1.Progress in biomarkers of non-small cell lung cancer for individualized treatment
Chinese Journal of Pharmacology and Toxicology 2016;30(4):375-380
Biomarkers of non-small cell lung cancer(NSCLC)can facilitate an efficient diagnosis, improve therapeutic effects,reduce the side effects of other treatments,ameliorate prognosis and predict relapse of the disease and drug resistance. This paper summarized the biomarkers which were newly discovered and their functions in clinical practices in order to guide individualized treatment and help adjust treatment. The exploration of biomarkers of NSCLC will become a priority in future research.
2.The inhibitory effect of 3', 5'-cCMP on the production of human interleukin-2 and the expression of interleukin-2 receptors in vitro
Chinese Journal of Pathophysiology 1989;0(05):-
0.2mM Cytidine 3', 5'-monophosphate (3', 5'-cCMP) inhibits not only the IL-2 production of human peripheral blood mononuclear cells (PBMC) but also the expression of IL-2 receptors. The inhibitory rate on expression of IL-2 receptors is 28.9+1.9%. The proliferation of CTLL-2 cells can be stimulated by 3', 5'-cCMP in concentration from 0.00625mM to 0.2mM when the presence of IL-2 is sufficient. The stimulative effect in low concentration of 3', 5'-cCMP is more obvious than that in high concentration.
3.Effect of Atorvastatin on Cardiac Function and Plasma C-reactiveprotein and Uric Acid Elevels in Patients Ischemic Cardiomyopathy
Journal of Medical Research 2006;0(10):-
Objective To study the effects of atorvastatin on ischemic cardiomyopathy patients with chronic heart failure and to investigate the changes of serum levels of CRP and serum levels of uric acid after treatment.Methods Fifty patients with ischemic cardiomyopathy(NYHAgradeⅡ~Ⅳ) were randomly divided into two groups: the therapy group received atorvastatin 10mg/d(n=25) for 4 weeks and the control group received placebo(n=25).In addition,20 healthy peoples were observed.Before and after treatment,the parameters of plasma uric acid,serum CRP and cardiac function evaluated by echocardiogram were measured.Results After 4 weeks,patients receiving atorvastatin exhibited a modest reduction in serum CRP and serum uric acid compared with control group(P
4.Roles of miR-494 in tumors
Mingchun LI ; Aibing WU ; Zhixiong YANG
Journal of International Oncology 2013;40(10):726-729
MiR-494 involves in cell cycle regulation,differentiation and apoptosis processes of normal ceils.Recent study shows that abnormal expression of miR-494 is associated with oncogenesis closely,and it participates in the invasion and metastasis of tumor cells and so on.MiR-494 is not only a tumor suppressor gene,but also can be considered as a cancer-promoting gene.MiR-494 can regulate the oncogenesis and development of the tumor through a variety of target genes and signaling pathways.
5.Chronopharmacokinetics of gefitinib and its mechanisms in tumor-bearing nude mice
Le WANG ; Changjiao LIU ; Mingchun LI
Chinese Journal of Pharmacology and Toxicology 2016;(2):144-150
OBJECTIVE To investigate the effect of the dosing time on the pharmacokinetics of gefitinib and its potential mechanism. METHODS Female BALB/c nude mice were housed under standardized 12 h light/dark circadian conditions(light on at 7:00,off at 19:00)for two weeks before a non-small cell lung cancer(NSCLC)model was established. Two weeks later,they were divided into 2 groups(8:00,20:00)randomly. Gefitinib was orally administered at the dose of 1 mg · kg-1 to the mice in each group at 8:00 or 20:00,respectively. Blood was collected at 10 different time points after each administration. Livers were collected every 4 h during the 24 h period from the non-administrated nude mice of NSCLC model. The plasma concentration of gefitinib was determined through an HPLC-MS/MS and the parameters were calculated by WinNonlin 6.3. The total RNA was extracted from livers,purified, synthesized to cDNA that was subjected to qRT-PCR analysis for mRNA expression levels of cyto?chrome P450 enzymes(Cyp)3a11,Cyp3a13,pregnane X receptor(PXR)and constitutive androstane receptor (CAR). RESULTS The area under the plasma concentration-time curve (AUC) and mean residence time (MRT) of 8:00 administration group were higher than those of 20:00 administration group(P<0.05). The clearance(Clz/F) of 8:00 administration group was lower than that of 20:00 administration group(P<0.05). The mRNA expression levels of PXR and CAR were consistent with those of Cyp3a11 and Cyp3a13. CONCLUSION Circadian rhythm exists in the pharmacokinetics of gefitinib and it may be closely related to CYP3A and its regulator genes.
