RESUMO
Trichomonas tenax is an oral protozoan with an estimated global pooled prevalence of 17% in the human population.1 Observational studies have demonstrated a significant statistical correlation between oral colonization by T. tenax and the progression of periodontal disease.2 Proposed pathogenic mechanisms for this protozoan include the production of tissue-damaging enzymes, induction of apoptosis in human cells, and dysbiosis of the oral microbiome.3 In patients for whom metronidazole (MTZ) is contraindicated, phytochemicals may offer a viable alternative for controlling T. tenax. Various plant extracts have shown promising in vitro activity against other trichomonads, such as T. vaginalis and Tritrichomonas foetus, as reviewed by Friedman et al.4.
Assuntos
Compostos Fitoquímicos , Trichomonas , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Trichomonas/efeitos dos fármacos , Tricomoníase/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Antiprotozoários/farmacologia , Antiprotozoários/uso terapêuticoRESUMO
BACKGROUND: We previously reported that the tomato glycoalkaloid tomatine inhibited the growth of Trichomonas vaginalis strain G3, Tritrichomonas foetus strain D1, and Tritrichomonas foetus-like strain C1 that cause disease in humans and farm and domesticated animals. The increasing prevalence of antibiotic resistance requires development of new tools to enhance or replace medicinal antibiotics. METHODS: Wild tomato plants were harvested and divided into leaves, stems, and fruit of different colors: green, yellow, and red. Samples were freeze dried and ground with a handheld mill. The resulting powders were evaluated for their potential anti-microbial effects on protozoan parasites, bacteria, and fungi. A concentration of 0.02% (w/v) was used for the inhibition of protozoan parasites. A high concentration of 10% (w/v) solution was tested for bacteria and fungi as an initial screen to evaluate potential anti-microbial activity and results using this high concentration limits its clinical relevance. RESULTS: Natural powders derived from various parts of tomato plants were all effective in inhibiting the growth of the three trichomonads to varying degrees. Test samples from leaves, stems, and immature 'green' tomato peels and fruit, all containing tomatine, were more effective as an inhibitor of the D1 strain than those prepared from yellow and red tomato peels which lack tomatine. Chlorogenic acid and quercetin glycosides were present in all parts of the plant and fruit, while caffeic acid was only found in the fruit peels. Any correlation between plant components and inhibition of the G3 and C1 strains was not apparent, although all the powders were variably effective. Tomato leaf was the most effective powder in all strains, and was also the highest in tomatine. S. enterica showed a minor susceptibility while B. cereus and C. albicans fungi both showed a significant growth inhibition with some of the test powders. The powders inhibited growth of the pathogens without affecting beneficial lactobacilli found in the normal flora of the vagina. CONCLUSIONS: The results suggest that powders prepared from tomato leaves, stems, and green tomato peels and to a lesser extent from peels from yellow and red tomatoes offer potential multiple health benefits against infections caused by pathogenic protozoa, bacteria, and fungi, without affecting beneficial lactobacilli that also reside in the normal flora of the vagina.
Assuntos
Antitricômonas/farmacologia , Antitricômonas/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Solanum lycopersicum/química , Solanum lycopersicum/parasitologia , Tricomoníase/tratamento farmacológico , Animais , California , Gatos/parasitologia , Bovinos/parasitologia , Feminino , Frutas/química , Humanos , Masculino , Folhas de Planta/química , Caules de Planta/química , Trichomonas/efeitos dos fármacosRESUMO
Potato peel, a waste product of the potato processing industry, is high in bioactive compounds. We investigated the in vitro antitrichomonad activity of potato peel powders prepared from commercial Russet, red, purple, and fingerling varieties as well as several known potato components, alkaloids and phenolic compounds, against three pathogenic strains of trichomonads. Trichomonas vaginalis is a sexually transmitted protozoan parasite that causes the human disease trichomoniasis. Two distinct strains of the related Tritrichomonas fetus infect cattle and cats. The glycoalkaloids α-chaconine and α-solanine were highly active against all parasite lines, while their common aglycone solanidine was only mildly inhibitory. α-Solanine was several times more active than α-chaconine. The phenolic compounds caffeic and chlorogenic acids and quercetin were mildly active against the parasites. Most of the potato peel samples were at least somewhat active against all three trichomonad species, but their activities were wide-ranging and did not correspond to their glycoalkaloid and phenolic content determined by HPLC. The two Russet samples were the most active against all three parasites. The purple potato peel sample was highly active against bovine and mostly inactive against feline trichomonads. None of the test substances were inhibitory toward several normal microflora species, suggesting the potential use of the peels for targeted therapeutic treatments against trichomonads.
