2.Studies on the thermal decomposition process and kinetics of purine drugs.
Jian ZHANG ; Rui-long SHENG ; Wen-peng MAI
Acta Pharmaceutica Sinica 2002;37(8):644-648
AIMTo study the thermal stability, decomposition process and kinetics of such purine pharmaceuticals as aciclovir (Acv), penciclovir (Pcv), and their parent substance, guanine.
METHODSUsing infrared technique, accelerating test method and thermogravimetry to investigate the thermal decomposition processes and using Coast-Redfern method, MKN method and Ozawa method to deal with the data to get kinetic functions.
RESULTSThe decomposition process and the formed products were derived, the kinetic model function was suggested by comparison of the kinetic parameters.
CONCLUSIONPcv and Acv's degrading product for the first step is guanine. The sequences of their thermal stabilities is: Pcv > Acv. The two drugs' kinetic equation of thermal decomposition is expressed as: da/dt = Ae-Ea/RT2(1-alpha)3/2.
Acyclovir ; analogs & derivatives ; chemistry ; Drug Stability ; Guanine ; chemistry ; Hot Temperature ; Kinetics ; Thermodynamics ; Thermogravimetry
3.Experimentally investigating the effect of buccal acupuncture on analgesic time-effect characteristics and monoamine neurotransmitters
Rui-Sheng PU ; Xiao-Li FANG ; Wang-Jun JIE ; Ding-Long LIU ; Cheng-Hong SU ; Yan-Ping YANG
Journal of Acupuncture and Tuina Science 2018;16(4):229-235
Objective:To investigate the analgesic time-effect characteristics and changes in concentrations of rabbit's hypothalamic 5-hydroxytryptamine (5-HT) and noradrenaline (NE) caused by buccal acupuncture in the rheumatoid arthritis (RA) rabbits,and to reveal the analgesic central mechanism of buccal acupuncture,thereby providing a theoretical basis for the treatment of pain by buccal acupuncture.Methods:Forty rabbits were randomly divided into a normal group,a model group,a body acupuncture group,and a buccal acupuncture group,with 10 rabbits in each group.No model was established in the normal group,while equal dose of normal saline was injected at the matched site and time point;rabbits in other groups were subjected to the establishment of RA models using egg protein.From the 27th day of the experiment,rabbits in each group received the designated intervention.Rabbits in the normal group and the model group were fixed for 30 min every day using the same method as those in the other groups.In the acupuncture group,Dubi (ST 35) and Zusanli (ST 36) on bilateral hind limbs were selected.Perpendicular needling (using the needles with 0.25 mm in diameter and 25 mm in length) was performed with twirling manipulation for 15 s at intervals of 5 min.The needles were retained for 30 min and acupuncture was performed once a day.In the buccal acupuncture group,the knee point in the buccal acupuncture and needles with a diameter of 0.25 mm and a length of 15 mm were selected.Oblique needling was performed with twirling manipulation for 15 s at intervals of 5 min.The needles were retained for 30 min and acupuncture was performed once a day.The thermal pain thresholds at the 0,5,15,30,60,120 and 240 min after the 1st and 10th acupuncture therapy were measured with a PL-200 thermal-inducing pain meter.After the 10th acupuncture therapy,rabbit's hypothalamus was removed,and the 5-HT and NE concentrations in the hypothalamus at the peak point of the acupuncture pain threshold curve were determined by high performance liquid chromatography (HPLC).Results:The analgesic effect was obvious at 5 min after buccal acupuncture started,peaked at 30 min,and decreased to the lowest value at 240 min.Rabbits in the body acupuncture group began to show significant analgesic effect at 15 min,which was peaked at 30 min,and began to decline at 60 min.The pain threshold at 240 min was still higher than that at 0 min.Compared with the model group,the concentrations of hypothalamic 5-HT in the buccal acupuncture group and the body acupuncture group was significantly increased,and the between-group differences were statistically significant (both P<0.05).The NE/5-HT ratios in hypothalamus in the buccal acupuncture group and the body acupuncture group were significantly lower than the ratio in the model group,and the differences were statistically significant (both P<0.05);difference in the decrease was statistically significant between the buccal acupuncture group and the body acupuncture group (P<0.05).Conclusion:The analgesic effect of buccal acupuncture shows an obvious time-dependent curve.It is characterized by rapid onset of pain relief,rapid increase and decline in pain threshold.5-HT and NE levels in rabbit's hypothalamus can be affected by buccal acupuncture,with increased 5-HT concentration and reduced NE/5-HT ratio.
