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Objective@#To explore prevalence and associated factors of nonalcoholic fatty liver disease (NAFLD) in overweight and obese children in Hohhot City, so as to provide the oretical basis for developing health education plans and implementing prevention and treatment of NAFLD in children.@*Methods@#A total of 156 overweight and obese children was enrolled from 4 primary schools in Hohhot City using cluster sampling method during 28th Aug. 2022 to 5th Mar. 2023. Height and weight were measured and body mass index was calculated, and fasting blood was taken in the early morning for fasting blood glucose, alanine aminotransferase, aspartate aminotransferase. Single factor analysis was conducted using ttest, χ2 test and Fishers exact probability method, while multivariate analysis was conducted using Logistic regression analysis and subject characteristic curves.@*Results@#The differences in age, waist circumference, hip circumference, fasting glucose, alanine aminotransferase, aspartate aminotransferase, gamma glutamyltransferase, uric acid, and triglyceride were statistically significant between the nonNAFLD and the NAFLD group (U/t=1 070.0-2 164.0, P<0.05). Significant differences were observed in aspartate aminotransferase (AST) and uric acid levels (AST OR=1.16, 95%CI=1.04-1.28; uric OR=1.01, 95%CI=1.00-1.01, P<0.05). The area under a receiver operating characteristic were 0.737 for aspartate aminotransferase and 0.665 for uric acid, respectively.@*Conclusions@#The prevalence of NAFLD is high in overweight/obese children in Hohhot, and both elevated aspartate aminotransferase and hyperuricemia could increase the risk of NAFLD in overweight/obese children. Special attention should be paid to the NAFLD in overweight and obese children. It is recommended to reduce both BMI and uric level in the prevention and treatment of NAFLD to achieve better treatment outcomes.
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@#Abstract: Objective To observe the curative effect of thread-hanging combined with cotton plug on stage Ⅲ paronychia. Methods Sixty-one patients with stage Ⅲ paronychia were selected and randomly divided into a treatment group and a control group. The treatment group (n=31) was treated with thread-hanging and tampon under local infiltration anesthesia, and changed dressing and tampon every day after operation. After the wound healed, the patient soaked his feet in warm water every day and changed the tampon himself until the symptoms subsided, and the knot did not receive special treatment, and the nail plate would naturally shed as it outgrew the paronychia. The control group (n=30) was treated with thread-hanging and nail groove reconstruction under nerve block anesthesia, and the dressing was changed every day after operation. After thread removal, the patients soaked their feet in warm water every day until the symptoms subsided, and the knot was not specially treated, and it naturally fell off with the growth of the deck beyond the nail groove. The postoperative Visual Analog Scale (VAS) pain score, pain duration, wound healing time, cure rate, effective rate and recurrence rate of paronychia, and patients' satisfaction with the operation were compared between the two groups. Results Compared with the control group, the treatment group had lower VAS pain scores on the first and third postoperative days (2.1±0.3) and (0.2±0.1) vs. (6.3±0.1) and (3.2±0.2), respectively, shorter duration of pain and wound healing time (3.3±0.3) days and (10.1±0.5) days vs. (5.2±0.3) days and (15.2±0.3) days, respectively, higher cure rate (87.1% vs. 66.7%), lower failure rate (12.9% vs. 33.3%), lower recurrence rate (7.4% vs. 20.0%), and higher patient satisfaction (97.0% vs.75.3%). The treatment group showed significant superiority over the control group in all outcomes. Conclusion For patients with stage Ⅲ paronychia, thread-hanging combined with cotton tampon without nail groove reconstruction is advantageous as it avoids additional skin trauma, and does not affect the nail appearance and normal periungual barrier after healing, , reduces patient discomfort, and shortens the time off work, resulting in a higher cure rate. This treatment approach is therefore worth promoting in clinical practice.
