杏香兔耳风的化学成分

目的 研究杏香兔耳风（Ainsliaea fragrans Champ．）的化学成分。从中找出活性物质。方法 利用硅胶、Sephadex LH-20柱层析和重结晶等方法，对化学成分进行分离纯化。根据理化性质和波谱数据对其进行结构鉴定。结果 从杏香兔耳风的全草中分得黄酮、酚类、倍半萜、三萜共10个化合物。分别为：槲皮素（quercetin，1）；木犀草素（hteohn，2）；芹菜素（apisenin，3）；小麦黄素（tricin，4）；木犀草素7-O-β-D-葡萄糖苷（1uteolin7-O--O-β-D-glucoside，5）；槲皮素-O-β-D-葡萄糖苷（quercefin-5-O-β-D-glucoside，6）；异香草酸（isovanillic acid，即3-hydroxy-4-methoxy-benzoicacid，7）；熊果苷（arbutin，8）；β-谷甾醇（β-sitosterol，9）；β-胡萝卜苷（β-sitosterol-D-glueoside，10）。结论 化合物1-8为首次从该植物中分得；1,4、6、7、8首次从该属植物中得到。     

高效液相色谱法测定暴马子皮药材中2个成分的含量

目的:建立测定暴马子皮药材中2个成分(紫丁香苷、sinapylaldehyde 4-O-β-D-glucopyranoside)的高效液相色谱分析方法。方法:采用Phenomenex Luna C18(4.6 mm×250 mm,5μm)色谱柱,流动相为甲醇(B)-0.1%醋酸水溶液(A),梯度洗脱,流速1.0 mL·min-1,DAD检测器,检测波长:284 nm;柱温25℃。结果:紫丁香苷、sinapylaldehyde 4-O-β-D-gluco-pyranoside的线性范围分别为0.2～0.8μg(r=0.9995)和0.04～0.16μg(r=0.9993),平均加样回收率(n=6)分别为99.9%(RSD=2.1%)和99.5%(RSD=2.9%)。结论:不同产地暴马子皮药材中所含紫丁香苷、sinapylaldehyde 4-O-β-D-gluco-pyranoside的含量存在显著性差异。本方法操作简便,结果准确,重复性好,可用于中药暴马子皮药材的质量控制。     

沙生蜡菊花中黄酮类成分的分离与鉴定

目的研究沙生蜡菊(Helichrysum arenarium(L.)Moench)花的化学成分。方法采用硅胶柱色谱?ODS柱色谱和HPLC柱色谱分离纯化,依据理化性质、波谱数据分析进行结构鉴定。结果从沙生蜡菊花的甲醇提取物中分离得到8个黄酮类化合物,分别鉴定为山奈酚3-O-β-D-吡喃葡萄糖苷(kaempferol 3-O-β-D-glucopyranoside,1)、木犀草素3′-O-β-D-吡喃葡萄糖苷(luteolin3′-O-β-D-glucopyranoside,2)、木犀草素7-O-β-D-吡喃葡萄糖苷(luteolin7-O-β-D-glucopyranoside,3)、木犀草素6-羟基-7-O-β-D-吡喃葡萄糖苷(luteolin6-hydroxy-7-O-β-D-glucopyranoside,4)、木犀草素3′-甲氧基-6-羟基-7-O-β-D-吡喃葡萄糖苷(luteolin3′-methoxyl-6-hydroxy-7-O-β-D-glucopyranoside,5)、黄芩素7-O-β-D-吡喃葡萄糖苷(scutellarein7-O-β-D-glucopyranoside,6)、山柰酚3-O-β-D-龙胆二糖苷(kaempferol3-gentiobioside,7)、山柰酚3-O-(3-β-D-吡喃葡萄糖基)-β-D-吡喃葡萄糖苷(kaempferol3-O-(3-β-D-glucopyranosyl)-β-D-glucopyranoside,8)。结论化合物2、4~8为首次从蜡菊属植物中分离得到。     

火绒草黄酮类成分的分离与鉴定(Ⅱ)

