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2018 Vol. 36, No. 2

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Advances in the mechanism of Traditional Chinese Medicine by network pharmacology method
XING Xinrui, LÜ Diya, CHAI Yifeng, ZHU Zhenyu
2018, 36(2): 97-102. doi: 10.3969/j.issn.1006-0111.2018.02.001
Abstract(4640) PDF (673KB)(1155)
Abstract:
Network pharmacology is the basis of system biology, systematically expounded the interaction of the principle and regulation between body and the drug, representing the idea of the modern biomedical philosophy and researching model. It could be more easily understand the mechanism of action of Traditional Chinese Medicine treatment of diseases by the network pharmacology-related technical means. Network pharmacology is widely used in Traditional Chinese Medicine research in the current. The application and development of network pharmacology in the field of Traditional Chinese Medicine research in recent years were introduced in this paper from the aspects of Traditional Chinese Medicine concept, network pharmacology and network pharmacology application.
Clinical application and research progress of apatinib in cancer treatment
GONG Xiaobin, LIU Shiyi, XIA Tianyi, WEI Hua, CHEN Wansheng
2018, 36(2): 103-107,130. doi: 10.3969/j.issn.1006-0111.2018.02.002
Abstract(2891) PDF (682KB)(719)
Abstract:
Antiangiogenic target therapy has been a hot topic in cancer treatment recently. Apatinib is a category 1.1 new medication developed domestically. It effectively inhibits angiogenic and exhibits promising anti-tumor activity in preclinical studies. Apatinib has been successfully applied in clinical trials of multiple malignancies, such as gastric cancer, lung cancer and breast cancer with satisfactory safety and efficacy profile. However, its mechanism of action is still not fully understood. Further researches should be carried on to improve its safety, effectiveness and marketability. This review summarized the mechanism of action, pharmacokinetics, clinical efficacy, safety and biomarkers, discussed the recent progress, hot issues and clinical prospects of apatinib,
Progress of tanshinone ⅡA on the mechanism of inflammatory response after cerebral ischemia
FENG Jingjing, LI Tiejun, ZHANG Yuefan
2018, 36(2): 108-111. doi: 10.3969/j.issn.1006-0111.2018.02.003
Abstract(2671) PDF (655KB)(1044)
Abstract:
Tanshinone ⅡA is a kind of phenanthraquinone derivatives derived from Salvia miltiorrhiza, which is one of the main active components of Danshen to play the protective role of cerebral ischemic injury. Inflammation plays an important role in the pathogenesis of cerebral ischemia. In recent years, much evidence shows that immune cells, adhesion molecules, inflammatory mediators have been involved in the pathogenesis of immune response in the central nervous system through induction or regulation of cerebral ischemia. In this paper, the research progress of mechanism of inflammatory response of tanshinone ⅡA after cerebral ischemia was reviewed, which provided a new idea for the study of the protective mechanism of tanshinone ⅡA in cerebral ischemia.
Synthesis and anti-oxidation activity of schisandrone derivatives
WANG Pengru, LI Wei, PENG Xuemi, ZHENG Wei, GUO Liangjun, JIN Yongsheng
2018, 36(2): 112-115,135. doi: 10.3969/j.issn.1006-0111.2018.02.004
Abstract:
Objective To design and synthesize schisandrone derivatives for the therapy of disease like AD,and to measure their anti-oxidation activity. Methods Ten compounds were synthesized,and seven of them were first reported.The influence all the compounds on SOD from the mouse serum were measured to evaluate anti-oxidation activity.Structure-activity relationship (SARs) were also discussed. Results Compounds 2, 3, 5 and 8 could increase the activity of SOD in mouse serum.Furthermore,Compounds 2, 3 and 5 showed better activities than schisandrone. Conclusion Synthesized schisandrone derivatives showed anti-oxidation activity.The SARs demonstrated the carbonyl of C-1 position and the methyls of C-2 and 3 had no influences to the anti-oxidant activity.
