2.Design, synthesis and anti-proliferative activity of novel coumarin derivatives linking Schiff base and aryl nitrogen mustard.
Wen-Hu LIU ; Shi-Bao WANG ; Jin-Xia CHANG ; Yi LIU
Acta Pharmaceutica Sinica 2014;49(2):217-224
To explore novel coumarin derivatives with more potent anti-proliferative activity, a series of novel compounds were designed and synthesized by linking Schiff base and N, N-bis (2-chloroethyl) amine pharmacophore of nitrogen mustards to the coumarin's framework. Their structures were confirmed by 1H NMR, MS and element analysis techniques. In vitro anti-proliferative activities were evaluated against HepG2, DU145 and MCF7 cell lines by the standard MTT assay. The results showed that some of the target compounds exhibited strong anti-proliferative activities against selected tumor cells, and compounds 7c, 7f, 7g, 7h and 7q were better than or equal to the activities of positive control, they deserved further development.
Antineoplastic Agents
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chemical synthesis
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pharmacology
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Cell Line, Tumor
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Cell Proliferation
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drug effects
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Coumarins
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chemical synthesis
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pharmacology
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Drug Design
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Drug Screening Assays, Antitumor
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Humans
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Nitrogen Mustard Compounds
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chemical synthesis
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pharmacology
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Schiff Bases
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Structure-Activity Relationship
3.Correlation of personality characteristics and quality-of-life in patients with chronic urticaria
Yu FU ; Yingqiu BAO ; Xiaofeng WEI ; Min YANG ; Wen SU ; Jianmin CHANG
Chinese Journal of General Practitioners 2015;14(10):768-770
WHO quality-of-life scales (WHOQOL-BREF) and Eysenck personality questionnaire (EPQ) were used for evaluating the quality-of-life and personality characteristics of 60 outpatients with chronic urticaria.According to statistical correlation analysis, a positive correlation existed between education level and psychological field (P < 0.05).And there were negative correlations between N scale, P scale and psychological field (P < 0.05, P < 0.01).The incidence and incurability of chronic urticaria was more correlated with anxiety and depression.The patients with chronic urticaria were more likely to have a worse quality-of-life than normal population.
4.Protection of quercetin against hyperbaric oxygen-induced apoptosis of human lens epithelial cell and its mechanism
Li-bin, CHANG ; Yong-zhen, BAO ; Yi, CHEN ; Wen-zhen, YU ; Xiao-xin, LI
Chinese Journal of Experimental Ophthalmology 2012;30(6):485-489
Background Oxidative stress-induced apoptosis of human lens epithelial cells (LECs) is associated with c-Jun N terminal kinase (JNK) pathway.Quercetin possesses the antioxidation by inhibiting the JNK pathway.However,whether quercetin can protect LECs from the oxygen-induced damage is still not proved.Objective This study attempted to invatigate the effects and its mechanism of quercetin against hyperbaric oxygeninduced LECs apoptosis. Methods Human LECs line SRA01/04 was cultivated and passaged in MEM medium containing 10% fetal bovine serum and 0.5% non-essential amino acids for 2 hours,with or without 20 μmol/LSP600125 or 1 μmol/L quercetin prior to exposure to hyperbaric oxygen.Each exposure session remained 6 hours in 99% O2 and 1%CO2 with a pressure chamber at 588 kPa.The viability of human LECs was detected by MTT.Cell apoptosis was assessed by flow cytometer using Annexin V-FITC apoptosis detection.The expression of JNK/p-JNK,c-Jun/p-c-Jun,caspase 3 and caspase 9 were detected by Western blot. Results LECs viability (A570 ) was 0.835 ±0.082,0.450±0.083,0.654±0.079,0.649±0.090 respectively in the blank control group,hyperbaric oxygen exposed group,hyperbaric oxygen+SP600125 group and hyperbaric oxygen+quercetin group.The A570 in the hyperbaric oxygen exposed group was significantly lower than the blank control group ( P =0.000),but those in hyperbaric oxygen + SP600125 group and hyperbaric oxygen+quercetin group were significantly higher than the hyperbaric oxygen exposed group ( P =0.003,0.002 ).The numbers of apoptosis cells were 3.17 ±0.74,19.77 ± 1.44,8.45 ±0.93,7.79 ±0.78 respectively in the blank control group,hyperbaric oxygen exposed group,hyperbaric oxygen+SP600125 group and hyperbaric oxygen+quercetin group.Apoptotic LECs were significantly increased in the hyperbaric oxygen exposed group compared with the blank control group ( P=0.000),but those in the hyperbaric oxygen+SP600125 group and hyperbaric oxygen+quercetin group were significantly reduced in comparison with hyperbaric oxygen exposed group (both P=0.000).In additional,expressions of p-JNK,p-c-Jun,caspase 3 and caspase 9 proteins in the cells were elevated in the hyperbaric oxygen exposed group compared with the blank control group (all P =0.000 ),however,those in the hyperbaric oxygen + SP600125 group and hyperbaric oxygen + quercetin group were declined when compared with the hyperbaric oxygen exposed group( all P<0.05 ). Conclusions JNK pathway is involved in the apoptotic procedure of human LECs induced by oxygen stress.SP600125 and certain concentration of quercetin can interdict the JNK signal pathway and endogenous apoptosis of LECs and further alleviate hyperbaric oxygen-induced damage of LECs.
