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    中药及天然药物
  • 中药及天然药物
    Taxane diterpenoids from leaves and stems of Taxus yunnanenses
    Yue Qin;Fng Qicheng;Ling Xiotin;He Cunheng
    1995, 30(S1): 1-3.
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    22 taxane diterpenoids were obtained from the leaves and stems of Tax us yunnanensis Cheng et L.K.Fu by CC.VLC. PTLC.MPLC,and HPLC chromatographic methods. Their structures were elucidated by FAB-MS,UV, 1R ，lH ,13C—NMR ,1H— 13C COSY,1H-1H COSY.HMBC and NOE spectra and X-ray crystallography. Five of them were new compounds and named taxin B( I ) , 2-deacetyl-taxin B(Ⅱ),taxayuntin E,F and G (Ⅲ～V),respectivcly.The remaining were known as taxoids including taxol,cephalomannine,10-deacety]-7-epi-taxol, 10-deacetyl-7-epi-cephalomannine. baccatin Ⅲ,10-deacetyl-baccatin Ⅲ,19-hydroxy-baccatin Ⅲ.taxagifine,I-hy-droxy-baccatin I.l-hydroxy-5-deacetyl baccatin I , 2-deacetoxy taxinine J,5-decinnamoyl-taxinine J.baccatin VI，taxicin, 7-xylosyl-10-deacetyl taxol,7-xylosyl-10-deacetyl cephalomannine and 7-xylosy 1-10-deacetyl taxol C.They included three skeleton types of taxanes (6/10/6,6/8/6 ,5/7/6),assignable to 7 subtypes.
  • 中药及天然药物
    The Comstituents of polysaccharide RCL from Rubia cordifolia
    Hung Rongqing;Wng Zuohu;Wng Hongxi;Wng ingji;M Chengyu
    1995, 30(S1): 3-5.
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    Polysaccharide RCL was obtained from Rubia cordifolia L.After conversion of the hydrolysates of RCL into aldononitriles acetylated derivatives,the components of RCL were identified by GC.The components of RCL includes rhamnose,arabinose,xylose, mannose,glucose and galactose in molar ratio of 1.0:0.31:0.46:0.25:0.42:1.05.
  • 中药及天然药物
    The isolation and structures of przewalskinic acid B and C
    Lu Xuezho;Xu Wenho;Shen Jixing
    1995, 30(S1): 5-6.
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    From the roots of Salvia przewalskii Maxim,two new phenolic acids,przewalskinic acid B(1) and C (Ⅱ)were isolated. Through the extensive analysis of spectras,their structures were elucidated as ?-isoferuloxyl-malconic acid(I) and a-feruloxylmalconic acid(Ⅱ).
  • 中药及天然药物
    Raising the yield and quality of oriental water-plantain rhizome
    Xie Zhenli
    1995, 30(S1): 6-8.
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    Oriental water-plantain rhizome has a liking for sunlight temperature of 16～20'C and humid soil. It matures in 160 days. Our city has a oceanic climate with a mean temperature of 21℃,the coldest being 15—C ,and rich sunlight. We transformed the summer,autumn seeds in winter because there were a lot of unoccupied field in winter. We had a higher per mu yield from 100 to 300 kg.At the beginning of winter,varieties of oriental water-pharntain rhizome were planted in good soil which was given 1500 kg night-soil,100 kg compound fertilizer 2～3 days after the rice had been harvested. The seedlings in 38～45 days were provided a shed in nursery garden given by water to make the temperture drop.The seedilings were transplanted to the field shallowly 6000 pears per mu. After 15～20 days，straw needed to cut,followed by water shallowly.Three times of urea were given to them every 20 days after transplanting:7.5 kg,15kg and 25 kg. And diseases and pests were avoided.Collected in 115 days, they were simmered for 2 days,turning over every 24 hours.After 3 days they were simmered again and sheded.So the medicine oriental water-plantain rhizome was prepared.
  • 中药及天然药物
    The measures for exporting ginseng to inicrease foreign exchaege
    Tng Xio jun
    1995, 30(S1): 8-11.
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    Ginseng is an important drug for exporting to increase foreign exchange. Through investigations,on problems of Ginseng export,the author put forward measures such as system of Ginseng export,quality,development of production,protection of wild resoures,publicity,etc.
