1.Pharmacokinetics of ginsenosides Rg1 and its metabolites in rats
Liang FENG ; Changjiang HU ; Lingying YU
Acta Pharmaceutica Sinica 2010;45(5):636-40
To study the pharmacokinetics of ginsenosides Rg1 and its metabolites after iv and oral administration in Wistar rats, the LC-MS/MS method was selected to determine ginsenosides Rg1 and its metabolites in plasma and their pharmacokinetic parameters were calculated. After oral administration of ginsenosides Rg1 to rats, ginsenosides Rg1, Rh1, F1 and protopanaxatriol (Ppt) could be detected in plasma. Their Tmax were 0.92, 3.64, 5.17, and 7.30 h, respectively; MRT were 2.68, 5.06, 6.65, and 5.33 h, respectively; AUC(o-t), were 2 363.5, 4 185.5, 3 774.3, and 396.2 ng x mL(-1) x h, respectively. After iv administration of ginsenosides Rg1 to rats, ginsenosides Rg1, Rh1 and FI could be detected in plasma. Their T1/2betaS were 3.12, 5.87, and 6.87 h, respectively; MRTs were 1.92, 5.99, and 7.13 h, respectively; AUCo-tS were 1 454.7, 597.5, and 805.6 ng x mL(-1) x h, respectively. So, it can be concluded that after oral administration, the amounts of metabolites were higher than the prototype in vivo, and the distribution and elimination of the metabolites were relatively slow. After iv administration, the amount of prototype were higher than that of the metabolites in vivo, and the distribution and elimination of the metabolites were relatively slow.
2.Molecular biology research of recombinant human endostatin targeted therapy of non-small-cell lung cancer
Changjiang LIU ; Xiaorong XU ; Guoying FENG
Chinese Journal of Biochemical Pharmaceutics 2014;37(4):100-105
Objective To investigate the relationship between molecular biological markers and recombinant human endostatin targeted therapy in non-small-cell lung cancer(NSCLC).Methods 68 cases patients with non-small-cell lung cancer to meet the requirements were randomly divided into group A (n=34)and group B (n=34).Group A received docetaxel and cisplatin(DP)and gefitinib;group B received recombinant human endostatin on the base of group A.The biological markers species,such as,EGFR,KRAS,VEGF,BRCA1,EML4-ALK,ERCC1,β-tubulin and CD3 were detected by immunohistochemical.The types of population for different programs were summarized according to the expression of biological markers and progression free survival (PFS)of the two groups. Results Group B median PFS was significantly longer than that in group A;no matter low or high expression of VEGF and BRCA1,group B median PFS was significantly longer than that in group A(P<0.05);high expression of ERCC1,KRAS,EML4-ALK andβ-tubulin,group B median PFS was significantly longer than that in group A(P<0.05);low expression of EGFR and CD3,group B median PFS was significantly longer than that in group A (P<0.05 ).Conclusion No matter low or high expression of VEGF and BRCA1 ,low expression of KRAS, ERCC1,EML4-ALK and β-tubulin and high expression of EGFR and CD3 in patients with non-small cell lung cancer may be more sensitive to the treatment of DP and gefitinib combined with recombinant human endostatin.
3.Abirritation of geraniol on neuropathic pain model rat and possible mechanism
Zili XING ; Qiyuan HAN ; Zhaohe FENG ; Changjiang XU ; Weiguo JIA
Chinese Pharmacological Bulletin 2017;33(4):535-541
Aim To study the analgesic effect of geraniol on neuropathic pain and to explore the possible mechanism.Method A neuropathic pain rat model of Spared Nerve Injury(SNI) was established to measure changes in the threshold of paw withdrawal before and after i.p.administration of geraniol.Patch clamp whole-cell recording was performed to measure activity of sodium channels using ipsilateral L3/L4/L5 dorsal root ganglion(DRG) cells isolated from the SNI rats.In addition, HEK 293 cells expressing hNav1.7 and hTRPA1 channels were used for measuring the changes in channel activities with or without geraniol by whole-cell patch clamp.Results Geraniol had a fast analgesic effect on hypersensitivity of mechanical pain in the SNI model.It significantly inhibited sodium channels on DRGs isolated from SNI rats and hNav1.7 but not hTRPA1 channels expressed by HEK293 cells.However, high concentrations of geraniol facilitated the activation of HTRPA1 channel stimulated by AITC.Conclusion Geraniol may abirritate hypersensitivity of mechanical pain in the SNI model by specifically inhibiting Nav1.7 channel activity on the DRG cells.
