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AIM: To develop and implement of a group-based acceptance and commitment therapy programme in helping clinical nurses with mental health problems during the sporadic COVID-19 outbreak period. BACKGROUND: In the face of the continuing COVID-19 pandemic, clinical nurses have a high risk of mental health issues. METHODS: A quasi-experimental design was used. Two hundred twenty-six nurses were recruited from four general hospitals to receive 10 sessions of acceptance and commitment therapy programme. The Symptom Checklist-90, Perceived Stress Scale and Connor-Davidson Resilience Scale were used to assess nurses' mental health symptom, perceived stress and psychological resilience at pre-intervention and 4-week post-intervention. RESULTS: The mean attendance sessions was 5.78. The Symptom Checklist-90 score was significantly lower at post-intervention than pre-intervention (P < 0.01), and there were no significant changes of perceived stress and psychological resilience. There were significant correlations among the changed rates of mental health, perceived stress and psychological resilience (P < 0.01). CONCLUSION: The acceptance and commitment therapy programme was effective in relieving mental health symptoms for clinical nurses and could protect clinical nurses' perceived stress and psychological resilience. However, a randomized controlled trial is needed to confirm the findings. IMPLICATION FOR NURSING MANAGEMENT: To facilitate clinical nurses' psychological health in crisis situation, nursing management team should provide and allocated appropriate resources to support the healthcare providers.
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Terapia de Aceitação e Compromisso , COVID-19 , Enfermeiras e Enfermeiros , Resiliência Psicológica , Humanos , COVID-19/epidemiologia , Saúde Mental , Pandemias , Surtos de DoençasRESUMO
Harmine (HAR) is a ß-carboline alkaloid with anti-inflammatory and antipruritic effect. However, the low bioavailability and side effects of HAR severely limited its clinical application. The main objective of this study was to develop harmine-loaded ethosomes (HLE) drug delivery system for topical application to treat inflammation. HLE were obtained by ethanol injection method and characterized. The morphology of HLE was evaluated by transmission electron microscopy (TEM). HLE exhibited a good biocompatibility with human embryonic skin fibroblasts and rat skin. The in vitro skin penetration studies showed that HLE had the greatest skin deposition than harmine-loaded liposomes (HLL) and harmine solution (HS). In vivo pharmacokinetic study demonstrated that AUC(0-∞) and Cmax of HLE in subcutaneous tissues were much higher than that of in blood. Moreover, for convenience of fixing on skin, HLE were mixed with gel. HLE gel significantly inhibited the overexpression of inflammation cytokines prostaglandin E2, interleuking (IL)-1ß, nitric oxide, and tumor necrosis factor-alpha (TNF-α) in the inflammation model of rat paw edema compared with HS gel. In short, HLE was promising formulation for topical delivery in treatment of inflammatory diseases.
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Anti-Inflamatórios/administração & dosagem , Sistemas de Liberação de Medicamentos , Harmina/administração & dosagem , Inflamação/tratamento farmacológico , Administração Cutânea , Animais , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/farmacologia , Área Sob a Curva , Modelos Animais de Doenças , Edema/tratamento farmacológico , Edema/patologia , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Harmina/farmacocinética , Harmina/farmacologia , Humanos , Inflamação/patologia , Lipossomos , Ratos , Ratos Sprague-Dawley , Pele/metabolismo , Absorção CutâneaRESUMO
Ulcerative colitis (UC) is usually accompanied with symptoms of abdominal pain, diarrhea, and bloody stool, which impair the quality of life of patients. Previous studies have shown that Andrographis paniculata extracts, which have andrographolide (AND) as their main compound, can relieve UC symptoms in patients. The aim of the study was to investigate the alleviating effect of AND on UC using the oxazolone (OXZ)-induced UC rat model. A total of 66 healthy male Sprague Dawley rats were used to evaluate the efficacy and mechanism of AND on UC (n = 11 per group) and grouped into control, model, SASP (sulfasalazine, positive control group, 500 mg/kg), AND-L (40 mg/kg), AND-M (80 mg/kg), and AND-H (120 mg/kg). The colonic disease activity index (DAI), colon length, spleen coefficient, pathological damage, and inflammation-related cytokine and protein expression levels were used as indices for evaluation. Results showed that the AND groups had reduced DAI and mortality, and significantly improved colon length and spleen coefficient compared with the model group. Furthermore, OXZ-induced histological injury was relieved significantly after AND treatment due to an improved crypt structure and reduced infiltration of inflammatory cells. Moreover, AND inhibited myeloperoxidase (MPO) activity and the secretion of interleukin-4 (IL-4), IL-13, and tumor necrosis factor α (TNF-α). The results of the anti-inflammatory mechanism revealed that AND blocked the signal transduction by reducing IL-4/IL-13 specific binding to IL-4 receptor (IL-4R) and inhibiting the phosphorylation of the signal transducer and activator of transcription 6 (p-STAT6). In conclusion, aside from natural plants, AND may be a candidate ingredient for UC therapy.