5.Study on index components and fingerprints of crude and processed Siegesbeckia Herbs.
Fan-Yao KONG ; Hui-Hua HU ; Zhi-Bao HAN ; Wen-Ying XU ; Meng-Xin FENG ; Chang-Hua MA
China Journal of Chinese Materia Medica 2014;39(15):2907-2911
The change of kirenol, darutigenol and darutoside in Siegesbeckia and its first to ninth processed products were studied, and the ten fingerprints were compared, which provided the experimental basis for the study of Siegesbeckia processing tech- nology. The samples were analysed by HPLC on a SunFire-C18 column (4.6 mm x 150 mm, 5 μm) with gradient elution of acetonitrile (0.1% formic acid)-water (0.1% formic acid) at a flow rate of 1.0 mL x min(-1). Column temperaturewas 30 °C and the detected wavelength was 215, 320 nm. The calibration curves of kirenol, darutigenol and darutoside were linear in the range of 2.180-26.16, 2.900-34.80, and 1.012-6.072 mg x L(-1), respectively, and the average recoveries were 96.4%, 97.2% and 96.3% wit RSD 2.2%, 1.7% and 2.4%. This method was simple, the result was stable and had good repeatability, recovery and precision. The re- sult was the basis of the chemical contents variation in the processing of Siegesbeckia Herbs and further clarifying the effect of the changing.
Asteraceae
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chemistry
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Chemistry, Pharmaceutical
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Chromatography, High Pressure Liquid
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Drugs, Chinese Herbal
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chemistry
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Temperature
6.Evaluation of early efficacy of neoadjuvant chemotherapy in patient with breast cancer based on dynamic contrast-enhanced MRI via comparing with 18F-FDG PET/CT
Yixue CHANG ; Shengbao WEN ; Haihua BAO ; Weixia LI ; Yousen WU
Journal of Practical Radiology 2024;40(2):222-225,269
Objective To investigate the predictive value of early efficacy of neoadjuvant chemotherapy(NAC)in patient with breast cancer via full quantitative parameters of dynamic contrast-enhanced magnetic resonance imaging(DCE-MRI).Methods Forty patients with breast cancer were selected.The 18 fluorodeoxyglucose positron emission tomography/computed tomography(18F-FDG PET/CT)and DCE-MRI were performed before and after two cycles of NAC.According to the decrease rate of maximum standardized uptake value(ΔSUVmax)of PET/CT before and after two cycles of NAC,all patients were divided into two groups,including good response group(24 cases)(ΔSUVmax>40%)and general response group(16 cases)(ΔSUVmax≤40%).The changes of full quantitative parameters of DCE-MRI between the two groups were observed and analyzed.Results There were statistically significant differences in changes of Ktrans and Kep between the two groups(P<0.05),however,there was no significant difference in the change of Ve between the two groups(P>0.05).There was a significant positive correlation between ΔKtrans and ΔSUVmax(r=0.850,P<0.001).There was a high positive correlation between ΔKtrans and ΔKep(r=0.727,P<0.001).Conclusion The full quantitative parameters of DCE-MRI are helpful to evaluate the early efficacy of NAC in breast cancer,which can reflect the changes of microcirculation in the lesion,further reflect the therapeutic effect of NAC,guide the clinical optimization of treatment plan in time,and achieve accurate evaluation and individualized treatment.
7.Self-care Experiences of Adolescents with Spinal Muscular Atrophy
Bao-Huan YANG ; Chia-Ying CHUNG ; Wen-Chin WENG ; Kao-Wen LO ; Yuh-Shiow LI
Asian Nursing Research 2021;15(4):231-238
Purpose:
We examined the self-care experiences of adolescents with spinal muscle atrophy (SMA) and their perceptions of the interactions between their body and the environment.
Methods:
We interviewed ten adolescents with SMA aged 13–18 years regarding personal care practices. Purposive sampling was conducted in two medical centers in northern Taiwan. Data were analyzed using the Giorgi analysis method.
Results:
Four constitutions were identified: (1) limited space for independent development, (2) multiple reconstructions of self-image to improve physical ability, (3) self-care of disease, and (4) developing activity styles to accommodate social culture.
