1.Novel hybrids of (phenylsulfonyl)furoxan and N-benzyl matrinol as anti-hepatocellular carcinoma agents.
Li-qin HE ; Qi YANG ; Ya-xian WU ; Xiao-shan WANG
Acta Pharmaceutica Sinica 2015;50(5):574-578
N-Benzyl matrinol was obtained by hydrolysis, benzylation and reduction reaction from matrine. A series of hybrids (8a-8n) from (phenylsulfonyl)furoxan and N-benzyl matrinol were synthesized and biologically evaluated as anti-hepatocellular carcinoma agents. All target compounds were evaluated for anti-proliferative activity against human hepatocellular Bel-7402, SMMC-7721, Bel-7404, and HepG2 cells in vitro by MTT method. The results indicated that all of these compounds had potent anti-proliferative activity which were more potent than their parent compound and 5-FU, especially 8a-8h and 8j showed the strongest anti-HCC HepG2 cell activity with IC50 values of 0.12-0.93 μmol x L(-1).
Antineoplastic Agents
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pharmacology
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Carcinoma, Hepatocellular
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Fluorouracil
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Hep G2 Cells
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Humans
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Liver Neoplasms
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Oxadiazoles
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pharmacology
2.Clinical effect of anterior vitrectomy for congenital cataract
Hua, HE ; Feng, ZHOU ; Qi, ZHU ; Qian, WANG ; Xue-Mei, WU ; Jian, MA ; Ya-Yun, WANG
International Eye Science 2015;(5):825-827
?AlM: To evaluate the clinical efficacy of posterior continuous curvilinear capsulorhexis ( PCCC ) combined with anterior vitrectomy in preventing posterior capsule opacification of congenital cataract surgery.
?METHODS:Postoperative clinical follow-up data of 82 cases ( 87 eyes ) with congenital cataract treated in Eye Center of our hospital from January 2011 to August 2014 were retrospectively analyzed. The patients were divided into the surgical control group ( 38 cases, 40 eyes, recieved phacoemulsification + PCCC ) and the study group ( 44 cases, 47 eyes, accepted phacoemulsification+ PCCC + anterior vitrectomy). The incidence of central optic axis opaque and postoperative visual acuity distribution were recorded at 1a follow - up. lntraoperative and postoperative complications were observed.
?RESULTS:The rate of central optic axis opaque grade 0 in control group was 37. 5%, compared to 76. 6% in study groups. The opacity distribution ratio of grade 1,2,3 and 4 in study group were lower than that of control group, and the central optic axis opacity distribution ratio in study group was significantly better than that of control group (P<0. 05). The 19 eyes(47. 5%) of visual acuity testing ≤0. 5 in control group , was higher than the 7 eyes(14. 89%) of that in the study group, The 21 eyes (52. 5%) of visual acuity testing >0. 5 in control group was lower than the 40 eyes ( 85. 11%) of that in study group. The visual acuity between two groups has statistical significance difference after 1a follow-up ( P<0. 05 ) , and the visual acuity in study group was significantly better than that in the control group. The postoperative intraocular pressure at 1mo and 1a follow-up was lower than before operation in two groups ( P<0. 05), but there was no significant difference between two groups in intraocular pressure (P<0. 05).
?CONCLUSlON: Combination of phacoemulsification, PCCC and anterior vitrectomy presents reliable clinical effects on postoperative central optic axis opacity distribution ratio and visual acuity, and it should be adopted to prevent the occurrence of posterior capsule opacification.
