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Azocalixarenes: a scaffold of universal excipients with high efficiency

Science China Chemistry 2024年第5期67卷 1697-1706页

作者： Yu-Xin Yue Yi-Lin Lin Meng-Meng Chen han-wen Tian Rong Ma Ze-han Wang Fang-Yuan Chen Yu-Chen Pan Dong-Sheng Guo College of Chemistry State Key Laboratory of Elemento-Organic ChemistryKey Laboratory of Functional Polymer Materials(Ministry of Education)Frontiers Science Center for New Organic MatterCollaborative Innovation Center of Chemical Science and Engineering(Tianjin)Nankai UniversityTianjin 300071China

Excipients are important components of pharmaceutical preparations that affect their quality, safety, and efficacy. Macrocyclic receptors are a family of supramolecular excipients with several advantages, including molecular-level protection, small sizes,fast kinetics of host-guest recognition, and modular construction. With the continuous advances in the medical field, personalized and precision medicine requires the development of excipients with low dosages, integrated modifying effects, universality,and controlled release. To meet these requirements, we have developed a new family of macrocyclic excipients based on calixarenes by integrating their covalent(broad chemical design space) and noncovalent(wide range of substrates) ***, azocalixarenes(Azo CAs) were designed, showing high binding affinities to a broad spectrum of active pharmaceutical ingredients(APIs), selectivity to interferents, and responsiveness to hypoxic microenvironments. Due to their highly efficient and controllable recognition, Azo CAs serve as low-dose excipients for 30 APIs. Molecular encapsulation by Azo CAs results in the integrated modification of the physicochemical properties of APIs, including solubility, stability, bioavailability,and biocompatibility. Moreover, Azo CAs can be reduced by azoreductases overexpressed in hypoxic microenvironments,leading to the controlled release of APIs. Collectively, Azo CA excipients have broad application prospects for a series of diseases such as enteritis, arthritis, stroke, cancer, bacterial infection and kidney injury, with diverse therapeutic modalities,including chemotherapy, photodynamic therapy, photothermal therapy, immunotherapy, boron neutron capture therapy, radiotherapy, fluorescence imaging, and their combinations.

关键词： supramolecular chemistry host-guest systems excipient calixarene molecular recognition

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Calcium/calcimimetic via calcium-sensing receptor ameliorates cholera toxin-induced secretory diarrhea in mice

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World Journal of Gastroenterology 2024年第3期30卷 268-279页

作者： Lie-Qi Tang Johnathan Fraebel Shi Jin Steven P Winesett Jane Harrell wen-han Chang Sam Xianjun Cheng Department of Pediatrics University of FloridaGainesvilleFL 32610United States College of Medicine University of FloridaGainesvilleFL 32610United States Applied Physiology and Kinesiology University of FloridaGainesvilleFL 32610United States Brain Rehabilitation Research Center Malcom Randall VA Medical CenterGainesvilleFL 32610United States Department of Medicine Endocrine Research UnitVeterans Affairs Medical CenterUniversity of CaliforniaSan FranciscoSan FranciscoCA 94121United States Department of Pediatric Gastroenterology Hepatologyand NutritionUniversity of Florida Shands Children’s HospitalGainesvilleFL 32608United States

