1.Preparation and Bioactivity of Cationic Porphyrins Bearing Mixed 3-quinolyl and 3-pyridyl Meso Groups
Lu TAO ; Shi DONGFANG ; Sun DAEKYU ; Han HAIYONG ; H.hurley LAURENCE
Journal of China Pharmaceutical University 2003;(2):109-115
AIM: To search for the potent telomerase inhibitors with structures of cationic porphyrins to improve the interactions between G-quadruplex and porphyrins by systematically varying the meso substituents. METHOD: Porphyrins bearing mixed 3-quinolyl/3-pyridyl meso groups were synthesized using the Adler-Longo method by condensation of aldehydes with pyrrole, followed by methylation and ion-exchange. The compounds were tested for the telomerase inhibitory activity and c-Myc inhibitory activity. RESULT: All compounds were found to be potent and approximately equivalent in terms of their ability to inhibit the action of telomerase in a cell-free assay. Compound 4 had the best inhibitory activity on c-Myc.
2.Design,Synthesis and Biological Activity of Cationic Porphyrins Bearing Mixed 3-Quinolyl and 4-Pyridyl Meso Groups
Tao LU ; Dongfang SHI ; Daekyu SUN ; Haiyong HAN ; H.hurley LAURENCE
Journal of China Pharmaceutical University 2005;(5):393-397
AIM:To search for the potent telomerase inhibitors with structures of cationic porphyrins to improve the interactions between G-quadruplex and porphyrins by systematically varying the meso substituents.METHODS:Porphyrins bearing mixed 3-quinolyl/4-pyridyl meso groups were synthesized using the Adler-Longo method by condensation of aldehydes with pyrrole,and then followed by methylation and ion exchange.The compounds were tested for the telomerase inhibitory activity and c-Myc inhibitory activity.RESULTS:All compounds were found to be potent and approximately equivalent in terms of their ability to inhibit the action of telomerase in a cell-free assay.Compound 4 had the best inhibitory activity on c-Myc.CONCLUSION:Cationic porphyrins would be the potential anticancer candidates.
3.Application value of spiral CT with 3D reconstruction on diagnosis and treatment of tibial plateau fractures
Jun TAO ; Jun SHENG ; Bin DONG ; Haiyong CUI ; Qiang LI
Chinese Journal of Primary Medicine and Pharmacy 2011;18(21):2916-2917
ObjectiveTo evaluate the value of application of spiral CT with 3D reconstructure on diagnosis and treatment of tibial plateau fractures.Methods15 cases of tibial fractures treated with x-ray and 16-slices spiral CT,3 D images were made,fractures were classified and evaluated with 3D images and treated with correct treatment.ResultsAll of the 15 patients got correct diagnosis by 16-slices spiral CT with 3D reconstructure,1 failed by x-ray.10 fractures were operated under 3D reconstructure guide and operation proved fractures revealed by 3D reconstructure finally.ConclusionSpiral CT with 3D reconstructure could offer more accurate location and classification of tibial plateau fractures,and it had obvious advantage on demonstration of spatial relationship,and it also could provide better planning and management for the tibial plateau fractures.
4.Diagnosis of small single solid thyroid nodule with real-time ultrasound elastography
Haijun DAN ; Yan WANG ; Haiyong DAN ; Baojin LU ; Tao LI ; Bing HU
Chinese Journal of Medical Imaging Technology 2010;26(1):63-65
Objective To assess the diagnostic value of ultrasonographic elastography for identifying suspected malignant thyroid nodules. Methods Fifty-one patients with small single solid thyroid nodule underwent two-dimensional and color power Doppler ultrasonography. The size, shape, boundary, internal echo and halo, calcification of thyroid nodule were observed with two-dimensional ultrasound. Then color Doppler ultrasonography was used to detect blood signal and distribution in the nodules. Longitudinal scanning of elastography was performed, and the findings on elastography were classified into Ⅰ-Ⅴ grades. The ultrasonographic results were compared with pathologic findings. Results Six patients were found with grade Ⅰ and Ⅱ benign lesions;9 with grade Ⅲ ( 6 benign and 3 malignant), 36 with Ⅳ and Ⅴ (2 benign and 34 malignant) lesions on ultrasonographic elastography. Taking the elasticity grade Ⅳ or Ⅴ as malignant standard, the diagnostic sensitivity was 91.89%, specificity was 85.71%, accuracy was 90.20%, while the positive and negative predictive value was 94.44% and 80.00%, respectively. Conclusion Real-time ultrasound elastography is a promising imaging technique that can assist in the differential diagnosis of malignant thyroid small single solid nodule.
