用微生物转化法合成4-孕甾-3,20-二酮的羟基类衍生物

目的:合成具有潜在活性的4-孕甾-3,20-二酮的羟基类衍生物.方法和结果:利用本中心筛选的总枝状毛霉(Maeor racemosus)进行微生物转化,得到的产物经熔点、红外、核磁和质谱分析,确定为预期产物14β-羟基-孕甾-3,20-二酮和7β,14β二羟基-孕甾-3,20-二酮.结论:用微生物转化法可以制备甾体的羟基类衍生物.     

5α -雄甾-2-烯-17-酮羟溴化反应产物的探讨

本文报道了5 -雄甾-2-烯-17-酮(Ⅱ)羟溴化反应产物的分离与结构。除正常产物2β-羟基-3 -溴-5 -雄甾-17-酮(Ⅳ)外,三个付产物(Ⅳa、Ⅳb和Ⅳc)的结构均经波谱及化学方法确证。它们分别为2β.3 -二溴-5 -雄甾-17-酮(Ⅳa),3 -溴-4β-羟基-5 -雄甾-17-酮(Ⅳb)和3 -羟基-4β-溴-5 -雄甾-17-酮(Ⅳc)。实验结果表明表雄酮的3-对甲苯磺酸酯(Ⅰ)经2.4.6-三甲基吡啶热消除法制备Ⅱ时,也生成并伴有5 -雄甾-3-烯-17-酮(Ⅲ)。     

3β-羟基-5,16-孕甾双稀-20-酮醋酸酯环氧化反应的研究

我们对3β-羟基-5,16-孕甾双烯-20-酮醋酸酯的(Ⅰ)环氧化反应进行了研究。当将氢氧化钠加入(Ⅰ)的甲醇溶液中时,在生成水解产物3β-羟基-5,16-孕甾双烯-20-酮(Ⅱ)的同时得到甲基化副产物3β-羟基-16α-甲氧基-5-孕甾烯-20-酮(Ⅲ)°(Ⅲ)和(Ⅱ)可互相转化。16α,17α-环氧化物的收率和质量受(Ⅲ)生成的影响,与pH值和反应时间相关。(Ⅲ)和(Ⅱ)的结构经元素分析、~1HNMR、IR和MS的测定而确证。     

鬼箭羽的化学成分研究

目的研究鬼箭羽Euonymus alatus的化学成分。方法利用硅胶、Sephadex LH-20、开放RP-C18柱色谱以及PTLC分离,经理化常数测定,结合1H-NMR、13C-NMR、EI-MS鉴定结构。结果从鬼箭羽95%乙醇提取物的氯仿萃取层中分得9个化合物,分别鉴定为表木栓醇(Ⅰ)、豆甾-4-烯-3-酮(Ⅱ)、6β-羟基-豆甾-4-烯-3-酮(Ⅲ)、β-谷甾醇(Ⅳ)、2,4-二羟基-3,6-二甲基苯甲酸甲酯(Ⅴ)、2,4-二羟基-6-甲基苯甲酸甲酯(Ⅵ)、4-甲基-7-甲氧基异苯并呋喃酮(Ⅶ)、香草醛(Ⅷ)、正二十八烷醇(Ⅸ)。结论化合物Ⅶ为一新天然产物,化合物Ⅴ~Ⅷ首次从该属植物中得到。     

狗肝菜的化学成分研究

目的对狗肝菜Dicliptera chinensis全草的化学成分进行研究。方法采用硅胶柱色谱和制备性薄层色谱进行分离、纯化,IR、NMR和MS等方法进行结构鉴定。结果从环己烷萃取部分得到13个化合物,分别鉴定为正三十六烷醇(Ⅰ)、硬脂酸(Ⅱ)、羽扇烯酮(Ⅲ)、羽扇豆醇(Ⅳ)、谷甾烷-4-烯-3-酮(Ⅴ)、豆甾烷-5-烯-7-酮-3β-棕榈酸酯(Ⅵ)、β-谷甾醇(Ⅶ)、齐墩果酸(Ⅷ)、3β,6β-豆甾烷-4-烯-3,6-二醇(Ⅸ)、6β-羟基-豆甾烷-4-烯-3-酮(Ⅹ)、3β-羟基-豆甾烷-5-烯-7-酮(Ⅺ)、去氢催叶萝芙叶醇(Ⅻ)和催叶萝芙叶醇(ⅩⅢ)。结论除Ⅱ化合物和Ⅶ外,皆为首次从该属植物中发现。     

