7β-(4,7-二取代香豆素-3-乙酰胺基)头孢菌素衍生物的合成及抗菌活性

以4,7-二取代香豆素-3-乙酸为侧链酸,用酰氯法与7-ACA,7-ADCA,7-ACT及一系列的3-取代苯甲基头孢母核<5c-5f)进行缩合,合成了一系列7β-(4,7-二取代香豆素-S-乙酰胺基)头孢菌素衍生物(2a-2m)。并且研究了7-ACA的3位乙酰氧基被取代酚取代及2a的3位乙酰氧基被取代吡啶取代的亲核取代反应,分别合成了一系列3-取代苯甲基头孢母核(5c-5f)及3-取代吡啶离子甲基头孢菌素衍生物(2n,20)。体外抑菌活性试验结果表明,所合成的14个新的头孢菌素衍生物对包括青霉素耐药菌株在内的革兰氏阳性菌都有较强的抑菌作用。     

6-取代香豆素-3-甲酰胺头孢菌素的合成

本文以6-取代香豆素-3-羧酸与头孢菌素母核缩合,合成了15个未见文献报道的6取代香豆素-3-甲酰胺头孢菌素化合物。其合成方法采用了Vilsmeier试剂法,改进了溶媒及摩尔配比,并进一步探索了分离纯化的过程,以元素分析、IR及NMR确证结构。抑菌试验表明,对某些革兰氏阳性菌具有不同程度的抑菌作用,而某些革兰氏阴性菌的效果则不明显。     

蒙药小白蒿化学成分的研究

目的 研究小白蒿Artemisia frigida氯仿和醋酸乙酯提取物中的化学成分。方法 采用硅胶和LH-20柱色谱法进行分离,运用各种波谱法和标准品对照法鉴定分离得到的化合物。结果 鉴定了13个化合物,分别为槲皮素(Ⅰ)、木犀草素(Ⅱ)、5,7,3′-三羟基-4′-甲氧基黄酮(Ⅲ)、5,7,3′-三羟基6,4′-二甲氧基黄酮(Ⅳ)、5,3′-二羟基-6,7,4′-三甲氧基黄酮(Ⅴ)、5,3′-二羟基3,6,7,4′-四甲氧基黄酮(Ⅵ)、对甲基苯酚(Ⅶ)、7-羟基香豆素(Ⅷ)、7-甲氧基香豆素(Ⅸ)、咖啡酸(Ⅹ)、β-谷甾醇(Ⅺ)、6,7-二羟基香豆素(ⅩⅡ)、7-羟基-5,6-二甲氧基香豆素(ⅩⅢ)。结论 所有化合物均为首次从该植物中分得。     

3-胺基苯丙酮、1-苯基-3-胺基丙醇类化合物的合成及其生物活性

本文合成了10个3-胺基苯丙酮(Ⅴ_(a-e))及1-苯基-3-胺基丙醇(Ⅵ_(b-e'))类新化合物。初步药理实验表明:Ⅴ_(a-e)均具有不同程度的正性肌力作用,其中Ⅴ_a的PEC_(50)为4.3±0.7(%),Ⅵ_(b-e')均具有较弱的负性肌力作用,其中Ⅵ_d还具有较强的利尿作用。     

单胺菌素衍生物的合成

以6-取代香豆素-3-甲酸、D-(-)-取代苯甘氨酸及L-苏氨酸为原料,合成了(3S,4S)-3-(6-取代香豆素-3-甲酰胺基-)-4-甲基-2-吖啶丁酮-1-磺酸钾(Ⅰ_(a-f)),(3S,4S)-3-(D-(-)-α-(6-取代香豆素-3-甲酰胺基-)苯乙酰胺基-)4-甲基-2-吖啶丁酮-1-磺酸钾(Ⅱ_(a-f))及(3S,4S)-3-(D-(-)-α-(6-取代香豆素-3-甲酰胺基-)对羟基苯乙酰胺基-)4-甲基-2-吖啶丁酮-1-磺酸钾(Ⅲ_(a-f))。初步体外抑菌试验结果表明,化合物Ⅱ_(a-f)及Ⅲ_(a-f)均有不同程度的广谱抗菌活性,化合物Ⅰ_(a-f)未显示明显的抗菌活性。     

