MDR逆转活性紫杉烷类化合物的合成

目的:合成天然产物taxinine NN-3和taxinine NN-14,研究其对肿瘤细胞的多药耐药逆转活性.方法:以紫杉宁为出发原料,通过选择性水解9,10位的乙酰氧基,制成原乙酸酯后再水解.结果:以紫杉宁为原料经过3步反应,可以同时获得taxinine NN-3,taxinine NN-4两种天然产物,其中taxinine NN-3的收率为25%,taxinineNN-4的收率为68%.结论:高收率地合成了taxinine NN-3和taxinine NN-14.     

MMP-14 在乳腺癌中的表达及临床意义

 目的 检测膜型-1基质金属蛋白酶(MMP-14)在乳腺癌中的表达并探讨其临床意义。方法 采用免疫组化的方法检测46例乳腺癌手术后标本中MMP-14蛋白的表达，探讨MMP-14表达与乳腺癌临床病理因子的关系。结果 MMP-14蛋白在正常乳腺组织中没有表达，在乳腺癌中表达的阳性率是52．2％。在Ⅰ期、Ⅱ期和Ⅲ期乳腺癌中表达的阳性率分别为12．5％、54．8％和85．7％(P<0．05)；在T1、T2和T3三组中的阳性率分别为11．1％、59．4％和8t)．O％(P<0．05)；在N0、N1和N2三组中的阳性率分别为27．3％、66．7％和100％(P<0．05)。MMP-14蛋白的表达与VEGR呈正相关(P<0．05)，但与ER、PR、c-erbB-2的状况无统计学差异(P>0．05)。结论 MMP-14的蛋白质在乳腺癌中的表达与肿瘤分期、肿瘤大小、淋巴结转移和VEGF呈正相关，有可能为判断乳腺癌浸润转移能力的一个指标。     

Convenient synthesis of D‐threo‐[dichloroacetyl 1–14C] chloramphenicol

A convenient synthesis of chloramphenicol labelled with carbon‐14 in the dichloroacetyl group at the 1 position is described. It was prepared as part of a 4‐step sequence from [1 ‐ ¹⁴C] glycine and the product was purified by preparative HPLC. A radiochemical yield of 47% was obtained based on [1 ‐ ¹⁴C] glycine and the product had a specific activity of 0.47 mCi/mmol. The procedure can be employed for the synthesis of high specific activity [¹⁴C] chloramphenicol, labelled at 1, 2 or both the positions of dichloroacetyl group. Copyright © 2005 John Wiley & Sons, Ltd.     

Synthesis of [14C]‐radiolabelled entecavir

Radiolabelled [¹⁴C]entecavir, ( 1 ), was prepared in 12 steps from (1S,2R,3S,5R)‐3‐(benzyloxy)‐2‐(benzyloxymethyl)‐6‐oxa‐bicyclo[3.1.0]hexane 2 . The chemical yield of [¹⁴C]entecavir was 14% from the epoxide 2 . Introduction of [¹⁴C] radiolabel was achieved by elaboration of 4,5‐diaminopyrimidine 8 with triethyl[¹⁴C]orthoformate to purine derivative 9 . The radiochemical yield of [¹⁴C]entecavir from triethyl[¹⁴C]orthoformate was 11.3%. Radiochemical purity of [¹⁴C]entecavir determined by HPLC was 99.8%. The specific activity of [¹⁴C]entecavir was 108 µCi/mg (29.9 mCi/mmol). Copyright © 2005 John Wiley & Sons, Ltd.     

穿心莲中穿心莲内酯、脱水穿心莲内酯在茎和叶中的分布

采用薄层扫描法分别测定了12批穿心莲商品药材中茎和叶所含穿心莲内酯和脱水穿心莲内酯的含量,并进行了比较,结果其总量在茎中平均占0.29%,在叶中平均占2.26%.因此建议穿心莲中叶所占比例应不少于35%.     

