抗生育化合物7α-甲基炔诺酮及其肟的合成

7α-甲基炔诺酮(Ⅰ)的口服抗促性腺激素活性和抑制排卵活性均强于炔诺酮,对大鼠口服给药0.1mg/天,即产生显著的抑制排卵作用。炔诺酮肟具有抗孕激素活性和抗着床活性。为寻找新的抗孕激素类抗生育药物,我们设计合成了7α-甲基炔诺酮肟(Ⅱ)。合成路线如下:     

非甾体抗生育药物的研究 Ⅱ.对-羟基苯丙烯酸衍生物的合成及其抗生育活性

据报道,对-羟基本丙烯酸(Ⅰ)对小鼠有很好的抗生育作用。鉴于芳基取代的苯乙烯美化合物亦有不同程度的抗生育活性,我们在对-羟基苯丙烯酸的α位,用芳基取代,合成了24个衍生物。初步药理筛选结果表明,化合物Ⅱ_(1,3,7,23)对小鼠有抗早孕作用(P<0.05～0.001),其中以化合物Ⅱ_1为显著(P<0.001)。     

GnRH Ⅱ与GnRH Ⅰ对子宫内膜异位症患者间质细胞分泌VEGF作用的比较

目的:测定GnRH Ⅱ与GnRH Ⅰ对子宫内膜异位症(Ems)患者离体培养子宫内膜间质细胞分泌血管内皮生长因子(VEGF)的影响,探讨GnRH Ⅱ对Ems患者可能的作用.方法:给予原代培养的Ems患者在位及异位子宫内膜间质细胞不同浓度的GnRH Ⅱ,GnRH Ⅰ类似物(戈舍瑞林,goserelin)处理,同时设对照组(不加GnRH),采用酶联免疫吸附法(ELISA)测定培养液中VEGF浓度,并进行比较.结果:Ems患者离体培养的异位子宫内膜间质细胞经48 h培养,能分泌VEGF,分泌量与在位子宫内膜间质细胞的相近,两者比较差异无统计学意义(P＞0.05).不同浓度的GnRH Ⅱ对Ems患者离体培养的在位和异位子宫内膜间质细胞VEGF的分泌有明显的抑制作用,呈剂量依赖性(P＜0.05),且较GnRH Ⅰ类似物(戈舍瑞林)的作用更强(P＜0.05).不同浓度的GnRH Ⅱ对Ems患者离体培养的异位子宫内膜间质细胞VEGF分泌的抑制作用明显强于在位(P＜0.05).结论:Ems患者的异位子宫内膜间质细胞具有分泌VEGF的功能,分泌量与在位子宫内膜的相近,这对Ems的形成和发展可能起重要作用.GnRH Ⅱ呈剂量依赖性地抑制异位内膜间质细胞分泌VEGF,其抑制作用明显强于在位,且GnRH Ⅱ明显强于GnRH Ⅰ,为寻找Ems抗血管形成方面的新药治疗提供了新的依据.     

芳姜黄酮和姜烯衍生物的合成及抗生育活性初探

叙述了四个倍半萜类衍生物——芳姜黄酮(Ⅰ)、对甲氧基芳姜黄酮(Ⅱ)、(-)-异丙水芹烯(Ⅲ)、(-)-水芹烯羧酸乙酯(Ⅳ)的合成及结构确证。(Ⅱ～Ⅳ)未见文献报道。初步药理筛选结果表明:(Ⅰ)抗生育活性不理想;(Ⅲ)具有一定的抗生育活性。     

万古霉素骨蜡复合体体外释放研究

目的 探讨万古霉素骨蜡复合体体外释放特性.方法 将万古霉素与骨蜡按质量比1%(Ⅰ组)、2%(Ⅱ组)、3%(Ⅲ组)分别制成万古霉素骨蜡复合体后进行28 d洗提实验,每24 h测定万古霉素释放浓度.结果 在不同时间点上,各组间万古霉素释放浓度差异有统计学意义(P<0.05);进一步分析结果显示,除d1时间点外,其他时间点上Ⅲ组的释放浓度值最高,其次分别为Ⅱ组、Ⅰ组(P<0.05).结论 不同比例的万古霉素骨蜡复合体在体外均能持续释放万古霉素;载药量越高,28 d内释放浓度越大.     