The construction of pharmacophore model for (1,3)-β-D-glucan synthase small molecule inhibitors
JIANG Yanjuan, CUI Lijun, HE Xiaomeng, LIU Na, SHENG Chunquan
2018, 36(2): 116-120. doi: 10.3969/j.issn.1006-0111.2018.02.005
Abstract:
Objective To perform the ligand-based computer-aided drug design and construct the pharmacophore model of (1,3)-β-D-Glucan Synthase (GS) small molecule inhibitors. Method Six small molecules with diverse structures and good inhibitory activity were selected to construct the training set. The HipHop algorithm in Catalyst pharmacophore generation module was utilized to construct the pharmacophore models. The pharmacophore models were evaluated by constructed Decoyset 3D database. Results Pharmacophore 02 has a good enrichment factor, sensitivity and specificity parameters. Pharmacophore model validation with Decoyset 3D database proved that the model has good distinguishing capability. Conclusion The pharmacophore model of GS small molecule inhibitors was constructed and tested. It will provide valuable information for design and discovery of novel small molecule GS inhibitors.
Study on extraction technology of Fuyuan Xingnao granule
SUN Lili, CHEN Zhenyi, QIN Chunxia, HU Xiang, FANG Bangjiang, LI Tiejun
2018, 36(2): 121-125. doi: 10.3969/j.issn.1006-0111.2018.02.006
Abstract(3058) PDF (660KB)(525)
Abstract:
Objective To study the extraction technology and optimize the extraction process of Fuyuan Xingnao granule. Methods The preliminary extraction process was designed by routine extraction method combined with the results of pharmacological activity experiment. The extraction process was optimized with orthogonal test. Results The extract was obtained by ethanol reflux extraction, water decoction extraction or ethanol precipitation followed by filtration and concentration. The optimal process for ethanol reflux extraction was extracting twice with 50% ethanol. The ratio of liquor to dry material was 8:1 for the first time and 6:1 for the second time. The extraction time was 120 minutes for the first time and 80 minutes for the second time. The optimal process for water decoction extraction was extracting twice with 120 minutes and 80 minutes each time. The ratio of liquor to dry material was 10:1 for the first time and 8:1 for the second time. The extraction temperature was100℃. The best ethanol precipitation process was 16 hour extraction with 80% ethanol. The ratio of ethanol to dry material was 2:1. Conclusion The quality of Fuyuan Xingnao granule extract with this optimized extraction process was in line with requirements of Pharmacopoeia of the People's Republic of China 2015, 4 Volumes(0104 granule).
Transient receptor potential type vanilloid 1 regulates EGFR related functions in pancreatic cancer cells
HUANG Jin, LIU Jingxue, ZENG Ying, YUAN Fang
2018, 36(2): 126-130. doi: 10.3969/j.issn.1006-0111.2018.02.007
Abstract:
Objective To evaluate the regulation of the TRPV1 receptor on the expression of EGFR protein and the effects on related cell functions. Methods Human pancreatic cancer cells PANC-1 were cultured and treated by over-expression and siRNA. Cell proliferations were detected by CCK-8 experiment. RT-PCR test was used to detect the expression of oncogenes Akt2 and K-ras. Results EGFR protein was down-regulated by TRPV1 over-expression or by agonist activation in pancreatic cancer cells. EGFR protein was increased by the interference of TRPV1 expression. The proliferation rate of pancreatic cancer cells was decreased and Akt2, K-ras were significantly inhibited by TRPV1 over-expressing. Conclusion The expression of TRPV1 in pancreatic cancer cells regulated the EGFR protein content. The cell proliferation and oncogene expression were inhibited by TRPV1 over-expressing.
Effects of combination therapy with ACEI and aldosterone receptor antagonist on Cys-C and urinary microprotein in patients with hypertensive nephropathy
TANG Huanjun
2018, 36(2): 131-135. doi: 10.3969/j.issn.1006-0111.2018.02.008
Abstract:
Objective To investigate the effects of combination therapy with ACEI and aldosterone receptor antagonist on Cys-C and urinary microprotein regulation. Methods Patients were randomly divided into two groups. The control group received benazepine hydrochloride only. The experimental group received benazepine and spironolactone treatment. The blood pressure, renal function, 24 h urinary protein, Cys-C, GFR, urinary microprotein and the correlation of GFR with Cys-C and urinary microprotein were recorded. Results There was no statistically significant difference between two groups in blood pressure (P>0.05). After treatment, the renal function of the experimental group was significantly improved compared to that of the control group. The 24 h urine protein, Cys-C and urinary microprotein were significantly lower in the experimental group than the control group (P<0.05). GFR was negatively correlated with Cys-C and urinary microprotein. Conclusion The combination therapy of ACEI and aldosterone receptor antagonist can improve renal function and reduce 24 h hematuria. GFR filtration ability was significantly improved with the reduction of Cys-C and urinary microprotein.
