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BACKGROUND: V pattern identification is essential for proper strabismus management. Graded recession is a tailored approach to treat inferior oblique overaction (IOOA). The aim is to evaluate the efficacy of graded recession of inferior oblique muscle for correction of different grades of V pattern. METHODS: Forty patients from 3 to 18 years old with V pattern strabismus and primary IOOA were evaluated by prism cover test to assess the grade of IOOA and amplitude of V-pattern. Graded recession of IO muscle depends on the amplitude of the V-pattern and degree of IOOA. Eight mm recession for amplitude 15 PD to 20 PD and mild IOOA (10 PD-15 PD or + 1) ,10 mm recession for amplitude 20-30 PD and moderate IOOA (15-25 PD or + 2) and maximum recession for amplitude more than 30 PD and marked IOOA (≥ 25 PD or + 3). Simultaneous correction of the horizontal deviation was performed. Follow up after I week,1 month ,3 month and 6-month. Trial Registration Number (TRN) (NCT05786053) on 23/3/2023. RESULTS: The mean age of the study patients was 9 ± 4.261. Twenty patients (50%) had V-pattern esotropia, 12 (30%) exotropia, 4 (10%) orthotropic and four (10%) had Dissociated vertical deviation (DVD). Four cases 10% were of grade 1, 20 cases (50%) grade 2 and 16 cases (40%) were of grade 3. Of eighty eyes, 66 eyes (82.5%) were fully corrected with no residual IOOA, and 14 eyes (17.5%) were under corrected. V-pattern was corrected in 28 cases 70% and only 12cases (30%) had residual V-pattern grade 1. CONCLUSIONS: Graded recession is an effective procedure for correction of V pattern strabismus with various grades of primary inferior oblique overaction. It can be tailored according to the the degree of IO overaction which is significantly related to the grade of V pattern. The 8 mm recession for IO was significantly related to recurrence or inadequate break of the V pattern in our studied cases. The grade of IOOA correlates with the amplitude of V-pattern. The amount of recession was planned according to preoperative IOOA and grade of V-pattern with frequent undercorrections obtained by the standard 8 mm recession. A + 2 overaction merits a 10-mm recession of the inferior oblique. A + 3 or + 4 overaction merits a 14-mm maximal recession.
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Transtornos da Motilidade Ocular , Doenças Orbitárias , Estrabismo , Humanos , Pré-Escolar , Criança , Adolescente , Músculos Oculomotores/cirurgia , Resultado do Tratamento , Procedimentos Cirúrgicos Oftalmológicos/métodos , Visão Binocular , Estrabismo/cirurgia , Estudos RetrospectivosRESUMO
This study was conducted to evaluate the influence of increased supplementation of zinc oxide (ZnO) on performance, quality of egg, blood chemistry, and antioxidant ability in serum of laying chickens (Hisex Brown) reared from 22 to 34 weeks of age. Seventy-two 22-week-old laying hens (Hisex Brown) were haphazardly separated into 3 handling collections of 24 chickens (6 replicates per treatment and four laying hens per replicate). Dietary treatments included basal diet without zinc addition for control group while the 2nd and 3rd groups contained basal diet with 25 or 75 mg ZnO/kg diet. Results showed that the higher level of ZnO (75 mg ZnO/kg diet) elevated (P < 0.01) feed intake during all studied periods compared with the control group and other groups that contained ZnO. The handling groups supplied with 75 mg ZnO/kg diet gave the worst feed: egg ratio within the whole period and the intervals compared with the control and other ZnO levels. Supplementation of zinc decreased egg number and egg output when compared with the control groups. Egg quality traits were statistically differed due to dietary ZnO supplementation except egg shape index, yolk %, and albumin %. Supplementation of zinc decreased triglyceride (P = 0.001) of laying hens. The low-density lipoproteins (LDL) cholesterol level in serum was decreased with 75 mg ZnO/kg in comparison with all treatment groups. Zinc supplementation increased the level of serum zinc without differences in supplemented zinc levels. Dietary supplemental zinc did not affect antioxidant parameters in the serum. It is concluded that dietary zinc supplementation up to 75 mg/kg used as effective supplement to enhance zinc status and antioxidant ability and activities in laying hens.