    • 药理
  • 药理
    The hypoglycemic effect of insulin oral microspheres in alloxan-treated diabetic rabbits
    Wng Siling;Su Desen;Zhng Jinghi;Yu Qin;Liu Yuln
    1995, 30(S1): 12-14.
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    The effectiveness of oral administration of insulin microspheres(IMS) was evaluated in alloxan-treated diabetic rabbits. Three doses were tested. The blood glucose levels were determined enzymatically by using the method of glucose oxidase. A significant difference in blood glucose level was noted after use of 6 u/20 g IMS when compared to control groups,and maintained for 5 hours.The hypoglycemic effect was linear with the doses of IMS within the range of 7.0u/20g～4.0u/20g. The findings may be of significance in the search for a suitable oral administration for insulin or perhaps other proteinaceous substances.
  • 药理
    Study of the serum with Sophora flavescens and Agrimonia pilosa on an-titumor activity
    Yu Shngci;Wng Liqin;Li Yikui;Li Yue
    1995, 30(S1): 14-16.
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    With the method of serum pharmacology,we studied the antitumor activity of the serum with Sophora flavescens Ait.(SFA) and Agrimonia pilosa Ledeb.(APL)-The results showed that the serum with SFA(S-SFA) could obviously inhibit the proliferation of S180and EAC cells in vitro.With the anti-staining method, we found that the S-SFA could inhibit EAC cells growth by 50.2% and the serum with APL(S-APL)by 1.5%;with the MTT assay , we found that when S-SFA was added and cultured with S180 and EAC cells for 3 days the percentage of cytotoxicity was 27.78%and 34.58% respectively,but the S-APL had no effect on S180 or EAC cells.Thesa experiments suggest that SFA has significant antitumor activity.
  • 药理
    Cigarette smoking does not enhance the metabolism of phenacetin,a marker of CYPIA2 activity,in Chinese healthy volunteers
    Sun Xiodong;Zhng Zhiping;Chen Chongshu;Zhou Zexiu;Yng Zhiwei
    1995, 30(S1): 16-18.
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    Cigarette smoking has been reported to induce cytochrome P450IA2(CYPIA2) activity in a population of white subjects.Many pharmacogenetic investigations found remarkable ethnic difference between orientals and Caucasians in oxidative metabolism,e.g. CYPIA2,of a lot of drugs.To clarify whether cigarette smoking increase the activity of CYPIA2 in Far Eastern populations,the effect of smoking on the kinetics and metabolism of phenacetin,an in vivo marker of CYPIA2 activity,was examined in 15 Chinese healthy volunteers(controls 8 and cigarette smokers 7).after a single oral dose of 900 mg phenacetin.The pharmacokinetic parameters of phenacetin in the smokers were very similar to those observed in the controls group.The only significant difference was a 30. 9% lower area under the curve(AUC)in the smokers.It is concluded that although cigarette smoking induced the metabolism of phenacetin in Caucasians.at the"dosage" of 10 cigarettes daily .smoking has little inducing effects on the activity of CYPIA2 in Chinese. This conclusion.however,did not rule out the possibility that at the higher"dosage" of cigarette,smoking might have the inducing effects on the activity of CYPIA2 in orientals.
  • 药理
    Anti-allergic effects of thymic immunosuppressive extract
    Shng Xueyun;Zhng Shiling;Jio o;Cheng Ynn;Lu Fengyou;Ji Jino;Wng Fengshn
    1995, 30(S1): 19-20.
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    The anti-allergic effects of thymic immunosuppressive extract from swine thymus were studied.The results showed that the extract shortened the diameter of blue spot of passive cutaneous anaphylaxis in rats and inhibited in vitro the anaphylactic contraction of guinea-pig ileum smooth muscle.The IC50 was 446.7mg/L.The extract also suppressed arthus reaction in rabbit.
  • 药理
    A computer-aided procedure and tracking technique for measuring water-maze performance
    Liu Xinmin;Chen Shngung;Meng Hui;Wng Shengping;Shng Weifng;Yu Shuren;Wng Li-wei;Su Shungning;Xio Peigen
    1995, 30(S1): 21-23.
