1.Lidamycin inhibits the proliferation of HERG K+ channel highly expressing cancer cells and shows synergy with anticancer drugs.
Boyang SHANG ; Yue SHANG ; Yongsu ZHEN ; Shuzhen CHEN
Acta Pharmaceutica Sinica 2011;46(11):1321-5
This study is to investigate inhibitory effects of lidamycin (LDM) on the proliferation of HERG K+ channel highly expressing cancer cells and its synergy with anticancer drugs. MTT assay was used to examine the inhibitory effects of lidamycin combined with various anticancer drugs on the proliferation of human lung cancer A549 cells, human colon cancer HT-29 cells and herg-stably-transfected A549 cells. Using the xenograft model of subcutaneously transplanted HT-29 in nude mice, inhibitory effect was appraised in vivo. The coefficient of drug interaction (CDI) was used to evaluate the synergistic effect of drug combination. LDM significantly inhibited the proliferation ofA549 cells and HT-29 cells with IC50 values of 2.14 and 4.64 ng mL(-1), respectively. The efficacy in HT-29 cells with high HERG potassium expression level is less potent than that in A549 cells with low expression level. In terms of IC50 values, LDM suppressed the growth of herg-stably-transfected A549 cells less potently than pCDNA3.1-stably-transfected A549 cells. There existed synergistic effects in the combinations of fluorouracil (5-FU) and LDM, doxorubicin (DOX) and LDM, or hydroxycamptothecine (HCPT) and LDM. CDI values of the combinations of 5-FU and LDM were more than 0.75. CDI values of LDM and DOX were more than 0.70, but some CDI values of LDM and HCPT were less than 0.70. As for the CDI values, synergistic effects of the combination of LDM and HCPT were the most potent of the three groups. There is no relationship between the inhibitory effect of the growth of cancer cells by 5-FU and HERG potassium expression level. HERG expression level negatively correlated with inhibitory effect on the proliferation of cancer cells by DOX. HERG expression levels and chemosensitivity were positively correlated for HCPT. In the model of subcutaneously xenograft transplanted HT-29 in vivo, LDM and/or HCPT effectively inhibited the growth of HT-29 in nude mice, and the optimum CDI of the combination of LDM and HCPT was less than 1. HERG expression level negatively correlates the chemosensitivity of cancer cells to LDM. There exist synergistic effects in vitro and in vivo in the combination of LDM and HCPT, which inhibitory effects of the proliferation of cancer cells positively modulated by HERG potassium expression level. HERG K+ channel may become a target of combined therapy for choosing anticancer drugs.
2.Effect of Weidongfang and hydrotalcite on bile reflux gastritis
Qin CHEN ; Boyang ZHU ; Xinhui PAN ; Jianhua REN ; Yi ZHONG
Chinese Journal of Primary Medicine and Pharmacy 2009;16(3):393-395
Objective To observe the effect of Weidongfang and hydrotalcite in treatment of bile reflux gastrifis.Methods Bile reflux gastritis were randomly assigned to 2 groups.30 eases in the Weidongfang group were treated with Weidongfang and hydrotalcite;30 cases in the mosapride group were treated with mosapride and hydrotalcite;and the course of treatment was 4 weeks for all.The clinical symptoms of bile reflux gastritis,the classify of extent of bile reflux and the accumulated points of pathological change of the gastric mucosa below gastroscope were evalumed before and after treatment.Results The significant and total effective rate in the Weidongfang group were 33.3% and 86.7%.Mosapride group 43.3% and 83.3%.Butthe classify of extent of bile reflux and the accumulated points of pathological change of the gastric mucosa of Weidongfang group were Similar to Mosapfide group below gastroscope.Conclusion Weidongfang and hydrotalcite were effective medicine in treatment of bile reflux gastritis.
