18β-甘草次酸A环官能团化衍生物的合成及抗肿瘤活性

采用化学方法对18β-甘草次酸A环进行改造, 合成了一系列新型18β-甘草次酸A环官能团化衍生物. 对人白血病细胞株HL-60、K562、肝癌细胞BEL-7404及乳腺癌细胞MDA-MB-231的体外抗肿瘤活性筛选结果表明, 化合物5对4种肿瘤细胞系的抑制活性均强于18β-甘草次酸; 构效关系分析表明, A环内烯键的形成对抑制肿瘤细胞增殖有重要影响; 同时利用Hoechst33258和AO/EB染色, 在荧光显微镜下观察到了细胞凋亡小体的形成.     

Red Yeast Rice Fermentation by Selected Monascus sp. with Deep-Red Color, Lovastatin Production but No Citrinin, and Effect of Temperature-Shift Cultivation on Lovastatin Production

Monascus pilosus NBRC4520 was selected for functional fermented food inoculation for its high lovastatin and low citrinin production with a deep-red color. For koji (mold rice) with high lovastatin production, separation of the growth phase and lovastatin production phase by shifting the temperature from 30 to 23 °C increased lovastatin production by nearly 20 times compared to temperature-constant cultivation. In addition, citrinin was not produced even in the lovastatin production phase, although the pigment was increased. With temperature-shift cultivation, 225 μg lovastatin/g dry koji was produced in 14 days without citrinin.     

吡啶二甲酸类配体-EDTA-铽三元配合物的荧光性能

对几种吡啶－２,６－二甲酸类配体与ＥＤＴＡ、铽的三元配合物在溶液中的荧光性能进行了研究,溶液ＰＨ值和溶剂效应对体系荧光的影响也分别进行了探讨。４－甲氧基吡啶－２,６－二甲酸和４－乙氧基吡啶－２,６－二甲酸等配体在这种三元体系中的敏化性能比常用的吡啶－２,６－二甲酸好,其中４－乙酰氨基吡啶－２,６－二甲酸特别优异。不论在二元配合物系还是在三元配合物体系中,均具有发光强度大、寿命长的特点。     

Neurotransmitter Transporter Family Including SLC6A6 and SLC6A13 Contributes to the 5‐Aminolevulinic Acid (ALA)‐Induced Accumulation of Protoporphyrin IX and Photodamage,through Uptake of ALA by Cancerous Cells

δ‐Aminolevulinic acid (ALA)‐induced protoporphyrin accumulation is widely used in the treatment of cancer, as photodynamic therapy (PDT). To clarify the mechanisms of ALA uptake by tumor cells, we have examined the ALA‐induced accumulation of protoporphyrin by the treatment of colon cancer DLD‐1 and epithelial cancer HeLa cells with γ‐aminobutyric acid (GABA)‐related compounds. When the cells were treated with GABA, taurine and β‐alanine, the level of protoporphyrin was decreased, suggesting that plasma membrane transporters involved in the transport of neurotransmitters contribute to the uptake of ALA. By transfection with neurotransmitter transporters SLC6A6, SLC6A8 and SLC6A13 cDNA, the ALA‐ and ALA methylester‐dependent accumulation of protoporphyrin markedly increased in HEK293T cells, dependent on an increase in the uptake of ALA. When ALA‐treated cells were exposed to white light, the extent of photodamage increased in SLC6A6‐ and SLC6A13‐expressing cells. Conversely, knockdown of SLC6A6 or SLC6A13 with siRNAs in DLD‐1 and HeLa cells decreased the ALA‐induced accumulation. The expression of SLC6A6 and SLC6A13 was found in some cancer cell lines. Immunohistochemical studies revealed that the presence of these transporters was elevated in colon cancerous cells. These results indicated that neurotransmitter transporters including SLC6A6 and SLC6A13 mediate the uptake of ALA and can play roles in the enhancement of ALA‐induced accumulation of protoporphyrin in cancerous cells.     

Phosphotungstic Acid Catalyzed One Pot Synthesis of 4,8,8‐Trimethyl‐5‐phenyl‐5,5a,8,9‐tetrahydrobenzo[b] [1,8]Naphthyridin‐6(7H)‐one Derivatives and Their Biological Evaluation Against A549 Lung Cancer Cells

A facile one pot multicomponent synthesis of 1,8‐naphthyridinone derivatives was developed using a mild and reusable phosphotungstic acid catalyst. A 2‐amino picoline, benzaldehyde derivatives and 1,3‐dicarbonyl cyclohexane were used to synthesize 1,8‐naphthyridinones, which was achieved by conventional heating under solvent‐free conditions. All synthesized compounds were characterized by spectral analysis and screened for anticancer activity against A549 lung cancer cells. The results from the cell viability assay showed that the synthesized compounds do have a biological effect at various concentrations on the lung cancer cells. Compounds 4F‐p‐CF₃ and 4H‐VAN showed potential as an antiproliferative agent and a dose‐dependent decline in cell viability was observed.