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Synthesis and anticancer activity containing benzyl piperidone study of curcumin-related compounds

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Journal of Chinese Pharmaceutical Sciences 2015年第8期24卷 524-529页

作者： Daiying Zhou suqing zhao Xi Zheng Zhiyun Du Kun Zhang Guangdong Food and Drug Vocational College Guangzhou 510520 China Guangdong University of Technology Guangzhou 510006 China

Sixteen curcumin-related compounds containing benzyl piperidone were synthesized and evaluated for their anticancer activity by the MTT assay towards cultured prostate cancer （PC-3）, pancreatic cancer （BxPC-3）, colon cancer （HT-29）, and lung cancer （H1299） cells. Compounds A1 and B3 exhibited potent growth inhibitory effects against these cells in culture. The IC50 values of these compounds were lower than 1 μM in all four cell lines.

关键词： Curcumin-related compounds Synthesis Anticancer activity

Comprehensive chemical profiling and quantitative analysis of ethnic Yi medicine Miao-Fu-Zhi-Tong granules using UHPLC-MS/MS

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Chinese Journal of Natural Medicines 2023年第3期21卷 214-225页

作者： LEI Xiaoying ZHANG Chen zhao suqing CHENG Shuohan ZHOU Wenbin XU Jiapeng ZHAN Ping ZEPER Abliz School of Pharmacy Minzu University of ChinaBeijing 100081China Key Laboratory of Mass Spectrometry Imaging and Metabolomics Minzu University of ChinaNational Ethnic Affairs CommissionBeijing 100081China Key Laboratory of Ethnomedicine of Ministry of Education Minzu University of ChinaBeijing 100081China Traditional Chinese Medicine Hospital of Chuxiong Yi Autonomous Prefecture(Traditional Yi Medicine Hospital of Yunnan Province) Chuxiong 675000China

Developing analytical methods for the chemical components of natural medicines remains a challenge due to its diversity and ***-Fu-Zhi-Tong(MFZT)granules,an ethnic Yi herbal prescription,comprises 10 herbs and has been clinically applied for gouty arthritis(GA)***,a series of chemical profiling strategies including in-house library matching,molecular networking and MS/MS fragmentation behavior validation based on ultra-high performance liquid chromatography-tandem mass spectrometry(UHPLC-MS/MS)were developed for qualitative analysis of MFZT granules.A total of 207 compounds were identified or characterized in which several rare guanidines were discovered and profiled into alkyl substituted or cyclic ***,network pharmacology analysis indicated that MFZT’s anti-gout mechanism was mostly associated with the nuclear factor kappa-B(NF-κB)signaling,nucleotide oligomerization domain(NOD)-like signaling and rheumatoid arthritis pathways,along with the synergistic effect of 84 potential active *** addition,a quantitative analytical method was developed to simultaneously determine the 29 potential effective *** them,berberine,pellodendrine,3-feruloylquinic acid,neoastilbin,isoacteoside and chlorogenic acid derivatives at higher concentrations were considered as the chemical markers for quality *** findings provide a holistic chemical basis for MFZT granules and will support the development of effective analytical methods for the herbal formulas of natural medicines.

关键词： Natural medicines Miao-Fu-Zhi-Tong granules Chemical profiling Quantitative analysis Network pharmacology

Quantification of soluble epoxide hydrolase inhibitors in experimental and clinical samples using the nanobody-based ELISA

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Journal of Pharmaceutical Analysis 2023年第9期13卷 1013-1023页

作者： Huiyi Yang Meng Qi Qiyi He Sung Hee Hwang Jun Yang Mark McCoy Christophe Morisseau suqing zhao Bruce D.Hammock Department of Pharmaceutical Engineering School of Biomedical and Pharmaceutical SciencesGuangdong University of TechnologyGuangzhouChina Department of Entomology and Nematology and UCD Comprehensive Cancer Center University of CaliforniaDavisCA 95616USA Langfang Normal University LangfangHebei065000China