(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠衍生物的合成与抗菌活性

以(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠为母核,选择D-(-)-2-(7或8-甲氧基香豆素-3-甲酰胺基)-2-苯或4-羟基苯乙酸和D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-苯或4-羟基苯乙酸作为边链,合成6个新的单胺菌素衍生物:(3S,4S)-3-[D-(-)-2-(8或7-甲氧基香豆素-3-甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(1-4);(3S,4S)-3-[D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(5-6)。初步体外抑菌试验表明,化合物Ⅳ_5,Ⅳ_6对革兰氏阴性菌有较强的抗菌活性。     

穿龙薯蓣地上部分的化学成分

目的研究穿龙薯蓣地上部分的化学成分。方法应用多种色谱技术进行分离纯化,根据化合物的理化性质和光谱数据分析鉴定其结构。结果得到10个化合物,分别鉴定为7-羟基-2,6-二甲氧基-1,4-菲醌(Ⅰ)、山柰酚-3-O-β-芸香糖苷(Ⅱ)、山柰酚-3-O-β-D-吡喃葡萄糖苷(Ⅲ)、(3S)-6,8-二羟基-3-苯基-3,4-二氢异香豆素(mon-troumarin,Ⅳ)、4′,5-二羟基-3,3′-二甲氧基联苄(Ⅴ)、薯蓣皂苷元(Ⅵ)、胡萝卜苷(Ⅶ)、β-谷甾醇(Ⅷ)、甘露醇(Ⅸ)、正癸烷(Ⅹ)。结论化合物Ⅰ~Ⅴ均为首次从该属植物中获得。     

(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠衍生物的合成与抗菌活性

以(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠为母核,选择D-(-)-2-(7或8-甲氧基香豆素-3-甲酰胺基)-2-苯或4-羟基苯乙酸和D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-苯或4-羟基苯乙酸作为边链,合成6个新的单胺菌素衍生物:(3S,4S)-3-[D-(-)-2-(8或7-甲氧基香豆素-3-甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(1-4);(3S,4S)-3-[D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(5-6)。初步体外抑菌试验表明,化合物Ⅳ_5,Ⅳ_6对革兰氏阴性菌有较强的抗菌活性。     

氮杂黄酮研究——Ⅱ.6,8-二氮杂异黄酮类化合物的合成

本文报道6,8-二氮杂—5,7-二羟基和6,8-二氮杂—5,7-二羟基-4′-甲基异黄酮以及它们相应的中间体的合成。在合成6,8-二氮杂异黄酮类化合物的过程中分离得到对环三苯乙酰化合物V和对羟基苯乙酸交酯Ⅵ两种副产物。     

滨蒿化学成分的研究

目的:研究滨蒿Artemisia scoparia Waldst.et kit.化学成分,阐明其药理作用物质基础.方法:薄层层析,硅胶反复柱层析,波谱分析技术和理化常数对照.结果:从80%乙醇提取物中分离并鉴定了9个化合物,分别为7-甲氧基香豆素(7-Methoxycoumarine,Ⅰ),Isosabandin(Ⅱ),6,7-二甲氧基香豆素(6,7-Dimethylesculetin,Ⅲ),6-羟基-7-甲氧基香豆素(7-Methylesculetin,Ⅳ),7-羟基-6-甲氧基香豆素(Scopoletin,Ⅴ),茵陈色原酮(Capillarisin,Ⅵ),绿原酸正丁酯(Chlorogenic acid butyl ester,Ⅶ),Isoscopoletin-β-D-glucopyranoside(Magnolioside,Ⅷ),β-谷甾醇(β-Sitosterol,Ⅸ).结论:化合物Ⅰ、Ⅱ、Ⅵ、Ⅶ为首次从该植物中分得,化合物Ⅶ为首次从该属植物中分离得到.根据HMBC首次对Isosabandin(Ⅱ)和茵陈色原酮(Ⅵ)的碳谱数据进行了归属.     

Value of D-Dimers in patients with acute aortic dissection

Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P ＜ 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (＞0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P ＜0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P ＜ 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.     

