抗真菌剂三氮唑含硫化合物的合成

合成了１３个三氮唑含硫化合物，均为未见文献报道的新化合物，对所合成的化合物，选择三种常见真菌进行体外最低抑菌浓度（ＭＩＣ）的测定，结果表明它们均有较好的抗真菌活性，有些化合物抑菌活性极高，有进一步研究和开发前景。     

Topographical analysis of the EEG effects of a subconvulsive dose of lidocaine in healthy volunteers

Background: The purpose of the present study was to assess the effects of intravenous lidocaine on spatial changes of electroen-cephalographic power and on psychomotoric status in conscious volunteers.
Methods: In 11 healthy volunteers lidocaine (2-min bolus, 100 mg; 15-min infusion, 40 μg kg^-1 min^-1) or placebo were given intravenously in a randomized, single-blinded, two-way crossover study. Haemodynamics and lidocaine plasma concentrations were measured at baseline and within a period of 30 min following bolus injection. Vigilance and emotional status were tested using visual analogue scales (VAS). Toxic CNS effects were evaluated by a questionnaire. The raw EEG (17 leads, reference C_z) and computed power spectra were continuously recorded.
Results: The chosen lidocaine dosage led to nearly constant plasma concentrations (unbound lidocaine 2.5 min and 15 min after bolus 0.36±0.14 μg/ml and 0.30±0.06 μg/ml, respectively [mean±SD]). The placebo caused no symptoms, changes in VAS-scores or EEG-parameters. Lidocaine induced pronounced subjective symptoms and significant increases in delta activity for 15 min, most dominant at the frontotemporal and occipital leads (max. +219% O₁). Frontal and occipital beta1 and beta2 power (max. +131% and +124% at O₁, respectively) was immediately increased after the bolus injection. No EEG changes occurred at central region C_z, and no interhemispheric EEG differences were noted. Theta, alphal, and alpha2 power remained unchanged.
Conclusion: The current data demonstrate simultaneous changes in psychomotoric status as well as delta and beta spectral power during lidocaine infusion. These data could be an indication that the pronounced frontotemporal and occipital EEG changes are the electroencephalographic expression of subjective sensations.     

The use of the rat facial nerve model to assess the effect of differing nerve anastomotic agents on the facial nerve

There are relatively few papers which prove that one nerve anastomotic agent for the facial nerve is superior to any other. Previous experiments on the division and anastomosis of the facial nerve have failed to consider the indeterminate variables involved, i.e. operator variability, controls and the reaction of the materials on normal nerve tissue. In this experiment, a variety of anastomotic agents were tested to see if the anastomotic agents themselves affected the extra-temporal facial nerve function. The absorbable suture, non-absorbable suture, glue and tube wrap used had no effect on normal nerve tissue or on the anastomosis of the sectioned facial nerve of the rat compared with simple laying together of the divided ends of the divided nerve.     

芪月降脂片中黄芪甲苷的含量测定

[目的 ]研究芪月降脂片中黄芪甲苷的含量测定方法 .[方法 ]用甲醇提取、水饱和正丁醇萃取、大孔吸附树脂处理供试品后 ,以双波长薄层扫描法测定黄芪甲苷的含量 .[结果 ]黄芪甲苷的平均回收率为 10 4 18% ,RSD为 3 2 5% .[结论 ]双波长薄层扫描法较为简便、经济且重现性较好 ,可用于制剂中黄芪甲苷的质量控制     

新型络合剂对肾镉促排作用及对微量元素影响的观察

为观察新型络合剂Ｇ－Ｃｙｓ－ＤＴＣ、Ｇ－Ｔｈｒ－ＤＴＣ对染毒大鼠肾内蓄积镉的络合促排作用及对肾皮质元素分布的影响，比较促排治疗对肾皮质铁、铜、锌等含量的影响，利用北京正负电子对撞机提供的硬Ｘ射线对肾皮质冰冻切片扫描及原子吸收分光光度法、Ｘ射线荧光测定染毒鼠肾皮质镉及其他元素含量。结果，新型络合剂Ｇ－Ｃｙｓ－ＤＴＣ、Ｇ－Ｔｈｒ－ＤＴＣ能大幅度降低肾内镉负荷。染毒肾皮质中Ｃｄ与Ｓｅ密切相关，而Ｚｎ和Ｓｅ的相关性下降。提示新型络合剂对肾内蓄积镉有较好驱排效果；硒和锌在镉中毒作用机制中可能起一定的保护作用。     

咪唑立宾在肾移植术后的应用

目的 探讨咪唑立宾（MZR）在肾移植术后的临床应用效果。方法 选取2003年8月至2004年4月间肾移植术后采用环孢素A（CsA）或他克莫司（FK506）＋MZR＋激素三联免疫抑制方案的患者112例，定期检查患者用药后的血常规、肝肾功能、尿酸、血糖、血脂等生化指标；对乙型肝炎病毒、丙型肝炎病毒、艾滋病病毒、巨细胞病毒、EB病毒、腺病毒及带状疱疹病毒进行抗原学或者抗体监测；疑有排斥反应时，行移植肾穿刺病理检查。统计病毒感染发生情况，评价该治疗方案的安全性。结果 肾移植术后随访12～20个月，患者的人／肾存活率均为96％；急性排斥发生率为11．6％，经冲击治疗后全部逆转；患者主要不良反应是高尿酸血症，但可以控制而不需要停药；巨细胞病毒感染率为11．6％，未发生巨细胞病毒病；有1例感染腺病毒。结论 MZR是一种安全有效的免疫抑制剂，病毒感染的发生率相对较低。由于肾移植术后应用MZR患者主要不良反应是高尿酸血症，因此要注意对患者的尿酸进行控制。     

