RESUMEN
Peptic ulcer is an acid-induced lesion that is usually found in the stomach and duodenum. It is usually a case of imbalance between the acid (and other injurious factors) and the mucosal defense mechanisms. Indomethacin is one of the most ulcerogenic drugs that is prescribed over-the-counter for the management of musculoskeletal problems. Capparis spinosa is one of the most important species in the Capparidaceae family, which has a wide range of diversity. Caper (Capparis spinosa L.) is a common member of the genus Capparis (Capparidaceae family). The present study was designed to compare the effect of C. spinosa extract as a gastroprotective agent with indomethacin as an induction agent and ranitidine as a standard drug. To this aim, 40 adult male Wistar rats were randomly divided into 4 groups (n=10 each), including Control +: indomethacin-treated group, Control -: receiving physiological saline solution, C.S: C. spinosa-treated group; and ranitidine-treated group (50 mg/kg) as a standard agent for the treatment of the gastric ulcer. After the experimental period, all the animals were sacrificed by anesthesia overdose and their stomachs were removed. The gastroprotective effect of C. spinosa was investigated by studying prostaglandin E2 (PGE2), Gastrin, anti-tumor necrosis factor alpha (TNF-α), and Interleukin 1 beta (IL1-ß), along with histopathological examination. The results showed a significant increase in PGE2 levels in the ranitidine-treated group with a significant reduction in Gastrin, TNF-α, and IL1-ß. The recorded data obtained from the histopathological study showed a significant improvement in the treated group with the extract of C. spinosa. The study concluded that C. spinosa had gastroprotective properties possibly through enhancing PGE2 which was acting as anti-inflammatory inhibiting neutrophil infiltration.
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Capparis , Extractos Vegetales , Úlcera Gástrica , Animales , Masculino , Ratas , Dinoprostona , Gastrinas , Indometacina/toxicidad , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ranitidina/farmacología , Ratas Wistar , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/tratamiento farmacológico , Úlcera Gástrica/prevención & control , Factor de Necrosis Tumoral alfaRESUMEN
Endophytic fungi are broadly dispersed residing inside plant tissues and have been demonstrated as a treasure for bioactive natural products. Unexplored harsh and heavy metal contaminant habitat of Avicennia marina may have diverse and potential fungal association. Therefore, this work aimed to isolate the culturable fungal endophytes associated with leaves of A. marina and to evaluate their medical potentialities. Seventeen isolates of endophyte fungi were isolated from healthy leaves and their antimicrobial activities were evaluated. Results showed that isolates had activity against micro-organisms in addition to their antioxidant activity produced a variety of phenolic compounds, besides exhibited a lowest cytotoxicity against ATCC-CCL-81 cell line. Consequently, selected endophytic fungal isolates were identified genetically as Chaetomium sp., Chaetomium madrasense, Chaetomium sp., Chaetomium globosum, Aspergillus hiratsukae, Aspergillus ochraceus, Alternaria tenuissima and Curvularia lunata with gene bank accession numbers MT089951, MT089952, MT089953, MT089954, MT089955, MT089956, MT089957 and MT089958 respectively. The most potent fungus extract was analysed using Gas chromatography-mass spectrometry which verified the presence of numerous bioactive compounds. These findings confirmed that new endophytic fungal strains derived from A. marina thrive in harsh ecosystem produce bioactive metabolites which can be recommended as a novel source for drug discovery.
