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1.
Sensors (Basel) ; 24(10)2024 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-38794076

RESUMO

Object detection is one of the core technologies for autonomous driving. Current road object detection mainly relies on visible light, which is prone to missed detections and false alarms in rainy, night-time, and foggy scenes. Multispectral object detection based on the fusion of RGB and infrared images can effectively address the challenges of complex and changing road scenes, improving the detection performance of current algorithms in complex scenarios. However, previous multispectral detection algorithms suffer from issues such as poor fusion of dual-mode information, poor detection performance for multi-scale objects, and inadequate utilization of semantic information. To address these challenges and enhance the detection performance in complex road scenes, this paper proposes a novel multispectral object detection algorithm called MRD-YOLO. In MRD-YOLO, we utilize interaction-based feature extraction to effectively fuse information and introduce the BIC-Fusion module with attention guidance to fuse different modal information. We also incorporate the SAConv module to improve the model's detection performance for multi-scale objects and utilize the AIFI structure to enhance the utilization of semantic information. Finally, we conduct experiments on two major public datasets, FLIR_Aligned and M3FD. The experimental results demonstrate that compared to other algorithms, the proposed algorithm achieves superior detection performance in complex road scenes.

2.
Macromol Rapid Commun ; 44(8): e2200918, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36639944

RESUMO

Metallo-supramolecular polymers represent a powerful platform to construct self-assembled morphologies. Copper-thiourea (Cu-TU) coordination interactions, though have been extensively studied in small molecular system, the role of TU motifs in synthetic polymers using metal-ligand coordination to afford supramolecular aggregation and their morphology are often overlooked. Herein, an amphiphilic random copolymer, poly(oligo(ethylene glycol) ethyl acrylate-r-acylthiourea) (P(OEGEA-r-ATU)), bearing pendant TU motifs behaving as the ligand to coordinate Cu, a design characterized by core-coordinated metallo-supramolecular polymer is rationally synthesized. Indeed, rod-like nano-objects are successfully generated via the self-assembly and coordination interaction between P(OEGEA-r-ATU) and Cu. The spatial distribution of TU moieties in polymer chain, along with their Cu chelating capability, featuring the interchain coordination interaction, is tightly related to metallo-supramolecular polymer organization. The specific Cu-TU coordination interactions enable the prompted robustness and stability of soft P(OEGEA-r-ATU), induce the polymer chain configuration, which eventually furnish efficient fabrication of rod-like nano-objects via straightforward nanoprecipitation procedure. These structural motifs of copper-coordinated, rod-like nano-objects from such metallo-supramolecular polymers endow the potential therapeutic properties, such as anti-inflammatory and antitumor effects.


Assuntos
Cobre , Tioureia , Cobre/química , Ligantes , Polímeros/química , Metais
3.
Biomacromolecules ; 23(11): 4519-4531, 2022 11 14.
Artigo em Inglês | MEDLINE | ID: mdl-36250649

RESUMO

Chemodynamic therapy (CDT) reflects an innovative cancer treatment modality; however, to enhance its relatively low therapeutic efficiency, rational combination with extra therapeutic modes is highly appreciated. Here, core-coordinated amphiphilic, elliptic polymer nanoparticles (Cu/CBL-POEGEA NPs) are constructed via the self-assembly of a glutathione (GSH)-responsive polymer-drug conjugate, bearing side-chain acylthiourea (ATU) motifs which behave as ligands capable of coordinating Cu(II), such a design is featured by combined chemo (CT)/CDT with dual GSH depletion collectively triggered by the Cu(II) reduction reaction and disulfide bond breakage. To do so, an amphiphilic random copolymer poly[oligo(ethylene glycol)ethyl acrylate-co-thiourea] [P(OEGEA-co-ATU)] is synthesized, followed by conjugation of chlorambucil (CBL) to ATU motifs linked via a disulfide bond, thus yielding the targeted P[OEGEA-co-(ATU-g-CBL)]. In such a system, hydrophilic POEGEA serves as the biocompatible section and ATU motifs coordinate Cu(II), resulting in core-coordinated elliptic Cu/CBL-POEGEA NPs. Benefitting from the GSH-induced reduction reaction, Cu(II) is converted into Cu(I) and subsequently react with endogenous H2O2 to create •OH, realizing GSH-depletion-promoted CDT. Additionally, the disulfide bond endows GSH-responsive CBL release and provokes further GSH decline, finally realizing combined CDT/CT toward enhancing antitumor outcomes, and in vitro as well as in vivo studies indeed reveal remarkable efficacy. Such a system can provide valuable advantages to create novel nanomedicines toward cascade antitumor therapy.


