Epoxyalkanoyls as novel ACE inhibitors

The epoxyalkanoyl derivatives were designed and synthesized as ACE inhibitors. Coupling of unsaturated carboxylic acids with amino acids and following epoxidation with dimethyldioxirane gave the epoxyalkanoyls with high yield. The inhibitory activity of synthesized compounds on angiotensin converting enzyme was IC₅₀ values of 0.06≈5.5 μM.     

传统腺样体切除术后腺样体残留情况调查

体统的腺样体手术为腺样体刮除术，为非直视下的手术，虽然多数患者手术后症状得得缓解，但临床上也常常看到手术后短时间内症状复发或者缓解不彻底的患儿，这类情况往往和腺样体手术切除不彻底有关。本院自2003年1月-2004年9月间对腺样体切除术后复发再次手术患者，以鼻内镜观察记录腺样体残留情况，对初次手术患者在进行传统腺样体刮除术并止血后，立即进行鼻内镜检查，了解腺样体残留情况并进行鼻内镜下处理，报告如下。     

ACTIVIT OF HUMAN PLACENTAL GAMMA GLOBULININ BLOCKING IMMUNE FUNCTIONS IN VITRO AND IN ABROGATING THE XENOGENEIC, LOCAL GRAFT-VERSUS-HOST-REEACTEON

In order to understand the mechanism of immunosuppression caused by infusion of placental gamma globulin (PGG) in patients with renal allografts, rheumatoid arthritis, and graft – versus –host disease (GCHD) following bone marrow transplantation (BMT) ,we have examined the effect of PGG in vitro and in a model of the xenogeneic , local graft –ver- sus – host reaction (LGVHR) .PGG inhibited lymphocyte proliferation in mixed lymphocyte cultures (MLC) (P<0.005) and depressed interleukin -2 (IL-2) levels in such cultures at 72 hours (P<0.01) . In contrast phytohemagglutinin (PHA) –and pokeweed mitogen (PWM) –induced T and B lymphocyte blastogenesis was not affected by such PGG treatment .PGG treatment .PGG neither decreased the [3H] TdR pulse incorporation in unstimulated lymphocytes nor affected cell viability .Cell cycle analysis by flow cytometry showed that PGG reduced the percentage of cells in S and G2, M phases during the MLC, but did not alter cell cycling during PWM-stimulated proliferation . An immunosuppressive effect of PGG on the LGCHR was tested in a model of intracutaneous transplantation of PGG –treat human lymphocytes into cyclophosphamide – immunosuppressed rats. Lymphoprep – separated human tonsillar lymphocytes were incubated with RPMI-1640 buffer containing：（1）PGG,4mg/ml,(2) human plasma albumin,4mg/ml,(3)mitomycin-C,25ug/ml, or (4) no additive. Cell of each preparation (3x107cells in 0.1ml) were injected intracutaneously into cyclophosphamide-treated male rats at separate abdominal locations. A fifth site received only the buffer solution. Five days after injection of cells ,each rat received [125 I]IUdR (10uCi) intraperitoneally and was killed after 5 hours. For each site of injection, the diameters of induration were measured and 125 I was counted . There was no difference between buffer – treated and a ibumin – treated groups either in the diameter of the area of induration (t=0.66;P>0.5)or in radioactive counts(t=0.22;P>0.05).In the PGG –treated group, the induration and radioactivity measurements were significantly less than in control groups (t=3.72 and P<0.1;t=2.62 and P<0.02,respectively ) Cytophilic antibodies in PGG were thought to inhibit an early phase of T cell activation, and not to be cytotoxicity .In the LGVHR, the immune response might be abrogated either by immuno- regulatory suppression of T cell function or by toxicity to the infused lymphoid cells. For some clinical purposes, immuno- modulating, human antibodies might be preferred to murine, monoclonal antibodies.     

再生丝素/NMMO·H2O溶液的流变性能

使用N-甲基吗啉-N-氧化物的水合物(NMMO·H2O)作为再生丝素的溶剂.可以得到w=0.10～0.25的再生丝素/NMMO·H2O溶液.研究了再生丝素/NMMO·H2O溶液流变性能,讨论了剪切速率、温度和溶液中的再生丝素的含量对再生丝素/NMMO·H2O溶液流变性能的影响.     