5.Different endovascular thrombus reduction techniques in the treatment of acute lower extremity arterial thrombosis
Haiyong LIU ; Xiaoming ZHANG ; Tao ZHANG ; Zenghui LIANG ; Yanan PAN ; Wei LIU ; Yijun ZHANG ; Yunxia CHEN
Chinese Journal of General Surgery 2021;36(8):600-603
Objective:To compare the clinical results of different endovascular thrombus reduction techniques in the treatment of acute lower extremity arterial thrombosis.Methods:The clinical data of 96 consecutive patients with acute femoral popliteal arterial thrombosis who were treated with catheter directed thrombolysis (CDT) and mechanical thrombus aspiration system (PMT) between Jan 2016 and Dec 2018 at Cangzhou People's Hospital and Peking University People's Hospital were retrospectively analyzed.Results:Ninty-six patients underwent thrombolytic surgery,including 36 with CDT thrombolysis, 28 with AngioJet aspiration alone and 32 with Rotarex aspiration alone. Angiojet thrombus aspiration reduced thrombus rate by 89.3% (25/28) and clinical success rate by 92.8% (26/28).The thrombus reduction rate of Rotarex group was 87.5% (28/32), and the clinical success rate was 96.8% (31/32). In the CDT thrombolytic group, the thrombolytic reduction rate was 61.1% (22/36), including 8 patients who underwent thrombectomy and 6 patients with PMT, with a clinical success rate of 86.1% (31/36). The rate of distal arterial embolization, puncture point and local subcutaneous hematoma and vascular rupture was 21.4%, 10.7% and 2.1%, respectively. There were no amputation cases reported during a mean 13 months follow-up.The survival rate was 97.9%. The first-stage patency rate of 67.8%, while the second-stage artery patency rate of 85.7% during the follow-up.Conclusion:Compared with CDT, PMT has higher efficiency and lower complication rate in the treatment of acute lower extremity arterial thrombosis.
6.Advances of the uricosuric drugs
Guilin YAO ; Haiyong WANG ; Tao LU
Journal of China Pharmaceutical University 2016;47(4):491-496
Promoting uric acid excretion is an important approach for the treatment of gout and hyperuricemia. There are two main approaches included in the mechanism: one is inhibiting the function of renal tubular uric acid transporter to reduce the absorption of uric acid, and promoting excretion; the other is using uricase to catalyze the oxidation of uric acid to a more water-soluble allantoin that can also increase excretion. The mechanisms and progress of the uricosuric drugs are reviewed in this paper, providing reference for the further research and development.
7.An analysis of the effect of artificial lengthening femoral head replacement in elderly patients with stage Ⅰ of unstable femoral intertrochanteric fracture
Zhanxing CHEN ; Haiyong CUI ; Yongjun HU ; Hai HU ; Jianhao DAI ; Liangliang FAN ; Qigang CHEN ; Weili JIANG ; Longfei ZHAO ; Xiaodi HE ; Jun TAO ; Keqing XU ; Zhaobo ZENG ; Yue LENG ; Xiaoli XING ; Jinsu YU ; Bin DONG
Chinese Journal of Primary Medicine and Pharmacy 2017;24(20):3062-3066
Objective To analyze of the effect of artificial lengthening femoral head replacement in elderly patients with stage Ⅰ of unstable femoral intertrochanteric fracture.Methods 203 patients with stage Ⅰ of unstable femoral intertrochanteric fracture were selected as the research object,and they were taken artificial lengthening femoral head replacement,among which 65caese were male,female in 138 cases.The Harris scoring,SF-36,VAS pain scores on admission,2 weeks after operation,postoperative follow-up limb were counted,and the pain of the affected limb and the hip scores were compared amond 3 time periods.Results All 203 cases of senile patients with follow-up,average operation time was 83.64 minutes,the intraoperative blood loss was 355.41mL.The curative effect was evaluated according to the Harris score,SF-36 and VAS pain scoring criteria,and the Harris scores of the affected limbs at admission,at 2 weeks after the operation and after the follow-up were (28.26 ± 5.50) points,(68.26 ±5.50) points,(93.13 ± 5.31) points,respectively,the differences were statistically significant (t =-71.27,-1 397.55,-46.07,all P < 0.01);The VAS pain scores were (8.19 ± 0.48) points,(3.53 ± 0.71) points,(0.23 ± 0.42) points,respectively,the differences were statistically significant (t =88.06,324.17,60.84,all P < 0.01).The sf-36 scores:physiological [(8.35 ± 1.24) points,(15.23 ± 2.17) points,(19.21 ± 2.12) points],social/family [(7.01 ±1.13) points,(14.12 ± 2.12) points,(19.85 ± 2.24) points],emotional [(4.83 ± 1.01) points,(10.12 ±1.22)points,(14.87 ± 1.32) points],function [(6.35 ± 1.21) points,(13.67 ± 1.87) points,(16.81 ±2.12) points],additional focus [(8.85 ± 1.45) points,(16.38 ± 2.12) points,(20.21 ± 2.42) points],total quality of life [(47.35 ± 4.76) points,(74.69 ± 5.87) points,(89.21 ± 6.12) points],the differences were statistically significant(-39.77,-62.92,-20.21,-44.87,-71.89,-26.79,-45.04,-89.01,-38.25,-45.79,-63.41,-15.29,-45.20,-60.39,-17.54,-52.12,-76.49,-22.58,all P<0.O1).Conclusion Artificial lengthening femoral head replacement in elderly patients with stage Ⅰ of unstable femoral intertrochanteric fracture has good clinical effect,intraoperative high safety,less postoperative complications,postoperative limb functional recovery is good,and it is worthy of clinical promotion and application.
8.Effects of acute normovolemic hemodilution on target-controlled infusion of etomidate blood concen-trations and adrenocortical function
Yinghui CUI ; Jiaming XU ; Tong LIU ; Haiyong TAO ; Xi-Aoyi XIE ; Shejun HU ; Xuefei WANG ; Jinghuo WANG ; Jianrong GUO
The Journal of Clinical Anesthesiology 2024;40(8):814-819
Objective To observe the effects of acute normovolemic hemodilution(ANH)on target-controlled infusion(TCI)of etomidate blood drug concentration and adrenal cortical function.Methods Sixty patients who undergo elective multisegmental spine surgery,35 males and 25 females,aged 30-60 years,BMI 20-25 kg/m2,ASA physical status Ⅰ or Ⅱ,were divided into two groups using random number table method:ANH group and control group,30 patients in each group.Both groups used a target-controlled infusion of etomidate for anesthesia induction and anesthesia maintenance.In the ANH group,ANH was performed after steady anesthesia induction,ideal Hct 28%to 30%,and transfused within 1 hour after surgery;the control group was routinely treated.The dosage of etomidate was recorded.Liquid chroma-tography-tandem mass spectrometry(LC-MS/MS)was used to detect etomidate blood concentrations at the immediate postoperative,10,20,and 30 minutes postoperative periods in the two groups,and the immedi-ate moment autologous blood collected into the storage bag,preserved in the storage bag for 1 hour,and the immediate moment transfused back in the ANH group.Plasma concentrations of cortisol(Cor),adrenocorti-cotropic hormone(ACTH),and aldosterone(ALD)were measured by chemiluminescence immunoassay(CLIA)before the induction of anesthesia,immediately after the operation,and at 1 day and 2 days postop-eratively.Results There was no significant difference in the total dosage of etomidate between the two groups.Compared with the immediate postoperative period,the plasma etomidate concentration was signifi-cantly decreased 10,20,and 30 minutes after surgery(P<0.05).Compared with the control group,the concentration increased significantly 10 minutes after surgery in the ANH group(P<0.05).The plasma concentrations of etomidate were(547.8±119.4)ng/ml at the immediate moment autologous blood collected into the storage bag,(536.7±107.8)ng/ml at the preserved in the storage bag for 1 hour,and(522.8±91.7)ng/ml at theimmediatemoment transfusedbackinthe ANHgroup.Comparedwithbeforein-duction of anesthesia,the concentration of Cor and ALD immediately after the operation decreased signifi-cantly(P<0.05)and the concentration of ACTH was significantly higher(P<0.05).There were no sta-tistically significant differences in the concentrations of Cor,ALD,and ACTH between the two groups before induction of anesthesia 1 day and 2 days postoperatively.Conclusion In the orthopedic surgery of TCI eto-midate,return transfusion of collected autologous blood transiently(about 10 minutes)increases etomidate blood concentrations,the function of adrenal cortical will recover to the preoperative level within 24 hours after the operation.