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Antioxidantes/metabolismo , Galinhas/fisiologia , Óvulo/fisiologia , Óxido de Zinco/metabolismo , Ração Animal/análise , Animais , Análise Química do Sangue/veterinária , Galinhas/sangue , Dieta/veterinária , Suplementos Nutricionais/análise , Relação Dose-Resposta a Droga , Feminino , Óvulo/efeitos dos fármacos , Óxido de Zinco/administração & dosagemRESUMO
PURPOSE: The importance of nursing competence arises from its central role in influencing and determining care outcomes. The employment of adequately educated staff, able to base clinical decisions on the best scientific evidence, is one of the components required for delivering high quality nursing care in the oncological field. The aim of this study is to analyze - through the Nurse Competence Scale - the level of competence of nurses working in oncological settings. METHOD: A descriptive study was performed between March and September 2017. The participants were recruited among the nursing staff working in the Day Hospital and the Units of the IRCCS -Regina Elena National Cancer Institute in Rome. The confidentiality and the anonymity of the subjects involved in the study were guaranteed by submitting a socio-cultural data sheet -specifically designed to collect demographic and education data - and the Nurse Competence Scale. RESULTS: The sample included 65 nurses (93%) and 5 head nurses (7%), with a mean age of 41.8 years, predominantly female (80%), who had been working in oncology units for a mean of 17.2 years. The Nurse Competence Scale showed a high level of competence in all dimensions. Moreover, the Chi-Square test allowed to identify the presence of significant associations between the different dimensions of the Nurse Competence Scale and the work experience >15 years and the age > 40 years. CONCLUSIONS: The results of our study show that, even if lacking specific oncology competence, nurses working in oncology care settings have developed a good level of clinical competences. Highlighting the importance of nursing care in the oncology area will increase the demand of both patients and organizations of high quality nursing care, consequently enhancing the nursing profession.
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Competência Clínica , Papel do Profissional de Enfermagem , Recursos Humanos de Enfermagem Hospitalar/normas , Enfermagem Oncológica/normas , Adulto , Distribuição de Qui-Quadrado , Feminino , Humanos , Masculino , Enfermeiros/estatística & dados numéricos , Recursos Humanos de Enfermagem Hospitalar/estatística & dados numéricos , Inquéritos e Questionários/estatística & dados numéricosRESUMO
Schistosomiasis remains to be the most common fibrotic disease resulting from inflammation and deposition of scar tissue around trapped parasitic eggs in the liver. Though chemotherapy eradicates matured worms efficiently and prevents the accumulation of schistosome eggs, fewer effective drugs are directed to reverse the present hepatic fibrosis. Therefore, treatment targeting hepatic fibrosis associated with schistosomiasis remains a challenging proposition. The present study was designed to investigate the potential complementary schistosomicidal and hepatoprotective activities of the methanol extract of Capparis spinosa L. (C. spinosa) with or without praziquantel (PZQ) and compare results with silymarin (Milk thistle), a known hepatoprotective and antifibrotic agent, on induced liver fibrosis by experimental Schistosoma mansoni (S. mansoni) infection. Total polyphenols in the extract were determined using colorimetric assay. C. spinosa L. caused a partial decrease in worm burden; a statistically significant reduction in hepatic and intestinal tissue egg load, what was associated histopathologically with decreasing in both the number and diameter of granulomas, as well as restoring serum aminotransferases (AST & ALT), alkaline phosphatase (ALP) and improving liver albumin synthesis. The best results were obtained in the group of mice treated with C. spinosa L. and PZQ together. Quantitative estimation of total polyphenols content using colorimetric assay showed that C. spinosa L. leaves contain higher concentration of polyphenolic compounds than fruits. It was concluded that C. spinosa L. has a promising hepatoprotective and antifibrotic properties and could be introduced as a safe and effective therapeutic tool with PZQ in the treatment of schistosomal liver fibrosis. Nevertheless further studies on the mechanism of action of C. spinosa L. in chronic liver diseases may shed light on developing therapeutic methods in clinical practice.