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    Using computer-aided control and video-tracking techniques to screen and study new drugs in animals has been forging rapidly. We applied those techniques to develop a computer-aided system for measuring water-maze performance. mainly spatial learning in the rat and mouse. The program utilized the video-tracking capabilities to measure the subject's attempt to search out the goal platform in square water-maze.The software in the system was designed in modularity and programmed with C++ language. The interfaces were designed as user friendly.The functions included,but not limited to:allowing the users to collect data including number of entries into culs de sac (which is scored in terms of number of errors);the latency period to reaching the goal;the learning in-dex (LI = total number of correct responses/total number of correct responses+total number of error responses.) and the swimming speed;providing hardcopy of screen graphics and results by various printers ;data file saving in and loading from hard disk and floppy disks,a unique approach to scientific data analysis.The computer-aided system made information refined as much as possible and guaranteed experimental results more scientific and reasonable.
    • 药剂
  • 药剂
    Development of nifedipine pellets with a high bioavailability
    Lu Weigen;Zhng Yn;Xiong Qunmei;o Yongchu;Sheng Qing;Chen Qinghu
    1995, 30(S1): 24-26.
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    A new technique was introduced to prepare nifedipine(NF) pellets by spheronization of solid disper- sion of NF and PVP. The characteristics of NF pellets in vitro and in vivo were studied. The dissolution rates of NF pellets. and regular NF tablets in market were 80% and≤5% respectively. The pharmacokinetics of the two prepa- ration. in humans showed that the AUC of NF pellets was bigger than that of the tablets significantly. The relative bioavailability of NF pellets was 196%.
  • 药剂
    Effects of different phospholipids on liposomal preparation
    .Yin Chunhu;M Liren;M Chengyu;.Liu Guojie
    1995, 30(S1): 27-29.
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    A high performance silica gel G plate was developed with chloroform-methanol-water-acetic acid(45:15:2:0.2).7% phosphato-molybdic acid was used as development agent and the detection was at 670 nm.The method was used to separate the components of three soyabean phospholipids from different factories in China and one imported egg phospholipid. The proliposomes which contained different phospholipids were prepared by the carrier disposition of membrance respectively,and the effects of four different phospholipids on liposomal forming, structure and entrapment efficiency were studied. The effects of the main component such as phos-phatidylethanolamin (PE) and phosphatidyl-inosine(PI)on liposomal forming and entrapment efficiency were marked. In contrast to PE and PI,phosphatidylcholine(PC)and lysolecithin(LPC)had no effects on them.Liposomal forming and high entrapment efficiency had nothing to do with the purity of phospholipids.
  • 药剂
    New pharmaceutical preparations——osmotic pump controlled release tablets
    Zhung Dinyou;Pn Weisn;Chen Dwei;Chen Jimin
    1995, 30(S1): 29-32.
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    Formula and preparation methods of albutorol sulfate osmotic pump controlled release tablets were studied by orthogonal design test,and in vitro dissolutions of the prepared tablets were determined by HPLC in 0.9% NaCl solution. The results showed that the prepared tablets presented a good characteristics of zero order kinetics in 8 hours,and the average release rate was 0.86mg/h.The results of study met the experimental purposes and laid a foundation to some extent of the development and application of albutorol sulfate osmotic pump controlled release tablets.
  • 药剂
    Preparation and solubility of coprecipitates of miconazole nitrate with polyvinylpyrrolidone
    .Xu Lijun;.Wei Shicho
    1995, 30(S1): 32-34.
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    The coprecipitates of miconazole nitrate (MCZ) with polyvinylpyrrolidone(PVP) are prepared by solvent method. Orthogonal experimental design was used in the synthesis of MCZ-PVP complex for optimization of the reactive conditions. The study showed that MCZ and PVP(1:12 ) were dissolved respectively in methylalco-hol. and mixed and heated for 15 minutes ,the coprecipitatc formed. The solubility of MCZ in coprecipitate was about 6. 2 times higher than the pure MCZ. X-ray differaction spectrum of 1:12 coprecipitate showed no crystalline structure of MCZ. MCZ was dispersed molecularly in the carrier of PVP.
  • 药剂
    The making of the solution of increasing pH values progressively and observation of the dissolution of ibuprofen sustained release preparation
    Du Qing
    1995, 30(S1): 34-36.
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    A new solution of increasing pH values progressively(H3P04 + HAc +H3B03+NaOH) was made and used in the dissolution test of oral sustained release preparation. With the increasing of dissolution time,the solution's pH values increased progressively and conformed to those,in the gastric and intestine juice.The dissolution test of ibuprofen sustained release preparation showed that the solution of increasing pH values progressively can reflect the changes of drug dissolution rate according to the pH values.
