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CoMFA Study on anti-proliferative activity of Fluoroquinolone Amide Derivatives

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Chinese Journal of Structural Chemistry 2022年第3期41卷 241-247,I0014页

作者： ENG Hui CAO Jing-Pei FENG Chang-Jun School of Chemical Engineering and Technology China University of Mining and TechnologyXuzhou 221116China Key Laboratory of Coal Processing and Efficient Utilization(Ministry of Education) Xuzhou 221116China School of Material&Chemical Engineering Xuzhou University of TechnologyXuzhou 221018China

The in vitro anti-proliferative activity(pICi,i=hp,ca,hl)of fluoroquinolone(rhodanineα,β-unsaturated ketone)amide compounds,referred to as“fluoroquinolone amide derivatives(FQADs)”towards Hep-3B,Capan-1 and HL60 cells,was studied by the 3D-QSAR method of comparative molecular field analysis(CoMFA).Based on the training set of 14 compounds,the prediction model was established,which was further verified by the test set of 5 compounds with template molecule *** is found that steric and electrostatic fields contribute 66.8%and 33.2%to pIChp,61.4%and 38.6%to pICca,and 61.5%and 38.5%to pIChl,*** Rcv 2(i.e,cross-validation coefficient)is 0.324,0.381,and 0.421 for pIChp,pICca,and pIChl,respectively,while the corresponding R2(i.e,non-cross-validation coefficient)all reach ***,the models were employed to estimate the activities of the training and test compounds,and the results show that the stability and predictability of developed models are very *** to the contour maps of steric and electronic fields,bulky groups linked to 2-,3-,4-positions of phenyl ring,and electropositive groups near the 4-position and electronegative groups far away may increase the anti-proliferative *** the information provided by the 3D contour maps,four new FQADs owing higher antiproliferative activity were designed,but their effectiveness should be further tested by experiments.

关键词： fluoroquinolone amide derivatives Hep-3B cell Capan-1cell HL60 cell anti-proliferative activity comparative molecular field analysis

anti-proliferative activity of cardiac glycosides isolated fromStreptocaulonjuventas:the relationships to chemical structures

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Anti-proliferative activity of cardiac glycosides isolated f...

Design,synthesis and anti-proliferative studies of a novel series of indirubin derivatives

第十一届全国博士生学术年会

作者：薛睿 Na Han Chun Ye 殷军 Development and Utilization Key Laboratory of Northeast Plant Materials School of Traditional Chinese MateriaMedicaShenyang Pharmaceutical University

The plants of Streptocaulon genus were proved to have potential anti-tumour activities in recent years,and the phytochemical studies indicated that the main chemical constituents of this genus were cardiac glycosides,triterpenoids,hemiterpenoids, phenylpropanoids,lignans,coumarins and *** a series of cardiac glycosides were isolated and identified from the active fraction of root ofStreptocaulonjuventas in our previous *** order to confirmwhether these cardiac glycosides were the active components,thecytotoxic activity of the 49 cardiac glycosides towardtwo cell lines, human lung A549 adenocarcinoma cell and normal human foetal lung fibroblast MRC-5 cell,were evaluated by MTT *** of tested compounds showed potent inhibitory effects towards both of the two cell lines,which were stronger than the positive control (cisplatin).Then the structure-activity relationships were discussed in detail,andit seemed that the structure-toxicity relationships of these compounds toward MRC-5 may be identical with that of A549 cell line,which indicated that these compounds may possess obvious cytotoxicity against normal human lung cell linesin *** results would lay a foundation for the further research on new drug development for anti-cancer.

关键词： cardiac glycosides Streptocaulonjuventas anti-proliferative activity A549 MRC-5

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Chinese Chemical Letters 2010年第12期21卷 1407-1410页

作者： Tian Cai Wang Ju Zhi Wei Chuan Sheng Guo Hui Bin Zhang Hou Xing Fan Center of Drug Discovery College of Pharmacy China Pharmaceutical University Nanjing 210009 China Shanghai Sun-sail Pharmaceutical Science & Technology Co. Ltd. Shanghai 201203 China

A series of novel derivatives of indirubin were synthesized and evaluated for their anti-proliferative activity against human cancer cell lines of SGC7901,A549,HL-60,SK-BR-3 and *** of the compounds displayed more potent activity than *** addition,the derivatives showed improved water solubility,which may be favorable to their pharmacokinetic performances.

