目的:观察银杏叶提取物(GbE)对正常大鼠海马内caspase-3和β淀粉样肽原蛋白(APP)水平的影响.方法:不同年龄组大鼠灌胃给予GbE 100 mg/kg后14天,采用免疫组织化学染色、图象分析系统定量分析测定大脑海马区caspase-3和APP的表达情况.结果:在3个不同的年龄组大鼠的海马区,给予GbE 组caspase-3和APP水平均明显高于对照组.结论:GbE能提高大鼠大脑海马区caspase-3和APP水平,其抗阿尔采末病的意义值得进一步研究.
作者:罗璨;吴芹;黄燮南;孙安盛;石京山 刊期: 2003年第02期
目的:研究分离纯化的人参皂苷Rb2对牛主动脉内皮细胞(BAEC)纤维蛋白溶酶活性的作用.方法:使用底物发光试剂S-2403测定细胞内PA的溶解产物.血管内皮细胞表面纤溶酶活性的测定采用BAEC纤维蛋白的载体技术.用酶谱分析和还原酶谱分析法通过培养液来分析细胞产生的纤溶酶原激活物(PA)和纤溶酶原激活物抑制剂(PAI-1).用Northernblot分析uPA,uPA receptor和PAI-1的mRNA表达.结果:Rb2对于血管内皮细胞产生的PA活性的促进作用表现出剂量、时间依赖性.Rb210 mg/L对内皮细胞处理9小时后,血管内皮细胞的PA活性提高了2.5倍.培养液中LDH检测表明Rb2未表现出明显细胞毒性.纤维蛋白测定表明,PA水平的增加进而提高了纤维蛋白溶酶的水平.Rb2能够显著增加培养液中尿激酶型PA(uPA)和其拮抗物(PAI-1)的水平,但Rb2对于uPA,其表面受体(uPAR)和PAI-1的mRNA水平无影响,同时添加Rb21 mg/L能够显著增强维甲酸(RA 0.001-1 μmol/L)对PA合成的刺激作用.结论:Rb2能增加血管内皮细胞表面纤溶酶的活性,是通过促进血管内皮细胞纤溶活性因子的分泌而不是通过增强其基因表达起作用的.
作者:刘建文;魏东芝;杜长斌;钟建江 刊期: 2003年第02期
AIM: To distinguish the component difference between two similar herbal formulas by pulse analysis method.Many Chinese herbs were found to have specific effects on the Fourier components of the blood pressure pulse; itmight infer a specific blood redistribution process on the body and reflect the health conditions of specific organsor tissues. The pulse effect of an herbal formula was similar to the linear combination of all its herbal compositions.METHODS: Two different versions of the herbal formula Liu-Wei-Dihuang were fed to the Wistar rats as a singleblind test. The blood pressure pulses on the rat tail artery were recorded and then transformed to the frequencydomain by Fourier analyzer. RESULTS: Formula A, Bai-Wei-Dihuang, with two more herbs Cortex Cinnamomiand Radix Aconiti added to Liu-Wei-Dihuang, increased the harmonic proportion of the 1st harmonic (C1) butdecreased C4, C5. Formula B is composed in the same way but without Rhizoma Batatatis and Poria cocos; itincreased the DC of the pulse spectrum (CO), but decreased C2, C3, C4, C5, C6. CONCLUSION: The componentadjustment of an herbal formula could be distinctly and quantitatively detected by pulse analysis method.
作者:王唯工;徐则林;鲍建国;王林玉英 刊期: 2003年第02期
目的:研究表没食子儿茶素没食子酸酯(EGCG)增强阿糖胞苷(AraC)对人白血病HL-60细胞的抗肿瘤活性.方法:采用生长曲线法、MTT法测定细胞增殖;以流式细胞光度仪分析联合用药对细胞周期和细胞凋亡的影响;以对消实验研究EGCG能否逆转脱氧胞苷(dCdR)的补救作用;以Western blot和细胞内钙测定探讨EGCG和AraC联合作用的分子机制.结果:合并EGCG能增强AraC对HL-60细胞的增殖抑制作用,倍增时间从48 h延长到70 h,生长饱和密度从5.78减少到5.54;合并EGCG后,AraC抑制HL-60细胞的增殖,IC50从(0.34±0.29)μmol/L减少到(0.11±0.09)μmol/(P<0.05).AraC可使HL-60细胞阻滞于G1期,S期细胞减少,低浓度的EGCG对细胞周期几乎无影响,但增强了AraC的细胞周期阻滞作用及细胞凋亡作用;对消实验表明单用AraC的IC50为0.03μmol/L,加上dCdR后IC50为0.02 mmol/L,而在给予EGCG后IC50减少到4.8 μmol/L;EGCG可增强AraC引起的bcl-2蛋白表达的下调,进一步升高AraC引起的肿瘤细胞内Ca2+浓度的增加.结论:AraC合并应用EGCG可增强对人白血病HL-60细胞的抗肿瘤活性.