6.Study on the transfection of dextran derivative nanoparticles to the mda-mb-435 human breast cancer cells
Mingchun LI ; Dongsheng LIANG ; Youwei LI ; Li LIU
Chinese Pharmacological Bulletin 2003;0(08):-
Aim To prepare the dextran derivative nanoparticles with higher transfecting efficiency to mda-mb-435 human breast cancer cells.Methods The dextran 40 and the sodium periodate were reacted with different mole ratio to form the intermediate:oxidized dextrans having different aldehyde content.With different reactants matching,the spermine were grafted onto the oxidized dextrans mentioned above to form the dextran-spermine imine conjugates which were reduced by the excess reducing agent NaBH4 to produce the end products 9 species of dextran derivative nanoparticles(extran-spermine amine conjugates).The dextran derivative nanipartical of the highest gene transfecting efficiency was selected from the 9 species of dextran derivative nanoparticles by the experiment of gene transfection,using the pEGFP-C1 plasmid as the reporter,the mda-mb-435 human breast cancer cells as the transfected cells.Results The dextran derivative nanoparticles with the highest transfecting efficiency was the one that had the highest content of spermine grafted onto the oxidized dextran40 obtained by the reaction between sodium periodate and dextran40 with the mole ratio of 0.8.Conclusion The dextran derivative nanoparticles of the highest transfecting efficiency to the mda-mb-435 human breast cancer had been prepared.
7.Study of Effective Substances Screening for Panax Notoginseng Based on Spectrum-effect Relationship
Xu LIU ; Xiao LI ; Xiaobo CUI ; Mingchun LI
China Pharmacist 2016;19(2):205-209
Objective:To investigate the protective effects of Panax notoginseng on myocardial ischemia injury in dogs and study the spectrum-activity relationship of Panax notoginseng. Methods:Firstly, the HPLC fingerprint analytical method for Panax notogin-seng was established, and then the dog model of acute myocardial ischemia was established by left anterior descending coronary liga-tion. Bivariate correlation analysis and multivariate regression analysis were used to correlate the spectrum-activity relationship between the fingerprints and the anti-myocardial ischaemia activity, and the spectrum-activity relationship and efficacy material foundation of Panax notoginseng were determined. Results:The main effective components were Ginseng saponin Rg1 and Rb1 and notoginseng sapo-nins R1 etc. Notoginseng saponins R1 could significantly inhibit the increase of serum lactate, and ginseng saponin Rg1 could inhibit the increase of FFA in serum, which was the main component in Panax notoginseng for the treatment of myocardial ischemia. Conclusion:The effective substances in Panax notoginseng are obtained by investigating the relationship between the spectrum and efficiency, and a new method for the evaluation of spectrum-activity relationship for Panax notoginseng is established. It can objectively reflect the inher-ent quality of the drug and provide a new strategy for the further research of traditional Chinese medicines.
