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1.
可逆性胆硷酯酶抑制剂二甲氨基甲酸-5-二氢吲哚酯的合成 总被引:1,自引:0,他引:1
为了深入研究催醒宁类化合物的结构与抑酶活性的关系,设计合成了-系列1-,3-或5-位不同取代的二氢吲哚类衍生物(中间体和终产物共24个新化合物)。中间体1,3-二甲基-5-烷氧基-2-二氢吲哚酮(A)的C3烷化。采用相转移催化方法进行;反应中还分离到三个副产物(Ⅶ~Ⅸ)。初筛结果表明:这些化合物大多有较强的抑酶活性;1,3-或5-位取代基的改变均明显影响其活性。 相似文献
2.
Braffman BH; Coleman BG; Ramchandani P; Arger PH; Nodine CF; Dinsmore BJ; Louie A; Betsch SE 《Radiology》1994,190(3):797
3.
This study was designed to determine whether the somatostatin analogue,
octreotide, could prevent embryonic loss by normalizing increased uterine
insulin-like growth factor-I (IGF-I) action related to hyperoestrogenaemia
following superovulation. Superovulated immature and
oestradiol-17beta-treated adult rats were infused with 100 or 300 microg/ml
of octreotide respectively, or injected daily with 1 or 10 microg of
octreotide from day 1 to day 3 of pregnancy. On day 3, embryos were
collected from the oviducts and uteri. Uterine luminal fluid was subjected
to embryo culture. The amounts of uterine IGF-I and IGF binding proteins
(IGFBP) were determined by radioimmunoassay and ligand binding assay
respectively. Octreotide infusion normalized uterine IGF-I action following
superovulatory and oestradiol-17beta treatment, by reducing IGF-I
concentrations and increasing IGFBP concentrations. Octreotide infusion
increased the number of normal embryos by 2.7-fold and 1.7-fold in
superovulated and oestradiol-17beta- treated rats respectively, and
reversed the detrimental effects of uterine luminal fluid on embryonic
development caused by superovulatory and oestradiol-17beta treatment. Daily
injections with octreotide had similar but reduced effects in all
parameters examined in both treatment groups. In conclusion, octreotide may
reduce embryonic loss, at least in part, by normalizing IGF-I action
following superovulation.
相似文献
4.
S Bydder NA Spry DRH Christie D Roos BH Burmeister H Krawitz S Davis DJ Joseph M Poulsen M Berry 《Journal of Medical Imaging and Radiation Oncology》2003,47(3):284-288
The purpose of this study was to prospectively examine the effectiveness and tolerability of a simple radiotherapy technique for the palliation of symptomatic liver metastases. Twenty‐eight patients with symptomatic liver metastases were enrolled from seven centres, and received targeted (partial or whole) liver irradiation consisting of 10 Gy in two fractions over 2 days. Symptoms at baseline were hepatic pain (27 patients), abdominal distension (19), night sweats (12), nausea (18) and vomiting (eight). Twenty‐two patients (76%) had failed previous treatment with chemotherapy, hormonal therapy and/or high‐dose steroids. Symptoms and potential toxicities were prospectively assessed at the time of treatment, then 2, 6 and 10 weeks later. Individual symptom response rates were 53?66% at 2 weeks. Partial or complete global symptomatic responses were noted in 15 patients (54%) overall. The treatment was well tolerated with two patients (7%) experiencing grade 3 toxicity (one vomiting and one diarrhoea); however, four patients reported temporary worsening of pain shortly after treatment. This simple and well‐tolerated treatment achieves useful palliation. 相似文献
5.
In the human erythrocyte membrane phosphatidylcholine and sphingomyelin reside mainly in the outer leaflet, whereas the aminophospholipids, phosphatidylethanolamine and phosphatidylserine, are mainly found in the inner leaflet. Maintenance of phospholipid asymmetry has been assumed to involve interactions between the aminophospholipids and the membrane skeleton, in particular spectrin. To investigate whether spectrin contributes to maintaining the phospholipid transbilayer distribution and kinetics of redistribution, we studied erythrocytes from hereditary spherocytosis patients whose spectrin levels ranged from 34% to 82% of normal. The phospholipid composition and the accessibility of membrane phospholipids to hydrolysis by phospholipases were in the normal range. Spin-labeled phosphatidylserine and phosphatidylethanolamine analogues that had been introduced into the outer leaflet were rapidly transported at 37 degrees C to the inner leaflet, whereas the redistribution of spin-labeled phosphatidylcholine was slower. The kinetics of transbilayer movement of these spin-labeled phospholipid in all samples was in the normal range and was not affected by the level of spectrin. Although these erythrocyte membranes contained as little as 34% of the normal level of spectrin and were characterized by several physical abnormalities, the composition, distribution, and transbilayer kinetics of the phospholipids were found to be normal. We therefore conclude that spectrin plays, at best, only a minor role in maintaining the distribution of erythrocyte membrane phospholipid. 相似文献
6.