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Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Diterpenos/uso terapêutico , Animais , Biomarcadores/metabolismo , Colite Ulcerativa/patologia , Colo/patologia , Citocinas/metabolismo , Diterpenos/farmacologia , Inflamação/patologia , Masculino , Oxazolona , Peroxidase/metabolismo , Ratos Sprague-Dawley , Receptores de Interleucina-4/metabolismo , Fator de Transcrição STAT6/metabolismo , Transdução de Sinais , Fator de Transcrição RelA/metabolismoRESUMO
The purpose of this study was to investigate the distribution of Chlamydia trachomatis (CT) genotypes in infective diseases of the female lower genital tract, especially in cervical diseases. This study included 128 CT-positive women. DNA was extracted from cervical swabs. Omp1 gene PCR-RFLP and sequencing were used to confirm the subtypes of CT. The association of subtypes with age, clinical symptoms, cervical cytology, and biopsy results was further analyzed. Omp1 gene PCR-RFLP and sequencing showed that the order of prevalent CT genotypes in the female lower genital tract was D (n=38, 29.69%), followed by E (n=28, 21.88%), G (n=21, 16.41%), and F (n=16,12.50%). Genotypes J, H, and K were comparatively rare. Genotype I was not identified in our samples. Further analysis showed that patients with genotype G were more frequently co-infected with other bacteria. Genotype G was also associated with mucopurulent cervicitis (MPC) and cervical intraepithelial neoplasia (CIN). Patients with genotype E were commonly co-infected with HR-HPV. Although genotype D was the most prevalent, it was a relatively low-risk type. These results provide information on distribution of CT genotypes in infective diseases of the female lower genital tract, which is instrumental to developing a vaccine for CT.
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Chlamydia trachomatis/genética , Trato Gastrointestinal Inferior/microbiologia , Porinas/genética , Adulto , China/epidemiologia , Chlamydia trachomatis/patogenicidade , Doenças Transmissíveis/etiologia , Doenças Transmissíveis/microbiologia , Feminino , Genitália/microbiologia , Genótipo , Humanos , Pessoa de Meia-Idade , Reação em Cadeia da Polimerase , Porinas/análise , Análise de Sequência de DNA , Neoplasias do Colo do Útero/virologia , Esfregaço Vaginal/métodos , Adulto Jovem , Displasia do Colo do Útero/virologiaRESUMO
Two new sesquiterpenes, microsphaeropsisin B (1) and C (2), and two new de-O-methyllasiodiplodins, (3R, 7R)-7-hydroxy-de-O-methyllasiodiplodin (4) and (3R)-5-oxo-de-O-methyllasiodiplodin (5), together with one new natural product (6) and twelve known compounds (3, 7-17), were isolated from the co-cultivation of mangrove endophytic fungus Trichoderma sp. 307 and aquatic pathogenic bacterium Acinetobacter johnsonii B2. Their structures, including absolute configurations, were elucidated by extensive analysis of spectroscopic data, electronic circular dichroism, Mo2(AcO)4-induced circular dichroism, and comparison with reported data. All of the isolated compounds were tested for their α-glucosidase inhibitory activity and cytotoxicity. New compounds 4 and 5 exhibited potent α-glucosidase inhibitory activity with IC50 values of 25.8 and 54.6 µM, respectively, which were more potent than the positive control (acarbose, IC50 = 703.8 µM). The good results of the tested bioactivity allowed us to explore α-glucosidase inhibitors in lasiodiplodins.
