译者：苏小赖
药物的靶向传递以及克服耐药性是目前筛查和治疗癌症 的主要临床挑战。 具有能够快速筛选药物和输送系统的能力对于内环境来说至关重要; 由于缺乏合适的肿瘤模型，目前解决此类问题的方法仍然有限。为了解决这个问题，我们研发了肿瘤微环境芯片（T-MOC），一种模拟肿瘤内药物间质流，血浆清除率及转运方式的新型微流体肿瘤模型。我们通过评估小分子多柔比星与透明质酸纳米颗粒（NP）制剂 在乳腺癌不同分子亚型的两种细胞系MCF-7和MDA-MB-231的送递和功效，证明了T-MOC的作用。多柔比星在两种细胞系中都有相似的蓄积性和渗透作用，而透明质酸纳米颗粒（NP） 在MDA-MB-231中的蓄积量高于MCF-7，这可能是由于透明质酸与MDA-MB-231表达的CD44的结合。 但由于其体积较大 ，NP的渗透性小于分子药物。 此外，与2D培养皿上的两种细胞亚系相比，在肿瘤微环境芯片（T-MOC） 上培养的两种细胞系显示 抗药性均增加，其中mda-mb-231通过增加CD44的表达来达到耐药性的肿瘤初始表型。当在免疫功能受损的小鼠中生长时，这两种细胞系都表现出与肿瘤微环境芯（T-MOC）相似的依赖性细胞型耐药和表型变化，这证实了肿瘤微环境芯（T-MOC） 对体内药物反应具有预测能力。 T-MOC的这种初步表征表明其具有将体外测试药物功效 的结果转化为对体内结果的预测以及对个体化药物进展的耐药机制的研究的潜力。
Differential response to doxorubicin in breast cancer subtypes simulated by a microfluidic tumor model
J. Control. Release
20 September 2017
10.1016/j.jconrel.2017.09.024
Altug Ozcelikkale, Kyeonggon Shin, Victoria Noe-Kim, Bennett D. Elzey, Zizheng Dong, Jian-Ting Zhang, Kwangmeyung Kim, Ick Chan Kwon, Kinam Park, Bumsoo Han
Successful drug delivery and overcoming drug resistance are the primary clinical challenges for management and treatment of cancer. The ability to rapidly screen drugs and delivery systems within physiologically relevant environments is critically important; yet is currently limited due to lack of appropriate tumor models. To address this problem, we developed the Tumor-microenvironment-on-chip (T-MOC), a new microfluidic tumor model simulating the interstitial flow, plasma clearance, and transport of the drug within the tumor. We demonstrated T-MOC's capabilities by assessing the delivery and efficacy of doxorubicin in small molecular form versus hyaluronic acid nanoparticle (NP) formulation in MCF-7 and MDA-MB-231, two cell lines representative of different molecular subtypes of breast cancer. Doxorubicin accumulated and penetrated similarly in both cell lines while the NP accumulated more in MDA-MB-231 than MCF-7 potentially due to binding of hyaluronic acid to CD44 expressed by MDA-MB-231. However, the penetration of the NP was less than the molecular drug due to its larger size. In addition, both cell lines cultured on the T-MOC showed increased resistance to the drug compared to 2D culture where MDA-MB-231 attained a drug-resistant tumor-initiating phenotype indicated by increased CD44 expression. When grown in immunocompromised mice, both cell lines exhibited cell-type-dependent resistance and phenotypic changes similar to T-MOC, confirming its predictive ability for in vivo drug response. This initial characterization of T-MOC indicates its transformative potential for in vitro testing of drug efficacy towards prediction of in vivo outcomes and investigation of drug resistance mechanisms for advancement of personalized medicine.
http://www.sciencedirect.com/science/article/pii/S0168365917308581
译者：小七
我们开发了一种有效且方便的钯催化串联Saegusa-Heck反应方案，它的潜在用途是合成对称和不对称的β，β-二芳基丙烯醛。实验证明，该方法可以得到中等到较高的产量。
Pd-Catalyzed Cascade Saegusa-Heck Reaction: Synthesis of β,β-Diarylacroleins from Aryl Propanals and Aryl Iodides
Eur. J. Org. Chem.
Accepted manuscript online: 9 September 2017
DOI: 10.1002/ejoc.201701025
Li Xiao, Yilin Zheng, Qiong Xie, Liming Shao
An efficient and convenient Pd-catalyzed cascade Saegusa-Heck protocol has been developed, and its potential use in the synthesis of symmetrical and unsymmetrical β, β-diarylacroleins with moderate to high yields has been investigated.
http://onlinelibrary.wiley.com/doi/10.1002/ejoc.201701025/full
译者：小七
我报道了可以快速制备的一种芳基型的二黄花烯支架，其可以很容易地在与两个氧杂蒽的氧原子相邻的4，5位置上的官能团中进行衍生：合成五种可能的四配位基、多核、金属结合配体。
A General Approach for Nanoparticle Composite Transport Materials toward Efficient Perovskite Solar Cells
Tetrahedron
18 September 2017
10.1016/j.tet.2017.09.026
Matthew Mudge, Alpesh Ramanlal Patel, Murat Bingül, Mohan Bhadbhade, Stephen B. Colbran
An aryl-bridged dixanthene scaffold is quickly prepared and readily derivatized with functional groups at the four 4,5-positions adjacent to the oxygen atoms of the two xanthene groups: syntheses of five potentially tetradentate, multinucleating, metal-binding ligands illustrate the usefulness of the methodology.
http://www.sciencedirect.com/science/article/pii/S0040402017309559
译者：啊达
我们已经报道一种高效的去氧基环化反应，它用于通过氧化还原催化各种联芳基羧酸来合成芴酮的反应。该过程吸引人的特点在于产生酰基，并且可以迅速参与分子内的自由基环化反应。该方法标志着首次通过光催化分子内酰基偶联来形成碳碳键，用于进一步合成反映条件温和、产量高、官能团兼容性好、有价值的芴酮产物。
Photoredox-Catalyzed Deoxygenative Intramolecular Acylation of Biarylcarboxylic Acids: Access to FluorenonesJ. Org. Chem.
September 26, 2017
10.1021/acs.joc.7b02197
Rehanguli Ruzi, Muliang Zhang, Keyume Ablajan, and Chengjian Zhu
An efficient deoxygenative radical cyclization reaction has been reported for the synthesis of fluorenones by employing various biarylcarboxylic acids via photoredox catalysis. Attractive features of this process include generation of acyl radical, which quickly underdone intramolecular radical cyclization. This method marks the first photocatalytic intramolecular acyl radical coupling for constructing carbon-carbon bond, which further synthesize the valuable fluorenone products with mild conditions, good yields and good functional-group compatibility.
http://pubs.acs.org/doi/10.1021/acs.joc.7b02197
译者：苏小赖
Catalytic Carbonylative Rearrangement of Norbornadiene via Dinuclear Carbon–Carbon Oxidative Addition
Chem. Commun.
22 Sep 2017
10.1039/C7CC06004A
Kohsuke Inomata, Hajime Kamoshida, Masaomi Ikari, Yutaka Ito and Takanori Kigawa
By in-cell NMR experiments, we have demonstrated that the protein folding state in cells is significantly influenced by the cellular health condition. hAK1 was denatured in cells under stressful culture conditions, while it remained functional and properly folded in cells continuously supplied with fresh medium.
http://pubs.rsc.org/en/content/articlelanding/2017/cc/c7cc06004a#!divAbstract
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