作者:徐峰;甄永苏 刊期: 2003年第02期
AIM:To study the structure-activity relationship of alkyl 9-nitrocamptothecin esters. METHODS: Two alkyl9-nitrocamptothecin (9NC) esters 5g and 5h were prepared by esterification reactions of 9NC with valeric anhy-dride and heptanoic anhydride, respectively. Eight 9NC esters 5a-5h were tested for cytotoxicity against humanleukemia cell lines HL-60 and U-937. Flow cytometry analysis was used to identify the cell cycle phase targeted bythe esters and quantify the extent of ester-induced cell death (apoptosis). RESULTS: Esters 5b and 5c demonstratedgreat abilities to inhibit growth of the leukemia cells followed by induction of apoptosis; esters 5a, 5e, and 5ginduced slight perturbations in the cell cycle at high concentrations; and esters 5d, 5f, and 5h were completelyinactive against the cell lines tested. Thus these esters showed the cell anti-proliferative activity in an order of5b≈5c>5a≈5e≈5g>5d≈5f≈5h. Esters 5b, 5c, and 5e were tested in vivo against various human carcinomas in nudemice grown as xenografts. Only 5b and 5c showed a significant antitumor activity. Particularly, ester 5b demon-strated an antitumor activity agalnst a broad spectrum of human carcinomas including breast, lung, colon, pancreas,stomach, ovarian, and melanoma, etc. CONCLUSION: These esters act like prodrugs of their parental9-nitrocamptothecin. High drug doses need to be administered to animals in order to inhibit growth, and induceregression, of human tumor xenografts in nude mice. These compounds may be developed into potent anticancerdrugs due to their low toxicity.
作者: 刊期: 2003年第02期
目的:观察川东獐牙菜(口山)酮对大鼠缺血再灌注损伤心肌的保护作用.方法:离体大鼠心脏全心停灌缺血20 min后再灌注40 min和在体大鼠通过结扎左冠状动脉前降支1h后再灌注3 h产生缺血再灌注损伤.离体心脏观测心功能(左室内压、左室内压变化大速率±dp/d tmax、心率)、冠脉流量,测定肌酸激酶(CK)释放量和心肌组织丙二醛(MDA)含量;在体大鼠观测心肌梗死面积和CK释放量.结果:(口山)酮(90和300 μg/L)能显著促进再灌注时心功能恢复,减少CK释放和降低MDA的含量.(口山)酮(0.5和1.0 mg/kg)均可显著缩小心肌梗死面积和降低CK浓度.结论:川东獐牙菜(口山)酮具有抗心肌缺血再灌注损伤的作用,其保护作用可能与抗脂质过氧化有关.
作者:姜德建;谭桂山;叶峰;杜艳华;徐康平;李元建 刊期: 2003年第02期
目的:研究蛇床子总香豆素(TCFC)对破骨细胞的作用,探讨其抗骨质疏松的作用机制.方法:采用原代培养的成骨细胞和骨髓单核细胞联合培养的方法,在1,25-(OH)2维生素D3和地塞米松作用下,使骨髓单核细胞分化形成破骨细胞.通过相差显微镜下的形态观察,抗酒石酸酸性磷酸酶染色和骨片上骨吸收陷窝的形成来鉴定破骨细胞.磷酸苯二钠法测定破骨细胞抗酒石酸酸性磷酸酶的活性,计算机图像分析技术测定骨片上破骨性骨吸收陷窝的面积,原子吸收光谱法测定破骨细胞和骨片联合培养的培养上清中钙的浓度.结果:蛇床子总香豆素(TCFC)2.5-25 mg/L抑制破骨细胞的形成和分化.TCFC 0.25-25 mg/L作用24-72 h,可以显著抑制抗酒石酸酸性磷酸酶的活性,TCFC 25 mg/L作用48 h和72 h分别可使其降低26.3%和24.1%.TCFC 25 mg/L可使破骨细胞在骨片上形成的吸收陷窝的面积减少25.05%,骨片中Ca2+的释放减少41.73%.结论:TCFC通过抑制破骨细胞的形成、抗酒石酸酸性磷酸酶的活性和骨吸收作用减少骨质丢失.