Assuntos
Acinetobacter/química , Acinetobacter/metabolismo , Produtos Biológicos/metabolismo , Endófitos/metabolismo , Trichoderma/química , Trichoderma/metabolismo , Produtos Biológicos/química , Dicroísmo Circular/métodos , Endófitos/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/metabolismo , Concentração Inibidora 50 , Macrolídeos/química , Macrolídeos/metabolismo , Sesquiterpenos/química , Sesquiterpenos/metabolismo , Zearalenona/análogos & derivados , Zearalenona/química , alfa-Glucosidases/química , alfa-Glucosidases/metabolismoRESUMO
To study the pharmacokinetic characteristics and absolute bioavailability of α-asarone through dry powder inhalation in rats, and compare with that through oral administration and intravenous injection. A HPLC method was established for the determination of α-asarone in rat plasma to detect the changes in plasma concentrations of α-asarone through dry powder inhalation (20 mg · kg(-1)), oral administration (80 mg · kg(-1)) and intravenous injection (20 mg · kg(-1)) in rats. DAS 2.0 software was used to calculate the pharmacokinetic parameters. The absolute bioavailability of α-asarone was calculated according to AUC(0-t)) of administration routes and administration doses. According to the results, α-asarone showed good linear relations (r = 0. 999 4) at concentrations between 0.282-14.1 mg · L(-1), with the limit of detection (LOD) at 0.212 mg · L(-1). Through dry powder inhalation, oral administration and intravenous injection of α-asarone, the metabolic processes of α-asarone in rats conformed to one, two and three compartment models respectively, with the elimination half-life of (95.48 ± 48.28), (64.34 ± 27.59), (66.99 ± 29.76) min. According to the bioavailability formula, the absolute bioavailability of α-asarone through dry powder inhalation and oral administration were 78.32% and 33. 60%, respectively. This study showed that significant increase in elimination half-life and absolute bioavailability of α-asarone through dry powder inhalation, which lays a theoretical foundation for preparing α-asarone dry powder inhalers.
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Anisóis/farmacocinética , Medicamentos de Ervas Chinesas/farmacocinética , Administração por Inalação , Derivados de Alilbenzenos , Animais , Anisóis/administração & dosagem , Anisóis/sangue , Disponibilidade Biológica , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/análise , Meia-Vida , Masculino , Ratos , Ratos Sprague-DawleyRESUMO
In this study, solvent evaporation method was used to preparing baicalin ethylcellulose microspheres for intranasal administration. The prepared microspheres were round with certain rough surface. The average drug loading and entrapment efficiency was (33. 31 ± 0. 045)% , (63. 34 ± 0. 11)% , respectively. As the characteristic crystalline peaks of baicalin were observed in the microspheres sample, the result of X-ray diffractometric analysis indicated that the baicalin was present in crystalline form after its entrapment in ethylcellulose matrix. By investigating the thermogram of microspheres sample, it was found that endothermic peak of baicalin was shifted from 211. 8 °C to 244. 2 °C and associated with the first broad endothermic peak of ethylcellulose. This could confirm that baicalin was loaded into ethylcellulose, nor simply physical mixture. The powder flowability test exhibited that the specific energy of microspheres was 3. 57 mJ . g-1 and the pressure drop was 2. 22 mBar when air kept the speed of 2 mm . s-1 through the powder bed with the force was 15 kPa. The consequence of the baicalin in vitro released from microspheres showed that the pure baicalin sample displayed faster (90%) release than microspheres sample (75%) in 7 h. Fitting model for release curve before 7 h, the results showed that the pure baicalin sample and the microsphere sample accorded with first order model (R2 = 0. 990 4) and Riger-Peppas model(R2 = 0. 961 2), respectively. Ex vivo rabbit nasal mucosa permeability experiment revealed that the value of cumulative release rate per unit area of the microsphere sample was 1. 56 times that of the pure baicalin sample. This provided the foundation for the in vivo pharmacokinetic study.
