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1.
Nat Prod Res ; 36(19): 5074-5080, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33939580

RESUMO

From the ethyl acetate extract (EtOAc) of the Vietnamese Garcinia mckeaniana leaves, a new flavone 8-C-glycoside 2'',6''-di-O-acetylvitexin (1), together with six known analogs 2-7 were isolated. Their structures were determined by spectral methods and compared with literature data. In α-glucosidase inhibitory assay, the EtOAc extract and its flavone and biflavone derivatives possessed the significant IC50 range of 9.17-97.53 µM, as compared with that of the positive control acarbose (249 µM). Flavones and biflavones showed are better than flavone glycosides in both α-glucosidase and acetylcholinesterase inhibitory activities[Formula: see text].


Assuntos
Flavonas , Garcinia , Acarbose , Acetilcolinesterase , Flavonas/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Garcinia/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Glicosídeos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Glucosidases
2.
Planta Med ; 88(13): 1141-1151, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34963183

RESUMO

Three prenylated xanthones, garcinone E (1: ), bannaxanthone D (2: ) and bannanxanthone E (3: ) were isolated from the leaves of Garcinia mckeaniana Graib. Their structures were elucidated by spectral methods and compared with literature data. To evaluate their anti-proliferative effects in tumor cells, firstly, cisplatin was used as a positive control and the effects of compound 1:  - 3: were determined by performing MTT assay in MDA-MB-231, CNE-2 and A549 cancer cells. The results showed compound 1:  - 3: exhibited stronger inhibitory effect than cisplatin in MDA-MB-231. Further effects of compound 1:  - 3: in TNBC MDA-MB-231 and MDA-MB-468 cells were examined by performing cell cycle and apoptosis assays. The results indicated that compound 1:  - 3: had ability to arrest cell cycle at G2/M phase and induce apoptosis. Furthermore, compound 2: significantly down-regulated PI3K, Akt and mTOR levels in both total proteins and phosphorylated form, which is its potential anti-cancer mechanism. These findings indicated that those prenylated xanthones might serve as promising leading compounds for the development of anticancer drug for TNBC.


Assuntos
Antineoplásicos , Neoplasias de Mama Triplo Negativas , Xantonas , Humanos , Fosfatidilinositol 3-Quinases/metabolismo , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Neoplasias de Mama Triplo Negativas/metabolismo , Neoplasias de Mama Triplo Negativas/patologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Xantonas/farmacologia , Xantonas/uso terapêutico , Cisplatino/farmacologia , Cisplatino/uso terapêutico , Serina-Treonina Quinases TOR/metabolismo , Apoptose , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Proliferação de Células , Linhagem Celular Tumoral
3.
Bioorg Med Chem Lett ; 37: 127841, 2021 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-33556568

RESUMO

A series of novel podophyllotoxin-naphthoquinone compounds 5a-p were synthesized in good yields using microwave-assisted four-component reactions of 2-hydroxy-1,4-naphthoquinone, aromatic benzaldehydes, tetronic acid and ammonium acetate. All the synthesized compounds were fully characterized by spectral data and evaluated for their cytotoxicity activities against KB, HepG2, Lu1, MCF7, and non-cancerous Hek-293 cell lines. Among 16 new compounds screened, compounds 5a, 5d, 5h, and 5k displayed high potent inhibitory activities with IC50 < 40 nM against HepG2 and SK-Lu-1 cell lines, and showed lower toxicity for non-cancerous Hek-293 cell line, demonstrating the potential importance of these compounds in the development of potential anticancer agents.


Assuntos
Antineoplásicos/farmacologia , Micro-Ondas , Naftoquinonas/farmacologia , Podofilotoxina/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Naftoquinonas/síntese química , Naftoquinonas/química , Podofilotoxina/síntese química , Podofilotoxina/química , Relação Estrutura-Atividade
4.
Int. microbiol ; 22(4): 437-449, dic. 2019. graf, tab
Artigo em Inglês | IBECS | ID: ibc-185062

RESUMO

Azurin, a bacteriocin produced by a human gut bacterium Pseudomonas aeruginosa, can reveal selectively cytotoxic and induce apoptosis in cancer cells. After overcoming two phase I trials, a functional region of Azurin called p28 has been approved as a drug for the treatment of brain tumor glioma by FDA. The present study aims to improve a screening procedure and assess genetic diversity of Azurin genes in P. aeruginosa and Azurin-like genes in the gut microbiome of a specific population in Vietnam and global populations. Firstly, both cultivation-dependent and cultivation-independent techniques based on genomic and metagenomic DNAs extracted from fecal samples of the healthy specific population were performed and optimized to detect Azurin genes. Secondly, the Azurin gene sequences were analyzed and compared with global populations by using bioinformatics tools. Finally, the screening procedure improved from the first step was applied for screening Azurin-like genes, followed by the protein synthesis and NCI in vitro screening for anticancer activity. As a result, this study has successfully optimized the annealing temperatures to amplify DNAs for screening Azurin genes and applying to Azurin-like genes from human gut microbiota. The novelty of this study is the first of its kind to classify Azurin genes into five different genotypes at a global scale and confirm the potential anticancer activity of three Azurin-like synthetic proteins (Cnazu1, Dlazu11, and Ruazu12). The results contribute to the procedure development applied for screening anticancer proteins from human microbiome and a comprehensive understanding of their therapeutic response at a genetic level


