甘草黄酮类化合物的抗血管生成作用研究

【目的】 血管生成(angiogenesis)是肿瘤生长与转移过程中的重要环节。本文采用斑马鱼胚胎血管生成模型研究甘草中黄酮类化合物的抗血管生成作用及其分子机制。 【方法】 首先在斑马鱼胚胎血管生成模型中研究4种甘草黄酮类化合物(异甘草素、光甘草定、甘草查尔酮A和甘草素)的抗血管生成作用。随后,选用上述作用较强的化合物处理人肺腺癌细胞系A549制备条件培养液,采用ELISA法检测条件培养液中重要的促血管生成因子20-羟二十烷四烯酸(20-hydroxyeicosatetraenoic acid,20-HETE)和血管内皮生成因子(vascular endothelial growth factor,VEGF)含量的变化,同时采用Transwell小室模型检测血管内皮细胞(HUVEC)迁移。最后,在小鼠肝癌H22和乳腺癌4T移植瘤模型中进一步验证其作用。 【结果】 在以上4种甘草黄酮类化合物中,异甘草素和光甘草定的抗斑马鱼胚胎血管生成作用相当,但明显强于甘草素和甘草查尔酮A。异甘草素可浓度(5、10和20 μmol/L)依赖性抑制内皮细胞迁移,抑制率最高可达74.8 %。异甘草素还可浓度(5~20 μmol/L)依赖性抑制A549细胞20-HETE和VEGF分泌,抑制率分别可达72.4 %和72.3 %。异甘草素25.0和50.0 mg/kg可显著抑制小鼠肝癌H22和乳腺癌4T移植瘤的生长和血管生成。 【结论】 4种甘草黄酮类化合物均对斑马鱼胚胎血管生成具有显著抑制作用,但异甘草素和光甘草定的作用明显强于甘草素和甘草查尔酮A。异甘草素可显著抑制人脐静脉内皮细胞迁移,其机理可能与抑制20-HETE和VEGF分泌有关。下一步有待采用人肝癌和乳腺癌裸鼠移植瘤模型进行研究。     

圆果甘草化学成分的研究

从河南产圆果甘草(Glycyrrhiza Squamulosa Franch.)中分离出8个化合物。其中5个黄酮类化合物:异甘草素(isoliquiritigenin,S-1)、刺甘草查尔酮(echinatin,S-2)、芒柄花素(formonon-etin,S-3)、4’,7-二羟基黄酮(4’,7-dihydroxyflavone,S-4)、阿芙萝摩辛(afrormosin,S-5),还有胡萝卜甙(daucosterol,S-6)和蔗糖(sucrose,S-7),均为首次得自圆果甘草。此外尚有1个化合物(S-8)结构待定。     

甘草查尔酮A减轻顺铂诱导的人肾小管上皮细胞HK-2损伤的实验研究

目的 考察甘草查尔酮A对顺铂致人肾小管上皮细胞HK-2损伤的影响。方法 将点板的HK-2细胞分为对照组(不含药的培养基)、顺铂组(顺铂20μM)、合用组(顺铂20μM和甘草查尔酮A 4μM)、甘草查尔酮A组(甘草查尔酮A 4μM);采用CCK8法测定细胞增殖,流式细胞术检测细胞凋亡,q RT-PCR检测HK-2中caspase-3、caspase-8、caspase-9的m RNA水平。结果 与对照组比较,甘草查尔酮A组各项指标比较差异均无统计学意义(P> 0.05),顺铂组则细胞活力降低,凋亡率增高,caspase-3、caspase-8、caspase-9的m RNA水平增高(P <0.05);与顺铂组相比,合用组使HK-2细胞活力由(40.52±5.65)%上升到(69.42±5.54)%(P <0.05);凋亡细胞比例由(20.33±1.81)%下降到(7.77±1.98)%(P <0.05);顺铂诱导的caspase-3、caspase-8、caspase-9的m RNA水平显著降低(P <0.05)。结论 甘草查尔酮A对顺铂致伤的肾小管上皮细胞...     

栽培甘草的化学成分研究

目的对栽培甘草的化学成分进行分离和鉴定。方法采用硅胶、葡聚糖凝胶LH-20、ODS柱等分离手段对栽培甘草的化学成分进行分离;利用NM R和M S等光谱技术对化合物进行鉴定。结果分离得到10个化合物,光甘草酮(g labrone,Ⅰ)、芒柄花素(form ononetin,Ⅱ)、对羟基苯甲酸(p-hydroxyben ic ac id,Ⅲ)、甘草查尔酮A(lic-ocha lcone A,Ⅳ)、6,7-二羟基香豆素(6,7-d ihydroxy coum arin,Ⅴ)、甘草黄酮A(licoflavone A,Ⅵ)、美迪紫檀素-3-O-葡萄糖苷(m ed icarp in-3-O-g lucos ide,Ⅶ)、芒柄花苷(onon in,Ⅷ)、甘草素-4′-芹菜糖苷(liqu iritigen in-ap iosy l(1-2)-g lucos ide,Ⅸ)、异甘草素-葡萄糖芹菜糖苷(licuras ide,Ⅹ)。结论其中化合物Ⅲ、Ⅴ为本属植物首次分得,化合物Ⅰ为本种植物首次分得,10个化合物均为首次从栽培甘草中得到。     

双波长紫外分光光度法测定甘草中总黄酮的含量

为测定甘草中总黄酮的含量,本研究采用甘草甙和甘草查尔酮为双对照品,利用甘草黄酮类化合物在220～280nm、340～390nm两段波长均出现吸收峰,采用双波长法双对照品测定甘草总黄酮的含量.结果,甘草甙线性回归方程为A=0.2805 35062275C,相关系数为0.99884;查尔酮线性回归方程为A=0.0082 63.28C,相关系数为0.99986.提示吸光度值A与浓度C之间呈良好的线性关系,可按标准曲线进行定量分析.平均回收率为96.3%～98.6%,RSD小于1%.结论,双波长紫外分光光度法测定甘草中总黄酮,操作简便、快速、准确,具有良好的分析应用前景.     