4.Study on the relationship between serum cytokeratin 19 level in hepatocellular carcinoma patients and the clinico-pathologic characteristics.
Yan LI ; Zhao-you TANG ; Bo TIAN ; Lun-xiu QIN ; Sheng-long YE ; Rui-xia SUN
Chinese Journal of Hepatology 2004;12(6):341-342
OBJECTIVEAs our previous comparative proteomics study on high and low metastasis human hepatocellular carcinoma (HCC) cell strains revealed that cytokeratin 19 (CK19) was related to higher metastasis potential, we further investigated the relationship between serum CK19 level in HCC patients and their clinico-pathologic characteristics.
METHODSSerum CK19 levels of 101 normal controls and 108 pathology-proven HCC patients were determined using radioimmunoassay, and the their correlation with clinico-pathologic parameters were studied.
RESULTSThe upper limit of one-side 98% confidence interval of normal serum CK19 level was 2.3 microg/L. Among 108 HCC patients, 24 (22.2%) had increased serum CK19 level, ranging from 2.4 to 45.5 microg/L. There were 12 patients (11.1%) with increased CK19 level but normal AFP level. The percentage of poor differentiated tumor was higher in CK19 increased cases (37.5%, 9/24) than in CK19 normal cases (20.2%, 17/84). Moreover, the presence of portal vein tumor emboli was significantly higher in CK19 increased cases (25.0%, 6/24) than in CK19 normal cases (6.0%, 5/84). (Chi-square = 7.403, P < 0.01) In addition, the percentage of TNM stage III/IV tumor was significantly higher in CK19 increased patients (54.2%, 13/24) than in CK19 normal cases. (chi-square = 13.300, P < 0.005)
CONCLUSIONSome HCC patients do have increased serum CK19 level, which could be related to portal vein tumor emboli, poor tumor differentiation and advanced tumor stages.
Adult ; Aged ; Biomarkers, Tumor ; blood ; Carcinoma, Hepatocellular ; blood ; pathology ; Female ; Humans ; Keratins ; blood ; Liver Neoplasms ; blood ; pathology ; Male ; Middle Aged ; Neoplasm Proteins ; blood ; Peptide Fragments ; blood ; genetics ; Proteome ; analysis
5.Analysis of differential gene expression in rat hepatic stellate cells activated by culture or hepatocellular carcinoma cell induction.
Yun-hong XIA ; Zheng-ji SONG ; Rong-xin CHEN ; Sheng-long YE ; Rui-xia SUN ; Qiong XUE
Chinese Journal of Oncology 2009;31(3):164-169
OBJECTIVEHepatic stellate cells (HSC) in hepatocellular carcinoma (HCC) transdifferentiate into extracellular matrix-producing myofibroblasts. Activated HSC can promote invasion and metastasis of HCC. To understand the differences of HSC in normal liver and HCC, we compared the gene expression patterns in HCC cell induction-activated and culture-activated rat HSC.
METHODSHSC were isolated by density centrifugation and exposed to conditioned medium from rat HCC cell line C5F. Expression of 22 012 genes in quiescent HSC, culture-activated HSC and HCC induction-activated HSC was analyzed by cDNA microarray and confirmed by real-time RT-PCR and Western blot.
RESULTS1672 genes were differentially expressed in culture-activated HSC, including proinflammatory factors, cell adhesion molecules, cell surface receptors, signaling transduction molecules and immune factors. 711 genes were differentially expressed in HCC induction-activated HSC. Some of them were identical to those in culture-activated HSC. HCC Induction-activated HSC showed specific gene expression patterns, including Raf1, Rac2, Adam17, Wnt6, MMP-9 and TNF, suggesting that HCC cells can specifically induce HSC activation.
