啤酒花活性成分黄腐酚抗骨质疏松作用研究

目的 对黄腐酚在动物及成骨细胞水平上的抗骨质疏松作用进行评价。方法 采用去卵巢小鼠骨质疏松模型进行体内药效学验证。运用Elisa试剂盒及Micro-CT检测方法,对小鼠血清生化指标及股骨骨密度、骨组织形态学进行评价。同时结合成骨细胞增殖、分化和矿化水平分析,以及骨形成相关蛋白的Western blot检测,对黄腐酚抗骨质疏松作用进行系统评价。结果 在体内药效学研究中,黄腐酚可显著提高去卵巢小鼠雌激素水平,降低高骨转换率;改善骨小梁微环境,增强骨密度。在成骨细胞水平上,黄腐酚既可以促进成骨细胞增殖、碱性磷酸酶（ALP）活性以及骨矿化水平,又可以提高骨桥蛋白（OPN）、骨涎蛋白（BSP）和骨形成蛋白（BMP-2）的表达。结论 本研究首次明确了黄腐酚具有抗骨质疏松作用,为开发治疗骨质疏松的药物提供新的资源。     

啤酒花经抗氧化途径减轻Aβ损伤成骨细胞作用研究

目的 探讨啤酒花改善β-淀粉样蛋白（Aβ）损伤成骨细胞的骨形成作用及其机制。方法 以新生24 h Wistar大鼠所分离的成骨细胞为研究对象,用Aβ_1-42寡聚体对成骨细胞进行损伤,并用啤酒花提取物进行药物干预。分别采用MTT法、碱性磷酸酶（ALP）活性检测以及茜素红染色法评价成骨细胞的增殖、分化及骨矿化水平,流式细胞仪检测成骨细胞凋亡。采用蛋白质印迹法检测骨形成相关蛋白及氧化应激Nrf2、FoxO1通路蛋白的表达水平,并用免疫荧光检测FoxO1蛋白的入核表达。结果 啤酒花提取物可显著促进Aβ损伤成骨细胞的增殖,提高ALP活性及骨矿化结节水平,抑制细胞凋亡率,并促进骨形成相关蛋白I型胶原酶（COL-I）及骨桥蛋白（OPN）的表达。此外,啤酒花提取物可显著激活Aβ损伤成骨细胞的Nrf2和FoxO1信号通路,促进该氧化应激信号通路相关蛋白的表达,通过抗氧化维持骨代谢平衡。结论 本研究表明啤酒花具有减轻Aβ损伤成骨细胞的作用,初步阐明其作用机制与抗氧化有关,为抗骨质疏松作用机制及药物研发提供了新思路。     

啤酒花中黄酮类成分的含量分析

目的 建立啤酒花中总黄酮和黄腐酚含量测定方法,对来自不同产地和品种的29个啤酒花样品中的总黄酮和黄腐酚进行测定。方法 用芦丁-AlCl₃分光光度法测定总黄酮的含量;用HPLC-UV法测定黄腐酚的含量。色谱条件：色谱柱为Dikma Technologies Diamonsil C₁₈柱（250 mm×4.6 mm,5 μm）;流动相为乙腈-1%冰醋酸梯度洗脱,流速为1.0 ml/min;柱温为25℃;检测波长为370 nm。结果 总黄酮回归方程为A=30.345C+0.016 8,r=0.999 9;黄腐酚回归方程为A=55 446C+9 040.5,r=0.999 9,表明总黄酮在20.2~404.0 μg/ml,黄腐酚在2.152~43.040 μg/ml范围内,线性关系良好,两者精密度和重复性RSD均<2%,平均加样回收率分别为102.71%和100.21%。结论 不同种类的啤酒花之间,总黄酮和黄腐酚含量存在巨大差异,进口啤酒花优于国产。     