4.The surgical methods and efficacy of 70 cases over 65 years old patients with aortic dissection
Yongtao FENG ; Ruixin FAN ; Shaoyi ZHENG ; Shaohong MA ; Xiaoping FAN ; Changjiang YU
Chinese Journal of Thoracic and Cardiovascular Surgery 2013;29(12):719-721
Objective To retrospectively analyze the surgical methods and efficacy in 70 cases of type A aortic dissection patients over 65 years old.Methods From January 2005 to May 2012,70 type A aortic dissection patients over 65 years old received surgical treatment.Among them,there were 47 males aged 65 to 78 years old with mean 71,23 females,aged 65 to 72 years old with mean 68.55 cases were acute onset,while 15 cases were chronically onset.Different surgical methods were selected depend on patients' situations.We followed up all patients after discharged from hospital to continue to observe their health situation and evaluate the therapeutic effects.Results After surgery,eight patients died in the hospital,62 patients were recovered and discharged from the hospital.The mortality rate is 11.4%.During the follow up period from 3 to 72 months,there were no dead,aneurysm rupture and others severe complications.9 cases received endovascular graft exclusion within 6 months after discharged from hospital.The survival patients were satisfactory healed with their daily living activity resumed.Conclusion For over 65 years old patients with aortic dissection,the accurate and rapid selection of surgical method could improve the survival rate and the quality of life with a lower occurrence rate of complications.
5.Lipid metabolism is improved by L- carnitine in semi- starved rats fed on high fat diet
Yu FENG ; Changjiang GUO ; Jingyu WEI ; Jijun YANG ; Yuzhang GE ; Lanxi GAO
Chinese Journal of Pathophysiology 2000;16(12):1313-1316
AIM: To investigate the effects of exogenous L - carnitine on lipid metabolism in semi - starved rats fed on high fat diet. METHODS: The semi - starved rats were restricted half in calorie intake on high fat diet for 2 week. L - carnitine was supplied at dose of 250 mg/kg· bw. The changes of plasma carnitine concentration, urinary excretion of ketone body, serum lipase activity, muscle carnitine palmitoyl transferase activity, triglyceride secretion and clearance rate were measured. RESULTS: The results showed that the concentration of plasma free camitine increased significantly in carnitine supplemented rats compared to normal and semi - starved rats. The activities of muscle carnitine palmitoyhransferase and serum lipase were significantly enhanced in carnitine supplemented rats. The triglyceride secretion rate (TGSR) was also improved remarkably by carnitine supplementation. Meanwhile, the urinary excretion of ketone body was reduced significantly in carnitine supplemented rats compared to semi - starved rats. CONCLUSION: It is concluded that carnitine supplementation can significantly increase the plasma concentration of free carnitine and accelerate the lipid metabolism in semi - starved rats fed on high fat diet.
