1.Synthesis and biological activity evaluation of phthalimide-donepezil hybrids
Jun-jie WANG ; Ye-shu MU ; Chen HONG ; Wen LUO
Acta Pharmaceutica Sinica 2024;59(3):651-660
A series of phthalimide-donepezil (PTA-DPZ) hybrids (
2.Effect of interaction between ADIPOQ gene 11377C/G polymorphism and physical activity on metabolic syndrome in children
Kaifeng WANG ; Ping YE ; Dan WANG ; Liufeng WU ; Weijia LIU ; Qing CHEN ; Jiandong LI
The Journal of Practical Medicine 2015;31(23):3853-3856
Objectve To study the effect of interaction between ADIPOQ 11377C/G (rs266729) gene polymorphism and physical activity in metabolic syndrome in children. Methods We conducted a case-control study in 114 cases and 114 controls. The genotype of ADIPOQ 11377C/G had been detected in direct sequenc-ing. The effect of interaction between gene polymorphism and physical activity was evaluated by a crossover analysis. Results Efficient physical activity was a protective factor (OR = 0.14); there was interaction between inefficient physical activity and CC genotype of 11377C/G which was a risk factor for metabolic syndrome in children. Conclusion Efficient physical activity can reduce the risk of metabolic syndrome in children. There was interaction between 11377C/G (rs266729) polymorphism and physical activity.
3.7-hydroxy sulfonation of liquiritigenin by recombinant SULT1A3 enzyme and HEK-SULT1A3 cells.
Yi-Dan ZHANG ; Hai-Ying LI ; Fan-Ye LIU ; Jie NIU ; Xiao WANG ; Chao LIANG ; Hua SUN
China Journal of Chinese Materia Medica 2019;44(19):4249-4256
In this study,liquiritigenin sulfonation was characterized using recombinant human sulfotransferases( SULTs). The chemical structure of liquiritigenin sulfate was determined by ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry( UPLC-Q-TOF-MS/MS). Then model fitting and parameter estimation were performed using the Graphpad Prism V5 software. Various SULT enzymes( SULT1 A1,1 A2,1 A3,1 B1,1 C2,1 C4,1 E1 and 2 A1) were able to catalyze the formation of liquiritigenin-7-O-sulfate. Sulfonation of liquiritigenin-7-hydroxy( 7-OH) by these eight SULT enzymes consistently displayed the classical Michaelis-Menten profile. According to the intrinsic clearance( CLint) value,the sulfonation rates of liquiritigenin-7-OH by expressed SULT enzymes followed the following rank order: SULT1 C4 > SULT1 A3 > SULT1 E1 > SULT1 A1 > SULT1 A2 > SULT1 B1 >SULT1 C2>SULT2 A1. Further,liquiritigenin-7-O-sulfonation was significantly correlated with the SULT1 A3 protein levels( P<0. 05).Then,human embryonic kidney( HEK) 293 cells over expressing SULT1 A3( named as HEK-SULT1 A3 cells) were conducted. As a result,liquiritigenin-7-O-sulfate( L-7-S) was rapidly generated upon incubation of the cells with liquiritigenin. Consistent with SULT1 A3,sulfonation of liquiritigenin-7-OH in HEK-SULT1 A3 cells also followed the Michaelis-Menten kinetics. The derived Vmaxvalues was( 0. 315±0. 009) μmol·min-1·g-1,Kmwas( 7. 04±0. 680) μmol·L-1,and CLintwas( 0. 045±0. 005) L·min-1·g-1. Moreover,the sulfonation characters of liquiritigenin( 7-OH) in SULT1 A3 were strongly correlated with that in HEK-SULT1 A3 cells( P<0. 001).The results indicated that HEK-SULT1 A3 cells have shown the catalytic function of SULT1 A3 enzymes. In conclusion,liquiritigenin was subjected to efficient sulfonation,and SULT1 A3 enzyme plays an important role in the sulfonation of liquiritigenin-7-OH. Significant sulfonation should be the main reason for the low bioavailability of liquiritigenin. In addition,HEK-SULT1 A3 cells were conducted and successfully used to evaluate liquiritigenin sulfonation,which will provide an appropriate tool to accurately depict the sulfonation disposition of liquiritigenin in vivo.