  • 药剂
    Effect of some penetration enhancers on physical structure of the nude mouse skin
    Yng Wenzhn;Zheng Junmin
    1995, 30(S1): 36-37.
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    Effects of some penetration enhancers ,azon.oleic acid or poloxamer 188,on the physical structure of nude mouse skin were investigated with the help of transmission electron microscopy. Azone and oleic acid could make the stratum corneum more loose.enlarge the cellular distance and increase the lipid fludity,on the other hand.poloxamer 18 8mainly interacted with corneum protein leading to the folding of stratum corneum.
  • 药剂
    Partial inclusion of the outer molecular sphere of carboplatin by a-CD
    Liu Weiping;Xiong Huizhou;Yng Ytkun;Pu Shoping
    1995, 30(S1): 38-39.
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    Inclusion action of the gviest carboplatin by a-cyclodetrin(a-CD)was studied.The results showed that the cyclobutyl group of the guest molecule enters the a-CD cavity under the intermolecular force.forming 1:I adduct,and that the inclusion can increase the aqueous solubility and stability，but has no influence on the coordination structrue of carboplatin.Therefore,a-CD is expected to be a new drug carrier of carboplatin.
  • 药剂
    Physical stability of w/o/w type multiple emulsion containing ammonium glycyrrhizinate
    Go Xioli;Sun Dinji
    1995, 30(S1): 39-41.
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    The physical stability of w/o/w type multiple emulsion containing ammonium glycyrrhizinate was assessed by several methods including centrifugation,storage in varions temperature,measurement of electrical conductivity.
    • 临床药学
  • 临床药学
    Pharmacokinetic interaction between diltiazem and metoprolol in healthy volunteers
    Yin Qiping;Wng HongtU;Zhng Jillghu;Shi Xiojin
    1995, 30(S1): 42-45.
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    The pharmacokinetic interaction between diltiazem and metoprolol was investigated in six healthy volunteers in a randomised and crossover way.Serum concentration of metoprolol .diltiazem and its active metabolite deacetyldiltiazem were determined by reversed phase HPLC. Mobile phase consisted of methanol-water-O.03 mol/L ammonium acetate-dichloromethane-triethylamine (65:25:5:5:0.5),and the wavelength was as follows :0～4 min (254 nm ) ?4～6 min (280 nm)i6～9min(238nm)；9～12min(254 nm).The calibration curves of metoprolol.diltiazem and deacetyldiltiazem were all linear in the range from 10 ng/ml to1000ng/ml and their analytical recoveries were 96.80%～100.76%,98.56%～100.26% and 99.49%～101.76% respectively.RSD of in-tra-day analysis and inter-day analysis were within 10% for the three. Self pair t-xest,showed that after coadministration.T1/2(ka)of metoprolol was shortened，T1/2(5)was prolonged,and Cl(s)was reduced significantly.Both cmex and AUCo～∞were increased evidently.T1/2(5) of diltiazem was shortenend, while cmax and AUCo~∞, of deacetyldilti-azem were augmented evidently. The results showed that diltiazem may accelerate the absorption rate of metoprolol and inhibit its metabolism in liver.Metoprolol may also have an effect on the elimination of diltiazem .especially on its deacetylation course.It is essential for physician to monitor drug concentrations when the two drugs are coadministered,and in some cases,dosage should be adjusted or administration design should be revised to avoid adverse effect.
  • 临床药学
    The effect of oral cisapride on the absorption of cyclosporine
    Hung Chunming;Lu Jixing;Lu hio;Dn Ming;Zhu Cijun;M Yujie
    1995, 30(S1): 45-47.
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    The effect of coadministered oral cisapride on the absorption of oral cyclosporine was studied in kidney transplant patients. The whole blood cyclosporine levels were analyzed by HPLC.Pharmacokinetic parameters were calculated with PKBP-N1 program and compared by paried test.The results indicated that steady state of multiple dosage oi cisapride did not affect the absoption of cyclosporine and its single dosage.KEY
  • 临床药学
    Pharmacokinetics of theopmyllini modesteliberantes in healthy volunteers
    Zhng Yun;Lio Shuqing;Wng Yiling;Cheng Huiqin;Zheng Xiuqin;Wu Yuin
    1995, 30(S1): 47-48.
