UV-irradiation-induced bioactivity on TiO2 coatings with nanostructural surface

Titania (TiO₂) coatings with nanostructural surface prepared using plasma spraying technology were irradiated by ultraviolet light in simulated body fluids to improve their bioactivity. The in vitro bioactivity of the coatings was evaluated by investigating the formation of apatite on their surfaces in simulated body fluids. Bone-like apatite was observed to precipitate on the UV-irradiated TiO₂ coating with nanostructural surface after it was immersed in simulated body fluid for a certain period, but not on the as-sprayed and UV-irradiated TiO₂ coatings without nanostructural surface. The results indicate that the nano-TiO₂ surface can be activated by UV-irradiation to induce its bioactivity. The ability of apatite formation on the nano-TiO₂ surface was improved with the increase of UV-irradiation time. The in vivo results reveal that the as-prepared TiO₂ coating with nanostructural surface cannot induce the formation of new bones during the implantation period, but the UV-irradiated TiO₂ coating with nanostructural surface could do so during an implantation time longer than 2 months. Our results indicate that the osseointegration ability of the plasma-sprayed TiO₂ coating with nanostructural surface can be improved by UV irradiation.     

扶正化瘀方体外给药方法及生物活性差异的探讨

目的:建立扶正化瘀方体外给药方法,观察不同批次间药效差异,为中药复方生物活性的质控奠定基础。方法:选择人肝细胞L-02、小鼠单核巨噬细胞RAW264.7和小鼠原代骨髓来源巨噬细胞(Bone Marrow-derived Macrophage,BMDM),分别建立肝细胞过氧化损伤模型和巨噬细胞活化模型,首先通过考察溶媒、作用浓度等因素对细胞效应的影响,基于扶正化瘀体外给药的最佳保肝抗炎效果,建立扶正化瘀浸膏体外配置给药方法;再比较不同批次的扶正化瘀浸膏对肝细胞损伤和巨噬细胞活化药效差异。结果:扶正化瘀浸膏以二甲基亚枫溶解不过滤,不同批次扶正化瘀的化学指标成分不同,但在细胞生物活性总体无显著性差异,其中批号171005与其他批次的部分生物活性略有不同。结论:确立了扶正化瘀方体外给药方法,发现其化学成分质控与细胞生物活性不一致。     

水柏枝化学成分、药理活性和质量标准研究进展

水柏枝为传统的藏蒙药,来源于柽柳科(Tamaricaceae)水柏枝属(Myricaria)多种植物的嫩枝叶,主要用于风疹和类风湿性关节炎的治疗。但该属植物化学成分研究不充分、药效物质基础和作用机制不明,导致水柏枝药材质量难以控制,严重影响了水柏枝的应用与开发。本文综述了水柏枝属7种主要基源植物的化学成分、药理活性及水柏枝药材的质量标准研究进展,为水柏枝的药效物质基础研究和质量控制提供参考。     

Integrating Incompatible Assay Data Sets with Deep Preference Learning

A large amount of bioactivity assay data is already accumulated in public databases, but the integration of these data sets for quantitative structure–activity relationship (QSAR) studies is not straightforward due to differences in experimental methods and settings. We present an efficient deep-learning-based approach called Deep Preference Data Integration (DPDI). For integrating outcome variables of different assay types, a surrogate variable is introduced, and a neural network is trained such that the total order induced by the surrogate variable is maximally consistent with given data sets. In a task of predicting efficacy of factor Xa inhibitors, DPDI successfully integrated 2959 molecules distributed in 129 assay data sets. In most of our experiments, data integration improved prediction accuracy strongly in interpolation and extrapolation tasks, indicating that DPDI is an effective tool for QSAR studies.     

多型短指软珊瑚Sinularia polydactyla(Ehreberg)中的氧化甾醇

目的充分利用我国南海药用资源,发现软珊瑚Sinularia polydactyla(Ehreberg)中抗肿瘤和抗炎活性成分。方法采用硅胶柱层析,物理常数比较和波谱方法(NMR、MS等)确定化合物的结构。结果从采自海南三亚海域的多型短指软珊瑚Sinularia polydactyla(Ehreberg)乙醇提取物的乙酸乙酯部位分离得到3个甾体类化合物。通过物理数据比较和波谱方法确定其结构分别是:24-亚甲基-9,11-开环胆甾-5-烯-3β,11-二醇-9-酮(1),9,11-开环麦角甾-5-烯-3β,11-二醇-9-酮(2),麦角甾-3β,5α,6β-三醇(3)。结论化合物1,2,3均首次从此种软珊瑚中得到。体外活性试验表明均具有抗炎活性和显著的细胞毒活性。     

海洋微生物次生代谢产物的结构特征和生物活性的研究进展

本文归纳了21世纪以来海洋微生物产生的次生代谢产物的结构类型及其抗菌、抗肿瘤、抗心脑血管疾病、抗炎症和酶抑制等生物活性,并展望了今后海洋微生物和海洋天然产物的发展方向。