3.Recent advances of diosgenin in its pharmacologic activities and mechanism
Lei YUE ; Ling CHEN ; Junping KOU ; Boyang YU
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(02):-
Diosgenin,an important steroid sapogenin,is one of major precursors of synthetic steroids.It is rich in natural resources and has various significant activities such as anti-tumor,anti-inflammation,and cardiovascular-protection and so on.Recently,it causes increasing attention of scholars all over the world due to its valuable application in medicine.In this paper,the latest international research advances of diosgenin in its pharmacologic activities and mechanism were reviewed.
4.Hemodynamics assessment by perfusion computed tomography in a canine model of portal hypertension
Yuanwei LIN ; Weijian CHEN ; Qiuli HUANG ; Yunjun YANG ; Pan LIANG ; Boyang YANG ; Hongqing WANG ; Dexin LIN ; Qiyu ZHANG ; Bing XIONG
Chinese Journal of General Surgery 2011;26(5):402-405
Objective To evaluate perfusion computed tomography in the assessment of portal vein pressure changes in an experimental dog model of liver cirrhosis and portal hypertension.Methods The canine model of cirrhosis and portal hypertension was induced by portal vein stenosis with combination of systemic thioacetamide(TAA) feeding in drinking water.All of the Beagles in control group and cirrhotic group underwent hepatic perfusion on a spiral CT scanner.The parameters of hepatic perfusion were calculated by the method of deconvolution.The portal vein pressure was measured by a laparotomy surgery.Results ① In control group, the portal vein pressure was ( 14.5 ± 2.2) cm H2O, while it was (23.1 ± 2.8) cm H2O in PHT group, there was significant difference in the portal vein pressure between the two groups (P<0.05).② The blood flow(BF) was (112 ±14) ml·100 g-1·min-1 in controls, while ( 96 ± 11) ml·100 g-1·min-1 in PHT group; the blood volume ( BV ) in control group and PHT group was (10 ±3) ml·100 g-1 and (11 ± 5) ml· 100 g-1, respectively; the mean transit time( MTT) was (7.1 ± 2.0) s and (10.4 ± 3.5) s, respectively; the hepatic arterial fraction (HAF) was ( 24 ± 5) % and ( 37 ± 6)% , respectively; the hepatic arterial perfusion (HAP) was(27 ±6) ml·100 g-1·min-1 and (35 ±5) ml·100 g-1·min-1, respectively; the portal venous perfusion (PVP) was (85 ± 13) ml·100 g-1·min-1 and (61 ±11) ml·100 g-1·min-1, respectively.There was significant difference in all parameters between the two groups except the parameter BV(P < 0.05).③ In PHT group, the PVP and BF were negatively correlated with the portal vein pressure, while positively correlated with MTT and HAF.Portal vein pressure was negatively correlated with PVP, the equation, Y = 36.624 -0.219X, was deduced with linear regression analysis, by which the portal vein pressure in PHT Beagles was ( 23.2 ± 2.4) cm H2O, which was correlated with the observed by laparotomy value (23.1 ± 2.8) cm H2O (r = 0.843, P < 0.05).Conclusion CT perfusion is a new non-invasive and effective method for assessment of portal vein pressure.