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Objective@#To investigate the association of the risk of overweight/obesity in children and adolescents with their early life factors and parental weight.@*Methods@#From June 1 to June 30 of 2022, the stratified randomized cluster sampling method was used to collect information using questionnaires from 5 370 primary and secondary school students in Hohhot City, Inner Mongolia Autonomous Region, and multivariate analysis were performed using multiple Logistic regression model estimation in a generalized linear model for parental BMI and early life factors in children and adolescents.@*Results@#The prevalence of overweight/obesity was 32.2% , and the prevalence of overweight/obesity among male students was 37.8%, which was higher than that of female students 26.1% χ 2= 84.59 , P <0.01). The results of the multirariate Logistic regression anaysis showed that the prevalence of overweight/obesity was higher in only paternal overweight ( OR=1.52, 95%CI =1.30-1.77), only maternal overweight ( OR=1.61, 95%CI = 1.31 -1.97), and parentl overweight ( OR=2.42, 95%CI =2.03-2.87)( P <0.05). The risk of overweight/obesity was higher in children with high birth weight ( OR=1.29, 95%CI =1.08- 1.55 ), children born by caesarean section ( OR=1.32, 95%CI =1.17- 1.48 ), and children whose mothers gained excessive weight during pregnancy ( OR=1.24, 95%CI =1.06-1.46), and the results were statistically significant ( P <0.05).@*Conclusions@#Overweight parents, excessive maternal weight gain during pregnancy, cesarean delivery, and high birth weight are associated with increased risk of overweight/obesity in children and adolescents. Attention should be paid to these aspects in obesity prevention and control.
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Abstract Background The impact of a literature report on a particular subject can be measured by its number of citations. Objective The purpose of this study was to evaluate the characteristics of the literature reports in the field of endovascular treatment of intracranial aneurysms (IAs) by analyzing the top 100 most cited articles. It should be noted that the focus of this study is to describe the bibliometric characteristics. Methods This bibliometric analysis dedicated only to endovascular treatment of IAs in our study. We searched the top 100 most cited articles in the field of endovascular treatment of IAs using the search tool of the Web of Science (WOS). We evaluated the characteristics of these high-impact publications, including publication year, category, journal, author's country, etc. Results The top 100 most cited articles were cited 281.3 times, on average. The United States has published the most articles every year compared with other countries. These highly cited articles are mostly published in the Journal of Neurosurgery. Eighty-six of the top 100 most cited articles were clinical studies. Conclusion The bibliometric analysis provides insight over the development and the growing trend in endovascular treatment of IAs. This study can help researchers better understand the global overview of this field, and it also provides leads about promising areas of future research and potential collaborations.
Resumo Antecedentes O impacto de um relato de literatura sobre um determinado assunto pode ser medido pelo seu número de citações. Objetivo O objetivo deste estudo foi avaliar as características dos relatos da literatura na área de tratamento endovascular de aneurismas intracranianos (AIs), analisando os 100 artigos mais citados. Ressalta-se que o foco deste estudo é descrever as características bibliométricas. Métodos Esta análise bibliométrica foi dedicada apenas ao tratamento endovascular dos AIs em nosso estudo. Pesquisamos os 100 artigos mais citados na área de tratamento endovascular de AIs usando a ferramenta de busca daWeb of Science (WOS). Avaliamos as características dessas publicações de alto impacto, incluindo ano de publicação, categoria, periódico, país do autor etc. Resultados Os 100 artigos mais citados foram citados 281,3 vezes, em média. Os Estados Unidos publicaram o maior número de artigos todos os anos em comparação com outros países. Esses artigos altamente citados são publicados principalmente noJournal of Neurosurgery. Oitenta e seis dos 100 artigos mais citados eram estudos clínicos. Conclusão A análise bibliométrica fornece informações sobre o desenvolvimento e a tendência crescente no tratamento endovascular das AI. Este estudo pode ajudar os pesquisadores a entender melhor a visão global desse campo e também fornece pistas sobre áreas promissoras de pesquisas futuras e potenciais colaborações.