甘草查尔酮A制备方法及药理作用研究进展

该文概述了甘草查尔酮A的不同制备方法,包括柱色谱法、制备色谱法、高速逆流法和生物合成法,以及国内外对甘草查尔酮A在抗炎、抗癌、抗肿瘤、抑菌、体内代谢和抗疟抗寄生虫等药理方向的研究进展。     

查尔酮类HIV整合酶抑制剂衍生物的合成

目的:合成查尔酮类HIV整合酶抑制剂衍生物。方法:本文采用经典的Claisen-Schmidt反应,在碱性条件下,以取代的苯乙酮和4-羧基苯甲醛为原料来合成查尔酮母核3-(4-羧基苯基)-1-(2-羟基-5-甲基苯基)-丙烯酮,再与不同的取代苯胺进行酰化反应得到查尔酮酰胺化合物。结果及结论:实验经过条件优化得到了3种查尔酮衍生物,并进行1H NMR和13CNMR、ESI-MS表征化合物结构。     

陈皮的药理作用及其临床应用

陈皮为常用中药,成品含挥发油1.5-2%,其中主要含右旋柠檬烯(d-limome-ne)、枸橼醛(citral)等、并含橙皮甙(hesperidin)约8.4%、新陈皮甙(ne-ohesperidin)、柑橘素(tangeretin)、川陈皮素(nobiletin)、二氢川陈皮素(citromitin)等及肌醇.橙皮甙为双氢黄酮类化合物,在碱性环境下,分子中γ-吡酮环破裂转变为查尔酮,如酸化后,又环合转变为原来的双氢黄酮类.     

查尔酮对人胃癌BGC823细胞生物学行为影响的初步研究

目的:研究查尔酮对人胃癌BGC823细胞生长抑制、细胞周期阻滞及诱导细胞凋亡的作用,为寻找预防肿瘤药物提供一定的线索.方法:细胞生长抑制采用MTT比色法检测,细胞周期阻滞用流式细胞仪检测,细胞凋亡用流式细胞仪及琼脂糖凝胶电泳检测.结果:浓度为6.25、12.5、25和50μmol/L的查尔酮呈剂量依赖性抑制BGC823细胞增殖.查尔酮诱导细胞凋亡率是对照的2.71、2.79、4.74倍.琼脂糖凝胶电泳可观测到12.5μmol/L、25μmol/L有DNA"梯子"现象.结论:查尔酮可以抑制BGC823细胞生长,并呈剂量-反应关系.查尔酮有将BGC823细胞增殖周期阻滞在G0/G1期趋势,查尔酮可以抑制肿瘤细胞的生长和增殖.     

胀果甘草的简便快速鉴定方法

目的：研究胀果甘草（Glycyrrhiza inflata Bat）的快速鉴定方法。方法利用超声辅助的乙醇提取法制备新疆胀果甘草和光果甘草的总黄酮类提取物;利用硅胶薄层色谱法分析2种甘草总黄酮提取物的斑点特征;利用制备薄层法分离薄层板上的特殊斑点并对所分离的单体成分进行结构分析。结果胀果甘草乙醇提取物在展开剂为乙酸乙酯∶甲酸∶水（8∶3∶1）的薄层色谱条件下所显示的一种特殊亮黄色斑点被鉴定为甘草查尔酮 A,色谱特征不同于其他甘草品种。结论以甘草查尔酮 A 为对照品的硅胶搏层色谱法是快速鉴别胀果甘草的简便方法,适合于甘草品种的快速鉴定及资源考察研究。     

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.     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

Acupuncture Combined with Spinal Tui Na for Treatment of Primary Dysmenorrhea in 30 Cases

Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.     

Luo Lingjie's Experience in Treating Chronic Nephropathy

In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.     

Dr.Zhang Ren's Experience in the Acupuncture Treatment of Different Diseases with the Same Therapeutic Principle

Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.     

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.     

猪肺磷脂注射液联合经鼻持续气道正压通气对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性的影响

目的 探讨猪肺磷脂注射液联合经鼻持续气道正压通气(NCPAP)对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性(CK-MB)的影响.方法 选取呼吸衰竭早产儿80例,分为观察组和对照组各40例.对照组采用NCPAP给氧治疗,观察组给予NCPAP给氧联合猪肺磷脂气管内给药.观察两组患儿治疗前及治疗12h、24 h后PaO2、PaCO2、血氧饱和度(SaO2)、pH的变化情况,检测治疗前及治疗5d后血清CK-MB水平;评估两组患儿的临床治疗效果.结果 两组患儿PaO2、PaCO2、SaO2、pH比较,差异均有统计学意义(P＜0.05),其中观察组治疗后的PaO2、SaO2、pH均高于对照组,PaCO2则低于对照组.两组的PaO2、SaO2、pH均随观察时间延长而升高(P＜0.05),PaCO2均随观察时间的延长而降低(P＜0.05).观察组治疗有效率为87.5％,显著高于对照组的70.0％ (P ＜0.05).治疗5d后两组患儿血清CK-MB水平均较前降低(P＜0.05),且观察组明显低于对照组(P＜0.05).结论 猪肺磷脂注射液气管内给药联合NCPAP可以显著降低呼吸衰竭早产儿CK-MB的含量,提高治疗有效率,起到很好的呼吸循环支持作用.