Arylsulfotransferase
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Flavanones/metabolism*
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Humans
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Tandem Mass Spectrometry
4.Meta-analysis of the interventional effects of music therapy on pain and anxiety of burn patients in wound dressing change.
Ye LI ; Fang Li LIU ; Ju YUAN ; Jing LI ; Zi Wei LIU ; Ningxiao GUAN
Chinese Journal of Burns 2022;38(11):1079-1084
Objective: To evaluate the interventional effects of music therapy on pain and anxiety of burn patients in wound dressing change. Methods: The meta-analysis method was adopted. Databases including China National Knowledge Internet, Wanfang Database, and VIP database were retrieved with the search terms in Chinese version of ", , /, /", and PubMed, Embase, and Cochrane Library were retrieved with the search terms in English version of "music, burn, dressing change/wound dressing, pain/ache/sore" to obtain the publicly published randomized controlled trials on the application of music therapy for wound dressing change in burn patients from the establishment of each database to May 2021. The outcome indexes included pain score/percentage and anxiety score after dressing change. Rev Man 5.4 and Stata 14.0 statistical software were used to conduct a meta-analysis of eligible studies. Results: A total of 520 burn patients from 7 studies were included, including 260 patients in music therapy group who received music therapy and 260 patients in routine dressing change group who received routine dressing change. The bias risk of all the 7 included studies was uncertain. Compared with those in routine dressing change group, the pain percentages (relative risk=0.06, 95% confidence interval=0.01-0.41, P<0.01) and pain scores after dressing change (standardized mean difference (SMD)=-0.91, 95% confidence interval=-1.61--0.22, P<0.05) of patients in music therapy group were significantly lower. Subgroup analysis showed that music type and timing of intervention might be the source of heterogeneity in pain scores after dressing change. The anxiety scores of patients in music therapy group were significantly lower than those in routine dressing change group (SMD=-0.64, 95% confidence interval=-1.09--0.19, P<0.01). There was no publication bias in pain or anxiety scores after dressing change. Conclusions: Music therapy can relieve the pain and anxiety of burn patients during dressing change.
Humans
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Music Therapy/methods*
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Pain/etiology*
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Anxiety/therapy*
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Burns/therapy*
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Bandages
5.Effect and mechanism of terminal fucosylation inhibitor on ciclosporin-induced renal epithelial-mesenchymal transition
Kaifeng MAO ; Jialiang LUO ; Fenwang LIN ; Daming ZUO ; Junsheng YE
Organ Transplantation 2022;13(5):626-
Objective To evaluate the effect and mechanism of terminal fucosylation inhibitor 2-deoxy-D-galactose (2-D-gal) on ciclosporin (CsA)-induced renal epithelial-mesenchymal transition (EMT). Methods Fifteen male C57BL/6 mice aged 8-10 weeks were randomly and evenly divided into the control group (Ctrl group), CsA group and CsA+2-D-gal group (
6.Factors associated with screw penetration after plating for proximal humerus fractures of Neer types Ⅱ&Ⅲ
Zhiyong CUI ; Yun TIAN ; Hui FENG ; Bingchuan LIU ; Kaifeng YE ; Zhishan ZHANG ; Hongquan JI ; Yan GUO ; Fang ZHOU
Chinese Journal of Orthopaedic Trauma 2018;20(4):323-328
Objective To analyze the factors that influence screw penetration after plating for proximal humerus fractures of Neer two-or three-part.Methods We reviewed the patients with proximal humerus fracture of Neer types Ⅱ & Ⅲ who had been treated from January 2006 to June 2017.The data were documented regarding gender,age,Neer classification,osteoporosis,surgical procedure,cephalic screw number,type of medial support and screw penetration.They were divided into 2 groups according to the presence or absence of screw penetration.x2 test and independent samples t test were used with software IBM SPSS 22.0.The multivariate logistic regression was used to identify the independent risk factors when there were two or more statistically significant factors.The two-side test was used and significance was set to P < 0.05.Results Altogether 78 patients were included in our analysis,including 27 males (34.62%) and 51 females (65.38%) with an average age of 57.41 years (from 18 to 85 years).Their average follow-up time was 7.7 months (from 3 to 24 months).There were 54 Neer two-part fractures (69.23%) and 24 Neer three-part ones (30.77%).Screw penetration was observed in 18 patients (23.08%) but not in the other 60 ones (76.92%).The x2 test and independent samples t test revealed that screw penetration was significantly associated with gender (P =0.003),osteoporosis (P =0.003) and cephalic screw number (P =0.003) but not with age (P =0.256),Neer classification(P =0.754),surgical procedure((P =0.308) or type of medial support (P =0.186).The multivariate logistic regression revealed that osteoporosis (P =0.027) and cephalic screw number (P =0.026) were independent risk factors for screw penetration.Conclusions After plating for proximal humerus fractures of Neer two-or three-part,the patients with osteoporosis and those receiving more than 5 cephalic screws may face a higher risk of screw penetration than those without osteoporosis and those receiving 4 cephalic screws.