Assuntos
Nanopartículas , Neoplasias , Humanos , Cobre/química , Clorambucila/farmacologia , Polímeros/uso terapêutico , Peróxido de Hidrogênio , Nanopartículas/química , Glutationa/química , Dissulfetos , Linhagem Celular Tumoral , Neoplasias/tratamento farmacológico , Neoplasias/patologia
4.
Water Sci Technol ; 82(7): 1296-1303, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33079710

RESUMO

Melamine foam is an important material in production and life. A series of porous carbon foams were obtained through a simple carbonization process of melamine foam at different temperatures. The carbon foams obtained at the carbonization temperature of 400 and 600 °C reveal a hydrophobic and even super-hydrophobic property (water contact angle larger than 150°) with a hexane adsorption much larger than that of melamine foam. However, the carbon foam obtained at the carbonization temperature of 800 °C reveals a super-hydrophilic property (water contact angle smaller than 5°) due to its severest shrinkage during the carbonization process. Interestingly, this series of carbon foams have an excellent performance in oil adsorption. However, the carbon membranes derived from the 800 °C carbon foam reveals oleophobicity under water (the adsorbed water at the surface was extremely important), which allows the penetration of water and blocks the infiltration of hexane at the same time. These different carbon forms have reversed applications in hexane/water separation.


Assuntos
Hexanos , Água , Adsorção , Carbono , Interações Hidrofóbicas e Hidrofílicas
6.
Bioorg Med Chem ; 21(2): 448-55, 2013 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-23245802

RESUMO

A series of novel thiazolyl-pyrazoline derivatives containing benzodioxole (C1-C20) have been designed and synthesized. Among of the synthesized compounds, 2-(5-(benzo[d][1,3]dioxol-5-yl)-3-(4-bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-4-(4-bromophenyl)thiazole (C6) displayed the most potent inhibitory activity for HER-2 (IC(50) = 0.18 µM for HER-2). Antiproliferative assay results indicated that compound C6 owned high antiproliferative activity against MCF-7 and B16-F10 in vitro, with IC(50) value of 0.09 and 0.12 µM, respectively, being comparable with the positive control Erlotinib. Docking simulation was further performed to determine the probable binding model. Based on the preliminary results, compound C6 with potent inhibitory activity in tumor growth would be a potential anticancer agent.


Assuntos
Antineoplásicos/síntese química , Benzodioxóis/química , Pirazóis/química , Tiazóis/química , Antineoplásicos/química , Antineoplásicos/toxicidade , Sítios de Ligação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Células MCF-7 , Simulação de Acoplamento Molecular , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/toxicidade , Estrutura Terciária de Proteína , Pirazóis/síntese química , Pirazóis/toxicidade , Receptor ErbB-2/antagonistas & inibidores , Receptor ErbB-2/metabolismo , Relação Estrutura-Atividade
7.
Acta Chim Slov ; 70(1): 12-20, 2023 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-37005630

RESUMO

Four new complexes of copper(II), nickel(II) and zinc(II), [CuL2] (1), [Ni3L2(4-BrSal)2(CH3COO)2(CH3OH)2]·2CH3OH (2), [ZnBr2(HL)2] (3) and [ZnL(dca)]n (4), where L is 5-bromo-2-((cychlopentylimino)methyl)phenolate, HL is the zwitterionic form of 5-bromo-2-((cychlopentylimino)methyl)phenol, 4-BrSal is the monoanionic form of 4-bromosalicylaldehyde, dca is dicyanamide anion, were synthesized and characterized by elemental analysis, IR and UV-Vis spectroscopy. The structures of the complexes were further confirmed by single crystal X-ray structure determination. Complex 1 is a mononuclear copper(II) compound, with a crystallographic two-fold rotation axis symmetry. The Cu atom is in distorted square planar coordination. Complex 2 is a trinuclear nickel(II) compound, with an inversion center symmetry. The Ni atoms are in octahedral coordination. Complex 3 is a mononuclear zinc(II) compound, while complex 4 is a dca bridged polymeric zinc(II) compound. The Zn atoms are in tetrahedral coordination. The compounds were assayed for their antimicrobial activities.

