单面针根茎的化学成分研究

目的 对单面针根茎中的化学成分进行研究。方法 采用硅胶柱层析和制备液相色谱法进行分离纯化,并根据波谱数据对单体化合物进行结构鉴定。结果 从单面针根茎的乙醇提取物中分离纯化得到10个化合物,分别鉴定为：原阿片碱（1）、别隐品碱（2）、四氢小檗碱（3）、白屈菜红碱（4）、二氢血根碱（5）、二氢白屈菜红碱（6）、6-丙酮基二氢血根碱（7）、对羟基苯甲醛（8）、异香草醛（9）、丁香醛（10）。结论 10个化合物均首次在单面针中分离得到。     

糙叶败酱乙酸乙酯部位的化学成分研究

目的 研究糙叶败酱乙酸乙酯部位的化学成分。方法 利用硅胶及Sephadex LH-20凝胶柱色谱对其化学成分进行分离、纯化,根据理化性质及波谱数据进行结构鉴定。结果 从糙叶败酱水提取物的乙酸乙酯萃取部位分离得到11个化合物,分别为7α-甲氧基莫罗苷（1）、7β-甲氧基莫罗苷（2）、1-辛醇（3）、2,3-壬烯烃（4）、lariciresinol（5）、Jatamanin J（6）、落叶松脂醇-4-O-β-D-葡萄糖苷（7）、黄花败酱醇（8）、Jatamanin A（9）、Scabroside A（10）、十六烷酸-α-单甘油酯（11）。结论 化合物1~4为首次从该植物中分离得到,其中化合物3,4为首次从败酱科败酱属植物中分离得到。     

葎草的化学成分研究

从葎草全草的75%乙醇提取物中分离得到11个化合物，分别鉴定为苯甲酸（1）、乌苏酸（2）、香草醛（3）、对香豆酸（4）、木栓酮（5）、白桦脂酸（6）、香草酸（7）、山柰酚（8）、山柰酚-4′-甲醚（9）、二氢山柰酚（10）、金丝桃苷（11）。化合物1~4、8~11为首次从该植物中分离得到。     

肝胆舒康胶囊联合硫普罗宁治疗非酒精性脂肪肝病的临床研究

目的 研究沉香Aquilaria sinensis的倍半萜类化学成分。方法 采用硅胶、ODS、Sephadex LH-20等多种柱色谱及制备型高效液相色谱等现代分离技术对沉香的化学成分进行分离纯化，并根据其理化性质、MS、1D和2D NMR等波谱方法进行结构鉴定；采用96孔板微量稀释法测试了分得的单体化合物对耐药金黄色葡萄球菌的抑菌活性。结果 从沉香95%乙醇提取物中分离得到7个倍半萜类化合物，分别鉴定为（+）-4a，5-二甲基-3-（丙-2-烯基）-八氢萘-2β，8a-二醇（1）、白木香酸（2）、白木香醇（3）、vetaspira-2（11），6-dien-14-al（4）、白木香醛（5）、（-）-10-表-γ-桉叶醇（6）、9β-羟基-α-沉香呋喃（7）。其中化合物1对耐甲氧西林金黄色葡萄球菌的最小抑菌浓度（MIC）为210 μmol/L。结论 化合物1为新的倍半萜类化合物，命名为2β，8aα-二羟基-11-烯-荒漠木烷，其对耐甲氧西林金黄色葡萄球菌有较好的抑制作用。     

三桠苦枝叶化学成分的分离、鉴定

目的 研究三桠苦[Evodia lepta（Spreng.）Merr.]枝叶的化学成分,为三桠苦的进一步研究奠定物质基础。方法 对三桠苦无水乙醇提取物的乙酸乙酯萃取物采用硅胶柱层析分离纯化,得到单体化合物,经波谱分析鉴定其化合物结构。结果 从三桠苦乙酸乙酯萃取物中分离得到6个单体化合物,分别为异吴茱萸酮酚（化合物1）、异吴茱萸酮酚甲醚（化合物2）、3,5-二羟基-4-乙氧基-6-乙酰基-7-甲氧基-2,2-二甲基苯并二氢吡喃（化合物3）、（cis）-3,4,5-三羟基-6-乙酰基-7-甲氧基-2,2-二甲基色烷（化合物4）和（trans）-3,4-二羟基-5-甲氧基-6-乙酰基-7-甲氧基-2,2-二甲基色烷（化合物5）和对羟基苯甲酸丁酯（化合物6）。结论 化合物1~6均为首次从三桠苦植物的枝叶中分离得到。     