目的对火绒草的化学成分进行研究,为进一步开发利用该植物资源提供依据。方法采用反复正相硅胶、反相ODS、Sephadex LH-20等柱色谱以及高效液相色谱法等手段进行分离纯化,并通过理化性质与光谱分析鉴定化合物的结构。结果从火绒草体积分数为70%的乙醇溶液提取物中又分离鉴定了7个黄酮类化合物,分别为芹菜素(apigenin,1)、山柰酚-3-O-(6″-O-乙酰基)-β-D-吡喃葡萄糖苷[kaempferol-3-O-(6″-O-acetyl)-β-D-glucopyranoside,2]、山柰酚-3-O-(6″-O-反式对香豆酰基)-β-D-吡喃葡萄糖苷[kaempferol-3-O-(6″-O-trans-p-coumaroyl)-β-D-glucopyranoside,3]、山柰酚-3-O-(6″-O-顺式对香豆酰基)-β-D-吡喃葡萄糖苷[kaempferol-3-O-(6″-O-cis-p-coumaroyl)-β-D-glucopyranoside,4]、槲皮素-7-O-β-D-吡喃葡萄糖苷(quercetin-7-O-β-D-glucopyranoside,5)、槲皮素-3-甲氧基-7-O-β-D-吡喃葡萄糖苷(quercetin-3-me-thoxy-7-O-β-D-glucopyranoside,6)、槲皮万寿菊素-7-O-β-D-吡喃葡萄糖苷(quercetagetin-7-O-β-D-glucopyranoside,7)。结论化合物1为首次从火绒草植物中分离得到,化合物2～7为首次从火绒草属植物中分离得到。     

杏香兔耳风的生药学鉴定

杏香兔耳风,又名一枝香,金边兔耳风.来源为菊科植物杏香兔耳风(Ainsliaeafrangrans champ)的全草.它具有清热解毒、消积散结、止咳、止血等功效.近年来含杏香兔耳风的成药研制颇多,且在临床上的应用也得到了肯定.但笔者查阅诸多文献资料,关于此药的生物学研究极少,特别是显微鉴别,未见报道.本文将对杏香兔耳风的生药学特征作一探讨.     

HPLC法测定不同产地杏香兔耳风中绿原酸和木犀草素的含量

目的：建立高效液相色谱法同时测定不同产地杏香兔耳风中绿原酸和木犀草素的含量.方法：采用Agilent ZORB-AX C18（250 mm×4.6 mm,5μm）色谱柱;流动相A为甲醇,流动相B为水（含0.2％磷酸）,梯度洗脱：0～15 min,A 25％～B75％,16～40 min,A 55％～B45％;流速：1.0 ml·min-1,柱温：30℃,检测波长为351 nm.结果：绿原酸和木犀草素保留时间分别约为10和28 min,与各自相邻峰的分离度均大于1.7.以峰面积对进样量进行线性回归,绿原酸回归方程为Y=3.16×105X-1.07×103（r =0.999 7）,线性范围0.762 ～ 15.240 μg,木犀草素回归方程为Y=1.69×105X＋ 1.35×103（r =0.999 6）,线性范围0.242～4.840 μg.绿原酸和木犀草素的平均回收率分别为98.2％和100.8％、RSD分别为1.92％和2.16％（n=6）.结论：本方法操作简便,结果准确,可用于杏香兔耳风药材的质量控制.     

杏香兔耳风的化学成分

目的研究杏香兔耳风(AinsliaeafragransChamp.)的化学成分,从中找出活性物质。方法利用硅胶、SephadexLH20柱层析和重结晶等方法,对化学成分进行分离纯化,根据理化性质和波谱数据对其进行结构鉴定。结果从杏香兔耳风的全草中分得黄酮、酚类、倍半萜、三萜共10个化合物,分别为:槲皮素(quercetin,1);木犀草素(luteolin,2);芹菜素(apigenin,3);小麦黄素(tricin,4);木犀草素7OβD葡萄糖苷(luteolin7OβDglucoside,5);槲皮素5OβD葡萄糖苷(quercetin5OβDglucoside,6);异香草酸(isovanillicacid,即3hydroxy4methoxybenzoicacid,7);熊果苷(arbutin,8);β谷甾醇(βsitosterol,9);β胡萝卜苷(βsitosterolDglucoside,10)。结论化合物1～8为首次从该植物中分得;1、4、6、7、8首次从该属植物中得到。     