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PURPOSE: We reviewed the experience of a tertiary cancer centre in the management of adrenocortical carcinoma (acc) treated over 40 years. We also searched the literature for guidelines related to the treatment of acc and for evidence for adjuvant radiation therapy (rt). METHODS: In a retrospective chart review, acc patients treated between January 1974 and December 2013 were identified, and patient demographics and tumour characteristics were extracted. Outcomes data, including dates and sites of failure, vital status, and cause of death, were collected. Overall survival was estimated using the Kaplan- Meier method. A medline search using PubMed, Ovid, and embase was used to review the literature about the role of rt and any available management guidelines for acc. RESULTS: Of 81 patients identified during the chart review, 39 had confirmed acc. In 32 patients, surgical resection was performed, including in 2 patients with M1 disease. Of those 32 patients, 16 received adjuvant systemic treatment (mitotane or concurrent chemoradiation). Only 6 patients received adjuvant rt, of whom 3 are still alive (2 living with distant failure). At a median follow-up of 3.8 years, 28 patients had died (72%), 10 were living (26%), and 1 had been lost to follow-up. Of the 22 patients for whom failure data were available, 2 experienced local failure, and the rest, distant failure. CONCLUSIONS: The current data are insufficient to make treatment recommendations. Use of collaborative databases and consensus about diagnostic and therapeutic guidelines are warranted for better identification of optimum management. Adjuvant rt could be a reasonable option for R1 disease, but further research is needed.
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Although its role and importance is less well studied, carbon monoxide (CO) has been identified as the second gasotransmitter in the GI tract. This study was performed to investigate the effect of modifying the endogenous CO production by altering heme oxygenase (HO) activity either by induction through hemin administration or inhibition by zinc mesoporphyrin administration on gastric secretion and ulceration induced by either cold restraint stress (CRS) or indomethacin (IND) treatment in adult male albino rats. Our results revealed that hemin significantly increased HO-1 levels with an increase in carboxyhemoglobin (COHb) level while zinc mesoporphyrin significantly decreased HO-1 levels with a decrease in COHb level in all groups. Hemin pretreatment significantly attenuated the gastric mucosal lesions induced by CRS and IND administration, which was accompanied by significant reduction in free and total acidity of gastric secretion, decreased proteolytic activity and marked attenuation of lipid peroxidation inspite of decreased NO and PGE2 levels. On the other hand, Inhibition of HO-1 activity by zinc mesoporphyrin prevented most of the effects caused by hemin administration except for its similar reduction in gastric mucosal NO and PGE2 levels. On conclusion, Hemin exerts a protective effect against CRS and IND-induced gastric ulcers possibly via inducing HO-1 and increasing endogenous production of CO (Tab. 2, Fig. 4, Ref. 75).
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Monóxido de Carbono/metabolismo , Mucosa Gástrica/efeitos dos fármacos , Heme Oxigenase-1/metabolismo , Hemina/farmacologia , Metaloporfirinas/farmacologia , Úlcera Gástrica/prevenção & controle , Animais , Resposta ao Choque Frio , Inibidores de Ciclo-Oxigenase , Suco Gástrico/efeitos dos fármacos , Suco Gástrico/metabolismo , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Heme Oxigenase-1/efeitos dos fármacos , Indometacina , Masculino , Ratos , Úlcera Gástrica/etiologia , Úlcera Gástrica/metabolismoRESUMO
