1.Synthesis of N-acyl chitosan derivatives and investigation of chitosan-modified docetaxel liposomes in vitro
Liang GE ; Hai QIAN ; Hao GAO ; Yaojian CHENG ; Jiabi ZHU
Journal of China Pharmaceutical University 2009;40(6):519-523
Aim: Synthesized N-acylated chitosan(NAC) was used to anchor on the surface of plain docetaxel li-posomes( PDL) in order to to sustain drug release. Methods; NAC of low substitution degrees were prepared using hexanoic(C_6), lauric( C_(12)), and palmitic( C_(16)) anhydrides. W-palmitoyl chitosan was chosen to anchor the do-cetaxel liposomes. In vitro release profiles of conventional liposmes and the anchored liposomes was compared. Results: Hexanoic(C_6), lauric( C_(12)), and palmitic( C_(16)) -branched chitosans were synthesized. It was found that N-acylated chitosan-anchored DXL liposomes (NDL) increase stabilities of docetaxel liposomes. 70% of docetaxel was released from PDL in 24 hours but 39% from NDL Conclusion: Liposomes anchored by the low substituted N-acylated chitosan could decrease the drug release.
2.Comparison on constituents from different parts between wild growing and cultivated planting of Ephedra sinica
Hai WU ; Lunzhao YI ; Jingming GAO ; Xiangqian LIU ; Yizeng LIANG
Chinese Traditional and Herbal Drugs 1994;0(09):-
Objective To compare the difference in constituents from different parts of wild and cultivated Ephedra sinica. Methods Using the solvent of 50% methyl alcohol to extract from the stems and roots of wild and cultivated E. sinica under heating reflux, respectively and then determine the content of ephedrine in each extractions by HPLC. The volatile oil was extracted by stream-distillation and analyzed by GC-MS method. Results The content of the ephedrine in extraction of stems and roots of wild E. sinica was 0.55% and 0.000 57% while the content of the cultivated was 0.26% and 0.001 7%. Forty-five compounds in the volatile oil were identified by GC-MS method, among them 13 compounds existed in both wild and cultivated E. sinica. Conclusion The content of the ephedrine is about two times of the cultivated in wild E. sinica′s stems, while it is very low in the roots of two kinds of herbs. And ephedrine is not found in the volatile oil.
3.The evaluation of super-selective prostatic arterial embolization in the treatment of benign prostatic hyperplasia
Zhilei QIU ; Quan WANG ; Kai CHENG ; Daosheng SU ; Xin LIANG ; Hai ZHU ; Jiangang GAO
Chinese Journal of Urology 2016;37(10):758-761
Objective To evaluate the clinical efficacy of super-selective prostatic arterial embolization(PAE) for the treatment of benign prostatic hyperplasia(BPH).Methods From February 2012to March 2015,a total of 17 patients with BPH who failed in medical treatment,or unwilling to accept surgery were selected for PAE as the study group.The mean age was 73 years (range 61-84 years) and the mean prostatic volume was 64.6 ml (ranging 50-85 ml).The study group underwent super selective arterial embolization.The internal iliac artery angiography was performed and the main blood vessel of prostate was showed.The femoral artery was punctured under local anesthesia and X-ray monitoring,a F4-5 Cobra catheter was inserted,and then the Embosphere microspheres were implanted.A total of 40 patients who underwent transurethral resection of the prostate(TURP) were selected as the control group.The mean age was 70 years (ranging 59-87 years).The mean prostatic volume was 68.7 ml(ranging 55-90 ml).All cases were followed up for 1 year.The changes of prostatic volume (PV),international prostate symptom score(IPSS),quality of life (QOL),pre-and post-treatment peak urinary flow (Qmax) were evaluated.Results For the 17 patients who underwent PAE,the PV decreased from (64.6 ± 10.2) ml to(42.0 ± 7.5) ml,the IPSS decreased from 23.9 ±4.9 to 13.1 ±3.5,QOL decreased from 4.1 ±0.7 to 2.1 ±0.7,and Q increased from (9.5 ± 3.7) ml/s to(21.8 ± 4.2) ml/s,which were statistically significant (P < 0.05) compared with the pre-treatment parameters.The post-operative parameters of the control group were also significantly improved compared with the preoperative parameters (P < 0.05).Conclusions PAE is safe and effective in treating BPH,especially for those failing in medical treatment,or unwilling to accept surgery.