CONCLUSIONThe gene expression patterns in HCC induction-activated HSC are different from those in culture-activated HSC. HCC induction-activated HSC may play a major role in the invasion and metastasis of HCC. In vivo activation should be considered as the standard for the study of HSC biology. HCC induction-activated HSC should be considered as the standard for HSC biology studies.
Animals ; Carcinoma, Hepatocellular ; metabolism ; pathology ; Cell Line, Tumor ; Cells, Cultured ; Gene Expression Profiling ; Gene Expression Regulation, Neoplastic ; Hepatic Stellate Cells ; metabolism ; pathology ; Liver Neoplasms ; metabolism ; pathology ; Male ; Oligonucleotide Array Sequence Analysis ; Rats ; Rats, Inbred F344
6.Advances in research on tumor targeted therapy of trastuzumab
Sheng-Long GU ; Rui ZHAO ; Miao-Fa YING ; Ming-Xing LI
Basic & Clinical Medicine 2018;38(5):722-726
Trastuzumab is a humanized monoclonal antibody that targets at human epidermal growth factor receptor 2(Her2)proto-oncogenes,which can act on Her2 over-expression of tumor cells,inhibits tumor cells proliferation, differentiation,migration and other physiological activities,reduces the risk of tumor metastasis and extend the sur-vival time of patients.
7.Effects of liver-soothing heat-clearing and spleen-fortifying method on the ex-pressions of cerebral bax and bcl-2 in rats with generalized anxiety disease
Ning DONG ; Qi-Sheng TANG ; Rui-Zhen ZHAO ; Bin LUO ; Wen-Long WANG
Journal of Beijing University of Traditional Chinese Medicine 2015;(6):383-387
Objective To explore the effects of liver-soothing heat-clearing and spleen-fortifying method on the expressions of bax and bcl-2 in cerebral Papez’ s circuit in rat with generalized Anxiety Disease ( GAD) . Methods A total of 40 male Wistar rats were divided into normal group, model group, treat-ment group, and control group, with 10 rats in each group. GAD model was established by using the stimulation of uncertain empty drinking bottle. Then the treatment group and control group were intragas-trically given Danzhi Xiaoyao San ( Cortex Moutan and Fructus Gardeniae Free Wanderer Powder ) and Buspirone Hydrochloride once a day for 7 consecutive days respectively. The model group was given dis-tilled water once a day for a week. The expressions of bax and bcl-2 in rat hippocampus and mamillary
body were measured by applying western blot assay after resecting rat brains. Results The expression of bax in hippocampus and mamillary body of model group increased significantly compared with normal group ( P<0 . 05 or P<0 . 01 ) and the expression of bcl-2 decreased markedly ( P<0 . 01 ) . Compared with model group, the level of bax in hippocampus and mamillary body of treatment group and control group was reduced ( P<0 . 05 or P<0 . 01 ) and the level of bcl-2 increased significantly ( P<0 . 05 or P<0 . 01 ) . Conclusion The therapeutic method of liver-soothing heat-clearing and spleen-fortifying method represented by Danzhi Xiaoyao San could reduce the level of bax in hippocampus and mamillary body of GAD rat brain, elevate the level of bcl-2 and reduce bax/bcl-2, prevent and inhibit cell apoptosis in Papez’ s circuit and then ameliorate anxiety symptoms.
8.Stimulatory Effect of Chemokine-like Factor 1 (CKLF1) on the Growth of Bone Marrow Cells
Wen-Ling HAN ; Min RUI ; Ying-Mei ZHANG ; Ying-Yu CHEN ; Ying-Cheng ZHONG ; Chun-Hui DI ; Quan-Sheng SONG ; Da-Long MA
Acta Academiae Medicinae Sinicae 2001;23(2):119-122
To investigate the activity of CKLF1 on the proliferation and differentiation of bone marrow cells. Methods Human low density bone marrow cells and mouse bone marrow cells were plated in 96-well microplate and supernatants from transfected COS-7 cell culture were added. The cell proliferation was assayed by MTT method after 5 days incubation. The enhancing effect of CKLF1 on the colony forma tion of human hematopoietic progenitor cells was identified in semi-solid culture. Results CKLF1 has obvi ous enhancing effect on both human and mouse bone marrow cells, it can stimulate the colony formation of human hematopoietic stem cells and has synergistic action with GM-CSF. Conclusion CKLF1 can pro mote the proliferation and differentiation of bone marrow cells.