BACKGROUND Enterotoxins produce diarrhea through direct epithelial action and indirectly by activating the enteric nervous ***-sensing receptor(CaSR)inhibits both *** latter has been well documented in vitro but not in *** hypothesis to be tested was that activating CaSR inhibits diarrhea in *** To determine whether CaSR agonists ameliorate secretory diarrhea evoked by cholera toxin(CTX)in *** CTX was given orally to C57BL/6 mice to induce *** and calci-mimetic R568 were used to activate *** maximize their local intestinal actions,calcium was administered luminally via oral rehydration solution(ORS),whereas R568 was applied serosally using an intraperitoneal *** verify that their actions resulted from the intestine,effects were also examined on Cre-lox intestine-specific CaSR *** outcome was measured biochemically by monitoring changes in fecal Cl-or clinically by assessing stool consistency and weight *** CTX induced secretory diarrhea,as evidenced by increases in fecal Cl-,stool consistency,and weight loss following CTX exposure,but did not alter CaSR,neither in content nor in ***,calcium and R568 were each able to ameliorate diarrhea when applied to diseased *** CaSR involvement is suggested by gene knockout experiments where the anti-diarrheal actions of R568 were lost in intestinal epithelial CaSR knockouts(villinCre/Casrflox/flox)and neuronal CaSR knockouts(nestinCre/Casrflox/flox).CONCLUSION Treatment of acute secretory diarrheas remains a global *** advances in diarrhea research,few have been made in the realm of diarrhea *** therapy has remained the standard of care,although it does not halt the losses of intestinal fluid and ions caused by *** is no cost-effective therapeutic for *** and other studies suggest that adding calcium to ORS or using calcimimetics to activate intestinal CaSR might

关键词： Cholera Enteric nervous system Secretory diarrhea Oral rehydration solution Calcium-sensing receptor Gene knockout

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带有整体单极的Reissner-Nordstrom-AdS黑洞在扩展相空间中的霍金辐射

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物理学报 2024年第2期73卷 104-111页

作者：韩亦文胡成洪云重庆工商大学物理系重庆400067 成都东软学院基础教学学院成都611844

本文研究了带有整体单极的Reissner-Nordstrom-AdS黑洞在扩展相空间中出射粒子的量子隧穿辐射过程.其中,将宇宙学参数视为动态变量而不同于之前研究工作中将其视为常数而忽略其贡献.具体地,在计算出射粒子隧穿率时将宇宙学参数引入计算... 详细信息

本文研究了带有整体单极的Reissner-Nordstrom-AdS黑洞在扩展相空间中出射粒子的量子隧穿辐射过程.其中,将宇宙学参数视为动态变量而不同于之前研究工作中将其视为常数而忽略其贡献.具体地,在计算出射粒子隧穿率时将宇宙学参数引入计算并将其解释为热力学压强.计算结果表明,出射粒子的隧穿率与粒子出射前后黑洞的贝肯斯坦-霍金熵差成正比,辐射谱偏离了纯热谱,该结果与将宇宙学参数视为常数的情况完全相同.这意味着在扩展相空间中可以得到粒子的隧穿概率,并且隧穿过程不依赖于热力学状参量,这一工作自然地进一步将霍金辐射推广到了带有整体单极Reissner-Nordstrom-AdS黑洞扩展相空间中.结果表明,整体单极子尽管影响粒子的动力学行为和热力学量,但并不影响熵变和隧穿率.

关键词：霍金辐射宇宙学参数热力学压强整体单级

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从目的论视角看梅亚苏对海德格尔的批判

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哲学研究 2024年第3期 92-101,125页

作者：文晗湖南大学岳麓书院

自黑格尔以来,目的论式的哲学体系似乎已成为了历史的遗迹。然而,有趣的是,我们在海德格尔的《存在与时间》中,可以发现海德格尔围绕此在的实际性生存建构起了一种目的论式的意义世界。但同时,这一围绕此在的目的论世界如海德格尔所言,... 详细信息

自黑格尔以来,目的论式的哲学体系似乎已成为了历史的遗迹。然而,有趣的是,我们在海德格尔的《存在与时间》中,可以发现海德格尔围绕此在的实际性生存建构起了一种目的论式的意义世界。但同时,这一围绕此在的目的论世界如海德格尔所言,又时时遭受着偶然性的事实性世界的冲击。这样一种事实性对实际性的冲击在此后的法国哲学之中成为了哲学家们讨论的主题,当代著名的法国哲学家梅亚苏,在其代表作《有限性之后》中就接续了海德格尔的主题,将这种事实性的原理发扬光大。由此,我们也能从中看到目的论哲学在当代的命运。

关键词：目的论实际性事实性无根据非理由律

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Investigating the relationship between intracranial atherosclerotic plaque remodelling and diabetes using high-resolution vessel wall imaging