4.Optimization on Fermentation and Purification of the Fibrinolytic Enzyme from Stenotrophomonas maltophilia
Gao-Xue WANG ; Chao-Jun LIANG ; Hai-Hong HUANG ; Jian-Fu WANG ; Ju-Lin YUAN ;
China Biotechnology 2006;0(09):-
The optimization on liquid fermentation and purification of the fibrinolytic enzyme from Stenotrophomonas maltophilia(DR-929) was investigated.The results showed the best fermentation are amidulin 2.0%,soya flour 1.0%,yeast extract 0.5%,NaCl 1.0%,CaCl2 0.02%,MgSO4 0.05%,inoculum of 36 hours,fermental time 4d,initial pH 8.0 or 9.0,temperature 25℃,volume of media 30ml,volume of inoculum 5% or 6%.The purification process includes the following steps: removing cells by the centrifugation,25%~70% saturation ammonium sulfate precipitation,HIC with Phenyl FF(high sub),IEC with Q-Sepharose FF,gel filtration chromatography with Superdex 75.SDS-PAGE electrophoresis was used to examine the purification effect,and the results indicated that homogeneous strap in SDS-PAGE and has a molecular weight around 28.3kDa.The purification factor and activity recovery of the fibrinolytic enzyme are 271.5 and 24.5%,respectively.
5.Analysis of eight Murraya species by flow injection-Qtrap-mass spectrometry
Hai-zhen LIANG ; Shuo YUAN ; Peng GAO ; Peng-fei TU ; Yong JIANG
Acta Pharmaceutica Sinica 2023;58(8):2454-2460
In this study, the flow injection (FI) technology combined with the unique step wise multiple ions monitoring scanning (step-wise MIM) mode of Qtrap-MS was first established for the identification and discrimination of eight
6.Effect of iptkalim on myocardial enzymes and free radicals metabolism with hypoxic pulmonary hypertension.
Jian-Hua CUI ; Liang GAO ; Dong-Xiang ZHANG ; Zhong-Hai XIAO ; Hai-Jun YANG ; Bin LI ; Guang-Quan MA ; Hai WANG
Chinese Journal of Applied Physiology 2012;28(5):385-388
OBJECTIVETo explore the effects of iptkalim on myocardial enzymes and free radicals metabolism with hypoxic pulmonary hypertension (HPH), in order to provide evidence for the mechanism of iptkalim on clinical treat.
METHODS110 young men stayed at high altitude above 5 000 m were divided into iptkalim group (n = 74) and placebo group (n = 36), aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyltransferase (gamma-GT), creatine kinase (CK), lactate dehydrogenase (LDH), superoxide dismutase (SOD), malonaldehyde (MDA), nitric oxide(NO) and nitric oxide synthase(NOS) were detected before and after took medicines for 6 mouths.
RESULTSAfter took medication for 6 mouths, ALT, AST, gamma-GT, CK and LDH were reduced, SOD, NO, and NOS were increased, MDA were reduced, there were very significant difference (P < 0.05).
CONCLUSIONOxygen free radicals have taken part in the process of HPH, iptkalim have the effect of anti-peroxidation of lipid and protect myocardial cells stress injured by hypoxia which related with mitochondrial membrane and cell membrane's K(ATP) channel activation.
