control. Physical-chemical characterization in plant raw material dried and crushed, its extract of the tincture and semi-solid formulation with antimicrobial activity. For the characterizations specific parameters for herbal drugs contained in the Brazilian Pharmacopoeia 4th Ed were used, the thermal analysis: thermogravimetry, differential thermal analysis and differential scanning calorimetry and infrared and ultraviolet spectroscopy. The evaluation of the antimicrobial activity by the disk diffusion method in solid identified the sensitivity of S. aureus (ATCC 25923) to the dried extract dissolved in DMSO at concentrations of 500, 250, 125 and 62.5 mg / mL. The HPLC drawing the profile of the composition of the sub-fractions A and B from the ethyl acetate fraction of the tincture and showed the range of maximum absorption at 290 nm similar to the maximum capacity of emodin being used a reference standard and an external marker. The method validation was performed by ultraviolet spectrophotometry, demonstrating a selective method, linear, repeatable and robust. Thermal analysis showed possible incompatibilities between the binary mixture of the extract of the tinsture with hydroxyethylcellulose and propylene, then obtaining non-homogeneous gel due to precipitation of proteins, triggered by the polyphenol-protein interaction. A preliminary evaluation of the stability of the formulation obtained remained within the normal parameters, show results within acceptable limits for the centrifuge tests, thermal stress and organoleptic characteristics.
Acesso aberto (Open Access)
Acetilbergenina: obtenção e avaliação das atividades antinociceptiva e anti-inflamatória
(Universidade Federal do Pará, 2010-01-22) BORGES, Jaqueline Cibene Moreira; SOUSA, Pergentino José da Cunha; http://lattes.cnpq.br/9909053957915090; SANTOS, Lourivaldo da Silva; http://lattes.cnpq.br/3232898465948962
Endopleura uchi (Huber) Cuatrec. (Humiriaceae), a Brazilian Amazon plant, commonly known as “uxi”, is used in folk medicine for the treatment of several pathologies, such as arthritis. Bergenin, one of the chemical constituents of E. uchi, has several biological activities, including anti-inflammatory and antinociceptive activities. In order to obtain a more potent derivative than bergenin it has decided to acetyl this substance. Acetylbergenin was tested in nociception and inflammation models. Bergenin was isolated from the chromatographic fractionation of aqueous extract from stem bark of E. uchi and the acetylbergenin was obtained by acetylation of bergenin. The substances were identified based on spectral analysis of 1H NMR, 13C NMR, DEPT and COSY, and comparison with literature data. For nociception models were carried out the abdominal writhing test, hot plate test and formalin test, while in the inflammation models were carried out the croton oil-induced ear edema, rat paw edema induced by carrageenan and dextran, carragenin-induced peritonitis test. Furthermore, the model of gastric ulcer induced by stress was used to assess the potential ulcerogenic of the substance. In the abdominal writhing test induced by acetic acid 0.6%, acetilbergenin doses of 1, 5, 10, 15 and 25 mg / kg blocked the number of writhing in 28.2%, 52.7%, 61.1 %, 68.3% and 95.0%, respectively, and dose-dependent manner when compared to the control group. The calculated ED50 was 6.8mg/kg. In the hot plate test (55ºC), acetylbergenin (6.8 mg/kg) did not induce alterations in the latency time when compared to the control group. In the formalin test, acetylbergenin (6.8mg/kg) inhibited 88.30% the algic stimulus in the second phase (inflammatory) compared to the control group. Furthermore, naloxone reversed the effect of acetylbergenin the second phase of this test. In the croton oilinduced dermatitis, acetylbergenin (6.8 mg/kg) provoked inhibitory effect in 75.60% in comparison to the control group. In the paw edema induced by carrageenan, acetylbergenin (6.8 mg/kg) was able to reduce the development of edema from the 2nd to the 5th hours compared to the control group. In the paw edema induced by dextran, acetylbergenin (6.8 mg/kg) reduced edema at all times. In carragenininduced peritonitis, acetylbergenin (6.8mg/kg) blocked 70% of the neutrophils number compared to the control group. In the trial of gastric ulcer, acetylbergenin blocked 78.55% in the generation of gastric lesions by stress when compared to indomethacin. The results suggest that acetylbergenin has an antinociceptive and anti-inflammatory activity which, according to the tests employed, is probably of peripheral origin.
Acesso aberto (Open Access)
Contribuição para o estudo microquímico e anatômico da casca e validação de um método espectrofotométrico para quantificação de alcalóides totais de Himatanthus lancifolius (Muell. Arg.) Woodson
(Universidade Federal do Pará, 2010-01-22) BARROS, Patricia Miriam Sayuri Sato; BORGES, Fernanda Iikiu; BARBOSA, Wagner Luiz Ramos; http://lattes.cnpq.br/1372405563294070
For the registration of phytomedicines and their availability to the users, ANVISA establishes quality, security and effectiveness parameters, stipulating control requirements similar to that ones applied to synthetic medicines. This work reports the investigation of the bark of Himatanthus lancifolius and its extracts aiming to contribute for the standardization of derivatives of this plant species, the assays were developed using commercial samples Q and S, and an authentic one provided by EMBRAPA – E. The microchemical, anatomical and chromatographic comparison of Q, S and E does not allow characterising both the commercial sample as H. lancifolius. The presence of ulein could not be characterised in any sample, even in E. The TLC and HPLC data show that the three samples have different chromatographic profile. The morphological and the microchemical characterisation of the barks of H. lancifolius shows cortex with groups of fibres of the primary phloem included, with crystals and lactifers in the region of the secondary phloem. The developed quantification method shows high selectivity at 281nm, what confers confidence for the detection of the alkaloids. The method is robust, according to the current regulation, and shows linearity, precision and accuracy, beside accessibility and is easy to execute. The total alkaloid fraction present in the aqueous extract of the collected sample (E) represents 0,219% of the dried extract. The author expects to have contributed for reducing the lack of methods for the quality control of phytomedicines from Himatanthus lancifolius.