Assuntos
Alcaloides/farmacologia , Antiprotozoários/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Solanum tuberosum/química , Tricomoníase/microbiologia , Trichomonas/efeitos dos fármacos , Animais , Doenças do Gato/tratamento farmacológico , Doenças do Gato/parasitologia , Gatos , Bovinos , Doenças dos Bovinos/tratamento farmacológico , Doenças dos Bovinos/parasitologia , Cromatografia Líquida de Alta Pressão , Tubérculos/química , Trichomonas/crescimento & desenvolvimento , Tricomoníase/tratamento farmacológicoRESUMO
1. This study was designed to evaluate the antitrichomonal effects of P. harmala alkaloid extract against T. gallinae, both in vitro and in vivo, as well as comparing it to that of metronidazole, conventional antitrichomonal medication and harmine and harmaline, the two alkaloids present in P. harmala. 2. T. gallinae were collected by the wet mount method from infected free-living pigeons. The in vitro assay was performed using multi-well plates containing test compounds in final concentrations of 5, 10, 15, 20, 30, 50 or 100 µg/ml. The in vivo assay was done on 60 experimentally infected pigeons dosed with metronidazole at 50 mg/kg body weight (BW) or alkaloids at 25 mg/kg BW. 3. The 24 h minimum inhibitory concentration (MIC) of alkaloid extract was 15 µg/ml while that of metronidazole was 50 µg/ml. Harmine and harmaline revealed 24 h MIC of 30 and 100 µg/ml, respectively. Treatment of infected pigeons with alkaloids led to a full recovery after 3 d but with metronidazole total eradication of trophozoites was not achieved. 4. In conclusion, data of the present study suggested P. harmala is a potent natural anti-trichomonal agent, effective against T. gallinae.
Assuntos
Antitricômonas/farmacologia , Doenças das Aves/tratamento farmacológico , Columbidae , Peganum/química , Extratos Vegetais/farmacologia , Tricomoníase/veterinária , Animais , Harmalina/farmacologia , Harmina/farmacologia , Metronidazol/farmacologia , Trichomonas/efeitos dos fármacos , Tricomoníase/tratamento farmacológicoRESUMO
Assuntos
Humanos , Artemisia absinthium/química , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Trichomonas/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacos , Linhagem Celular , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis/isolamento & purificação , Extratos Vegetais/isolamento & purificaçãoRESUMO
Artemisia absinthium is an aromatic and medicinal plant of ethnopharmacological interest and it has been widely studied. The use ofA. absinthium based on the collection of wild populations can result in variable compositions of the extracts and essential oils (EOs). The aim of this paper is the identification of the active components of the vapour pressure (VP) EO from a selected and cultivated A. absinthium Spanish population (T2-11) against two parasitic protozoa with different metabolic pathways: Trypanosoma cruzi and Trichomonas vaginalis. VP showed activity on both parasites at the highest concentrations. The chromatographic fractionation of the VP T2-11 resulted in nine fractions (VLC1-9). The chemical composition of the fractions and the antiparasitic effects of fractions and their main compounds suggest that the activity of the VP is related with the presence of trans-caryophyllene and dihydrochamazulene (main components of fractions VLC1 and VLC2 respectively). Additionally, the cytotoxicity of VP and fractions has been tested on several tumour and no tumour human cell lines. Fractions VLC1 and VLC2 were not cytotoxic against the nontumoural cell line HS5, suggesting selective antiparasitic activity for these two fractions. The VP and fractions inhibited the growth of human tumour cell lines in a dose-dependent manner.