异氟烷复合硬膜外麻醉对腹部手术病人应激性高血糖的调控作用

目的:研究腹腔手术病人围术期红细胞应激性高血糖的变化及不同麻醉方法对其影响。方法:40例ASAⅠ～Ⅱ级择期腹腔手术病人,按麻醉方式随机分成两组,每组20例。Ⅰ组采用异氟烷吸入为主的全身麻醉;Ⅱ组采用异氟烷吸入联合连续硬膜外阻滞。分别于麻醉前30min、手术90min、术后60min及术后第1、2天共5个时点测定血糖、红细胞醛糖还原酶(AR)活性及血浆谷胱甘肽(GSH)、丙二醛(MDA)、一氧化氮(NO)浓度。结果:与麻醉前值比较,两组病人血糖浓度自术中90min开始,至术后第1天升高显著(P<0.01),Ⅰ组病人术后第1天血糖浓度显著高于Ⅱ组(P<0.05);与麻醉前值比较,Ⅰ组术后第1天AR活性显著升高(P<0.01),而Ⅱ组各时点AR活性的变化趋势与I组相似,但与麻醉前比较均无统计学差异(P>0.05),其术后第1天的变化幅度低于Ⅰ组(P<0.05)。Ⅰ组病人术后第1天GSH、MDA浓度与麻醉前值比较有差异(P<0.05);与麻醉前值比较,两组病人血浆NO浓度均有所降低;Ⅰ组病人血浆NO浓度术后第1天显著下降(P<0.01),其中Ⅰ组病人术后第2天仍显著低于麻醉前值,Ⅱ组病人各时点NO浓度与麻醉前值相比,无显著性差异。结论:腹腔手术中、手术后存在明显的应激性高血糖反应;采用异氟烷复合硬膜外麻醉可在一定程度上减缓手术创伤对红细胞应激性高血糖的影响。     

用于唇部的结痂制剂

一种新制剂含有过氧化天然油(Ⅰ)和α-乙酰扁桃酸(madelic acidⅡ)。过氧化油最好选用甜杏仁油、玉米和芝麻油,制剂以含(Ⅰ)65％～99％,(Ⅱ)1％～35％为最宜。可制成乳剂、膏剂或凝胶或专作成唇膏。局部使用本制剂有结痂作用,在角质损     

非甾体抗生育药的研究 Ⅲ.马兜铃次酸开环衍生物的合成及其抗生育活性

自印度马兜铃(Aristolochia indica L.)中提得的马兜铃次酸(Aris-tolic acid)(Ⅰ)及其甲酯,经动物实验证明具有较好的抗着床和引产作用。为了寻找结构简化、活性更强的抗生育药,我们合成了马兜铃次酸开环衍生物(Ⅱ_(1-8))。鉴于对-羟基苯丙烯酸类化合物亦有抗生育作用,因此将五个苯丙烯酸型中间体作为Ⅲ_(1-5)化合物。初步药理试验表明:Ⅱ类化合物无抗着床和抗旱孕作用。化合物Ⅲ_1和Ⅲ_2分别具有显著的抗早孕和抗着床作用(P<0.01,P<0.05),Ⅲ_4兼有上述二种作用(P<0.01)。这说明菲环破裂后,抗生育活性消失,而具有苯丙烯酸型结构的中间体仍能保持抗生育作用。     