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World Journal of Diabetes 2024年第1期15卷 72-80页

作者： Yong-Qian Mo Hai-Yu Luo han-wen Zhang Yu-Feng Liu Kan Deng Xiao-Lei Liu Biao Huang Fan Lin Department of Radiology Peking University Shenzhen HospitalShenzhen 518000Guangdong ProvinceChina Department of Ultrasound Peking University Shenzhen HospitalShenzhen 518000Guangdong ProvinceChina The Second School of Clinical Medicine Southern Medical UniversityGuangzhou 510282Guangdong ProvinceChina Department of Radiology The First Affiliated Hospital of Shenzhen UniversityHealth Science CenterShenzhen Second People’s HospitalShenzhen 518036Guangdong ProvinceChina Research Department Philips HealthcareGuangzhou 518000Guangdong ProvinceChina Department of Radiology Guangdong Provincial People’s HospitalGuangdong Academy of Medical SciencesGuangzhou 510000Guangdong ProvinceChina

BACKGROUND Intracranial atherosclerosis,a leading cause of stroke,involves arterial plaque *** study explores the link between plaque remodelling patterns and diabetes using high-resolution vessel wall imaging(HR-VWI).AIM To investigate the factors of intracranial atherosclerotic remodelling patterns and the relationship between intracranial atherosclerotic remodelling and diabetes mellitus using *** Ninety-four patients diagnosed with middle cerebral artery or basilar artery INTRODUCTION Intracranial atherosclerotic disease is one of the main causes of ischaemic stroke in the world,accounting for approx-imately 10%of transient ischaemic attacks and 30%-50%of ischaemic strokes[1].It is the most common factor among Asian people[2].The adaptive changes in the structure and function of blood vessels that can adapt to changes in the internal and external environment are called vascular remodelling,which is a common and important pathological mechanism in atherosclerotic diseases,and the remodelling mode of atherosclerotic plaques is closely related to the occurrence of *** remodelling(PR)is an outwards compensatory remodelling where the arterial wall grows outwards in an attempt to maintain a constant lumen *** a long time,it was believed that the degree of stenosis can accurately reflect the risk of ischaemic stroke[3-5].Previous studies have revealed that lesions without significant luminal stenosis can also lead to acute events[6,7],as summarized in a recent meta-analysis study in which approximately 50%of acute/subacute ischaemic events were due to this type of lesion[6].Research[8,9]has pointed out that the PR of plaques is more dangerous and more likely to cause acute ischaemic *** studies[10-13]have found that there are specific vascular remodelling phenomena in the coronary and carotid arteries of diabetic ***,due to the deep location and small lumen of intracranial arteries and limitations of i

关键词： High-resolution vessel wall imaging Intracranial atherosclerosis Vascular remodelling Magnetic resonance imaging

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中国传统“道-艺”观论要

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求是学刊 2024年第4期51卷 148-158页

作者：韩文革武汉理工大学学报社科版编辑部武汉430063

中国传统“道-艺”观对中国艺术创造产生了深远的影响,在“道-艺”二元结构中去认识和处理艺术问题,充分彰显出中国古代文艺理论的民族性。中国传统“道-艺”观既丰富又立体,其中,“道器”论是对本体(本原之道)与实在(艺术之象)之隐显... 详细信息

中国传统“道-艺”观对中国艺术创造产生了深远的影响,在“道-艺”二元结构中去认识和处理艺术问题,充分彰显出中国古代文艺理论的民族性。中国传统“道-艺”观既丰富又立体,其中,“道器”论是对本体(本原之道)与实在(艺术之象)之隐显关系的总体归纳;“道贯”论是对艺术创造中“一”与“多”关系的辩证提摄;“载道”论确立了中国古代艺术社会学“道主而艺从”的文艺认知格局;“同道”论主要涉及文化原型和艺术同构内秘之诠解;“乐道”论表征着中国古代艺术对审美境界与人生境界之合一的高度提倡。全面了解中国传统“道-艺”观,对我们认识和理解中国艺术的生命意识、宇宙意识和超越意识具有重要意义。