9.The investigation of the technology of microcell mediated chromosome transfer for functional localization of metastasis suppressor genes for liver cancer on human chromosomes.
Hu LIU ; Sheng-long YE ; Jiong YANG ; Zhao-you TANG ; Yin-kun LIU ; Lun-xiu QIN ; Shuang-jian QIU ; Rui-xia SUN
Chinese Journal of Medical Genetics 2006;23(5):540-543
OBJECTIVEIn order to seek the functional evidence that there could be metastatsis suppressor gene for liver cancer on human chromosomes, the objective of this study is to establish a method of microcell mediated chromosome transfer (MMCT).
METHODSHuman chromosome 8 randomly marked with neo gene was introduced into highly metastatic rat liver cancer C5F cell line by treating the single human chromosome donor cells with sequential steps of micronucleation, enucleation and microcell fusion. Double selections of G418 and HAT were applied to screen positive microcell hybrids, which were cloned by single cell isolation. Microcell hybrid clones were confirmed by STS-PCR and WCP-FISH.
RESULTSMicrocell hybrids resistant to HAT and G418 were obtained, from which 15 clones were obtained by single-cell isolation cloning. STS-PCR and WCP-FISH proved that human chromosome 8 had been successfully introduced into rat liver cancer cell line C5F. The human chromosome 8 introduced into C5F was found to have random loss of chromosome fragments by STS-PCR and consistent recombination with rat chromosome by WCP-FISH.
CONCLUSIONThe successfulls introduction of human chromosome into highly metastatic rat liver cancer cell line has established the technical basis for functional localization of metastasis suppressor gene(s) for liver cancer on human chromosomes.
Animals ; Cell Line, Tumor ; Chromosome Mapping ; methods ; Chromosomes, Human, Pair 8 ; genetics ; Genes, Tumor Suppressor ; Genetic Techniques ; Humans ; In Situ Hybridization, Fluorescence ; Liver Neoplasms ; genetics ; pathology ; Polymerase Chain Reaction ; Rats
10.Relationship between DLC-1 expressions and metastasis in hepatocellular carcinoma.
Li-jie SONG ; Sheng-long YE ; Kai-feng WANG ; Yong-qiang WENG ; Chun-min LIANG ; Rui-xia SUN ; Yan ZHAO ; Yin-kun LIU ; Zhao-you TANG
Chinese Journal of Hepatology 2005;13(6):428-431
OBJECTIVESTo study the relationship between the expression level of DLC-1 mRNA (located in 8p) and the invasion/metastasis of human hepatocellular carcinoma (HCC).
METHODSFifty-one surgical specimens of human HCC were divided into high-invasive and low invasive groups according to their clinicopathological features. DLC-1 mRNA expression was studied in the 51 HCC specimens as well as 5 different metastasis potential cell lines using real-time quantitative PCR (RQ-PCR).
RESULTSThe expression level of DLC-1 mRNA in HCC specimens with high invasiveness was significantly lower than that with low invasiveness (P < 0.05). The expression levels of DLC-1 mRNA were significantly different between non-metastatic (Hep3B and HepG2) and metastatic (MHCC97-H, MHCC97-L and HCCLM3) cell lines (P < 0.05). From MHCC97-L to HCCLM3, with an increase of invasiveness and metastatic potentials, the expression level of DLC-1 decreased correspondingly, and its expression level in HCCLM3 was significantly lower than that in MHCC97-L (P < 0.01).
CONCLUSIONThe expression of DLC-1 mRNA may play an important role in inhibiting the invasiveness and metastasis of HCC.
Carcinoma, Hepatocellular ; metabolism ; pathology ; Cell Line, Tumor ; GTPase-Activating Proteins ; Gene Expression Regulation, Neoplastic ; Humans ; Liver Neoplasms ; metabolism ; pathology ; Mutagenesis, Site-Directed ; Neoplasm Metastasis ; Neoplasm Recurrence, Local ; RNA, Messenger ; biosynthesis ; genetics ; Tumor Suppressor Proteins ; biosynthesis ; genetics