1.The in vitro anti-atherosclerotic activity of compound E0869.
Xiao WANG ; Chang LIU ; Peng LIU ; Ni LI ; Yan-Ni XU ; Shu-Yi SI
Acta Pharmaceutica Sinica 2015;50(4):440-446
ATP-binding cassette transporter A1 (ABCA1) and scavenger receptor class B type I (SR-BI/CLA-1) are the key proteins in reverse cholesterol transport (RCT). The high expression of ABCA1 and SR-BI/CLA-1 can decrease the danger of atherosclerosis. The purpose of the study is to find ABCA1 and CLA-1up-regulators for treating atherosclerosis by using cell-based high throughput screening models. Among 20 000 compounds screened, E0869 [1-(3, 4-dimethylphenyl)-1-oxopropan-2-yll4-((methylsulfonyl)methyl)benzoate] was found as the positive hit. The up-regulated activities of E0869 in ABCAl1-LUC and bCA-l1-LUC HepG2 cell were 160% and 175%, respectively. The EC50 values of E0869 in ABCAl1-LUC and CLA-l1-LUC HepG2 cell were 3.79 and 1.42 pμol- x ,(-1) respectively. E0869 could upregulate the mRNA and protein levels of ABCA1, SR-BI/CLA-1 and ABCGJ1genes in HepG2 and RAW264.7 cells by Real-Time Quantitative PCR and Western blotting analysis, but could not influence the expression of FAS, SREBP-l1 and CD36. Foam cell assay showed that E0869 could inhibit lipids accumulation in mouse peritoneal macrophages RAW264.7. Cholesterol efflux assay showed that E0869 could induce HDL-mediated cholesterol efflux in mouse peritoneal macrophages RAW264.7. In conclusion, E0869 could up-regulate ABCA1 and CLA-1 activity, and had good anti-atherosclerotic activity in vitro.
ATP Binding Cassette Transporter 1
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metabolism
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Animals
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Atherosclerosis
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drug therapy
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Biological Transport
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Cholesterol
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Hep G2 Cells
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High-Throughput Screening Assays
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Humans
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Macrophages, Peritoneal
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drug effects
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Mice
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RNA, Messenger
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Scavenger Receptors, Class B
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metabolism
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Up-Regulation
2.Experimental study of hematopoietic stem cell transplantation for the treatment of murine systemic lupus erythematosus
Li NI ; Guanxian LIU ; Guangfu DONG ; Yongjun SHI ; Xiao CUI
Chinese Journal of Rheumatology 2010;14(8):530-534,后插一
Objective To study the effect of mixed purified autogenic and allogeneic hematopoietic stem cell transplantation for the treatment of systemic lupus erythematosus. Methods Thirty-six MRL/lpr mice were randomly divided into the control group, the study group,the mixed group ( the ratio of autogenic to hematopoietic stem cells, mixed in different proportions were infused intravenously after 60Co irradiation. The study group were treated with daily intraperitoneal infusion of dexamethasone 1 mg·kg-1·d-1, while the control group were treated with intraperitoneal infusion of equivalent volume of saline daily. The changes of serum creatinine level, the urine protein excretion of the mice and blood WBC count were compared. Repeat measures ANOVA was used for data analysis. ELISA was used for anti-nuclear antibody detection Light microscopy, electronic micros-copy, immunofluorescence were applied to detect the pathological changes in renal tissue. Results Serum creatinine and urine protein excretion levels increased with time in the ontrol group, while those of the transplant group and the study group decreased. The reduction in mixed transplantation group and the study group was more evident compared with that of the allogeneic group. The difference was statistically significant (P<0.05), but there was no significant difference between the mixed transplantation groups and the study group (P>0.05). The histopathologic damage was most serious in the control group as pathological injury score of most mice were in grade 3 or 4. The majority of the histopathologic damage of the allogeneic group was in grade 2. Most f pathological damage of the study drug group and the mixed transplantation group were grade 1 or 2. Conclusion Mixed hematoopoietic stem cell transplantation for the treatment of murine systemic lupus erythematosus can effectively correct heavy proteinuria in murine systemic lupus erythematosus so improve the renal damage. It is a safe and effectively way to treat murine systemic lupus erythematosus.