关键词： anti-proliferative activity Indirubin Sunitinib

Construction of the Molecular Structure Model of the Zhaotong Lignite Using Simulation and Experiment Data

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Chinese Journal of Structural Chemistry 2022年第3期41卷 137-147,I0011页

作者： ZHANG Dian-Kai LI Yan-Hong CHANG Li-Ping ZI Chang-Yu ZHANG Yuan-Qin TIAN Guo-Cai ZHAO Wen-Bo Faculty of Chemical Engineering Kunming University of Science and TechnologyKunming 650500China Key Laboratory of Coal Science and Technology Taiyuan University of TechnologyMinistry of Education and Shanxi Province 030024China State Key Laboratory of Complex Nonferrous Metal Resources Clean Utilization Kunming University of Science and TechnologyKunming 650093China

Aiming to better understand the physiochemical properties of lignite, we select Zhaotong lignite as object and adopt simulation and experiment data to construct its molecular structure. Firstly, the important parameters including carbon skeleton, valence state and functional group of the sample are obtained by ultimate analysis, 13 C NMR, XPS and Py-GC/MS. Results indicate that the ratio of aromatic carbon and aromatic bridge carbon to surrounding carbon of the sample are 40.32% and 0.14, respectively. Such results imply that the aromatic structure of the sample is dominated by benzene and naphthalene. Moreover, the ratio of aliphatic carbon is 51.55%, and the aliphatic structure is mainly comprised by methyl, methylene, quaternary carbon and oxygen-aliphatic carbon. Oxygen atoms principally exist in ether, carbonyl and carboxyl groups, of which ether accounts for 70.2%. Additionally, the contents of pyridine, pyrrole and quaternary nitrogen are 25.2%, 46.3% and 13.0%, respectively. Based on the aforementioned results, the molecular structure model of Zhaotong lignite is constructed by the method of computer-aided molecular design. Subsequently, the molecular formula of Zhaotong lignite is calculated as C;H;O;N;. Finally, in order to verify the reasonability of the constructed model, the 13 C NMR of the molecular structure model is simulated by employing the basis set of GIAO/6-31G at the Gaussian 09 computing platform. These simulated results agree well with the experimental ones, which suggests that the molecular structure model of Zhaotong lignite is accurate and reasonable.

关键词： fluoroquinolone amide derivatives Hep-3B cell Capan-1cell HL60 cell anti-proliferative activity comparative molecular field analysis

Identification of novel bioactive proanthocyanidins with potent antioxidant and anti-proliferative activities from kiwifruit leaves

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Food Bioscience 2022年第2期46卷 539-549页

作者： Ji-Min Lv Mostafa Gouda Alaa El-Din Bekhit Ya-Ke He Xing-Qian Ye Jian-Chu Chen College of Biosystems Engineering and Food Science National-Local Joint Engineering Laboratory of Intelligent Food Technology and EquipmentZhejiang Key Laboratory for Agro-Food ProcessingZhejiang Engineering Laboratory of Food Technology and EquipmentZhejiang UniversityHangzhou310058China Department of Nutrition and Food Science National Research CentreDokki12622GizaEgypt Department of Food Science University of OtagoOtagoNew Zealand

Agro-wastes contribute major social,economic,and environmental challenges for food production and circular economy *** current increasing demand for clean label food production and use of natural bioactive compounds could turn these challenges into opportunities providing avenues for proper utilization of agro-wastes to produce valuable *** study aimed to investigate the potential use of kiwifruit(Actinidia chinensis)leaves as a source of proanthocyanidins(PAs)bioactive phenolic *** leaves PAs were extracted,purified,identified,and evaluated for their antioxidant and anti-proliferative *** structural composition of the purified PAs was characterized using HPLC-QTOF-MS/MS and *** results showed that purified kiwifruit leaves PAs(PKLPs)comprised mainly procyanidins,propelargonidins,and prodelphindins ranging from dimers to hexamers with(epi)catechin as terminal units and(epi)afzelechin or(epi)gallocatechin as dominant extension *** study reports the structure of novel PKLPs monomer fractions was unique compared to the PAs that extracted from the other plant *** PKLPs exhibited higher phenolic content than the skin and flesh of several kiwifruit ***,the PKLPs exhibited higher in vitro antioxidant activity in chemical-based(DPPH,ABTS,and FRAP)assays and H2O2-induced injury cell model than ascorbic,Trolox,and catechin(panti-proliferation activity(IC_(50)=186.04±2.61μg/mL)against HepG2 cells was *** conclusion,this study demonstrated that kiwifruit leaves waste could serve as a sustainable and low-cost source of PAs,a group of multi-functional bioactive compounds that plays a key role in the food and pharmaceutical industries.