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    Pharmacokinetics of oral theopmyllini modesteliberantes was studied in six healthy volunteers.Each volunteer was given theopmyllini modeste-liberantes tablets in single dosage of 500mg alternatively.The serum drug concentration was determined by TDx.The data were disposed by PKBP-Nl pharmacokinetic program. The characteristics of pharmacokinetics shown as single compartment model and the main pharmacokinetic parameters were as follows:T1/2:13.04±7.12h，Ka:0.32±0.15,Tmnx6.88±1.97h,cmax:10.62±1.13.
    • 药品检验
  • 药品检验
    The measurement of RP-HPLC behaviour of two hundred of drugs and the establishment and application of their databases
    Ling Guijin;Zhu Li
    1995, 30(S1): 49-51.
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    The chromatographic behaviours of about two hundred of drugs were investigated under reversed-phase condition using methanoI-water system of more than 40 different pH values as elucnts. The capacity factors of these drugs were measured on several ODS columns. In terms of the characterization of retention values as function of the mobile phase pH ?the drugs were divided into three classes ： basic.acidic and neutral. The elution order reversal was frequently encountered with basic drugs within pH4～5. The database program was written by using the languages of Foxbnse +2.1 and of Foxpro 2.5 for windows.The databases and the classification might play important roles in the recognition of the trends of chromatographic behaviour of these drugs and the determination of initial chromatographic condition and reduce analysis time and efforts.It may help us to obtain the optical separation results ano to select the best internal standards.
  • 药品检验
    Dissolution of calcium supplements
    Mei Dn;Li Dkui;Png Gnohui
    1995, 30(S1): 51-54.
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    The dissolution of calcium preparations in water and 0. 1 mol/L HC1 medium was determined by complexometric titration.The results showed that the dissolution of tablets calcium gluconate.lactate and carbonate were in consistentr with regulations of ChP 1990 or USP XXⅢ,but the dissolution of some chewing tablets, capsule were lower than 55%.
  • 药品检验
    Determination of bufogenin in Bufo venom and its preparations by RP-HPLC
    .Peng Jin;.Guo Xinqing
    1995, 30(S1): 54-56.
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    A RP-HPLC method was established for the determination of bufogenin in Bufo venon(Chansu) and its preparations. The mobile phase consisted of a mixture of CH3OH-H2O(60:40), The flow rate was 1 ml/min. The detection was at 299 nm and no internal standard was used. Linear calibration curve for bufogenin was measured with a rang oi 19. 3 to 96. 5 μg/ml. With the correlation coefficient of 0.9996,the RSD of within-day and day to day was 1.26% and 4. 66% respectively.The method is simple,fast and accurate.
  • 药品检验
    Determination of carbamazepine and its metabolites in plasma by reverse-phase high-performance liquid chromatography
    Wei Jin wen;Chen Sholin;Li Rmihu
    1995, 30(S1): 56-57.
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    A high performance liquid chromatographic method for the determination of carbamazepine and its metabolites 10,ll-epoxycarbamazepine and 10,ll-dihydro-10,11-trans-dihydroxycarbamamazcpine in plasma was devloped. Methanol and water were used as mobile phase-The wave-length of UV detector was 210 nm. The lowest detective concentration of carbamazepine,10.11-cpoxycarbamazepine and 10>ll-dihydro-10,11-trans-dihydroxycar-bamazepinc was 0.02,0.04and0.05pg/ral respectively. The recovery was95.72%±1.04%,96.86%±1. 21% and 96.63%±1.08% repectively.The wlthin-day and between-day precisions were all less than 3% and 4%,respectively.
  • 药品检验
    Determination of propranolol hydrochloride in serum by HPLC with flu-orescence detector
    .Zhng Hui;Yu Chen;Hong Youci;.Chen Qiucho;Chen Weili;Li Xuening
    1995, 30(S1): 57-60.
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    To 1.0 ml of serum containing propranolol hydrochloride were added verapamili hydrochloridum(internal standard,IS) and 0.1 ml of 2.0mol/L NaOH. The mixture was extracted with diethyl ether for 2 times.After extraction,the combined organic phase was evaporated to dryness and the residue was dissolved in the mobile phase and washed with peyroleum ether. After centrifugation,20ul of the lower layer was subjected to HPLC.A YWG-C18(10μm)column(200mm×5mm) was used and the column temperature was kept at 50'C.The flow rate of mobile phase[methanol-20 mmol/L NaAc buffer(pH4.5)-HAc-DA=50:48.7:0.7:0.6]was1.0ml/min. Excitation and emission wavelengths were set at 290 and 340 nm.The retention times of propranolol hydrochloride and IS were 7.1 and9.9min respectively. The detection limit of propranolol hydrochloride was 10pg(S/N≥4:1). The extraction recoveries of propranolol hydrochloride and IS were ever 92%. The relative standard deviations of within-day and between-day were1.37%～2.48%and1.10%～5.70%(n=6)respectively.