Assuntos
Artemisia absinthium/química , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Trichomonas/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacos , Linhagem Celular , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Óleos Voláteis/isolamento & purificação , Extratos Vegetais/isolamento & purificaçãoRESUMO
Trichomonas gallinae is the causative agent of canker in pigeon. This work was carried out to investigate in the vitro and in vivo efficacy of aqueous water extract of garlic (AGE) on the growth of T. gallinae infecting pigeons compared to those of metronidazole (MTZ). MTZ and AGE were added, at different concentrations, to glucose-serum broth medium containing 1 × 10(4) trophozoites/ml. In the in vivo experiment, 48 squabs were grouped into four groups. The first group (gr. I) was not infected and not treated. Each squab of the other group was infected with 1 × 10(4) trophozoites. The second group (gr. II) was infected and not treated. On day 0, the third group (gr. III) was treated with MTZ (50 mg/kg BW) and the fourth group (gr. IV) was treated with AGE (200 mg/kg BW) for seven successive days in drinking water. In vitro study revealed that the MLC, 24, 48, and 72 h post treatment were 50, 25, and 12.5 µg/ml, respectively, for MTZ and 75, 50, and 50 mg/ml, respectively, for AGE. Garlic (200 mg/kg BW) had the highest antitrichomonal effect and shortened course of treatment of pigeons from 7 days in gr. III to 5 days. Squabs in gr. II suffered from macrocytic hypochromic anemia, whereas squabs in grs. III and IV showed normal blood pictures. Serum total protein, albumin, and globulin were increased, whereas AST, ALT, and the total cholesterol were decreased in grs. III and IV when compared to those of gr. II. Pigeons protected with AGE showed increased body weight and reduced mortality percentage than the other groups. Our results indicated that garlic may be a promising phytotherapeutic agent for protection against trichomoniasis in pigeons.
Assuntos
Antitricômonas/farmacologia , Columbidae/parasitologia , Alho/química , Metronidazol/farmacologia , Extratos Vegetais/farmacologia , Tricomoníase/veterinária , Animais , Doenças das Aves/tratamento farmacológico , Trichomonas/efeitos dos fármacos , Tricomoníase/tratamento farmacológico , Trofozoítos/efeitos dos fármacosRESUMO
In our presented research, we made an attempt to predict the 3D model for cysteine synthase (A2GMG5_TRIVA) using homology-modeling approaches. To investigate deeper into the predicted structure, we further performed a molecular dynamics simulation for 10 ns and calculated several supporting analysis for structural properties such as RMSF, radius of gyration, and the total energy calculation to support the predicted structured model of cysteine synthase. The present findings led us to conclude that the proposed model is stereochemically stable. The overall PROCHECK G factor for the homology-modeled structure was -0.04. On the basis of the virtual screening for cysteine synthase against the NCI subset II molecule, we present the molecule 1-N, 4-N-bis [3-(1H-benzimidazol-2-yl) phenyl] benzene-1,4-dicarboxamide (ZINC01690699) having the minimum energy score (-13.0 Kcal/Mol) and a log P value of 6 as a potential inhibitory molecule used to inhibit the growth of T. vaginalis infection.
Assuntos
Antitricômonas/farmacologia , Antitricômonas/uso terapêutico , Cisteína Sintase/antagonistas & inibidores , Cisteína Sintase/química , Simulação de Dinâmica Molecular , Tricomoníase/tratamento farmacológico , Trichomonas/enzimologia , Domínio Catalítico , Cisteína Sintase/metabolismo , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Ligação de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas/efeitos dos fármacos , Ligantes , Reprodutibilidade dos Testes , Software , Especificidade por Substrato/efeitos dos fármacos , Termodinâmica , Trichomonas/efeitos dos fármacos , Interface Usuário-ComputadorRESUMO
Eugenia uniflora, used ethnomedically in some tropical countries as an anti-infective, has shown anti-malarial and anti-trypanocidal activities. Therefore using bioactivity guided fractionation, anti-trichomonal activity of E. uniflora leaf was investigated. Anti-trichomonal activities of leaf methanol extract and its fractions against Trichomonas gallinae as well as their cytotoxicities using an in vitro haemaglutination assay were determined. Anti-trichomonacidal activities of the extract improved on purification up to a stage. Subfractions E(2-5) had LC(50) and LC(90) values of 4.77 - 5.28, 18.49 - 25.00 and 4.53 - 5.18, 18.32 - 19.07 µg/ml at 24 and 48 hrs, respectively that were better than those of metronidazole. Further purification of E(2-5) led to loss of activity suggesting that the active components were probably working synergistically and additively. Demonstration of low haemaglutination titre values of 0.00 - 5.33 by methanolic extract and its partition fractions suggested their low toxicity profile. The established safety of the leaf indicated that its anti-trichomonal activity was not due to non-specific cytotoxicity, hence could be used in ethnomedicine as an anti-trichomonal agent.
