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1.
自从1966年W all等首次从喜树中分离出喜树碱并发现其具有显著抗癌活性后[1],至今已有20多种化学成分从中分离出来,包括喜树碱(cam p-tothecine,CPT)、10-羟基喜树碱、11-羟基喜树碱、10-甲氧基喜树碱、喜树次碱、白桦脂酸、喜果苷(v incoside-lactam VCS-LT)等[2,3]。人工合成  相似文献   

2.
喜树碱是我国特有植物喜树中分离得到的具有显著抗癌活性的重要次生代谢产物,利用生物技术大量生产喜树碱类抗癌药物是目前研究的热点。喜树碱生物合成途径是多酶催化的复杂过程,阐明喜树碱的生物合成机制,对应用代谢工程的策略调控代谢流量,使次生代谢朝喜树碱合成的方向进行至关重要。喜树碱有着与其他萜类化合物相同的上游合成途径,以及广泛的药物来源,因此弄清喜树碱合成机制对理解整个植物次生代谢的网络调控也具有重要意义。综述喜树碱的生物合成途径、相关酶及其表达调控,并对喜树碱的合成研究进行展望。  相似文献   

3.
喜树Camptotheca acuminata Decne.为珙桐科落叶乔木,我国特有树种,分布于我国长江流域及西南各省。喜树全株含抗肿瘤生物碱喜树碱(camptothecin,CPT)及衍生物。1966年美国的Wall等首次从喜树中分离出喜树碱,抗肿瘤实验证明这种吲哚类生物碱具有抗癌活性,但由于其副作用较大,未能实现临床应用。20世纪80年代以来的研究发现了喜树碱通过抑制拓扑异构酶Ⅰ(topoisomeraseⅠ)来发挥细胞毒性的独特抗癌机制,引发了喜树碱抗癌研究的新热潮。  相似文献   

4.
目的:考察广西不同采收期喜树果中喜树碱成分的动态积累情况,确定喜树果药材最佳采收期。方法:采用高效液相色谱法(HPLC)测定广西部分地区同一植株不同采收期喜树果中喜树碱含量。色谱条件:色谱柱:Dikma Diamonsil(钻石)C18柱(4.6mm×250mm,5μm),流动相:甲醇—水(55∶45),流速:0.8mL/min,柱温:室温,检测波长:254nm。结果:测得喜树碱在0.112~0.672μg范围内有良好线性关系,平均回收率为102.16%,RSD=2.91%(n=6)。不同采收期喜树果中喜树碱含量在0.065%~0.21%之间。结论:广西不同采收期喜树果中喜树碱成分的动态积累有一定差异,广西产喜树果最佳采收期应为每年的8,9月份。  相似文献   

5.
抗肿瘤药喜树碱及其类似物的研究开发   总被引:4,自引:0,他引:4  
自1996年发现喜树碱的抗肿瘤活性以来,对其以及其类似物的结构和活动的关系,全成工艺、制剂技术、临床研究等工作一直没有停止。喜树碱是唯一有选择性抑制DNA拓扑我酶-Ⅰ作用的植物抗癌药。研究证明,存在于喜树果实中的微量羟基喜树大理活性最高的喜树大严似物,毒副作用也明显低于喜树碱。  相似文献   

6.
不同干燥方法对喜树果中喜树碱含量的影响   总被引:1,自引:0,他引:1  
李嘉  黄瑞松  黄建猷  邓治旭 《广西医学》2006,28(11):1699-1701
目的探讨不同干燥方法对喜树果中喜树碱含量的影响。方法对采集到的喜树果鲜药材分别采用阴干、曝晒、40℃、60℃、80℃-100℃烘干的方法进行干燥,并采用HPLE法测定喜树果不同干燥品中喜树碱的含量。结果不同干燥方法对喜树果药材中喜树碱含量有一定影响,其中阴干品含量最高,40℃烘12h及60℃烘4—8h含量变化不大,曝晒(37℃)24h及40℃烘18-24h、80℃烘2-6h、100℃烘1-3h含量均有减少。结论不同干燥方法对喜树果药材中喜树碱含量有不同的影响。喜树果药材宜采用阴干或一定时间低温烘干的方法干燥。  相似文献   

7.
目的分析当年生喜树Camptotheca acuminata幼苗各部位中喜树碱的量及其生物合成途径中色氨酸合酶(TSB)和色氨酸脱羧酶(TDC)的活性。方法用HPLC检测温室内不同氮素形态下砂培喜树幼苗各部位中喜树碱的量及TSB和TDC活性。结果不同氮素形态下喜树幼苗幼叶中喜树碱量明显高于其他器官(P<0.01),其次为茎皮和成叶,根中的最低。TSB活性在不同氮素形态下以幼叶最高,茎皮、成叶和根依次减弱,与喜树碱量呈现良好的器官对应性。不同氮素形态下TDC活性的最高部位为茎皮,其次为幼叶,成叶和根很低,与喜树碱的量缺乏器官对应性。结论当年生喜树幼苗喜树碱量以及TSB和TDC活性存在明显的组织器官特异性,喜树碱的量和TSB活性最高部位为幼叶,茎皮中TDC活性最大。  相似文献   

8.
喜树碱类抗癌药的研究进展   总被引:2,自引:0,他引:2  
喜树碱 (camptothecin ,CPT)是从珙桐科植物喜树(Camptothecaacuninata)中分离提取的五环生物碱 ,是唯一有选择性抑制DNA拓扑异构酶I (TopoI)作用的植物抗癌药。该生物碱在体外对Hela细胞和L12 10 细胞及啮齿类动物具有较强的抗肿瘤活性 ,因而引起人们的广泛关注。由于喜树碱的水溶性和脂溶性都比较差 ,其钠盐的抗癌活性较低 ,临床应用受到严格限制。其后人们从喜树中分离出 10 -羟基喜树碱 (HCPT) ,合成了毒性小、抗肿瘤作用更强的喜树碱衍生物 ,使喜树碱类药物在肿瘤防治中起到了重…  相似文献   

9.
目的 建立喜树果药材中喜树碱定量测定的HPLC方法,并对不同产地喜树果药材中喜树碱的量进行比较分析。方法 用HPLC法测定喜树果药材中喜树碱的量,色谱条件:色谱柱为Dikma Diamonsil C18柱(250 mm×4.6 mm,5 μm),流动相为甲醇-水(55∶45),体积流量:0.8 mL/min,检测波长:254 nm。结果 喜树碱在0.112~0.672 μg与峰面积有良好的线性关系,平均回收率为102.19%,RSD=2.90%(n=6)。40批不同产地喜树果药材中喜树碱的量为0.031 5%~0.242 4%。结论 建立的喜树果定量测定方法准确可靠,不同产地喜树果药材中喜树碱的量有较大差异。  相似文献   

10.
喜树碱是喜树中提取的一种生物碱,在治疗胃癌中,取得了肯定效果。对肝癌也有一定的疗效。而10—羟基喜树碱(以下简称羟基喜树碱),也是从喜树中分离的另一种生物碱,在临床上对肝癌、胃癌也获得一定的疗效。喜树碱混悬剂是我国工人、科研人员在喜树碱的基础上制成又一种抗癌药物,通过临床治疗,对肝癌疗效较好,尤其结合  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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