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Aim To study the transport mechanism of bergenin passing through blood-brain barrier ( BBB ) . Methods MTT assay was used to investigate the tox-icity of bergenin on MDCK-MDRl cells. Molecular docking was used to predict the binding mode and effect ability of bergenin with P-gp. In vitro MDCK-MDRl cell monolayer model was used to analyze trans¬port characteristics of bergenin and the effect of con¬centration, time and verapamil (a P-gp inhibitor) on the transport of bergenin. Results Bergenin was non-toxic to MDCK-MDRl cells within the concentration of 5 to 40 jjunol • L . There was hydrogen-bond and hy-drophobic interaction between P-gp and bergenin, and P-gp-bergenin was more stable than P-gp-verapamil. The P value of bergenin transported from AP to BL (PappAP
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OBJECTIVE:To study the compositi on of the volatile oil from Compound chaihu guizhi decoction ,and to evaluate its in vitro anti-proliferative activity on human lung adenocarcinoma A 549 cells. METHODS :The volatile oil from Chaihu guizhi decoction was extracted according to the steam distillation method of general rules 2004 in the 2015 edition of Chinese Pharmacopoeia(part Ⅳ). The volatile oil components were analyzed by GC-MS combined with Kováts index ,and the relative content of each component was calculated by peak area normalization method. Using different concentrations of cisplatin (4,8, 16,32,64 mg/L)as positive control ,MTT assay was used to detect the inhibitory effects of different concentrations of volatile oil from Chaihu guizhi decoction (25,50,100,200,400 mg/L)on in vitro proliferation of A 549 cell after 48 h of treatment. Negative control group (with cells but without drugs )was set up. RESULTS :A total of 71 chemical components were isolated from the volatile oil ,among which there were 59 compounds identified ,sum of peak areas accounting for 84.99% of the total peak area. The compounds with relatively high content included ar-curcumene (17.65%),β-bisabolene(9.57%),β-ocimene(7.05%), α-curcumene(5.35%),2,5-dimethylbenzaldehyde(4.24%),linalyl isobutyrate (2.70%),α-cedrene(2.48%),δ-cadinene (2.07%). Compared with negative control group ,the proliferation rate of cells were decreased significantly in 4-64 mg/L cisplatin groups and 25-400 mg/L volatile oil from Chaihu guizhi decoction groups (P<0.05). IC 50 of cisplatin and volatile oil from Chaihu guizhi decoction to in vitro proliferation of A 549 cells were 10.150 and 73.526 mg/L. CONCLUSIONS :The volatile oil from Chaihu guizhi decoction mainly includes ar-curcumene ,β-bisabolene,β-ocimene,α-curcumene,which shows certain inhibitory effect on in vitro proliferation of A 549 cells.
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OBJECTIVE:To establish a method for simultaneous determination of calycosin glucoside ,ononin,calycosin, formononetin,astragaloside Ⅳ,isoastragaloside Ⅱ,cycloastragenol and isoastragaloside Ⅰ in Astragalus membranaceus before and after bidirectional solid fermentation with Cordyceps kyushuensis ,and to investigate the effects of fermentation on the contents of above 8 components in A. membranaceus . METHODS :HPLC-DAD-ELSD was adopted. The determination was performed on Agilent 5 TC-C18 column with mobile phase consisted of 0.1% formic acid aqueous solution-acetonitrile (gradient elution )at the flow rate of 1 mL/min. The column temperature was set at 30 ℃. DAD detection wavelength was set at 260 nm,ELSD evaporation tube temperature was 100 ℃,atomizer temperature was 80 ℃,carrier gas flow rate was 1.6 L/min;injection volume was 15 μL. RESULTS:The eight components had a good linear relationship within their respective ranges of concentration (all R2>0.999 0); RSDs of precision ,stability and repeatability tests were all less than 3%(n=3 or n=6);the recoveries was 97.88%-101.32%, and RSDs were 1.22%-2.39%(n=6). Setting the content of components in unfermented A. membranaceus as 100%,after bidirectional solid fermentation with C. kyushuensis ,the change rates of 8 components were -98.51%,-96.41%,-94.74%, -96.40%,289.20%,20.25%,-75.05%,562.46%,respectively. CONCLUSIONS :After fermentation with C. kyushuensis ,the contents of active components as astragaloside Ⅳ,isoastragaloside Ⅰ and isoastragaloside Ⅱ can be increased significantly in A. membranaceus .