Assuntos
Antitricômonas/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Folhas de Planta , Syzygium , Trichomonas/efeitos dos fármacos , Animais , Dose Letal MedianaRESUMO
Many drugs with very different affinity to a large number of receptors are described. Thus, in this work, we selected drug-target pairs (DTPs/nDTPs) of drugs with high affinity/nonaffinity for different targets. Quantitative structure-activity relationship (QSAR) models become a very useful tool in this context because they substantially reduce time and resource-consuming experiments. Unfortunately, most QSAR models predict activity against only one protein target and/or they have not been implemented on a public Web server yet, freely available online to the scientific community. To solve this problem, we developed a multitarget QSAR (mt-QSAR) classifier combining the MARCH-INSIDE software for the calculation of the structural parameters of drug and target with the linear discriminant analysis (LDA) method in order to seek the best model. The accuracy of the best LDA model was 94.4% (3,859/4,086 cases) for training and 94.9% (1,909/2,012 cases) for the external validation series. In addition, we implemented the model into the Web portal Bio-AIMS as an online server entitled MARCH-INSIDE Nested Drug-Bank Exploration & Screening Tool (MIND-BEST), located at http://miaja.tic.udc.es/Bio-AIMS/MIND-BEST.php . This online tool is based on PHP/HTML/Python and MARCH-INSIDE routines. Finally, we illustrated two practical uses of this server with two different experiments. In experiment 1, we report for the first time a MIND-BEST prediction, synthesis, characterization, and MAO-A and MAO-B pharmacological assay of eight rasagiline derivatives, promising for anti-Parkinson drug design. In experiment 2, we report sampling, parasite culture, sample preparation, 2-DE, MALDI-TOF and -TOF/TOF MS, MASCOT search, 3D structure modeling with LOMETS, and MIND-BEST prediction for different peptides as new protein of the found in the proteome of the bird parasite Trichomonas gallinae, which is promising for antiparasite drug targets discovery.
Assuntos
Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos/métodos , Glucosefosfato Desidrogenase/metabolismo , Internet , Inibidores da Monoaminoxidase/química , Monoaminoxidase/metabolismo , Proteínas de Protozoários/metabolismo , Trichomonas , Animais , Antiparasitários/química , Antiparasitários/farmacologia , Columbidae/microbiologia , Descoberta de Drogas , Glucosefosfato Desidrogenase/química , Indanos/síntese química , Indanos/química , Modelos Moleculares , Modelos Teóricos , Dados de Sequência Molecular , Estrutura Molecular , Monoaminoxidase/química , Inibidores da Monoaminoxidase/síntese química , Peptídeos/química , Conformação Proteica , Proteínas de Protozoários/química , Relação Quantitativa Estrutura-Atividade , Trichomonas/química , Trichomonas/efeitos dos fármacos , Trichomonas/enzimologiaRESUMO
The active ingredient of Huyinling, a combination of Chinese traditional medicine, was extracted by five different ethanol concentrations (40%-80%). There were seven groups named as five Huyinling ethanol extract groups (40%, 50%, 60%, 70%, and 80%), metronidazole group and blank control. Each Huyinling ethanol extract group was further divided into five subgroups with final concentration of 6.25, 12.5, 25, 50, and 100 mg/ml, respectively. Metronidazole group was given 10 microg/ml of the drug. Each group had 4 wells with 125 microl T. tenax(2 x 10(5)/ml). At 12 h, 24 h and 48 h after drug treatment, the anti-T. tenax effect of Huyinling ethanol extract was tested by microscope counting method. At 24 h the effect of Huyinling on T. tenax was examined with methyl thiazolyl tetrazolium (MTl) assay. The results showed that the higher concentration of Huyinling ethanol extract, the better effect on anti-T. tenax. 60% Huyinling ethanol extract group with concentrations of 6.25 mg/ml and 12.5 mg/ml showed higher anti-T. tenax effect than other groups (P < 0.01). The ethanol extract of Huyinling granules has a remarkable effect on T. tenax, and among the groups, 60% ethanol extract shows the best anti-T. tenax activity.