Meta-analysis on renal toxicity of vancomycin given by continuous infusion vs intermittent infusion
ZHENG Lili, XUAN Yuanhuan, JIANG Qian, FAN Fangfang, YAO Li, ZHAO Shengjun
2018, 36(2): 136-139,146. doi: 10.3969/j.issn.1006-0111.2018.02.009
Abstract:
Objective To compare the renal toxicity of vancomycin with continuous infusion vs intermittent infusion. Methods The databases of EMBASE, PUBMED, the Cochrane Register of Controlled Trials, CBM, CNKI and WanFang were searched. The Cochrane Revman5.2 software was used for Meta-analysis. Results Two RCTs and eight observational studies were included in the systematic literature search with total of 1 764 patients. 1 037 patients received vancomycin with continuous infusion while 727 patients with intermittent infusion. The Meta-analysis indicated that there was no significant difference in renal toxicity between continuous infusion group and intermittent infusion group(P>0.05). Conclusion Vancomycin continuous infusion cannot effectively reduce the incidence of renal toxicity.
The changes of content and proportion of main components in glycyrrhiza uralensis Fisch under different processing and extraction conditions
LIU Jinghua, LIU Yanan, HU Yingying
2018, 36(2): 140-146. doi: 10.3969/j.issn.1006-0111.2018.02.010
Abstract:
Objective To explore the licorice herbs principal component isomer content and percentage change in different processing and extracting conditions. Methods RP-HPLC method were used with 18 beta glycyrrhizic acid (18β-Gly) and 18 alpha glycyrrhizic acid (18α-Gly) as the basis of evaluation, determination of main components and impurities of licorice pieces, effects of processing temperature and processing time on licorice pieces and standard mixture of principal components and impurities the content of 18-Gly and 18α-Gly and 18β-Gly ratio change. Results During the process of Glycyrrhiza uralensis Fisch, increasing the processing temperature and prolonging the processing time caused the decomposition of 18β-Gly and 18α-Gly, which was the main component isomer of licorice root, and the total content of licorice root was slightly decreased. During the processing, the main components did not change the conformation, and had no effect on the proportion of the two. The content of 18β-Gly and 18α-Gly content of glycyrrhizic acid in Glycyrrhiza uralensis Fisch after processing were lower than those before processing in 18β-Gly and 18α-Gly. Conclusion The processing time of licorice pieces could not be too long, the temperature could not be too high, so as to avoid excessive loss of active ingredients. Baking conditions suitable for baking temperature was 65℃, time was 1-2 h. The processing condition was convenient, the time and the temperature were controllable, and the sample quality was stable.
Cost-effectiveness analysis of Danshenchuanxiongqin injection vs salvianolate injection for angina pectoris
FENG Shuang, HU Ming
2018, 36(2): 147-155. doi: 10.3969/j.issn.1006-0111.2018.02.011
Abstract:
Objective To compare the cost-effectiveness of Danshenchuanxiongqin injection versus salvianolate injection for angina pectoris. Methods Databases including CBM, CNKI, VIP, Cochrane library, Pubmed, Embase and Wanfang were electronically searched for the randomized controlled trials (RCTs) on the comparison between Danshen Chuanxiongqin injection and Dsnshenduofensuanyan injection. Literatures were screened and data were extracted in accordance with the inclusion and exclusion criteria. Clinical efficacy of the two drugs were obtained through indirect Meta-analysis. Economic evaluation was carried out using the cost-effectiveness analysis, direct medical cost data included the cost of conventional treatment, drug, examination and hospital expenses. Results Through indirect Meta-analysis, the improvement efficiency of angina were 89.51% and 92.52% for Danshenchuanxiongqin injection and salvianolate injection. The success rates of ECG were 81.40% and 84.05% for two drugs. The costs of Danshenchuanxiognqin injection and salvianolate injection were 4099.71 and 5410.16 CNY. The Cost-effectiveness ratio of angina improve of two drugs were 45.80 and 58.48, while the ECG improve were 50.36 and 64.37. And the sensitivity analysis results were stable. Conclusion Compared to salvianolate injection, salvianolate injection was probably cost-effective for angina pectoris.
