顺-3-甲基芬太尼的4-N-丙酰基结构类似物的合成与镇痛活性及构效关系的研究

以不同电性的基团取代顺-3-甲基芬太尼中4-N-丙酰基上的乙基,合成某些顺-3-甲基芬太尼的结构类似物。药理试验结果表明,所合成的化合物均有典型的吗啡样作用。化合物3的镇痛活性略强于顺-3-甲基芬太尼。应用半经验的INDO方法对4个代表化合物进行了量子化学计算,讨论了电子结构与镇痛活性间的关系,化合物3由于氯乙烯基的引入具有与顺-3-甲基芬太尼不同的电子结构特征,氯乙烯基可能作为电子接受体参与了与受体的作用。     

顺-3-甲基芬太尼的4-N-丙酰基结构类似物的合成与镇痛活性及构效关系的研究

以不同电性的基团取代顺-3-甲基芬太尼中4-N-丙酰基上的乙基,合成某些顺-3-甲基芬太尼的结构类似物。药理试验结果表明,所合成的化合物均有典型的吗啡样作用。化合物3的镇痛活性略强于顺-3-甲基芬太尼。应用半经验的INDO方法对4个代表化合物进行了量子化学计算,讨论了电子结构与镇痛活性间的关系,化合物3由于氯乙烯基的引入具有与顺-3-甲基芬太尼不同的电子结构特征,氯乙烯基可能作为电子接受体参与了与受体的作用。     

N-(1-乙氧羰基-3-苯氨甲酰基丙基)甘氨酰甘氨酸衍生物的合成

报道4个N-(1-[1-乙氧羰基-3-(对甲)苯氨甲酰基]丙基甘氨酰｝-N-取代甘氨酸(XI_1～4)和5个1-[1-乙(或甲)氧羰基-3-(对甲)苯氨甲酰基]丙基-4-取代-1,4-哌嗪-2,5-二酮(XII_1～5)共9个估计有血管紧张素转化酶抑制活性化合物的合成和鉴定。所有这些化合物及9个相应的酯(X_1～9)均未见文献报道。药理初试结果,化合物XII₂,XII₅,XI₄和XII₁均有较强降压活性。     

中国羊踯躅花化学成分研究

从国产杜鹃花科植物羊踯躅(Rhododendron molle G.Don)的花中分离得到两种有药理活性的成分。经光谱(IR,MS,¹HNMR,¹³CNMR,¹H-¹H COSY,¹H-¹H NOESY,¹³C-¹H COSY)等分析证明其中一种为新的四环二萜类化合物。命名为羊踯躅素Ⅲ(rhodomollein Ⅲ)(1)。     

TRILINOLEIN INHIBITS THE ADHESION OF NEUTROPHILS TO ENDOTHELIAL CELLS

1. Trilinolein is a triacylglycerol with linoleic acid as the only type of fatty acid in all three esterified positions of glycerol. It was recently reported to have a myocardial protective effect in coronary ligated rats. We now study its effect on the adhesion of human neutrophils to cultured bovine endothelial cells. 2. Pretreatment of an endothelial monolayer with trilinolein at concentrations ranging from 10^-10 to 10^-6 mol/L significantly inhibited neutrophil adhesion to endothelial cells. Trilinolein was less potent than sodium nitroprusside in inhibiting neutrophil adhesion. 3. The inhibitory effect of trilinolein was antagonized by methylene blue and N^G-nitro-L-arginine methyl ester. The inhibitory effect of trilinolein was not mediated through linoleic acid because linoleic acid did not inhibit neutrophil adhesion. 4. Pretreatment of neutrophils with trilinolein did not reduce neutrophil adhesion. However, in neutrophils activated with N-formyl-methionyl-leucyl-phenylalanine, trilinolein inhibited the neutrophil adhesion to endothelial cells. 5. We conclude that trilinolein inhibits neutrophil adhesion to the endothelial monolayer by stimulating the nitric oxide and cyclic GMP pathways in endothelial cells. It may also inhibit neutrophil adhesion by scavenging free radicals. The inhibitory effect of trilinolein on neutrophil adhesion may play a role in its myocardial protective activity.     