3.In-Vitro Anti-HBV Activity of Bushen Jianpi Formula
Wanwan HE ; Ni LIU ; Huiquan XIAO ; Riyong LUO ; Yutong ZHU
Journal of Guangzhou University of Traditional Chinese Medicine 2001;0(01):-
[Objective]: To study the in-vitro anti-HBV activity of Bushen Jianpi Formula (BJF). [Methods] 2.2.15 cell strain was cultured in vitro to observe the effect of BJF on its secretion of HBsAg and HBeAg. [Results] After the addition of BJF for ten days, median toxic concentration of BJF was 37.80g/L, median inhibitory concentrations of HBsAg and HBeAg were 19.05g/L and 9.55g/L, and the therapeutic index was 1.98and 3.96. [Conclusion] It is suggested that BJF has an in-vitro inhibitory effect on the secretion of HBeAg.
4.The in vitro anti-atherosclerotic activity of compound IMB-1680.
Ting-Ting FENG ; Yong-Zhen LI ; Ni LI ; Chang LIU ; Xiao WANG ; Yan-Ni XU ; Shu-Yi SI
Acta Pharmaceutica Sinica 2014;49(5):602-607
In the previous study, a high-throughput screening method was established to find the antagonists of CD36. In the present study, a new compound named IMB-1680 was found using this method. The anti-atherosclerotic activities of IMB-1680 were then evaluated. Dose-dependent activities of IMB-1680 were detected by using Sf9 [hCD36] and CHO [hCD36] models. Fluorescence microscopic photography and flow cytometry were used to analyze uptake of mLDL. Foam cell test with RAW264.7 macrophages was used to examine lipid accumulation. The results showed that IMB-1680 inhibited CD36 activity with IC50 of 2.80 and 8.79 micromol x L(-1) in Sf9[hCD36] and CHO [hCD36] cells, respectively. Fluorescence microscopic photography and flow cytometry revealed that IMB-1680 could significantly reduce DiI-AcLDL uptake. Meanwhile, IMB-1680 also could reduce lipids accumulation in RAW264.7 macrophages. In all, the data indicated that IMB-1680 might be a potent effective anti-atherosclerotic leading compound.
Animals
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CD36 Antigens
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antagonists & inhibitors
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genetics
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metabolism
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CHO Cells
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Cells, Cultured
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Cricetulus
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Dose-Response Relationship, Drug
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Foam Cells
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cytology
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High-Throughput Screening Assays
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Humans
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Lipoproteins, LDL
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metabolism
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Macrophages
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cytology
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metabolism
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Mice
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Molecular Structure
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Plasmids
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Receptors, Scavenger
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antagonists & inhibitors
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Sf9 Cells
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Spodoptera
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Transfection
5.Optimization of Purification Technology for Total Flavonoids from Callicarpa nudiflora Hook. et Arn. by Macroporous Adsorption Resin
Yong LIU ; Pengwei ZHANG ; Wenqin SU ; Xiao LIU ; Keming GONG ; Ni XIANG
Herald of Medicine 2015;(5):640-643
Objective To optimize purification technology of total flavonoids in Callicarpa nudiflora Hook. et Arm. by macroporous adsorption resin. Methods Macroporous resin models including AB-8, D-101, HP-20, HP2MG, were optimized by static adsorption and desorption experiments regarding to adsorption rate and desorption rate of total flavonoids. Purification technology parameters of total flavonoids were optimized by single factor test. Results HP-20 macroporous resin presented the best purification efficiency,the optimum purification conditions were that taking 4. 46 mg·mL-1 of total flavonoidsat pH 3. 0, loading at 3 BV·h-1, washed with 3BV of water at 3 BV·h-1,then eluted with 4 BV 75% ethanol at 2 BV·h-1, finally obtaining the total flavonoids from the dry extract of Callicarpa nudiflora Hook. et Arn. with the purity of 47. 4%. Conclusion HP-20 macroporous resin is suitable for preliminary purification of total flavonoids in Callicarpa nudiflora Hook. et Arn.