Research of combined liver-kidney transplantation model in rats

Objective： To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods： SD rats served as both donors and recipients. 4℃ sodium lactate Ringer＇s was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava （IVC） inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results： Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion： This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.     

BLOOD PRESSURE CHANGE WITH AGE IN SALT-SENSITIVE TEENAGERS

Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P＜ 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P＜ 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.     

安心颗粒对急诊经皮冠状动脉介入术后生活质量影响的研究

目的：评价使用安心颗粒对急诊经皮冠状动脉介入术（PPCI）术后生活质量的影响.方法：将160例接受PPCI的急性ST段抬高型心肌梗死患者随机分为安心颗粒组（术前顿服安心颗粒8.8g,术后安心颗粒4.4 g/次,每日2次）和对照组（仅接受基础药物治疗）.所有患者均服用阿司匹林、氯吡格雷和阿托伐他汀.分别在入院时、出院前1d、出院后180 d时,应用心肌梗死多维度量表（MIDAS）、中文版SF-36评价量表对患者生活质量评分.并观察术后30 d以内的出血并发症、血小板减少症发生情况.结果：入院时和出院前1d,两组患者的心肌梗死MIDAS、SF-36量表评分比较无差异（P＞0.05）;出院后180 d时,与对照组比较,安心颗粒组MIDAS、SF-36评分明显减低（P＜0.05）;组内与入院时比较,两组出院前1d、出院后180 d时,MIDAS、SF-36评分均降低（P＜0.05）.两组患者在随访期间均无大量出血、少量出血、重度和极重度血小板减少症发生,安心颗粒组有4例、对照组有7例发生不明显出血（P＞0.05）.两组发生轻度血小板减少症的患者数比较无差异（P＞0.05）.结论：PPCI使用安心颗粒,能改善急性ST段抬高型心肌梗死患者的生活质量,且不增加出血风险.     

The comparative studies of the influences of Urapidil and Nicardipine on sino-atrial node function, atrio-ventricular node function and hemodynamics

Objective:To investigate the influences of urapidil and nicardipine on rabbit sinus function,atrio-ventricular node function and hemodynamics.Methods:Thirty-two Angora's rabbits were selected and randomly divided into four groups.U1 group:urapidil 0.25 mg/kg;U2 group:urapidil 0.5 mg/kg;N1 group:nicardipine 10 μg/kg;N2 group:nicardipine 20 μg/kg.All these medicine were administrated within 30 seconds.Measurements were taken before and after the administration of urapidil or nicardipine for the following data:mean blood pressure(MAP),heart rate(HR),sino-atrial conduction time(SACT),maximal sinoatrial recovery time(SNRTmax)corrected sinus node recovery time(CSNRT),index of sinus node recovery time(SNRTI),Wenckebach A-V conduction frequency (WB),and P-R interval.Results:Significant MAP and HR changes were identified in all of the four groups before and after administration of both urapidil and nicardipine.No significant changes could be found in the rest of the parameters.Intergroup analysis showed that SACT and CSNRT of N1 and N2 groups were shorter than those of the U2 group(P＜0.01);the MAP decreased(P＜0.01)and the HR increased drastically(P＜0.01).Conclusions:Neither urapidil(0.25 mg/kg,0.5 mg/kg)nor nicardipine(10μg/kg,20μg/kg)has any significant influence on rabbit sinus function or rabbit atrio-ventricular node function.Nicardipine could be a better choice than urapidil for parafunctional sinus node patients.     

Expression of OPGmRNA and ODFmRNA in the patients of hip fracture due to osteoporosis

Objective：To investigate the gene expression of osteoprotegerin（OPG） and osteoclast differentiation factor（ODF） in the bone tissue of patients with hip fracture due to osteoporosis. Methods：OPGmRNA and ODFmRNA in the bone tissue in 50 cases of osteoporosis sufferers（over 50 years old） with hip fracture（Observer Group） and 30 cases of hip facture sufferers with no osteoporosis（Control group） were analyzed with the Semi-Quantitative RT-PCR method. Results：The mRNA expressed of ODF, OPG were both high in the patients with hip fracture. In the control group, the expression of OPG mRNA was observed, while the expression of ODF mRNA was very slight. Conclusion：Aged patients contained all signals including OPG, ODF that are essential for inducing osteoclastogenesis and promoting bone resorption.     