5.Evaluation of hemodynamic outcomes after carotid artery stenting using cerebral perfusion CT
Boyang YANG ; Weijian CHEN ; Hongqing WANG ; Yunjun YANG ; Haibo HUANG ; Yuxia DUAN ; Fengli FU ; Yuanwei LIN ; Pan LIANG ; Bing XIONG
Chinese Journal of Radiology 2010;44(12):1280-1284
Objective To evaluate 1-week and 1-year outcomes of carotid artery stenting (CAS)using cerebral perfusion CT(PCT). Methods The clinical database of 20 patients with unilateral carotid artery stenosis( ≥60% ) who underwent CAS were retrospectively reviewed. Relative cerebral blood volume (rCBV), relative cerebral blood flow(rCBF) and relative mean transit time( rMTT) were measured by using cerebral PCT within one week before CAS and at one week and at one year after CAS. Cerebral MRI was performed within one week before CAS. The noncontrast CT was performed within one week before CAS and immediately after CAS. The arteriography was performed at one year after CAS. The variance analysis was performed to determine whether there were significant differences of rCBV, rCBF, rMTT in anterior cerebral artery area( ACA area), middle cerebral artery area( MCA area), posterior cerebral artery area( PCA area),basal ganglia area, front and back cortical watershed area( CWS area) and internal watershed area( IWS area) among the different time points. Results In the three measures, there was no significant difference of rCBV in all areas among the three time points( P > 0. 05 ) , and there was no significant difference of rCBF and rMTT in PCA area( P > 0. 05 ), but there were significant differences of rCBF and rMTT in all other areas among the three time ponits(P <0. 01). In one week before CAS, at one week and at one year after CAS, rCBF of 20 patients is 0. 86 ±0. 06, 0. 95 ±0. 04, 0. 98 ±0. 07 in ACA area, 0. 81 ±0. 04, 1.06 ±0. 04, 1.03 ±0.07 in MCA area, 0. 84 ±0. 06, 0. 97 ±0. 04, 0. 96 ±0. 04 in basal ganglia, 0. 78 ±0. 03,0. 97 ±0. 03, 0. 96 ±0. 02 in front CWS area, 0. 77 ±0. 03, 1.00 ±0. 02, 0. 98 ±0. 03 in back CWS area,and 0. 80 ± 0. 04, 0. 94 ± 0. 03, 0. 93 ± 0. 04 in IWS area ( F = 18. 95, 146. 41,63.03,540. 85,415.97,164.19, P<0. 01). rMTT is 1.17 ±0.05, 1.04±0.04, 1.01 ±0.06 in ACA area, 1.41±0.06, 1.08±0.04, 1.07±0.04 in MCA area, 1.20±0.06, 1.06±0.04, 1.05±0.04 in basal ganglia, 1.41 ±0.05,1.10 ±0. 05, 1.09 ±0. 04 in front CWS area, 1.43 ±0. 10, 1.07 ±0. 06, 1.08 ±0. 06 in back CWS area,1.29±0.10, 1.09 ±0.05, 1.11 ±0.07 in IWS area (F=51.74, 248. 89, 70.08, 381.68, 288.94,41.53, P <0. 01 ). There were significant differences of rCBF and rMTT between those measured one week before CAS and one week or one year after CAS ( P < 0. 01 ), but there were no significant differences of rCBF or rMTT in any area measured between those at 1 week after CAS and those measured at 1 year after CAS(P>0.05). Conclusions Hemodynamic outcome at one year after CAS is good in the absence of contralateral carotid artery steno-occlusive disease. In addition, the coherence of results between 1-week and 1-year indicates that the outcome of one week after CAS could predict long-term hemodynamic outcome.
