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991.
992.
Jun Soo Park Jeong Soo Kim Myoung Jin Ho Dong Woo Park Eun A. Kim Yong Seok Choi Sun Woo Jang Myung Joo Kang 《Molecules (Basel, Switzerland)》2021,26(6)
The incorporation of permeation enhancers in topical preparations has been recognized as a simple and valuable approach to improve the penetration of antifungal agents into toenails. In this study, to improve the toenail delivery of efinaconazole (EFN), a triazole derivative for onychomycosis treatment, topical solutions containing different penetration enhancers were designed, and the permeation profiles were evaluated using bovine hoof models. In an in vitro permeation study in a Franz diffusion cell, hydroalcoholic solutions (HSs) containing lipophilic enhancers, particularly prepared with propylene glycol dicaprylocaprate (Labrafac PG), had 41% higher penetration than the HS base. Moreover, the combination of hydroxypropyl-β-cyclodextrin with Labrafac PG further facilitated the penetration of EFN across the hoof membrane. In addition, this novel topical solution prepared with both lipophilic and hydrophilic enhancers was physicochemically stable, with no drug degradation under ambient conditions (25 °C, for 10 months). Therefore, this HS system can be a promising tool for enhancing the toenail permeability and therapeutic efficacy of EFN. 相似文献
993.
Ying-Ji Xin Soojung Choi Kyung-Baeg Roh Eunae Cho Hyanggi Ji Jin Bae Weon Deokhoon Park Wan Kyunn Whang Eunsun Jung 《Molecules (Basel, Switzerland)》2021,26(2)
Bidens pilosa L. (Asteraceae) has been used historically in traditional Asian medicine and is known to have a variety of biological effects. However, the specific active compounds responsible for the individual pharmacological effects of Bidens pilosa L. (B. pilosa) extract have not yet been made clear. This study aimed to investigate the anti-inflammatory phytochemicals obtained from B. pilosa. We isolated a flavonoids-type phytochemical, isookanin, from B. pilosa through bioassay-guided fractionation based on its capacity to inhibit inflammation. Some of isookanin’s biological properties have been reported; however, the anti-inflammatory mechanism of isookanin has not yet been studied. In the present study, we evaluated the anti-inflammatory activities of isookanin using lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. We have shown that isookanin reduces the production of proinflammatory mediators (nitric oxide, prostaglandin E2) by inhibiting the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in LPS-stimulated macrophages. Isookanin also inhibited the expression of activator protein 1 (AP-1) and downregulated the LPS-induced phosphorylation of p38 mitogen-activated protein kinase (MAPK) and c-jun NH2-terminal kinase (JNK) in the MAPK signaling pathway. Additionally, isookanin inhibited proinflammatory cytokines (tumor necrosis factor-a (TNF-α), interleukin-6 (IL-6), interleukin-8 (IL-8), and interleukin-1β (IL-1β)) in LPS-induced THP-1 cells. These results demonstrate that isookanin could be a potential therapeutic candidate for inflammatory disease. 相似文献
994.
Fang Sheng Bangyan Hu Qiang Jin Jiangbo Wang Cuiyun Wu Zhengrong Luo 《Molecules (Basel, Switzerland)》2021,26(10)
Husk and pellicle as the agri-food waste in the walnut-product industry are in soaring demand because of their rich polyphenol content. This study investigated the differential compounds related to walnut polyphenol between husk and pellicle during fruit development stage. By using ultra-high performance liquid chromatography-quadrupole-orbitrap (UHPLC-Q-Orbitrap), a total of 110 bioactive components, including hydrolysable tannins, flavonoids, phenolic acids and quinones, were tentatively identified, 33 of which were different between husk and pellicle. The trend of dynamic content of 16 polyphenols was clarified during walnut development stage by high-performance liquid chromatography (HPLC). This is the first time to comprehensive identification of phenolic compounds in walnut husk and pellicle, and our results indicated that the pellicle is a rich resource of polyphenols. The dynamic trend of some polyphenols was consistent with total phenols. The comprehensive characterization of walnut polyphenol and quantification of main phenolic compounds will be beneficial for understanding the potential application value of walnut and for exploiting its metabolism pathway. 相似文献
995.