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Objective@#To analyze the relationship between sleep and poor vision of primary and middle school students aged 7-18 years, and to provide evidence for further student eye health promotion.@*Methods@#Data was collected from the Chinese National Survey on Students’ Constitution and Health in 2014. A total of 173 555 primary and middle school students were examined with the 5 m standard visual acuity chart. Sleep, homework time, milk consumption and exercise duration were collected by questionnaire survey.@*Results@#Only 5.60% of students aged 7-18 years had enough sleep, and the poor vision rate among students with insufficient sleep was higher than that of students with sufficient sleep(69.11% vs 67.76%), and the difference is statistically significant(χ2=7.87,P=0.01). After adjusted for other related factors, it showed that students’ sleep was closely related to poor vision(P<0.01), and adequate sleep was the protective factor of students’ poor vision (OR=0.92,95%CI=0.88-0.96).@*Conclusion@#Adequate sleep is conducive to preventing the occurrence of poor vision of primary and secondary school students in China. We should take measures to ensure that students get enough sleep.
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Objective@#To investigate indoor air quality monitoring and management in primary and secondary schools, so as to provide scientific basis for health protection of students and healthy school environment.@*Methods@#Stratified sampling method was adopted to select schools for investigation. Data of daily ventilation and ventilation was collected from relevant principals of schools through questionnaire survey. Chi-square test was used to analyze the difference of ventilation and ventilation among different types of schools.@*Results@#Daily indoor air quality testing indicators: 317 schools (13.2%) have tested the concentration of CO2 in the air environment. Daily detection of CO2 in urban schools was significantly better than that in township schools, and the difference is statistically significant(χ2=72.06, P<0.01); Non-boarding schools were superior than boarding schools(χ2=21.89, P<0.01). The proportion of schools that routinely tested for carbon monoxide, particulate matter and volatile pollutants was 6.5%, 7.5% and 9.3%, respectively. Of the schools that participated in the survey, 80.8% had a daily ventilation system. Among them, 925 schools (38.5%) had a cumulative daily ventilation time of more than 90 minutes in cold season, and 331 schools (13.8%) had a daily ventilation time of less than 30 minutes.@*Conclusion@#Regulations and standards for school air quality monitoring needs to be improved. The Center for Disease Control and Prevention or other qualified institutions are suggested to lead air quality monitoring in schools testing, creating a healthy learning and living environment for primary and secondary school students.
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OBJECTIVE:To optimize the extraction technology of total flavonoids for Bone healing formulation in order to use it for preparation research. METHODS:With the content of total flavonoids as the index,L9(34)orthogonal test was employed to investigate the effects of volume fraction of the solvent ethanol,the amount of solvent,extraction times and extraction time on the extraction of total flavonoids for Bone healing formulation to determine the optimal levels of the factors,and verification tests were conducted. RESULTS:The optimal extraction technology of total flavonoids was 1 h reflux extraction for 3 times,with 70% etha-nol 10 times as much as the amount of medicinal materials. Verification tests showed the average content of total flavonoids was 62.03 mg/ml(RSD=0.84%,n=3),that is to say,6.20 g total flavonoids might be extracted from 100 g medicinal materials for the formulation. CONCLUSIONS:The optimal technology is stable and feasible and can be used for the extraction of total flavo-noids for Bone healing formulation and provide a experimental basis for the preparation of Bone healing liniment.
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OBJECTIVE:To investigate transdermal behavior in vitro of total flavonoids and its monomer components in Guyu liniment. METHODS:Vertical Franz diffusion cell was adopted to perform a test on excised mouse skin as transdermal barrier. UV spectrophotometry was used to determine the content of total flavonoids,and HPLC to determine the content of monomer flavo-noid hydroxysafflor yellow A(HSYA)to observe transdermal absorption in vitro within 12 hours. RESULTS:The accumulative per-meation quantity Q of the total flavonoids and HSYA in Guyu liniment increased with time(t),demonstrating a significant correla-tion with t1/2,and transdermal absorption was in conformity with Higuchi equation (r=0.995 6,0.999 5);permeate flux of total flavonoids and HSYA were 126.24,47.516μg/(cm2·h). CONCLUSIONS:The transdermal behavior of total flavonoids in Guyu lin-iment is similar to that of HSYA. Both belong to matrix diffusion-type transdermal drug delivery system,with the characteristic of long-term sustained release.
