Synthesis and mechanism of biological action of morpholinyl-bearing arylsquaramides as small-molecule lysosomal pH modulators

Lysosomal pH is an important modulator for many cellular processes. An agent that is capable of regulating lysosomal pH may find a wide range of potential applications in the field of biomedicine. In this study, we describe the synthesis of a family of morpholinyl-bearing arylsquaramides as small-molecule lysosomal pH modulators. These compounds are able to efficiently facilitate the transmembrane transport of chloride anions as mobile carriers across vesicular and cellular phospholipid membranes. They are capable of specifically alkalizing liposomes, disrupting the homeostasis of lysosomal pH and inactivivating lysosomal Cathepsin B enzyme. Anion transport is considered as the probable mechanism of action for the high efficiency of these compounds to modulate lysosomal pH. The present findings present a novel means to efficiently regulate lysosomal pH, which is in contrast to the methods shown by conventional lysosomal pH modulators that generally function by either acting as a weak base/acid, or releasing a basic/acidic component in lysosomal environments to change lysosomal pH.

A family of small-molecule arylsquaramides were synthesized as transmembrane anion transporters for modulating lysosomal pH.     

Functional utilization of biochar derived from Tenebrio molitor feces for CO2 capture and supercapacitor applications

Biochar has attracted great interest in both CO₂ capture and supercapacitor applications due to its unique physicochemical properties and low cost. Fabrication of eco-friendly and cost-effective biochar from high potential biomass Tenebrio molitor feces can not only realize the functional application of waste, but also a potential way of future carbon capture and energy storage technology. In this study, a novel KOH activation waste-fed Tenebrio molitor feces biochar (TMFB) was developed and investigated in terms of CO₂ capture and electrochemical performance. When activated at 700 °C for 1 h, the specific surface area of the feces biochar (TMFB-700A) increased significantly from 232.1 to 2081.8 m² g⁻¹. In addition, well-developed pore distribution facilitates CO₂ capture and electrolyte diffusion. TMFB-700A can quickly adsorb a large amount of CO₂ (3.05 mol kg⁻¹) with excellent recycling performance. TMFB-700A also exhibited promising electrochemical performance (335.8 F g⁻¹ at 0.5 A g⁻¹) and was used as electrode material in a symmetrical supercapacitor. It provided a high energy density of 33.97 W h kg⁻¹ at a power density of 0.25 kW kg⁻¹ with 90.47% capacitance retention after 10 000 charge–discharge cycles. All the results demonstrated that TMFB could be a potential bifunctional material and provided valuable new insights for Tenebrio molitor feces high-value utilization.

Biochar has attracted great interest in both CO₂ capture and supercapacitor applications due to its unique physicochemical properties and low cost.     

青少年颈椎病的病因病机及预防

青少年颈椎病很少有人研究，笔者在临床中发现高中学生中时有颈椎病发生，比例约占学生总数１５．７９％，年龄均在１５—１９岁间。通过对５００余名高中、小学生的坐姿、睡姿调查发现：学生从小学一年级就开始的铅笔习字和枕高不合标准—使坐姿、睡姿改变—迫使颈椎生理弧度改变—颈部生物力学早期综合性失衡—颈部解剖学、组织学改变—最终出现病理学改变—颈椎病发生。Ｘ线平片证实：学生颈椎病主要是颈椎曲度值改变，与增生关系不大。并针对青少年颈椎病出现的病因病机，提出了一套保健措施，自编《青少年颈部保健操》。希望引起学校、家长、教育、卫生等对青少年颈椎病预防的重视     

基于QSPR 研究绿原酸类化合物与血清白蛋白的结合

本文选取32个小分子化学成分和9个天然产物化学成分为训练集,利用Dragon软件计算分子描述符,应用WEKA软件中CfsSubsetEval评价方法和BestFirst-D1-N5搜索方法进一步筛选描述符,利用Linear Regression方法建立了分子结构与其血清蛋白结合常数值logK的定量结构-性质相关性模型(相关系数为0.9557)。应用该模型对10个绿原酸类化合物的logK进行预测,结果显示绿原酸的logK预测值为4.51,与文献报道的logK值在4~7范围内基本相符。研究结果为进一步探讨绿原酸与血清蛋白的结合情况提供指导,为研究药物与血清蛋白的结合提供思路。     