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Objective To observe the effect of postconditioning (PostC) on the expression of platelet-leukocyte aggregation (PLA) during the process of myocardial ischemia and reperfusion in rats, and to explore the mechanisms of ischemic postconditioning (PostC) alleviating myocardial ischemia-reperfusion injury (MIRI). Methods Sixty rats were randomly divided into six groups:sham,reperfusion injury(I/R),postconditioning(PostC),SP600125(inhibition of c-Jun N-terminal kinase,I-JNK),anisomycin and postconditioning(Ani+PostC)and anisomycin(Ani)groups.After constructing the model of myocardial ischemia reperfusion in rats,the levels of myocardial injury markers were detected by using the CK-MB kits and TnI kits. The levels of PLA at different time points were detected by using flow cytometry.The myocardial infarction area were measured by using 2.3.5-Triphenyte-trazoliumchloride(TTC)staining,and the level of phosphorylation of JNK(P-JNK) was determined by using Western blot method. Results (1) The levels of CK-MB, TnI and the infarct size were significantly higher in the I/R group than those in the Sham group(P<0.05).The levels of CK-MB,TnI and the infarct size were significantly lower in the PostC group and I-JNK group than those in the I/R group(P<0.05).Compared with the PostC group,the levels of CK-MB,TnI and the infarct size were significantly higher in the Ani+PostC group and Ani group(P<0.05).(2)Compared with the Sham group,the expression levels of PLA significantly increased in the I/R group at different time points after ischemia (P<0.05). At different time points of MIRI, the expressions of PLA increased gradually in I/R group, Ani+PostC group and Ani group (P<0.05). At the time point of reperfusion for 60 minutes and reperfusion for 3 hours,the expressions of PLA were significantly lower in the PostC group and I-JNK group compared with those of I/R group (P<0.05).Compared with the PostC group,the expressions of PLA were significantly higher in the Ani+PostC group and Ani group (P<0.05). (3) Compared with the Sham group, the expression levels of P-JNK were significantly higher in the I/R group(P<0.05).PostC and I-JNK inhibited the production of P-JNK(P<0.05),while Ani promoted the increase of P-JNK (P<0.05).Compared with the PostC group,the expression levels of P-JNK were significantly higher in the Ani+PostC group and Ani group (P<0.05). Conclusion PostC can reduce the expression of PLA during reperfusion by inhibiting the phosphorylation of JNK,thereby reducing myocardial ischemia-reperfusion injury.
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Objectives:To explore the possible mechanisms of ischemic postconditioning on alleviating myocardial ischemia-reperfusion injury, focusing on the inflammatory-thrombus related mechanisms. Methods:Rats were randomly divided into six groups (n=10 each):sham group, ischemia-reperfusion injury group, postconditioning group, SB203580 group, anisomycin+postconditioning (Ani+postconditioning) group and anisomycin (Ani) group. After establising the model of myocardial ischemia reperfusion in rats, the levels of myocardial injury markers troponin I (TnI) and creatine kinase isoenzyme (CK-MB), level of leukocyte-platelet aggregation (PLA) were detected by flow cytometry at different time points, myocardial infarction area was measured by using TTC staining and the level of phosphorylation of p38 MAPK (P-p38 MAPK) was determined by Western blot. Results:Compared with the I/R group, the levels of CK-MB, TnI, the infarct size and the expression of PLA at 60 min and 3 h reperfusion were significantly reduced in the postconditioning group and SB203580 group (P＜0.05). Compared with the postconditioning group, the levels of above parameters were significantly higher in the SB203580 group, Ani+postconditioning group and Ani group (P＜0.05). Compared with the I/R group, the expression of P-p38 MAPK in the postconditioning group, SB203580 group, Ani+postconditioning group was significantly reduced (P＜0.05), while it was significantly upregulated in the Ani group (P＜0.05). Furthermore, compared with the postconditioning group, the expression of P-p38 MAPK in the Ani+postconditioning group and Ani group was significantly upregulated (P＜0.05). SB203580 group presented the similar protection effect as the postconditioning group. Cardioprotective effects of postconditioning was partially reduced in the Ani+postconditioning group. Conclusions:Ischemia postconditioning can reduce the expression of PLA during reperfusion by inhibiting the phosphorylation of p38MAPK, thereby attenuating myocardial ischemia-reperfusion injury.