基于Micro-CT技术分析淫羊藿苷和朝藿定C对糖皮质激素性骨质疏松症小鼠骨组织微结构的影响

目的 应用Micro-CT技术观察淫羊藿苷和朝藿定C对糖皮质激素性骨质疏松症（GIOP）小鼠模型骨组织骨量、骨微结构的影响。方法 8周龄C57/BL6雄性小鼠随机分为4组：对照组、模型组、淫羊藿苷（200 mg/kg）组和朝藿定C（200 mg/kg）组,除对照组外,其他3组小鼠im地塞米松5 mg/kg,0.125 mg/次,每周3次,制备GIOP模型,对照组im等体积的生理盐水,造模同时,每天ig给药1次,连续60 d后取材,采用micro-CT方法对胫骨近端骨微结构进行三维分析;HE染色病理切片观察胫骨近端骨组织病理形态。结果 骨量参数：与对照组比较,模型组骨矿物质含量（BMC）、骨矿物质密度（BMD）、组织矿物含量（TMC）、组织矿物质密度（TMD）均显著下降（P<0.05、0.01）;与模型组比较,淫羊藿苷组、朝藿定C组BMC、BMD、TMC、TMD指标均显著提高（P<0.05）;其中朝藿定C组各指标均较淫羊藿苷组显著升高（P<0.05）。与对照组比较,模型组相对骨体积（BV/TV）、骨小梁数量（Tb.N）、骨小梁厚度（Tb.Th）指标均显著下降（P<0.05）,骨小梁分离度（Tb.Sp）、结构模型指数（SMI）均显著提高（P<0.05）;与模型组比较,淫羊藿苷、朝藿定C组BV/TV、Tb.N、Tb.Th显著升高,Tb.Sp、SMI显著下降（P<0.05）,其中朝藿定C组各指标均较淫羊藿苷组改善显著（P<0.05）。HE染色病理切片示,模型组骨小梁数目明显减少,稀疏断裂,大部分不能连接成网状,骨髓腔明显增大,骨小梁结构出现较大的空白区域;淫羊藿苷及朝藿定C组小鼠骨小梁明显宽厚,数目也显著增加,骨小梁断裂较少,骨小梁光滑,接近对照组,其中朝藿定C组增加较淫羊藿苷组明显。结论 地塞米松诱导的骨质疏松小鼠模型成功建立,朝藿定C和淫羊藿苷抗骨质疏松活性明显,主要通过增加骨量和改善骨小梁微结构来最终提高骨强度,其中朝藿定C抗骨松作用更强;Micro-CT技术与传统的检测方法相比,在中药干预GIOP骨微结构参数分析上具有便捷、高效,经济,图像多维、全面,准确的优势。     

右归饮联合盐酸雷洛昔芬给药治疗小鼠骨质疏松症

目的 观察右归饮和盐酸雷洛昔芬联合给药对骨质疏松模型小鼠的治疗作用,并研究其作用机制。方法 将C57BL/6雌性小鼠切除卵巢制备骨质疏松模型,手术12周后将小鼠随机分为4组：模型组、右归饮（0.1 g/只）组、盐酸雷洛昔芬（10mg/kg）组和联合给药（右归饮0.1 g/只与盐酸雷洛昔芬10 mg/kg联合给药）组,另设假手术组,连续7周每天ig给药1次。给药结束后,将动物处死,Micro-CT测定骨密度和骨组织微形态,并测定骨形态计量指标——骨体积分数（BV/TV）、骨表面积/骨体积（BS/BV）、骨小梁的平均厚度（Tb.Th）、骨小梁数量（Tb.N）、骨小梁分离度（Tb.Sp）;试剂盒法测定血清中I型胶原氨基端（P1NP）、胶原羧基端（CTx）水平;分离并培养骨髓间充质干细胞,体外培养7 d,CCK-8法测定细胞增殖率,试剂盒法检测分化相关指标碱性磷酸酶（ALP）水平。结果 与模型组比较,右归饮组、盐酸雷洛昔芬组和联合给药组的骨密度、BV/TV、Tb.Th、Tb.N显著升高,BS/BV和Tb.Sp显著降低（P<0.05）;与盐酸雷洛昔芬组比较,联合给药组的BV/TV、Tb.Th、Tb.N显著升高,BS/BV和Tb.Sp显著降低（P<0.05）。联合给药组P1NP水平、细胞增殖率均显著高于其他各组（P<0.05、0.01）。ALP水平显著高于假手术组、模型组、盐酸雷洛昔芬组,显著低于右归饮组（P<0.01）。结论 在给药时间相同的前提下,右归饮和盐酸雷洛昔芬联合给药比单独给药更有效地抑制小鼠骨丢失,通过促进细胞的增殖和分化提高骨形成能力,达到增加骨密度、治疗骨质疏松的效果。     