Assuntos
Antitricômonas/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Trichomonas/efeitos dos fármacosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Clausena lansium (Fool's Curry Leaf) is used for various ethnomedical conditions in some countries, including bronchitis, malaria, viral hepatitis, acute and chronic gastro-intestinal inflammation, and as a spicy substitute of the popular Curry leaf tree (Murraya koenigii). AIM OF THE STUDY: This study was to evaluate the ethnomedical uses of the stem bark in inflammatory conditions, hepatotoxicity and to determine the anti-diabetic and anti-trichomonal properties of the plant. MATERIALS AND METHOD: Anti-trichomonal, in vivo and in vitro antidiabetic and insulin stimulating, anti-inflammatory, hepatoprotective and anti-oxidant activities using Trichomonas gallinae, glucose loaded rats and in vitro insulin secreting cell line (INS-1 cell), carrageenin-induced rat paw oedema, CCl(4)-induced hepatotoxicity and DPPH scavenging ability methods respectively for the extracts and some isolates were determined. RESULTS: A dichloromethane extract was superior over methanolic extract with respect to an anti-trichomonal activity which was measured after 24 and 48 h. The isolated compounds imperatorin and 3-formylcarbazole had the main anti-trichomonal activity (LC(50)s of 6.0, 3.0 and 3.6, 9.7 microg/mL after 24 and 48 h, respectively). Methanolic extract (100 mg/kg) induced maximum and significant (p<0.05) anti-hyperglycaemic activity of 15.8% at 30 min and a 38.5% increase in plasma insulin at 60 min, compared to control. The increase in plasma insulin after 60 min, compared to 0 min, was 62.0% (p<0.05). The significant 174.6% increase of insulin release from INS-1 cells (in vitro) at 0.1 mg/ml indicates that it mediates its antidiabetic action mainly by stimulating insulin release. Imperatorin and chalepin were the major active constituents increasing in vitro insulin release to 170.3 and 137.9%, respectively. 100 mg/kg of the methanolic extract produced an anti-inflammatory activity after 4 h. A sedative effect was not observed. 100 and 200 mg/kg of methanolic extract administered i.p., reduced CCl4-induced hepatotoxicity firstly by 5.3 and 8.4% reduction in phenobarbitone-sleeping time respectively, secondly by reversing the reduction in serum liver proteins by 7.0-8.8%, serum AST, ALT and ALP activities by 27.7-107.9% and thirdly by diminishing increased values of plasma AST, ALT and ALP activities by 13.2-83.8%. The extract exhibited antioxidant activities. CONCLUSION: The hepatoprotective activity of C. lansium is partly due to its anti-oxidant and anti-inflammatory properties and confirms its folkloric use in the treatment of gastro-intestinal inflammation, bronchitis and hepatitis. In addition the use of C. lansium stem bark would be useful in diabetes and trichomoniasis.
Assuntos
Anti-Inflamatórios/farmacologia , Intoxicação por Tetracloreto de Carbono/tratamento farmacológico , Clausena , Edema/tratamento farmacológico , Hiperglicemia/tratamento farmacológico , Extratos Vegetais/farmacologia , Trichomonas/efeitos dos fármacos , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/uso terapêutico , Glicemia , Proteínas Sanguíneas/metabolismo , Carbazóis/isolamento & purificação , Carbazóis/farmacologia , Linhagem Celular , Clausena/química , Enzimas/sangue , Furocumarinas/isolamento & purificação , Furocumarinas/farmacologia , Hipnóticos e Sedativos/farmacologia , Insulina/sangue , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fitoterapia , Casca de Planta , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Caules de Planta , Ratos , Ratos WistarRESUMO
AIM OF THE STUDY: The ethanolic stem bark extract of Harungana madagascariensis (Hypericaceae), (Choisy) Poir were evaluated for their activities on Trichomonas gallinae (Rivolta) Stabler isolated from the pigeon (Columba livia). It was also tested for their anti-malarial activity on N67 Plasmodium yoelii nigeriensis (in vivo) in mice and on Plasmodium falciparum isolates in vitro. MATERIALS AND METHODS: The anti-trichomonal screening was performed in vitro using Trichomonas gallinae culture. The minimum lethal concentration (MLC) is the lowest concentration of the test extract in which no motile organisms were observed. The anti-malarial effects were determined in-vivo for suppressive, curative and prophylactic activities in mice receiving a standard inoculum size of 1 x 10(7) (0.2 ml) infected erythrocytes of Plasmodium yoelii nigeriensis intraperitoneally, and the in vitro was performed against 3 isolates of Plasmodium falciparum in a candle jar procedures. RESULTS: The IC(50) of the extract and metronidazole (MDZ) (Flagyl) on Trichomonas gallinae at 48 h are 187 and 1.56 microg/ml. The IC(50) of the extract, chloroquine (CQ) and artemether (ART) on Plasmodium falciparum are between 0.052 and 0.517 microg/ml for the extract and 0.021 and 0.0412 microg/ml for ART and CQ, respectively. The actions of the extract in in vivo study on Plasmodium yoelii nigeriensis showed that in both suppressive and prophylactic tests the percentages chemo-suppressive were between 28.6-44.8% and 30.2-78.2% respectively, while only 80 mg/kg of the extract reduced the parasitaemia level when compared to the control and the standard drugs in curative test. CONCLUSIONS: Harungana madagascariensis stem bark extract therefore exhibited significant anti-protozoan effects against Trichomonas and Plasmodium both in vivo and in vitro.