7.Upregulation of IL-18 expression in blood CD4+ Th2 cells of patients with allergic rhinitis.
Junling WANG ; Huanzhang SHAO ; Ling YE ; Yijie ZHANG ; Bingyu QIN
Chinese Journal of Cellular and Molecular Immunology 2023;39(12):1100-1107
Objective To investigate the expressions of IL-18, IL-18 binding protein isoform a (IL-18BPa) and IL-18 receptor α (IL-18Rα) in blood CD4+ Th2 cells of patients with allergic rhinitis (AR) and the effects of allergens on their expressions. Methods Blood samples of AR patients and healthy control subjects (HCs) were collected. Peripheral blood mononuclear cells (PBMCs) and CD4+ T cells sorted by immunomagnetic beads were stimulated by crude extract of Artemisia sieversiana wild allergen (ASWE), Platanus pollen (PPE) and house dust mite extract (HDME). Flow cytometry was used to detect the expression of IL-18, IL-18BPa and IL-18Rα in CD4+ Th2 cells, and BioPlex was used to detect the level of plasma IL-4 and analyze its correlation with the proportion of IL-18+ Th2 cells. Results Compared with HCs, the proportion of IL-18+ cells was increased in Th2 cells of AR patients; MFI of IL-18 was increased, while that of IL-18Rα was decreased. Moreover, allergens induced IL-18 and IL-18Rα expression in sorted CD4+ Th2 cells of HCs and induced IL-18Rα in that of AR patients. Additionally, elevated plasma IL-4 level was found in AR patients, which was moderately correlated with the percentage of IL-18+ Th2 cells. Conclusion Allergens may be involved in the pathogenesis of AR by inducing expression of IL-18 in peripheral blood CD4+ Th2 cells.
Humans
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Th2 Cells
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Interleukin-18/metabolism*
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Up-Regulation
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Leukocytes, Mononuclear/metabolism*
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Interleukin-4/metabolism*
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Rhinitis, Allergic/metabolism*
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Allergens
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Cytokines/metabolism*
8. Hippocampal vascular injury and cognitive impairment in a mixed mouse models of Alzheimer's disease and type 2 diabetes mellitus
Xiao-Ping CHEN ; Zhao-Xia YAN ; Hong-Ye CHANG ; Bei-Bei CHEN ; Yan-Wei XING ; Wen-Juan FAN
Acta Anatomica Sinica 2021;52(6):863-869
Objective To study the effect of type 2 diabetes mellitus (T2DM) on the cerebral blood vessels in Alzheimer's disease (AD), and to explore its mechanism of influence on the pathogenesis of Alzheimer's disease. Methods To generate a mouse model with AD complicated with long-term T2DM, forty 6-month-old APP/PS1 transgenic mice were fed with high-sugar and high-fat diet for 6 months, that was, when mice at 12 months of age, they were intraperitoneally injected with 1% streptozotocin solution for 4 consecutive days. Then, mice were randomly divided into 4 groups: the normal control group, AD model group, T2DM model group and AD complicated with T2DM model group, 10 mice were used in each group. The learning and memory ability of the mice were tested by the mouse step-down assay, and the vascular morphology of the mice's hippocampal CAI area was observed by ink perfusion. Then oil red 0 staining and immunofluorescent staining were applied to test the pathological indices of the hippocampal area in the model. Results Compared with the control group, AD combined with T2DM mice showed decreasing significantly abilities in the learning and memory (P<0.05), and the blood vessels in the hippocampus became thinner and the vascular density decreased. Moreover, T2DM promoted lipid deposits and vascular leak in the hippocampus of the model. Additionally, the expression of β-site amyloid precursor protein cleaving enzyme-1 (BACE-1), nuclear factor (NF)-κB and matrix metalloproteinase (MMP) -9 were increased compared with the controls in the hippocampal CAI region. Conclusion T2DM plays a negative regulatory role on learning and memory functions of mice, accelerates the onset of AD and result in cerebrovascular lesions. In addition, the abnormal expression of MMP-9 may also be one of the causes of AD vascular lesions.