The clinicopathological and immuohistochemical analysis of solid-pseudopapillary tumor of the pancreas： report of 9 cases

Objective：To investigate the clinical features, pathological characteristics and immunophenotype of solid-pseudopapillary tumor of the pancreas（SPTP）. Methods：Nine surgically treated cases of SPTP were retrospectively reviewed. Hematoxylin and Eosin（HE） staining and immunohistochemical staining were used to analyze all cases, and the general clinical data was collected. Results：Six patients were asymptomatic except for a palpable mass. Two patients complained of vague-epigastric pain. One patient appeared jaundice. The tumor was encapsulated and solid tissues alternately with cystic tissues. Histologically, the histological structure of solid portion was pseudopapillary with a fibrovascular core. Tumor cells were uniform and medium-sized which were arranged in sheets ets or nests or pseudopapillary patterns. Immunohistochemical studies demonstrated that SPTP proved positive in vimentin（9/9 cases）, AAT（9/9 cases）, NSE（9/9 cases）, ACT（7/9 cases）, CK20（2/9 cases）, CgA（1/9 cases）, S-100（3/gcases）, PR（4/gcases）, Syn（3/9 cases） and CD56（5/9cases）, negative in CEA and ER. Conclusion：SPTP is a tumor predominantly occurring in young women frequently without special symptoms. This tumor has various characteristical histological patterns with different immunophenotype.     

Dynamic Changes in Serum Estradiol and Progesterone levels in Patients of Premenstrual Syndrome with Adverse Flow of Liver-qi

Objective:To probe into the influence of changes of ovarian hormones on the pathogenesis of the specific sub-type premenstrual syndrome(PMS)and reveal partial microcosmic mechanisms of adverse flow of liver-qi.Methods:Estradiol(E2)and progesterone(P)levels in serum were determined at different phases of menstrual cycle by radioimmunoassay.Results:In the group of PMS with adverse flow of liver-qi.the secretive peak value Of E2 and P at the follicular phase significantly decreased,and the secretive peak value at the luteal phase did not come into being.Conclusions:Low E2 and P secretive peak at the follicular phase and absence of secretive peak at the luteal phase is one of the microcosmic mechanisms of PMS with adverse flow of liver-qi.One of the pathophysiologic mechanisms of specific sub-type PMS is probably the continuous low level of E2and P.     

Real-time Three-dimensional Echocardiography in Assessment of Left Ventricular and Right Ventricular Volumes

Real-time three-dimensional echocardiography (RT3DE)is a new ultrasound technique that enables dynamic threedimensional visualization and quantification of the heart in real time. Investigation of feasibility and methodology of RT3DE in determining left ventricular (LV) and right ventricular (RV) volumes, RT3DE was performed in 35 normal adults using Philips SONOS 7500 system with a 2-4 MHz matrix array transducer. The 60°×60° "pyramid" volume database was obtained and analyzed on a TomTec echo workstation. Both LV and RV volumes were calculated with four 3DE methods (i.e. apical 2, 4, 8, and 16-plane) through manually tracing ventricular endocardial borders in end diastole and end systole. Stroke volumes were then calculated. LV volume was also measured by 2DE Simpson's rule using GE VIVID 7 ultrasound machine.     

SCREENING FOR A 21-CHROMOSOME ABNORMALITY IN PREIMPLANTED EMBRYOS OF ELDERLY WOMEN

Increasing maternal age is the only etiological factor unequivocally linked to Down's syndrome in humans. The occurrence rate of newborns with Down's syndrome is about 1/220 in women over 35 years old. However, the occurrence rate in embryos fertilized in vitro, of the elder woman is unclear. Using FISH we screened the number of chromosome 21 in preimplanted embryos of 5 elderly women (average age, 38.4 years) to study the feasibility and necessity of screening trisomy 21 in embryos in patients over 35 years old at the in vitro fertilization (IVF) center.