Assuntos
Antimaláricos/farmacologia , Antiprotozoários/farmacologia , Antitricômonas/farmacologia , Clusiaceae/química , Animais , Antimaláricos/isolamento & purificação , Antiprotozoários/isolamento & purificação , Antitricômonas/isolamento & purificação , Artemeter , Artemisininas/farmacologia , Cloroquina/farmacologia , Feminino , Malária Falciparum/tratamento farmacológico , Malária Falciparum/parasitologia , Masculino , Metronidazol/farmacologia , Camundongos , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Caules de Planta/química , Plasmodium falciparum/efeitos dos fármacos , Plasmodium yoelii/efeitos dos fármacos , Trichomonas/efeitos dos fármacosRESUMO
The methanolic extract of Murraya koenigii leaf was screened for toxicological and biochemical effects on rats because of the folkloric uses as an anti-dysentery and anti-diabetes. The extract was moderately toxic (LD(50)=316.23 mg/kg body weight) to rats and had appreciable effect on the liver and kidney at higher doses leading to liver inflammation. It had little or no effect on haematology and relative organ weight of lungs, heart and spleen. Acute doses (500 mg/kg) reduced significantly serum globulin, albumin, urea, glucose, total protein, aspartate transaminase (AST), and increased cholesterol and alanine transaminase (ALT) indicating hepatic injury. However, chronic administration for 14 days gave a significant (p<0.05) reduction in the serum cholesterol, glucose, urea, bilirubin, ALT and AST showing that the plant has hypoglycaemic and hepatoprotective effects after prolonged use. The activity demonstrated by some of the isolated carbazole alkaloids and their derivatives against Trichomonas gallinae confirmed that the anti-trichomonal activity of the leaf may be due to its carbazole alkaloids. The order of activity was C(18)>C(23)>C(13). Girinimbine and girinimbilol with IC(50) values of 1.08 and 1.20 microg/ml were the most active. Acetylation of girinimbilol and mahanimbilol improved their activities to 0.60 and 1.08 microg/ml.
Assuntos
Alcaloides/toxicidade , Murraya/química , Murraya/toxicidade , Fitoterapia , Extratos Vegetais/farmacologia , Trichomonas/efeitos dos fármacos , Alcaloides/química , Estruturas Animais/efeitos dos fármacos , Animais , Antitricômonas/farmacologia , Antitricômonas/toxicidade , Carbazóis/farmacologia , Carbazóis/toxicidade , Columbidae/parasitologia , Contagem de Eritrócitos , Hematócrito , Dose Letal Mediana , Fígado/efeitos dos fármacos , Nigéria , Tamanho do Órgão/efeitos dos fármacos , Extratos Vegetais/toxicidade , Folhas de Planta/química , Ratos , Soro/química , Soro/efeitos dos fármacos , Soro/enzimologia , Fatores de Tempo , Testes de Toxicidade Aguda/métodos , Trichomonas/isolamento & purificaçãoRESUMO
Dorstenia barteri and D. convexa extracts and some isolated components of the former were investigated for effectiveness against Trichomonas gallinarum and compared with quercetin and quercitrin. The antioxidant activity of the extracts/compounds was also determined. The minimum lethal concentrations (MLCs) for the extract of D. barteri leaves and twigs at 24 h were found to be 15.625 and 15.625 microg/ml, respectively. However, the MLCs of the leaf and twig extract of D. convexa were 125 and 437.5 microg/ml, respectively. The prenylated and geranylated chalcones were as active as the prenylated flavones, 6-prenylapigenin and the diprenylated derivative 6,8-diprenyleridictyol. The order of the antitrichomonal activity of the compounds at 24 h was: quercetin (0.121 microg/ml) > quercitrin (0.244 microg/ml) > or = bartericin B (0.244 microg/ml) > bartericin A (0.73 microg/ml) > stigmasterol (0.98 microg/ml) > 6,8-diprenyleridictyol = isobavachalcone = dorsmanin F (31.25 microg/ml). D. barteri extracts, quercitrin, and bartericin A, and the prenylated flavonoids had potent antioxidant properties. The twig extract of D. barteri was more potent than the leaf extract. Moderate (EC50 >50 microg/ml) and high (EC50 <50 microg/ml) antioxidant activities were detected in the leaf and twig extracts of D. barteri and the prenylated flavonoids. Prenylated flavonoids and the isolated compounds with antioxidant properties described here may account for the anti-inflammatory action of these extracts. The antitrichomonal and antioxidant activities shown by the extracts and compounds in this study are consistent with the ethnomedicinal and local use of the Dorstenia species studied.
