《本草图经》兴化军防己的本草考证

对《本草图经》中兴化军防己的附图及文字记载进行本草考证,探究其原植物品种。通过古今文献考证和植物学比较研究,从植物形态、药材性状、产地分布及性味功用等方面进行分析,认为《本草图经》中的兴化军防己应为今之防己科植物木防己[Cocculus orbiculatus (L.) DC.],为防己类中药的古今品种沿革及基原考证提供参考。     

药用植物浸提液抑制蛋白核小球藻生长的化感效应

研究了11种药用植物浸提液对水华藻种蛋白核小球藻的影响,结果显示:黄连、重楼、贯众、防己4种药用植物的浸提液均有抑藻效应。当药用植物浸提液的相对浓度为1g/L处理时,其半抑制效应时间LT50的排序为:防己重楼黄连贯众。进一步研究防己的相对浓度梯度抑藻效应,结果表明:在相对浓度为2g/L时,实验3d后的藻细胞几乎全部死亡;防己的抑藻效应受贮藏时间和贮藏温度的影响不显著。在所研究的药用植物中,防己的抑藻效果最好,在抑藻方面有较大应用前景,其它3种药用植物对轻度藻类爆发的控制也有潜在应用价值。     

防己抑藻效应及其化感物质的HPLC分析

通过常温水浸提方法获得12种药用植物浸提液,并分别研究其抑藻效应。结果显示：防己水浸提物(相对浓度1 g·L^-1)抑制蛋白核小球藻的效应最强,最大比生长率为-0.28 d^-1。防己甲醇浸提物对蛋白核小球藻的抑藻效应显著,且持续时间长,最低有效抑藻浓度为30 mg·L^-1。HPLC鉴定结果显示：防己水浸提液和甲醇浸提液中主要含有防己诺林碱、粉防己碱等生物碱类化学成分,防己对治理水华发生有较大的应用前景。     

防己水煮液逆转MCF-7/ADM多药耐药细胞的初步研究

目的：观察中药防己水煮液对MCF-7／ADM多药耐药细胞的逆转作用,并对防己水煮液的逆转MCF-7多药耐药细胞株的有效组分作初步追踪。方法：用SRB显色法观察防己水煮液对MCF-7野生型细胞的毒性作用及对MCF-7／ADM多药耐药细胞的逆转作用,并用相同方法跟踪防己水煮液不同分离组分逆转MCF-7多药耐药细胞株的作用,确定有效组分。结果：对耐2．0μg／mLADM的MCF-7／ADM多药耐药细胞,当阿霉素浓度降到0．25μg／mL时,防己水煮液对MCF-7／ADM多药耐药细胞的逆转效果比较明显,即0．25μg／mL阿霉素为防己水煮液逆转MCF-7／ADM多药耐药细胞的敏感浓度点;对MCF-7／ADM多药耐药细胞起逆转作用的有效成分大部分集中在经正丁醇萃取所得相和水相中,而极性低的有机溶剂相中基本不合可以逆转MCF-7／ADM多药耐药细胞的有效组分。     

汉防己甲素联合顺铂对乳腺癌细胞的作用

目的:汉防己甲素和顺铂联合作用乳腺癌细胞,来提高癌细胞对顺铂的敏感性.方法:运用原子力显微镜对乳腺癌细胞表面的超微结构进行表征;MTr法和流式细胞术检测细胞的生长抑制率和细胞周期变化.结果:顺铂和汉防己甲素分别作用乳腺癌细胞48h IC50值为26.33μmoL/l和5.6μmok/l;联合用药组的IC50值为汉防己甲素2.5μmol/L和顺铂13.32μmol/l,在低浓度的联合用药作用乳腺癌细胞24h细胞膜表面结构被破坏,产生孔洞,作用48h被严重破坏使细胞周期在S比例增加为51.7%±0.30%.结论:提高了癌细胞对抗癌药物的敏感性,联合用药通过改变了细胞膜的结构对癌细胞进行有效杀伤,抑制肿瘤细胞生长.     