6.Intrahepatic biliary papillomatosis:a report of 9 cases
Caide LU ; Changjiang LU ; Shengdong WU ; Jue ZHOU ; Feng QIU ; Jing HUANG
Chinese Journal of Hepatobiliary Surgery 2010;16(5):328-332
Objective Intrahepatic biliary papillomatosis(IBP)is a rare disease that is characterized by multiple numerous papillary adenomas in the intrahepatic biliary duct(IBD).The clinical features and outcome,however,are not well known.The clinicopathologic features,treatments and follow-up results were retrospectively analyzed in order to improve the efficiency of diagnosis and treatment for the disease.Methods Between August 2006 and October 2008,9 patients were diagnosed with IBP by histological findings at a tertiary referral center,Ningbo Medical Center(University of Ningbo,College of Medicine,Ningbo,China).The authors retrospectively reviewed the medical records to obtain clinical,radiological and pathologic data.The therapeutic results and follow-up data were also reviewed.Results The ratio of male to female was 2:7 and the middle age was 59 years.Repeated episodes of fever and right upper quadrant abdominal pain with or without jaundice were the common clinical manifestations.There were intrahepatic choledocholithiasis and/or history of previous biliary operation in 8 cases.The level of CA19-9 and CEA were almost normal.Imaging workup demonstrated cyst-like dilatation of intrahepatic biliary tree with or without liver atrophy,which were more obvious in the mucin-hypersecreting IBP.All of the 9 cases underwent curative resection with an adequate resection margin.Macroscopic findings demonstrated that the tumors of 9 cases were all located in the left lobe with mucin-hypersecreting type in 7 cases.The diameter of numerous papillary granular was usually less than 10 mm(from 2 to 5 mm.frequently)and friable,that filled the dilated IHD dispersive.Fine fibrovascular cores lined by dysplastic epithelial cells were frequently found under microscope.Few foci of stromalinvasion were noticed in the two cases with malignant transformation.All of the 9 cases survived and there was no recurrence.Conclusion IBP occurs more often in middle and old women who have history of biliary disease. Repeated episodes of cholangitis are the common clinical manifestations. Extra- and intrahepatic biliary tract dilatation is the common imaging finding.MRCP/ERCP is more valuable than others in diagnosis. Clinical and histological finding shows that IBP is a premalignant disease with high malignant potential. Curative resection should be done as earlyas possible for the long-term survival rate. The use of cholangioscopy in operation and rapid biopsy of resection margin will benefit the curative resection.
7.Lipid metabolism is improved by L-carnitine in semi-starved rats fed on high fat diet
Yu FENG ; Changjiang GUO ; Jingyu WEI ; Jijun YANG ; Yuzhang GE ; Lanxing GAO
Chinese Journal of Pathophysiology 2000;0(12):-
AIM: To investigate the effects of exogenous L-carnitine on lipid metabolism in semi-starved rats fed on high fat diet. METHODS: The semi-starved rats were restricted half in calorie intake on high fat diet for 2 week. L-carnitine was supplied at dose of 250 mg/kg?bw. The changes of plasma carnitine concentration, urinary excretion of ketone body, serum lipase activity, muscle carnitine palmitoyl transferase activity, triglyceride secretion and clearance rate were measured. RESULTS: The results showed that the concentration of plasma free carnitine increased significantly in carnitine supplemented rats compared to normal and semi-starved rats.The activities of muscle carnitine palmitoyltransferase and serum lipase were significantly enhanced in carnitine supplemented rats. The triglyceride secretion rate(TGSR) was also improved remarkably by carnitine supplementation. Meanwhile, the urinary excretion of ketone body was reduced significantly in carnitine supplemented rats compared to semi-starved rats. CONCLUSION: It is concluded that carnitine supplementation can significantly increase the plasma concentration of free carnitine and accelerate the lipid metabolism in semi-starved rats fed on high fat diet.
8.Molecular Cloning of Two Novel Temporins From Lithobates catesbeianus and Studying of Their Antimicrobial Mechanisms
Ruili ZHAO ; Junyou HAN ; Wenyu HAN ; Liancheng LEI ; Changjiang SUN ; Xin FENG ; Lina JIANG ; Hongwei QIAO ; Linjun CAI
Progress in Biochemistry and Biophysics 2009;36(8):1064-1070
Temporins are a kind of small,hydrophobic and C-terminus amidated antimicrobial peptides from Rana species.They are effective against bacteria,fungi,yeast,protozoa and viruses.Two novel temporins named as temporin-La(LLRHWKILEKYLanifc) and temporin-Lb(LFRHVVKIFEK.Ylamid.) were cloned from Lithobates catesbeianus.Synthetic peptides of temporin-La and temporin-Lb showed strong antimicrobial activities against bacteria tested,especially Gram-positive bacteria.Besides,temporin-La showed no haemolytic activity to rabbit erythrocytes at the concentration of 250 mg/L while temporin-Lb showed weak haemolytic activity(LC50≈ 230 μmol/L).Transmission electron microscopy showed that temporin-La and temporin-Lb induced different effects on bacterial structure of Staphylococcus aureus.
