手性还原剂用于苯乙酮的不对称还原研究

（１Ｓ，２Ｒ）－１－二丁氨基－１，２－二氢－２－茚醇（ＲＯＨ）与氢化铝锂形成的手性试剂首次用于苯乙酮的不对称还原研究．根据手性试剂制备后的使用方法（方法Ａ∶立即使用；方法Ｂ∶回流１０ ｍ ｉｎ 后使用），苯乙酮还原后可分别给出对映体过量值达６０％ ～７６％ 的不同主产物Ｒ－（＋ ）－１－苯基乙醇和Ｓ－（－）－１－苯基乙醇．研究了反应物物质的量之比（ＬｉＡｌＨ４ ｖＲＯＨｖＰｈＣＯＭｅ）对立体选择性的影响，当反应物物质的量之比为１．０ｖ１．５０ｖ１．５０时有较高的对映体过量值和转化率．这种手性还原剂为不对称合成光学活性醇提供了一种选择．     

1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二甲酸甲异丁酯的合成

1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二甲酸甲异丁酯为一抗高血压新药,作者报道了其三步法的合成方法,并对Hanstzch合成法中制备邻硝基苯亚甲基乙酰乙酸异丁酯的方法进行了改进,反应时间缩短,得率提高至58%.对产物分子结构采用元素分析、红外光谱(IR)、核磁共振氢谱(1H-NMR)及碳谱(13C-NMR)进行了鉴定.     

四-(4-三甲铵苯基)卟啉测定食品中的超痕量锌

以水溶性α,β,γ,δ-四-(4-三甲铵苯基)卟啉[T-4-TAP)P]作显色剂,测定食品中的痕量锌。对实验条件及共存离子的干扰进行了探讨。室温下,在弱酸性介质中,经7-碘-8羟基卟啉-5-磺酸催化,反应生成1:1络合物。最大吸收波长为422nm摩尔吸收系数为4.0×10~5 1·mo1~(-1)·cm~(-1),桑德尔指数为0.16ng·cm~(2-1),变异系数为1.6—3.7%,回收率为90.8%。本方法适用于分析食品中的痕量锌。     

"2×4"简化固定矫治器与(牙合)垫式活动矫治器的临床应用对照

目的:本研究旨在比较"2×4"简化固定矫治器与(牙合)垫式活动矫治器的矫治效果.方法:本文对20例8至14岁前牙反(牙合)儿童分别采用两种不同的矫治方法,对矫治前后X线头颅定位片及模型进行对比观察.结果:使用固定矫治器组,即"2×4"技术多用唇弓组,治疗效果明显优于(牙合)垫式活动矫治器组,同时分析了两种方法的矫治特点,适应证.结论:提出对反覆(牙合)过大者,用活动矫治器较省时,对反覆盖过大者用固定矫治效果颇佳.     

Pichia stipitis木糖醇脱氢酶基因XYL2在酿酒酵母中的表达

通过PCR方法克隆得到树干毕赤氏酵母木糖醇脱氢酶(XDH)基因XYL2.将该基因连入酵母表达载体pYX212的强启动子磷酸丙糖异构酶(TPI)启动子下,得到融合表达载体pYX-XYL2.通过电转化方法将pYX-XYL2转入酿酒酵母Saccharomyces cerevisiae W303-1A中,酶活测定表明在酿酒酵母中树干毕赤氏酵母木糖醇脱氢酶基因XYL2得到活性表达,酿酒酵母转化子粗酶液中木糖醇脱氢酶比活为每毫克蛋白0.6 U左右,约为供体菌的2.4倍.与基因供体菌不同,木糖醇脱氢酶基因在酿酒酵母中表达不需木糖诱导,为组成型表达.     