6.Comparative study between multi-slice CT angiography and digital subtraction angiography in detection of intracranial micro-aneurysms
Fengli FU ; Weijian CHEN ; Yunjun YANG ; Hongqing WANG ; Yuxia DUAN ; Boyang YANG ; Yuanwei LIN ; Xianxi TAN ; Ming ZHONG ; Qichuan ZHUGE
Chinese Journal of Radiology 2010;44(3):229-233
Objective To investigate the value of multi-slice computed tomography angiography (MSCTA)in the detection of intracranial micro-aneurysms(aneurysm≤3 mm in maximal diameter, IMA).Methods The clinical history and images of 826 patients with suspected intracranial aneurysms were retrospectively analyzed.All patients underwent MSCTA on 16-slice row CT before hospitalization(from 2 h to 4 d after symtom onset).All intracranial aneurysms were confirmed by digital subtraction angiography (DSA), three-dimensional rotational angiography (3DRA) or surgery.Two independent radiologists assessed all the images.The MSCTA findings were compared with the DSA/3DRA results.The sensitivity, specificity, and accuracy of MSCTA for diagnosis of IMA was calculated.The diagnostic consistency between DSA/3 DRA and MSCTA was determined by Kappa statistics.The prevalence of multiple aneurysms between the group of patients with IMA and the group of patients without IMA was evaluated by Chi-square test Results A total of 889 aneurysms in 788 of the 826 patients were detected.Among them, 706 patients had single aneurysm and 82 patients had multiple aneurysms.No aneurysms were detected in 38 patients.Among the 212 patients who underwent DSA/3 DRA, 271 aneurysms were found and 232 were IMA.MSCTAdetected 229 IMA.There was 1 false-positive finding and 4 false-negative findings by MSCTA.The sensitivity, specificity and accuracy of MSCTA for IMA was 98.3% (228/232), 97.4% (38/39), 98.2% (266/271).There was excellent agreement between two techniques (Kappa=0.927, P<0.05).The prevalence of multiple aneurysms was 21.2% (45/212) in the patient group with IMA and 6.4% (37/576) in the group without IMA.There was statistically significant difference between the two groups (X~2=36.421, P<0.01).Conclusions The detection value of IMA by MSCTA was high.The cutoff level of diameter of intracranial IMA should be adjusted from 4-5 mm to ≤3 mm.
7.Role of abnormal hemodynamics and vascular remodeling in pan-vascu-lar diseases
Yuexing LI ; Qian LI ; Boyang CHEN ; Shuai CHEN ; Yunzhi CHEN
Chinese Journal of Pathophysiology 2024;40(5):931-937
Vascular remodeling is a physiological and pathological process in which abnormal changes in vas-cular cells and non-cellular components lead to the remodeling of inward and outward blood vessel wall or changes in lu-men diameter.As the channels for blood flow,blood vessels are continuously affected by hemodynamic forces.When sens-ing the abnormal blood flow forces,the mechanically sensitive cell membrane structures such as G protein-coupled recep-tors,ion channels,cell surface glycocalyx,and integrins,as well as the extracellular matrix will induce the process of vas-cular endothelial dysfunction,endothelial-mesenchymal transition,smooth muscle cell phenotypic switching,pericyte morphological changes and extracellular matrix remodeling to participate in vascular remodeling.As shown by research,abnormal hemodynamics caused abnormal changes in vascular structure and function,which was the basic process for the occurrence and development of pan-vascular diseases such as atherosclerosis,hypertension,diabetes,non-alcoholic fatty liver disease,pulmonary hypertension and COVID-19.This paper reviewed the interaction and molecular mechanism be-tween abnormal hemodynamics and vascular remodeling,and analyzed its influence on the pathogenesis of pan-vascular diseases,which could provide reference for formulating prevention and treatment strategies for pan-vascular diseases.
8.Application of primary PCI in elderly patients with AMI
Zhengming XU ; Tianchang LI ; Yu CHEN ; Xianfeng LI ; Yi CAO ; Yigang QIU ; Boyang ZHANG ; Zhichao WANG ; Xingyu CHEN
Chinese Journal of Geriatric Heart Brain and Vessel Diseases 2018;20(3):250-252
Objective To assess the feasibility,safety and efficacy of primary PCI in elderly patients with AMI.Methods Three hundred and sixty-four AMI patients were divided into ≥75 years old group (n=90) and <75 years old group (n=274).The successful operation rate,preoperative complication rate,mortality and incidence of major adverse cardiovascular events (MACE) were recorded during their hospital stay time.Results The successful operation rate was 94.4%,the postoperative TIMI 3 blood flow rate was 87.8%,and the preoperative complication rate was 10.0 % in ≥75 years old group.The mortality and incidence of MACE were significantly higher in ≥75 years old group than in<75 years old group during the hospital stay time (12.2% vs 2.9%,P =0.001;16.7 % vs 5.1%,P =0.000).Conclusion Transradial primary PCI is a safe,feasible and effective therapy for ≥75 years old AMI patients.