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Celulose/análogos & derivados , Composição de Medicamentos/métodos , Flavonoides/farmacocinética , Administração Intranasal , Pressão do Ar , Animais , Celulose/química , Flavonoides/administração & dosagem , Flavonoides/química , Masculino , Microesferas , Mucosa/metabolismo , Tamanho da Partícula , Pós , Coelhos , Solventes , Difração de Raios XRESUMO
OBJECTIVE: By studying the process of reverse osmosis system for traditional Chinese medicine materials physicochemical parameters affecting the osmotic pressure of its relevance, new compound system reverse osmosis process design methods were explored. METHOD: Three concentrations materials for high, middle and low were dubbed with Sini decoction as a model drug, and pretreated by 50 thousand relative molecular weight cut-off ultrafiltration membrane. The viscosity, turbidity, conductivity, salinity, TDS, pH value and osmotic pressure of each sample were determined after the reverse osmosis to study the physical and chemical parameters between their respective correlations with the osmotic pressure, and characterized by HPLC chromatograms showing changes before and after the main chemical composition of samples of reverse osmosis. RESULT: Conductivity-osmotic pressure, salinity-osmotic pressure of the linear correlation coefficient, TDS-osmotic pressure between the three sets of parameters were 0.963 8, 0.932 7, 0.973 7, respectively. Reverse osmosis concentrate and its characteristic spectrum ultrafiltrate HPLC similarity were up to 0. 968 or more, except the low concentrations. CONCLUSION: There is a significant correlation between the three physicochemical parameters (conductivity, salinity, TDS) and osmotic pressure of each sample system, and there is also significant linear correlation between salinity, conductivity, TDS. The original chemical composition of Sini decoction material concentrate was completely remained after the process of reverse osmosis.
Assuntos
Química Farmacêutica/métodos , Medicamentos de Ervas Chinesas/química , Fenômenos Químicos , Cromatografia Líquida de Alta Pressão , Peso Molecular , Pressão Osmótica , Propriedades de Superfície , ViscosidadeRESUMO
BACKGROUND: Myocardial infarction (MI) is an acute condition in which the heart muscle dies due to the lack of blood supply. Previous research has suggested that autophagy and angiogenesis play vital roles in the prevention of heart failure after MI, and miR-106a is considered to be an important regulatory factor in MI. But the specific mechanism remains unknown. In this study, using cultured venous endothelial cells and a rat model of MI, we aimed to identify the potential target genes of miR-106a and discover the mechanisms of inhibiting autophagy and angiogenesis. METHODS: We first explored the biological functions of miR-106a on autophagy and angiogenesis on endothelial cells. Then we identified ATG7, which was the downstream target gene of miR-106a. The expression of miR-106a and ATG7 was investigated in the rat model of MI. RESULTS: We found that miR-106a inhibits the proliferation, cell cycle, autophagy and angiogenesis, but promoted the apoptosis of vein endothelial cells. Moreover, ATG7 was identified as the target of miR-106a, and ATG7 rescued the inhibition of autophagy and angiogenesis by miR-106a. The expression of miR-106a in the rat model of MI was decreased but the expression of ATG7 was increased in the infarction areas. CONCLUSION: Our results indicate that miR-106a may inhibit autophagy and angiogenesis by targeting ATG7. This mechanism may be a potential therapeutic treatment for MI.