BACKGROUND: The Convolvulus genus is distributed all over the world and has a long history in traditional medicine. As nanotechnology expands its reach into areas like drug delivery and biomedicine, this study intends to assess the potential of Convolvulus arvensis L. extracts as anti-bacterial, anti-inflammatory and anti-cancer agents, along with chemical profiling of the methanolic (MeOH) extract active ingredients. METHODS: The chemical composition of an 85% MeOH extract was investigated by liquid chromatography with an electrospray source connected to mass spectrometry (LC-ESI-MS). Both the 85% MeOH extract and n-butanol fraction of C. arvensis were loaded for the first time on alginate/chitosan nanoparticles. The 85% MeOH extract, n-butanol fraction and their loaded nanoparticles were tested for their cytotoxicity, anticancer, anti-inflammatory and antibacterial activity (against pathogenic bacteria, E. coli and S. aureus). RESULTS: The chemical investigation of 85% MeOH extract of C. arvensis underwent LC-ESI-MS analysis, revealing twenty-six phenolic substances, of which 16 were phenolic acids, 6 were flavonoids, 1 glycolipid, 1 sesquiterpene and 2 unknown compounds. The FT-IR spectra confirmed the encapsulation of the 85% MeOH extract and n-butanol fraction onto alginate/chitosan nanoparticles and small size obtained by TEM maintained them nontoxic and enhanced their anti-inflammatory activity (the IC50 was decreased from 1050 to 175 µg/ml). The anti-cancer activity against HepG2 was increased and the cell viability was decreased from 28.59 ± 0.52 to 20.80 ± 0.27 at a maximum concentration of 1000 µg/ml. In addition, the MIC of encapsulated extracts was decreased from 31.25 to7.78 µg/ml in E. coli (Gm-ve) and from 15.56 to 7.78 µg/ml in S. aureus (Gm + ve) bacteria. CONCLUSION: Both alginate and chitosan are excellent natural polymers for the encapsulation process, which affects positively on the bioactive constituents of C. arvensis extracts and improves their biological properties.
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Anti-Infecciosos , Quitosana , Convolvulus , 1-Butanol , Quitosana/farmacologia , Escherichia coli , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureus , Alginatos , Anti-Inflamatórios , Metanol , Extratos Vegetais/farmacologiaRESUMO
BACKGROUND: Trichinellosis, a zoonosis caused by the genus Trichinella, is a widespread foodborne disease. Albendazole, one of the benzimidazole derivatives, is used for treating human trichinellosis, but with limited efficacy in killing the encysted larvae and numerous adverse effects. Cyperus rotundus L. is a herbal plant with a wide range of medicinal uses, including antiparasitic, and is frequently used in traditional medicine to treat various illnesses. METHODS: LC-ESI-MS was used to identify the active phytoconstituents in the methanol extract (MeOH ext.) of the aerial parts of C. rotundus and its derivate fractions ethyl acetate (EtOAc fr.), petroleum ether (pet-ether fr.), and normal butanol (n-BuOH fr.). The in vivo therapeutic effects of C. rotundus fractions of the extracts were evaluated using the fraction that showed the most promising effect after detecting their in vitro anti-Trichinella spiralis potential. RESULTS: C. rotundus extracts are rich in different phytochemicals, and the LC-ESI-MS of the 90% methanol extract identified 26 phenolic compounds classified as phenolic acids, flavonoids, and organic acids. The in vitro studies showed that C. rotundus extracts had a lethal effect on T. spiralis adults, and the LC50 were 156.12 µg/ml, 294.67 µg/ml, 82.09 µg/ml, and 73.16 µg/ml in 90% MeOH ext., EtOAc fr., pet-ether fr. and n-BuOH fr., respectively. The n-BuOH fr. was shown to have the most promising effects in the in vitro studies, which was confirmed by scanning electron microscopy. The in vivo effects of n-BuOH fr. alone and in combination with albendazole using a mouse model were evaluated by counting adults in the small intestine and larvae in the muscles, in addition to the histopathological changes in the small intestine and the muscles. In the treated groups, there was a significant decrease in the number of adults and larvae compared to the control group. Histopathologically, treated groups showed a remarkable improvement in the small intestine and muscle changes. Remarkably, maximal therapeutic effects were detected in the combination therapy compared to each monotherapy. CONCLUSION: Accordingly, C. rotundus extracts may have anti-T. spiralis potential, particularly when combined with albendazole, and they may be used as synergistic to anti-T. spiralis medication therapy.
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Anti-Helmínticos , Cyperus , Humanos , Albendazol , Extratos Vegetais/uso terapêutico , Cyperus/química , Metanol , Anti-Helmínticos/farmacologia , Anti-Helmínticos/uso terapêutico , ÉteresRESUMO
[This retracts the article DOI: 10.1016/j.heliyon.2021.e06205.].