Adolescent ; Adult ; Altitude ; Creatine Kinase ; blood ; Free Radicals ; metabolism ; Humans ; Hypertension, Pulmonary ; blood ; etiology ; metabolism ; Hypoxia ; complications ; L-Lactate Dehydrogenase ; blood ; Male ; Myocardium ; enzymology ; Potassium Channels ; agonists ; Propylamines ; pharmacology ; Young Adult
7.The study of multi-detector CT on the grouping and measuring of the hepatic veins
Xian-Liang WANG ; Guang DONG ; Hai GENG ; Wen-Gang WANG ; Lin-Kun LI ; Wei GAO ; Rong-Fang WANG ;
Chinese Journal of Radiology 2001;0(07):-
Objective To study the three-dimensional topography of the hepatic vein(HV),the inferior vena cava(IVC)and the inferior right hepatic vein(IRHV)in the retrohepatic and pre-IVC tunnel in human beings,and to provide an anatomic reference for liver surgery.Methods One hundred and ten volunteers underwent CT scanning at 60 to 75 s after injection of contrast medium,and their HV,IVC and IRHV were reconstructed into MPR and 3D-MIP images.The hepatic veins were grouped according to the way by which the hepatic vein enters IVC.The angle between the right hepatic vein and the middle hepatic vein or the trunk of hepatic vein was measured,and the width from right hepatic vein to middle hepatic vein or to the trunk of hepatic vein on IVC was recorded.The frequency of IRHV was observed,and the length of the tunnel was measured.Results Among the 110 volunteers,there were 6 cases(5.45%)with three hepatic veins respectively entering IVC,98 cases(89.10%)with right hepatic vein and a common trunk of the middle hepatic vein and the left hepatic vein entering IVC,and 6 cases(5.45%)with left hepatic vein and a common trunk of the right hepatic vein and the middle hepatic vein entering IVC.The mean value of the angles between the right hepatic vein and the middle hepatic vein or the trunk of hepatic vein was(55? 18)?.The width from the fight hepatic vein to the middle hepatic vein or to the trunk of hepatic vein was (21?7)mm.The IRHV was observed in 30 cases(27.27%).The mean value of the tunnel length was (53?11)mm.Conclusion The parameters of the retrohepatic and pre-IVC tunnel in human beings can be measured accurately by the imaging of MPR,which can provide an anatomic reference for the liver surgery.
8.Study on the differences between moxibustion at different points in the effects on the anti-fatigue ability of rats undergoing one-time exhaustive swimming
Hai-Long LIU ; Lei GAO ; Ya-Hui ZHANG ; Yu-Lei LIANG ; Tian-Yuan LÜ ; Xin YANG ; Zhi-Guo ZHAO
Journal of Acupuncture and Tuina Science 2020;18(4):256-261
Objective: To observe the effects of moxibustion at Shenshu (BL 23), Zusanli (ST 36) and Shenque (CV 8) on the energy metabolism and endocrine metabolism indicators of rats undergoing one-time exhaustive swimming, and to explore the differences between moxibustion at different points in the effects on anti-exercise fatigue. Methods: Forty-eight male SPF rats were randomly divided into a blank group, a model group, a non-meridian and non-acupoint group, a Shenshu (BL 23) group, a Zusanli (ST 36) group, and a Shenque (CV 8) group using random number table method, with eight rats in each group. Except for the blank group, rats in the other groups were subjected to replicating the one-time exhaustive model using the weight-bearing swimming experiment. Except for the model group, the other model rats received mild moxibustion immediately after swimming. Rats in the non-meridian and non-acupoint group received mild moxibustion at bilateral subcostal non-meridian and non-acupoint points, those in the Shenshu (BL 23) group received mild moxibustion at bilateral Shenshu (BL 23), those in the Zusanli (ST 36) group received mild moxibustion at bilateral Zusanli (ST 36), and those in the Shenque (CV 8) group received mild moxibustion at Shenque (CV 8) for 15 min. Four hours after the exhaustive swimming, femoral artery blood was collected to detect blood lactate (BLA), lactate dehydrogenase (LDH), creatine kinase (CK), creatinine (CRE), blood urea nitrogen (BUN), cortisol (C) and testosterone (T) levels, and calculate the T/C ratio. Results: Compared with the blank group, rat's serum levels of BLA, LDH, CK, BUN and C in the model group and the non-meridian and non-acupoint group were increased, and serum levels of CRE and T, and T/C ratios were decreased (P<0.01 or P<0.05); compared with the model group and the non-meridian and non-acupoint group, the serum levels of BLA, LDH, CK, BUN and C in the Shenshu (BL 23) group, Zusanli (ST 36) group and Shenque (CV 8) group were decreased, and the serum CRE and T levels, and the T/C ratios were increased (all P<0.01); compared with the Shenshu (BL 23) group, the serum CK level was decreased in the Shenque (CV 8) group (P<0.01), the serum levels of T and C were decreased in the Zusanli (ST 36) group and Shenque (CV 8) group (P<0.01 or P<0.05), and the T/C ratio was increased in the Shenque (CV 8) group (P<0.01); compared with the Zusanli (ST 36) group, the serum CK and BUN levels were decreased (P<0.01, P<0.05), and the T/C ratio was increased in the Shenque (CV 8) group (P<0.05). Conclusion: Moxibustion at Shenshu (BL 23), Zusanli (ST 36) and Shenque (CV 8) shows different anti-fatigue effects by regulating the energy metabolism and endocrine metabolism in rats undergoing one-time exhaustive swimming. Moxibustion at Shenshu (BL 23) is better in promoting energy synthesis. Moxibustion at Shenque (CV 8) is more effective in regulating synthesis and decomposition of the skeletal muscle proteins.