关键词：中国古代艺术 “道-艺”观民族性

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教育政策研究中的反身性主题分析:价值、策略与示例

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黑龙江高教研究 2024年第4期42卷 9-14页

作者：张瀚文香港大学中国香港999077

作为揭示数据内容的主要方法,主题分析被广泛用于解释质性数据。由于研究范式的差异,不同主题分析方法处理数据的方式也不尽相同。这造成了质性方法的错误标记和不当使用,可能导致政策建议失当。以概念化大学生借款人债务经历的质性调... 详细信息

作为揭示数据内容的主要方法,主题分析被广泛用于解释质性数据。由于研究范式的差异,不同主题分析方法处理数据的方式也不尽相同。这造成了质性方法的错误标记和不当使用,可能导致政策建议失当。以概念化大学生借款人债务经历的质性调查为例,研究详述了反身性主题分析的六步骤流程,旨在厘清和消解适用反身性主题分析可能存在的混淆和误区,并为在教育政策研究中使用这种分析方法提供方向和技巧。反身性主题分析突出了研究者在知识生产中的积极参与:开放、有机的编码和主题生成过程是研究者对质性资料意义模式的主动诠释。对主题的深入解释更能把握公共问题的复杂性和多面性,这有助于教育决策科学化。

关键词：范式反身性主题分析助学贷款反身性主题分析

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Pien Tze Huang Inhibits Migration and Invasion of Hepatocellular Carcinoma Cells by Repressing PDGFRB/YAP/CCN2 Axis Activity

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Chinese Journal of Integrative Medicine 2024年第2期30卷 115-124页

作者： LUO Zhi-yi TIAN Qi CHENG Niang-mei LIU wen-han YANG Ye CHEN Wei ZhanG Xiang-zhi ZHENG Xiao-yuan CHEN Ming-sheng ZHUANG Qiu-yu ZHAO Bi-xing LIU Cong-sheng LIU Xiao-long LI Qin WANG Ying-chao The United Innovation of Mengchao Hepatobiliary Technology Key Laboratory of Fujian Province Mengchao Hepatobiliary Hospital of Fujian Medical UniversityFuzhou(350025)China Fujian Pien Tze Huang Enterprise Key Laboratory of Natural Medicine Research and Development Zhangzhou Pien Tze Huang Pharmaceutical Co.Ltd.ZhangzhouFujian Province(363099)China College of Biological Science and Engineering and Mengchao Med-X Center Fuzhou UniversityFuzhou(350116)China Department of Internal Medicine Mengchao Hepatobiliary Hospital of Fujian Medical UniversityFuzhou(350025)China

Objective:To investigate the effects of Pien Tze Huang(PZH) on the migration and invasion of HCC cells and underlying molecular ***:Cell counting kit-8(CCK-8) was applied to evaluate the cell viabilities of SMMC-7721,SK-Hep-1,C3A and HL-7702(6 × 10^(3)cells/well) co-incubated with different concentrations of PZH(0,0.2,0.4,0.6,0.8 mg/mL) for 24 ***,wound healing assay,CCK-8and Annexin V-FITC/PI staining were conducted to investigate the effects of PZH on the migration,invasion,proliferation and apoptosis of SK-Hep-1 and SMMC-7721 cells(650 μg/mL for SK-Hep-1 cells and 330 μg/mL for SMMC-7721 cells),*** vivo,lung metastasis mouse model constructed by tail vein injection of HCC cells was used for evaluating the anti-metastasis function of ***-Hep-1 cells(10^(6)cells/200 μL per mice) were injected into B-NDG mice via tail *** 8 mice were randomly divided into PZH and control groups,4 mice in each *** 2-d inoculation,mice in the PZH group were administered with PZH(250 mg/kg,daily) and mice in the control group received only vehicle(PBS) from the 2nd day after xenograft to day *** analysis based on RNA-seq was subsequently used for deciphering anti-tumor mechanism of *** real-time polymerase chain reaction(qRT-PCR) and Western blot were applied to verify RNA-seq *** reporter assay was performed to examine the transcriptional activity of yes-associated protein(YAP).Results:PZH treatment significantly inhibited the migration,invasion,proliferation and promoted the apoptosis of HCC cells in vitro and in vivo(P<0.01).Transcriptome analysis indicated that Hippo signaling pathway was associated with anti-metastasis function of *** study showed PZH significantly inhibited the expressions of platelet derived growth factor receptor beta(PDGFRB),YAP,connective tissue growth factor(CCN2),N-cadherin,vimentin and matrix metallopeptidase 2(MMP2,P<0.01).Meanwhile,the phosphorylatio