  • 药品检验
    In vitro/in vivo correlation study of nicardipine sustained release tablets
    Qi Meiling;Sun Ynli;Yo Lin;Zheng Junmin;Zhng Ruhu
    1995, 30(S1): 60-62.
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    Nicardipine sustained release tablets(NC SR)given orally released the drug gradually, prot\：'J nearly constant blood level,and extended the drug efficacy.Based on the results of in vitro dissolution and in vivo absorption,we investigated the IVIVC of NC SR. The dissolution tesi was proceeded on ChP 90(I),method I.The standard curve was linear at the concentration range from 0.5fig/ml to16μg/ml.The regression equation was A =-2.07X10-3+4.74×10-2c(r=0.9999,n= 6).The nicardipine levels in haman plasma were determined by RP1P-HPLC The linear concentration range for this method was 2. 5～160ng/ml.The regression equation was A=2313+130.1c(r=0,9995,n=6). The limit of quantitation was 2.5ng/ml.The relative average recovery was74.44%.The witliin-day RSD was3.8%(n=5)，the between-day RSD was6.2%(n=5).The IVIVC regression equation was F=9.19+0.913f(r=0.9465>n=5).The significant correlation between in vivo absorption and tn vitro dissolution was validated by correlation coefficient test(P<0. 05).
    • 药物化学
  • 药物化学
    Synthesis of analogues of huperzine A
    Wu ogen;i Donglu
    1995, 30(S1): 63-66.
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    Huperzine A,a new alkaloid isolated from Huperzia serata (Thumb.)Trev =Lycopodium serrat Thumb,has been found to be a potent acetycholinesterase inhibitor.Since a deficiency of acetylcholino in the central cholinergic system is believed to constitute one of the hallmarks of Alzheimer's dementia, reversible inhibitors of AChE that can enter the central nervous system may serve as palliative agents in the treament of this disease.Huperzine A has been shown to improve rat memory and to help alleviate, the memory problems of aged individuals with Alzheimer's dementia in clinic trials. In our study on structure-activity relationships of huperzine A and search for the drug on the treatment of Alzheimer's disease,six analogues with the pharmacophoric moiety of both acetylcholine and huperzine A.compounds(2),(3),(4),(5),(6)and(7),have been prepared. All analogues were tested for their inhibitory activities of acetylcholinesterase from rat erythrocyte membrane. None of them has yet achieved the activity of the natural huperzine A.
  • 药物化学
    Conformation-activity relationships of dibenz;[b,e]oxepin/dibenzo[b,e]thiepin hydroxycarboxylates
    Go Shouhi;Yun Liuhong
    1995, 30(S1): 66-68.
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    The prefercd conformations of ciibenz[b,e] oxepin/dibtinzoL[d,e]thiepin hydroxycarboxylates were determined by using the met hod of systematic conformation search and quantum chemisuy AM1 calculation On the basis of the conformations of the tricyclic compounds and their pharmacological results.we discussed their confor-mation-activity relationships, and proposed that it would be favourable to forming hydrophobic action between these compounds and the receptor if the two benzene rings in the tricyclic hydroxycarboxylate anticholinergecs werc close to parallel.The increase of the dihedral angle between the two benzene rings or the replacement of oxygen atom with sulfur atom in the cycle would decrease thei:anticholinergic activities.We suggested that the active con-formations of non-tricyclic compounds be different from their prefered conformations.
    • 生物工程
  • 生物工程
    A novel nucleoside transport inhibitor derived from fungus reverses multidrug and the resistance to apoptosis in cancer cells
    Di Jie;Zhen Yongsu
    1995, 30(S1): 69-71.