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OBJECTIVES: To estimate the level of anhedonia among adolescents and explore the association between anhedonia and childhood trauma (CT). DESIGN: A stratified random cluster sample of adolescents participated in a survey, which included three questionnaires: Snaith-Pamilton Pleasure Scale, Childhood Trauma Questionnaire and Patient Health Questionnaire-9. SETTING: The study was conducted in 60 classes in 10 primary, middle and high schools in five economically developed cities along the Southeast Coast of China from April to October 2022. PARTICIPANTS: One thousand seven hundred and forty-five adolescents with ages ranging from 9 to 18 years participated in the study. PRIMARY AND SECONDARY OUTCOMES: The primary outcome was the level of anhedonia, CT and depression among adolescents. The association between anhedonia and CT was determined. RESULTS: The mean scores of anhedonia, CT and depression were 24.88 (6.18), 36.75 (8.87) and 4.46 (5.36), respectively. Anhedonia scores of boys (24.24±6.12) and girls (25.62±6.16) were different (t=-4.69, p<0.01). After controlling for sex, age, the presence of siblings and depression, CT was associated with adolescent anhedonia. Emotional abuse (ß=0.14), emotional neglect (ß=0.15) and physical neglect (ß=0.10) positively predicted adolescent anhedonia (p<0.01), whereas physical abuse negatively predicted adolescent anhedonia (ß=-0.07, p<0.01). Sex had a moderating effect on the relationship between adolescent anhedonia and emotional neglect during childhood, and the negative effect of emotional neglect on adolescent anhedonia in girls was greater than in boys. CONCLUSIONS: CT, including emotional abuse, physical abuse, emotional neglect, and physical neglect, was an independent predictor of adolescents' ability to experience pleasure in daily life. Therefore, awareness of CT should be promoted. Emotional neglect had a more severe effect on anhedonia among girls than among boys, suggesting that emotional neglect should be paid much attention among girls.
Assuntos
Experiências Adversas da Infância , Anedonia , Maus-Tratos Infantis , População do Leste Asiático , Adolescente , Criança , Feminino , Humanos , Masculino , Estudos Transversais , Inquéritos e Questionários , ChinaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The seeds of Peganum harmala Linn have been widely used for the treatment of nervous, cardiovascular, gastrointestinal, respiratory, and endocrine diseases and many other human ailments. However, tremor toxicity occurs after overdose and is tolerated following multiple dosing. Thus far, little is known about the underlying mechanisms of tremors and tremor tolerance. AIM OF THE STUDY: To investigate the potential mechanisms of tremors and tremor tolerance induced in rats by the repeated administration of total alkaloid extracts from the seeds of P. harmala (TAEP). MATERIALS AND METHODS: A tremor model was induced in male Wistar rats by administering TAEP at a dose of 150 mg/kg/day. To evaluate tremor action, behavioral assessment was conducted by using a custom-built tremor acquisition and analysis system. To investigate the relationships between tremors and neurotransmitter levels in the brain, various neurotransmitters were simultaneously quantified by an ultra-performance liquid chromatography combined with electrospray ionization-tandem mass spectrometry (UPLC-ESI-MS/MS) system, and the association between these two parameters was analyzed using Pearson correlation coefficients. To further elucidate the potential mechanisms of the alterations of neurotransmitter levels in cortical tissues, the protein expression levels of several important enzymes and transporters that are closely related to neurotransmitter levels were investigated. In addition, neuropathological analysis was conducted to assess the effect of TAEP on neurons in the brain. To further clarify the potential mechanisms of TAEP-induced neurodegeneration in the brain, c-fos was subjected to immunohistochemical analysis, and oxidative stress markers were examined. RESULTS: Tremors initially occurred in rats after the oral administration of TAEP at a dose of 150 mg/kg/day. However, they were tolerated following repeated dosing. The levels of 5-hydroxytryptamine (5-HT) and glycine (Gly) in cortical tissues were most likely associated with the tremor response. Tremor tolerance also likely resulted from the degeneration of cerebellar Purkinje cells. Furthermore, the alteration of 5-HT levels was mainly attributed to the downregulated expression of monoamine oxidase A (MAO-A). The degeneration of Purkinje neurons might have resulted from the overexpression of c-fos and increased oxidative stress in the cerebellum after the multiple dosing of TAEP. CONCLUSION: The tremor response induced by TAEP at high doses is closely related to the concentrations of 5-HT and Gly in cortical tissues. Tremor tolerance may also be attributed to the degeneration of cerebellar Purkinje cells after the repeated dosing of TAEP. Further studies should be conducted to elucidate the interaction of the alkaloids on the neurotransmitter receptors, the expression of related neurotransmitter receptors, the specific signaling pathway involved in regulating MAO-A, and the mechanism of the loss and functional recovery of cerebellar Purkinje neurons.
