灵芝生物碱甲和乙的合成

灵芝为担子菌类多孔菌科灵芝属植物的子实体。人工培养的有赤芝、紫芝、薄盖灵芝和树舌等。灵芝是我国广泛流传的珍贵药物之一。近年来,对于灵芝的临床疗效和药理作用做了多方面的研究,证明对慢性气管炎、慢性肝炎、冠心病、白细胞减少症、慢性克山病和神经衰弱等都有一定的疗效,特别是对神经系统和肝脏功能具有调节作用。深层培养的薄     

大花紫玉盘中新多氧取代环己烯类的结构鉴定

从番荔枝科紫玉盘属植物大花紫玉盘( Uvaria grandiflora Roxb.)根茎中分得4种新的多氧取代环己烯及已知化合物zeylenol,应用波谱分析、X-射线衍射、园二色谱和 Mosher 酯制备等手段确定了全部新化合物的结构及其绝对构型,分别命名为大花紫玉盘醇A(1),B(2),E(3)和F(4)。     

下消化道出血221例分析

0　引言　下消化道出血是消化科的常见病 ,是指十二指肠空肠移行部 ,屈氏韧带以下的小肠和大肠疾病引起的肠道出血 .有人认为一般不包括痔和肛裂出血 [1 ] .临床最常见为慢性出血 ,但有时出血量大危及生命 ,需要做紧急处理 ,现将我院1992 - 0 1/ 1999- 0 8门诊及病房收治的 2 2 1例下消化道出血进行分析 ,报告如下 :1　临床资料　男 12 0例 ,女 10 1例 ,年龄 14～ 72 (平均 42 )岁 ,病程 16 h～ 10 a.患者分别以脓血便、暗红色血便、鲜血便或果酱色血便为主诉前来就诊 ,其中有休克症状的大出血者6例 .血 Hb<110 g·L- 1 40例 ,<80 g·L- 1…     

Myocardial infarct size quantification by MR imaging early after coronary artery occlusion in dogs

The feasibility of using magnetic resonance (MR) imaging to estimate myocardial infarct size was explored in an in vitro model using only the inherent differences in contrast between infarcted and noninfarcted myocardium. Eight dogs underwent coronary occlusion; their hearts were removed 6 hours later. Estimates of T2 for normal and infarcted myocardium were derived from MR images. Infarct size was quantified anatomically using triphenyltetrazolium-chloride (TTC) staining and compared with MR estimates. The T2 values derived from the images clearly discriminated between infarcted (126 +/- 22 msec) and normal myocardium (88 +/- 10 msec, P less than .05), providing images with good contrast between normal and infarcted myocardium. Comparable differences in T2 values were also noted from spectrometric determinations. Estimates of infarct size by MR imaging compared well with TTC estimates (r = 0.98) over a wide range of infarct sizes from 3% to 29% of the left ventricular mass. These results suggest the potential for in vivo quantification of infarct size based on the inherent contrast difference between infarcted and normal myocardium.     

Ipragliflozin Does Not Prolong QTc Interval in Healthy Male and Female Subjects: A Phase I Study

Background

Ipragliflozin, a potent, selective sodium glucose cotransporter 2 inhibitor, is in development for the treatment of type 2 diabetes mellitus. The International Conference on Harmonisation recommends that the safety investigation of new drugs include characterization of each agent’s effects on the QT/QTc interval.

Objective

The goal of this study was to assess the effect on cardiac repolarization (QTc interval) of repeated oral dosing of ipragliflozin at therapeutic (100 mg/d) and supratherapeutic (600 mg/d) levels in healthy subjects.

Methods

This was a double-blind, placebo- and active-controlled, 4-way crossover study. Subjects were randomized to 1 of 4 treatment sequences each including the following 4 treatments: placebo for 7 days; ipragliflozin 100 mg/d for 7 days; ipragliflozin 600 mg/d for 7 days; and active control moxifloxacin 400 mg on day 7 only. The primary assessment of QTc was based on Fridericia’s correction for heart rate (QTcF). Continuous 12-lead ECG interval extraction assessments were conducted on day 7. The least squares mean treatment difference from placebo and corresponding 2-sided 90% CIs were calculated for QTcF up to 14 hours postdose on treatment day 7. Ipragliflozin was deemed unlikely to have a clinically relevant effect on QTcF if the upper bound of the maximum treatment difference from placebo for ipragliflozin across all time points was < 10 ms. Assay sensitivity for QTcF interval prolongation was confirmed if the lower bound of the 2-sided 90% CIs for the mean moxifloxacin QTcF difference from placebo, determined at sampling time closest to average T_max, was > 5 ms.

Results

A total of 88 subjects were randomized to treatment (n = 22 per sequence; 10 males and 12 females). The largest upper bounds of the 90% CIs of mean treatment differences from placebo were 4.44 and 3.39 ms for ipragliflozin 600 and 100 mg, respectively, in all subjects, indicating no clinically relevant effect on QTcF interval. No specific effects were observed when the data were analyzed according to sex. No subject showed outlier QTcF intervals > 480 ms or a time-matched change from baseline > 60 ms. Moxifloxacin confirmed assay sensitivity for QTcF interval prolongation; the lower bound of the 2-sided 90% CIs at 3 hours postdose was 11.7 ms (> 5 ms).

Conclusions

No clinically meaningful QTc interval prolongation was observed in these healthy subjects who received ipragliflozin doses up to 600 mg/d for 7 days. ClinicalTrials.gov identifier: NCT01232413.     

恶性肿瘤淋巴管生成与转移的研究进展

淋巴道转移是肿瘤转移的重要途径,也是判断预后的重要依据. 随着淋巴管生成因子及许多淋巴管特异性标记物的发现,肿瘤新生淋巴管调控与淋巴道转移机制研究得以深入开展. 大量的研究发现,恶性肿瘤和瘤周组织内存在新生的淋巴管,新生的淋巴管密度和淋巴管标记物的表达强度均与淋巴结转移密切相关. 这为揭示恶性肿瘤淋巴道转移机制和开发淋巴管靶向治疗提供了重要的研究途径. 现就近年来肿瘤淋巴管生成与转移的研究进展作一综述.     

银杏内酯类合成物F抗血小板激活因子和组织胺的实验研究

目的：研究银杏内酯类化合物Ｆ（简称药物Ｆ）同时拮抗组织胺（ＨＡ）和血小板激活因子（ＰＡＦ）的作用。方法：测定离体豚鼠肺组织的收缩率以及用药物Ｆ后的致敏豚鼠肺功能的变化。结果：（１）加入药物Ｆ后离体豚鼠的气管条和肺条对ＨＡ的收缩率分别由（５０．９７±１６．００）％和（５４．２４±１２．１７）％降至（２１．６９±３．８５）％和（２２．９７±１７．７８）％（Ｐ〈０．０５）；（２）药物Ｆ保护后，离体豚鼠肺