作者:秦路平;张巧艳;田野苹;郑汉臣;黄矛;黄宝康 刊期: 2003年第02期
目的:研究了静脉注射银杏叶提取物对大鼠四脑动脉阻断和大脑中动脉阻断时脑电的影响.方法:在利用FFT技术对脑电波进行定量分析的基础上,研究了银杏叶提取物对大鼠全脑缺血及大脑中动脉阻断时脑电的影响.结果:静脉注射8、16 mg/kg银杏叶提取物能显著增强全脑缺血大鼠在复灌后脑电图各波恢复,4 mg/kg也有作用但较弱.对大脑中动脉阻断模型,iv银杏叶提取物16、32 mg/kg能显著增强大鼠中动脉阻断后阻断侧的脑电图各波的功率谱.结论:银杏叶提取物可减轻大脑缺血造成的损伤.
作者:章蕴毅;李佩芬;李端 刊期: 2003年第02期
目的:探讨苦参碱(Mat)对大鼠原位肝移植冷缺血再灌注损伤的肝窦内皮细胞的保护作用及其机制.方法:应用大鼠原位肝移植模型,供肝保存5小时.1 26只大鼠随机分为对照组、Mat 40 mg/kg治疗组、Mat 80 mg/kg治疗组和假手术组,分别检测移植术后1、2、4小时血透明质酸及肝组织细胞间粘附分子-1的含量,并观察肝血窦内皮细胞形态学的改变.结果:与对照组比较,治疗组术后各时点的透明质酸和细胞间粘附分子-1表达均显著降低,肝血窦内皮细胞形态变化也有明显改善.结论:苦参碱在大鼠原位肝移植冷缺血再灌注中保护肝血窦内皮细胞免受损伤.
作者:朱新华;仇毓东;史敏科;吴波;郑晓刚;丁义涛 刊期: 2003年第02期
AIM: To examine the efficacy of Saenghyuldan and its components, Ginseng Radix, Paeoniae Radix Alba, andHominis Placenta extracts (SHD, GR, PRA, and HP, respectively) on the hemopoiesis in a myelosuppression modelsystem. METHODS: Susceptibility to cyclophosphamide (CP) and S 180 carcinoma was determined in SHD, GR,PRA, and HP-treated mice. Analysis of peripheral blood and bone marrow cells was demonstrated by changes incell types and histopathologic examination. The expression of cytokine mRNAs involved in hemopoiesis wasexamined by RT-PCR. RESULTS: SHD and its seperated components (GR, HP, and PRA, respectively) signifi-cantly increased the survival in CP- and S180-treated mice. The hematology data demonstrated that all the agentsaugmented monocyte and leucocyte counts in the peripheral blood and increased bone marrow density and the ratioof leukocyte to erythrocyte in the bone marrow. These findings were positively correlated with the up-regulation ofcytokine mRNA expression such as granulocyte colony-stimulating factor (GM-CSF), erythropoietin (EPO),thrombopoietin (TPO), stem cell factor (SCF), and c-Kit. CONCLUSION: SHD is an effective remedy for thebone marrow failure and myelosuppression occurring during chemotherapy.
作者: 刊期: 2003年第02期
AIM: To evaluate the therapeutic effects of Gamichunggantang (GCT) on hyperlipidemia through high cholesteroldiet model. GCT is an Oriental herbal medication, which has been used for the treatment of fatty liver, hyperlipi-demia or alcoholic liver disease in Daejeon University Oriental Hospital, Korea since 1999. METHODS:Rats werefed with high cholesterol diet for 4 weeks and GCT was administrated for 2 weeks from 2 weeks later in experi-mental days. The levels of serum total cholesterol, HDL-cholesterol, and triglyceride were analyzed every week.Absolute and relative liver weight to body, and histophathological changes were determined at last day. And, lipidmetabolism-related gene expressions (ACAT and DGAT) in liver tissue were analyzed by using RT-PCR. RESULTS:In GCT group, TG levels were reduced at 3 and 4 weeks after GCT administration (39.4 %, P<0.05 and 36.3 %,P<0.01 respectively). Total cholesterol levels also were reduced at 3 weeks (20.5 %, P<0.05) and 4 weeks (35.86 %,P<0.01) after GCT administration, but HDL-cholesterol levels were increased significantly (P<0.05) at 3 weeks(14.7 %) and 4 weeks (25.5 %) compared with hyperlipidemia-induced group without GCT. In the GCT treatedgroup, liver weight was lower and lipid accumulation was decreased in histological finding. ACAT gene expressionwas suppressed compared with hyperlipidemia-induced group but not DGAT. CONCLUSION: GCT possessespreventive or therapeutic effects on diet-induced hyperlipidemia by inhibiting the intestinal absorption and storage ofexogenous and endogenous cholesterol.