四烯甲萘醌保护成骨细胞氧化损伤的作用研究

目的 考察四烯甲萘醌(MK₄)对成骨细胞氧化损伤的保护作用,阐明MK₄防治骨质疏松作用机制。方法 采用过氧化氢(H₂O₂)刺激小鼠成骨细胞系（MC3T3-E1）氧化应激模型,考察细胞活力、ALP活性和骨结节面积,DCFH-DA法检测活性氧(ROS)水平,JC-1检测线粒体膜电势,Annexin V-FITC/PI法检测细胞凋亡率,RT-PCR法考察氧化应激相关基因FoxO1、FoxO3、SOD、Bcl-2和bax等的mRNA表达。结果 10 μmol/L四烯甲萘醌能显著提高H₂O₂刺激的成骨细胞增殖、ALP活性、骨结节形成面积和增强细胞膜电势,显著降低H₂O₂刺激的成骨细胞内丙二醛和活性氧水平,同时显著降低成骨细胞凋亡率和细胞凋亡因子bax/Bcl-2的mRNA表达水平,显著提高抗氧化酶SOD和转录因子FoxO1、FoxO3的mRNA表达。结论 四烯甲萘醌可通过调控FoxO通路保护成骨细胞氧化损伤和通过下调bax/Bcl-2比例,降低成骨细胞凋亡。     

复方骨肽注射液应用于胸腰椎骨质疏松性骨折患者中的效果及对患者骨密度与骨代谢的影响

目的 分析复方骨肽注射液在胸腰椎骨质疏松性骨折患者中的应用价值。方法 选取2018年1月至2020年1月我院收治的96例胸腰椎骨质疏松性骨折患者为研究对象。所有患者随机分为甲组（钙尔奇D联合复方骨肽注射液治疗）和乙组（钙尔奇D治疗）,各48例。比较两组治疗后的中医症状评分、骨代谢、骨质疏松程度、骨密度水平、视觉模拟评分（VAS）、腰椎疾患治疗成绩评分（JOA）。结果 治疗后,甲组的中医症状评分、JOA评分均高于乙组（P<0.05）;甲组的骨碱性磷酸酶（BALP）、Ⅰ型前胶原氨基端前肽（PIINP）水平明显低于乙组（P<0.05）;3级骨质疏松患者比例甲组低于乙组（P<0.05）,骨密度水平甲组高于乙组（P<0.05）;VAS甲组低于乙组（P<0.05）。结论 复方骨肽注射液治疗胸腰椎骨质疏松性骨折患者,可有效改善其骨代谢、骨密度水平,缓解疼痛程度,促进腰椎功能恢复。     