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To investigate the effects of Gegen Qinlian decoction on the expression of P-glycoprotein (P-gp) and multi-drug resistance protein (MRP) in epithelial cells of human colon adenocarcinoma Caco-2 cells．The effects of different concentrations of Gegen Qinlian decoction on the expression levels of p-gp and MRP1-6 mRNA in Caco-2 cells were detected by real time quantitative reverse transcriptase PCR (qRT-PCR).12 h after drug treatment (5.00 g·L⁻¹), the expression levels of MDR1 and MRP1-6 were significantly down-regulated at concentration of 5.00 g·L⁻¹; the mRNA expression levels of MDR1，MRP1，MRP2，MRP4，MRP5 and MRP6 were significantly down-regulated at concentration of 2.50 g·L⁻¹; only the expression levels of MRP2 and MRP5 were significantly affected at concentration of 1.00 g·L⁻¹. The results showed that the expression levels of MDR1 and MRP1-6 mRNA in Caco-2 cells could be down-regulated in a dose-dependent manner. Gegen Qinlian decoction may reduce drug efflux by down-regulating the mRNA expression of cell transporters in Caco-2 cell, and increase the time of drug action, thereby enhancing the bioavailability of chemotherapeutic drugs.
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AIM To study the chemical constituents from the twigs and leaves of Cryptomeria fortunei Hooibrenk ex Otto et Dietr.METHODS The ethyl acetate fraction of 95％ ethanol extract from C.fortunei was isolated and purified by silica,MCI,and Sephadex LH-20 column,then the structures of obtained compounds were identified by physicochemical properties and spectral data.RESULTS Eleven compounds were isolated and identified as isopimaric acid (1),sandaracopimaric acid (2),acetylisocupressic acid (3),imbricataloic acid (4),isocupressic acid (5),pinifolic acid (6),13-epicupressic acid (7),19-acetylagathadiol (8),agatadiol (9),phytol (10),elemol (11).CONCLUSION Compounds 1-10 are identified as diterpenoids and compound 11 is identified as sesquiterpenoid;Compounds 2,3,6-11 are obtained from this plant for the first time.
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This study investigated the relationship among the severity of hearing impairment,vestibular function and balance function in patients with idiopathic sudden sensorineural hearing loss (ISSNHL).A total of 35 ISSNHL patients (including 21 patients with vertigo) were enrolled.All of the patients underwent audiometry,sensory organization test (SOT),caloric test,cervical vestibular-evoked myogenic potential (cVEMP) test and ocular vestibular-evoked myogenic potential (oVEMP) test.Significant relationship was found between vertigo and hearing loss grade (P=0.009),and between SOT VEST grade and hearing loss grade (P=0.001).The abnormal rate of oVEMP test was the highest,followed by the abnormal rates of caloric and cVEMP tests,not only in patients with vertigo but also in those without vertigo.The vestibular end organs were more susceptible to damage in patients with vertigo (compared with patients without vertigo).Significant relationship was found between presence of vertigo and SOT VEST grade (P=0.010).We demonstrated that vestibular end organs may be impaired not only in patients with vertigo but also in patients without vertigo.The cochlear and vestibular impairment could be more serious in patients with vertigo than in those without vertigo.Vertigo does not necessarily bear a causal relationship with the impairment of the vestibular end organs.SOT VEST grade could be used to reflect the presence of vertigo state in the ISSNHL patients.Apart from audiometry,the function of peripheral vestibular end organs and balance function should be evaluated to comprehensively understand ISSNHL.Better assessment of the condition will help us in clinical diagnosis,treatment and prognosis evaluation of ISSNHL.