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Antioxidantes/farmacología , Avicennia/microbiología , Extractos Celulares/farmacología , Hongos/química , Hongos/efectos de los fármacos , Alternaria/química , Aspergillus/química , Aspergillus ochraceus/química , Productos Biológicos/farmacología , Chaetomium/química , Curvularia/química , Clima Desértico , Descubrimiento de Drogas , Endófitos/química , Endófitos/aislamiento & purificación , Hongos/aislamiento & purificación , Cromatografía de Gases y Espectrometría de Masas , Hojas de la Planta/microbiologíaRESUMEN
The potential increased frequency and severity of drought associated with environmental change represents a significant obstacle to efforts aimed at enhancing food security due to its impact on crop development, and ultimately, yield. Our understanding of the impact of drought on crop growth in terms of plant aerial tissues is much more advanced than knowledge of the below-ground impacts. We undertook an experiment using X-ray Computed Tomography that aimed to support measurements of infrared gas exchange from plant shoots with quantification of 3D root architecture traits and the associated soil structural characteristics. Winter wheat (cv. Zebedee) was assessed at two early growth stages (14 and 21 days) under four water treatments (100, 75, 50 and 25 % of a notional field capacity (FC) and across two soil types (sandy loam and clay loam)). Plants generally grew better (to a larger size) in sandy loam soil as opposed to clay loam soil, most likely due to the soil structure and the associated pore network. All plants grew poorly under extreme water stress and displayed optimal growth at 75 % of FC, as opposed to 100 %, as the latter was most likely too wet. The optimal matric potential for root and shoot growth, inferred from the water release curve for each soil type, was higher than that for photosynthesis, stomatal conductance and transpiration suggesting root and shoot growth was more affected by soil water content than photosynthesis-related characteristics under water deficit conditions. With incidences of drought likely to increase, identification of wheat cultivars that are more tolerant of these conditions is important. Studies that consider the impact of water stress on both plant shoots and roots, and the role of the soil pore system such as this offer considerable potential in supporting these efforts.
RESUMEN
The assembly of binuclear Cu(i) metallaclips with 2,2'-bis-dipyrrin based metalloligands gives rise to a diversity of architectures featuring a recurring π-stacked compact tetranuclear metallacycle but differing in their nuclearity and dimensionality depending on the nature of the capping ligands and metal cations.
RESUMEN
Background Childhood-onset systemic lupus erythematosus (cSLE) is a lifelong autoimmune disorder. The vitamin D receptor (VDR) gene is a potential candidate gene for cSLE susceptibility. In this study, we aimed to investigate the FokI polymorphism in the VDR gene in Egyptian children and adolescents with SLE, to determine whether this polymorphism could be a genetic marker for cSLE susceptibility or disease activity and we also measured the serum level of 25-hydroxyvitamin D [25(OH) D] to assess its relation to such polymorphism. Methods This was a case-control study, which included 300 patients with cSLE and 300 age, sex, and ethnicity-matched healthy controls. All participants were genotyped for the VDR gene FokI (rs2228570) polymorphism by polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP), while the serum [25(OH) D] levels were measured by enzyme-linked immunosorbent assay (ELISA). Results The VDR FokI FF genotype and F allele were overrepresented among cSLE patients compared with the controls, [odds ratio (OR) = 2.7; 95% confidence interval (CI): 1.6-4.4 for the FF genotype; p = 0.000; and OR = 1.6; 95% CI: 1.27-2.05 for the F allele; p = 0.000, respectively]. We found a significant association between VDR FokI FF genotype with lupus nephritis (OR: 4.8; 95% CI: 2.2-10.6; p = 0.002); and high disease activity index score ( p = 0.01). Conclusions The FokI polymorphism in the VDR gene may contribute to susceptibility to SLE in Egyptian children and adolescents. Moreover, the FF genotype constituted a risk factor for the development of lupus nephritis and was associated with low serum [25(OH) D] levels as well as higher disease activity index score among studied patients with cSLE.
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Predisposición Genética a la Enfermedad , Lupus Eritematoso Sistémico/genética , Polimorfismo Genético , Receptores de Calcitriol/genética , Adolescente , Estudios de Casos y Controles , Niño , Desoxirribonucleasas de Localización Especificada Tipo II , Femenino , Humanos , Lupus Eritematoso Sistémico/sangre , Lupus Eritematoso Sistémico/etiología , Masculino , Estudios Prospectivos , Vitamina D/análogos & derivados , Vitamina D/sangreRESUMEN
The reaction of 3-aryl-2,4-dicarboethoxy-5-hydroxy-5-methylcyclohexanones 1with benzalacetone, dibenzalacetone, benzalacetophenone, and 4-benzal-1-phenyl-3-methyl pyrazolone has been investigated to give Michael compounds 2-5. hydrolysis of the dioxo derivative 4 afforded1,5-dicarbonyl derivative 6which On condensation with hydrazine and/or substituted hydrazine and hydroxylamine produced1,2-diazepine and 1,2-oxazepine derivatives 7,8 respectively. Reaction of ß-Keto ester 1 with 1,3-diphenylacetone afforded 9. The structures of the hitherto unknown compounds have been confirmed by analytical and spectral data. The newly synthesized compounds have been screened to test their antimicrobial and antifungal activity.