8.Chronopharmacokinetics of erlotinib in tumor-bearing mice
Jiao LIU ; Mingchun LI ; Peipei WANG ; Bin ZHANG
Chinese Journal of Pharmacology and Toxicology 2014;(3):403-407
OBJECTIVE To investigate the effect of the dosing time on the pharmacokinetics oferlotinib.METHODS Female C57BL mice were contained under standardized 12h light/dark circadianconditions (lights on at 7:00,off at 19:00)for 3 weeks and randomly assigned into six groups.Erlotinibhydrochloride was orally administrated to the mice in each group at 8:00,12:00,16:00,20:00,24:00and 4:00,respectively.Blood was drawn from the eyeballs of the mice at 12 different time points aftereach administration.The plasma concentration of erlotinib was determined through a high-performanceliquid-chromatographic assay and the parameters were calculated by WinNonlin. RESULTSThe area under curre (AUC)and mean residence time (MRT)of these groups were apparently differ-ent.AUC0 ~24 h and MRT0 ~24 h were the lowest in the 20:00 administration group as compared to othergroups (P<0.01 ).Tmax of the 20:00,24:00 and 4:00 groups was apparently higher than that of the8:00 and 12:00 groups (P<0.01 ).The clearance of the light phase groups was lower than that of thedark phase groups (P<0.01 ),with the highest in the 20:00 group.The peak value of cmax appeared inthe 12:00 group and the lowest in the 20:00 group (P<0.01 ).CONCLUSION Circadian rhythm playsa critical role in pharmacokinetics of erlotinib in mice.
9.Comparison of Steam Distillation and Supercritical CO2 Method in the Extraction of Volatile Constituents from Compound Kuhuang Prescription by GC-MS
Yanqin CHENG ; Qingjie FU ; Zhe ZHANG ; Liyan ZHAO ; Mingchun LI
China Pharmacist 2014;(5):725-728
Objective:To compare the steam distillation( SD) and supercritical CO2 ( SFE-CO2 ) method in the extraction of vola-tile constituents from such 3 traditional Chinese drugs as cnidium monnieri, radix sileris and atractylodes lancea in compound Kuhuang prescription. Methods:Essential oil was extracted from the 3 traditional Chinese drugs by SD and SFE-CO2 method, respectively. The components were identified by GC-MS, and their relative contents were calculated with peak area normalization method. Results:To-tally 36 components were isolated and identified using SD extraction and 31 components were identified using SFE-CO2 extraction, a-mong them, 22 components were the same and their relative molecular weight mainly concentrated within 200-230. Conclusion: SFE-CO2 method can extract effective components from the 3 traditional Chinese drugs in compound Kuhuang prescription with higher selec-tivity, which is the more suitable extraction method for essential oil from the prescription.
10.A Quality Standard Study onQingyan Granule
Yan MA ; Mingchun LI ; Yanwei FU ; Hua ZHANG ; Yanqin CHENG
Chinese Journal of Information on Traditional Chinese Medicine 2015;(1):87-90
Objective To establish the standard for quality control ofQingyan Granule. Methods The chief components of the preparation, Sophora Tonkinensis radix et rhizoma, Adenophorae radix, Lonicera japonica caulis, and Ophiopogonis radix were identified by TLC qualitatively. The contents of licorice glycosides and glycyrrhizic acid were determined by HPLC. The separation was performed on Thermo Syncronis C18 column (4.6 mm×250 mm, 5μm) with mobile phase consisted of acetonitrile with 0.05% phosphoric acid solution (A)-0.05% phosphoric acid solution (B), and gradient elution (0-8 min, 19%A;8-35 min, 19%→50%A). Detection wavelength was 237 nm, and flow rate was 1 mL/min.Results The spots in TLC were clear. There were spots with same color on the corresponding location of reference substance and reference herbal, negative control without interference. The linear range for licorice glycosides was 0.05-0.5μg (r=0.999 9). The average recovery was 99.97%, RSD=1.74% (n=9). The linear range for glycyrrhizic acid was 0.1-2μg (r=0.999 9). The average recovery was 99.74%, RSD=1.28% (n=9). Conclusion The method is simple, accurate, with high reproducibility, which can be used for quality control ofQingyan Granule.