苯海拉明对汉防己及其他一些镇痛药的加强作用

汉防己(Stephania tetrandra S.Moore)含有汉防己甲素(tetrandrine),乙素(deme-thyl tetrandrine)及丙素等生物碱。久保田及陈氏等曾证明:汉防己甲素有解热作用,对平滑肌及心脏均具抑制作用。最近赵氏采用改良 Woolfe,Macdonald 氏小白鼠热板法,证明二者均能提高小白鼠之痛阈;但据同氏报告,临床土未能看到明显的镇痛效果。因此我们乃改用电刺激小白鼠尾巴法,以测定汉防己甲素、乙素及汉防己流浸膏等之镇痛作用。结果发现三者均具有一定镇痛作用;同时发现三者在一定剂量范围内,剂量增加,镇痛作用反减弱;且发现较大剂量之汉防己甲素,能增强士的宁的毒性,并能对抗戊巴比妥钠之作用。鉴于汉防己甲素及乙素之镇痛作用不甚强大,乃试行合并用药,以期提高其镇痛作用,先试抗组织胺药——苯海拉明。结果发现:苯海拉明可以明显地加强汉防己甲素及乙素之镇痛作用,并能延长其作用时间;而对它们的毒性无明显影响。苯海拉明同时可显著地加强并延长吗啡,地美露及安替匹林等镇痛药的镇痛作用。     

汉防己甲素及其联合氟康唑对白念珠菌细胞周期影响的初步研究

目的 探讨汉防己甲素联合氟康唑对白念珠菌细胞周期的影响.方法 将白念珠菌CA-1菌悬液与汉防己甲素和（或）氟康唑共培养12h,应用流式细胞仪测定空白对照组、汉防己甲素组、氟康唑组及汉防己甲素联合氟康唑组DNA含量.比较细胞周期各期DNA含量变化并计算增殖抑制率PI％,分析汉防己甲素及其联合氟康唑对白念珠菌细胞周期的影响.结果 汉防己甲素、氟康唑组与对照组S期DNA含量相比,分别能增加17.25％ （P =0.018）与6.54％ （P ＞0.05）,其联合运用效果更明显,S期DNA含量可增加31.52％ （P =0.002）.这说明汉防己甲素能将白念珠菌细胞阻滞在S期.结论 汉防己甲素能抑制白念珠菌细胞DNA合成,阻断白念珠菌细胞周期进程,抑制细胞分裂,其与氟康唑联用时阻滞作用更显著.     

中国产3种防己科植物细胞学研究

报道了3种国产防己科植物的染色体数目。金线吊乌龟Stephania cepharantha Hayata为二倍体2n=22,部分居群的一些个体存在B染色体;轮环藤Cyclea racemosa Oliv．为二倍体2n=24;木防己CDcculus orbiculatus(L)DC为四倍体2n=4x=52.3个种的染色体基数分别为x=11,12,13。观察了木防己的小孢子母细胞减数分裂过程,其减数分裂过程正常,且花粉粒具较高活性。     

汉防己甲素滴眼液对高眼压模型大鼠的降眼压作用

目的比较观察汉防己甲素滴眼液与0.5%噻吗心安滴眼液对高眼压模型大鼠及正常大鼠降眼压的作用。方法正常SD大鼠共分4组：不同浓度的汉防己甲素滴眼液组（0.1%、0.2%、0.3%）及阳性对照组0.5%噻吗心安,药物滴右眼各一滴,阴性对照组生理盐水滴左眼、测量滴药前24h和滴药后1、3、6、24、48、72h的眼压。应用倍频532激光对SD大鼠右眼上巩膜静脉以及小梁网所在区域实施光凝术建立高眼压大鼠模型。高眼压模型鼠共分5组：不同浓度的汉防己甲素滴眼液0.05%、0.1%、0.2%、0.3%及阳性对照组0.5%噻吗心安,右眼即模型眼滴用药物,左眼作为空白对照。测量术前后的眼压。结果汉防己甲素滴眼液对大鼠正常眼压无降压作用（P〉0.05）。对高眼压大鼠用药后24h、72h、1周后,0.3%汉防己甲素滴眼液组降低眼压的幅度与0.5%噻吗心安滴眼液降低眼压的幅度相似（P〉0.05）;0.05%、0.1%、0.2%汉防己甲素滴眼液组也有明显的降压作用,但与0.5%噻吗心安滴眼液相比,降压幅度低于后者（P〈0.05）。结论0.05%、0.1%、0.2%、0.3%汉防己甲素滴眼液均有降低大鼠高眼压的作用,其中0.3%浓度的汉防己甲素滴眼液降眼压效果与0.5%的噻吗心安类似。汉防已甲素滴眼液作为一种治疗青光眼的药物有着良好应用前景。     

吸果夜蛾优势种群的发生与防治

在湖北,鸟咀壶夜蛾与咀壶夜蛾是吸果夜蛾的优势种群。鸟咀壶夜蛾一年出现4次为害高峰;咀壶夜蛾一年出现4次为害期,但仅第4次形成为害高峰期。两者的幼虫均以木防己为食,木防己的分布及密度直接与两种夜蛾的发生及虫口密度相关。根除果园周围吸果夜蛾幼虫的寄主植物--木防己是防治吸果夜蛾的有效措施。用除草剂涂茎防除木防己是一种简便易行、一次防除、长期受益的好方法。     