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BACKGROUND: Transcript profiling of differentiating secondary xylem has allowed us to draw a general picture of the genes involved in wood formation. However, our knowledge is still limited about the regulatory mechanisms that coordinate and modulate the different pathways providing substrates during xylogenesis. The development of compression wood in conifers constitutes an exceptional model for these studies. Although differential expression of a few genes in differentiating compression wood compared to normal or opposite wood has been reported, the broad range of features that distinguish this reaction wood suggest that the expression of a larger set of genes would be modified. RESULTS: By combining the construction of different cDNA libraries with microarray analyses we have identified a total of 496 genes in maritime pine (Pinus pinaster, Ait.) that change in expression during differentiation of compression wood (331 up-regulated and 165 down-regulated compared to opposite wood). Samples from different provenances collected in different years and geographic locations were integrated into the analyses to mitigate the effects of multiple sources of variability. This strategy allowed us to define a group of genes that are consistently associated with compression wood formation. Correlating with the deposition of a thicker secondary cell wall that characterizes compression wood development, the expression of a number of genes involved in synthesis of cellulose, hemicellulose, lignin and lignans was up-regulated. Further analysis of a set of these genes involved in S-adenosylmethionine metabolism, ammonium recycling, and lignin and lignans biosynthesis showed changes in expression levels in parallel to the levels of lignin accumulation in cells undergoing xylogenesis in vivo and in vitro. CONCLUSIONS: The comparative transcriptomic analysis reported here have revealed a broad spectrum of coordinated transcriptional modulation of genes involved in biosynthesis of different cell wall polymers associated with within-tree variations in pine wood structure and composition. In particular, we demonstrate the coordinated modulation at transcriptional level of a gene set involved in S-adenosylmethionine synthesis and ammonium assimilation with increased demand for coniferyl alcohol for lignin and lignan synthesis, enabling a better understanding of the metabolic requirements in cells undergoing lignification.
Assuntos
Regulação da Expressão Gênica de Plantas , Lignanas/biossíntese , Lignina/biossíntese , Pinus/metabolismo , Proteínas de Plantas/genética , S-Adenosilmetionina/biossíntese , Madeira/crescimento & desenvolvimento , Parede Celular/genética , Parede Celular/metabolismo , Pinus/genética , Pinus/crescimento & desenvolvimento , Proteínas de Plantas/metabolismo , Madeira/genética , Madeira/metabolismo , Xilema/genética , Xilema/crescimento & desenvolvimento , Xilema/metabolismoRESUMO
Oxidative stress-energy depletion therapy using oxidative stress induced by D-amino acid oxidase (DAO) and energy depletion induced by 3-bromopyruvate (3BP) was reported recently (El Sayed et al., Cancer Gene Ther., 19, 1-18, 2012). Even in the presence of oxygen, cancer cells oxidize glucose preferentially to produce lactate (Warburg effect) which seems vital for cancer microenvironment and progression. 3BP is a closely related structure to lactate and pyruvate and may antagonize their effects as a novel mechanism of its action. Pyruvate exerted a potent H(2)O(2) scavenging effect to exogenous H(2)O(2), while lactate had no scavenging effect. 3BP induced H(2)O(2) production. Pyruvate protected against H(2)O(2)-induced C6 glioma cell death, 3BP-induced C6 glioma cell death but not against DAO/D-serine-induced cell death, while lactate had no protecting effect. Lactate and pyruvate protected against 3BP-induced C6 glioma cell death and energy depletion which were overcome with higher doses of 3BP. Lactate and pyruvate enhanced migratory power of C6 glioma which was blocked by 3BP. Pyruvate and lactate did not protect against C6 glioma cell death induced by other glycolytic inhibitors e.g. citrate (inhibitor of phosphofructokinase) and sodium fluoride (inhibitor of enolase). Serial doses of 3BP were synergistic with citrate in decreasing viability of C6 glioma cells and spheroids. Glycolysis subjected to double inhibition using 3BP with citrate depleted ATP, clonogenic power and migratory power of C6 glioma cells. 3BP induced a caspase-dependent cell death in C6 glioma. 3BP was powerful in decreasing viability of human glioblastoma multiforme cells (U373MG) and C6 glioma in a dose- and time-dependent manner.