3.The relationship between four GWAS-identified single nucleotide polymorphisms and female breast canc-er in Henan population
Yaning HE ; Qi CHEN ; Hui LIU ; Xianfu SUN ; Chaojun LIU ; Yingbo SHAO ; Ya ZHAO
Chinese Journal of Endocrine Surgery 2015;(5):367-371
Objective To verify the association between common breast cancer susceptibility loci which have been confirmed in European and Asian populations and breast cancer susceptibility in sporadic breast cancer among the Han nationality in Henan province , and to analyze their genotypes in the internal type of breast cancer . Methods In 253 breast cancer patients ( the case group ) and 343 patients who had benign breast lesions ( the control group), rs2046210(6q25.1), rs2981582(EGFR2), rs889312(MAP3K1), and rs3803662(TOX3/TNRC9)were genotyped by SNP im-LDR technique.According to estrogen receptor(ER), progesterone receptor (PR), human epidermal growth factor receptor 2(HER2)and Ki67, breast cancer are divided into 5 types:Lu-minal A, Luminal B, HER2-enrich, Luminal HER2, and triple negative breast cancer ( TNBC).Results rs2046210(6q25.1), rs2981582(EGFR2), rs889312(MAP3K1)had no statistical differences between the case group and the control group(P=0.421, 0.459, and 0.468), but the genotype of rs3803662(TOX3/TNRC9)in the case group and the control group had statistical difference (P=0.037).The allelic frequencies of rs3803662 between the case group and control group were different in codominant inheritance ( OR=2.19, 95%CI:1.19-4.02)and recessive genetic models (OR =2.06,95% CI:1.15 -3.70).Compared with AA and GA, GG in-creased the risk of breast cancer ( P =0.012, 0.015 ).The genotypes of rs2046210 ( 6q25.1 ), rs2981582 (EGFR2), rs889312(MAP3K1), and rs3803662(TOX3/TNRC9)had no difference in different types of breast cancer.Conclusions Four common breast cancer susceptibility loci from GWAS are not entirely associated with breast cancer risk among the Han nationality in Henan province .Only rs3803662(TOX3/TNRC9)is confirmed to increase the risk of breast cancer .Different genotypes of 4 loci distribute equally in different types of breast cancer .
4.Research progress of ionizable lipid nanoparticles for siRNA delivery
Ya-nan ZHAO ; Wei HE ; Quan-lin SHAO ; Hua-yu LIU ; Ming-qi LIU ; Ran MO
Acta Pharmaceutica Sinica 2023;58(8):2292-2299
Small interfering RNA (siRNA) is the initiator of RNA interference and inhibits gene expression by targeted degradation of specific messenger RNA. siRNA-mediated gene regulation has high efficiency and specificity and exhibits great significance in the treatment of diseases. However, the naked or unmodified siRNA has poor stability, easy to degrade by nuclease, short half-life, and low intracellular delivery. As an emerging non-viral nucleic acid delivery system, ionizable lipid nanoparticles play an important role in improving the druggability of siRNA. At present, one siRNA drug based on ionizable lipid nanoparticles has been approved for the treatment of rare disease. This review introduces the research progress in ionizable lipid nanoparticles for siRNA delivery, focusing on the effect of each component of lipid nanoparticles on the efficiency of siRNA-mediated gene silencing, which provides new references for the studies on ionizable lipid nanocarriers for siRNA delivery.
5.Neurobehavioral function of neonatal mice following excitotoxic brain damage.
Zhi-Ye QI ; Xiang-Ying HE ; Qi LI ; Ya-Xiong MO ; Kun LIANG
Chinese Journal of Contemporary Pediatrics 2009;11(3):191-193
OBJECTIVETo assess the changes of neurobehavioral function in a neonatal mouse model of excitotoxic brain damage.
METHODSFifty-five 5-day-old ICR neonatal mice were randomly assigned to three groups: blank (no intravenous) control (n=20), saline control (n=20) and excitotoxic brain damage model (ibotenic acid treatment, n=15). Behavioral function was evaluated by the surface righting reflex test (postnatal days 6-10), the swimming test (postnatal days 8-12) and the Y-maze discrimination learning test (postnatal days 33-34).
RESULTSRighting time in the surface righting reflex test in the ibotenic acid treatment group on postnatal days 6-10 was more prolonged than that in the two control groups (p<0.05). Swimming test scores in the ibotenic acid treatment group were significantly lower than those in the two control groups (p<0.05). In the Y-maze discrimination learning test, the mice from the ibotenic acid treatment group performed significantly worse than two control groups, presenting with increased learning times (19.79+/-2.42 vs 16.29+/-2.48 or 16.30+/-2.37; p<0.05) and achieving a lower correct percentage (86.7% vs 96.5% or 95.0%) (p<0.05).
CONCLUSIONSThe developmental reflexes and learning and memory functions were impaired in neonatal mice following excitotoxic brain damage. Behavioral testing is useful in the evaluation of early developmental reflexes and long-term neurobehavioral outcome in neonatal mice with excitotoxic brain damage.