乳杆菌制剂和(或)达克宁治疗外阴阴道假丝酵母菌病的疗效比较

目的探讨乳杆菌制剂治疗外阴阴道假丝酵母菌病(VVC)的疗效。方法将2006年5月至7月在温州医学院附属二院确诊为VVC的患者分为3组,单纯使用达克宁栓者(A组)40例,联合使用达克宁栓及定君生阴道栓者(B组)40例,单纯使用定君生者40例(C组),进行对照。对3组的临床症状及真菌学检查结果进行分析讨论。结果停药3~5 d时,A、B组患者的疗效差异无显著性(P>0.05),C组患者的疗效明显低于A、B两组(P<0.05);停药30~37 d时,A、C组患者的疗效差异无显著性(P>0.05),B组患者的疗效明显高于A、C两组(P<0.05)。结论在应用阴道用乳杆菌治疗VVC时,应首先应用抗真菌药物,当真菌感染得以控制之后再使用乳杆菌,帮助恢复阴道内菌群环境。     

辽宁某高校医学生抗菌药物认知水平调查

目的了解医学生对抗菌药物的认知水平及自主应用抗菌药物状况。方法采用分层整群抽样方法抽取调查对象,进行抗菌药物认知和使用的问卷调查。结果医学生抗菌药物认知较以前有提高,但仍存在误区。结论对抗菌药物应用认知水平的缺乏和不适当应用抗菌药物的现象在低年级医学生中依然存在,加强对抗菌药物应用知识的普及和宣传教育仍是当前之必需。     

Aspirin and bleeding peptic ulcers in the elderly.

A case-control study was performed to determine whether aspirin confers a similar risk of bleeding from gastric or duodenal ulcers in the elderly as non-aspirin, non-steroidal anti-inflammatory drugs. The intake of analgesics in 230 patients with bleeding ulcers aged 60 and over and in hospital and community controls matched for age and sex was examined. Those who had taken aspirin were between two and three times more likely to be admitted to hospital with bleeding ulcers. This increased risk was not accounted for by aspirin taken for indigestion or by concurrent use of non-aspirin, non-steroidal anti-inflammatory drugs. A similar effect was not seen for paracetamol. When aspirin and other non-steroidal anti-inflammatory drugs were considered together the overall risk attributed to the drugs suggested that these drugs may be responsible for over a third of admissions for bleeding peptic ulcers in the elderly.     

Downregulation of JNK/SAPK activity is associated with the cross-resistance to P-glycoprotein-unrelated drugs in multidrug-resistant FM3A/M cells overexpressing P-glycoprotein

In the present study, cross-drug resistance in multidrug-resistant (MDR) cells, which overexpress P-glycoprotein (Pgp), a mdr1 gene product, against Pgp-unrelated drugs, and its relevance to c-Jun N-terminal kinase (JNK)/stress-activated protein kinase (SAPK) activity were examined. The multidrug-resistant FM3A/M cells overexpressing Pgp were resistant to apoptotic cell death induced either by Pgp-related drugs including vincristine and vinblastine, which are pumped out by Pgp, or by the Pgp-unrelated drugs including 5'-fluorouracil (5-FU) and bleomycin, which are not targets for Pgp, compared with the parental FM3A cells. Verapamil reversed the resistance of FM3A/M cells to apoptosis induced by the Pgp-related drugs but not that induced by the Pgp-unrelated drugs. Interestingly, FM3A/M cells have shown significantly lower basal and drug-stimulated JNK/SAPK activities than FM3A cells. After transfection with pEBG-SEK or pEBG-SAPK constructs, FM3A/M cells recovered the basal and Pgp-unrelated drug-stimulated activities of JNK/SAPK and the susceptibility to Pgp-unrelated drug-induced apoptotic cell death comparable to those of FM3A cells. Furthermore, FM3A cells became resistant to apoptotic cell death induced by vincristine and 5-FU after transfection with pEBG-SEK(K --> R), a dominant negative inhibitory mutant of SEK. These results suggest that downregulation of JNK/SAPK activity appears to confer on Pgp-associated FM3A/M cells a cross-resistance to Pgp-unrelated drugs.     