Assuntos
Alcaloides/toxicidade , Peganum , Extratos Vegetais/toxicidade , Sementes , Tremor/induzido quimicamente , Tremor/metabolismo , Alcaloides/isolamento & purificação , Animais , Esquema de Medicação , Masculino , Monoaminoxidase/metabolismo , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Wistar , Serotonina/metabolismoRESUMO
Based on daily temperature data of 86 weather stations during winter producing season from 1961 to 2017 in Guangdong Province, the temporal and spatial distribution of extreme chilling was analyzed. The return periods of extreme chilling at county level were calculated with the theory of generalized extreme value distribution to provide technical support for extreme chilling risk assessment and early warning together with real-time meteorological disaster prevention and mitigation in winter planting areas. Results showed that there was a general downward trend of the extreme values of chilling accumulation in main winter planting zones. Zhanjiang and Meizhou had declined significantly since the mid-1980s, while Maoming, Shaoguan and Guangzhou had declined significantly since the 21st century. The extreme minimum temperature followed a curve trending generally downward first and upward later on, with a significant rising in Shaoguan from later 1980s while a descending in Guangzhou in the last five years. The order of the number of extreme value stations of chilling accumulation was 1970s ï¼ the 21st century ï¼ 1990s ï¼ 1960s ï¼ 1980s. The order of the number of stations of extreme minimum temperature was 1960s ï¼ 1990s ï¼ the 21st century ï¼ 1970s ï¼ 1980s. The theoretical forecast values of cold disaster of 2, 5, 10, 20, 50, and 100 year return period showed obvious zonal distribution characteristics. The chilling accumulation diminished from the north to the south and the extreme minimum temperature was higher in the south and lower in the north, which was consistent with the distribution trend in the actual occurrence of cold damage. Typical cases showed more extended chilling return periods in the south than in the north. In Zhanjiang and Maoming, the main producing areas of winter crops in Guangdong Province, the return period of cold damage was long, the probability of extreme cold damage was small but the damage was heavy, and the area of winter crops was in the front rank, which should be paid attention. Our results could provide scientific reference for local government and relevant departments in Guangdong Province to guide winter planting and develop countermeasures against climate change.
