N-（噻唑-2-基）-[1-（4-氯苄基）吲哚-3-基]草酰胺的合成及抗肿瘤活性

【目的】研究N-（噻唑-2-基）-[1-（4-氯苄基）吲哚-3-基]草酰胺的合成方法,探讨抗肿瘤活性。【方法】以吲哚为原料,经3步反应合成了新的吲哚草酰胺化合物,结构经质谱及核磁共振谱证实。用MM法评价它的体外抗肿瘤活性。【结果】合成了N-（噻唑-2-基）-[1-（4-氯苄基）吲哚-3-基]草酰胺及其衍生物。前者对HeLa的半数抑制率IC50为1-20μmol,SKOV3为6．55μmol;其衍生物对HeLa的半数抑制率IC50为3．65μmol,SKOV3为4．87μmol。【结论】N-（噻唑-2-基）．[1-（4-氯苄基）吲哚-3-基]草酰胺及其衍生物均具有强效的抗肿瘤活性。     

锐孔-凝固浴法制备薏苡仁酯微胶囊的工艺研究

目的探讨锐孔-凝固浴法制备薏苡仁酯微胶囊化的工艺条件，得出包埋率高、感官质量好的薏苡仁酯微胶囊产品。方法丙酮为溶剂提取薏苡仁酯；以海藻酸钠为壁材，锐孔一凝固浴法进行微胶囊化。结果正交实验得出微胶囊化最佳工艺条件：壁材海藻酸钠初始溶液的质量浓度为8g/L，芯材薏苡仁酯与壁材海藻酸钠的质量之比为0．6：1，乳化剂在壁材与芯材乳化分散液中的质量浓度为单甘酯0．5g／L及蔗糖酯0．5g／L，固化液CaCl2的质量浓度为10g／L。结论由此得到的微胶囊于室温下鼓风干燥，包埋率达80．4％，包埋效果好。     

高良姜乙醇提取物微囊的制备及其性能表征

【目的】探究高良姜乙醇提取物微囊的最佳制备工艺及其性能表征。【方法】以阿拉伯胶（GA）-壳聚糖（CS）为囊壁材料,采用复合凝聚法制备微囊,以载药量和包封率为指标,通过正交设计法筛选微囊最佳制备工艺,并采用高效液相色谱（HPLC）法测定微囊中高良姜乙醇提取物的含量,利用红外光谱仪及扫描电子显微镜对所制备的微囊进行性能表征。【结果】高良姜乙醇提取物微囊的最佳制备条件为壁材比（GA/CS） 6∶1,芯壁比1∶1,凝聚时间45 min,固化剂用量3 mL。此条件下制备高良姜乙醇提取物微囊的载药量为27.17%,包封率为80.07%,且高良姜乙醇提取物微囊缓释性能优于高良姜乙醇提取物。【结论】复合凝聚法制备高良姜乙醇提取物微囊具有较好的包封性,方法简单且稳定可靠,可行性高。     

月见草油-姜黄素微胶囊制备及对动脉硬化大鼠脂质代谢初探

目的:拟考察以月见草油同姜黄素制备微胶囊的方法及其形状,并进一步的考察其对动脉粥样硬化模型大鼠的治疗效果。方法:首先以喷雾干燥的方式制备微胶囊,以姜黄素-月见草油及半合成脂肪酸甘油酯为芯材,并以明胶及β-环糊精为壁材,制备微胶囊。通过对微胶囊表征参数及溶出特性的测定后,确定其产品的稳定性,并进一步的考察其溶出度以及其对动脉粥样硬化模型大鼠的治疗效果。结果:根据之前设定的配方可设定配置产品的配方为:芯材∶壁材=1∶20,明胶∶β-环糊精=1∶1,姜黄素∶月见草油∶半合成脂肪酸甘油酯=1∶40∶2,最终可以获得形态稳定的微胶囊,微胶囊的粒径范围在2.7~8.8μm,平均粒径为6.2μm。经过计算,该微胶囊包埋率为28.8%,SEM结果显示,其颗粒稳定光滑无裂痕。根据红外光谱的结果可知,该微胶囊的芯材同壁材是通过物理键相结合的,同时,本微胶囊在模拟胃液中稳定,释放程度较低,而在模拟肠液中,其释放程度较高,而且可以达到缓释释放的目的。而制得的月见草-姜黄素微胶囊可以显著性的降低大鼠的血脂参数,经过12周的灌胃,大鼠的TG、TC、LDL-C及HDL-C水平均显著下降。HE染色显示,微胶囊组的血管同立普妥组类似,与模型组比较,内膜较光滑,平滑肌细胞排列较规则,炎性细胞浸润减少。结论:以月见草油同姜黄素制备的微胶囊稳定性及生物利用度均有所提高,并抑制了高脂饮食模型大鼠的动脉硬化形成,其机制可能与调节脂质代谢相关。     