Animals ; Animals, Newborn ; Behavior, Animal ; drug effects ; Brain ; drug effects ; Excitatory Amino Acid Agonists ; toxicity ; Female ; Ibotenic Acid ; toxicity ; Male ; Maze Learning ; drug effects ; Mice ; Mice, Inbred ICR ; Swimming
6.Mechanism of PC12 cell differentiation induced by total salvianolic acid
Yang SHEN ; Qi ZHANG ; Jia-Qi ZHAO ; Ya-Juan TIAN ; Qin-Qing LI ; Shi-Feng CHU ; Wen-Bin HE
Chinese Journal of Pharmacology and Toxicology 2018;32(2):99-104
OBJECTIVE To study the differentiation of PC12 cells induced by total salvianolic acid (Tsa) and the mechanism. METHODS MTT assay was used to detect the effect of Tsa 0.01, 0.1 and 1.0 μg·L-1on proliferation of PC12 cells and on the cells damaged by oxygen and glucose deprivation (OGD).The number of projections of PC12 cells was statistically analyzed.Western blotting was applied to detect the levels of microtubule-associated protein2 (MAP-2), extracellular signal-regulated kinase1/2 (ERK1/2), phosphorylated ERK1/2(p-ERK1/2), mitogen-activated protein kinase kinase1/2(MEK1/2) and p-MEK1/2 proteins.MEK inhibitor U0126 was examined for its effect on expressions of p-ERK1/2 and ERK1/2 protein in PC12 cells induced by Tsa 1.0 μg·L-1.RESULTS Compared with normal control group, Tsa 1.0 μg·L-1could promote PC12 cell proliferation, and the survival rate was increased by 90%, but the survival rate of PC12 cells was not affected by Tsa 0.01 or 0.1 μg·L-1. Compared with OGD injured group,PC12 cells injured by OGD could be repaired by Tsa 0.1 or 1.0 μg·L-1,and the survival rate was increased to (47.7±1.8)% and (63.2±13.0)%, respectively (P<0.05, P<0.01). Compared with normal control group,Tsa 0.01,0.1 and 1.0 μg·L-1could promote the growth of PC12 cell projections (P<0.01). Western blotting results showed that Tsa could promote the expressions of MAP-2, p-ERK1/2 and p-MEK1/2 proteins, and this effect could be blocked by U0126 inhibitor (P<0.01). CONCLUSION Tsa can induce the proliferation and differentiation of PC12 cells, the mechanism of which is possibly the activation of p-MEK and p-ERK1/2.
7.The rheology properties of common hydrophilic gel excipients.
Yan-Long HOU ; He-Ran LI ; Ya-Nan GAO ; Yan WANG ; Qi-Fang WANG ; Lu XU ; Zhen-Yun LIU ; Hong-Tao CHEN ; San-Ming LI
Acta Pharmaceutica Sinica 2014;49(8):1181-1187
To investigate theological properties of common hydrophilic gel excipients such as Carbopol based on viscosity, the viscosity was determined by rotation method and falling-ball method. Linear regression was made between ln(eta) and concentration, the slope of which was used to explore the relation between viscosity and concentration of different excipients. The viscosity flow active energy (E(eta)) was calculated according to Arrhenius equation and was used to investigate the relation between viscosity and temperature of different excipients. The results showed that viscosities measured by two methods were consistent. Concentration of guargum (GG) and hydroxypropylmethyl cellulose (HPMC) solution had a great influence on the viscosity, k > 5; while concentration of polyvinylpyrrolidone-K30 (PVP-K30) and polyethylene glycol 6000 (PEG6000) exerted a less effect on viscosity, k < 0.2; viscosity flow active energy of different excipients were close, which ranged from 30 to 40 kJ x mol(-1). Therefore, theological properties study could provide the basis for application of excipients and establish a foundation for the research of relation between excipients structure, property and function.
Excipients
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chemistry
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Gels
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chemistry
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Polyethylene Glycols
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chemistry
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Polyvinyls
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chemistry
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Povidone
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chemistry
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Rheology
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Temperature
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Viscosity
8.The construction of a novel recombinant virus Δ67R-RGV and preliminary analyses the function of the 67R gene.