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Schistosoma mansoni causes intestinal schistosomiasis, a disease that is prevalent in several regions worldwide. To date, a protective vaccine against S. mansoni is still lacking. Several promising antigens have been discovered and evaluated for vaccine protection, such as Sm14 and Sm28GST. In this short communication, we report the successful detection of an alternatively spliced truncated form of Sm14 which was highly expressed in an Egyptian strain of S. mansoni. This truncated Sm14 (TrSm14) protein was formerly reported to be practically non-existent and its complementary DNA (cDNA) was thought to be 'a rare misprocessing of mRNA precursor'. Our finding demonstrates that there is inter-strain variation in the S. mansoni transcriptome and subsequently in the role/function of the expressed proteins. We expressed TrSm14 successfully in Escherichia coli as a fusion protein with the schistosomal antigen Sm28GST. The fusion protein was purified using metal affinity chromatography and was found to be reactive with serum from S. mansoni-infected patients. This suggests a possible diagnostic value for this protein in detection of anti-schistosomal antibodies. In addition, this fusion protein could offer a potential bivalent vaccine candidate against S. mansoni that is worthy of further investigation.
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Proteínas de Transporte de Ácidos Grasos/genética , Proteínas de Transporte de Ácidos Grasos/aislamiento & purificación , Proteínas del Helminto/genética , Proteínas del Helminto/aislamiento & purificación , Schistosoma mansoni/metabolismo , Empalme Alternativo , Animales , Egipto , Proteínas de Transporte de Ácidos Grasos/análisis , Proteínas de Transporte de Ácidos Grasos/metabolismo , Femenino , Proteínas del Helminto/análisis , Proteínas del Helminto/metabolismo , Masculino , Schistosoma mansoni/química , Schistosoma mansoni/genética , Esquistosomiasis/parasitologíaRESUMEN
Iminopropanehydrazonoyl cyanide 4 was achieved upon reaction of antipyrine diazonium salt 2 with 3-iminobutanenitrile (3) in EtOH/AcONa. 3-Aminopyrazole derivative 5 was obtained upon reaction of 4 with hydrazine hydrate. Diazodization of 5 afforded the diazonium salt 6 which coupled with active methylene compounds 7-10, 19, 20, 25, 29 and 32 in pyridine to give aryl hydrazone derivatives 11-14, 21, 22, 26, 30 and 33, respectively. Refluxing of compounds 11-14, 21, 22, 26 and 33 in acetic acid afforded the pyrazolotriazines 15-18, 23, 24, 28 and 35, respectively. The newly synthesized compounds were screened for their cytotoxic and antioxidant activities. The results showed clearly that compounds 4, 5, 13, 22, and 24 displayed promising in vitro anticancer activity against four different cell lines (HepG2, WI 38, VERO and MCF-7). Compounds 4 and 22 are the more potent antioxidant and anticancer agents. On the other hand, most of the compounds exhibited good cytotoxic activity toward (EAC).
