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1.
目的:探讨微生物对青蒿素(I)的转化作用。方法:通过华根霉和雅致小克银汉霉在土豆培养基中发酵产酶,对青蒿素进行转化。结果:两株菌对底物均有转化作用,分离出去氧青蒿素deoxyartemisinin(Ⅱ),3α羟基去氧青蒿素3α-hydroxydeoxyartemisinin(Ⅲ)和9β-羟基青蒿素9β-hydroxyartemisinin(Ⅳ)共3个产物,其中Ⅳ为一新化合物,同时振荡条件下底物在无菌培养基中也能发生微量转化得到产物Ⅱ。结论:青蒿素易被实验两株真菌转化,同时过氧桥也易断裂而失去一个氧原子成为去氧青蒿素,丧失抗疟活性,起作用的可能是土豆培养基中的铁元素。  相似文献   

2.
肾上腺素能β1受体亚型特异性抗体的制备及鉴定   总被引:2,自引:0,他引:2  
[目的]制备和鉴定β1受体亚型特异性抗体。[方法]人工合成β1受体细胞膜外第二环197-222位氨基酸序列作为抗原。连接钥孔冒贝血蓝蛋白(KLH)增加抗原性后免疫兔获得抗血清,通过凝胶又扩散实验和ELISA法鉴定其效价;通过免疫荧光法及ELISA法鉴定其特异性;通过离体蛙心灌流实验鉴定其药理活性。[结果]该抗血清效价高(分别为1:64和1:10^6)、特异性强,能和心肌β1受体发生特异性结合(1:10^4-1:10^5),为异丙肾上腺素的非竞争性拮抗剂。(pD2′-1.62)。[结论]成功制备的β1受体亚型特异性抗体可能成为进一步研究β1受体分布,功能和定量的有力工具。  相似文献   

3.
目的:为了进一步揭示中药苍白秤钩风Diploclisia glaucescens 药理活性的物质基础,研究并开发其活性成分,对采自广西的苍白秤钩风藤茎的化学成分进行了系统研究。方法:经硅胶、反相硅胶和Sephadex LH-20反复柱层析分离纯化并通过波谱分析鉴定了9个化合物的结构。结果:9个化合物分别被鉴定为:(2,3)反式-N-对羟基苯乙基阿魏酰胺(1),1,5-二羟基-3-甲基-蒽酮(Ⅱ),商陆酸3-O-β-D葡萄糖醛酸-28-O-β-D葡萄糖苷(Ⅲ),商陆酸3--O-β-D葡萄糖-28-O-β-D葡萄糖苷(Ⅳ),商陆酸3--O-β-D葡萄糖醛酸苷(Ⅴ),商陆酸-3-O-β-D葡萄糖苷(Ⅵ),豆甾醇(Ⅶ),豆甾醇-3-O-β-D葡萄糖苷(Ⅷ),3-甲氧基-4-羟基-苯甲酸(Ⅸ)。结论:化合物Ⅰ,Ⅱ为首次从本属植物中分离得到,通过仔细解析Ⅱ的二维相关谱(^1H-^1HCOSY,HMQC,HMBC),对化合物Ⅱ的碳谱数据进行了重新归属。药理实验表明化合物Ⅰ具有较好的免疫增强活性,化合物Ⅳ-Ⅵ有了具有一定的免疫增强活性。  相似文献   

4.
目的:对抗疟药物青蒿素(Ⅰ)进行了生物转化研究。方法:利用长春花及银杏植物细胞悬浮培养细胞进行生物转化。用硅胶柱色谱进行产物的分离,波谱方法鉴定产物的结构。结果:此两种植物悬浮细胞体系均能将青蒿素转化成3α-羟基去氧青蒿素(Ⅱ)。结论:此两种植物悬浮细胞体系均有有效转化青蒿素。  相似文献   

5.
目的研究流苏龙胆Gentiana panthaica中的仙酮类成分。方法采用多次的硅胶柱色谱法分离纯化,并通过理化性质和光谱与波谱分析技术鉴定其化学结构。结果从流苏龙胆中分离得到6个[口山]酮类化合物,分别鉴定为:1-羟基-2,3,4,7-四甲氧基[口山]酮(Ⅰ)、1,8-二羟基-3,5-二甲氧基[口山]酮(Ⅱ)、1-羟基-2,3,4,5-四甲氧基[口山]酮(Ⅲ)、1-羟基-2,3,7-三甲氧基[口山]酮(Ⅳ)、1-羟基-2,3,5-三甲氧基[口山]酮(Ⅴ)和1,7-二羟基-2,3,5-三甲氧基[口山]酮(Ⅵ)。结论6个化合物均为首次从该植物中分离得到。  相似文献   