Carbon‐14 labeling of hydrochlorothiazide via [14C]formaldehyde production from [14C]carbon dioxide at ambient temperature

[¹⁴C]Formaldehyde was synthesized by reducing ¹⁴CO₂ at ambient temperature with Schwartz's reagent. The [¹⁴C]formaldehyde was then used in the radiosynthesis of high specific activity (2.1 GBq/mmol) [¹⁴C]hydrochlorothiazide via cyclization of 4‐amino‐5‐chloro‐1,3‐benzenedisulfonamide.     

S100A14, a mediator of epithelial-mesenchymal transition,regulates proliferation,migration and invasion of human cervical cancer cells

S100A14 is an EF-hand calcium-binding protein that has been reported to exert its biological effects on different types of cells. However, the potential clinical significance and biological functions of S100A14 in cervical cancer has not yet been clarified. In this study, we firstly examined the correlation between S100A14 expression and clinical-pathological parameters in cervical cancers. Next, we observed the effect of S100A14 on cell cycle progression, cell proliferation, migration and invasion by employing lentiviral-mediated overexpression and knockdown of S100A14 in cervical cancer cells. Furthermore, we investigated the underlying mechanism of S100A14 affecting cell migration and invasion. Immunohistochemistry analysis demonstrated that S100A14 expression was associated with the International Federation of Gynecology and Obstetrics (FIGO) stage (P = 0.025) and lymph node (LN) metastasis (P = 0.001). Functional assays showed that S100A14 overexpression increased the proportion of G2/M phase, promoted cell proliferation, migration, and invasion, whereas S100A14 knockdown exhibited adverse effect on above properties. Mechanistic investigation demonstrated that S100A14 can act as a mediator of epithelial-mesenchymal transition (EMT). And overexpression of S100A14 increased expression of N-cadherin and Vimentin while decreased expression of E-cadherin. The opposite results were observed in S100A14-silenced cells. Taken together, our data indicate that S100A14 has a crucial role in cervical cancer progression. This study significantly increases our understanding of S100A14 functional roles in cervical cancer, which may lead to the development of a novel therapeutic target for cervical cancer.     

A Comparison of Endodontic Treatment Factors,Operator Difficulties,and Perceived Oral Health–related Quality of Life between Elderly and Young Patients

IntroductionThe purpose of this study was to compare endodontic treatment factors, treatment difficulties, and oral health–related quality of life (OHRQOL) between elderly and young patients.MethodsA total of 150 adults, 75 elderly (≥65 years) and 75 young patients (18–64 years), were recruited. Operators enumerated difficulties associated with communication, diagnosis, rubber dam application, access cavity preparation, canal localization, working length determination, instrumentation, and obturation after root canal treatment. The number of treatment visits, maxillary first molars with a second mesiobuccal canal, and the technical quality of the root filling were registered. Patients filled out questionnaires on pain, attendance of regular dental visits, esthetics, and masticatory function and the Oral Health Impact Profile-14.ResultsSignificantly more elderly had necrotic pulp (P < .001) and needed root canal treatment on teeth with full-coverage crown/bridge abutment (P < .001). It was significantly difficult to perform access cavity preparation and localize root canals on the elderly and on teeth with a full-coverage crown/bridge abutment. In regression analysis, the elderly presented with difficulties only during canal localization (P < .05). Second mesiobuccal canals were obturated in 43.5% of the young patients and 23.1% of the elderly patients. There were no significant differences in the number of treatment visits or the technical quality of root filling between the 2 groups. There were no significant differences in pain sensation, esthetics, masticatory function, or regular dental visits between the 2 groups. Elderly patients reported a significantly better OHRQOL (P < .05). Patients experiencing pain, patients needing treatment on anteriors/premolars, and females reported a significantly poorer OHRQOL (P < .05).ConclusionsThe elderly presented with treatment difficulty during canal localization and had better OHRQOL compared with young patients.     

Essential Oils of Annual Sideritis Species Growing in Turkey

Water distilled essential oils of five annual Sideritis species collected from different regions of Turkey were analysed by GC/MS. Results are tabulated and compared with main components of the essential oils of perennial Sideritis species from Turkey.