Research on quality control of Huoguwan
YE Shengying, GUO Qi, LEI Hong, YANG Ying
2018, 36(2): 156-161. doi: 10.3969/j.issn.1006-0111.2018.02.012
Abstract:
Objective To establish the quality control method for Huoguwan. Methods TLC was applied to detect the component of Danshen, Dihuang, Danggui, Chuanxiong, Sanqi, Tubiechong, and Zhicaowu in this compound preparation. HPLC was used to measure the concentration of Renshenzaogan Rg1, Rb1 and Sanqizaogan R1. Unitary C18 analytical column(4.6 mm×250 mm,5 μm)was used with acetonitrile-water as the mobile phase (Flow rate:1.0 ml/min, column temperature:30℃, wavelength:203 nm). Results Each component showed distinct spots on TLC without interference. There are good linear relationship for Sanqizhaogan R1 in the range of 39.92-399.2 μg/ml, Renshenzhaogan Rb1 in 84.28 -842.8 μg/ml and Renshenzhaogan Rg1 in 135.86-1 358.6 μg/ml. The recovery was 102.35%, 103.84% and 102.97% respectively. Conclusion The above described procedure was accurate and reproducible, which can be used as a method for the quality control of Huoguwan.
Study on improving the quality standard of Taohong Tongmai granule
JIN Weihua, CHEN Hua, ZHANG Ming, YU Botao, PU Zhiqiang, SONG Zonghui
2018, 36(2): 162-165,169. doi: 10.3969/j.issn.1006-0111.2018.02.013
Abstract:
Objective To improve the quality standard of Taohong Tongmai granule. Methods TLC was used to make qualitative identification of Paeoniae Radix Rubra,Rehmanniae Radix,Glycyrrhizae Radix; The effective components of the main walnut kernel were identified by HPLC; and HPLC was used to do quantitative determination of Paeoniflorin,the determination was performed on Agilent HC-C18(250mm×4.6mm,5μm)column with mobile phase consisted of Acetonitrile-water (13:87) at the flow rate of 1.0 ml/min, the column temperature was 30℃ and the detection wavelength was set at 230 nm. Results These TLC spots were fairly clear, and the blank test showed no interference;The paeoniflorin at the range of 1.79-57.28 μg/ml was linear with peak area(r=0.999 9),its average recovery rate was 99.99% and RSD was 2.05%(n=9). Conclusion The quality standard of Taohong Tongmai granule had been improved,identification method was better reproducibility, the determination method of paeoniflorin content had enhanced the controllability of product quality.
Evaluation of hypoglycemic drug-drug interactions by software
SHI Fanghong, LI Hao, LIU Xiaoyan, ZHANG Zaili
2018, 36(2): 166-169. doi: 10.3969/j.issn.1006-0111.2018.02.014
Abstract(3055) PDF (858KB)(696)
Abstract:
Objective To evaluate and analyze the drug-drug interactions (DDI) of different antidiabetic drugs. Methods DDI database Lexi-InteractionTM was used to evaluate DDI for 28 commonly used antidiabetic medications (including insulin and 27 non-insulin preparations). Results 882 DDIs were identified for 28 drugs. Category C was the top rated DDI (69.8%). Category C, D, X were accounted for 91.2% of the total DDI. 28 medication combinations belonged to category X, which should be avoided to use together. Sulfonylureas had the most DDI, followed by metformin. Alpha-glucosidase inhibitors had least DDI. Conclusion Hypoglycemic drugs with less DDI, such as α-glycosidase inhibitors, glucagon-likepeptide1(GLP-1)analogs and sodium-dependent glucose transporters 2 inhibitor (SGLT2i)should be considered with high priority for patients taking multiple antidiabetic medications, elderly patients and patients with liver-kidney dysfunction.