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Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Antioxidantes/síntesis química , Antioxidantes/farmacología , Antipirina/química , Pirazoles/farmacología , Animales , Antineoplásicos/química , Antioxidantes/química , Bleomicina/farmacología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Chlorocebus aethiops , Daño del ADN , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Células Hep G2 , Humanos , Células MCF-7 , Estructura Molecular , Pirazoles/síntesis química , Pirazoles/química , Relación Estructura-Actividad , Células VeroRESUMEN
Mammalian meiosis is a process that allows diploid progenitor germ cells to produce haploid gametes after proceeding through 2 rounds of cell divisions. The first division (MI) is unique and results in the separation of homologous chromosomes, while the second division (MII) leads to the separation of sister chromatids similar to a somatic cell division. However, the mechanisms by which meiotic cells regulate their 2 very different cell divisions are not well understood. We postulated a role for epigenetic chromatin modifications in regulating these processes. We found prior to the onset of MI that pericentromeric heterochromatic regions, which are enriched with histone H3K9me2 throughout meiosis, become enriched at late pachytene with H3S10ph and at diplotene with H4K5ace and H4K16ace, but remain underacetylated at other sites examined. RNA polymerase II, which is clearly excluded from pericentromeric heterochromatin at pachytene, becomes exclusively associated with these regions from diplotene to MI. By contrast, pericentromeric heterochromatic regions at MII are not engaged by RNA polymerase II nor enriched with H3S10ph. Furthermore, we found DICER to localize exclusively to pericentromeric heterochromatin at MI, but not MII. These results are significant since they suggest: (1) that distinct chromatin modifications differentiate the 2 meiotic divisions; (2) a role for repetitive DNA elements and RNAi in mammalian meiosis; (3) H3K9me2 is not sufficient to block RNA polymerase II elongation through heterochromatin, and (4) H3S10ph provides a 'binary switch' to activate transcription in heterochromatin.
Asunto(s)
Centrómero/genética , Epigénesis Genética , Heterocromatina/genética , Meiosis , Células Cultivadas , Centrómero/metabolismo , Heterocromatina/metabolismo , Histonas/metabolismo , Humanos , Masculino , ARN Polimerasa II/metabolismoRESUMEN
1. The effects of a surgical operation, to implant a guide cannula in the chick hypothalamus for microdialysis, on behavioural responses and neural activity in broiler chicks are described. 2. General behavioural activities (feeding, preening, sitting, drinking, cage pecking and beak wiping), open field and locomotor activity tests were conducted to evaluate the effects related to surgery in the immediate 4 d following this procedure. Perfusion of Ringer solution with high K(+) after 4 d of guide cannula implantation was used to estimate the neural activity resulting from surgery through stimulation of monoamine release by in vivo brain dialysis. 3. The results of direct behavioral observations indicated that the stress provoked by surgical guide cannula insertion caused behavioural alterations that are particularly evident in the immediate days following this procedure. Open-field tests on day 4 after surgery showed that, compared to the intact control chickens, the treated chicks had a shorter latency to ambulate and defecate, with more vocalisation. Locomotor activity was less in the treated chicks than in the controls. 4. After 4 d of guide cannula implantation, the serotonin concentration started to increase 30 min after the onset of perfusing high-K(+) Ringer solution. It reached its highest value at one hour, suggesting that the 4 d after surgery is enough to alleviate some neurochemical dysfunction resulting from surgery. The results of behavioural observations, open-field and locomotor activity tests indicate that the surgical operation caused stress and fear in chicks which persisted up to 4 d.
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Conducta Animal/fisiología , Aminas Biogénicas/análisis , Pollos/cirugía , Hipotálamo/cirugía , Actividad Motora/fisiología , Vocalización Animal/fisiología , Animales , Masculino , Microdiálisis/veterinaria , Grabación de Cinta de VideoRESUMEN
In an effort to establish new candidates with improved antibacterial activities, we reported here the synthesis and in vitro antibacterial evaluation of various series of 2-substituted-3a,4,9,9a-tetrahydro-4,9-benzeno-benz[f]isoindole-1,3-diones: 4-acetyl-phenyl 2, 2,2-dibromoacetylphenyl 3, benzimidazole 4, acetylbenzimidazole 5, aminophenyl 6, acetamide 7, naphthalene 8, disulfide 9, mercaptophenyl 10, hydroxyphenyl 11, phenyl ester 12, triazole 13, benzothiophene 14, benzothiazole 15 phenylazo 16a, b and aminomethane 17 derivatives. The newly synthesized compounds were characterized by (IR, (1)H NMR, (13)C NMR and mass spectrum studies). Representative compounds of the synthesized products were established and evaluated as antibacterial agents.