9.Gene expression of tumor cells both in vitro and in vivo enhanced by integrin-targeting adenovirus vector.
Jian-qing GAO ; Hai-liang CHEN ; Shinsaku NAKAGAWA ; Hiroyuki MIZUGUCHI ; Wen-quan LIANG
Acta Pharmaceutica Sinica 2006;41(11):1116-1120
AIMTo construct an efficient recombinant viral vector for gene therapy.
METHODSFirst-generation adenovirus (Ad) vector was modified with the RGD peptide inserted into the fiber. Both in vitro and in vivo experiments of gene expression in different tumor cells with conventional and recombinant vectors were conducted. RT-PCR was used for detecting the expression of coxackievirus and adenovirus receptor and integrin at the surface of Meth-A cells.
RESULTSFiber-mutant adenovirus vector showed a notably enhanced gene expression in A2058, B16BL6, OV-HM, and Meth-A tumor cells compared with that of conventional ones. In vivo study carried out using Meth-A tumor-bearing mice also demonstrated that the intra-tumoral injection of recombinant adenovirus induced strong gene expression in these CAR-deficient tumor cells.
CONCLUSIONThe recombinant vector can be a promising one for effective cancer gene therapy.
Adenoviridae ; genetics ; Amino Acid Sequence ; Animals ; Base Sequence ; Cell Line ; Cell Line, Tumor ; Enterovirus ; genetics ; Female ; Gene Expression Regulation, Neoplastic ; Genetic Therapy ; methods ; Genetic Vectors ; Green Fluorescent Proteins ; genetics ; metabolism ; Humans ; Integrins ; genetics ; metabolism ; Luciferases ; genetics ; metabolism ; Mice ; Mice, Inbred BALB C ; Microscopy, Fluorescence ; Mutation ; Neoplasm Transplantation ; Neoplasms, Experimental ; genetics ; pathology ; therapy ; Oligopeptides ; genetics ; Receptors, Virus ; genetics ; metabolism ; Reverse Transcriptase Polymerase Chain Reaction ; Transfection
10.Preparation and release behavior of chitosan scaffolds encapsulating proteins loaded in PLGA microspheres.
Gang HAN ; Hai-Liang CHEN ; Xiao-Yi SUN ; Jian-Qing GAO ; Wen-Quan LIANG
Acta Pharmaceutica Sinica 2006;41(6):493-497
AIMTo prepare cells scaffolds with the characteristics of sustained release of proteins.
METHODSChitosan scaffolds was prepared by freeze-drying. Porosity and water content of scaffolds were determined. Bovine serum album (BSA) was selected as a model protein. Poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by double emulsion solvent evaporation and encapsulated into chitosan scaffolds. The morphology of PLGA microspheres and various scaffolds were observed using scanning electron microscope. Release behavior of BSA from various chitosan scaffolds was investigated.
RESULTSThe chitosan scaffold represents porous. At the -70 degrees C of quenching temperature, the porosity and water content of chitosan scaffolds were 78.6% +/- 1.5% and 85.1% +/- 6.2%, respectively. PLGA microspheres can be uniformly encapsulated into scaffolds without any morphology change. Significant sustained release of BSA from PLGA microspheres encapsulated into scaffolds was obtained. The cumulative release at 168 h was only 33.5%, while that of BSA from chitosan scaffolds at 24 h was above 90%. The release behavior can be controlled by adjusting the amount of chitosan in scaffolds and the type of PLGA.
CONCLUSIONThe novel chitosan scaffolds encapsulating PLGA microspheres proved to be a promising cells scaffolds with controlling the release of growth factors in tissue engineering.
Chitosan ; administration & dosage ; chemistry ; Drug Carriers ; Freeze Drying ; methods ; Lactic Acid ; chemistry ; Microspheres ; Polyglycolic Acid ; chemistry ; Polymers ; chemistry ; Serum Albumin, Bovine ; metabolism ; Tissue Engineering ; methods