N-甲基-N-顺式-苯乙烯基-桂皮酰胺对青霉素 致痫大鼠痫样放电的影响

 【目的】 探讨黄皮核提取物N-甲基-N-顺式-苯乙烯基-桂皮酰胺对青霉素(PNC)诱发大鼠癫痫的影响&#65377;【方法】 32只SD大鼠随机分成正常对照组 (20 mL/L吐温80 + 生理盐水)&#65380;模型对照组 (20 mL/L吐温80 + PNC)&#65380;低剂量桂皮酰胺组(桂皮酰胺75 mg/kg + PNC)&#65380;高剂量桂皮酰胺组(桂皮酰胺150 mg/kg + PNC),每组8只&#65377;建立大鼠皮层定位注射青霉素诱发惊厥模型,观察并分析两剂量的桂皮酰胺腹腔注射前处理给药对造模后大鼠惊厥发作程度和皮层脑电图的影响&#65377;【结果】 两种剂量的N-甲基-N-顺式-苯乙烯基-桂皮酰胺均可减轻大鼠癫痫发作程度,延长痫样放电的潜伏期,减少痫波持续时间,在发作后期减少痫波发放频率,与模型对照组比较,差异明显(P < 0.05或P < 0.01)&#65377;然而,对于棘波最高和最低波幅的影响,桂皮酰胺组与模型对照组比较差异无统计学意义(P > 0.05)&#65377;【结论】 天然产物黄皮核提取物N-甲基-N-顺式-苯乙烯基-桂皮酰胺对大鼠皮层定位注射青霉素诱发的惊厥发作和痫样放电具有明显的抑制作用,该天然产物具有一定的抗惊活性&#65377;     

改性胺微胶囊固化剂制备工艺的优化与性能

以改性胺1618固化剂为囊芯、脲醛树脂为壁材单体,采用界面聚合技术,成功制备了一种新型聚脲改性胺微胶囊固化剂。通过正交设计试验,考察了芯壁质量比、乳化剂种类和质量分数及搅拌速率对微胶囊包覆率、粒径大小及分布情况的影响,并确定了最佳制备工艺条件。采用马尔文激光粒度仪、扫描电镜对微胶囊粒径大小、分布情况及表面形貌进行表征,采用热重分析仪及傅里叶变换红外光谱对其化学结构进行表征,通过拉伸试验对自修复材料的断裂力学性能进行研究。结果表明,该微胶囊含有固化剂芯材,其热稳定温度为198 °C,当芯壁质量比为0.7∶1、乳化剂为阿拉伯胶、乳化剂质量分数为1.5%、搅拌速率为800 r/min时,所制备的微胶囊包覆率达到79.8%,平均粒径为207.5 nm,呈规则的球形,分散性及表面致密性好。当基体材料中加入质量分数为1%的微胶囊后,拉伸强度提高64%,弹性模量提高287%。     

杜仲叶提取物微胶囊化研究

目的：探讨杜仲叶提取物微胶囊化壁材选取及最佳配比工艺研究。方法：选用阿拉伯胶和β-环状糊精（1：1）做为杜仲叶提取物的微胶囊壁材，利用喷雾干燥进行微胶囊化。结果：阿拉伯胶和β-环状糊精（1：1）做为杜仲叶提取物的微胶囊壁材，微胶囊化能达到较好的效果，芯材与壁材的最佳配比为0．1g／g。     