沙生蜡菊花降脂活性部位化学成分的分离与鉴定(Ⅱ)

目的沙生蜡菊花降脂活性部位中的化学成分研究。方法采用硅胶、ODS、制备HPLC等多种色谱方法分离纯化,依据理化性质、波谱数据分析进行结构鉴定。结果从沙生蜡菊花的降脂活性部位中分离得到11个化合物,并分别鉴定为:丁香苷(syringin,1)、二氢丁香苷(dihydrosyringin,2)、(E)-4-hydroxybenzalacetone-3-O-β-D-glucopyranoside(3)、4-烯丙基-2-甲氧基苯基1-O-β-D-呋喃芹糖(1-6)-β-D-吡喃葡萄糖苷[4-allyl-2-methoxyphenyl 1-O-β-D-apiofuranosyl-(1-6)-O-β-D-glu-copyranoside,4]、苔黑酚-β-D-吡喃葡萄糖苷(orcinol-β-D-glucopyranoside,5)、7-hydroxy-5-me-thoxyphthalide-7-O-β-D-glucopyranoside(6)、5,7-dihydroxyphthalide-7-O-β-D-glucopyranoside(7)、undulatoside A(8)、adenosine(9)、maltol-3-O-β-D-apiofuranosyl-(1-6)-β-D-glucopyranoside(10)、2,4,6-三羟基苯乙酮-2,4-二-O-β-D-吡喃葡萄糖苷(2,4,6-trihydroxylacetophenone-2,4-di-O-β-D-glu-copyranoside,11)。结论化合物1～11均为首次从蜡菊属植物中分离得到。     

杏香兔耳风片联合射频热消融治疗重度宫颈糜烂的疗效观察

目的 评价杏香兔耳风片联合射频热消融治疗重度宫颈糜烂的临床疗效。方法 选取160例重度宫颈糜烂患者,随机分为治疗组和对照组,各80例。对照组：予以射频消融治疗。治疗组：在射频热消融治疗前后加用杏香兔耳风片。结果 治疗组、对照组治愈率分别为92.5%、76.25%,2组有显著性差异(P<0.01)。治疗组术后阴道排液时间及出血时间均少于对照组,2组有显著性差异(P<0.05)。结论 杏香兔耳风片联合射频热消融治疗重度宫颈糜烂疗效肯定、并发症轻,是一种值得推广的治疗方法。     

维药蜀葵花化学成分的分离与鉴定(Ⅱ)

目的对维药蜀葵花(Althaea rosea(Linn.)Cavan.)的化学成分进行进一步的研究。方法采用正相硅胶、反相ODS、Sephadex LH-20等柱色谱及高效液相色谱手段进行分离纯化,并通过理化性质与波谱分析方法鉴定化合物的化学结构。结果从蜀葵花体积分数为95%的乙醇提取物中分离得到9个黄酮类单体成分,分别鉴定为槲皮素(quercetin,1)、槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,2)、槲皮素-3-O-(6″-O-反式对香豆酰基)-β-D-吡喃葡萄糖苷(quercetin-3-O-(6″-O-trans-p-coumaroyl)-β-D-glucopyranoside,3)、槲皮素-3-O-芸香糖苷(quercetin 3-O-rutinoside,4)、槲皮素-7-O-β-D-吡喃葡萄糖苷(quercetin-7-O-β-D-glucopyranoside,5)、槲皮素-4'-O-β-D-吡喃葡萄糖苷(quercetin 4'-O-β-D-glucopyranoside,6)、槲皮素-3'-甲氧基-3-O-芸香糖苷(quercetin 3'-methoxy-3-O-β-D-rutinoside,7)、杨梅素-3-O-β-D-吡喃葡萄糖苷(myricetin-3-O-β-D-glucopyranoside,8)和芹菜素-4'-O-β-D-吡喃葡萄糖苷(apigenin-4'-O-β-D-glucopyranoside,9)。结论化合物3、7、9为首次从蜀葵属中分离得到,化合物6为首次从蜀葵花中分离得到。     

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.     

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...     

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.