Overexpression of protease-activated receptors-1,-2, and-4 (PAR-1, -2, and -4) in prostate cancer

BACKGROUND: Although protease-activated receptors (PARs) have been described to play a role in different malignancies, their expression and biological activity in prostate cancer are mostly unknown. METHODS: PAR expression in radical prostatectomy specimens was investigated by immunohistochemistry (IHC, 40 patients) and RT-PCR. Their role in LNCaP prostate cancer cell migration and Rac1/Cdc42 signaling was assessed with Boyden chamber analysis and Western blot, respectively. RESULTS: PAR mRNA expression was higher in cancer, and protein expression was increased in PAR-1 (45%), PAR-2 (42%), and PAR-4 (68%), compared to normal glands. Increased PAR-1 (periglandular stroma) was associated with higher rates of biochemical recurrence (median follow-up, 5 years; P = 0.006). LNCaP migration was enhanced twofold and Rac1/Cdc42 signaling was activated by stimulation of PAR-1 and PAR-2. CONCLUSIONS: PARs are overexpressed in prostate cancer and may serve as potential predictors of recurrence. The data suggest potential role of PARs in autocrine and paracrine mechanisms of prostate cancer.     

纳米氧化锆强韧化高孔隙率磷酸钙人工骨细胞支架生物学评价

目的：对自行研制的纳米氧化锆强韧化高孔隙率磷酸钙人工成骨细胞支架[hyper-porosity Ca3(PO4)：bone cells frame／NM ZrO2 reinforced以下简称支架]的体外生物相容性进行评价。方法：采用细胞毒性试验、溶血试验和急性全身中毒试验3种方法。结果：(1)培养的L929成骨细胞经支架浸提液处理后形态良好，增值旺盛，材料毒性评级为0级；(2)溶血率为2．23％(小于5％)，符合溶血试验标准要求；(3)无急性全身中毒反应。结论：支架复合物具有良好的生物相容性。     

加味小承气颗粒剂对小鼠腹腔巨噬细胞合成白三烯B_4及对细胞内游离钙浓度的影响

目的：研究加味小承气（ＸｉａｏＣｈｅｎｇＱｉ,ＸＣＱ）颗粒剂治疗腹腔炎症机理与小（大）鼠腹腔巨噬细胞（ＭΦ）合成释放白三烯Ｂ４以及对细胞内游离钙浓度的影响。方法：应用高效液相色谱分析ＬＴＢ４,应用Ｆｕｒａ－２／ＡＭ及荧光分光光度计测定细胞内钙离子浓度。结果：不同浓度的ＸＣＱ颗粒剂（０１５～１０ｇ／Ｌ）明显抑制大鼠（ＭΦ）合成释放白三烯Ｂ４并抑制小鼠细胞内钙离子释放（静止期细胞内钙离子浓度为６３４５±１２４４ｎｍｏｌ／Ｌ,与对照组（１４８３９±１６６２ｎｍｏｌ／Ｌ）比较有显著性差别,在细胞外钙浓度增高条件下,ＸＣＱ尚促使外钙内流。结论：小承气颗粒剂抗炎机理与抑制小（大）鼠（ＭΦ）合成释放白三烯Ｂ４及调节细胞内外钙离子浓度有关。     

Infiltration and tissue concentration of intravesically instilled (2"R)-4'-O-tetrahydropyranyladriamycin or adriamycin in rat bladder tumor induced by BBN

Rats with bladder tumor induced by BBN were treated by intravesical instillation of 0.8 mg of (2"R)-4'-O-tetrahydropyranyladriamycin (THP) (9 rats) or adriamycin (ADM) (8 rats) dissolved in 0.2 ml of distilled water. Thirty minutes later, the bladder was removed surgically. Rats without the tumor received the same treatment of THP (8 rats) or ADM (9 rats). THP and ADM infiltrations to the normal bladder tissue and the tumor were estimated by the use of the photonic microscope system, since both drugs were known to emit characteristic fluorescence. It was found that infiltration of THP to the tumor tissue was more prominent in amounts and deeper than that of ADM, while smaller amounts of THP infiltrated into the normal mucosa compared to ADM. The fact might explain the clinical finding that THP instilled intravesically in half a concentration of ADM showed the same effect on the tumor as ADM. Subsequently, tissue concentrations of THP and ADM were estimated by high performance liquid chromatography. Either THP or ADM was instilled intravesically for 30 minutes to 6 rats with bladder tumor. Similarly, either THP or ADM was instilled in 5 rats without the tumors. Contrary to the result of the photonic microscope system, the tissue concentration of THP was not different from that of ADM not only in the tumor tissues but also in the normal bladder ones. Furthermore, the tissue concentration of both drugs in the normal bladder was higher than that in the bladder tumor.(ABSTRACT TRUNCATED AT 250 WORDS)     