To ensure proper dosage of a drug,analytical quantification of it in biofluid is *** chromatography mass spectrometry(LC-MS)is the conventional method of choice as it permits accurate identification and ***,it requires expensive instrumentation and is not appropriate for bedside *** soluble epoxide hydrolase(sEH)inhibitors(EC5026 and TPPU)as examples,we report development of a nanobody-based enzyme-linked immunosorbent assay(ELISA)for such small molecules and its use to accurately quantify the drug chemicals in human *** optimized conditions,two nanobody-based ELISAs were successfully established for EC5026 and TPPU with low limits of detection of 0.085 ng/mL and 0.31 ng/mL,respectively,and two order of magnitude linear ranges with high precision and *** assay was designed to detect parent and two biologically active metabolites in the investigation of a new drug candidate *** addition,the ELISAs displayed excellent correlation with LC-MS analysis and evaluation of inhibitory *** results indicate that nanobody-based ELISA methods can efficiently analyze drug like *** methods could be easily implemented by the bedside,in the field in remote areas or in veterinary *** work illustrates that nanobody based assays offer alternative and supplementary analytical tools to mass spectrometry for monitoring small molecule medicines during clinical development and *** of nanobody based pharmaceutical assays are discussed.

关键词： Nanobody Immunoassay Soluble epoxide hydrolase inhibitors Metabolites Small molecules

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制药工程专业导论课程的教学探索与实践

高等药学教育研究 2024年第1期 21-26页

作者：郑俊霞赵肃清卢宇靖叶金星丁金龙广东工业大学生物医药学院广东广州510006

制药工程专业导论是面向制药工程专业新生的第一门专业基础课,是后继专业课的先导课程,对加深学生的专业认知度、培养学生对专业学习的兴趣及主动性具有重要意义。文章以广东工业大学制药工程专业为例,探讨了专业导论课程的重要性,并对... 详细信息

制药工程专业导论是面向制药工程专业新生的第一门专业基础课,是后继专业课的先导课程,对加深学生的专业认知度、培养学生对专业学习的兴趣及主动性具有重要意义。文章以广东工业大学制药工程专业为例,探讨了专业导论课程的重要性,并对课程的教学内容、教学方法以及考核方式进行了探索和实践,旨在更好地提高制药专业导论的教学效果,从而达到课程的教学目标。

关键词：制药工程专业导论教学探索与实践教学内容教学方法考核方式

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GPC3蛋白结构的分析及其表达纯化

分子诊断与治疗杂志 2024年第4期16卷 751-755页

作者：梁锦慧苏静怡龚鑫邱伟鹏崔锡平赵肃清广东工业大学生物医药学院广东广州510006

目的了解GPC3蛋白结构,构建GPC3蛋白的原核表达纯化系统,高效表达和纯化出GPC3蛋白。方法从GenBank中获取基因序列,通过Protparam、SOPMA、SWISS-MODEL等在线软件对GPC3蛋白(25-554 aa)的结构进行分析。从不同载体和菌株中筛选出相对优... 详细信息

目的了解GPC3蛋白结构,构建GPC3蛋白的原核表达纯化系统,高效表达和纯化出GPC3蛋白。方法从GenBank中获取基因序列,通过Protparam、SOPMA、SWISS-MODEL等在线软件对GPC3蛋白(25-554 aa)的结构进行分析。从不同载体和菌株中筛选出相对优势的组合,优化其表达条件,并诱导表达TrxA-GPC3融合蛋白,通过包涵体的溶解和复性、亲和层析、标签切割和分子筛纯化等方法分离纯化出无TrxA标签的GPC3蛋白。结果GPC3蛋白的相对分子质量为60.26 kDa,等电点为5.76,不稳定系数为41.27,脂肪系数为83.66,平均亲水系数为-0.312,是不稳定的亲水性蛋白,其主要为α-螺旋和无规则卷曲结构,引入标签的TrxA-GPC3融合蛋白比GPC3蛋白更稳定。通过对比筛选出表达效率较高的BL21(DE3)-pET32a-GPC3工程菌,其在0.5%的葡萄糖浓度和0.1 mmol/L的IPTG浓度条件下,结合20℃的诱导温度及16 h的诱导时间,可显著提高蛋白表达量,通过亲和层析得到纯度90%以上的TrxA-GPC3融合蛋白,利用凝血酶将TrxA标签切除,最后通过分子筛纯化得到单一的GPC3蛋白。结论利用生物信息学分析了GPC3蛋白的理化性质和结构,并在原核系统中成功表达和纯化了GPC3蛋白,为高特异性抗体的制备或筛选以及结构-功能研究奠定了基础,同时也为其它蛋白的表达纯化提供科学的指导意义。