秋海棠抗炎作用及其机制研究

摘 要 目的： 探讨秋海棠不同溶剂提取物的抗炎作用及其机制研究。方法: 制备秋海棠醇提取物、石油醚提取物、乙酸乙酯提取物、正丁醇提取物、水提取物,以 脂多糖（LPS）诱导RAW 264.7巨噬细胞活化,不同溶剂提取物作用24 h后,ELISA法检测上清液中肿瘤坏死因子-α（TNF-α）、白细胞介素1β（IL-1β）的含量,Griess法测定一氧化氮（NO）的含量。 结果: 秋海棠乙酸乙酯提取物、正丁醇提取物能极显著抑制TNF-α、IL-1β、NO的含量（P<0.01）,秋海棠醇提取物、乙酸乙酯提取物能极显著抑制NO的含量（P<0.01）。 结论:秋海棠醇提取物、乙酸乙酯提取物、正丁醇提取物抗炎作用显著,其机制可能与减少炎症因子的释放有关。     

箭叶蓼的化学成分研究

箭叶蓼Polygonum sieboldii Meisn.来源于蓼科蓼属,为治疗风湿性关节炎的民间药用植物,全草入药。本课题组在以往的基础上继续对箭叶蓼乙醇提取物进行成分研究,从中分离鉴定了10个化合物,分别为：槲皮素（1）,槲皮素-3-O-鼠李糖苷（2）,异鼠李素（3）,麦黄酮（4）,7,4′-二甲氧基山柰酚（5）,芦丁（6）,鼠李糖甲酯（7）,蔗糖（8）以及β-谷甾醇（9）和胡萝卜苷（10）。箭叶蓼中主要含有黄酮醇及其苷类物质,以上化合物均为首次从箭叶蓼中分得。     

羊蹄化学成分及其抗肿瘤活性研究

从羊蹄乙醇提取物分离鉴定了2个萘类化合物、5个蒽醌类化合物及其他4个化合物。萘类为2-甲氧基-6-乙酰基-7-甲基胡桃醌（1）、3-乙酰基-2-甲基-1,4,5-三羟基-2,3-环氧萘醌醇（2）、蒽醌类为大黄素甲醚（3）、大黄素（4）、大黄酚-8-O-β-D-葡萄糖苷（5）、大黄素-8-O-β-D-吡喃葡萄糖苷（6）、大黄酚（7）,以及壬酸十五醇酯（8）、β-胡萝卜苷（9）、5-甲氧基-7-羟基-1（3H）-苯骈呋喃酮（10）和没食子酸（11）。化合物1、8~10为首次从羊蹄中分离得到,1、8为首次从酸模属植物中分离得到;体外细胞试验表明,化合物1对人肝癌HepG-2细胞、子宫癌Hela细胞、肺癌A549细胞具有较强的抑制作用,其IC₅₀分别为2、1.8、4.6 μmol·L^-1,化合物2对人肝癌细胞HepG-2的IC₅₀为100 μmol·L^-1。     

复方石韦片的质量控制

目的：研究北鹤虱(天名精的果实)的化学成分。方法：通过各种色谱手段（silica gel、ODS、HPLC）对北鹤虱甲醇提取物的二氯甲烷层进行分离纯化,通过¹H-NMR、¹³C-NMR等波谱技术确定化合物的结构。结果：分离并鉴定了5个倍半萜类化合物,分别为特勒内酯（1）、3-epiisotelekin（2）、11β,13-dihydro-1-epi-inuviscolide（3）、天名精内酯酮（4）、天名精内酯醇（5）。结论：化合物2、3为首次从天名精属植物分离得到。     

两个不同产区藏药刺柏叶中挥发油成分的GC-MS分析

摘 要 目的： 对甘肃榆中和碌曲的藏药刺柏叶中挥发油化学成分进行比较分析。 方法: 采用水蒸气蒸馏法提取挥发油,利用GC MS联用技术对其进行分离分析。结果:甘肃榆中和碌曲的得油率分别为0.21%和1.45%,两个地区刺柏叶中前者挥发油共分离出40个峰,鉴定出38个化合物,占分离物质的95%,后者挥发油共分离出51个峰,鉴定出47个化合物,占分离物质的92%。甘肃榆中刺柏叶中挥发油的主要成分为α-蒎烯（44.92%）,1-石竹烯（9.23%）、(-)-异喇叭烯（6.50%）、α-石竹烯（5.60%）、月桂烯（4.54%）、d-杜松烯（3.37%）;碌曲刺柏叶中挥发油的主要成分为二-非手性-α-柏木烯（31.87%）、环己烯（15.28%）、γ-榄香烯（10.05%）、澳白檀醇（5.80%）、α-蒎烯（5.79%）。结论: 两者刺柏叶挥发油成分有所不同,其得率及主要成分都有较大差异。该方法对建立刺柏质量标准控制有参考价值。     

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.     

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,5μm)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...     

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.     

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。     

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。     

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.