The immunologic function of 1B2+ double negative (CD4-CD8-) T cells in the 2C transgenic mouse

BACKGROUND: 2C mice bearing the cytotoxic TCR for class I L(d) on a C57BL/6 (B6) background have a preponderance of 1B2+CD8+ T cells directed against L(d). These naive CD8+ T cells are not directly cytotoxic without prior in vivo or in vitro activation. However, after in vitro sensitization, they become highly cytotoxic and will acutely and specifically reject a tolerant L(d+) BALB/c heart graft. Anti-lymphocyte serum (ALS) treatment eliminates CD4+ and CD8+ cells and a large double negative (CD4-CD8-) 1B2+ non-cytotoxic transgenic cell population remains. The immunological function of this unique peripheral population of T cells is investigated in the 2C transgenic mouse. MATERIALS AND METHODS: To determine the activation characteristics of the 2C CD4-CD8- T cells, 2C peripheral T cells were analyzed for 1B2+, CD8+, and CD4+ marker by FACS before and 48-h after 0.5 cc ALS i.p. Similarly, in vitro, the response of these 2C CD4-CD8- T cells remaining after deletion of mature CD4+ and CD8+ T cells with ALS plus complement were evaluated by mixed lymphocyte culture and cytotoxic T lymphocyte after 7 days culture with BALB/c, IL-2, or BALB/c + IL-2. Parallel experiments were performed with control non-transgenic B6 mice. Following in vitro culture with BALB/c + IL-2, 2C CD4-CD8- T cells were injected into B6 mice with a tolerant BALB/c heart (tolerization via anti-CD4 mAb and intrathymic BALB/c) to determine their immunogenicity. RESULTS: While peripheral T cells in control B6 mice have <5% CD4-CD8- cells, transgenic 2C mice have a significantly increased percentage at 29 to 35% (P < 0.01). After the deletion of CD4+ and CD8+ T cells with either in vivo or in vitro ALS, 2C CD4-CD8- T cells increased to 96 to 99%. After 7-day culture, the 2C CD4-CD8- T cells decreased again to 33 to 38%. Simultaneously, 2C CD8+ T cells decreased from 56 to 62% to 0.1 to 3% after ALS treatment, but again increased to 61 to 70% after in vitro culture. Untreated 2C cells responded to IL-2 or BALB/c antigen equally well. However, after ALS treatment, CD4-CD8- T cells responded to IL-2 and IL-2 plus antigen, but not BALB/c antigen alone. Finally, CD4-CD8- T cells cultured for 7 days with BALB/c + IL-2 rejected the tolerant BALB/c heart in 5.3 +/- 0.3 days. CONCLUSION: In the periphery of transgenic 2C mice is a unique CD4-CD8- population of T cells bearing the transgenic specific marker 1B2. These non-cytotoxic cells can be optimally stimulated to develop marked specific L(d) cytotoxicity in parallel with the expression of the CD8+ epitope.     