鼻咽癌肝肺转移的放疗加中药治疗探讨

目的 :观察放疗加中药治疗鼻咽癌肝肺转移的疗效。方法 :90例患者随机分成对照组 45例和治疗组 45例。治疗组采用放疗加中药法 ,对照组采用单纯放疗法。结果 :治疗组鼻咽癌肝肺转移有效率为 82 .2 % ,肝转移的平均生存期12 .0 5月 ,肺转移为 14 .2 6月 ,肝肺均转移为 5 .96月。对照组有效率为 5 7.8% ,肝转移的平均生存期 8.38月 ,肺转移为 9.30月 ,肝肺均转移为 5 .5 3月。结论 :对鼻咽癌肝肺转移的放疗配合应用中药治疗能更好缓解症状 ,控制肿瘤 ,减轻反应 ,延长患者生存期。     

脑卒中继发癫痫的临床研究

目的：对脑卒中继发癫痫的临床研究情况进行调查与分析,从而为今后的临床治疗工作提供可靠的参考.方法：随机抽取在2006年1月至2011年12月这段时间里我院收治的以及文献报道的脑卒中继发癫痫的患者病例共42例,对这42例患者的临床治疗资料进行回顾性分析.结果：通过统计分析结果发现,在这42例患者中,早发型患有24例,在这4例患者中出血性脑卒中患者有17例,缺血性脑卒中患者7例;迟发型癫痫18例,在这18例患者中出血性脑卒中患者7例,缺血性脑卒中患者有11例.结论：出血性脑卒中患者发生早发型癫痫的可能性相对较大,而对于缺血性脑卒中患者则是偏向于迟发型癫痫.     

运动疗法在冠心病康复中运用的研究进展

<正>随着人们生活水平的提高,冠心病(CHD)的发病率和病死率呈上升趋势,给社会和家庭造成严重的经济负担。冠心病的治疗方法主要包括药物治疗、介入治疗、手术治疗、康复治疗等。其中运动疗法是心脏康复最经典、最主要的手段,自面世以来已有半个多世纪的历史,其内容、方案和作用已为临床所公认。我国现代心脏康复医学是从20世纪80年     

葛根素对油酸致大鼠急性肺损伤组织中核因子-κB表达的影响

摘 要 目的:观察核因子 κB（NF-κB）在油酸致大鼠急性肺损伤时肺组织中的表达变化,探讨葛根素对急性肺损伤的保护作用及其可能机制。方法: 24只大鼠随机分为3组：对照组（Control）、油酸组（OA）、葛根素预处理组（Pue）。Control组大鼠尾静脉注射生理盐水0.1 ml·kg^-1;OA组大鼠尾静脉注射油酸0.1 ml·kg^-1;Pue组大鼠在注射油酸前30 min腹腔注射葛根素30 mg·kg^-1。光镜下观察肺组织病理形态学改变,免疫组织化学染色技术观察NF-κB在肺组织中的表达变化。结果 Pue组较OA组肺组织损伤情况明显减轻。OA组肺组织NF-κB的阳性表达（0.39±0.07）与Conrtol组（0.12±0.04）相比显著增加（P<0.05）;应用葛根素后肺组织NF-κB的阳性表达（0.24±0.05）明显减少,但仍高于Conrtol组（P<0.05）。结论 葛根素可能通过抑制NF-κB的表达减轻急性肺损伤时肺组织的炎症反应。     

RP-HPLC法测定斑蝥素脂肪乳剂中斑蝥素的含量

目的　首次建立RP HPLC法测定斑蝥素脂肪乳剂中斑蝥素的含量。方法　采用C18柱 ,甲醇 水系统为流动相 ,梯度洗脱 ,紫外检测器 (检测波长为 2 2 7nm ,灵敏度为 0 0 0 5AUFS) ,对斑蝥素脂肪乳剂中斑蝥素进行含量测定。结果　样品处理简单 ,且能将斑蝥素与脂肪乳中的油脂、磷脂等主要杂质分离出来 ,斑蝥素在 2 0 8～ 31 2 μg·ml-1范围内峰面积与浓度线性关系良好 (r=0 994 ) ,最低可定量浓度为 1 0 4 μg·ml-1,样品回收率为 94 8%以上 ,进样精密度为 1 0 2 % (n =5 )。结论　该法测定脂肪乳样品分离效果好 ,回收率高 ,可作为斑蝥素脂肪乳剂质量控制方法。