No disponible


Assuntos
Azurina/genética , Técnicas In Vitro/métodos , Variação Genética/efeitos dos fármacos , Microbioma Gastrointestinal/genética , Azurina/uso terapêutico , Bacteriocinas/genética , Microbioma Gastrointestinal/efeitos dos fármacos , Metagenômica , Biologia Computacional/métodos , Antineoplásicos/farmacologia
5.
Int Microbiol ; 22(4): 437-449, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30895406

RESUMO

Azurin, a bacteriocin produced by a human gut bacterium Pseudomonas aeruginosa, can reveal selectively cytotoxic and induce apoptosis in cancer cells. After overcoming two phase I trials, a functional region of Azurin called p28 has been approved as a drug for the treatment of brain tumor glioma by FDA. The present study aims to improve a screening procedure and assess genetic diversity of Azurin genes in P. aeruginosa and Azurin-like genes in the gut microbiome of a specific population in Vietnam and global populations. Firstly, both cultivation-dependent and cultivation-independent techniques based on genomic and metagenomic DNAs extracted from fecal samples of the healthy specific population were performed and optimized to detect Azurin genes. Secondly, the Azurin gene sequences were analyzed and compared with global populations by using bioinformatics tools. Finally, the screening procedure improved from the first step was applied for screening Azurin-like genes, followed by the protein synthesis and NCI in vitro screening for anticancer activity. As a result, this study has successfully optimized the annealing temperatures to amplify DNAs for screening Azurin genes and applying to Azurin-like genes from human gut microbiota. The novelty of this study is the first of its kind to classify Azurin genes into five different genotypes at a global scale and confirm the potential anticancer activity of three Azurin-like synthetic proteins (Cnazu1, Dlazu11, and Ruazu12). The results contribute to the procedure development applied for screening anticancer proteins from human microbiome and a comprehensive understanding of their therapeutic response at a genetic level.


Assuntos
Azurina/genética , Microbioma Gastrointestinal , Pseudomonas aeruginosa/genética , Pseudomonas aeruginosa/isolamento & purificação , Adolescente , Adulto , Azurina/metabolismo , Criança , Meios de Cultura/metabolismo , Fezes/microbiologia , Feminino , Variação Genética , Humanos , Masculino , Filogenia , Pseudomonas aeruginosa/crescimento & desenvolvimento , Pseudomonas aeruginosa/metabolismo , Adulto Jovem
6.
J Phys Chem Lett ; 9(7): 1561-1567, 2018 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-29518338

RESUMO

Knowledge of the vibrational structure of a semiconductor is essential for explaining its optical and electronic properties and enabling optimized materials selection for optoelectronic devices. However, measurement of the vibrational density of states of nanomaterials is challenging. Here, using the example of colloidal nanocrystals (quantum dots), we show that the vibrational density of states of nanomaterials can be accurately and efficiently measured with inelastic X-ray scattering (IXS). Using IXS, we report the first experimental measurements of the vibrational density of states for lead sulfide nanocrystals with different halide-ion terminations and for CsPbBr3 perovskite nanocrystals. IXS findings are supported with ab initio molecular dynamics simulations, which provide insight into the origin of the measured vibrational structure and the effect of nanocrystal surface. Our findings highlight the advantages of IXS compared to other methods for measuring the vibrational density of states of nanocrystals such as inelastic neutron scattering and Raman scattering.

7.
Bioorg Med Chem Lett ; 27(8): 1665-1669, 2017 04 15.
Artigo em Inglês | MEDLINE | ID: mdl-28318944

RESUMO

Four new dammarane-type triterpenoids (1-4) and twelve known compounds (5-16) were isolated from the leaves of Viburnum sambucinum Reinw. ex Blume. Their structures were determined by spectral data analysis, including MS and 2D NMR. Cytotoxic activity evaluation in vitro against four cancer cell lines (KB, LU-1, HepG2 and MCF7) suggested that the octanor-dammarane derivatives were the main cytotoxic components of the leaves of V. sambucinum.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Triterpenos/química , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Neoplasias/tratamento farmacológico , Folhas de Planta/química , Triterpenos/isolamento & purificação , Viburnum/química , Damaranos
8.
J Appl Crystallogr ; 48(Pt 3): 702-710, 2015 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-26089763

RESUMO

This study is carried out in the context of III-V semiconductor monolithic integration on silicon for optoelectronic device applications. X-ray diffraction is combined with atomic force microscopy and scanning transmission electron microscopy for structural characterization of GaP nanolayers grown on Si. GaP has been chosen as the interfacial layer, owing to its low lattice mismatch with Si. But, microtwins and antiphase boundaries are still difficult to avoid in this system. Absolute quantification of the microtwin volume fraction is used for optimization of the growth procedure in order to eliminate these defects. Lateral correlation lengths associated with mean antiphase boundary distances are then evaluated. Finally, optimized growth conditions lead to the annihilation of antiphase domains within the first 10 nm.

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