9.Synergistic effect of atorvastatin and probucol on severity of coronary lesion in patients with borderline coronary lesion
Changjiang GE ; Shuzheng Lü ; Hong LIU ; Lixia FENG ; Xiantao SONG ; Xin CHEN ; Kang MENG ; Fei YUAN ; Fengqing JI ; Yong HUO
Chinese Journal of Emergency Medicine 2012;21(3):277-281
Objective To study the changes of plasma cystatin C level (PcyC),and evaluate the effects of the joint use of atorvastatin and probucol on PcyC and severity of coronary lesion in patients with borderline lesion of coronary artery.Methods One hundred and thirty consecutive patients with borderline coronary lesion assessed by quantitative coronary angiography were enrolled into borderline coronary lesion group (BCL),and another 136 subjects without coronary lesion were enrolled as controls (CTR).And in the meantime,the subjects in BCL group were randomized (closed envelope method) into routine treatment subgroup ( RTT,n =60),and combined treatment subgroup in which patients were treated with atorvastatin 20 mg plus probucol 1.0 g daily in addition to routine medication ( CBT,n =70) for 6 months.There were no statistical differences in basic clinical features between two subgroups.PcyC,high-sensitive C-reactive protein (hs-CRP),total cholesterol (TC),low-density lipoprotein cholesterol (LDL-C),high-density lipoprotein cholesterol ( HDL-C ) and triglycerides (TG) were determined.Of them,104 patients in BCL group rechecked by coronary angiography.Comparison of biomarkers carried out between two groups by using a number of independent-sample t-test and analysis of variance.For enumeration data,chi-square test was used to compare mean values of biomarkers between groups. P < 0.05 was considered statistically significant.Results PcyC levels were significantly higher in BCL group than those in CTR group ( P < 0.05 ).Compared with RTT subgroup,levels of PcyC,TC,LDL-C,TG and hs-CRP were more significantly decreased in CBT subgroup (P < 0.05,P < 0.01 ).Moreover,there was a trend of slight decrease in the mean percent of stenosis (MPS) of coronary artery with borderline lesion in RTT subgroup treated for 6 months,whereas more marked decrease in the MPS of coronary artery with borderline coronary lesion in CBT subgroup treated for 6 months ( P > 0.05 ; P < 0.05 ).Conclusions Cystatin C plays an important role in the pathogenesis of coronary artery,and PcyC is associated with severity of coronary lesion,the combination of atorvastatin and probucol decreases the PcyC level,and it may be the treatment of choice for borderline lesion of coronary artery.
10.Posterior debridement, interbody fusion, internal fixation for treatment of lumbar discitis.
Lin CHEN ; Jun CHENG ; Bo LI ; Fang-Biao ZHAN ; You ZHANG ; Shi-Long FENG
China Journal of Orthopaedics and Traumatology 2017;30(5):475-478
OBJECTIVETo evaluate the clinical effects of posterior debridement, interbody fusion with internal fixation in the treatment of lumbar discitis.
METHODSThe clinical data of 13 patients with lumbar discitis treated from January 2005 to June 2012 was retrospectively analyzed. There were 9 males and 4 females, aged from 31 to 68 years old with an average of 56 years old. There were 2 cases on L3, 4, 4 cases on L4, 5, and 7 cases on L5S1. Two cases complicated with diabetes, 4 cases with hypertension, and 1 case with obsolete pulmonary tuberculosis. ESR level of 13 cases was 12-89 mm/h with an average of 42 mm/h; and C reactive protein fluctuations level was level 8-114 ng/L with an average of 47 ng/L. All the patients denied history of operation or injection, and the main symptom was severe pain and limitation of motion in lumbar, with no efficacy for conservative methods. Preoperative VAS was from 5 to 10 points with an average of 7.8 points. All patients were treated with posterior debridement, interbody fusion, and internal fixation.
RESULTSAll the patients left hospital after wound healing, and the effective antibiotics were continuously used for 4 weeks intravenously and 2 weeks for orally. All patients were followed up from 7 to 24 months with an average of 18 months. VAS decreased for 0-1 point. No internal fixation breakage, and recurrence were found. Bone graft got fusion, and postoperative pathology showed phlogistic changes.
CONCLUSIONSOne-stage posterior debridement, interbody fusion with internal fixation was an effective method in treating lumbar discitis, and it lead to quicker relived pain relief and earlier mobilization.