Assuntos
Mudança Climática , Temperatura Baixa , China , Estações do Ano , Tempo (Meteorologia)RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The seeds of Peganum harmala Linn, in which the most abundant active compounds are harmaline and harmine, have been widely used as a traditional medicine in various countries to treat a broad spectrum of diseases including asthma, cough, depression, Parkinson's and Alzheimer's diseases. However, few studies on long-term or subchronic toxicity of seeds of P. harmala were reported after overdose. AIM OF THE STUDY: To investigate the subchronic toxicity and concomitant toxicokinetics of total alkaloid extracts from seeds of P. harmala (TAEP) after oral administration for four weeks in rats. MATERIALS AND METHODS: The subchronic toxicity and concomitant toxicokinetics of TAEP were evaluated after 28-day oral administration in rats at daily dose levels of 15, 45, and 150â¯mg/kg. The signs of toxicity and mortality were monitored and recorded daily. The body weight and average food consumption were measured weekly. The analyses of hematology, biochemistry, urine, relative organ weights and histopathology were conducted at the termination of treatment and recovery phase. For concomitant toxicokinetics study, the plasma toxicokinetic parameters, tissue distribution, and excretion of predominant ingredients harmaline and harmine in TAEP and metabolites harmalol and harmol were tested. RESULTS: Following initial repeated exposure to high-dose (150â¯mg/kg/day) of TAEP excitotoxic reaction, such as tremor, was observed, but tolerated on the fourth day after multiple dosing. The significant alterations in blood glucose and lipid metabolism in liver were observed, but recovered after four weeks of drug withdrawal. The no-observed-adverse-effect level (NOAEL) of TAEP was considered to be 45â¯mg/kg/day under the present study conditions. There were no significant gender differences in most indexes of subchronic toxicity throughout the experimental period with the exception of food consumption and body weight. In concomitant toxicokinetics study, the alterations of dynamic characteristic for harmaline, harmine and metabolite harmol after multiple oral administration at three doses had been observed. Harmaline, harmine and metabolites harmalol and harmol were widely distributed in organs and there was no accumulation in the tissues examined. The reduction of harmaline and metabolite harmalol in brain after multiple dosing at dose of 150â¯mg/kg might be closely related to the tremor tolerance. The main excretory pathway for metabolites harmalol and harmol was urinary excretion via kidney. CONCLUSIONS: The results revealed that TAEP at doses of 15 and 45â¯mg/kg/day in rats might be safe. Excitotoxic reaction such as tremor occurred initially at dose of 150â¯mg/kg/day, however, the toxicity was tolerant and reversible. In addition, harmaline and harmine in TAEP had a quick absorption into blood and metabolized to harmalol and harmol, and there was no drug accumulation in the detected tissues. Further studies should be investigated to clarify the mechanisms of tremor tolerance and neurotoxicity of TAEP.
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Alcaloides/farmacocinética , Alcaloides/toxicidade , Peganum , Extratos Vegetais/farmacocinética , Extratos Vegetais/toxicidade , Administração Oral , Animais , Feminino , Alcaloides de Harmala/sangue , Masculino , Ratos Wistar , Sementes , Testes de Toxicidade Subcrônica , Toxicocinética , Tremor/induzido quimicamenteRESUMO
One new depsidone, botryorhodine H (1), together with three known analogues, botryorhodines C, D and G (2-4), were obtained from the mangrove endophytic fungus Trichoderma sp. 307 by co-culturing with Acinetobacter johnsonii B2. Structures were determined by 1D and 2D NMR analyses and high-resolution mass spectrum. Compounds 1-3 showed α-glucosidase inhibitory activity with IC50 ranging from 8.1 to 11.2 µM, and compound 1 exhibited potent cytotoxicity against rat prolactinoma MMQ and rat pituitary adenoma GH3 cell lines (IC50 = 3.09 and 3.64 µM).
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Inibidores de Glicosídeo Hidrolases/farmacologia , Trichoderma/química , Acinetobacter/citologia , Animais , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Linhagem Celular , Técnicas de Cocultura , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/uso terapêutico , Concentração Inibidora 50 , Estrutura Molecular , Neoplasias Hipofisárias/tratamento farmacológico , Extratos Vegetais/química , Policetídeos/química , Policetídeos/isolamento & purificação , Prolactinoma/tratamento farmacológico , RatosRESUMO
Two different culture media were used to cultivate fungus Aspergillus ruber 1017 and resulted in the isolation of one new compound (1) and 23 known compounds (2-24). Alkaloids were the major metabolite in soybean medium instead of anthraquinone from rice medium. The structures of these compounds were elucidated according to spectroscopic analysis and comparison with reported data. Antibacterial activities of compounds 1-12 against 12 aquatic bacteria were evaluated.