关键词： PienTzeHuang hepatocellular carcinoma RNA-seq Hippo yes-associated protein

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1.6-μm single-frequency erbium-doped fiber laser based on two cascaded subrings

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Chinese Optics Letters 2024年第4期22卷 77-82页

作者：翟雅琦文瀚陈浩伟陆宝乐白晋涛 State Key Laboratory of Energy Photon-Technology in Western China International Collaborative Center on Photoelectric Technology and Nano Functional MaterialsInstitute of Photonics&Photon-TechnologyNorthwest UniversityXi’an 710127China Shaanxi Engineering Technology Research Center for Solid State Lasers and Application Shaanxi Provincial Key Laboratory of Photo-electronic TechnologyNorthwest UniversityXi’an 710127China

We demonstrate a stable narrow linewidth single-frequency erbium-doped fiber laser(EDFL)operating at 1.6μm.A Fabry–Perot fiber Bragg grating and two cascaded subrings are incorporated in the main ring cavity to achieve singlefrequency *** experimentally measured optical signal-to-noise ratio is greater than 73 ***,the linewidth of the EDFL is measured to be about 480 Hz by the self-built short-delayed self-heterodyne interferometry *** laser shows superior stability,with no mode-hopping during the 60-min observation *** proposed EDFL provides a new experimental idea for realizing a single-frequency fiber laser in the L-band.

关键词： erbium-doped fiber laser two cascaded subrings single frequency

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自然暴露与盐雾加速环境下钢筋混凝土劣化规律及等效关系

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吉林大学学报（工学版） 2024年第2期54卷 494-505页

作者：冯琼田浩正乔宏霞念腾飞韩文文兰州理工大学土木工程学院兰州730050 兰州理工大学西部土木工程防灾减灾教育部工程研究中心兰州730050

针对西部盐渍土地区病害严重的问题,选取西部盐渍土地区典型环境开展钢筋混凝土自然暴露试验,同时模拟当地腐蚀环境设计室内盐雾干湿循环加速试验;采用钢筋腐蚀电流和混凝土损伤度表征钢筋混凝土内部钢筋及保护层的劣化规律;基于Weibul... 详细信息

针对西部盐渍土地区病害严重的问题,选取西部盐渍土地区典型环境开展钢筋混凝土自然暴露试验,同时模拟当地腐蚀环境设计室内盐雾干湿循环加速试验;采用钢筋腐蚀电流和混凝土损伤度表征钢筋混凝土内部钢筋及保护层的劣化规律;基于Weibull分布函数建立两种环境下钢筋混凝土的劣化模型,并进行竞争失效分析;利用可靠度等价条件,结合当量概念,建立两种环境下的等效关系。结果表明:钢筋混凝土在室内加速与自然暴露环境下的劣化规律相似,其规律均是强化效应和劣化效应相互作用的结果;Weibull分布函数可以有效地描述钢筋混凝土在室内加速与自然暴露环境下的性能劣化过程;内部钢筋劣化至中位寿命的时间略早于混凝土保护层;室内盐雾干湿循环加速劣化钢筋混凝土1 d可模拟盐渍土地区自然暴露劣化12.7 d。

关键词：土木工程材料钢筋混凝土西部盐渍土地区腐蚀劣化 Weibull分布函数等效关系

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