Kuang X.-Y. Jin S.-Q. Cao Y.-H. Zhang Y.-M. Dong S.-G. Zhu L.-H. Lin L.-W. Lin C.-J. 《电化学》2021,(6):624-636
The ordinary organic coatings on aluminum alloy usually encounter a problem of low adhesion to the substrate, which results in destruction and failure of the long-term protective performance of the anticorrosion systems. The surface modification of aluminum alloy is able to enhance the adhesion of organic coating on aluminum alloys, and to improve their protective performance. In this work, a combined surface modification of anodic oxidation and mussel adhesion protein/CeO2/3-aminopropyltriethoxysilane composite film (MCA) was developed on the aluminum alloy. The adhesion of modified polyurethane coated on the treated aluminum alloy and its corrosion protective performance were evaluated comprehensively by using contact angle, adhesion strength, electrochemical impedance spectroscopy (EIS), and scanning reference electrode technique (SRET). The measurements of EIS and SRET demonstrated that the MCA composite film on anodic oxidized Al possessed self-healing function and provided effective protection against early corrosion of aluminum alloy. The pull-off test showed that both anodic oxidation treatment and MCA composite film modification were able to increase the adhesion of modified polyurethane coating on aluminum alloy, and their combined action were supposed to remarkably enhance the adhesion strength up to 17.1 MPa. The reason for the improvement of adhesion was that the anodic oxidation treatment and MCA composite film modification could improve the surface roughness of aluminum alloy, and enhance the surface wettability and surface polarity, which is beneficent to enhance the bonding of the modified polyurethane coating to aluminum alloy surface. The EIS results showed that no any corrosion occurred for the modified polyurethane coating on the treated aluminum alloy during 65 d immersion in 3.5wt.% NaCl solution. The impedance value in low frequency range of the modified polyurethane coating always maintained at a high order of magnitude on the aluminum alloy treated by anodic oxidation and MCA composite film modification, showing an excellent protective performance of the coating system. The evaluation of Neutral Salt Spray (NSS) indicated that the modified polyurethane coating on the treated aluminum alloy owned superior corrosion protection performance, and the adhesion strength remained 13.1 MPa and no any corrosion was found at the scratch locations even after 1200 h of salt spray testing. It was concluded that combination of anodic oxidation and MCA composite film were capable of significantly improving the adhesion of modified polyurethane coating on aluminum alloy and providing long-term effective corrosion protection for aluminum alloy. © 2021 Authors. All rights reserved. 相似文献
996.
Shukun Wei Xiaoyou Hu Lingyu Du Linlin Zhao Hongjuan Xue Chaolun Liu James J. Chou Jin Zhong Yimin Tong Shuqing Wang Bo OuYang 《Molecules (Basel, Switzerland)》2021,26(5)
Hepatitis C Virus (HCV) is the key cause of chronic and severe liver diseases. The recent direct-acting antiviral agents have shown the clinical success on HCV-related diseases, but the rapid HCV mutations of the virus highlight the sustaining necessity to develop new drugs. p7, the viroporin protein from HCV, has been sought after as a potential anti-HCV drug target. Several classes of compounds, such as amantadine and rimantadine have been testified for p7 inhibition. However, the efficacies of these compounds are not high. Here, we screened some novel p7 inhibitors with amantadine scaffold for the inhibitor development. The dissociation constant (Kd) of 42 ARD-series compounds were determined by nuclear magnetic resonance (NMR) titrations. The efficacies of the two best inhibitors, ARD87 and ARD112, were further confirmed using viral production assay. The binding mode analysis and binding stability for the strongest inhibitor were deciphered by molecular dynamics (MD) simulation. These ARD-series compounds together with 49 previously published compounds were further analyzed by molecular docking. Key pharmacophores were identified among the structure-similar compounds. Our studies suggest that different functional groups are highly correlated with the efficacy for inhibiting p7 of HCV, in which hydrophobic interactions are the dominant forces for the inhibition potency. Our findings provide guiding principles for designing higher affinity inhibitors of p7 as potential anti-HCV drug candidates. 相似文献
997.