Investigation of the anti-complement agents, FUT-175 and K76COOH, in discordant xenotransplantation

Abstract: We examined whether hyperacute rejection (HAR) of a discordant xenograft in a nonhuman primate model could be inhibited by the anticomplement agents, FUT-175 (FUT) and K76COOH (K76). The inhibitory effect of FUT and K76 on baboon sera was studied in vitro by i) complement-mediated hemolysis of sheep erythrocytes (by measuring serum CH50) and ii) cytotoxicity to cultured pig kidney (PK15) cells. The in vivo administration of FUT (at 0.2–25 mg/kg/h i.v. continuously) and K76 (50 mg/kg i.v. bolus) allowed evaluation of the serum levels of these drugs. Both FUT and K76 inhibited serum CH50 in a concentration-dependent manner. An enhanced effect was obtained by combining K76 with FUT therapy. High concentrations of FUT (>10^-4 M) and K76 (>10³ μxg/ml) were necessary to suppress serum CH50 to <5% of the normal level. However, PK15 cytotoxicity remained at >50% in the presence of i) 10^-4 M of FUT, ii) 10³ μg/ml of K76, and iii) 10^-6 M of FUT + 10³ μg/ml of K76. Pig heart transplantation (HTX) was performed in two baboons receiving FUT (1 mg/kg/h i.v. continuously) and K76 (at 200 mg/kg ×1 or 400 mg/kg + 200 mg/kg × 2 i.v, respectively). Cytotoxicity of the serum to PK15 cells at the time of HTX showed 39% and 1% cell death, respectively, in these two baboons, and the CH50 level was 1% (of control level) and 0%, respectively. Graft survival was 4.5 hours and 10 hours (with death of the baboon), respectively (compared with a mean of 29 minutes in control experiments). Both excised grafts showed typical features of hyperacute rejection. Immunopathological studies revealed deposition of C1q, C3d, C6, properdin, and Factor B, demonstrating that complement activation was not fully inhibited by FUT and K76. We conclude that i) FUT and K76 are indeed potent complement inhibitors, ii) the dosages of FUT and K76 necessary to suppress complement-mediated injury cannot be extrapolated from previously reported data obtained from serum CH50 levels, and iii) higher (possibly toxic) dosages will be required to inhibit complement activation completely. It seems unlikely that HAR will be prevented by these drugs alone, although they may be beneficial when combined with other forms of therapy.     

服用抗精神病药物的老年人与成年人心电图比较

目的：观察老年与成年精神病人服用抗精神病药物后的心电图（ＥＣＧ）改变。方法：８４例老年精神病病人（男性３５，女性４９例，年龄６３±ｓ３ａ）与１００例成年精神病病人（男性５０例，女性５０例，年龄４０±１０ａ），服用抗精神病药物前及服２ｍｏ以上的首次ＥＣＧ资料进行比较。抗精神病药包括吩噻嗪类、丁酰苯类及三环类抗抑郁剂和抗躁狂药等。结果：８４例老年病人中ＥＣＧ异常６３例（７５％），１００例成年人中ＥＣＧ异常４６例（４６％）（Ｐ＜０．０５）。结论：由于老年人服抗精神病药后易发生ＥＣＧ异常，因此开始剂量宜低，增量要小，严密监测心脏功能。     

Structure-activity relationship of macrocyclic and linear gadolinium chelates: Investigation of transmetallation effect on the zinc-dependent metallopeptidase angiotensin-converting enzyme

Transmetallation between commercially available solutions of gadolinium (Gd) chelates and the zinc (Zn)-dependent angiotensin-converting enzyme (ACE) was investigated. In vitro, the strongest inhibitions were observed for the linear Gd complexes, Gd diethylene-triamine pentaacetic acid (DTPA) bis-methylamide (BMA) (IC₅₀ = .016 ± .006 mmol/1) and Gd-DTPA (IC₅₀ = .350 ± .034 mmol/1). The two macrocycles Gd tetraazacyclododecane tetraacetic acid (DOTA) and Gd-HP-DO3A were similar and 400 times less active than Gd-DTPA-BMA. These effects were mainly due to the presence of free ligand for DTPA and calcium (Ca) chelate in the case of DTPA-BMA because the addition of Zn²⁺ in the same quantities suppresses their inhibitory effects. In vivo, these two solutions of linear Gd chelates significantly inhibited ACE activity (Gd-DTPA: 67 ± 9% versus baseline; and Gd-DTPA-BMA: 73 ± 2% versus baseline at the clinical dose of .1 mmol/kg), whereas no significant effect was observed for the two macrocyclic chelates Gd-DOTA and Gd-HP-DO3A. Formulating the Gd chelate solution with either an excess of free ligand or Ca chelate (to decrease Gd³⁺ release) in the case of linear Gd chelate may have deleterious biologic consequences.