关键词： Proanthocyanidins Agro-waste valorisation HPLC-QTOF-MS/MS antioxidant potential anti-proliferative activity

Synthesis and Characterization of Novel Azo-containing or Azoxy-containing Schiff Bases and Their antiproliferative and Cytotoxic Activities

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Chemical Research in Chinese Universities 2015年第1期31卷 60-64页

作者： SU Ran LU Lei ZHENG Songzhi JIN Yinghua AN Shengji College of Chemistry College of Life Science Jilin University Changchun 130012 P. R. China

A series of novel Schiff base derivatives was designed and synthesized from 3,3＇-azobenzaldehyde and 3,3＇-azoxybenzaldehyde. The newly synthesized compounds were characterized by FTIR, ^1H NMR, MS and elemental analysis and tested for their in vitro antiproliferative activities against HeLa cell lines. At the same time, the impact on the antitumor activity of the sulfanilamido, benzamido, phenolic hydroxyl or thiourea groups was investigated and discussed. Compounds 4, 6 and 10 were found to exhibit strong cytotoxic activity.

关键词： Schiffbase Azo Azoxy anti-proliferative activity Cytotoxic activity

Retinoic acid affects basic cellular processes and SOX2 and SOX18 expression in breast carcinoma cells

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BIOCELL 2021年第5期45卷 1355-1367页

作者： ISIDORA PETROVIC MILENA MILIVOJEVIC ANA ARSENIJEVIC ANDRIJANA LAZIC NATASA KOVACEVIC GRUJICIC MARIJA SCHWIRTLICH JELENA POPOVIC MILENA STEVANOVIC Institute of Molecular Genetics and Genetic Engineering University of BelgradeBelgradeSerbia Institute of Cell Biology School of Biological SciencesThe University of EdinburghEdinburghUK Department of Radiation Oncology Feinberg School of MedicineNorthwestern UniversityChicagoILUSA Faculty of Biology University of BelgradeBelgradeSerbia Serbian Academy of Sciences and Arts BelgradeSerbia

Genetic and molecular heterogeneity,together with intrinsic and acquired resistance to therapy,represent the major obstacles to the successful treatment of different types of breast *** evidence demonstrates that SOX transcription factors in breast carcinomas could act both as oncogenes and tumor suppressors and have been associated with tumor stage and grade,poor prognosis,and therapy *** SOX2 and SOX18 overexpression has been correlated with poor prognosis in breast carcinomas,and these genes are recognized as potential antitumor *** aim was to evaluate the effect of retinoic acid(RA),a well-known cyto-differentiating agent,on breast carcinoma cells in vitro and to investigate the potential of RA treatment to modify the expression of SOX2 and SOX18 *** applying various experimental approaches,we evaluated the effect of RA on basic cellular processes in SK-BR-3 and MCF7 breast carcinoma cell *** have shown that RA inhibits cell growth,reduces the number of Ki-67 positive cells,and causes cell-cycle *** effect was more prominent in SK-BR-3 cell line that lacks SOX2 expression,including a higher decrease in cell viability,reduction in colony formation,and significant remodeling of cellular *** have shown that RA treatment led to the downregulation of SOX2 expression in MCF7 cells and to the reduction of SOX18 expression in both cell *** functional analysis,we showed that the anti-proliferative effect of RA in both cell lines was not based on the activity of stemness marker SOX2,pointing to a SOX2-independent mechanism of *** ability of RA to reduce SOX2/SOX18 expression raises the possibility that these genes can be used as biomarkers to distinguish RA-responders from ***,our study shows that the response of breast carcinoma cell lines to RA treatment may vary,highlighting that the development of RA-based therapy should consider differences in breast carcinoma subtypes.

