https://ri.ufs.br/jspui/handle/riufs/2447 2026-04-25T18:02:11Z https://ri.ufs.br/jspui/handle/riufs/12226 Título: Derivados p-Mentânicos : estudos de relação estrutura-atividade e avaliação de novos candidatos a agentes antitumorais Autor(es): Andrade, Luciana Nalone Abstract: Cancer is a disease of high incidence, high mortality and difficult to treat, and there is therefore a constant social interest in the search for more effective therapies. In this sense, essential oils and their constituents are promising source of natural products as antitumor substances. Thus, the aim of this study was to evaluate the cytotoxic activity of 19 p-menthane derivatives structurally correlated with perillyl alcohol against three strains of human tumor cells: ovarian adenocarcinoma (OVCAR-8), colon carcinoma (HCT-116) and glioblastoma (SF-295) using the colorimetric MTT assay. The tests were performed in triplicate in a single concentration of 25 μg/ml. The results demonstrated that all substances tested were less cytotoxic than the perillyl alcohol, with the exception of 1,2-perillaldehyde epoxide (EP-1) and 8,9-periallaldehyde epoxide (EP-2) (IG = 95.66 to 99.89%) and IC50 ranging from 2.68 to 3.92 and 1.03 to 1.75 mg/ml, respectively. The perillyl benzoate was the least cytotoxic substance, with a value (GI = 2.86 to 5.02%). The monoterpenes (+)-limonene epoxide, (-)-hydroxy-carvone (-HC) and perillaldehyde had intermediate cytotoxic activity, with (IG = 58.40 to 94.01%). Given these results, the structural characteristics that can contribute to understand the cytotoxicity of perillyl alcohol and its analogs were identified. In general, substitution of C-C double bonds per epoxide groups added to the aldehyde group increased cytotoxicity. The presence and location of ketone and epoxide groups in p-menthane skeleton influence the cytotoxic activity. The addition of hydroxyl groups in the chemical structure resulted in less cytotoxic compounds, as was the case of the cis-carveol and sobrerol. As well, acetylation of such groups led to an overall decrease in cytotoxicity, indicating that lipophilicity plays a major role in the decrease of cytotoxic activity. In addition, the enantioselectivity to perform an important role in the cytotoxicity of natural compounds, as observed for (-)- and (+)-hydroxy-carvone. These results demonstrate that different functional groups and their positions in p-menthane skeleton influence the cytotoxic activity. Next was evaluated the in vivo antitumor activity of the compounds EP-1, EP-2 and (-HC) in Sarcoma 180-bearing mice (S180). In this test, the administration of EP-1 and EP-2 (100 or 200 mg/kg/day) inhibited the development in S180-inoculated mice. The inhibition was 33.4 and 56.4% for EP-1 and 38.4 and 58.7% for EP-2 at both doses, respectively. Already (-HC) (50 or 100 mg/kg/day) showed no antitumor activity in vivo. There were no changes in biochemical parameters in animals treated with EP-1 and EP-2. In relation to hematological analysis, these compounds showed a reduction in the number of total leukocytes and alterations in the differential count, a result expected as due to S180 tumor. The mechanism of action of EP-1 and EP-2 were then studied. None of the compounds tested induced hemolysis. The viability of HL-60 cells was affected by both monoterpenes after an exposure period of 24h, when analyzed by trypan blue exclusion. Both EP-1 and EP-2 reduced the number of viable cells associated with an increase in the number of non-viable cells, which contributes to the increased number of dead cells in the morphological analysis. The incorporation of ethidium bromide/acridine orange, the treated cells, cytotoxicity suggests apoptosis and necrosis pathway. Therefore, front of results, can conclude that EP-2 was more potent in vitro compared to EP-1, however, both substances showed cytotoxic activity through apoptotic and necrotic processes. These data suggest that EP-1 and EP-2 present a potential and promising anticancer potential and moreover, appropriate structural modifications are possible to develop novel anticancer agents. 