6.The establishment of VX2 hepatic carcinoma model in rabbits and the observation of its growing and metastatic characteristics
Zhi LI ; Caifang NI ; Fenglin DONG ; Rong XIAO ; Hang LIU ; Yizhi LIU ; Yonghai JIN ; Jian SHEN
Journal of Interventional Radiology 2009;18(9):691-694
Objective To establish VX2 hepatic carcinoma model in rabbits by implanting the tumor fragment into the liver through percutaneous puncture under ultrasound guidance and to observe its growing and metastatic characteristics, to determine the optimal time for interventional experiment study with the model. Methods Inoculation of VX2 carcinoma fragment was performed in 28 New Zealand white rabbits. PET/CT and ultrasonography (US) examinations were carried out in the second, third and forth week after the inoculation, and each time two tumor-bearing rabbits were sacrificed for pathologic study. Results The successful rate of model establishment was 89.28% (25/28). On PET or CT scans, single lesion in the liver was demonstrated in 25 rabbits. Two, three and four weeks after the inoculation, the maximum diameter of the tumor was (4.82±0.80) mm, (16.05±2.89) mm and (30.08±5.38) mm respectively, while the metastasis rates was 0% (0/25), 13.04% (3/23), 76.19% (16/21) respectively. No significant necrosis was found in the second week after inoculation, only tiny coagulation necrosis was revealed in the third week, and massive necrosis was seen in the forth week. Conclusion Percutaneous inoculation of the tumor fragment into the liver under ultrasonographic guidance is a simple method to establish VX2 hepatic carcinoma in rabbits with a high successful rate. The third week after inoculation is the suitable time for making interventional experiment study.
7.A comparison study of the clinical features between Chinese and Indian primary congenital glaucoma patients
Mao, LI ; Xiao-Ming, CHEN ; Ya-Li, LIU ; Ru-Gang, PAN ; Dong-Jing, LIU ; Ni, LI
International Eye Science 2006;6(2):282-290
· AIM: To summarize the clinical features of Chinese primary congenital glaucoma and to investigate the discrepancies of the clinical features between the Chinese and Indian patients.congenital glaucoma patients were reviewed. The clinical features were summarized as several quantifiable clinical parameters and the severity of the disease was evaluated. Both the quantified clinical features and severity were statistically compared with those of the Indian patients, which were cited from the previous published articles.included in the study. In Chinese patients, sex ratio (male to female )was about 2:1, family history was presented in 3 patients (7.5%) and consanguinity was found in one patient (2.5%). The main symptoms and signs observed in Chinese patients spanned a wide spectrum of manifestations. The most frequent signs noted on the initial examination were enlarged eyeball (42.5%) and decreased visual acuity (35.0%). Compared with Indian patients, Chinese patients had a later onset, a delayed diagnosis, more severe corneal changes and more severe optic nerve damages (P<0.01). The combined tabeculectomy and trabeculotomy operation was preferred by both Chinese and Indian doctors whereas a higher proportion of Indian patients received the combined operation (P<0.01). The proportions of the severity grade were different between Chinese and Indian patients. Most Chinese patients were in the severe grade while most Indian patients were in the very severe grade (P<0.01).patients were sporadic and non-consanguineous.Compared with Indian patients, Chinese patients had a relative later onset, a delayed diagnosis and treatment.More attempts are needed in Chinese PCG prevention and treatment.
8.The in vitro anti-atherosclerotic activity of compound E0869.
Xiao WANG ; Chang LIU ; Peng LIU ; Ni LI ; Yanni XU ; Shuyi SI
Acta Pharmaceutica Sinica 2015;50(4):440-6
ATP-binding cassette transporter A1 (ABCA1) and scavenger receptor class B type I (SR-BI/CLA-1) are the key proteins in reverse cholesterol transport (RCT). The high expression of ABCA1 and SR-BI/CLA-1 can decrease the danger of atherosclerosis. The purpose of the study is to find ABCA1 and CLA-1up-regulators for treating atherosclerosis by using cell-based high throughput screening models. Among 20 000 compounds screened, E0869 [1-(3, 4-dimethylphenyl)-1-oxopropan-2-yll4-((methylsulfonyl)methyl)benzoate] was found as the positive hit. The up-regulated activities of E0869 in ABCAl1-LUC and bCA-l1-LUC HepG2 cell were 160% and 175%, respectively. The EC50 values of E0869 in ABCAl1-LUC and CLA-l1-LUC HepG2 cell were 3.79 and 1.42 pμol- x ,(-1) respectively. E0869 could upregulate the mRNA and protein levels of ABCA1, SR-BI/CLA-1 and ABCGJ1genes in HepG2 and RAW264.7 cells by Real-Time Quantitative PCR and Western blotting analysis, but could not influence the expression of FAS, SREBP-l1 and CD36. Foam cell assay showed that E0869 could inhibit lipids accumulation in mouse peritoneal macrophages RAW264.7. Cholesterol efflux assay showed that E0869 could induce HDL-mediated cholesterol efflux in mouse peritoneal macrophages RAW264.7. In conclusion, E0869 could up-regulate ABCA1 and CLA-1 activity, and had good anti-atherosclerotic activity in vitro.