Wang Zi-Jian Yu Yong-Ji Zhai Rui-Zhi Chen Xin-Yu Wu Chun-Ting Jin Guang-Yong 《Journal of Russian Laser Research》2016,37(1):97-101
We report a narrow pulse width optical parametric oscillator based on periodically poled MgO:LiNbO3 (PPMgLN) with a high repetition rate under quasi-phase matched conditions. When the maximum pumping power of the 1,064-nm laser was 14.57 W, the acousto-optical (A-O) Q-switch repetition rate was 100 kHz, and the PPMgLN crystal grating period was 29.5 μm. A 1,474-nm signal light output power of 4.21 W and a 3,828 nm idler light output power of 1.547 W were obtained, corresponding to a pulse width of 9.52 ns and 9.65 ns, respectively. The overall optical–optical conversion efficiency was 39.5%. Additionally, by changing the temperature from 25°C to 150°C, a tunable signal wavelength of 1,474–1,499 nm and idler wavelength at 3,676–3,828 nm of the output laser were achieved. 相似文献
998.
空间推进所用的电子回旋共振离子源(ECRIS)应具有体积小、效率高的特点. 本文研究的ECRIS使用永磁体环产生磁场, 有效减小了体积, 该离子源利用微波在磁场中加热电子, 电子与中性气体发生电离碰撞产生等离子体. 磁场在微波加热电子的过程中起关键作用, 同时影响离子源内等离子体的约束和输运. 通过比较四种磁路结构离子源的离子电流引出特性来研究磁场对10 cm ECRIS性能的影响. 实验发现: 在使用氩气的条件下, 特定结构的离子源可引出160 mA的离子电流, 最高推进剂利用率达60%, 最小放电损耗为120 W·A-1; 所有离子源均存在多个工作状态, 工作状态在微波功率、气体流量、引出电压变化时会发生突变. 离子源发生状态突变时的微波功率、气体流量的大小与离子源内磁体的位置有关. 通过比较不同离子源的引出离子束流、放电损耗、气体利用率、工作稳定性的差异, 归纳了磁场结构对此种ECRIS引出特性的影响规律, 分析了其中的机理. 实验结果表明: 保持输入微波功率、气体流量、引出电压不变时, 增大共振区的范围、减小共振区到栅极的距离, 离子源能引出更大的离子电流; 减小共振区到微波功率入口、气体入口的距离能降低维持离子源高状态所需的最小微波功率和最小气体流量, 提高气体利用率, 但会导致放电损耗增大. 研究结果有助于深化对此类离子源工作过程的认识, 为其设计和性能优化提供参考. 相似文献
999.
本文根据统计理论分析了激光线宽对外差探测结果的影响, 并讨论了激光线宽对杨氏干涉条纹对比度的影响. 本文基于解析结果做了数值仿真, 所得结果表明激光线宽增加时, 外差探测方式仍可以检测到中频信号, 但在线宽较大时, 受噪声影响无法准确地提取到中频频率. 为验证理论分析结果, 使用线宽为1 MHz的激光光源进行了8.1 km外场实验, 实验结果与数值分析结论一致, 即不会因为线宽增加而无法检测到中频信号. 文中所得结论对于外差探测光源的选择有重要指导意义, 因此根据测量目标的特性和测量要求, 可按照文中结论评估光源的线宽指标. 相似文献
1000.
Jin FangZhou Chen HongWei Rong Xing Zhou Hui Shi MingJun Zhang Qi Ju ChenYong Cai YiFu Luo ShunLong Peng XinHua Du JiangFeng 《中国科学:物理学 力学 天文学(英文版)》2016,59(3):1-7
A triad mode resonance, or three-wave resonance, is typical of dynamical systems with quadratic nonlinearities. Suspended cables are found to be rich in triad mode resonant dynamics. In this paper, modulation equations for cable’s triad resonance are formulated by the multiple scale method. Dynamic conservative quantities, i.e., mode energy and Manley-Rowe relations, are then constructed. Equilibrium/dynamic solutions of the modulation equations are obtained, and full investigations into their stability and bifurcation characteristics are presented. Various bifurcation behaviors are detected in cable’s triad resonant responses, such as saddle-node, Hopf, pitchfork and period-doubling bifurcations. Nonlinear behaviors, like jump and saturation phenomena, are also found in cable’s responses. Based upon the bifurcation analysis, two interesting properties associated with activation of cable’s triad resonance are also proposed, i.e., energy barrier and directional dependence. The first gives the critical amplitude of high-frequency mode to activate cable’s triad resonance, and the second characterizes the degree of difficulty for activating cable’s triad resonance in two opposite directions, i.e., with positive or negative internal detuning parameter. 相似文献