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Objective@#To simulate the hypoxic environment of cells in vivo more approximately, a hypoxia control device which can control oxygen concentration automatically for cell culture in vitro was developed. @* Methods@#In vitro cell cultur e hypoxia control device consisted of hardware and software which were controlled by computer. The hardware was composed of oxygen detection and control system, nitrogen gas pipeline, cell culture and anti-jamming device, and the software was based on Clanguage. When oxygen controlle rreads the oxygen concent ration more than the set value, the nitrogen gas pipeline opens and nitrogen enter into the incubator; when reaching the set value, the nitrogen gas pipeline closes and nitrogen is not allowed to pass through. Circularly, a constant oxygen concentration was reached and maintained. This device was further verified by comparing the set value of the equipment with figures of the oxygen meter and by monitoring fluctuation condition after the oxygen concentration reaching the set value. @* Results @# There was no significant difference between the oxygen concentration set in the in vitro cell culture hypoxia control device and the actual oxygen concentration in the measured box (P > 0.05), and the accuracy of the device to set the value of the simulation up to ± 0.5% of the requirements to meet the system accuracy requirements, and can remain stable for a long time. @*Conclusion @#The device can effectively control the oxygen concentration to the required requirements, to meet the conditions in the hypoxic conditions for in vitro cell culture.
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Objective: To investigate the characteristics of intestinal absorption of glycyrrhetinic acid in rats in the multicomponent environment. Methods: The effect of multicomponent environment on intestinal absorption of glycyrrhetinic acid was investigated in rat model of in situ single-pass intestinal perfusion, HPLC was used to determine the concentration of glycyrrhetinic acid in intestinal perfusion fluid samples, the effective permeability coefficient (Peff), absorption rate constant (Ka), and absorption fraction (Fa) of glycyrrhetinic acid in rats ileum were calculated, the effects of glycyrrhetinic acid with different mass concentration and P-glycoprotein (P-gp) inhibitor verapamil, as well as the compatibility of different components on intestinal absorption of glycyrrhetinic acid were examined,. Results: The Peff, Ka, and Fa values of glycyrrhetinic acid perfusion liquid (10 and 20 µg/mL) in the ileum segment had no significant difference. Added with 100 µmol/L verapamil, Peff, and Fa values of 10 µg/mL glycyrrhetinic acid increased, which illustrated that the glycyrrhetinic acid might be the substrate of P-gp; In two components compatibility, the effect of baicalin on absorption of glycyrrhetinic acid was the most obvious, Peff value of glycyrrhetinic acid was from (4.05 ± 0.78) × 10-5 cm/s to (2.18 ± 0.63) × 10-5 cm/s, and the penetration of glycyrrhetinic acid was reduced. The puerarin consociation baicalin and berberine had no obvious effect on permeability of glycyrrhetinic acid. In the three components compatibility condition, the experimental results showed that after glycyrrhetinic acid combined with puerarin and berberine, the permeability coefficient did not change, while the permeability coefficient changed, but not obviously, glycyrrhetinic acid combined with baicalin and berberine had lower permeability, Peff values were from (4.05 ± 0.78) × 10-5 cm/s down to (1.35 ± 0.69) × 10-5 cm/s, and the effects of baicalin on glycyrrhetinic acid was evident. Conclusion: Glycyrrhetinic acid can be absorbed in the ileum of rats, and has no obvious influence on Peff and Ka values within a certain range of quality concentration. The absorption mechanism is determined to be passive diffusion, glycyrrhetinic acid is substrate of P-gp, and saturation phenomenon exists transporters; Baicalin has significant effects on glycyrrhetinic acid absorption, which may be related to the induction by P-pg expression, increasing the glycyrrhetinic acid from cell to the extracellular discharge, reducing the penetration of glycyrrhetinic acid, and influencing the absorption.
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One of the top-level researches of biopharmaceutics classification system of Chinese materia medica (CMMBCS) is the study on single component in compound Chinese medicine. The medicines shall be classified according to its solubility and intestinal permeability, as well as the ascending degree in multicomponent environment. Based on above, we chose berberine as the main object to explore the change rules of its solubility and intestinal permeability in Gegen Qinlian decoction. Shaking flask-HPLC was used to detect the solubility changes of berberine in compounds. The qualitative investigation of berberine in intestinal absorption was measured by everted gut sac, and the quantitative research of berberine in intestinal absorption was measured by single-pass intestinal perfusion experiment, while the qualitative and quantitative research of berberine absorption into blood was measured by in intestinal perfusion with venous sampling experiment.