黄腐酚对人卵巢癌耐药细胞株SKOV3/DDP耐药性的影响及其机制★

目的 探讨黄腐酚降低人卵巢癌耐药细胞株SKOV3/DDP耐药性的机制。方法 将KOV3/DDP细胞分为卵巢癌组（无干扰）、10 μmol·L^-1黄腐酚组（10 μmol·L^-1黄腐酚培养）、20 μmol·L^-1黄腐酚组（20 μmol·L^-1黄腐酚培养）、40 μmol·L^-1黄腐酚组（40 μmol·L^-1黄腐酚培养）、80 μmol·L^-1黄腐酚组（80 μmol·L^-1黄腐酚培养）、160 μmol·L^-1黄腐酚组（160 μmol·L^-1黄腐酚培养）。采用CCK-8检测SKOV3/DDP细胞存活率；克隆形成实验检测SKOV3/DDP细胞克隆数目；流式细胞仪检测SKOV3/DDP细胞凋亡率；CCK-8检测黄腐酚对SKOV3/DDP细胞DDP耐药性的影响；免疫印迹检测SKOV3/DDP细胞中耐药蛋白ABCB1、MDR-1和P-gp的表达。结果 与卵巢癌组相比，10 μmol·L^-1黄腐酚组SKOV3/DDP细胞存活率无明显变化（P>0.05）；与10 μmol·L^-1黄腐酚组相比，20、40、80、160 μmol·L^-1黄腐酚组SKOV3/DDP细胞存活率均显著降低（P<0.05）。卵巢癌组及10、20、40、80、160 μmol·L^-1黄腐酚组SKOV3/DDP细胞克隆数目分别为（86±12）、（82±10）、（61±11）、（46±9）、（29±11）及（20±7），组间比较，差异有统计学意义（F=43.270， P<0.001）。卵巢癌组及10、20、40、80、160 μmol·L^-1黄腐酚组SKOV3/DDP细胞凋亡率分别为（2.56±0.20）%、（3.20±0.36）%、（15.21±1.22）%、（26.30±1.60）%、（33.20±2.25）%及（45.63±2.10）%，组间比较，差异有统计学意义（F=775.200， P<0.001）。与DDP相比，DDP联合黄腐酚对SKOV3/DDP细胞的活性抑制率较高，差异有统计学意义（P<0.05）；与卵巢癌组相比，10 μmol·L^-1黄腐酚组ABCB1、MDR-1和P-gp蛋白表达水平无显著差异（P>0.05）；与10 μmol·L^-1黄腐酚组相比，20、40、80、160 μmol·L^-1黄腐酚组SKOV3/DDP细胞中ABCB1、MDR-1和P-gp蛋白表达水平均显著降低（P<0.05）。结论 黄腐酚可降低卵巢癌SKOV3/DDP细胞的耐药性，抑制细胞活性，促进细胞凋亡，可能与下调ABCB1、MDR-1和P-gp蛋白表达相关。     

啤酒花总查尔酮的提取工艺及对氧化损伤心肌细胞的保护作用研究

目的 探讨啤酒花总查尔酮的最佳提取工艺及其对过氧化氢(H₂O₂)氧化损伤H₉C₂心肌细胞的保护作用。方法 采用正交试验法研究了提取时间、料液比与提取次数对啤酒花总查尔酮得率的影响,并研究了总查尔酮对过氧化氢氧化损伤H₉C₂心肌细胞保护作用。结果 总查尔酮最佳提取工艺条件为,提取时间5 min、料液比1:20、提取次数2次,此条件下黄腐酚得率可达19.9 µg·mL^-1,明显提高过氧化氢损伤H9C2细胞细胞存活率,并降低乳酸脱氢酶（LDH）含量、提高超过氧化歧化酶（SOD）和过氧化氢酶（CAT）活性。结论 在最佳条件下黄腐酚具有较高的提取得率,对过氧化氢损伤H9C2心肌细胞具有较好的保护作用,为啤酒花进一步研究与开发提供依据。     

加减青娥方体外对RAW264.7细胞向破骨细胞分化的影响

目的 探讨加减青娥方抑制骨质疏松的作用机制。方法 在体外培养的小鼠破骨前体RAW264.7细胞中加入不同浓度的加减青娥方提取物,利用抗酒石酸酸性磷酸酶(TRAP)染色法检测核因子κ B受体活化因子配体(RANKL)诱导的RAW264.7细胞分化为破骨细胞的数量及其活性的影响;利用荧光定量PCR(RT-PCR)法检测RANKL诱导的RAW264.7细胞分化为破骨细胞雌激素受体(ER)mRNA表达。结果 加减青娥方可抑制RANKL诱导的RAW264.7细胞分化为破骨细胞,该作用可能是通过调控ERα mRNA的表达实现的。结论 加减青娥方可通过调控ERα基因的表达,抑制破骨细胞的分化、增殖,从而实现增加骨密度、防治骨质疏松的作用。     

Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

New 2,6-piperidinediones 2_a–g and 4_a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides l_a–g or cycloalkylidenes 3_a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4_a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5_a–m. Some new selected compounds 2_a–c,f, 4_a–d & 5_e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2_f.     

EFFECT OF POLICOSANOL SUCCESSIVE DOSE INCREASES ON PLATELET AGGREGATION IN HEALTHY VOLUNTEERS

Policosanol is a cholesterol-lowering drug with hypocholesterolemic effects demonstrated in experimental models, healthy volunteers and type II hypercholesterolemic patients. In addition, antiplatelet effects of policosanol have been shown in experimental models and healthy volunteers. The effect of successively increasing doses of policosanol on platelet aggregation was investigated in a randomized, placebo-controlled, double-blind study conducted in 37 healthy volunteers. The volunteers were on a placebo-baseline period (two tablets per day) for 7 days and thereafter they received randomly, under double-blind conditions, placebo or policosanol (10mgday⁻¹) for 7 days. After this period dosage was doubled to 20mgday⁻¹for the next 7 days and then again doubled to 40mgday⁻¹, while the control group received placebo tablets all the time. Platelet aggregation as well as coagulation time was measured at baseline and after each dosing step. Results showed that antiplatelet effects of policosanol were successfully enhanced throughout the study, thus suggesting a dose-dependent relationship. No significant effect was reached during the first dosing period, but significant reductions of epinephrine and ADP-induced platelet aggregation were observed after the second one. Finally, a significant inhibition of platelet aggregation induced by all the agonists was observed at the last dosing step. Coagulation time remained unchanged during the trial.     

NEURAMIDE STIMULATES ADRENOCORTICOTROPIN BUT NOT PROLACTIN RELEASE FROM RAT PITUITARY

Neuramide (NMD), a substance found in crude preparations of porcine stomach extract, is a viral inhibitor that also has putative immunostimulatory effects. The effects of NMD on stress-hormone (ACTH and prolactin—PRL) release were assessed inin vivoandin vitrostudies. In the former, blood levels of corticosterone and PRL were measured in NMD-treated male rats.In vitroexperiments were performed to evaluate the effects of NMD and three of its fractions (obtained with high performance liquid chromatography) on ACTH and PRL release from perfused rat pituitary slices. NMD increased plasma corticosterone levelsin vivoand produced dose-dependent increases inin vitropituitary release of ACTH. No effects on PRL secretion were observedin vivoorin vitro. The stimulatory effects on ACTH release were caused by the NMD fraction with a molecular weight of >5000<10000Da.     

鼻渊净胶囊的HPLC指纹图谱研究

目的 建立鼻渊净胶囊的高效液相色谱（HPLC）指纹图谱。方法 采用Agilent SB-C₁₈（4.6 mm×250 mm,5 μm）色谱柱,乙腈-水为流动相、以1.0 ml/min流速行梯度洗脱,检测波长210 nm,柱温30 ℃,洗脱时间为80 min。采用中药色谱指纹图谱相似度评价系统（2004A版）对检测出色谱进行指纹图谱相似度评价。结果 建立了鼻渊净胶囊的HPLC指纹图谱,确定了20个共有峰,15个峰归属到各药材,其中5个峰确认了化学成分;10批样品的指纹图谱的整体相似度与对照图谱比较,均在90%以上。结论 所建立的鼻渊净胶囊指纹图谱有助于从整体上控制该制剂的质量。     