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Antibacterianos/síntesis química , Antibacterianos/farmacología , Indoles/síntesis química , Indoles/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría InfrarrojaRESUMEN
Treatment of 2-cyano-N-(9,10-dioxo-9,10-dihydro-anthracen-2-yl)-acetamide (1) with phenyl isothiocyanate/dimethylsulphate afforded the corresponding ketene N,S-acetal 2 which upon treatment with hydrazine hydrate and 4-aminoantipyrine afforded the pyrazolo derivatives 3 and 4, respectively. 3-aminopyrazole derivative 3 was utilized as key intermediate for the synthesis of pyrazolo[3,4-d]pyrimidine 5, pentaaza-as-indacene 6, triaza-cyclopenta[c]phenanthrene 7, pyrazolo[1,5-a]pyrimidine 8, 9 and (dimethyl-pyrrol-1-yl)pyrazole 10 derivatives. Furthermore, treatment of 1 with DMF/DMA gave the corresponding acrylamide derivative 11 which upon treatment with hydrazine hydrate afforded the corresponding 3-aminopyrazole derivative 12. Moreover, coupling of 1 with 4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-3-diazonium chloride gave the hydrazone derivative 13 which upon cyclization with acetic acid afforded the corresponding pentaaza-fluorene derivative 14. Representative compounds of the synthesized products were evaluated as antimicrobial agents. Some of these compounds exhibited promising activities.
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Antraquinonas/farmacología , Antibacterianos/farmacología , Pirazoles/química , Alternaria/efectos de los fármacos , Antraquinonas/síntesis química , Antraquinonas/química , Antibacterianos/síntesis química , Antibacterianos/química , Ciclización , Fusarium/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Pseudomonas aeruginosa/efectos de los fármacos , Staphylococcus epidermidis/efectos de los fármacos , Estereoisomerismo , Relación Estructura-ActividadRESUMEN
2-(5-oxothiazolidinone)-cyanoacetamido derivative 3 was prepared in two steps by reaction of 2-(2-cyano-acetylamino)-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxamide (1) with phenyl isothiocyanate and chloroacetyl chloride, which diazocoupled with p-tolyldiazonium chloride in pyridine to afford the corresponding hydrazono derivative 4. Also, condensation of 3 with p-anisaldehyde gave the corresponding arylidine derivative 5. Treatment of 2 with dimethyl sulfate afforded the ketene N,S-acetal 9 which give 5-amino pyrazole derivative 10 upon treatment with hydrazine hydrate. Compound 10 was used as key intermediate for synthesis of pyrazolo[5,1-c][1,2,4]triazine 13a, b, pyrazolo[5,1-a]pyrimidine 14-17 and pyrolo pyrazole 18 derivatives. Finally, condensation of 1 with DMF-DMA afforded the corresponding acryloamide derivative 19, which afforded the corresponding pyrazole derivative 20 upon heating with hydrazine hydrate. All new synthesized compounds were evaluated as antimicrobial agents; some of them exhibited promising activities.
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Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Tiazoles/síntesis química , Tiazoles/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Pirazoles/síntesis química , Pirazoles/farmacologíaRESUMEN
Dibenzobarrelene 1 was reacted with cyanoacetic acid hydrazide and thiosemicarbazide to give the corresponding 3-oxo-propiononitrile and thioamide derivatives 2 and 16, respectively. The base-catalyzed reaction 3-oxo-propiononitrile derivative 2 with phenyl isothiocyanate yielded the non-isolable intermediate 3. Treatment of 3 with dilute HCl afforded the corresponding thiocarbamoyl derivative 4. The intermediate 3, thiocarbamoyl 4 and thioamide derivatives 16 were utilized as key intermediates for the synthesis of some new thiazole 5, 6a, 6b, 7, 8, 10a, 10b, 12, 14a, 15, 17a, 17b, and 18; and thiophene 13a-d derivatives, respectively. The newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR and mass spectral studies. Representative compounds of the synthesized product were tested and evaluated as antibacterial agent.