关键词：肝细胞癌 GPC3蛋白生物信息学亲和层析

Comprehensive chemical profiling and quantitative analysis of ethnic Yimedicine Miao-Fu-Zhi-Tong granules using UHPLC-MS/MS

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Chinese Journal of Natural Medicines 2023年第3期 214-225页

作者： LEI Xiaoying ZHANG Chen zhao suqing CHENG Shuohan ZHOU Wenbin XU Jiapeng ZHAN Ping ZEPER Abliz School of Pharmacy Minzu University of China Key Laboratory of Mass Spectrometry Imaging and Metabolomics Minzu University of ChinaNational Ethnic Affairs Commission Key Laboratory of Ethnomedicine of Ministry of Education Minzu University of China Traditional Chinese Medicine Hospital of Chuxiong Yi Autonomous Prefecture (Traditional Yi Medicine Hospital of Yunnan Province)

Developing analytical methods for the chemical components of natural medicines remains a challenge due to its diversity and complexity. Miao-Fu-Zhi-Tong(MFZT) granules, an ethnic Yi herbal prescription, comprises 10 herbs and has been clinically applied for gouty arthritis(GA) therapy. Herein, a series of chemical profiling strategies including in-house library matching, molecular networking and MS/MS fragmentation behavior validation based on ultra-high performance liquid chromatography-tandem mass spectrometry(UHPLC-MS/MS) were developed for qualitative analysis of MFZT granules. A total of 207 compounds were identified or characterized in which several rare guanidines were discovered and profiled into alkyl substituted or cyclic ***, network pharmacology analysis indicated that MFZT's anti-gout mechanism was mostly associated with the nuclear factor kappa-B(NF-κB) signaling, nucleotide oligomerization domain(NOD)-like signaling and rheumatoid arthritis pathways, along with the synergistic effect of 84 potential active compounds. In addition, a quantitative analytical method was developed to simultaneously determine the 29 potential effective components. Among them, berberine, pellodendrine, 3-feruloylquinic acid, neoastilbin, isoacteoside and chlorogenic acid derivatives at higher concentrations were considered as the chemical markers for quality control. These findings provide a holistic chemical basis for MFZT granules and will support the development of effective analytical methods for the herbal formulas of natural medicines.

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化工建筑设备用的微孔保温毯性能测定及应用

陶瓷学报 2013年第2期34卷 210-214页

作者：赵素青东北师范大学吉林长春130024

化工建筑设备用的微孔保温毯对产品有着重要影响。新开发出一种新型微孔保温毯，主要成份为SiO2，MgO和SiC，粒子直径为10—35nm，粒子之间的空隙能够形成一个纳米级的半封闭的热对流场所，可以有效抵消热对流方式导致的热能损失。对该... 详细信息

化工建筑设备用的微孔保温毯对产品有着重要影响。新开发出一种新型微孔保温毯，主要成份为SiO2，MgO和SiC，粒子直径为10—35nm，粒子之间的空隙能够形成一个纳米级的半封闭的热对流场所，可以有效抵消热对流方式导致的热能损失。对该新型微孔保温毯的导热系数进行了测试，并且与之前一直使用的普通硅酸铝陶瓷纤维毯的保温性能进行了对比测试，在相同的温度下，新型微孔保温毯的导热系数明显低于普通陶瓷纤维毯，显示出更加优良的阻热性能。然后将两种保温材料应用于砖砌高温窑炉的内层保温铺敷，以期得到实际应用下的保温性能对比。由系统计算的最优保温厚度和冷面温度分别为40ram和49℃，仅为原有普通陶瓷纤维棉厚度的一半，而冷面温度却可以降低12℃，并且全年问可减少37％的热能损失。