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To validate in situ rats intestinal single pass perfusion model based on P-glycoprotein (P-gp). Firstly, phenol red perfusion was carried out to verify the close connection structure of intestinal epithelial cells, and the integrity of the intestinal epithelium, with a gravimetric method for correcting water flux. The level of phenol red was determined by high performance liquid chromatography (HPLC) both before and after perfusion. Secondly, the positive drug digoxin specified by FDA was used to validate the model. After different mass concentrations of verapamil were given in the rats, the absorption parameters of digoxin in ileum of rats were observed and compared. The results showed that the phenol red was absorbed in rats ileum segment, with an effective permeability coefficient of (1.09±0.62)×10 ⁻⁶ cm•s ⁻¹. The experiment results indicated that the close connection structure of intestinal epithelial cells was normal, and the integrity of the intestinal epithelium was maintained well. In digoxin perfusion experiment, in case no verapamil was given, digoxin showed certain degree of absorption in rat ileum, with an effective permeability coefficient (Peff) of (1.07±0.59)×10 ⁻⁵ cm•s ⁻¹; after mass concentrations of 0.01,0.1 mmol•L ⁻¹ verapamil were given, the absorption of digoxin was on the rise in rat ileum, with an effective permeability coefficient Peff of (1.58±0.69)×10 ⁻⁵, (3.28±0.95)×10 ⁻⁵ cm•s ⁻¹ respectively (P<0.05). Digoxin perfusion experiment verified that P-gp expression in small intestine epithelium was intact and can be used in the research of P-gp efflux transporter.
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Five cassane diterpenes were isolated from the 95% ethanol extract of the seeds of Caesalpinia bonduc (Leguminosea) by a combination of various chromatographic methods, including silica gel, Sephadex LH-20, and semi-preparative HPLC. On the basis of spectroscopic techniques, their structures were identified as 3β-acetoxy-cassa-12,14(17),15-trien-7β-ol (1), caesalmin C (2), caesall E (3), caesalpinin MJ (4), and 1-deacetylcaesalmin C (5). Among them, compound 1 is a new compound and 2, 4, 5 were isolated from the plant for the first time.
الملخص
The study of single component in the multicomponent environment is one of the basic researches for biopharmaceutics classification system of Chinese materia medica (CMMBCS). That is to say, the classification research shall be based on the respective lift of solubility and permeability in the multicomponent environment, besides solubility and intestinal permeability of the single component. We chose berberine as the main research object to investigate the changes of its solubility and intestinal permeability in Huanglian decoction. Shake-flask and HPLC were used to detect the solubility of berberine in different pH buffer solutions and different concentrations of Huanglian decoction. In situ single-pass intestinal perfusion (SPIP) and intestinal perfusion with venous sampling (IPVS) were carried out to study berberine's intestinal absorption and absorption into blood, respectively.
الملخص
In the study of biopharmaceutics classification system of Chinese materia medica (CMMBCS), the interactions of multiple components in the absorption should be taken into consideration in simultaneous multi-component determination. To investigate the absorption of multiple components, the in vitro everted gut sac model was used in this study, wtih lotus leaves as the research object. Aquantitative analysis was also carried out for the known components in this study. Totally 19 components in lotus extracts were absorbed by the intestinal tract, the Papp levels of the known components were nuciferine (1×10⁻⁵-1×10⁻⁶ cm•s⁻¹), rutin (1×10⁻⁶-1×10⁻⁷ cm•s⁻¹), hyperoside (1×10⁻⁶ cm•s⁻¹), isoquercitrin (1×10⁻⁶-1×10⁻⁷ cm•s⁻¹) and astragalin (1×10⁻⁶-1×10⁻⁷ cm•s⁻¹), respectively. These components showed a low permeability under a multi-component environment. This study was carried out to lay a foundation for further relevant target studies for different categories of components.