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An HPLC method for the determination of geniposide concentration in mouse plasma was developed and the pharmacokinetics after intranasal administration of Xingnaojing microemulsion (XNJ-M) and mPEG2000-PLA modified Xingnaojing microemulsion (XNJ-MM) were investigated. Eighty mice were treated by XNJ-M and XNJ-MM nasally. The plasma samples were collected at different times and the drug in samples was detected by HPLC. The pharmacokinetic parameters were calculated by the software of Kinetica. The pharmacokinetic parameters of geniposide of XNJ-M were C(max) (4.36 +/- 2.69) mg x L(-1), t(max) 1 min, MRT (29.73 +/- 4.54) min, AUC (53.63 +/- 14.03) mg x L(-1) x min. The pharmacokinetic parameters of geniposide of XNJ-MM were C(max) (9.75 +/- 4.14) mg x L(-1), t(max) 1 min, MRT(22.34 +/- 2.90) min, AUC (131.87 +/- 40.13) mg x L(-1) x min. Geniposide can be absorbed into blood in a higher degree after intranasal administration with XNJ-MM compared to XNJ-M, which maybe caused by its less irritating and more absorption.
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Animales , Masculino , Ratones , Medicamentos Herbarios Chinos , Química , Emulsiones , Iridoides , Sangre , Farmacocinética , Ácido Láctico , Química , Poliésteres , Polietilenglicoles , Química , Polímeros , QuímicaRESUMEN
Current work aimed to develop and evaluate a transdermal delivery system of hydrogel patch for ferulic acid to treat skin damage induced by UV radiation. VISCOMATE[TM] NP700, dihydroxy aluminium aminoacetate, glycerine, tartaric acid were used in combination in different ratios to design the hydrogel patch. In vitro release rate was selected as an index to optimize the formulation. The formulated hydrogel patch was evaluated by several parameters like tacking strength, cohesive strength, peeling strength, residuals after peeling and drug content determination. The in vitro penetration was determined by Franz diffusion technology with hairless mouse skin as permeability media. Different kinetics models were employed to simulate the release and penetrate patterns of ferulic acid from patches in order to investigate the drug transport mechanism. The residual drugs in the patch and skin were determined after the penetration experiment. The optimized preparation was dihydroxy aluminium aminoacetate: NP700: glycerine: ferulic acid as a ratio of 0.02:0.4:1.5:1.25:0.25. The cumulative percentage of release was 60.4465 +/- 1.7679% for 24h, which results from a combination of diffusion effect and polymer erosion effect. For the barrier of stratum corneum, the cumulative penetrate rate was only 1.3156 +/- 0.3588% and the release mechanism turn out to be the effect of erosion of polymer surface. The residual drugs in the patch were 97.5949 +/- 1.4932%. The in vitro data revealed that it was easy for ferulic acid to release from the paste while difficult to permeate through the skin barrier, which resulted in most of drugs residued in the paste. Hence, further experiments will be necessary for finding the penetration enhancer in ferulic acid transdermal delivery
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Xingnaojing (XNJ) is an effective clinical drug used to treat acute stroke. Compared with injection administration, its nasal administration has better brain targeting. Therefore, through nasal administration, XNJ microemulsion could help solve the drug load of compound components of different polarities contained in large-dose and high-concentration traditional Chinese medicines, and reduce irritation to nasal mucosa In this study, the modified volume correction method and the improved rat in situ nasal perfusion model were adopted to compare the nasal absorption of geniposide contained in different XNJ preparations. The results showed that the constant absorption rate of geniposide (GE) in XNJ-D was (2.95 +/- 0.25) x 10(-3) min(-1), whereas the constant absorption rate of GE in XNJ-M was (2.16 +/- 0.21) x 10(-3) min(-1). This indicated that the rat nasal absorption of GE in different XNJ preparations complied with the first-order process and could be considered as passive absorption. GE in XNJ-D was absorbed faster than that in XNJ-M, which provided basis for the development of nasal preparations of XNJ.