Crystal structure and optical activity of 2-(3,4-dimethoxyphenyl)-4-oxo-4H-chromen-3-yl acetate
ZHANG Kaixia, WANG Chaoming, JIN Yongsheng
2018, 36(2): 170-172,179. doi: 10.3969/j.issn.1006-0111.2018.02.015
Abstract:
Objective To investigate the structure and optical activity of flavonoid derivative:2-(3,4-dimethoxyphenyl) -4-oxo-4H-chromen-3-yl acetate ( 4 ). Methods The absolute configuration was obtained by X-ray single crystal diffraction. The optical rotation of the compound was determined by the SGW® -1 automatic polarimeter. Results X-ray single crystal diffraction showed that compound 4 belongs to the orthorhombic space group P212121 with a=7.763 (2)Å, b=13.930 (4)Å and c=14.906 (4), α=β=γ=90.00°, V=1611.91 (8) Å3, Z=8. There is no hydrogen bonding between the molecules in this crystal state. The molecules maintain their stable arrangement in space by van der Waals forces. It can be seen from the single-crystal data that there is a 33.9 (2)° torsion of the dimethoxy-substituted benzene ring in the compound 4 with respect to the 4H-chromene skeleton, suggesting that there may exist optical activity. Further experimental results of the optical rotation proved that the compound has a L-rotatory, specific rotation[α]D19.1=-5.077°. Conclusion The results of the single crystal indicated that the benzene ring substituted with dimethoxy group in compound 4 has a 33.9 (2)° torsion relative to the 4H-chromene skeleton, which results in chirality and optical activity. This is the first report that non-flavonoid-glycoside has optical activity.
Optimization of extraction technology for Toufu irrigation by orthogonal test
PENG Yong, CHEN Rujing, LIU Duo, CHAI Weihan, ZHU Quangang
2018, 36(2): 173-175. doi: 10.3969/j.issn.1006-0111.2018.02.016
Abstract(2741) PDF (866KB)(689)
Abstract:
Objective To optimize the extraction process and improve the quality of Toufu irrigation. Methods Matrine assay was selected to be the indicator for the extraction efficacy. Orthogonal test was used to determine the optimal water amount, extraction time and extraction frequency. Results The best extraction process was to extract 90 minutes twice with the water amount 8 times of the dry herbal material by weight. Conclusion This process is feasible and repeatable. It can be used for the quality control of the preparation.
Therapeutic observation and pharmacoeconomic analysis of two first-line chemotherapy regimens in advanced NSCLC
ZHU Wenyu, JIANG Qi, ZHANG Liang, WU Juan, WANG Jie, DING Hongzi
2018, 36(2): 176-179. doi: 10.3969/j.issn.1006-0111.2018.01.017
Abstract(1230) PDF (650KB)(816)
Abstract:
Objective To evaluate the cost-effectiveness of two chemotherapy regimens in NSCLC for the purpose of lower cost, higher quality medical care. Methods 56 patients with advanced NSCLC were divided into two groups from our hospital, group PP (pemtrexal+cisplatin, n=30) and group GP (gemcitabine+cisplatin, n=26), and analyzed by pharmacoeconomic cost-effectiveness method, and retrospective analysis was also applied. Results Effective rates of two regimens were 46.67%, 42.31%, no significant difference. But there was significant difference in the incidence rate of ADR between the two groups. The cost of chemotherapy regiments were 31 985.48 and 27 683.15 yuan. The average length of stay was 10.94 and 13.91 days. Compared to group GP, for each unit of efficacy, the cost in group PP were increased 986.77 yuan. Conclusion From the analysis of cost-effectiveness, group PP had higher chemotherapy costs, but better safety than group GP.
Study on the application of epinephrine hydrochloride in senile ptosis surgery
HUANG Wei, YU Juan, DENG XiaoLi, WANG LiQin, SUN Qiang
2018, 36(2): 180-182. doi: 10.3969/j.issn.1006-0111.2018.02.018
Abstract(2947) PDF (640KB)(580)
Abstract:
Objective To explore the application of mixed anesthesia with epinephrine hydrochloride and lidocaine in senile ptosis surgery. Methods 90 senile ptosis cases (180 eyes) treated from January 2016 to June 2016 were randomly divided into experimental group and control group. Subcutaneous infiltration anesthesia with lidocaine and epinephrine hydrochloride was used in the experimental group, while the control group received lidocaine only. The heart rate, blood pressure, blood loss, visual field definition, operation time, incision state, cornea and recovery rate of the two groups were observed. Results ① The systolic blood pressure of the patients in the experimental group was significantly higher than that of the control group (P<0.05). There was no significant difference between two groups in diastolic blood pressure and heart rate (P>0.05). ② The experimental group achieved better results than the control group in operation time, anesthesia time, amount of bleeding, visual field clarity, eyelid congestion and wound healing (P<0.05); ③ There was no significant difference (P> 0.05) between two groups in incisional dressing bleeding, fluid seepage and cornea status. Conclusion The mixed anesthesia of epinephrine hydrochloride and lidocaine had little effect on the patients' diastolic blood pressure and heart rate. It reduced the blood loss during operation and the postoperative eyelid congestion. The clarity of intraoperative vision and recovery time were also improved with the mixed anesthesia.