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abstract The aim of this study was to evaluate the effects of caffeine, tea polyphenol and daidzein on the pharmacokinetics of lansoprazole and its metabolites. Rats were intragastrically administered caffeine (30 mg·kg-1, once per day), tea polyphenol (400 mg·kg-1, once per day) or daidzein (13.5 mg·kg-1, once per day) for 14 days, followed by an intragastric administration of lansoprazole (8 mg·kg-1) on the 15th day. The plasma concentrations of lansoprazole and its two primary metabolites, 5-hydroxylansoprazole and lansoprazole sulfone, were determined by high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS). Tea polyphenol significantly elevated the Area Under the Curve (AUC) of lansoprazole from 680.29 ± 285.99 to 949.76 ± 155.18 μg/L.h and reduced that of lansoprazole sulfone from 268.82 ± 82.37 to 177.72 ± 29.73 μg/L.h. Daidzein increased the AUC of lansoprazole from 680.29 ± 285.99 to 1130.44 ± 97.6 μg/L.h and decreased that of lansoprazole sulfone from 268.82 ± 82.37 to 116.23 ± 40.14 μg/L.h. The pharmacokinetics of 5-hydroxylansoprazole remained intact in the presence of tea polyphenol or daidzein. Caffeine did not affect the pharmacokinetics of lansoprazole and its metabolites. The results imply that tea polyphenol and daidzein may inhibit the in vivo metabolism of lansoprazole by suppressing CYP3A.
resumo O objetivo deste estudo foi avaliar os efeitos da cafeína, do polifenol do chá e da daidzeína na farmacocinética do lansoprazol e de seus metabólitos. Administraram-se, intragastricamente, aos ratos cafeína (30 mg·kg-1, uma vez ao dia), polifenol do chá(400 mg·kg-1, uma vez ao dia) ou daidzeína (13,5 mg·kg-1, uma vez ao dia), por 14 dias, seguindo-se a administração de lansoprazol (8 mg·kg-1) no 15º. dia. As concentrações plasmáticas do lansoprazol e de seus dois metabólitos primários, 5-hidroxilansoprazol e sulfona de lansoprazol, foram determinadas por cromatografia líquida de alta eficiência acoplada com espectrometria de massas (CLAE-EM/EM). O polifenol do chá elevou, significativamente, a Área Sob a Curva (ASC) do lansoprazol de 680,29 ± 285,99 para 949,76 ± 155,18 μg/L.h e reduziu a da sulfona de lansoprazol de 268,82 ± 82,37 para 177,72 ± 29,73 μg/L.h. A daidzeína aumentou a ASC do lansoprazol de 680,29 ± 285,99 para 1130,44 ± 97,6 μg/L.h e reduziu a da sulfona de lansoprazol de 268,82 ± 82,37 para 177,72 ± 29,73 μg/L.h. A farmacocinética do 5-hidroxilansoprazol permaneceu intacta na presença de polifenol do chá ou daidzeína. A cafeína não afetou a farmacocinética do lansoprazol e de seus metabólitos. Os resultados sugerem que o polifenol do chá e a daidzeína podem inibir o metabolismo in vivo do lansoprazol por supressão da CYP3A.
الموضوعات
Rats , Caffeine/pharmacokinetics , Polyphenols/pharmacokinetics , Lansoprazole/pharmacokinetics , Rats , Pharmacokineticsالملخص
Background & objectives: angiotensin II receptor type 1 (AaT1) is known to be involved in the pathogenesis of hypertension. tThis study was undertaken to explore the effect of active immunization against AaT1 receptor on blood pressure and small artery remodelling in spontaneously hypertensive rat (SHR). Methods: Male SHR and Wistar rats aged two months were actively immunized with different peptides (AaTR12185、AaTR10014 and AaTR12181) corresponding to particular sequences of rat receptor, while another SHR group was given losartan (10 mg/kg/day) orally once a day. Aanti-AaT1 receptor antibodies were detected by ELISAa and blood pressure was measured. The effect of the antibodies on the artery and vascular smooth muscle cells (VSMCs) proliferation was studied. Results: all immunized animals produced antibodies against the particular peptides. The systolic blood pressure was decreased in the SHR immunized with peptide-AaTR12181 compared with the control. However, no changes were observed in the SHR immunized with other two peptides. The Wistar rats immunized with the three peptides did not show any changes in blood pressure. The media/lumen area ratio of the mesenteric artery was reduced in SHR immunized with and similar to that of the SHR treated with losartan. The antibody from SHR immunized with AaTR12181 had no effect on the proliferation of VSMC. But it could inhibit the proliferation caused by angiotensin II and its effect at the titre of 1:40 was similar to that of 1μmol/l losartan. Interpretation & conclusions: Our findings demonstrated that the antibody from SHR immunized with AaTR12181 had the effect of reducing blood pressure and target organ protection similar to losartan. Aactive immunization against AaT1 receptor may be a promising strategy in future for the treatment of hypertension.