9.Prediction of hemorrhagic transformation in acute ischemic stroke using permeability surface of CT perfusion
Bing XIONG ; Weijian CHEN ; Fengli FU ; Yuxia DUAN ; Boyang YANG ; Hongqing WANG ; Yunjun YANG ; Pan LIANG ; Yi LIN ; Shu WANG ; Nan WU ; Qiuyun TONG
Chinese Journal of Radiology 2012;46(7):593-597
Objective To investigate the value of permeability surface (PS) in predicting hemorrhagic transformation (HT) in acute ischernic stroke (AIS) using CT peffusion (CTP).Methods The study included 31 consecutive patients who presented symptoms suggestive of an AIS for 3-9 h. All patients underwent CT examination (noncontrast CT,CTP).HT was determined by follow-up CT images.According to presence of HT,the AIS was divided into HT group (PSHT,11 patients) and non-HT group(PSNo-HT,20 patients).PS,cerebral blood flow (CBF),cerebral blood volume (CBV) and mean transit time (MTT) on both sides of brains were measured.The relative PS(rPS),relative CBF (rCBF),relative CBV(rCBV) and relative MTT(rMTT) were obtained by calculating the ratio of the values of bilateral regions.The rPS between PSHT and PSNo-HT was compared with an exact Wilcoxon signed-rank test. The rCBF,rCBV,rMTT and the PS of the ischemic side between PSHr and PSNo-HT were compared with independent-sample t test.Meanwhile,Spearman rank correlation analysis was conducted to analyze the relationship between the CTP parameters and HT.ResultsThe PS value of ischemic side was (1.61±0.77) ml · min - 1 · 100 g-1 for the PSHT group,and the value was (0.91 ± 0.49) ml · min - 1 · 100 g- 1 for the PSNo-HT group.For the PSHT group,rPS,rCBF,rCBV,rMTT were 2.76 ±0.78,0.32 ±0.18,0.66 ±0.31,2.67 ±0.71,and for the PSNo-HT group,rPS,rCBF,rCBV,rMTT were 1.35 ±0.19,0.50±0.21,0.91 ±0.28,2.62 ± 1.31.Compared with PSNo-HT,PSHT had higher rPS and PS value,and there were significant statistical differences (U =0.000,t =3.070,P <0.01).But rCBF and rCBV values were lower in the PSHT group compared to the PSNo-HT group,and there were significant statistical differences (trCsF =2.343,trCBV =2.210,P < 0.05).There was no significant statistical difference in rMTT between the two groups(t =0.118,P > 0.05).Significant positive correlations were detected between the rPS and PS with HT(r=0.496,0.821,P <0.01).ConclusionsThe value of rPS is helpful in predicting HT in AIS.And it can be used as a predictor in determining clinical personalized treatment and thus reduce the incidence of adverse events.
10.Advances of active ingredients of traditional Chinese medicine in the preven-tion and treatment of osteoarthritis
Han HAN ; Yuanyuan ZHANG ; Li PAN ; Zhengdong CHEN ; Lixuan XUE ; Boyang YU ; Jun-Ping KOU
Journal of China Pharmaceutical University 2018;49(3):279-285
Osteoarthritis (OA),a common chronic degenerative joint disease,rises gradually with age,which seri-ously affects the quality of life of middle-aged and elderly patients. Currently,the therapeutic medications such as nonsteroidal anti-inflammatory drugs (NSAIDs)and analgesics might improve OA symptoms,but cannot prevent the development of OA. The active ingredients of traditional Chinese medicine (TCM)have unique advantages in the treatment of OA. This article reviews the research progress of active ingredients of TCM in the prevention and treatment of OA reported by domestic and foreign journals in the past five years from the aspects of inhibition of the secretion of inflammation-related factors,improvement of cartilage matrix synthesis and catabolic imbalance, inhibition of chondrocyte apoptosis,promotion of chondrocyte proliferation,and regulation of estrogen levels,with an attempt to provide a theoretical basis for the development of new drugs for OA.