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.Establishment and characteristics of a human chordoma cell line.
Dian-zhong ZHANG ; Bao-an MA ; Qing-yu FAN ; Heng CHANG ; Yan-hua WEN
Chinese Journal of Oncology 2003;25(3):234-237
OBJECTIVETo present an established human chordoma cell line for chordoma research.
METHODSThe specimens pathologically identified as chordoma were cultured, using primary tissue culture in vitro. The surviving cells were analyzed by morphology, histochemical stain, cell cycling analysis, karyotype analysis, electron microscopic observation, heterotransplantation and study of invasive capacity in vitro.
RESULTSThe newly established cell line CM-319 has been maintained in continual cultures for over 100 generations in two years. Its morphological observation, histochemical staining properties, electron microscopic observation and heterotransplantation showed the common characteristics of chordoma. The doubling time of cells was about 33 hours. Cell cycle analysis showed: G(1) 55.6%, G(2) 21.9% and S 22.5%, G(2)/G(1) = 1.90. Chromosome analysis showed a hypotriploid feature and the success rate of heterotransplantation was 100%. It is capable of invasion in vitro.
CONCLUSIONCM-319, as a cell line derived from human chordoma cells, may serve for further studies of chordoma.
Animals ; Cell Line, Tumor ; Cell Proliferation ; Chordoma ; genetics ; pathology ; Humans ; Mice ; Mice, Inbred BALB C ; Neoplasm Invasiveness
9.Diagnosis and treatment of sellar germinoma.
Yi YANG ; Zu-yuan REN ; Chang-bao SU ; Ren-zhi WANG ; Wen-bin MA
Acta Academiae Medicinae Sinicae 2003;25(3):350-353
That eleven patients with sellar germinomas were confirmed by pathological examinations were retrospectively reviewed. In the 11 patients, 2 were males and 9 were females. Mean age was 16.8 years old and mean history was 2.6 years. Among them, 11 patients had diabetes insipidus, 6 patients had visual disturbances, 5 patients had retarded growth, and 5 patients had hypopituitary function. The diameter of tumor was 1-3 cm in 8 cases and greater than 3 cm in 3 cases. MRI showed hypointensity or homogeneous on T1-weighted images in 8 cases. The tumors were fibrous, purple grey or reddish in color with rich blood supply. Germinomas were confirmed by postoperative pathological examinations. All patients received postoperative irradiation. Postoperative follow-up was from 3 months to 6 years. Diabetes insipidus was improved in 9 cases. Visual function were improved in 4 cases, but hypopituitarism and retarded growth were unchanged. In conclusion, when MRI shows sellar parenchyma tumor with unclear boundary in young patients with diabetes insipidus and hypopituitarism, sellar germinoma should be highly suspected. Otherwise, radiation therapy may profitably aid to confirm the diagnosis since irradiation is the main treatment of sellar germinomas.
Adolescent
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Adult
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Brain Neoplasms
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diagnosis
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surgery
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Diagnosis, Differential
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Female
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Germinoma
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diagnosis
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surgery
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Humans
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Magnetic Resonance Imaging
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Male
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Pineal Gland
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Pinealoma
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diagnosis
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surgery
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Pituitary Neoplasms
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diagnosis
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surgery
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Retrospective Studies
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Sella Turcica
10.Intestinal absorption of the effective components of Schisandra chinensis Baill by rats single-pass perfusion in situ.
Xin-Min CHEN ; Jun-Song LI ; Wen LI ; Lei HAN ; Xun-Hong LIU ; Liu-Qing DI ; Bao-Chang CAI
Acta Pharmaceutica Sinica 2010;45(5):652-658
The aim of the study is to investigate rat intestinal absorption behavior of three main active components, schisandrol A, schisandrin A and schisandrin B in Schisandra chinensis Baill extracts in intestine of rats. With phenol red as the indicator, in situ single pass intestinal perfusion (SPIP) model was used and the concentrations of three main active components in perfusion solution of different intestinal segments (duodenum, jejunum, ileum, and colon) were determined by HPLC in combination with diode array detection. The results showed that the absorption rate constant (Ka) and effective permeability values (Peff) of three main active components in Schisandra chinensis Baill extracts had significant difference (P < 0.05) at different concentrations of perfusion solution, the Ka and Peff first increased and then decreased with the increase of drug concentration, the middle concentration was higher than those of the other two concentrations. The saturate absorption phenomena were observed, and it suggested that the transport mechanisms of three main active components in vivo were similar to active transport or facilitated diffusion. Three active components can be well absorbed in all of the intestinal segments, while duodenum is the best absorption region. The Ka and Peff of three active components in jejunum and ileum had no significant difference (P > 0.05). The absorption of the three active components displayed significant difference (P < 0.05) at different intestinal segments of rats. Schisandrin A had the best absorption in duodenum. The Ka and Peff among three active components were sequenced as follows: schisandrin A > schisandrin B > schisandrol A in other intestinal segments, and there is significant difference (P < 0.05) between them.
Animals
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Chromatography, High Pressure Liquid
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Colon
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metabolism
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Cyclooctanes
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administration & dosage
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isolation & purification
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pharmacokinetics
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Dose-Response Relationship, Drug
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Drugs, Chinese Herbal
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administration & dosage
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isolation & purification
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pharmacokinetics
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Duodenum
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metabolism
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Fruit
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chemistry
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Ileum
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metabolism
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Intestinal Absorption
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Jejunum
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metabolism
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Lignans
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administration & dosage
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isolation & purification
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pharmacokinetics
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Male
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Perfusion
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Permeability
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Plants, Medicinal
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chemistry
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Polycyclic Compounds
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administration & dosage
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isolation & purification
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pharmacokinetics
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Rats
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Rats, Sprague-Dawley
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Schisandra
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chemistry