9.Chemical constituents from ripe fruit of Cornus officinalis.
Xian-Sheng YE ; Jun HE ; Jia-Lin ZHANG ; Xiao-Bin PANG ; Lei ZHANG ; Hao-Yi QIAO ; Xue-Ge PAN ; Jia ZHANG ; Shu-Na LIU ; Wei-Ku ZHANG ; Jie-Kun XU
China Journal of Chinese Materia Medica 2016;41(24):4605-4609
To investigate the chemical compounds from the fruit of Cornus officinalis, six compounds were isolated and determined by extensive spectroscopic analysis as 6'-O-acetyl-7α-O-ethyl morroniside (1), (-)-isolariciresinol 3α-O-β-D-glucopyranoside(2), apigenin (3), cirsiumaldehyde(4), p-coumaric acid (5), caffeic acid (6). Compound 1 was a new iridoid glucoside,and compounds 2-4 were obtained from the Cornus genus for the first time. Compounds 2-6 were evaluated for the viability of PC12 cells when exposed in conditions of oxygen and glucose deprivation. The MTT results showed that compound 4 increased cell viability moderately in OGD/R treated PC12 cells at the concentration of 1.0 μmol•L⁻¹.
10.Ginsenoside Rb1 Protects Human Umbilical Vein Endothelial Cells against High Glucose-Induced Mitochondria-Related Apoptosis through Activating SIRT3 Signalling Pathway.
Shi-Ye KE ; Shu-Jie YU ; Ding-Hui LIU ; Guang-Yao SHI ; Min WANG ; Bin ZHOU ; Lin WU ; Zhi-Ming SONG ; Jie-Ming ZHU ; Chao-Dong WU ; Xiao-Xian QIAN
Chinese journal of integrative medicine 2021;27(5):336-344
OBJECTIVE:
To investigate whether ginsenoside Rb1 (Rb1) can protect human umbilical vein endothelial cells (HUVECs) against high glucose-induced apoptosis and examine the underlying mechanism.
METHODS:
HUVECs were divided into 5 groups: control group (5.5 mmol/L glucose), high glucose (HG, 40 mmol/L) treatment group, Rb1 (50 µ mol/L) treatment group, Rb1 plus HG treatment group, and Rb1 and 3-(
RESULTS:
Rb1 ameliorated survival in cells in which apoptosis was induced by high glucose (P<0.05 or P<0.01). Upon the addition of Rb1, mitochondrial and intracellular reactive oxygen species generation and malondialdehyde levels were decreased (P<0.01), while the activities of antioxidant enzymes were increased (P<0.05 or P<0.01). Rb1 preserved the mitochondrial membrane potential and reduced the release of Cyt-c from the mitochondria into the cytosol (P<0.01). In addition, Rb1 upregulated mitochondrial biogenesis-associated proteins (P<0.01). Notably, the cytoprotective effects of Rb1 were correlated with SIRT3 signalling pathway activation (P<0.01). The effect of Rb1 against high glucose-induced mitochondria-related apoptosis was restrained by 3-TYP (P<0.05 or P<0.01).
CONCLUSION
Rb1 could protect HUVECs from high glucose-induced apoptosis by promoting mitochondrial function and suppressing oxidative stress through the SIRT3 signalling pathway.