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Antineoplásicos Alquilantes/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Glioblastoma/metabolismo , Glioma/metabolismo , Ácido Láctico/antagonistas & inibidores , Piruvatos/farmacologia , Ácido Pirúvico/antagonistas & inibidores , Apoptose/efeitos dos fármacos , Ácido Cítrico/metabolismo , D-Aminoácido Oxidase/farmacologia , Eletroforese em Gel de Poliacrilamida , Glioblastoma/tratamento farmacológico , Glioma/tratamento farmacológico , Glicólise/efeitos dos fármacos , Humanos , Peróxido de Hidrogênio/metabolismo , Immunoblotting , Ácido Láctico/farmacologia , Estresse Oxidativo , Ácido Pirúvico/farmacologia , Sais de Tetrazólio , TiazóisRESUMO
Angiogenesis is critical for cancer growth and metastasis. Steps of angiogenesis are energy consuming, while vascular endothelial cells are highly glycolytic. Glioblastoma multiforme (GBM) is a highly vascular tumor and this enhances its aggressiveness. D-amino acid oxidase (DAO) is a promising therapeutic protein that induces oxidative stress upon acting on its substrates. Oxidative stress-energy depletion (OSED) therapy was recently reported (El Sayed et al., Cancer Gene Ther, 19, 1-18, 2012). OSED combines DAO-induced oxidative stress with energy depletion caused by glycolytic inhibitors such as 3-bromopyruvate (3BP), a hexokinase II inhibitor that depleted ATP in cancer cells and induced production of hydrogen peroxide. 3BP disturbs the Warburg effect and antagonizes effects of lactate and pyruvate (El Sayed et al., J Bioenerg Biomembr, 44, 61-79, 2012). Citrate is a natural organic acid capable of inhibiting glycolysis by targeting phosphofructokinase. Here, we report that DAO, 3BP and citrate significantly inhibited angiogenesis, decreased the number of vascular branching points and shortened the length of vascular tubules. OSED delayed the growth of C6/DAO glioma cells. 3BP combined with citrate delayed the growth of C6 glioma cells and decreased significantly the number and size of C6 glioma colonies in soft agar. Human GBM cells (U373MG) were resistant to chemotherapy e.g. cisplatin and cytosine arabinoside, while 3BP was effective in decreasing the viability and disturbing the morphology of U373MG cells.
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Quelantes/farmacologia , Ácido Cítrico/farmacologia , D-Aminoácido Oxidase/metabolismo , Inibidores Enzimáticos/farmacologia , Glioblastoma/tratamento farmacológico , Neovascularização Patológica/tratamento farmacológico , Estresse Oxidativo/efeitos dos fármacos , Piruvatos/farmacologia , Trifosfato de Adenosina/genética , Trifosfato de Adenosina/metabolismo , Animais , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Cisplatino/farmacologia , Citarabina/farmacologia , D-Aminoácido Oxidase/genética , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/genética , Metabolismo Energético/efeitos dos fármacos , Metabolismo Energético/genética , Glioblastoma/enzimologia , Glioblastoma/genética , Hexoquinase/antagonistas & inibidores , Hexoquinase/genética , Hexoquinase/metabolismo , Células Endoteliais da Veia Umbilical Humana , Humanos , Peróxido de Hidrogênio/metabolismo , Camundongos , Neovascularização Patológica/enzimologia , Neovascularização Patológica/genética , Neovascularização Patológica/patologiaRESUMO
Cryptosporidiosis causes diarrhea in both immunocompetent and immunocompromised individuals, with acute manifestations occurring particularly in children and the elderly. Up till now, there is no curative therapy for cryptosporidiosis, so discovery of new classes of drugs are of great importance. This study aimed to examine the effect of methanol leaves extracts of the three Podocarpus species; P. macrophyllus (Thunb.), P. gracilior (Pilg.) and P. elongatus (Aiton) L' Hér. ex Pers and their combination on Cryptosporidium parvum (C. parvum) in experimentally infected mice in comparison with the commercially used drug, Nitazoxanide. As well as spectrophotometric estimation of the total phenolic and flavonoid content of these extracts was done. Results revealed that treatment with these three Podocarpus extracts and their combination showed a significant reduction of the number of C. parvum oocyst shed in the stool of infected mice compared to infected control group and Nitazoxanide- infected treated group at P < 0.001. The combination of the three Podocarpus extracts was the most effective treatment showing the lowest number of oocysts shedding in comparison with other used extracts and Nitazoxanide. Histopathological inspection of sections from ilium and colon displayed signs of improvement after treatment with P. macrophyllus and P. gracilior extracts and more remarkable improvement when the three extracts were combined. It was concluded that the three Podocarpus species extracts used in this study had a promising anti-Cryptosporidium activity especially when they were combined.