Differential regulation of IGFBP-3 by the androgen receptor in the lineage-related androgen-dependent LNCaP and androgen-independent C4-2 prostate cancer models

BACKGROUND: Despite evidence implicating insulin-like growth factor binding protein-3 (IGFBP-3) as a growth inhibitor of prostate cancer (CaP), little is known about changes in its regulation and function during progression to androgen independence. METHODS: The expression levels of IGFBP-3 were determined by cDNA microarray analysis and tissue microarrays (TMAs) after androgen ablations. LNCaP (LN-BP3) and C4-2 (C4-2-BP3) sublines were used to compare the apoptotic effects of IGFBP-3 in LNCaP (androgen-dependent) and C4-2 (androgen-independent) cells. RESULTS: After androgen deprivation, IGFBP-3 mRNA levels increased more in C4-2 compared to LNCaP cells. Androgens suppressed IGFBP-3 levels in a dose-dependent manner in LNCaP and C4-2 cell. IGFBP-3 expression was increased after NHT in human CaP tissues. Apoptotic rates increased in LN-BP3, but not C4-2-BP3 cells, following doxycycline-mediated IGFBP-3 induction. CONCLUSIONS: C4-2 cell survival in an androgen-depleted environment may be facilitated through differential resistance to the apoptotic effects elicited by IGFBP-3.     

Phorbol ester (TPA) reduces prostaglandin E2-stimulated cAMP production by desensitization of prostaglandin E2 receptors in a clonal osteoblast-like cell line,MOB 3-4

Summary A clonal osteoblast-like cell line, MOB 3-4, increased cAMP production in response to prostaglandin E₂ (PGE₂) (5–500 ng/ml). The purpose of this study was to show the effects of tumor-promoting phorbol ester (e.g., 12-O-tetradecanoylphorbol 13-acetate, TPA) on basal and PGE₂-stimulated cAMP production and the affinity of PGE₂ receptors in the cells. Pretreatment with TPA (1 nM–10 μM) for 30 minutes increased basal cAMP production, whereas it markedly reduced the PGE₂-stimulated cAMP production in the presence of 0.1 mM isobuthylmethyl xanthine. Both the TPA increase and reduction were dose- and time-dependent. However, TPA exerted no effect on forskolinor cholera toxin-stimulated cAMP production. Copretreatment with TPA and H-7, an inhibitor of protein kinase C (PKC), prevented the TPA-induced increase in basal cAMP production, whereas it did not prevent the reduction of the PGE₂-stimulated cAMP production. On the other hand, TPA (0.1–10 μM) decreased³H-PGE₂ binding in a dose- and time-dependent manner. Scatchard analysis revealed that TPA decreased the apparent affinity of PGE₂ receptors without effect on their apparent number. In addition, 1-oleoyl-2-acetylglycerol (12.6 μM), a synthetic diacylglycerol analog, did not mimic the TPA action on³H-PGE₂ binding. Thus, TPA at relatively high concentrations appeared to increase basal cAMP production by a PKC-mediated mechanism, and it appeared to directly act on PGE₂ receptors to decrease their apparent affinity and thereby reduce the PGE₂-stimulated cAMP production in the clonal osteoblast-like MOB 3-4 cell line.     

Promoting effect of sodium chloride in 2-stage urinary bladder carcinogenesis in rats initiated by N-Butyl-N-(4-hydroxybutyl)-nitrosamine

Summary The promoting effect of sodium chloride (NaCl) in 2-stage urinary bladder carcinogenesis in F344 rats initiated by 2 doses of N-butyl-N-(4-hydroxybutyl)nitrosamine (BBN) was investigated. The incidences of PN hyperplasia were significantly higher in rats initiated with 0.01 or 0.05% BBN when they were given diet containing 10% NaCl for 32 weeks than when they were given control diet. The incidence of papilloma in rats given 0.05% BBN followed by diet containing 10% or 5% NaCl tended to be higher than that in control rats. The urine of rats given diet containing NaCl was larger in volume and had lower osmolality than that of controls. The total urinary sodium and chloride contents were also increased, whereas those of potassium and phosphorus were decreased. No calculus formation or crystalluria was observed. These data suggest that excess intake of sodium as NaCl has a weak promoting effect in 2-stage urinary bladder carcinogenesis.