Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 4 de 4
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
J Nat Prod ; 86(1): 182-190, 2023 01 27.
Artigo em Inglês | MEDLINE | ID: mdl-36580354

RESUMO

Previous chemical investigation of the Irish deep-sea soft coral Duva florida led to the identification of tuaimenal A (10), a new merosesquiterpene containing a highly substituted chromene core and modest cytotoxicity against cervical cancer. Further MS/MS and NMR-guided investigation of this octocoral has resulted in the isolation and characterization of seven additional tuaimenal analogs, B-H (1-7), as well as two known A-ring aromatized steroids (8, 9), and additional tuaimenal A (10). Tuaimenals B, F, and G (1, 5, 6), bearing an oxygen at the C5 position, as well as monocyclic tuaimenal H (7), show increased cervical cancer inhibition profiles in comparison to that of 10. Tuaimenal G further displayed potent, selective cytotoxicity with an EC50 value of 0.04 µM against the C33A cell line compared to the CaSki cell line (EC50 20 µM). These data reveal the anticancer properties of tuaimenal analogs and suggest unique antiproliferation mechanisms across these secondary metabolites.


Assuntos
Antozoários , Neoplasias do Colo do Útero , Animais , Humanos , Feminino , Antozoários/química , Neoplasias do Colo do Útero/tratamento farmacológico , Espectrometria de Massas em Tandem , Florida , Linhagem Celular Tumoral
2.
Cells ; 11(21)2022 11 03.
Artigo em Inglês | MEDLINE | ID: mdl-36359884

RESUMO

Human topoisomerase 1B regulates the topological state of supercoiled DNA enabling all fundamental cell processes. This enzyme, which is the unique molecular target of the natural anticancer compound camptothecin, acts by nicking one DNA strand and forming a transient protein-DNA covalent complex. The interaction of human topoisomerase 1B and dimethylmyricacene, a compound prepared semisynthetically from myricanol extracted from Myrica cerifera root bark, was investigated using enzymatic activity assays and molecular docking procedures. Dimethylmyricacene was shown to inhibit both the cleavage and the religation steps of the enzymatic reaction, and cell viability of A-253, FaDu, MCF-7, HeLa and HCT-116 tumor cell lines.


Assuntos
Camptotecina , DNA Topoisomerases Tipo I , Humanos , DNA Topoisomerases Tipo I/genética , DNA Topoisomerases Tipo I/metabolismo , Camptotecina/farmacologia , Simulação de Acoplamento Molecular , DNA/metabolismo
3.
J Nat Prod ; 85(10): 2395-2398, 2022 10 28.
Artigo em Inglês | MEDLINE | ID: mdl-36122192

RESUMO

Four undescribed sesquiterpenoids, crannenols A-D (1-4), have been isolated from CHCl2 and MeOH extracts of the deep-sea bamboo coral Acanella arbuscula. The corals were collected from a submarine canyon on the edge of Ireland's Porcupine Bank via a remotely operated vehicle. The structure elucidation of these (Z,E)-α-farnesene derivatives was achieved using a combination of 1D and 2D NMR, electron impact (1, 2), and electrospray ionization (3, 4) mass spectrometry.


Assuntos
Antozoários , Sesquiterpenos , Animais , Antozoários/química , Sesquiterpenos/química , Espectroscopia de Ressonância Magnética
4.
J Enzyme Inhib Med Chem ; 37(1): 1404-1410, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35603503

RESUMO

Nature has been always a great source of possible lead compounds to develop new drugs against several diseases. Here we report the identification of a natural compound, membranoid G, derived from the Antarctic sponge Dendrilla antarctica displaying an in vitro inhibitory activity against human DNA topoisomerase 1B. The experiments indicate that membranoid G, when pre-incubated with the enzyme, strongly and irreversibly inhibits the relaxation of supercoiled DNA. This compound completely inhibits the cleavage step of the enzyme catalytic mechanism by preventing protein binding to the DNA. Membranoid G displays also a cytotoxic effect on tumour cell lines, suggesting its use as a possible lead compound to develop new anticancer drugs.


Assuntos
Antineoplásicos , Neoplasias , Regiões Antárticas , Antineoplásicos/química , Antineoplásicos/farmacologia , DNA/química , DNA Topoisomerases Tipo I/metabolismo , DNA Topoisomerases Tipo II/metabolismo , Humanos , Inibidores da Topoisomerase
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...