Ⅰ、Ⅲ型前胶原基因第2外显子核酶对靶RNA的体外切割活性的研究

目的 体外研究锤头型α1Ⅰ型及Ⅲ型前胶原基因第2外显子片段核酶对各自靶RNA分子的切割活性及反应条件。同时观察两反义核酶对瘢痕中成纤维细胞胶原合成的影响。方法 将含α1Ⅰ型及Ⅲ型前胶原基因第2外显子片段的重组质粒(pT-Ⅰ、pT-Ⅲ)，经体外^32P标记转录后形成产物靶RNA。同时将含特异性核酶基因的重组质粒(pT-gⅠ、pT-gⅢ)进行非标记的体外转录，产物(核酶)与各自的^32P-靶RNA按不同的条件混和反应，电泳后放射自显影观察结果。将构建好的核酶以脂质体包裹后导入培养的成纤维细胞内，采用图像分析法观察核酶对成纤维细胞Ⅰ型、Ⅲ型胶原蛋白mRNA合成的影响。结果 两种核酶在37℃、42℃均能有效切割各自的靶RNA，对Mg^2 浓度的要求范围较宽(10～20mmol／L)；反应温度从65℃逐渐降至并维持在37℃的条件下核酶切割活性显提高。Ⅰ、Ⅲ型胶原蛋白mRNA的表达明显降低，胶原蛋白生成降低，胶原生成明显受抑制。结论 针对α1Ⅰ型及Ⅲ型前胶原基因第2外显子片段的核酶能有效地在体外对靶RNA进行切割并能有效地抑制瘢痕中成纤维细胞胶原的合成。     

Stability of poly(D,L-lactide-co-glycolide) and leuprolide acetate in in-situ forming drug delivery systems.

In-situ forming drug delivery systems are prepared by dissolving a drug and a biodegradable polymer (poly(D,L-lactide-co-glycolide), PLGA) in a biocompatible organic solvent (In-situ implant, ISI) or further emulsified into an external phase (oil or aqueous solution), resulting in oil-in-oil or oil-in-water emulsions (In-situ forming microparticles, ISM). The chemical stability of PLGA and the drug is a major concern. In this study, the stability of PLGA and leuprolide acetate in the in-situ forming systems and lyophilized sponges was investigated. The degradation of PLGA increased with increasing storage temperature and water content in the biocompatible solvents. A faster degradation occurred in polar protic solvents (2-pyrrolidone, PEG 400, triethyl citrate) than in polar aprotic solvents (N-methyl-2-pyrrolidone, DMSO, triacetin, ethyl acetate). The presence of leuprolide acetate significantly accelerated PLGA degradation, especially in solution state. PLGA was stable in oily suspensions at 4 degrees C and degraded only slightly faster than solid powder at 25 degrees C. No interaction between the oils and the PLGA was observed as indicated by an unchanged T(g) of approx. 47 degrees C. PLGA underwent a slight degradation at 4 degrees C after 150 days in water and saturated sodium chloride solution. The degradation was slower in saturated sodium chloride solution than in water at 25 degrees C. Residual acetic acid in lyophilized sponges facilitated the PLGA degradation in contrast to dioxane. Leuprolide acetate did not affect the PLGA stability negatively. However, lidocaine significantly enhanced the polymer degradation in the sponges. Finally, leuprolide acetate was chemically stable in the sponges, the oils and the polymer solutions in suspension state, but unstable (aggregation) when dissolved in the polymer solutions and stored at 25 degrees C and 40 degrees C.     

Localization of ulnar neuropathy at the elbow using new stimulator for the inching test.

OBJECTIVE: To evaluate the usefulness of the TenElectrodes, a new stimulator for inching test, in the diagnosis and localization of ulnar neuropathy at the elbow (UNE). METHODS: Sixty-two ulnar nerves in 40 control subjects and 24 ulnar nerves in 23 patients with typical symptoms and signs of UNE were studied. The inching test of ulnar motor nerve using TenElectrodes was done along 8 cm across the elbow in the extended position. RESULTS: In the inching test of the control group, the mean segmental latency difference was 0.19+/-0.08 ms. Maximal latency difference over a 1 cm segment did not exceed 0.40 ms in any of the controls but exceeded 0.5 ms or more in all clinical UNE patients. In all UNE patients, the lesion sites were identified by the inching test using TenElectrodes: the retroepicondylar groove (54.2%), the humeroulnar arcade (29.2%), and dual compression (16.6%). CONCLUSIONS: TenElectrodes is a useful stimulator for the inching test in the diagnosis of UNE. The precise localization of compression was possible in all patients with UNE and the most common site was the retroepicondylar groove.     

端粒酶活性检测在乳腺癌诊断中的意义

[目的 ]探讨细针穿刺乳腺肿瘤组织的端粒酶活性检测在乳腺癌诊断中的意义 .[方法 ]用聚合酶链反应 酶联免疫吸附测定法检测 79例术前乳腺肿瘤细针穿刺活检标本和大体标本的端粒酶活性 ,并与病理诊断进行比较 .[结果 ]乳腺癌 6 5例中穿刺组织端粒酶呈阳性的为 5 7例 ,阳性率为 88% ;大体组织端粒酶呈阳性的为 5 4例 ,阳性率为 83% .淋巴结转移者端粒酶活性高于无淋巴结转移者 .乳腺良性疾病 14例中端粒酶呈阳性的为 2例 ,阳性率为 14 % .[结论 ]术前乳腺肿瘤穿刺组织的端粒酶活性检测有利于乳腺肿瘤的早期诊断及鉴别诊断 .