Conclusion
The self-care lived experiences of patients reflect dynamic changes in the body and environment. Self-existence was exhibited by adjustment, practice, and creativity of physical activity to integrate into society. Nursing staff should understand the self-care experiences and needs of adolescents with SMA to develop a database of self-care skills. This study recommended that nursing staff improve their ability to guide patients in taking care of themselves by developing body awareness self-care courses and individual care plans in response to various stages of disability to help patients delay deterioration, realize their physical potential, and promote independence and social development.
8.Production and characterization of anti-estrone monoclonal antibody.
Yong-Cheng WANG ; Zhen-Quan GUO ; Yuan-Zong LI ; Wen-Bao CHANG
Biomedical and Environmental Sciences 2002;15(2):103-112
OBJECTIVEDetermination of estrone (E1) levels has a significant meaning in evaluating physiological effect and diagnosing some diseases. In order to detect free E1 in biological fluids, a monoclonal antibody specific for E1 was prepared after the complete antigen of E1 was synthesized. The purified monoclonal antibody was fully characterized for later immunoassay.
METHODS3-O-carboxymethyl ether derivative of E1 was synthesized and in turn coupled to bovine serum albumin (BSA) to form complete antigen E1-BSA. A monoclonal antibody (McAb) specific for E1 was produced both in vitro and in vivo by a hybridoma anti-E1. Anti-E1 was prepared by fusion of SP2/0 murine myeloma cells with spleen cells isolated from immunized BALB/c mouse. The McAb was characterized by enzyme-linked immunosorbent assay (ELISA), SDS-PAGE and Western-blotting. The specificity of the immunoassay was investigated by determining the cross-reactions of E1 analogs when free E1 was detected by competitive indirect enzyme-linked immunosorbent assay (CI-ELISA).
RESULTSAnalysis revealed that anti-E1 McAb (E1-McAb) was of the IgG1 type, the molecular weight of E1-McAb was 164,000 daltons. The affinity constant of E1-McAb with coated complete antigen was 8.2 x 10(8) L/mol. The linear range for free E1 determined by CI-ELISA was 10 pg/mL-10 ng/mL. The detection limit was 21.4 pg/mL (defined as twice the standard deviation of the blank).
CONCLUSIONThe CI-ELISA developed with E1-McAb was both sensitive and specific. The prepared E1-McAb can be used in some immunoassays.
Animals ; Antibodies, Monoclonal ; biosynthesis ; immunology ; Antibody Affinity ; Antibody Specificity ; Blotting, Western ; Cross Reactions ; Electrophoresis, Polyacrylamide Gel ; Enzyme-Linked Immunosorbent Assay ; Estrone ; immunology ; Female ; Hybridomas ; immunology ; Mice ; Mice, Inbred BALB C
9.The application of tunica vaginalis flap in urethral repair.
Wen-yong XUE ; Chang-bao QU ; Xiao-lu WANG ; Feng-xiang ZHANG ; Chun-sheng KANG
Chinese Journal of Plastic Surgery 2007;23(1):45-47
OBJECTIVETo investigate the application of tunica vaginalis flap in repairing the deformity of urethra and urethral fistulas.
METHODSTunica vaginalis flap from the scrotum were used to wrap the reconstructed urethra in the 38 cases of hypospadias urethroplasty and urethral fistulas repair from 2002.
RESULTSAll of cases were followed up for six months to one year. There was a fistula reoccurred after epispadias fistula repair, the repair was successful in other patients. There was no recurrent fistulas or urethral strictures. Penile cosmesis was excellent and erected well.
CONCLUSIONSThe application of tunica vaginalis flap in urethral repair can raise achievement ratio and reduce the incidence of urethral fistulas. The flap is ease to mobilize with no harmful effects on the testicles.
Adolescent ; Child ; Child, Preschool ; Follow-Up Studies ; Humans ; Hypospadias ; surgery ; Male ; Scrotum ; surgery ; Surgical Flaps ; Testis ; surgery ; Urethra ; surgery ; Urethral Diseases ; surgery ; Urinary Fistula ; surgery ; Young Adult
10.Correction of pediatric concealed penis by using a modified Devine' s technique.
Chang-bao QU ; Wen-yong XUE ; Xiao-lu WANG ; Feng-xiang ZHANG ; Chun-sheng KANG
Chinese Journal of Plastic Surgery 2006;22(5):342-343
OBJECTIVETo discuss the diagnosis of pediatric concealed penis and evaluate the results after the correction of the pediatric concealed penis.
METHODSTwenty patients with pediatric concealed penis were treated by using a modified Devine's technique.
RESULTSThe appearance with a straightening penile was achieved in all of the patients. All of the patients recovered well after the operation without any complications.
CONCLUSIONSThe modified Devine' s technique could be a safe and effective method for the correction of the pediatric concealed penis with satisfactory outcome.
Adolescent ; Child ; Humans ; Male ; Penis ; abnormalities ; Reconstructive Surgical Procedures ; methods ; Skin Transplantation ; Surgical Flaps