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Aspergillus/metabolismo , Meios de Cultura/farmacologia , Alcaloides/isolamento & purificação , Alcaloides/metabolismo , Antraquinonas/metabolismo , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Aspergillus/química , Bactérias/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Oryza/metabolismo , Glycine max/metabolismo , Análise EspectralRESUMO
Fungus Alternaria brassicae 93 isolated from crinoid (Comanthina schlegeli), which was collected from the South China Sea. Six compounds were isolated from A. brassicae 93, including one new compound (1), along with five known compounds, ochratoxin A methyl ester (2), cis-4-hydroxym-ellein (3), (R)-7-hydroxymellein (4), trans-2-anhydromevalonic (5) and protocatechuic acid (6). Their structures were determined by spectroscopic methods and comparison with reported data. Cytotoxicity against two human cancer cell lines and antibacterial activity against twelve aquatic bacteria of compound 1 were also tested.
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Alternaria/metabolismo , Antibacterianos/farmacologia , Metabolismo Secundário , Alternaria/química , Alternaria/isolamento & purificação , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Linhagem Celular Tumoral/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos/métodos , Humanos , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/metabolismo , Hidroxibenzoatos/farmacologia , Isocumarinas/isolamento & purificação , Isocumarinas/metabolismo , Espectroscopia de Ressonância Magnética , Ácido Mevalônico/análogos & derivados , Ácido Mevalônico/isolamento & purificação , Ácido Mevalônico/metabolismo , Estrutura Molecular , Oceanos e Mares , Ocratoxinas/isolamento & purificação , Ocratoxinas/metabolismo , Microbiologia da ÁguaRESUMO
OBJECTIVE: To understand the status of Oncomelania hupensis snail distribution and diffusion in main drainages of Hexi Reservoir and evaluate the snail control effect of the schistosomiasis control engineering of Hexi Reservoir. METHODS: The O. hupensis snails were investigated by using the straw curtain method and fishing net method in different areas of the main drainages of Hexi Reservoir, and the results were analyzed. RESULTS: A total of 1 800 straw curtains were used and 37 snails were found in Naxi stream. Totally 5 870 kg floats were salved and no snails were found. CONCLUSION: The schistosomiasis control engineering of Hexi Reservoir is effective in the prevention of the snail diffusion, but there are still snails in the upstream. rherefore, the snail surveillance and control need to be strengthened.
Assuntos
Água Doce/parasitologia , Caramujos/crescimento & desenvolvimento , Animais , China , Reservatórios de Doenças/parasitologia , Humanos , Dinâmica Populacional , Schistosoma/isolamento & purificação , Schistosoma/fisiologia , Esquistossomose/parasitologia , Esquistossomose/transmissão , Caramujos/parasitologiaRESUMO
OBJECTIVE: To evaluate the effect of schistosomiasis control projects in Hexi Reservoir on Oncomelania hupensis snail control. METHODS: The canal hardening + main water system widening + the overflow dam project, the concrete slope protection, the banking and reclamation + concrete slope protection project, the environment reform project, and the comprehensive treatment were implemented in the tail area, the hydro-fluctuation belt, the rainwater harvesting zoon of the upstream area, the dam area, and the downstream area of the reservoir, respectively. The changes of the snail situation were investigated before and after the construction of the reservoir, and the snail control effects of the schistosomiasis control projects in different parts of the reservoir were analyzed. RESULTS: There were no Oncomelania snails found 3 years in the bottom area, dam area, hydro-fluctuation belt, tail region and downstream of the dam after the construction and storage of the reservoir and the implementation of the schistosomiasis control projects. In the rainwater harvesting zoon of the upstream area, the density of living snails decreased from 0.620 4 snails/0.1 m2 in 2009 to 0.113 2 snails/0.1 m2 in 2013, but the snail area still remained. CONCLUSIONS: The schistosomiasis control projects in Hexi Reservoir have effectively prevented the diffusion of Oncomelania snails from the rainwater harvesting zone of the upstream area to the dam area, and they are effective in the snail control.