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1.
J Microbiol Biotechnol ; 31(5): 696-704, 2021 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-33820887

RESUMO

Levan is an industrially important, functional biopolymer with considerable applications in the food and pharmaceutical fields owing to its safety and biocompatibility. Here, levan-type exopolysaccharide produced by Pantoea agglomerans ZMR7 was purified by cold ethanol precipitation and characterized using TLC, FTIR, 1H, and 13C NMR spectroscopy. The maximum production of levan (28.4 g/l) was achieved when sucrose and ammonium chloride were used as carbon and nitrogen sources, respectively, at 35°C and an initial pH of 8.0. Some biomedical applications of levan like antitumor, antiparasitic, and antioxidant activities were investigated in vitro. The results revealed the ability of levan at different concentrations to decrease the viability of rhabdomyosarcoma and breast cancer cells compared with untreated cancer cells. Levan appeared also to have high antiparasitic activity against the promastigote of Leishmania tropica. Furthermore, levan had strong DPPH radical scavenging (antioxidant) activity. These findings suggest that levan produced by P. agglomerans ZMR7 can serve as a natural biopolymer candidate for the pharmaceutical and medical fields.


Assuntos
Frutanos/metabolismo , Pantoea/metabolismo , Polissacarídeos Bacterianos/metabolismo , Antineoplásicos/química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Antioxidantes/química , Antioxidantes/metabolismo , Antiparasitários/química , Antiparasitários/metabolismo , Antiparasitários/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Meios de Cultura , Frutanos/química , Frutanos/farmacologia , Humanos , Leishmania tropica/efeitos dos fármacos , Pantoea/isolamento & purificação , Polissacarídeos Bacterianos/química , Polissacarídeos Bacterianos/farmacologia
2.
Spectrochim Acta A Mol Biomol Spectrosc ; 246: 118963, 2021 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-33017789

RESUMO

The mono- (1) and bi-nuclear (2) copper(II) complexes containing N-substituted isatin thiosemicarbazone(s) were synthesized, and characterized by analytical and spectroscopic (UV-Visible, FT-IR and EPR) techniques. Bimetallic nature of complex 2 was confirmed by single crystal X-ray crystallography. The structures predicted by spectroscopic and crystallographic methods were validated by computational studies. From the spectroscopic, crystallographic and computational data, the structures were found to be distorted square planar for 1 and distorted square pyramidal for 2. Molecular docking studies showed hydrogen bonding and hydrophobic interactions of the complexes with tyrosinase kinase receptors. Complex 1 exhibited promising cytotoxic activity against Jurkat (leukemia) cell line, and complex 2 displayed more activity against HeLa S3 (cervical) and Jurkat cell lines with the IC50 values of 3.53 and 3.70 µM, respectively. Cytotoxicity of 1 (Jurkat) and 2 (Jurkat and HeLa S3) was better than that of cisplatin. Morphological changes in A549 (lung), HeLa S3 and Jurkat cell lines were examined in presence of the active complexes with the co-staining of Hoechst, AO (acridine orange) and EB (ethidium bromide) by fluorescence microscope.


Assuntos
Antineoplásicos , Complexos de Coordenação , Isatina , Tiossemicarbazonas , Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Cobre , Cristalografia por Raios X , Isatina/farmacologia , Simulação de Acoplamento Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , Tiossemicarbazonas/farmacologia
3.
Comb Chem High Throughput Screen ; 23(7): 611-623, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32067614

RESUMO

AIM AND OBJECTIVE: Platinum (II) and platinum (IV) of pyrophosphate complexes have been prepared and characterized to discover their potential as antitumor drugs. This study was conducted to prepare and characterize new ternary platinum (II) complexes with formamidine and pyrophosphate as an antitumor candidate. MATERIALS AND METHODS: The complexes have been characterized by mass, infrared, UV-Vis. spectroscopy, elemental analysis, magnetic susceptibility, thermal analyses, and theoretical calculations. They have been tested for their cytotoxicity, which was carried out using the fastcolorimetric assay for cellular growth and survival against MCF-7 (breast cancer cell line), HCT- 116 (colon carcinoma cell line), and HepG-2 (hepatocellular cancer cell line). RESULTS: All complexes are diamagnetic, and the electronic spectral data displayed the bands due to square planar Pt(II) complexes. The optimized complexes structures (1-4) indicated a distorted square planar geometry where O-Pt-O and N-Pt-N bond angles were 82.04°-96.44°, respectively. Results also show that all complexes are neutral, stable and non-hygroscopic and have noticeable cytotoxicity with IC50 (µM): 0.035-0.144 MCF-7(breast cancer cell line), 0.042-0.187 HCT-116 (colon carcinoma cell line), and 0.063-0.168 HepG-2 (hepatocellular cancer cell line). Moreover, the results show that the complex (4) has the best IC50 value. CONCLUSION: The complexes showed noticeable cytotoxicity and are considered as promising antitumor candidates for further applications.


Assuntos
Amidinas/farmacologia , Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Teoria da Densidade Funcional , Difosfatos/farmacologia , Platina/farmacologia , Amidinas/química , Antineoplásicos/síntese química , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Difosfatos/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Platina/química , Relação Estrutura-Atividade , Células Tumorais Cultivadas
4.
Spectrochim Acta A Mol Biomol Spectrosc ; 152: 358-69, 2016 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-26232580

RESUMO

A series of new ternary palladium(II) complexes of the type [Pd(L1-4)ox]·xH2O where L=formamidine ligands and ox=oxalate, were synthesized and characterized by elemental analyses, magnetic susceptibility, UV-Vis, infrared (IR) and mass spectroscopy and thermal analysis. The spectroscopic data indicated that the formamidine ligands act as bidentate N2 donors and the oxalate as O2 ligand. The complexes (1-4) are diamagnetic and the optimization of their structures indicated that the geometry is distorted square planer with O-Pd-O and N-Pd-N bond angles ranged 82.70-83.87° and 88.21-95.02°; respectively which is acceptable for the heteroleptic complexes. The dipole moment of the complexes (13.97-18.77Debye) indicating that the complexes are more polarized than the ligands (1.93-4.96Debye). The complexes are thermally stable as shown from their relatively higher overall activation energies (441-688kJmol(-1)). The ligands and the complexes are proved to have good cytotoxicity with IC50 (µM) in the range of (0.011-0.168) against MCF-7, (0.012-0.150) against HCT-116, (0.042-0.094) against PC-3 and (0.006-0.222) against HepG-2 cell lines, which open the field for further application as antitumor compounds.


Assuntos
Amidinas/química , Antineoplásicos/química , Complexos de Coordenação/química , Oxalatos/química , Paládio/química , Amidinas/farmacologia , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Complexos de Coordenação/farmacologia , Humanos , Ligantes , Modelos Moleculares , Neoplasias/tratamento farmacológico , Oxalatos/farmacologia , Paládio/farmacologia
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