赤芝子实体中灵芝酸类成分的研究

自赤芝［Ｇａｎｏｄｅｒｍａｌｕｃｉｄｕｍ（Ｆｒ．）Ｋａｒｓｔ．］子实体的二氯甲烷提取物中分离得到一个新的四环三萜化合物，命名为灵芝酸ＤＭ（ｇａｎｏｄｅｒｉｃａｃｉｄＤＭ，Ｉ）。根据光谱（ＵＶ，ＩＲ，１ＨＮＭＲ，１３ＣＮＭＲ，ＭＳ２ＤＮＭＲ）分析，确定其结构为Ｉ式。同时还分离得到二个已知的灵芝酸类化合物，即灵芝酸Ａ（ｇａｎｏｄｅｒｉｃａｃｉｄＡ，Ｉ）和灵芝酸Ｃ（ｇａｎｏｄｅｒｉｃａｃｉｄＣ，ＩＩ）。     

Cyclopiazonic acid增加SHR和WKY血管平滑肌细胞Ca~(2+)-依赖性外向K~+-电流

采用全细胞及细胞贴附式斑片钳技术记录自发性高血压大鼠(SHR)和Wistar-Kyoto对照鼠(WKY)培养主动脉平滑肌细胞的Ca~(2+)-依赖性外向K~+电流[I_(k(Ca))],测定肌浆网Ca~(2+)泵抑制剂CPA对其影响.CPA能增加I_K(Ca))单通道开放时间,缩短关闭时间,增加全细胞I_(K(Ca))幅度,这些作用与Ca~(2+)相关并可被K~+通道阻断药glybenclamide阻断。CPA作用在SHR和WKY之间无明显差异。结果提示高血压状态下血管平滑肌的功能改变可能与I_(K(Ca))无关。     

导致成人与儿童患者30天脑室腹腔分流失败的原因分析（英文）

OBJECTIVE The aim of this study was to provide a comprehensive benchmark of 30-day ventriculoperitoneal(VP)shunt failure rates for a single institution over a 5-year study period for both adult and pediatric patients,to compare this with the results in previously published literature,and to establish factors associated with shunt failure.METHODS A retrospective database search was undertaken to identify all VP shunt operations performed in a single,regional neurosurgical unit during a 5-year period.Data were collected regarding patient age,sex,origin of hydrocephalus,and whether the shunt was a primary or secondary shunt.Operative notes were used to ascertain the type of valve inserted,which components of the shunt were adjusted/replaced(in revision cases),level of seniority of the most senior surgeon who participated in the operation,and number of surgeons involved in the operation.Where appropriate and where available,postoperative imaging was assessed for grade of shunt placement,using a recognized grading system.Univariate and multivariate models were used to establish factors associated with early(30-day)shunt failure.RESULTS Six hundred eighty-three VP shunt operations were performed,of which 321 were pediatric and 362 were adult.The median duration of postoperative follow-up for nonfailed shunts(excluding deaths)was 1263 days(range 525-2226 days).The pediatric 30-day shunt failure rates in the authors'institution were 8.8%for primary shunts and 23.4%for revisions.In adults,the 30-day shunt failure rates are 17.7%for primary shunts and 25.6%for revisions.In pediatric procedures,the number of surgeons involved in the operating theater was significantly associated with shunt failure rate.In adults,the origin of hydrocephalus was a statistically significant variable.Primary shunts lasted longer than revision shunts,irrespective of patient age.CONCLUSIONS A benchmark of 30-day failures is presented and is consistent with current national databases and previously published data by other groups.The number of surgeons involved in shunt operations and the origin of the patient's hydrocephalus should be described in future studies and should be controlled for in any prospective work.The choice of shunt valve was not a significant predictor of shunt failure.Most previous studies on shunts have concentrated on primary shunts,but the high rate of early shunt failure in revision cases(in both adults and children)is perhaps where future research efforts should be concentrated.     

Surgical management of hepatocellular carcinoma

Hepatocellular carcinoma(HCC) is the second most common cause of death from cancer worldwide. Standard potentially curative treatments are either resection or transplantation. The aim of this paper is to provide an overview of the surgical management of HCC, as well as highlight current issues in hepatic resection and transplantation. In summary, due to the relationship between HCC and chronic liver disease, the management of HCC depends both on tumourrelated and hepatic function-related considerations. As such, HCC is currently managed largely through nonsurgical means as the criteria, in relation to the above considerations, for surgical management is still largelyrestrictive. For early stage tumours, both resection and transplantation offer fairly good survival outcomes(5 years overall survival of around 50%). Selection therefore would depend on the level of hepatic function derangement, organ availability and local expertise. Patients with intermediate stage cancers have limited options, with resection being the only potential for cure. Otherwise, locoregional therapy with transarterial chemoembolization or radiofrequency ablation are viable options. Current issues in resection and transplantation are also briefly discussed such as laparoscopic resection, ablation vs resection, anatomical vs non-anatomical resection, transplantation vs resection, living donor liver transplantation and salvage liver transplantation.