The anti-inflammatory activity of Enicostemma littorale and Mollugo cerviana

The anti-inflammatory activity of E. littorale and M. cerviana was assessed by carrageenan-induced inflammation and cotton pellet granuloma method in rats. E. littorale and M. cerviana exerted 54 and 26% anti-inflammatory activity for a dose of 100 mg/100 g body wt, respectively, in carrageenan-induced acute inflammation. In chronic inflammation of cotton pellet granuloma, E. littorale and M. cerviana exerted 30 and 46% anti-inflammatory activity at the above dosage, respectively. The optimal dose for these drugs was determined in carrageenan inflammation. The effect of the alcoholic extract of these drugs on human erythrocyte membrane stabilization and inhibition of cobra venom phospholipase A2 was studied in vitro and the drugs were found to be effective. Further, these drugs were found to inhibit the levels of lipid peroxides, acid phosphatase, and gamma-glutamyl transpeptidase activity in the exudate of cotton pellet granuloma. The effects were compared with those of standard anti-inflammatory drug, hydrocortisone. A possible mode of action of these drugs is suggested.     

Generalization of a prototype intelligent hybrid system for hard gelatin capsule formulation development

The aim of this project was to expand a previously developed prototype expert network for use in the analysis of multiple biopharmaceutics classification system (BCS) class II drugs. The model drugs used were carbamazepine, chlorpropamide, diazepam, ibuprofen, ketoprofen, naproxen, and piroxicam. Recommended formulations were manufactured and tested for dissolution performance. A comprehensive training data set for the model drugs was developed and used to retrain the artificial neural network. The training and the system were validated based on the comparison of predicted and observed performance of the recommended formulations. The initial test of the system resulted in high error values, indicating poor prediction capabilities for drugs other than piroxicam. A new data set, containing 182 batches, was used for retraining. The percent of the test batches were used for cross-validation, resulting in models with R²≥70%. The comparison of observed performance to the predicted performance found that the system predicted succcessfully. The hybrid network was generally able to predict the amount of drug dissolved within 5% for the model drugs. Through validation, the system was proven to be capable of designing formulations that met specific drug performance criteria. By including parameters to address wettability and the intrinsic dissolution characteristics of the drugs, the hybrid system was shown to be suitable for analysis of multiple BCS class II drugs. Published: October 22, 2005     

ICU患者呼吸道感染病原菌的分布及耐药性监测

目的了解华中科技大学同济医学院附属同济医院ICU患者呼吸道感染病原菌的分布及细菌耐药性特征,指导临床合理、科学地使用抗菌药物,为有效控制危重患者肺部感染提供依据。方法回顾分析该院2004年1月至2008年12月ICU患者呼吸道感染的病原菌分布情况,并分析其耐药性变化。结果该院ICU患者呼吸道感染病原菌主要为鲍曼不动杆菌(aba)、铜绿假单胞菌(pae)和金葡菌(sau),其中泛耐药菌株有增多趋势。耐苯唑西林金葡菌(MRSA)的检出率在77.5%~100%。药敏数据显示,pae对常用抗菌药物耐药率均较高,在25.5%~95.3%;aba仅对头孢哌酮/舒巴坦耐药率低,为12.2%,但中敏率较高,为41.7%,对其他常用抗菌药物耐药率均较高。MRSA对所有的β-内酰胺类抗菌药物均耐药,苯唑西林敏感的金葡菌(MSSA)对青霉素和红霉素耐药率较高,分别为97.1%和47.2%,对其他常用抗菌药物较敏感。结论该院ICU患者呼吸道感染以aba、pae和sau为主,且耐药现象严重,对临床常用抗菌药物有多重耐药现象,临床医生应根据药敏结果合理使用抗菌药物。     

Effects of cimetidine-like drugs on recombinant GABAA receptors

Even though conventional systemic doses of cimetidine and other histamine H(2) antagonists display minimal brain penetration, central nervous system (CNS) effects (including seizures and analgesia) have been reported after administration of these drugs in animals and man. To test the hypothesis that cimetidine-like drugs produce these CNS effects via inhibition of GABA(A) receptors, the actions of these drugs were studied on seven different, precisely-defined rat recombinant GABA(A) receptors using whole-cell patch clamp recordings. The H(2) antagonists famotidine and tiotidine produced competitive and reversible inhibition of GABA-evoked currents in HEK293 cells transfected with various GABA(A) receptor subunits (IC(50) values were between 10-50 microM). In contrast, the H(2) antagonist ranitidine and the cimetidine congener improgan had very weak (if any) effects (IC(50) > 50 microM). Since the concentrations of cimetidine-like drugs required to inhibit GABA(A) receptors in vitro (greater than 50 microM) are considerably higher than those found during analgesia and/or seizures (1-2 microM), the present results suggest that cimetidine-like drugs do not appear to produce seizures or analgesia by directly inhibiting GABA(A) receptors.