花椒油的超临界CO2萃取与微胶囊的直接制备

研究了超临界CO2萃取花椒油,并直接采用同轴喷嘴喷雾干燥制备微胶囊。考察了相同的萃取压力、温度、时间和壁材浓度下,壁材流量、CO2流量和干燥温度对包埋率的影响,对不同干燥条件下获得的微胶囊形态的电镜扫描结果进行了比较。结果表明:花椒油微胶囊制备的最佳工艺条件为:壁材进样量为1mL/min,CO2气体流量为2 L/min,进风温度为80℃。在此基础上得到的微胶囊包埋率达57.8%,相对包埋率达77.4%。     

五指毛桃不同采收部位挥发油及醇提物成分的分析

【目的】确定五指毛桃不同采收部位的质量。【方法】应用气相色谱．质谱联用(GC-Ms)法分别对五指毛桃不同采收部位中挥发油的含量和成分以及醇提物的成分进行分析。【结果】五指毛桃根皮中挥发油的含量高于根木质部;五指毛桃根皮与根木质部所含的化学成分相似,挥发油成分以十六酸、油酸 亚油酸、亚油酸酰胺、软脂酸酰胺、硬脂酸酰胺、邻苯二甲酸二丁酯为主;其乙醇提取物中以补骨脂素、十六酸、十六酸乙酯、佛手内酯、油酸、亚油酸为主。根皮中补骨脂素的含量高于木质部。【结论】五指毛桃不同采收部位所含化学成分相似,其中根皮部的挥发油成分和补骨脂素含量均高于木质部。     

具有薄荷香味的相变微胶囊的制备与表征

利用界面聚合法,以异佛尔酮二异氰酸酯与己二胺为单体聚合形成的聚脲为外壳,以正十八烷、薄荷素油的混合物为芯材,制备了具有薄荷香味的相变微胶囊。利用光学显微镜、扫描电镜、红外光谱仪、差示扫描量热仪、热重分析仪等对微胶囊的形貌、化学结构和热性能进行了表征。结果表明：制备的微胶囊为球形,平均粒径约7.0 μm,有较高的储热能力和较好的热稳定性;芯材中添加8.3%的正十四醇或高熔点石蜡,可很好地抑制相变微胶囊的过冷现象。     

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…     

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.     

Development on Adjustable Calibration Marker for Shock Wave Focus

Shock wave lithotripsy （SWL） is a treatment of choice for upper urinary stones. However, this procedure is inappropriate for obese patients because the focus is often unable to reach the target owing to the limited focal distance in shock wave source. Although treating such patients in a blast path may increase the application length of shock wave source, it＇s difficult to find this path on the lithotripter monitor. For this reason, we invented an adjustable calibration marker in order to set an effective focus in the shock wave hath.     

Study on the TCM Pathogenesis of Angiopathic Complications of Type II Diabetes

Excess production of reactive oxygen species(ROS)of mitochondrion mediated by hyperglycemia is the common pathogenesis of angiopathic complications of diabetes.TCM holds that the damp from the dysfunction of spleen.kidney and liver is the causative factor of complications of diabetes.This is similar to the mechanism of Ros resulting in angiopathic complications of diabetes.When the angiopathic complications of type II diabetes mellitus(T2DM)are difierentiated as caused by turbid damp in TCM can be explained as ROS.Since the obstruction of pathogenic damp in channels and collaterals is said to be the main pathogenesis,the treating principle should be dissolving the damp to remove the obstruction.     

Leptin, Ghrelin and TNF-α before and after Hypo-caloric Traditional Chinese Diet and Auricular Acupuncture

INTRODUCTION Obesity is a complex emergent problem, which can be possibly solved not only by the diet but also by the life style and promotion of a constant physical exercise. 1, 2 No doubt careful attentions must be given to the nutritional condition of obese people, the dietary habits, the somatic build (i.e. distribution of fat mass) and the organic functions linked to formation of the fat mass. All the parameters should be constantly monitored before, during and after a diet treatment. 3, 4, 5     

Relationship between Dysglycemia and Carotid Atherosclerosis in Tibetan Population

People with dysglycemia are at high risk for atherosclerotic diseases. This study aims at investigating the atherosclerotic vascular damage in dysglycemia and its metabolic origin in Tibetan population.     

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.