8.
Acta Chim Slov ; 69(3): 694-699, 2022 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-36196828

RESUMO

Two new oxidovanadium(V) complexes, [VOL1(HQ)] (1) and [VOL2(SAH)] (2), were prepared by the reaction of [VO(acac)2] (where acac = acetylacetonate) with N'-(3-ethoxy-2-hydroxybenzylidene)nicotinohydrazide (H2L1) and 8-hydroxyquinoline (HHQ), and N'-(2-hydroxy-4-methoxybenzylidene)nicotinohydrazide (H2L2) and salicylhydroxamic acid (HSAH), respectively, in methanol. Crystal and molecular structures of the complexes were determined by elemental analysis, infrared spectroscopy and single crystal X-ray diffraction. The V atoms in both complexes are in octahedral coordination. Thermal stability of the complexes was studied. Both complexes can decrease the blood glucose level in alloxan-diabetic mice, but the blood glucose level in the treated normal mice was not altered.


Assuntos
Diabetes Mellitus Experimental , Insulinas , Aloxano , Animais , Glicemia , Diabetes Mellitus Experimental/tratamento farmacológico , Hidrazonas/química , Hidroxiquinolinas , Ligantes , Metanol , Camundongos , Oxiquinolina
9.
Acta Chim Slov ; 68(4): 1008-1015, 2021 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-34918755

RESUMO

Three new copper(II) complexes, [Cu(LH)2]Br2 (1), [Cu(LH)2]NCS2 (2), and [Cu(LH)2](NO3)2 (3), where LH is the zwitterionic form of 2-bromo-6-((2-(isopropylamino)ethylimino)methyl)phenol (HL), were synthesized and characterized by elemental analysis, IR and UV-vis spectroscopy. The structures of the complexes were further confirmed by single crystal X-ray structure determination. All compounds are mononuclear copper(II) complexes. The Cu atoms in the complexes are coordinated by two imino N and two phenolate O atoms from two LH ligands, forming square planar coordination. The compounds were assayed for their antimicrobial activities.

10.
Acta Chim Slov ; 67(4): 1301-1308, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33533474

RESUMO

Four new copper(II) complexes, [CuL1(?1,1-N3)]n (1), [CuL1(?1,3-NCS)]n (2), [Cu(HL2)2](SCN)2 (3) and [Cu(L2)2] (4), where L1 and L2 are 2-((2-(dimethylamino)ethylimino)methyl-4,6-difluorophenolate and 2,4-difluoro-6-((3-morpholinopropylimino) methyl)phenolate, respectively, and HL2 is 2-((2-(dimethylammonio)ethylimino)methyl-4,6-difluorophenolate, were synthesized and characterized by elemental analysis, IR and UV-vis spectroscopy. The structures for the complexes were further confirmed by single crystal X-ray structure determination. Complexes 1 and 2 are polymeric copper(II) complexes, with the Cu atoms in square pyramidal coordination. Complexes 3 and 4 are mononuclear copper(II) complexes, with the Cu atoms in square planar coordination. The complexes were assayed for their antimicrobial properties.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Complexos de Coordenação/farmacologia , Bases de Schiff/farmacologia , Antibacterianos/síntese química , Antifúngicos/síntese química , Aspergillus niger/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Complexos de Coordenação/síntese química , Cobre/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Bases de Schiff/síntese química
11.
Mini Rev Med Chem ; 20(10): 908-920, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32116191

RESUMO

Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neurodegenerative diseases such as depression, Parkinson's disease and Alzheimer's disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single heterocyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure- activity relationship to provide better correlation among different structures and their receptor interactions.


Assuntos
Descoberta de Drogas , Compostos Heterocíclicos/farmacologia , Inibidores da Monoaminoxidase/farmacologia , Compostos Heterocíclicos/química , Humanos , Inibidores da Monoaminoxidase/química
12.
Spectrochim Acta A Mol Biomol Spectrosc ; 227: 117675, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31670047

RESUMO

By modifying the 10-butyl-2-methoxy-10H-phenothiazine-3-carbaldehyde with malonontrile group, a new fluorescent sensor PBM for selective detection of hydrazine in ratiometric mode has been developed. Probe PBM owned the advantages of quick response (10 min), remarkable Stokes shift (168 nm for PBM, 161 nm for PBM-NH2), excellent selectivity, high sensitivity (detection limit of 63.2 nM was obtained from in vitro experiment), profound ratiometric change (82-fold) and low cytotoxicity in response to hydrazine. Additionally, it could be utilized to monitor hydrazine in gas state with various concentrations through vivid color changes and imaged hydrazine in living MCF-7 cells with excellent performance.