藤黄属植物Garcinia afzelii中2个新的异戊二烯呫吨酮

藤黄属植物G.afzelii Engl.是一种广泛分布于喀麦隆和加纳的矮小树木,在加纳其叶和花用作抗菌药。作者用二氯甲烷-甲醇(1∶1)混合溶剂从其茎皮分离得到2个新的异戊二烯基化吨酮afzeliixanthone A(1)和B(2),3个已知的吨酮(3~5)以及β-谷甾醇和豆甾醇。化合物1和2的结构主要通过一维和二维核磁共振谱、质谱确定。评价了这2个新化合物和该植物粗提物的抗氧化活性。该植物茎皮用二氯甲烷-甲醇(1∶1)提取,提取物进行硅胶柱色谱分离,以正己烷、醋酸乙酯、甲醇梯度洗脱,洗脱物再反复经TLC分离得到化合物1~5,以及β-谷甾醇与豆甾醇的混合物。…     

变色马兜铃石油醚可溶性成分的分离和鉴定

从变色马兜铃Aristolochia versicolar S.M.Hwang块根醇提物的石油醚溶解部分中分得12个结晶性成分,其中8个化合物经化学和光谱测定分别鉴定为豆甾-4-烯-3,6-二酮、豆甾烷-3,6-二酮、β-谷甾醇、马铃兜酸A、马兜铃酸A-甲酯、6-甲氧基马兜铃次酸甲酯、胡罗卜甙和硬酯酸。其余三个可能为新化合物。经药理试验,马兜铃酸A和6-甲氧基马兜铃次酸甲酯(B_5)具抗生育作用,豆甾-4-烯-3,6-二酮具细胞毒活性。     

大白口蘑子实体的化学成分研究

目的研究大白口蘑(Tricholoma giganteum Massee)子实体的化学成分。方法大白口蘑子实体的乙酸乙酯部位经过硅胶、RP-18、Sephadex LH-20等多种材料进行分离纯化,通过现代波谱技术进行结构鉴定。结果分离鉴定了12个化合物,它们分别为:亚油酸甲酯(1)、亚油酸(2)、麦角甾-4,6,8(14),22-四烯-3-酮(3)、麦角甾-5,7,22-三烯-3β-醇(4)、过氧麦角甾醇(5)、麦角甾-7,22-二烯-3β,5α,9α-三羟基-6酮(6)、麦角甾-7,22-二烯-3β,5α-二羟基-6酮(7)、麦角甾-7,22-二烯-3β,5α,6α,9α-四醇(8)、麦角甾-7,22-二烯-3β,5α,6β,9α-四醇(9)、麦角甾-7,22-二烯-3β,5α,6β-三醇(10)、3β-O-glucopyranosyl-5α,6β-dihydroxy-ergosta-7,22-diene(11)、脑苷脂D(12)。结论化合物1-3、6-12均为首次从该种真菌中分离得到。     

11β-【4-(N,N-二甲氨基)苯基】-17α-(丙炔-1)Δ-~(4.9)一雌甾二烯-17β-羟-3-酮(RU-486)的合成

抗旱孕药物的研究对计划生育具有重要意义。Jean G T等合成了系列11-β取代19去甲基孕激素类化合物,发现11β-[4-(N,N—二甲氨基)苯基]-17α-(丙炔-1)-Δ~(4,9)-雌甾二烯-17β-羟-3-酮具有抗旱孕的活性(简称RU-486)。它是一种结构新型的抗早孕药,具有终止娠妊的作用。药理学研究表明RU-486与孕激素受体有较强的亲和力,能阻     

RP-HPLC测定注射用福美司坦的含量

福美司坦(formestane,化学名:4-羟基雄甾-4-烯-3,17-二酮)为一甾体类抗肿瘤药(Ⅰ类芳香化酶抑制剂),最早由英国Ciba-Geigy公司研制,并于1993年上市,目前国内已有申报.……     

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.