Xing HUANG ; Chao PEI ; Li-Bo HE ; Qi-Ya ZHANG
Chinese Journal of Virology 2014;30(5):495-501
The Rana grylio virus (RGV) is a member of the genus Ranavirus. It belongs to the family Iridoviridae, and contains the gene 67R encoding dUTPase. In order to investigate the function of 67R in the replication and infection of RGV, we constructed Δ67R-RGV, a recombinant virus with deletion of 67R. First, we constructed the plasmid pGL3-67RL-p50-EGFP-67RR which carried an enhanced green fluorescence gene (EGFP) as a selectable marker. After homologous recombination between pGL3-67RL-p50-EG- FP-67RR and the RGV genome, Epithelioma papulosum cyprini (EPC) cells were infected with the resulting mixture. Through ten successive rounds of plaque isolation via EGFP selection, all plaques emitted green fluorescence, and finally Δ67R-RGV was generated. Total DNA of Δ67R-RGV infected cells was extracted for PCR analyses. Simulateously, mock infected and wild-type RGV (wt-RGV) infected cells were used as a comparison. Results showed that 67R could be detected in wt-RGV infected cells, but that only the EGFP gene was detected in Δ67R-RGV infected cells. Furthermore, one-step growth curves of wt-RGV and Δ67R-RGV were similar. Therefore, 67R and its encoding product dUTPase might not be essential for the growth of RGV. These results suggest that, homologous recombination and recombinant rana- virus could be used to study the gene function of viruses in aquatic animals.
Genes, Viral
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physiology
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Genome, Viral
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Polymerase Chain Reaction
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Pyrophosphatases
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genetics
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Ranavirus
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genetics
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Recombination, Genetic
9.Job satisfaction and its influential factors in oil production workers.
Ya-hui HE ; Xian-hai MENG ; Shan-fa YU ; Xiu-ying QI
Chinese Journal of Industrial Hygiene and Occupational Diseases 2008;26(3):161-164
OBJECTIVETo investigate the job satisfaction and its influential factors in oil production workers.
METHODS423 oil production workers were investigated using the Occupational Stress Instrument.
RESULTSThe job satisfaction, job organization satisfaction, job itself satisfaction in the workers aged < 30 years old (45.69 +/- 10.98, 22.63 +/- 6.16, 23.07 +/- 5.39 respectively) were lower than those in workers aged > or = 30 years old (49.34 +/- 10.12, 24.60 +/- 5.40, 24.74 +/- 5.36 respectively) (P < 0.01). The job satisfaction in the groups of different service length was significantly different. The job satisfaction in the workers of service length 5-10 years was the lowest compared with those of service length < 5 years and > 10 years (P < 0.05). The gender, education, marriage did not show obvious influence on the job satisfaction. The relationship between psychological health, work locus of control, coping strategies, affective balance and social support showed a statistical significance difference (P < 0.01). Regression was analyzed by taking job satisfaction as strain and personal characters, occupational stress factors, coping as independent variables. Five variables entered regression equation. They were work locus of control, affective balance, social support, psychological health and coping strategies.
CONCLUSIONThe job satisfaction of oil production workers is affected by multiple factors such as the age, work length and social support.
Adult ; China ; Cross-Sectional Studies ; Extraction and Processing Industry ; Female ; Humans ; Job Satisfaction ; Male ; Middle Aged ; Petroleum ; Surveys and Questionnaires ; Young Adult
10.Hipbone biomechanical finite element analysis and clinical study after the resection of ischiopubic tumors.
He YA-QI ; Zhang XUE-LIN ; Tang BING-HANG ; Yang ANG
Chinese Medical Sciences Journal 2012;27(3):153-160
OBJECTIVETo investigate the changes of hipbone biomechanics after the resection of ischiopubic tumors and their relationships with the complications in the convalescent stage, and directing the postoperative pelvic reconstruction.
METHODSDICOM data were used to create an intact hipbone finite element model and postoperative model. The biomechanical indices on the same region in the two models under the same boundary condition were compared. The differences of displacement, stress, and strain of the two models were analyzed with statistical methods.
RESULTSThe distribution areas of the hipbone nodes' displacement, stress, and strain were similar before and after the simulated operation. The sacroiliac joint nodes' displacement (P=0.040) and strain (P=0.000), and the acetabular roof nodes' stress (P=0.000) and strain (P=0.005) of two models had significant differences, respectively.But the sacroiliac joint nodes' stress (P=0.076) and the greater sciatic notch nodes' stress (P=0.825) and strain (P=0.506) did not have significant differences.
CONCLUSIONSThe resection of ischiopubic tumors mainly affect the biomechanical states of the homolateral sacroiliac joint and acetabular roof. The complications in the convalescent stage are due to the biomechanical changes of the sacroiliac joint and the acetabular roof and disappearances of the stabilization and connection functions of the pubic symphysis and superior ramus of pubis.
Acetabulum ; physiopathology ; Biomechanical Phenomena ; Finite Element Analysis ; Humans ; Pelvic Bones ; physiopathology ; Pelvic Neoplasms ; physiopathology ; surgery ; Sacroiliac Joint ; physiopathology