Assuntos
Corantes Fluorescentes/química , Hidrazinas/química , Imageamento Tridimensional , Fenômenos Ópticos , Fenotiazinas/química , Sobrevivência Celular , Humanos , Concentração de Íons de Hidrogênio , Células MCF-7 , Espectrometria de Fluorescência , Espectrofotometria Ultravioleta , Fatores de Tempo
13.
Acta Chim Slov ; 67(4): 1281-1289, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33533465

RESUMO

Two vanadium(V) complexes derived from the bromo and chloro-substituted hydrazones N'-(4-bromo-2-hydroxybenzylidene)- 2-chlorobenzohydrazide (H2L1) and N'-(3-bromo-5-chloro-2-hydroxybenzylidene)-3-methylbenzohydrazide (H2L2) with the formula [VOL1(OCH3)(CH3OH)] (1) and [VOL2(OCH3)(CH3OH)] (2) were newly synthesized and characterized by IR, UV-Vis and 1H NMR spectroscopy. The structures of H2L1 and the complexes were further confirmed by single crystal X-ray diffraction. Both vanadium complexes are mononuclear, with the metal atoms coordinated by the hydrazone ligands, methanol ligands, and methanolate ligands, and the oxo groups, forming octahedral geometry. The hydrazones and the vanadium complexes were assayed for the antimicrobial activities on Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas fluorescence, and the fungi Candida albicans and Aspergillus niger. The existence of the bromo and chloro groups in the hydrazone ligands may improve the antimicrobial property.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Complexos de Coordenação/farmacologia , Hidrazonas/farmacologia , Antibacterianos/síntese química , Antifúngicos/síntese química , Aspergillus niger/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Complexos de Coordenação/síntese química , Hidrazonas/síntese química , Ligantes , Testes de Sensibilidade Microbiana , Estrutura Molecular , Vanádio/química
14.
Acta Crystallogr Sect E Struct Rep Online ; 65(Pt 5): o975, 2009 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-21584015

RESUMO

The title Schiff base compound, C(14)H(11)ClN(2)O(3), was prepared by the reaction of 5-chloro-salicylaldehyde and 4-hydroxy-benzohydrazide. The mol-ecule exists in a trans configuration with respect to the methyl-idene group. The dihedral angle between the two benzene rings is 40.1 (2)°. An intra-molecular O-H⋯N hydrogen bond helps to stabilize the mol-ecular conformation. In the crystal structure, mol-ecules are linked into a three-dimensional network by inter-molecular N-H⋯O and O-H⋯O hydrogen bonds.

15.
Acta Chim Slov ; 66(2): 484-489, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33855515

RESUMO

A new linear trinuclear Schiff base nickel(II) complex, [NiNiL(α2-α1:α1-OAc)(OH2)2]·H2O, where L is the dianionic form of N,N'-bis(5-chloro-2-hydroxybenzylidene)-1,3-propanediamine (H2L), was synthesized and characterized by elemental analyses, IR spectroscopy, and X-ray single-crystal determination. There are three bridges across the Ni-Ni atom pairs, involving two phenolate O atoms of a Schiff base ligand, and an O-C-O moiety of a α2-α1:α1-OAc group. The Ni atoms have octahedral coordination. The acetate bridges linking the central and terminal nickel atoms are mutually trans. The adjacent NiαααNi distances are 3.047(1) α. The complex was evaluated for its antibacterial (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa) and antifungal (Candida albicans and Aspergillus niger) activities by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method.

16.
Acta Chim Slov ; 66(3): 675-680, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33855539

RESUMO

Three new cobalt(II), zinc(II) and cadmium(II) complexes, [CoL2]·2CH3OH·H2O (1), [ZnL2] (2) and [Cd(HL)2(NO3)]N3 (3), were prepared from 2-hydroxy-N'-(pyridin-2-ylmethylene)benzohydrazide (HL). The complexes have been characterized by IR, UV-Vis and single-crystal X-ray diffraction techniques. X-ray analysis indicates that the complexes are mononuclear species, with the metal atoms in octahedral coordination. The hydrazone compound and its complexes were evaluated for their antibacterial (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas fluorescence) and antifungal (Candida albicans and Aspergillus niger) activities. The complexes have effective activities against the bacteria.