9.Effects of Tansvaginal Aspiration of Hydrosalpinx Combined Auricular Point Sticking on IVF-ET Outcomes.
Jin-xia AN ; Ya-li NI ; Xiao-ling LIU ; Xi-hong GAO ; Yan WANG
Chinese Journal of Integrated Traditional and Western Medicine 2015;35(6):682-685
OBJECTIVETo explore effective pretreated methods for hydrosalpinx before frozen embryo transfer (FET).
METHODSA randomized controlled study was performed on 229 FET cycles of hydrosalpinx patients. They were assigned to two groups by random digit table, Group A (94 cases), Group B (89 cases), and Group C (46 cases). Patients in Group A received transvaginal aspiration of hydrosalpinx combined with auricular point sticking. Those in Group B received transvaginal aspiration of hydrosalpinx group. Those in Group C received no transvaginal aspiration of hydrosalpinx. Pregnancy outcomes of FET, endometrial and subendometrial blood flow distribution on the embryo transfer day were compared among the three groups.
RESULTSThere was no statistical difference in the endometrial thickness on FET day, the number of transfer embryos, the number of transferred good quality embryos among the three groups (P > 0.05). The clinical pregnancy rate and the embryo implantation rate were significantly higher in Group A than in Group C (P < 0.05), and the clinical pregnancy rate was significantly higher in Group A than in Group B (P < 0.05). The early abortion rate and the transfer cycle cancel rate were significantly lower in Group A than in Group C (P < 0.05). Type A endometrial and subendometrial blood flow distribution was dominant in Group A, which was significantly higher in Group A than the rest two groups (P < 0.05). Type A distribution rate was also significantly higher in Group B than in Group C (P < 0.05).
CONCLUSIONTransvaginal aspiration of hydrosalpinx combined with auricular point sticking before FET could improve the endometrial receptivity and improve outcomes of IVF.
Embryo Implantation ; Embryo Transfer ; methods ; Female ; Fertilization in Vitro ; methods ; Humans ; Pregnancy ; Pregnancy Outcome ; Pregnancy Rate
10.Research on the relationship between sensation seeking, personality charateristic and health-risk behaviors of medical freshmen
Nina LI ; Zuoji ZHANG ; Hongjing WANG ; Zhaojun NI ; Xiao CHEN ; Yan LIU ; Xiuning YUE ; Dong SONG
Chinese Journal of Behavioral Medicine and Brain Science 2011;20(12):1077-1079
Objective To study the relationship between sensation seeking,personality characteristics and health-risk behaviors of medical freshmen.Methods Sensation Seeking Scale ( SSS),Eysenck Personality Questionnaire( EPQ),Adolescent Health-Risk Behaviors Questionnaire were applied in this survey to 384 freshmen from two medical colleges.Results ① The health risk behaviors were comnmon in the medical college freshmen (5.2%,48.2% ),and the score of health risk behaviors had a significant difference between boys and girls,boys risk behaviors were much more than girls(P< 0.05 ).②The correlations between the risk behaviors (such as smoking,drinking,fighting,suicidal ideas,using internet too long,poor eating behavior,lack of physical exercise) and sensation seeking personality traits were strong.The health-risk behaviors were all correlated with extraversion(E)and neuroticism (N) significantly( 66.78 ± 10.29 vs 60.57 ± 9.09,t =2.54,P < 0.01 ;7.11 ± 3.23 vs 5.33 ±2.89,t =2.81,P < 0.05 ).③The results of logistic regression analysis showed that male mother' s high education level,sensation seeking,Eysenck' s P,N dimension were effective prediction factors of freshmen ' s health-risk behaviors.Conclusion Medical college freshmen who have higher levels of sensation seeking,Eysenck' s P,N dimension are more prone to health risk behaviors.