关键词： Breast carcinoma anti-proliferative activity Transcription factors MCF7 cell line SK-BR-3 cell line

SF3B1 modulators affect key genes in metastasis and drug influx: a new approach to fight pancreatic cancer chemoresistance

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Cancer Drug Resistance 2021年第4期4卷 904-922页

作者： Ornella Randazzo Stella M.Cascioferro Camilla Pecoraro Widad Ait Iddouch Amir Avan Barbara Parrino Daniela Carbone Ugo Perricone Godefridus J.Peters Patrizia Diana Elisa Giovannetti Department of Medical Oncology Cancer Center AmsterdamAmsterdam UMCVU University Medical CenterAmsterdam 1081 HVThe Netherlands Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche(STEBICEF) Universitàdegli Studi di PalermoPalermo 90133Italy Metabolic Syndrome Research Center Mashhad University of Medical SciencesMashhad 91886-17871Iran Cancer Research Center Mashhad University of Medical SciencesMashhad 91886-17871Iran Student Research Committee School of MedicineMashhad University of Medical SciencesMashhad 91886-17871Iran Drug Discovery Unit Fondazione Ri.MEDPalermo 90128Italy Department of Biochemistry Medical University of GdanskGdansk 80-210Poland Cancer Pharmacology Lab AIRC Start Up UnitFondazione Pisana per la ScienzaPisa 56124Italy.

Aim:Because mutations of splicing factor 3B subunit-1(SF3B1)have been identified in 4%of pancreatic ductal adenocarcinoma(PDAC)patients,we investigated the activity of new potential inhibitors of SF3B1 in combination with gemcitabine,one of the standard drugs,in PDAC cell ***:One imidazo[2,1-b][1,3,4]thiadiazole derivative(IS1)and three indole derivatives(IS2,IS3 and IS4),selected by virtual screening from an in-house library,were evaluated by the sulforhodamine-B and wound healing assay for their cytotoxic and antimigratory activity in the PDAC cells SUIT-2,Hs766t and Panc05.04,the latter harbouring the SF3B1 *** effects on the splicing pattern of proto-oncogene recepteur d’origine nantais(RON)and the gemcitabine transporter human equilibrative nucleoside transporter-1(hENT1)were assessed by PCR,while the ability to reduce tumour volume was tested in spheroids of primary PDAC ***:The potential SF3B1 modulators inhibited PDAC cell proliferation and prompted induction of cell *** compounds showed an interesting anti-migratory ability,associated with splicing RON/ΔRON shift in SUIT-2 cells after 24 h ***,IS1 and IS4 potentiated the sensitivity to gemcitabine in both conventional 2D monolayer and 3D spheroid cultures,and these results might be explained by the statistically significant increase in hENT1 expression(P<0.05 *** control cells),potentially reversing PDAC ***:These results support further studies on new SF3B1 inhibitors and the role of RON/hENT1 modulation to develop effective drug combinations against PDAC.

关键词： Pancreatic ductal adenocarcinoma gemcitabine indole derivatives anti-proliferative activity anti-migratory activity SF3B1 RON hENT1

Cell Proliferation Inhibition by Sericin from the Wild Silkworm, Cricula trifenestrata

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Advances in Biological Chemistry 2016年第1期6卷 28-33页

作者： Wenqi Liu Mayumi Karimazawa Taku Ozaki Ying An Masao Miyazaki Koichi Suzuki Ken-ichi Tsutsumi Tetsuro Yamashita United Graduate School of Agricultural Sciences Iwate University Morioka Japan Office of Research Exchange Iwate University Morioka Japan Research Center for Child Mental Development Hirosaki University Graduate School of Medicine Hirosaki Japan

Sericin is a major silk protein, and recent studies have shown that sericin has numerous physiological activities against cultured cells. For example, it accelerates mammalian cell proliferation and protects insect cells against cell death. In this study, we examined the activities of sericin prepared from the wild silkworm, Cricula trifenestrata. The results presented here indicated that C. trifenestrata sericin has anti-proliferative activity against feline kidney cells, while sericin from Bombyx mori promoted cell proliferation. The components of the sericin preparation that played a role in inhibition of proliferation were analyzed by fractionation through partition chromatography (Folch method) and reversed-phase chromatography. Our analysis showed that at least two components in the C. trifenestrata sericin preparation promoted the anti-proliferative activity in an additive or even synergistic manner. Therefore, differences in components between insect species may contribute to different activities against cultured cells.

关键词： Sericin Wild Silkworm Cell Death anti-proliferative activity