2015-07-24T00:00:00Z https://ri.ufs.br/jspui/handle/riufs/3308 Título: Prospecção tecnológica de óleos essenciais de Schinus terebinthifolius e desenvolvimento de um creme vaginal à base de Ocimum basilicum para tratamento de candidíase Autor(es): Almeida, Mônica Batista de Abstract: Vaginal candidiasis is a disease with high prevalence in adult women. This study aimed to : ( i ) assess the antiCandida activity of essential oil ( EO ) of S. terebinthifolius front lines of cases of recurrent vaginal candidiasis ; ( II ) produce a antiCandida vaginal cream from OE O. basilicum and evaluate the technological process and this cream antiCandida activity in vitro . The major compounds of OE leaves and dried fruits of S. Terebinthifolius were, respectively, the (+) - camphene (20.1%) and R- ? - pinene (22.1%). In terms of minimum inhibitory concentration (MIC ) and minimum fungicidal , OE Fruit S. terebinthifolius showed bands between 25-200 mg / ml , demonstrating activity against C. parapsilosis ( ATCC 22019 ) and a clinical strain , C. albicans (ATCC 18804) and C. glabrata (ATCC 2001) , not being active on these clinical isolates. Regarding OE leaves, no significant action was observed. The OE dried fruit showed fungistatic , however , no fungicide both OE action, in contrast, leaves and fresh fruits showed antiCandida activity, unless the standard strain of C. glabatra the essential oil from fresh fruits . The major compound of OE O. basilicum (Maria - Bonita) was linalol (72.08%). MIC values ranged between this SO 0.78 to 1.56 mg / ml. Before its antifungal action, was produced a vaginal cream. The samples were stored in these distinct conditions: controlled, refrigerator and oven temperature. In controlled and cooler temperatures, no changes in the formula, however, samples at 45 ° C showed slight changes in texture from the 15th day. It can be concluded that the EO of dried leaves and fruits of S.terebinthifolius Raddi not have antiCandida activity, however, the EO extracted from fresh material Botanical demonstrate such activity . The O. basilicum presents antiCandida action. Tests for antimicrobial activity of vaginal cream in its various concentrations showed satisfactory results compared to a synthetic antifungal.Keywords: Vaginal candidiasis, essential oils, Candida spp., Schinus terebinthifolius Raddi, Ocimum basilicum, vaginal cream, anti-candida. 2013-04-19T00:00:00Z https://ri.ufs.br/jspui/handle/riufs/3305 Título: Processo biotecnológico para obtenção dos compostos 2-feniletanol, acetato de 2-feniletil e B-cariofileno pela utilização de resíduo de goiaba Autor(es): Galvão, Mércia de Sousa Abstract: The increasing demand for flavors in the world market requires new strategies for obtaining these compounds which can be produced via fermentation processes using low cost substrates such as agroindustrial residues. This turns out to be a viable process and the aroma compounds generated are classified as natural. Large volumes of waste in the form of bagasse, husks, kernels or seeds including from the processing of fruit pulp are generated and these can be used as substrates in these fermentations. Thus the main purpose of this work was to use agro-industrial residues for the production of volatile aroma compounds by fermentation processes. In this regard, we investigated the potential of the production of volatile compounds by submerged fermentation using guava, passion fruit and umbu processing waste as substrates using endophytic microorganisms isolated from guava, passion fruit and umbu as well as by using the pure cultures (Aspergillus niger, Kluyveromyces marxianus and Kluyveromyces lactis) to produce volatile compounds characteristic of fruity or floral aroma. Initially the fruit pulp and wastes from the processing of guava, passion fruit and umbu were chemically characterized (moisture, ash, fiber, proteins, lipids, sugars, titratable acidity, Aw, pH and soluble solids). Fermentation with different microorganisms in synthetic medium was performed and the fermented products analyzed for aroma note. From the results of this sensory analysis, the guava residue and the yeast Kluyveromyces lactis were selected since these constituents in the medium produced fruity and floral aromas. The volatile compounds produced were captured by two headspace techniques (SPME and Purge & Trap) and analyzed in a system of gas chromatography coupled to mass spectrometry. Sixty-two microorganisms were isolated and out of these six were selected. The fermented products were analyzed for pH, soluble solids and reducing sugars as well as to establish the kinetics of the fermentation process at every 24 hours for five days. The main aroma descriptors in the fermented products were fruity, honey, fruity green, plum, guava, banana