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Animales , Masculino , Ratas , Absorción , Administración Intranasal , Medicamentos Herbarios Chinos , Farmacocinética , Emulsiones , Iridoides , Farmacocinética , Nariz , Metabolismo , Ratas Sprague-DawleyRESUMEN
Objective: To compare the absorption characteristics of Luodian Borneolum and muscone after nasal unidirectional perfusion with different Xingnaojing preparations in rats. Methods: The nasal unidirectional perfusion model was used, the contents of Luodian Borneolum and muscone were determined by GC method, and the absorption of Luodian Borneolum and muscone in Xingnaojing Nasal Drop (XN) and Xingnaojing Microemulsion (XM) were compared. Results: The absorption rate constants (Ka) of Luodian Borneolum in XN and XM were (1.00 ± 0.02)and (0.76 ± 0.03) min-1, respectively, and the Ka values of muscone in XN and XM were (0.76 ± 0.02) and (0.58 ± 0.10) min-1, respectively. Conclusion: The absorption of Luodian Borneolum and muscone in XN are both faster than that in XM.
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Objective: To develop an HPLC method for the determination of geniposide concentration in mouse brain and to investigate the pharmacokinetics after iv injection of Xingnaojing Injection. Methods: Forty mice were iv injected with Xingnaojing Injection 18 mg/kg (by geniposide), and the brain samples were collected at 1, 3, 5, 10, 30, 60, 90, 120 min after eyeball bleeding and 5 mice were sacrificed by cervical dislocation. The whole brain of mice was separated quickly to prepare brain homogenates, and the concentration of geniposide was detected by HPLC. The pharmacokinetic parameters were calculated by the software of Kinetica and the fitting method was noncompartmental. Results: The calibration curve was in good linear in the range of 54-1620 ng/g, r=0.9991. The extraction recoveries of geniposide brain drug concentration at 216, 864, and 1620 ng/g were (102.60 ± 4.28)%, (102.16 ± 4.48)%, and (97.66 ± 3.25)%, respectively. And the RSD values of inter-and intra-day were below 4.10%. The pharmacokinetic parameters were that the Cmax was (1 246.0 ± 520.7) ng/g, the tmax was 1 min, the MRT was (50.5 ± 1.9) min, and the AUC was (35780.3 ± 6148.0) ng/(g·min). Conclusion: The HPLC method for determining geniposide concentration in brain is simple, rapid, sensitive, and suitable for pharmacokinetic studies.
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<p><b>OBJECTIVE</b>Allgrove syndrome is a rare autosomal recessive disorder characterized by the triad of adrenal insufficiency, achalasia and alacrima and many cases have multi-systems disorder: endocrine, gastrointestinal tract, eyes and nervous system. This syndrome is also known as achalasia-addisonianism-alacrima syndrome or triple A syndrome. Allgrove syndrome is now known to be caused by mutations of AAAS gene encoding the aladin protein. In the present paper, we report a Chinese mainland girl with Allgrove syndrome with mutations in the AAAS gene.</p><p><b>METHOD</b>The patient was a 7-year-old girl complained of coma and dark skin; she was treated as Addison disease for 2 years and had vomiting for 9 months before the second admission. Gene analysis was performed after extracting genomic DNA by amplification and sequencing of the specific fragments of AAA gene.</p><p><b>RESULTS</b>The patient was confirmed to have adrenal insufficiency at the age of 5 years and 6 months. During the second hospitalization, she was found to have a remarkable brisk reflexion, bilateral optic nerve atrophy, alacrima and achalasia besides ACTH resistance. The girl was born to consanguineous parents. Based on these findings, she was diagnosed as having Allgrove syndrome. Mutation analysis revealed a novel homozygous deletion of a single G, c.771delG, in exon 8 of the AAAS gene. This frame shift mutation was predicted to create a premature stop codon at locus 290, p.R258GfsX33, leading to a truncated and non-functioning aladin protein. Both the parents were heterozygous for the mutation.</p><p><b>CONCLUSION</b>The clinical manifestations and AAAS gene mutations analysis confirmed the diagnosis of Allgrove syndrome. Gene analysis indicated that this syndrome is an autosomal recessive inherent disorder. ALADIN is significant for the normal cell function. When compared with reported cases, it seems that there are no remarkable relation between gene mutation loci and clinical manifestations in Allgrove syndrome.</p>