Synthesis and Biological Activity of Oxidation Products of the Antiprogestine Mifepristone

Summary.  Selenium dioxide oxidation allows the selective introduction of a hydroxyl group at position 6 of the steroid skeleton of the antihormone (11β, 17β)-11-(4-dimethylamino-phenyl)-17-hydroxyl-17-(1-propynyl)-estra-4,9-dien-3-one (mifepristone, RU 486) and leads in a one-step procedure to two diastereomeric oxidation products. Their structure (6α- and 6β-hydroxy-mifepristone) was determined by NMR spectroscopy. The antiprogestinic activity of the oxidation products is comparable to that of mifepristone. Received August 25, 2000. Accepted (revised) October 24, 2000     

Boron complexes of S-trityl- -cysteine and S-tritylglutathione

S-Trityl- -cysteine and S-tritylglutathione have been converted to 1,3,2-oxazaborolidine-5-ones by reaction with B-methoxydialkylborane derivatives. The synthesis of dicyclohexyl[S-trityl-(R)-cysteinato-O,N]boron (2), diisopinocampheyl[S-trityl-(R)-cysteinato-O,N]boron (3) and 9-borabicyclo[3.3.1]non-9-yl[S-tritylglutathionato-O,N]boron (5), dicyclohexyl[S-tritylglutathionato-O,N]boron (6) and diisopinocampheyl[S-tritylglutathionato-O,N]boron (7) from S-trityl- -cysteine and S-tritylglutathione, respectively, with potential application in boron neutron capture therapy is reported. The structure of 9-borabicyclo[3.3.1]non-9-yl[S-trityl-(R)-cysteinato-O,N]boron 1 has been determined by X-ray diffraction.     

X射线荧光光谱法分析癌症村土壤主量元素

由于工业的快速发展带来了许多诸如环境污染等不利的方面,“癌症村”就是一个沉重的例子。应用X射线荧光光谱法测定了一个较典型癌症村土壤中主量元素的含量。该村土壤中主量元素SiO₂,TiO₂,Al₂O₃,Fe₂O₃,MnO,MgO,CaO,Na₂O,K₂O和P₂O₅含量分别为66.05%,0.66%,11.37%,3.93%,0.075%,1.97%,5.47%,1.90%,2.11%和0.20%。各元素含量在测定范围之内,各种元素的分析精度较高,都在0.20%～0.005%之间,X射线荧光光谱法是一种测定污染土壤中主量元素的快速、有效的方法。     

Self‐Assembling Proteins for Design of Anticancer Nanodrugs

Inspired by the diverse protein‐based structures and materials in organisms, proteins have been expected as promising biological components for constructing nanomaterials toward various applications. In numerous studies protein‐based nanomaterials have been constructed with the merits of abundant bioactivity and good biocompatibility. However, self‐assembly of proteins as a dominant approach in constructing anticancer nanodrugs has not been reviewed. Here, we provide a comprehensive account of the role of protein self‐assembly in fabrication, regulation, and application of anticancer nanodrugs. The supramolecular strategies, building blocks, and molecular interactions of protein self‐assembly as well as the properties, functions, and applications of the resulting nanodrugs are discussed. The applications in chemotherapy, radiotherapy, photodynamic therapy, photothermal therapy, gene therapy, and combination therapy are included. Especially, manipulation of molecular interactions for realizing cancer‐specific response and cancer theranostics are emphasized. By expounding the impact of molecular interactions on therapeutic activity, rational design of highly efficient protein‐based nanodrugs for precision anticancer therapy can be envisioned. Also, the challenges and perspectives in constructing nanodrugs based on protein self‐assembly are presented to advance clinical translation of protein‐based nanodrugs and next‐generation nanomedicine.     

大肠癌与微量元素研究

对48例大肠癌患者手术前后血清和正常大肠组织与癌组织中微量元素测定、比较，发现大脑癌患者手术前后血清微量元素变化，除Cr、Mn有显著差异外均无显著差异，而癌瘤组织与正常大脑组织中Ca、Cd、Mn、Zn、Cu/Zn有明显差异，探讨了大肠癌发生的机理。大肠癌病因是复杂的，但与微量元素改变有一定关系，并指出，组织测定观察微量元素变化比血清测定观察更敏感。     

Applications of slow positrons to cancer research: Search for selectivity of positron annihilation to skin cancer

Slow positrons and positron annihilation spectroscopy (PAS) have been applied to medical research in searching for positron annihilation selectivity to cancer cells. We report the results of positron lifetime and Doppler broadening energy spectroscopies in human skin samples with and without cancer as a function of positron incident energy (up to 8 μm depth) and found that the positronium annihilates at a significantly lower rate and forms at a lower probability in the samples having either basal cell carcinoma (BCC) or squamous cell carcinoma (SCC) than in the normal skin. The significant selectivity of positron annihilation to skin cancer may open a new research area of developing positron annihilation spectroscopy as a novel medical tool to detect cancer formation externally and non-invasively at the early stages.     

中红外光纤技术用于肿瘤在体原位诊断的研究

本文采用傅里叶变换红外光谱法与中红外光纤及ATR探头联用,首次实现了肿瘤组织的在体原位检测,即在有血液循环的活体组织中获得了具有很好信噪比的中红外光谱。实验结果表明在体原位的正常和肿瘤组织的光谱特征同我们先前液氮冰冻样品以及新鲜离体检测的结果是相似的,即符合液氮和新鲜离体样品研究中所得到的鉴别癌症与正常组织光谱变化规律,例如图1所列出的肠癌的原位在体光谱,与离体癌变组织光谱相似,这一创新结果表明中红外光纤-红外光谱仪联用可能发展成一种外科手术中无损、快速、准确的在体检测的方法。     

Progress in Molecular Chaperone Regulation of Heat Shock Protein 90 and Cancer

Heat shock protein 90 (HSP90) is a member of genetically conserved heat shock protein family. As an important molecular chaperone in eukaryotic cells, HSP90 plays a key regulatory role in maintaining cellular protein homeostasis. HSP90 clients encompass a wide range of proteins, thus HSP90 is involved in diverse biological process. With the deeper study, it is found that HSP90 takes an important part in the development and metastasis of cancer, and has become a promising target for the study of anticancer biology. In this review, the progress of HSP90 as molecular chaperone and its relationship with cancer are discussed.     

A cancer cell turn-on protein-CuSMn nanoparticle as the sensor of breast cancer cell and CH3O-PEG-phosphatide

A cancer activated protein-inorganic nanoparticle was used as breast cancer cell turn-on fluorescence sensor and NIR activated attenuator.     

高压液相色谱法测定肿瘤患者血清中假尿苷的含量

建立了血清中假尿苷含量的高效液相色谱测定法。结果表明，假尿苷在０３７５～１２μｍｏｌ／Ｌ范围内线性关系良好。最低检测量为００１５μｍｏｌ／Ｌ，回收率为９２７％，日内和日间相对标准偏差（ＲＳＤ）分别为４２％和４７％。用该法测定正常人及肝癌、肺癌、食管癌患者血清中假尿苷含量发现，３种肿瘤患者血清中假尿苷含量明显高于正常人（Ｐ＜００５），说明血清假尿苷可作为诊断恶性肿瘤的一种标志物。