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Antibacterianos/química , Antibacterianos/farmacología , Tiazoles/química , Tiazoles/farmacología , Tiofenos/química , Tiofenos/farmacología , Antibacterianos/síntesis química , Bacillus/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad , Tiazoles/síntesis química , Tiofenos/síntesis químicaRESUMEN
3-(1,4-Dioxo-3,4,4e,5,10,10a-hexahydro-1H-5,10-benzeno-benzo[g]phthalazin-2-yl)-3-oxo-propiononitrile (1) was utilized as key intermediate for the synthesis of some new iminocoumarin 2, chromenone 3, aminothiazole 4, triazepine 5a, b and 6, hydrazono-propiononitrile 7, pyridopyrazotriazine 8, monobromo 9, dibromo 10 quinoxaline 11, ketene N,S-acetal 13, ketene S,S-diacetal 17 and 18a, b and methyl dithioate 20 derivatives, respectively. The newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR and mass spectral studies. Representative compounds of the synthesized product were tested and evaluated as antibacterial agent.
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Antibacterianos/química , Antibacterianos/farmacología , Bacillus thuringiensis/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Ftalazinas/química , Ftalazinas/farmacología , Animales , Antibacterianos/síntesis química , Azepinas/síntesis química , Azepinas/química , Azepinas/farmacología , Cumarinas/síntesis química , Cumarinas/química , Cumarinas/farmacología , Ratones , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Ftalazinas/síntesis química , Triazinas/síntesis química , Triazinas/química , Triazinas/farmacologíaRESUMEN
The synthesis, in vivo and in vitro antitumor evaluation, and QSAR studies of some novel pyrazole analogs against Ehrlich Ascites Carcinoma (EAC) cells were described. In vitro results revealed that compounds 10, 6 and 4 were the most potent analogs against EAC, respectively. Moreover, in vivo evaluation of compounds 6 and 10 proved their capability to normalize the blood picture in comparison to 5-FU, a well known anticancer drug. These novel pyrazole analogs were molecularly designed with the goal of having significant potent cytotoxic effect against EAC cells. To develop a QSAR model capable of identifying the key molecular descriptors associated with the biological activity of the novel pyrazole analogs and predicting the cytotoxic effect for other novel pyrazole analogs against EAC cells, different QSAR models, using different physicochemical and topological molecular descriptors, were developed. Different molecular descriptors were predicted solely from the chemical structures of 16 pyrazolo-diazine and triazine analogs following the prediction of the equilibrium molecular geometry of each analog at the DFT level using B88-LYP functional energy and double zeta valence polarized (DZVP) basis set. It was found that dipole moment, excitation energy, the energy value of LUMO, solvent accessible surface area, and heat of formation were the key molecular descriptors in descriping the cytotoxic effect of those compounds against EAC.
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Antineoplásicos/química , Antineoplásicos/uso terapéutico , Compuestos Azo/química , Compuestos Azo/uso terapéutico , Carcinoma de Ehrlich/tratamiento farmacológico , Pirazoles/química , Pirazoles/uso terapéutico , Triazinas/química , Triazinas/uso terapéutico , Animales , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Compuestos Azo/síntesis química , Compuestos Azo/farmacología , Carcinoma de Ehrlich/mortalidad , Quinasa de la Caseína II/química , Quinasa de la Caseína II/metabolismo , Dominio Catalítico , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Masculino , Ratones , Modelos Moleculares , Estructura Molecular , Unión Proteica , Pirazoles/síntesis química , Pirazoles/farmacología , Relación Estructura-Actividad Cuantitativa , Sobrevida , Triazinas/síntesis química , Triazinas/farmacologíaRESUMEN
OBJECTIVE: To compare patient satisfaction with two routes of misoprostol for term labour induction. DESIGN: Prospective randomised trial. SETTING: Tertiary care hospital. POPULATION: A total of 170 women admitted at > or = 37 weeks of gestation for induction of labour. METHODS: Women were randomised to receive 50 micrograms of either sublingual or vaginal misoprostol. MAIN OUTCOME MEASURES: Patient satisfaction with the route of administration. RESULTS: Despite a similar proportion reporting the labour induction as more painful than expected in both groups, a significantly lower proportion mentioned that the pelvic examinations were very painful in the sublingual group (19.7 versus 36.1%, relative risk [RR] 0.5, 95% CI 0.3-0.9). Request for analgesia was similar in both groups. More women in the sublingual group thought that the labour experience was better than expected (RR 2.0, 95% CI 1.2-3.3), had a positive attitude towards induction in subsequent pregnancies (RR 1.6, 95% CI 1.1-2.3) and preferred the same route in subsequent pregnancies (RR 3.1, 95% CI 2.2-4.5). Mean number of misoprostol doses, oxytocin augmentation, tachysystole and hyperstimulation, induction to vaginal delivery interval, vaginal delivery after a single dose, vaginal birth within 12 and 24 hours, and caesarean delivery rates were similar in both groups. CONCLUSION: Sublingual misoprostol (50 micrograms) is associated with a significantly higher patient satisfaction rate compared with a similar dose of vaginal misoprostol. Sublingual administration offers additional choice to women, in particular those wishing to avoid vaginal administration.