الملخص
Mung bean seed coat (MBSC) is a healthcare product in Asian countries. The aim of this study was to investigate the effect of an MBSC ethanol extract on the bioavailability of cyclosporine A (CsA) in rats. Rats were orally dosed with CsA alone or in combination with MBSC ethanol extracts (500 mg/kg, p.o.). The blood levels of CsA were assayed by liquid chromatography with an electrospray ionization source and tandem mass spectrometry (LC-MS/MS). The everted rat intestinal sac technique was used to determine the influence of MBSC on the absorption of CsA. The results reveal that combined CsA intake with MBSC decreased the Cmax, AUC0-t, t1/2z and MRT0-t values of CsA by 24.96%, 47.28%, 34.73% and 23.58%, respectively (P<0.05), and significantly raised the CL/F by 51.97% (P<0.01). The in vitro results demonstrated that significantly less CsA was absorbed (P<0.05). The overall results indicate that after being concomitantly ingested, MBSC reduced the bioavailability of CsA, at least partially, in the absorption phase.
O tegumento da semente de feijão-mungo (MBSC) é um produto para tratamento de saúde em países asiáticos. O objetivo deste estudo foi investigar o efeito de extrato etanólico de MBSC na biodisponibilidade da ciclosporina A (CVsA) em ratos. Administrou-se aos ratos CsA sozinha ou em associação com extrato etanólico de MBSC (500 mg/kg, p.o.), por via oral. Os níveis sanguíneos de CSA foram determinados por cromatografia a líquido com ionização por electrospray, associada à espectrometria de massas (LC-MS/MS). Utilizou-se a técnica de inversão do saco intestinal de rato para determinar a influência do MBSC na absorção de CsA. Os resultados revelaram que a ingestão combinada de CsA e MBSC diminuiu os valores de Cmax, AUC0-t, t1/2z e MRT0-t de CsA em 24%, 47,28%, 34,73% e 23,58%, respectivamente (P<0.05), e aumentou, significativamente, CL/F em 51,79% (P<0.05). Os resultados in vitro demostraram que, significativamente, menos CsA foi absorvida (P<0.05). Os resultados totais indicaram que após ser concomitantemente ingerida, a MBSC reduziu, ao menos parcialmente, a biodisponibilidade de CsA, na fase de absorção.
الموضوعات
Rats , Rats/classification , Biological Availability , Cyclosporine , Fabaceae/classification , Seeds/classification , Biological Availabilityالملخص
Anti-HER2 monoclonal antibody (Sc7301)-paclitaxel (TAX) immunoconjugate was prepared and its specific binding to tumor cells was investigated in this study.Sc7301 was conjugated to TAX by the active ester method and then the TAX-Sc7301 immunoconjugate was obtained.After purification and labeling by Cyano-fluorescein isothiocyanate (FITC),the specific binding of TAX-Sc7301to HER2-positive tumor cells (SKOV3) and HER2-negative tumor cells (HepG2) was evaluated respectively.TAX-Sc7301 (20 nmol/L) showed distinct specific binding to SKOV3 cells rather than HepG2cells.And the uptake of the immunoconjugate by SKOV3 cells was increased with the TAX-Sc7301concentration (3-48 nmol/L) and the incubation time (P＜0.05).It was concluded that the TAX-Sc7301immunoconjugate is potentially applicable as a targeted agent against HER2-positive tumor cells.