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Criptosporidiose , Cryptosporidium parvum , Cryptosporidium , Animais , Criptosporidiose/tratamento farmacológico , Fezes , Feminino , Metanol/farmacologia , Metanol/uso terapêutico , Camundongos , Oocistos , Extratos Vegetais/farmacologiaRESUMO
A new homoisoflavan, identified as (3 R)-7-hydroxy-3',4'-methylenedioxyhomoisoflavan, was isolated from Dracaena cinnabari Balf. f. resin. The structure was elucidated by one- and two-dimensional NMR spectroscopy as well as high resolution mass spectrometry. In addition, a diverse group of flavonoids were isolated, representing homoisoflavans, flavans, flavanones, chalcones and dihydrochalcones. The compounds were evaluated for their α-glucosidase and COX-II inhibition activity. The obtained IC50 values of the tested flavonoids gave an insight about some key structural features to their α-glucosidase and COX-II inhibitory activity. For α-glucosidase inhibitory activity, a flavanone skeleton was favorable over a flavan. For COX-II inhibition, the introduction of a fused heterocyclic ring at the homoisoflavan skeleton enhanced the activity.
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Chalconas , Dracaena , Chalconas/química , Chalconas/farmacologia , Inibidores de Ciclo-Oxigenase 2 , Dracaena/química , Flavonoides/farmacologia , Inibidores de Glicosídeo Hidrolases , Extratos Vegetais/química , Resinas Vegetais/química , alfa-GlucosidasesRESUMO
Six phenolic compounds (talaroflavone (1), alternarienoic acid (2), altenuene (3), altenusin (4), alternariol (5), and alternariol-5-O-methyl ether (6)) were isolated from the solid rice culture media of Alternaria sp., an endophyte isolated from the fresh leaves of three desert plants, Lycium schweinfurthii Dammer (Solanaceae), Pancratium maritimum L. (Amaryllidaceae) and Cynanchum acutum L. (Apocynaceae). Compounds 2, 3, and 4 exhibited potent α-glucosidase and lipase inhibitory activities suggesting that they might act as naturally occurring anti-diabetic candidates. The same compounds showed potent binding in the active site for both enzymes with desirable pharmacokinetic properties. The isolated bioactive compounds were not exclusive to a certain host plant which reveals the dominant ecological standpoints for consequent optimization. This could lead to a cost-effective and reproducible yield applicable to commercial scale-up.
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Tomato (Lycopersicon esculentum Mill.) is important food in daily human diets. Root rot disease by Fusarium oxysporum caused huge losses in tomato quality and yield annually. The extensive use of synthetic and chemical fungicides has environmental risks and health problems. Recent studies have pointed out the use of medicinal plant essential oils (EOs) and extracts for controlling fungal diseases. In the current research, Mentha spicata and Mentha longifolia EOs were used in different concentrations to control F. oxysporum. Many active compounds are present in these two EOs such as: thymol, adapic acid, menthol and menthyl acetate. These compounds possess antifungal effect through malformation and degradation of the fungal cell wall. The relative expression levels of distinctly upregulated defense-related WRKY genes (WRKY1, WRKY4, WRKY33 and WRKY53) in seedling root were evaluated as a plant-specific transcription factor (TF) group in different response pathways of abiotic stress. Results showed significant expression levels of WRKY, WRKY53, WRKY33, WRKY1 and WRKY4 genes. An upregulation was observed in defense-related genes such as chitinase and defensin in roots by application EOs under pathogen condition. In conclusion, M. spicata and M. longifolia EOs can be used effectively to control this plant pathogen as sustainable and eco-friendly botanical fungicides.