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Trabajo de Parto Inducido/métodos , Misoprostol , Oxitócicos , Satisfacción del Paciente , Administración Intravaginal , Administración Sublingual , Adulto , Femenino , Humanos , Trabajo de Parto Inducido/psicología , Embarazo , Resultado del EmbarazoRESUMEN
Microcystin LR (MC-LR), a liver-specific toxin synthesized by Microcystis aeruginosa, was investigated. MC-LR initiated reactive oxygen species formation followed by damaging DNA and some other cellular components. We investigated the ability of MC-LR to induce oxidative DNA damage by examining the formation of 8-hydroxydeoxyguanosine (8-OH-dG) using HPLC with electrochemical detection. Melatonin, vitamin C (ascorbate), and vitamin E (as Trolox), all of which are free radical scavengers, markedly inhibited the formation of 8-OH-dG in a concentration-dependent manner. The concentration that reduced DNA damage by 50% (IC(50)) was 0.55, 31.4, and 36.8 microM for melatonin, ascorbate, and Trolox, respectively. The results show that melatonin is 60- and 70-fold more effective than vitamin C or vitamin E, respectively, in reducing oxidative DNA damage. These findings are consistent with the conclusion that melatonin's highly protective effect against microcystin toxicity relates, at least in part, to its direct hydroxyl radical scavenging ability.
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Ácido Ascórbico/farmacología , Desoxiguanosina/análogos & derivados , Melatonina/farmacología , Microcistinas/farmacología , Vitamina E/farmacología , 8-Hidroxi-2'-Desoxicoguanosina , Animales , Células Cultivadas , Cromatografía Líquida de Alta Presión , Daño del ADN , Desoxiguanosina/análisis , Desoxiguanosina/metabolismo , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/farmacología , Depuradores de Radicales Libres/farmacología , Concentración 50 Inhibidora , Hígado/efectos de los fármacos , Hígado/metabolismo , Ratones , Microcistinas/química , Estructura Molecular , Oxidación-Reducción/efectos de los fármacos , Vitaminas/farmacologíaRESUMEN
Inactivation of the X chromosome occurs in female somatic cells and in male meiosis. In both cases, the inactive X chromosome undergoes changes in histone modifications including deacetylation of core histone proteins and enrichment with histone H3 lysine 9 (H3-K9) dimethylation. In this study we show that while the inactive X in female somatic cells is largely devoid of H3-K4 dimethylation, the inactive X in male meiosis is enriched with this modification. However, the inactive X chromosome in female somatic cells and the inactive X and Y in male meiosis are devoid of H3-K4 trimethylation. Further, trimethylation of H3-K4 is present at discrete regions along most of the autosomes, while H3-K4 dimethylation shows a more homogenous staining. Also, the Y chromosome is largely devoid of H3-K4 di- and trimethylation in somatic cells of both humans and mice, however, the Y chromosome is enriched with H3-K4 di- but not trimethylation throughout spermatogenesis. Our results provide insights into the differences between female somatic cells and male germ cells in inactivating the X chromosome, and suggest that trimethylation, and not dimethylation, of H3-K4 is a more robust indicator of the active regions of the genome.