Styles LA; Schalkwijk CG; Aarsman AJ; Vichinsky EP; Lubin BH; Kuypers FA 《Blood》1996,87(6):2573-2578
Acute chest syndrome (ACS) is associated with significant morbidity and is the leading cause of death in patients with sickle cell disease (SCD). Recent reports suggest that bone marrow fat embolism can be detected in many cases of severe ACS. Secretory phospholipase A2 (sPLA2) is an important inflammatory mediator and liberates free fatty acids, which are felt to be responsible for the acute lung injury of the fat embolism syndrome. We measured SPLA2 levels in 35 SCD patients during 20 admissions for ACS, 10 admissions for vaso-occlusive crisis, and during 12 clinic visits when patients were at the steady state. Eleven non-SCD patients with pneumonia were also evaluated. To determine if there was a relationship between sPLA2 and the severity of ACS we correlated SPLA2 levels with the clinical course of the patient. In comparison with normal controls (mean = 3.1 +/- 1.1 ng/mL), the non- SCD patients with pneumonia (mean = 68.6 +/- 82.9 ng/mL) and all three SCD patient groups had an elevation of SPLA2 (steady state mean = 10.0 +/- 8.4 ng/mL; vaso-occlusive crisis mean = 23.7 +/- 40.5 ng/mL; ACS mean = 336 +/- 209 ng/mL). In patients with ACS sPLA2 levels were 100- fold greater than normal control values, 35 times greater than values in SCD patients at baseline, and five times greater than non-SCD patients with pneumonia. The degree of SPLA2 elevation in ACS correlated with three different measures of clinical severity and, in patients followed sequentially, the rise in SPLA2 coincided with the onset of ACS. The dramatic elevation of SPLA2 in patients with ACS but not in patients with vaso-occlusive crisis or non-SCD patients with pneumonia and the correlation between levels of SPLA2 and clinical severity suggest a role for SPLA2 in the diagnosis and, perhaps, in the pathophysiology of patients with ACS. 相似文献
7.
In order to study the pattern of B cell involvement in acute nonlymphocytic leukemia (ANLL), multiple B lymphoid cell lines were established by Epstein-Barr virus transformation of peripheral blood mononuclear cells from two patients with the disease who were heterozygous for the X chromosome-linked glucose-6-phosphate dehydrogenase (G6PD). In one patient, the progenitor cells involved by the leukemia exhibited multipotent differentiative expression, whereas in the other patient the cells showed differentiative expression restricted to the granulocytic pathway. In the patient whose abnormal clone showed multipotent expression, the ratio of B-A G6PD in B lymphoid cell lines was skewed in the direction of type B (the enzyme characteristic of the leukemia clone) and significantly different from the 1:1 ratio expected. It is, therefore, likely that the neoplastic event occurred in a stem cell common to the lymphoid series as well as to the myeloid series. In contrast, evidence for B cell involvement was not detected in the patient whose ANLL progenitor cells exhibited restricted differentiative expression. These findings underscore the heterogeneity of ANLL. Clinically and morphologically similar malignancies in these two patients originated in progenitors with different patterns of stem cell differentiative expression. This difference may reflect differences in cause and pathogenesis. 相似文献
8.
Gupta Mudit Kandula Srinivas Reddy Satheesha BH 《Ethiopian journal of health sciences》2014,24(4):285-290
Background
The lateral cephalogram is the most common diagnostic radiograph used in clinical orthodontics. Significant cervical spine pathology can be detected on the routine lateral cephalogram. The aim of this study is to sensitize clinicians for examining the cervical area of lateral cephalogram carefully and thus record anatomical variations.Materials and Methods
The presence and types of ponticuli posticus were investigated on 650 lateral cephalograms which were randomly selected from archived records at AECS Maaruti College of Dental Sciences & Research Centre, BangaloreResults
The prevalence rate of Ponticulus Posticus in our study was found to be 11.1%. Though there was slight female predominance of 11.7% as compared to 10.4% in males, difference was not statistically significant.Conclusion
Ponticulus posticus is a common anomaly in the Indian population. If any such anomaly is detected or suspected, it must be documented in the patient''s health record and specialist consultation must be sought. The lateral cephalogram must thus be considered as one of the baseline screening tool for detecting anomalies and pathology in the cervical spine region. 相似文献9.
温热治疗肿瘤的基础研究进展 总被引:2,自引:1,他引:1
在肿瘤治疗学中,温热治疗是指运用不同方法对恶性肿瘤进行热治疗,他常与放疗、化疗联用,肿瘤的温度常在40-43℃.现综述温热治疗的细胞死亡、体内温热治疗的特征以及温热治疗的效应器等方面的研究进展. 相似文献
10.
Grossman RI; Braffman BH; Brorson JR; Goldberg HI; Silberberg DH; Gonzalez- Scarano F 《Radiology》1988,169(1):117-122
Thirteen patients with definite multiple sclerosis (MS), studied 16-24 months previously with magnetic resonance (MR) imaging with and without enhancement by intravenously administered gadolinium diethylenetriaminepentaacetic acid (DTPA) dimeglumine, were reexamined with a similar protocol. Assessment of enhancement and clinical activity in both studies revealed that enhancement was observed in 13 of 14 cases in which clinical activity had changed within 4 weeks of the study and thus appeared more sensitive than clinical examination in determining active disease. The 3-minute postinjection, short repetition time image (TR) was the most efficient for depicting enhancement. Enhancing lesions (active plaques) arose from previously hyper- or isointense regions on long TR images. Previously active lesions reverted to areas of iso- or hyperintensity on long TR images. Serial comparison of long TR images in this population reveals a decrease in high-intensity lesions on long TR images in some cases and an increase in others. The findings of high-intensity regions on long TR images and previously enhancing lesions both becoming isointense suggests that transient inflammatory changes with concomitant edema without demyelination and/or with significant remyelination may occur in some MS lesions. MS lesions are dynamic; both active and inactive lesions may show dramatic change on longitudinal MR imaging studies. 相似文献