PDGF-BB和bFGF对牙周膜细胞增殖的影响

目的:探讨血小板衍生生长因子-BB(PDGF-BB)和碱性成纤维细胞生长因子(bFGF)对人牙周膜(PDL)细胞增殖的影响。方法:体外培养人PDL细胞与不同浓度的PDGF-BB,bFGF或PDGF-BB+bFGF作用。用四唑盐(MTT)法观察PDL细胞增殖的情况。结果:PDGF-BB明显促进PDL细胞增殖,第3天最大显效浓度为10 ng/ ml,比对照组增加34%(P<0.001),最小显效浓度为1 ng/ml,比对照组增加25%(P<0.001)。PDGF-BB在1 d～9 d,0.1 ng/ml～10 ng/ml范围内呈浓度时间依赖关系,峰值位于第9天,10 ng/ml处,比对照组增加20%(P<0.001)。bFGF也能明显促进PDL细胞增殖,第3天最大显效浓度为50 ng/ml,比对照组增加71%(P<0.001),最小显效浓度为1 ng/ml,比对照组增加23%(P<0.001)。bFGF在1d～6 d,1 ng/ml～50 ng/ml范围内呈浓度时间依赖关系,峰值位于第6天,50 ng/ml处,比对照组增加79%(P<0.001)。PDGF-BB与bFGF最大与最小显效浓度联合作用均在1 d～9 d内呈浓度时间依赖关系,峰值位于第9天,最大显效浓度联合作用比对照组增加46%(P<0.001),最小显效浓度联合作用比对照组增加17%(P<0.001)。结论:PDGF-BB和bFGF均可促进人PDL细胞增殖,在一定范围内呈浓度时间依赖关系,二者联合对PDL细胞增殖具有协同效应。     

实验性氯菧酚胺的抗生育作用

为寻找一种抗雌索性质的抗生育药物,本文每日用200μg、400μg及2000μg不同剂量的氯蔗酚胺,分别给交配后第1,第3及第6天的大鼠服用,连续5d。发现交配后第1及第3天服各种剂量药物的雌鼠均未妊娠,而于交配后第6天服药的各组大鼠与对照组一样均有妊娠。提示氯蔗酚胺对在输卵管阶段的大鼠配子有杀灭作用,而对种植后的胚泡则无抗生育作用。     

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.     

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.     

Electro-Acupuncture Combined with the Trigger Point Needle-Embedding for Treatment of Primary Trigeminal Neuralgia in 31 Cases

In recent years, the author of this essay has applied electro-acupuncture combined with the trigger point needle-embedding for treatment of primary trigeminal neuralgia in 31 cases, yielding satis- factory results as reported in the following.     

Investigation of Matrix Metalloproteinase -1, 2 and tissue inhibitor of matrix metalloproteinases-1 in Endometriosis

Objective： To explore the role of matrix metalloproteinase-1,2 （MMP-1, MMP-2） and tissue inhibitor of matrix metalloproteinases-1 （TIMP-1） in endometriosis. Methods： The eutopic and ectopic endometria from 40 subjects suffering from endometriosis and regular.endometria from 40 subjects （excluding endometriosis） were collected and examined by in situ hybridization technology and western blot assay. Results： Both expressions of MMP-1 and -2 were stronger in ectopic endometrium and eutopic endometrium than in normal endometrium. On the contrary, the expression of TIMP-1 in ectopic endometrium and eutopic endometrium was lower. The differences were significant （P 〈 0.01 ）. Moreover, there was no relationship among the expressions of MMP-1, 2 and TIMP-1 in ectopic endometrium. Conclusion： The expressions of MMP-1, 2 and TIMP-1 lose balance and lack of periodic changes in ectopic endometrium , which explains the biological invasive behavior of endometriosis. It was suggested-that regulating the balance between the MMPs and TIMP-1 should be an ideal therapeutic target to endometriosis.     

Shi Da-zhuo (史大卓) —An outstanding cardiologist of integrative medicine

Prof. SHI Da-zhuo, Ph.D., male, was born on March 20, 1960. Prof. SHI entered the Ph.D. program in 1990 at the China Academy of Chinese Medical Sciences under the supervision of Prof. CHEN Ke-ji, majoring in the treatment of cardiovascular diseases. After receiving his Ph.D. degree in 1993, Prof. SHI started working at the Cardiovascular Center in Xiyuan Hospital affiliated to China Academy of Chinese Medical sciences.     

Persist in and Carry Forward the Integrative Medical Research——Speech at the 6th National General Congress of Chinese Association of Integrative Medicine by Academician CHEN Zhu,Minister of Ministry of Health

The 6th National General Congress of Chinese Association of Integrative Medicine （CALM） was convened at 19-20, April 2008 in Beijing. Academician CHEN Zhu, the minister of Ministry of Health indicated at the congress that the integration of Chinese and Western medicine is very well in keeping with the situation of our country and the general rule of development in medical science; and as a good integration of Chinese medicine and Western medicine, it is mutually beneficial and advantageous to both of them. Seeing the creativity shown in integrative medical investigation in theoretic and methodological sides, we should and must persist in and develop it.