6.
目的:分析乌拉尔甘草Glycyrrhiza uralensis的化学成分。方法:采用正、反相硅胶柱层析分离,应用液谱方法进行结构鉴定。结果:从甘草中共分离出3个三萜皂苷、2个香豆素和8个黄酮类化合物,其中一个三萜皂苷为新化合物。结论:通过ESI-MS,^1HNMR,^13CNMR,HMQC和HMBC分析,将新三萜皂苷的结构鉴定为3-O-[β-D-葡萄糖醛酸甲酯-(1→2)-β-D-葡萄糖醛酸]-24-羟基-甘草内酯。  相似文献   

7.
大黄酸-雌激素偶联物的合成及其药理学活性   总被引:5,自引:0,他引:5  
目的:设计并合成大黄酸-雌激素偶联物,以期在保留雌激素对骨的作用的同时降低其对子宫内膜增殖的刺激。方法:经雌酚酮或雌二醇3-位酚羟基以烷基哌嗪或聚乙二醇哌嗪为桥合成与大黄酸相连的衍生物,通过MS,^1H NMR,IR确定结构,并研究目标化合物对小鼠子宫内膜增殖的影响、对体外培养小鼠胚胎长骨生长的影响。结果:合成的10个目标化合物中,部分目标物能促进体外培养小鼠胚胎长骨的生长,桥链为乙基或丙基时,化合物的活性较雌酚酮相比减弱,当桥链为三聚乙二醇时,对骨的促生长活性增强。所测定的目标物均未对小鼠显示出刺激子宫内膜增殖的作用。结论:大黄酸-雌激素偶联物保留了雌激素对骨的作用,且降低了其对子宫内膜增殖的刺激作用。  相似文献   

8.
羊齿天门冬的化学成分   总被引:3,自引:0,他引:3       下载免费PDF全文
目的:对羊齿天门冬Asparagus filicinus Ham,ex D.Don的化学成分进行研究。方法:运用多种层析分离方法进行分离纯化,通过^1H NMR、^13C NMR等波谱技术确定化合物的结构。结果:分离并鉴定了10个化合物,其中包括5个蜕皮甾酮类化合物:β-ecdysterone(1)、25-hydroxydacryhainansterone(2)、stachystemneB(3)、5-deoxykaladaslemne(4)、calonystemne(5),2个木脂紊类化合物:syrlngaresinol-4'-O-β-D-glucopyranoside(6)、(+)-nyasol(7),1个苯丙素类化合物:1-O-femloylglyceml(8),p谷甾醇(9)和β-胡萝卜苷(10)。结论:其中化合物2-10均为首次从该植物中分离得到,2为新的天然产物。  相似文献   

9.
米非司酮17位侧链代谢物[17β-羟基-11β-(4-二甲氨基苯基)-17α-(1-丙炔醇基)-4.9雌甾二烯-3-酮(4)]是米非司酮口服后主要代谢物之一。本文以3,3-乙二氧基-5(10),9(11)-雌甾二烯-17-酮(5)为起始物,经环氧化、11β位芳香烃化、17位丙炔醇化、水解制得目标产物(4),中间体和产品均以红外、核磁共振等波谱数据确证结构。  相似文献   

10.
目的:设计合成6-[4-(4-取代乙酰胺基哌嗪基)苯基]-4,5-二氢-3(2H)-哒嗪酮和6-[4-(4-取代酰胺基哌嗪基)苯基]-5-甲基-4,5-二氢-3(2H)-哒嗪酮两类化合物,寻找作用更强的血小板聚集抑制剂。方法:以乙酰苯胺为原料,经傅克反应、满尼希反应、环合反应、酰化反应合成两类中间体(M)和(N),再经缩合和取代反应得到两类目标化合物,参考Bonn方法进行体外抑制血小板聚集实验。结果:共合成目标化合物12个,其中10个属首次报道,通过元素分析,^1H-NMR确证结构。其中化合物(9)抑制血小板聚集作用的活性最强,为对照物CCI-17810的60多倍;化合物(6)、(7)、(10)、(11)、(12)的活性也优于CCI-17810.结论:目标化合物具有较强的抑制血小板聚集活性。  相似文献   

11.
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.  相似文献   

12.
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.  相似文献   

13.
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.  相似文献   

14.
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.  相似文献   

15.
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.  相似文献   

16.
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.  相似文献   

17.
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.  相似文献   

18.
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.  相似文献   

19.
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.  相似文献   

20.
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.  相似文献   

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