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Two new compounds, 11S-methoxy-11,12-dihydro phytuberin (2) and 9S-methoxy-benzocyclononan-7-one (6), together with twenty-six known ones were isolated from Lycium schweinfurthii (Solanaceae). Their planar structure was established by extensive spectroscopic analyses. The absolute configuration of compound 6 was determined by time dependent density functional theory calculations (TDDFT). The cytotoxic potential of the isolates was assessed in cultured skin cancer (G-361) and colon cancer (HCT-116 and CaCo-2) cell lines. Certain flavonoids showed the highest cytotoxic activity, with IC50 values ranging from 7.1 to 63.3 µM; meanwhile 5-flurouracil showed IC50 values ranging from 62.4 to >100 µM. All compounds showed minimal toxicity towards normal cells from skin (NHDF-4) and colon (CCD-841), indicating their potential selectivity and safety as cytotoxic candidates.
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Antineoplásicos , Lycium , Antineoplásicos/química , Antineoplásicos/farmacologia , Células CACO-2 , Flavonoides , Humanos , Lycium/química , Estrutura MolecularRESUMO
A new C-linked chalcone-dihydrochalcone dimer, named dracidione, was isolated from the ethyl acetate extract of dragon's blood resin of Dracaena cinnabari Balf. f. Structure elucidation of the new compound was carried out by means of one- and two-dimensional NMR spectroscopy in addition to high resolution mass spectrometry. The unique structure incorporated a chalcone and a dihydrochalcone, which is reported for the first time from nature. Furthermore, dracidione showed moderate α-glucosidase inhibitory activity with IC50= 40.27 µg/ml.
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Chalconas/farmacologia , Dracaena , Chalconas/química , Chalconas/isolamento & purificação , Resinas VegetaisRESUMO
A new glucoside, 3-methoxy-4-O-ß-D-glucopyranosyl-methyl benzoate, has been isolated from Lycium schweinfurthii along with five known compounds through bioactivity guided fractionation of the total plant methanolic extract towards α-glucosidase inhibitory activity. All the isolated compounds were tested for their inhibitory effect on α-glucosidase enzyme. As a result, four of them showed a potent inhibitory activity and thus constitute a therapeutic approach to decrease postprandial hyperglycemia in diabetic patients.
Assuntos
Glucosídeos/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Lycium/química , 1-Butanol/química , Acetatos/química , Fracionamento Químico , Diabetes Mellitus , Glucosídeos/química , Glucosídeos/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Humanos , Metanol/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Glucosidases/metabolismoRESUMO
BACKGROUND: The plant kingdom is considered one of the most common sources for structural and biological diversity. In particular, the wild category acquires our attention to investigate the phytochemical and the biological evaluations. METHODS: Dobera glabra was exposed to phytochemical examination using HPLC-ESI-MS analysis. Furthermore, the anti-inflammatory activity was evaluated using carrageenan-induced rat paw edema model, whereas both the central and peripheral analgesic activities were tested via hot plate test in rats and acetic acid-induced writhing in mice, respectively. RESULTS: Twenty phenolic compounds of D. glabra aqueous leaves extract were emphasized by liquid chromatography coupled with mass spectrometry. Moreover, D. glabra exhibited both anti-inflammatory and peripheral analgesic activities. Furthermore, D. glabra significantly decreased the immune expression of MMP-9, TNF-α and TGF-ß1 in the hind paw of rats. CONCLUSION: D. glabra possess peripheral anti-nociceptive and anti-inflammatory effects in rats mediated through its anti-oxidant and anti-inflammatory activities. The activity of D. glabra leaves extract might be attributed to the presence of hydroxy and keto structures.