17.
Acta Chim Slov ; 66(3): 719-725, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33855543

RESUMO

Two new VV complexes with the bromo-substituted hydrazones N'-(3-bromo-2-hydroxybenzylidene)-3-hydroxy-4-methoxybenzohydrazide (H2L1), N'-(3-bromo-2-hydroxybenzylidene)-3,5-dimethoxybenzohydrazide (H2L2), [VOL1(OCH3)(CH3OH)] (1) and [VOL2(OCH3)(CH3OH)] (2), were synthesized and structurally characterized by IR, UV-Vis and 1H NMR spectroscopy, as well as single-crystal X-ray determination. The V atom in the mononuclear complexes are six-coordinated in octahedral geometry. The free hydrazones and the complexes were studied on their antibacterial activity on S. aureus, B. subtilis, E. coli and P. fluorescence, and antifungal activity on C. albicans and A. niger. The bromo groups of the hydrazone ligands may increase their antibacterial activity.

18.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 9): o1829-30, 2008 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-21201804

RESUMO

The title Schiff base compound, C(19)H(16)N(2)O(3), prepared by the reaction of 2-meth-oxy-1-naphthyl-aldehyde and 2-hydroxy-benzohydrazide, crystallizes with two independent mol-ecules in the asymmetric unit. Each mol-ecule exists in a trans configuration with respect to the methyl-idene group. The naphthyl ring system make dihedral angles of 65.0 (2)° and 55.8 (2)° with the planes of the benzene rings. Intra-molecular N-H⋯O and O-H⋯O hydrogen bonds help to stabilize the mol-ecular conformations. In the crystal structure, mol-ecules are linked into one-dimensional chains parallel to the c axis by inter-molecular O-H⋯N and O-H⋯O hydrogen bonds.

19.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 9): o1831, 2008 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-21201805

RESUMO

The mol-ecule of the title Schiff base compound, C(20)H(18)N(2)O(3), prepared by the reaction of 2-meth-oxy-1-naphthyl-aldehyde and 4-methoxy-benzohydrazide, exists in a trans configuration with respect to the imine group. The naphthyl ring system makes a dihedral angle of 71.4 (2)° with the mean plane of the benzene ring. In the crystal structure, mol-ecules are linked into one-dimensional chains parallel to the c axis by inter-molecular N-H⋯O hydrogen bonds.

20.
Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi ; 34(10): 937-941, 2018 Oct.
Artigo em Zh | MEDLINE | ID: mdl-30554588

RESUMO

Objective To investigate the diagnostic value of human papillomavirus (HPV) E6/E7 mRNA combined with P16/antigen KI-67(ki67) immunocytochemical double staining in the atypical squamous cells of undetermined significance (ASCUS). Methods A total of 272 patients were selected and the results of HPV E6/E7 and P16/ki67 immunocytochemical double staining in the remaining cytological specimens were retrospectively analyzed. HPV E6/E7 gene was detected by HPV E6/E7 gene detection kit and Panther molecular diagnostic instrument. P16/ki67 was detected by immunocytochemical staining and Ventana Benchmark Ultra immunohistochemical staining instrument. Then we analyzed the difference of positive rate between the two detection methods in the same grade of cervical epithelial lesions, explored the difference of the two detection methods and their combined detection in the diagnosis of high grade squamous intraepithelial lesions (HSIL), and finally evaluated the role of different detection methods in shunt diagnosis of ASCUS. Results Histopathological findings of cervical cytology ASCUS includes chronic cervicitis, low-grade squamous intraepithelial lesions (LSIL), HSIL and cervical cancer. The positive rate of simple molecular diagnosis or immunocytochemical staining increased with the severity of cervical lesions. In cervicitis and LSIL lesion group, the difference between the positive rates of the two methods was obvious, but in HSIL and cervical cancer lesion group, there was no significant difference between the positive rates of the two methods. The sensitivity, specificity, Yoden index, coincidence rate, positive predictive value and negative predictive value were 95.65%, 85.40%, 0.81, 87.13%, 57.14% and 98.97%, respectively. Conclusion The detection of HPV E6/E7 and P16/ki67 immunocytochemical staining has certain significance in ASCUS shunt diagnosis. The combined detection of HPV E6/E7 and P16/ki67 can significantly improve the sensitivity of shunt diagnosis and maintain a good specificity.


Assuntos
Células Escamosas Atípicas do Colo do Útero/virologia , Inibidor p16 de Quinase Dependente de Ciclina/análise , Antígeno Ki-67/análise , Proteínas Oncogênicas Virais/análise , Proteínas E7 de Papillomavirus/análise , Infecções por Papillomavirus/diagnóstico , Feminino , Humanos , Imuno-Histoquímica , Papillomaviridae , RNA Mensageiro , Estudos Retrospectivos , Neoplasias do Colo do Útero/diagnóstico , Neoplasias do Colo do Útero/virologia , Displasia do Colo do Útero/diagnóstico , Displasia do Colo do Útero/virologia
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