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    Antibiotic C3368-B(CB),a new nucleoside transport inhibitor.is produced by a fungus strain from a soil sample collected in Antarctica. In this study the new nucleoside transport inhibitor was used for reversing multidrug resistance and the resistance to apoptosis in cancer cells. By MTT assay,combined with CB(20 umol/L) ,the IC50 of adriamycin (ADM) for human breast cancer cells (MCF-7/ADM) was reduced from 14. 5 umol/L. to 4. 0 umol/L.and by clonogenic assay,from 4. 0 umol/L to 0. 7 umol/L. CB(20 umol/L) enhanced the ADM uptake in MCF-7/ADM cells,The ADM level in MCF-7/ADM cells increased from 1.7 ug/107cells to 3.0 ug/107 cells after 1 h exposure to CB.However,little effect on ADM level was found in- MCF-7 cells. By flow cytometry,CB(20 umol/L) reduced the efflux of daunomycin (DNM) and increased its retention in MCF-7/ADM cells.CB(20umol/L) also increased the fluorescence intensity of DNM in MCF-7/ADM cells and promoted the redistribution of DNM from the membrane to the nucleus. As shown by RT-PCR assay.CB(20umol/L) reduced the enhanced mdr-1gene expression in MCF-7/ADM cells after 3～7 days of treatment.Examined by DNA electrophoresis,nuclear morphology and flow cytometry,CB(20(umol/L)reversed apotosis resistance in MDR cells.These results suggest that CB is a new type of biochemical modulators reversing MDR and the resistance to apoptosis.
  • 生物工程
    Enhancing plasma fibrinolytic after t-PA gene transfer
    .Cui Ning;Hn Qinqin;Chen Hozhu;.Lin ing;Peng Luying;Song Houyn
    1995, 30(S1): 71-74.
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    The method of direct injection of nude plasmid DNA into skeletal muscle and myocardium is sufficient to perform gene transfer in vivo. However,foreign gene expression was limited to the local site of DNA injection.It is difficult to produce a system therapeutic effect.The objectives of the present study were:(a)to test the feasibility of gene transfer via subcutaneous tissue;(b)to study whether protracted expression of DNA persists after gene transfer;(c)to determine the minimum DNA amount which is able to express significantly recombinant t-PA in plasma. The expression plasmids containing t-PA cDNA were mixed with transaction solution.Kunming mice were injected with the mixture via subcutaneous tissue.The mice were segregated into 6 groups according to the materials and amount of recombinant plasmid injected.The t-PA activity in plasma was measured by using a synthetic-peptide substract S-2390.Injection with 40 /ig of DNA yielded a statistically significant(P<0.05) increase in t-PA activity. The peak of t-PA activity(3.63±0.24 U/ml)was on the tenth day after injection and slowly reduced subsequently.The t-PA activity was raised for 2 months.The simple method of injection of recombinant plasmid resulted in the significant increase of t-PA activity in plasma.It might be applied to the prevention and treatment of thrombosis diseases.
  • 生物工程
    The establishment and validation of E.coli recA/uvrB differential DNA repair test
    Wng Jicheng;Zhng Huijun;Qin tili
    1995, 30(S1): 74-77.
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    The E. coli recA/uvrB differential DNA repair test(E.coli DDRT) was first established and validated with 21 various compounds in China. The results showed that 13 were positive among 21 chemicals tested. The general concordance was 65% (13/20) with Ames test,80% (12/15) with E.coli DDRT(using different strains) results published in the literature,and 76. 5%(13/17) with animal carcinogenecity test. Among these compounds,4-aminophenol,catechol ,DES,thioacetamide were positive in E.coli DDRT but negetive in Ames test ,and conversely,4-AAF,benzidine ,CP,DMSO were negetive in E.coli DDRT but positive in Ames test.The reasons for this disagreement were discussed. The differential killing index (DKI) was caculated to quantitatively compare relative genotoxic potency among chemicals tested. These results suggest that the method established by now is practical and reproducible and can be applied to screen the mutageneeity of chemicals.
    • 药物与临床
  • 药物与临床
    Dengzhanhua injection for reversal of 22 cases of primary acute renal failure（addition typical case）
    Li Lixin;He Zhenhi
    1995, 30(S1): 161-162.
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    We studied 22 patients with primary acute renal failure，treated by Dengzhanhua injection. Patients's urine volume，serum creatinine·creatinine clearance，urine sodium，and index of renal failure had signficant chancges after Dengzhanhua injection．In all patients expect one who died of primary disease acute renal failure was markedly improved. It was showen that Dengzhanhua injection is significant is reversing primary acute renal failure.