作者: 刊期: 2003年第02期
AIM: To study the anti-inflammatory effects of aqueous extract from Dichroafebrifuga root (AEDF) for suppres-sion in the process of lipopolysaccharide (LPS)-induced sepsis in the rat liver. METHODS: The inhibitory effect ofAEDF on the alteration of inflammatory proteins was investigated by Western blot and immunohistochemical analysis.RESULTS: Western blot analysis showed that the level of nuclear factor (NF)-κ Bp65 was markedly up-regulatedand (I)-κ Bα was down-regulated by LPS (8 mg/kg) challenge. However, AEDF 100 mg/kg inhibited induction ofNF-κ Bp65 and degradation of I-κBα in the liver of LPS-challenged rats. Immunohistochemical analysis showedthat while the expression of the NF-κ Bp65, tumor necrosis factor (TNF)-α, and inducible nitric oxide synthase(iNOS) tended to increase, that of I-κ Bα was decreased in the hepatocytes of rats challenged with LPS. A slightdecline of NF-κ Bp65, TNF-α, and iNOS, but an increase of I-κ Bα were observed in the hepatocytes of the ratspretreated with AEDF. CONCLUSION: AEDF may act as a therapeutic agent for inflammatory disease through aregulation of inflammation-related proteins.
作者: 刊期: 2003年第02期
AIM: To find the anti-inflammatory and anti-platelet aggregatory activity of human placental extract (HPE, Placentrex).METHODS: The HPE was studied for anti-inflammatory effect in Wistar rats on carrageenin, serotonin (5-HT),and prostaglandin E1 (PGE1) induced edema in acute model and cotton pellet induced granuloma on sub-acutemodel. Anti-platelet aggregation was studied against protection of adinosine diphosphate (ADP)-induced aggrega-tion of human platelet through in vitro study. RESULTS: HPE showed positive results both in acute and sub-acutemodels of inflammation. Highly significant (P<0.01) results were obtained against 5-HT induced acute inflamma-tion and cotton pellet induced sub-acute inflammation in comparison with standard (diclofenac sodium) and control(normal saline) drugs. The anti-inflammatory property of HPE in animal model was well supported with clinicalstudy of platelet aggregation. There was highly significant (P<0.01) inhibition of platelet aggregation with HPE atdifferent doses against ADP. CONCLUSION: Our data suggest that human placental extract may be useful insuppressing inflammation and platelet aggregation.
作者: 刊期: 2003年第02期
AIM: Compounds containing Bupleurum possess immunomodulating effects. KY88 LIVER LIVO (KY88) is ablend of such compound. The aim of this study is to investigate the effects of KY88 on the production of cytokinesby lymphocytes in vitro. METHODS: Seventy Sprague Dawley rats were used of which 40 were orally fed with 4mg purified KY88 for 35 d. Normal human lymphocytes were isolated and cultured in standard conditions. Theculture medium was collected at zero and 72 h after the KY88 treatment. The cytokines, including interleukin-1 β(IL-1β), IL-2, IL-4, IL-6, tumor necrosis factor-α (TNF-α), and interferon-γ, were measured by ELISA kits.RESULTS: TNF-α levels in the supernatant of cultured human lymphocytes significantly increased after the treat-ment of PHA and KY88. The mean levels were (855±251), (399± 145), and (176±49) ng/L after the treatment withKY88 at the concentrations of 10, 1 and 0.1 g/mL respectively. However, the level in the control group withoutspecific treatment was only (68±4) ng/L. The difference between KY88 10 g/mL and control groups was signifi-cant (P<0.05). All other cytokines did not show significant variations between KY88 and the control groups. KY88may regulate the immune function through the induction of TNF-o expression.
作者: 刊期: 2003年第02期
综述了钩藤总碱、钩藤碱和异钩藤碱对心血管系统和神经系统等方面的药理作用,包括降低血压、减慢心率、抗心律失常、脑缺血保护,以及镇静等作用,其作用机制与钙通道阻滞、钾通道开放、以及神经递质转运和代谢的调节有关.
作者:石京山;余俊先;陈修平;徐瑞霞 刊期: 2003年第02期