Investigation of the prevalence of tetQ, tetX and tetX1 genes in Bacteroides strains with elevated tigecycline minimum inhibitory concentrations

In this study, the antibiotic susceptibilities to tigecycline and tetracycline of 35 selected Bacteroides fragilis group strains were determined by Etest, and the presence of tetQ, tetX, tetX1 and ermF genes was investigated by polymerase chain reaction (PCR). tetQ was detected in all 12 B. fragilis group isolates (100%) exhibiting elevated tigecycline minimum inhibitory concentrations (MICs) (≥8 μg/mL) as well as the 8 strains (100%) with a tigecycline MIC of 4 μg/mL, whilst tetX and tetX1 were present in 15% and 75% of these strains, respectively. All of these strains were fully resistant to tetracycline (MIC ≥ 16 μg/mL). On the other hand, amongst the group of strains with tigecycline MICs < 4 μg/mL (15 isolates), tetQ, tetX and tetX1 were found less frequently (73.3%, 13.3% and 46.7%, respectively). All but two strains harbouring the tetQ gene in this group were non-susceptible to tetracycline, with a MIC > 4 μg/mL. These data suggest that in most cases tigecycline overcomes the tetracycline resistance mechanisms frequently observed in Bacteroides strains. However, the presence of tetX and tetX1 genes in some of the strains exhibiting elevated MICs for tigecycline draws attention to the possible development and spread of resistance to this antibiotic agent amongst Bacteroides strains. The common occurrence of ermF, tetX, tetX1 and tetQ genes together predicted the presence of the CTnDOT-like Bacteroides conjugative transposon in this collection of Bacteroides strains.     

INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF THE CLASS III ANTIARRHYTHMIC SUBSTANCE / -SOTALOLIN VITRO: REVERSIBLE INHIBITION OF CHOLINESTERASE ISOENZYMES FROM BLOOD AND THE HUMAN CENTRAL NERVOUS SYSTEM

Inhibitory effects of the class III antiarrhythmic compound / -sotalol on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and the human caudate nucleus and on serum cholinesterase (ChE; EC 3.1.1.8) were studiedin vitrousing a spectrophotometric kinetic assay with acetylthiocholine (ASCh) as substrate. Sotalol concentrations in the assays varied from 0.32 to 3.2m . All isoenzymes studied were inhibited by / -sotalol in a reversible and concentration-dependent manner. Double reciprocal plots of the reaction velocity against varying ASCh concentrations revealed that / -sotalol reduced substrate affinity (apparent Michaelis constant, KM, increased) of serum ChE, but did not change the enzyme's maximal rate of ASCh hydrolysis (V_max). Thus, / -sotalol inhibition of serum ChE was of the competitive type (rate constant for reversible competitive inhibition: K_i=0.51m ). In contrast, / sotalol reduced the maximal reaction velocity of the AChE isoenzyme from the central nervous system (caudate nucleus), but had no influence on substrate affinity of the enzyme (K_Mwith ASCh unchanged) indicating purely non-competitive inhibition kinetics (rate constant of reversible non-competitive inhibition: K_i′=0.44m ). / -sotalol inhibition of erythrocyte AChE was of mixed competitive/non-competitive type (K_i=0.31m , K_i′=0.49m ). Non-competitive / -sotalol inhibition of caudate nucleus AChE and the non-competitive component of erythrocyte AChE inhibition cannot be overcome by increased concentrations of the cholinergic transmitter acetylcholine (ACh). Peak / -sotalol plasma levels as described in the literature for both humans (15μ ) and experimental animals (dogs: 18μ ; rats: 260μ ) as well as maximal myocardial concentrations of the substance (dogs: 46μ ; rats: 478μ ) are in the range of about 2% to 100% of the sotalol inhibition rate constants determined in the present paper for cholinesterase isoenzymesin vitro. Thus, / -sotalol inhibition of ACh hydrolysisin vivomay contribute to both the well known antiarrhythmic potential and proarrhythmic side effects of the compound.     