Assuntos
Antioxidantes/farmacologia , Antitricômonas/farmacologia , Flavonoides/farmacologia , Moraceae/química , Trichomonas/efeitos dos fármacos , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antitricômonas/química , Antitricômonas/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos , Flavonoides/química , Flavonoides/isolamento & purificação , Testes de Sensibilidade Parasitária , Extratos Vegetais/farmacologia , Quercetina/análogos & derivados , Quercetina/farmacologiaRESUMO
Dorstenia barteri and D. convexa extracts and some isolated components of the former were investigated for effectiveness against Trichomonas gallinarum and compared with quercetin and quercitrin. The antioxidant activity of the extracts/compounds was also determined. The minimum lethal concentrations (MLCs) for the extract of D. barteri leaves and twigs at 24 h were found to be 15.625 and 15.625 æg/ml, respectively. However, the MLCs of the leaf and twig extract of D. convexa were 125 and 437.5 æg/ml, respectively. The prenylated and geranylated chalcones were as active as the prenylated flavones, 6-prenylapigenin and the diprenylated derivative 6,8-diprenyleridictyol. The order of the antitrichomonal activity of the compounds at 24 h was: quercetin (0.121 æg/ml) > quercitrin (0.244 æg/ml) > or = bartericin B (0.244 æg/ml) > bartericin A (0.73 æg/ml) > stigmasterol (0.98 æg/ml) > 6,8-diprenyleridictyol = isobavachalcone = dorsmanin F (31.25 æg/ml). D. barteri extracts, quercitrin, and bartericin A, and the prenylated flavonoids had potent antioxidant properties. The twig extract of D. barteri was more potent than the leaf extract. Moderate (EC50 >50 æg/ml) and high (EC50 <50 æg/ml) antioxidant activities were detected in the leaf and twig extracts of D. barteri and the prenylated flavonoids. Prenylated flavonoids and the isolated compounds with antioxidant properties described here may account for the anti-inflammatory action of these extracts. The antitrichomonal and antioxidant activities shown by the extracts and compounds in this study are consistent with the ethnomedicinal and local use of the Dorstenia species studied.
Assuntos
Animais , Antioxidantes/farmacologia , Antitricômonas/farmacologia , Flavonoides/farmacologia , Moraceae/química , Trichomonas/efeitos dos fármacos , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antitricômonas/química , Antitricômonas/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos , Flavonoides/química , Flavonoides/isolamento & purificação , Testes de Sensibilidade Parasitária , Extratos Vegetais/farmacologia , Quercetina/análogos & derivados , Quercetina/farmacologiaRESUMO
Ethyl ether, ethyl acetate and n.butanol extracts of Cotula cinerea L. were tested for their antiprotozoal activity against two species of Trichomonas: Trichomonas intestinalis and Trichomonas vaginalis. It has been found that the growth of both Trichomonas was significantly inhibited.
Assuntos
Antiprotozoários/farmacologia , Asteraceae/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Trichomonas/efeitos dos fármacos , Animais , Antiprotozoários/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos , Marrocos , Extratos Vegetais/química , Especificidade da Espécie , Trichomonas vaginalis/efeitos dos fármacosRESUMO
The extracts of six plants selected on the basis of folk-medicine reports were examined for their antibacterial effects against eight pathogenic bacteria. The results showed that n-butanol extract of Calotropis procera proved to be the most effective against the bacteria tested using the paper disc diffusion method. The antiprotozoal activity was also examined and showed that ethyl ether extract of Sium nodiflorum exhibits a parasiticidal effect against Trichomonas intestinalis and vaginalis.