Effectiveness and safeness of granulocyte macrophage colony stimulating factor and whole lung lavage therapy in idiopathic pulmonary alveolar proteinosis
LIU Guodong, ZHOU Li, ZHANG Wenjing, WANG Zhuo
2018, 36(2): 183-185. doi: 10.3969/j.issn.1006-0111.2018.02.019
Abstract(2895) PDF (646KB)(847)
Abstract:
Objective To observe the effectiveness and safeness of granulocyte macrophage colony stimulating factor(GM-CSF) and whole lung lavage therapy for patients with idiopathic pulmonary alveolar proteinosis (IPAP). Methods Two IPAP patients who were hospitalized in Changhai Hospital from August 2015 to March 2017 were enrolled for the study. Both patients were treated with GM-CSF therapy after whole lung lavage. One patient received GM-CSF by subcutaneous injection and the other by inhalation. Results Both patients' conditions were improved after GM-CSF and whole lung lavage therapy. Conclusion Treatment with subcutaneous injection or inhalation of granulocyte macrophage colony stimulating factor and whole lung lavage is safe and effective for IPAP patients.
302 cases of adverse drug reaction reports
XIN Rujuan, PAN Huijun, LI Ying, AN Duopeng, ZHU Quangang
2018, 36(2): 186-188,191. doi: 10.3969/j.issn.1006-0111.2018.02.020
Abstract(3158) PDF (653KB)(695)
Abstract:
Objective To study the features, general patterns and predisposing factors of adverse drug reactions (ADR) occurred in our hospital and to provide the guidance for rational and safe use of drugs in clinic. Methods 302 cases of ADR were reported from September 2015 to September 2017 in our hospital. Age distribution, gender, route of administration, drug categories, systems or organs involved, clinical manifestations, adverse reaction types involved in ADRs were analyzed retrospectively. Results Among the 302 ADR reports, 137 cases are male patients (accounting for 45.4%) and 165 cases were female patients (accounting for 54.6%). 27.8% of ADR was related to anti-infective agents. 70.2% of ADR came from oral administration and 24.8% ADR was due to intravenous administration. The main clinical manifestations of ADR were lesion of skin and its appendants (61.6%) and followed by the digestive system injury (15.9%). Conclusion The multiple factors may lead to high frequency of ADR. In order to promote rational drug use and reduce the occurrence of ADR, clinicians should pay attention to the ADR monitoring and strictly follow the clinical indications of medications.
Pharmacoeconomic evaluation on three different anti-hypertensive treatments
ZHANG Zhaowei, FANG Tianzi
2018, 36(2): 189-191. doi: 10.3969/j.issn.1006-0111.2018.02.021
Abstract(2827) PDF (643KB)(910)
Abstract:
Objective To compare three different anti-hypertension therapeutic projects by pharmacoeconomic evaluation and to find out the best therapeutic project. Methods Retrospective study was used.120 patients with hypertension were randomly assigned to group A (fosinopril sodium),group B(valsartan),group C(amlodipine besylate tablet),the therapeutic effects were observed and were evaluated by cost minimization analysis. Results The total efficiency of A,B,C group were 90.7%, 92.3%, 92.1% (P>0.05) respectively. The incidence of adverse reaction were 16.7%,7.7%,13.2%(P>0.05) respectively. The costs were 287.3 yuan, 378.7 yuan and 320.4 yuan respectively. Conclution The effectiveness of the three groups was similar. In terms of pharmacoeconomics, group A was the best therapeutic project.