喙果黑面神化学成分研究

目的研究大戟科植物喙果黑面神(Breynia rostrata Merr.)的化学成分。方法利用硅胶、凝胶等色谱技术分离纯化化学成分,根据化合物的理化性质和光谱数据进行结构鉴定。结果从喙果黑面神的正丁醇萃取部分分离得到4个化合物,分别鉴定为6-O-甲基丙酰基-α-D-吡喃葡糖(6-O-methylpropanoyl-α-D-glucopyranose,1);4″-苯酚基-6-O-甲基丙酰基-β-D-吡喃葡糖苷(4″-phenolic-6-O-methylpropanoyl-β-D-glucopyranoside,2);1-O-没食子酰基-β-D-吡喃葡糖苷(1-O-galloyl-β-D-glucopyranoside,3);熊果苷(arbutin,4)。结论化合物1和2为新化合物,3和4均为首次从该种植物分离得到。     

AMELIORIATION OF CHEMICALLY-INDUCED HEPATOCYTE INJURY BY CYCLOSPORINE A

Cyclosporine A, beside its current applications, possesses potential hepatoprotective effects. This study was directed to investigate the effect of Cyclosporine A pretreatment on hepatic injury due to carbon tetrachloride (CCl₄) and -galactosamine. Rats were injected by two successive doses of Cyclosporine A (5mgkg⁻¹day⁻¹). Six hours after the second dose, 1mlkg⁻¹of CCl₄was administered i.p. Effects associated with Cyclosporine A pretreatment were examined by using isolated hepatocytes and hepatocytes that were immobilized and continuously perfused. -Galactosamine (5m ) was added directly to the perfusion medium. After isolation, hepatocytes were examined histologically by light and electron microscopy, immobilized and perfused for further metabolic functional activity evaluation. Cyclosporine A pretreatmentin vivoproduced hepatoameliorative effects of various degrees which were statistically significant as manifested by: (1) an increased trypan blue exclusion after CCl₄; (2) an improved ureagenesis after CCl₄; (3) a reduction in the lipid droplets accumulation in the cytoplasm produced by CCl₄administration; (4) well preserved cytoplasmic organelles as mitochondria, endoplasmic reticulum ER, nuclear chromatin structures that were altered by CCl₄; and (5) an increased hepatocytes survival in the agarose gel matrix, reduction of LD leakage and improvement of ureagenesis after -galactosamine addition to the perfusion medium. The beneficial effect of Cyclosporine A pretreatment in modifying hepatotoxicity of chemical insults merits further studies.     

EFFECTS OF 2-GUANIDINE-4-METHYLQUINAZOLINE ON GASTRIC ACID SECRETION IN RATS

In this study 2-guanidine-4-methylquinazoline (2-GMQ) appeared to decrease basal and stimulated gastric acid secretion, while structurally related compounds as dimethyl- biguanide, cyanoguanidine and 2-cyanoamino-4-methylpyrymidine did not. Thus, there is an antisecretory effect when the biguanide group is associated with a lipophilic structure. The antisecretive effects exerted by 2-GMQ are associated with anti H₂-histamine activity.The anti H₂-histamine nature of the effects of 2-GMQ was confirmed by the capacity of this compound of depressing the chronotropic activity of the isolated guinea pig auricle increased by histamine, as well as relaxant activity in rat uterus contracted by histamine, since both preparations are rich in H₂-histamine receptors.     

栝楼不同药用部位质量控制的研究进展

瓜蒌子、瓜蒌皮、瓜蒌、天花粉来源于栝楼的不同药用部位,4味药材均为常用的大宗药材,现行版《中国药典》对其制定的质量标准过于简单,无法科学合理地控制其质量。本文对瓜蒌子、瓜蒌皮、瓜蒌、天花粉安全性和有效组分的研究进行综述,明确了相关研究存在的问题并针对问题提出建议,为科学全面的药材及饮片标准的制定提供参考依据。