and alcohol type notes. Forty-three volatile compounds were detected in the fermented product obtained by using the Guava residue in the medium. Among the compounds identified were: Ò {caryophyllene, 2-phenylethyl acetate, × n- humulene, bisabolene, humulene, 3-methyl butanol, bergamoteno, × n-cadinene, caryophyllene oxide and 2-phenylethanol. The production of volatile compounds was quite rapid and in most cases, this production occurred on the first day of fermentation and had achieved its maximum concentration between 24-48h of fermentation. According to the response surface method analysis, the conditions of the manufacturing process were optimized. Increased production of 2- phenylethyl acetate was achieved at concentrations varying from 25 and 35g/L of yeast extract, 40 to 60 g/L glucose. Ò-caryophyllene was obtained at concentrations varying between 120 and 140g/L of guava waste, and an agitation performed between 160 and 180 rpm. The production of 2-phenylethanol was obtained at agitation varying from 228rpm and 5g/L glucose. From these optimized conditions, scale-up of fermentation was performed in a bioreactor wherein 6 times larger concentration of 2-phenylethanol and Ò-caryophyllene compounds, and 1.5 times higher concentration of 2-phenylethyl acetate were obtained. This study reveals that guava residue can be used to produce aroma compounds of great importance for the flavor and fragrance industry, the compounds being 2-phenylethyl acetate, 2-phenylethanol and Ò -caryophyllene. 2014-02-28T00:00:00Z https://ri.ufs.br/jspui/handle/riufs/3303 Título: Estudo das propriedades farmacológicas e toxicológicas do óleo essencial de cymbopogon winteranus em roedores Autor(es): Leite, Bárbara Lima Simioni Abstract: The genus Cymbopogon (Poaceae) is composed of more than 100 species found in tropical countries, and about 56 species have essential oils with aromatic characteristics and some ones have mediinal, pharmaceutical and industrial importance. The essential oils of the genus are rich in mono-and sesquiterpenes. Among the species of the genus Cymbopogon winterianus Jowitt, popularly known as |citronella|, |Java citronella| or |jacapé| is used in folk medicine as a repellent, antimicrobial, analgesic, anxiolytic and for the treatment of epilepsy. The aim of this study was to evaluate pharmacological and toxicological properties of the essential oil extracted from the leaves of Cymbopogon winterianus (EOC) in experimental protocols. Analysis by GC-MS showed the major components are citronellal, citronellol and geraniol. In pharmacological screening the main changes observed were: ptosis, sedation and decreased ability to raise. In the test of acute toxicity LD 50 was calculated in 1953.8 mg / kg (1580.9 to 2326.7) (p.o.) and in 567.3 mg / kg (395.8 to 758.2) (ip). The OEC decreased the number of crossings in the test of spontaneous movement and increased the sleep time induced by thiopental. In the the rota-rod task EOC did not interfere the motor coordination of the animals. Antinociceptive, anti-inflammatory and antioxidant effects were performed using the tests of writhing induced by acetic acid, nociception induced by formalin into the paw hot plate, the carrageenan-induced inflammation and sequestering activity of free radicals (DPPH). The results showed that the OEC reduced the response to pain, the migration of neutrophils to the abdominal cavity and is very efficient in sequestering the free radicals. In the evaluation of acute and subchronic toxicity, the animals were treated respectively with EOC in a single dose (900 mg / kg - po) and daily doses of 50mg/kg (po). In the acute test, the main behavioral changes were ptosis, sedation, decreased response to touch, decreased ability to raise and analgesia. No changes suggestive of toxicity in acute and subchronic tests were found in the assessment of body weight, water intake and feed and organ weights. In the evaluation of biochemical parameters, there were significant changes in the dosage of aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase (p <0.05) in both acute and subchronic tests. The results together suggest that EOC possess depressant, antinociceptive, antiinflammatory and antioxidant properties without loss of motor coordination. In addition, EOC showed toxicity, since histological changes were found in kidney and liver in the acute assay and in liver in the subchronic assay. 2012-03-12T00:00:00Z