关键词：微孔保温化工建筑设备导热系数保温厚度应用

硫脲修饰Cd掺杂ZnO水溶性量子点的制备及表征

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化学学报 2011年第7期69卷 777-782页

作者：赵斌赵肃清张焜刘端苏娟广东工业大学轻工化工学院广东511400

在非水稀溶液中以聚乙烯吡咯烷酮K-30为稳定剂,硫脲为表面修饰剂,制备Cd掺杂ZnO水溶性量子点荧光体;同时研究了基质的优化及硫脲含量对ZnO量子点发光性能的影响,Eu和Li的共掺杂对ZnO:Cd量子点发光性能的影响.采用紫外光谱、荧光发射光... 详细信息

在非水稀溶液中以聚乙烯吡咯烷酮K-30为稳定剂,硫脲为表面修饰剂,制备Cd掺杂ZnO水溶性量子点荧光体;同时研究了基质的优化及硫脲含量对ZnO量子点发光性能的影响,Eu和Li的共掺杂对ZnO:Cd量子点发光性能的影响.采用紫外光谱、荧光发射光谱、红外光谱和透射电镜、XRD对样品进行表征.结果表明:经Cd优化基质后、Eu和Li的共掺杂使量子点荧光强度明显增强;硫脲修饰后纳米颗粒分布更加均匀、晶粒更小、荧光光谱蓝移、量子点产率增加;该样品XRD衍射峰是馒头峰,属于无定形态;红外光谱图中因硫脲引起的NH2和C—NH2伸缩振动吸收峰分别为3189.0,1088.2 cm-1,硫脲修饰的最佳浓度大约为32 mg/mL.该量子点制备方法简单易行,具有较好的稳定性及高荧光量子效率,为进一步应用于生物标记奠定基础.

关键词： ZnO Cd掺杂硫脲修饰荧光强度光谱蓝移

4种邻苯二甲酸酯塑化剂人工抗原的合成及免疫检测

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食品科学 2016年第5期37卷 114-120页

作者：赖丹郑盛武赵肃清广东工业大学轻工化工学院广东广州510006

以4-硝基邻苯二甲酸为原料,衍生合成4种结构类似物,并分别通过重氮化法和活泼酯法与载体蛋白牛血清白蛋白(bovine serum albumin,BSA)和卵清白蛋白(ovalbumin,OVA)偶联制得人工抗原。利用紫外光谱扫描和十二烷基硫酸钠-聚丙烯酰胺凝胶电... 详细信息

以4-硝基邻苯二甲酸为原料,衍生合成4种结构类似物,并分别通过重氮化法和活泼酯法与载体蛋白牛血清白蛋白(bovine serum albumin,BSA)和卵清白蛋白(ovalbumin,OVA)偶联制得人工抗原。利用紫外光谱扫描和十二烷基硫酸钠-聚丙烯酰胺凝胶电泳(sodium dodecyl sulfate-polyacrylamide gel electroporesis,SDS-PAGE)检测鉴定人工抗原,并用4种与BSA偶联的人工抗原作免疫原免疫新西兰大白兔。利用酶联免疫吸附实验(enzymelinked immunosorbent assay,ELISA)检测抗体灵敏度和特异性。经紫外光谱和SDS-PAGE证实人工抗原偶联成功,经免疫分析法检测抗体效价,4-氨基邻苯二甲酸二丁酯-BSA(dibutyl 4-aminophthalate-BSA,DBAP-BSA)抗体效价达到1∶64 000,4-戊二单酰邻苯二甲酸二丁酯-BSA(dibutyl 4-carboxylphthalte-BSA,DBCP-BSA)、4-氨基邻苯二甲酸二异丁酯-BSA(diisobutyl 4-aminophthalate-BSA,Di BAP-BSA)和4-氨基邻苯二甲酸二环己酯-BSA(dicyclohexyl 4-aminophthalate-BSA,DCHAP-BSA)抗体效价均达到1∶128 000。DBAP-BSA、DBCP-BSA、Di BAP-BSA和DCHAP-BSA分别对邻苯二甲酸二丁酯(dibutyl phthalate,DBP)、DBP、邻苯二甲酸二异丁酯(diisobutyl phthalate,Di BP)和邻苯二甲酸二环己酯(dicyclohexyl phthalate,DCHP)4种抗体的IC50值为0.305、0.268、0.104、0.247μg/m L。四者之间交叉反应率低,反应特异性较好。

关键词：邻苯二甲酸酯人工抗原抗体