RESUMO
The Zimbabwean medicinal plant Monadenium lugardae was evaluated as a potential source of new anticancer constituents. Four new tetracyclic triterpene (1-4) were isolated, accompanied by four previously known triterpenes (5-8). Against a panel of human tumor cell lines, lugardstatins 1 (1) and 2 (2) had good cancer cell growth inhibitory activity. All of the triterpene structures (1-8) were established by 1D and 2D NMR spectrometric and HR mass spectrometric analysis.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Euphorbia/química , Plantas Medicinais/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Leucemia P388 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Triterpenos/química , ZimbábueRESUMO
Two new cyclodepsipeptides designated bacillistatins 1 (1) and 2 (2) have been isolated from cultures of a sample of Bacillus silvestris that was obtained from a Pacific Ocean (southern Chile) crab. Each 12-unit cyclodepsipeptide strongly inhibited growth of a human cancer cell line panel, with GI(50)'s of 10(-4)-10(-5) microg/mL, and each compound was active against antibiotic-resistant Streptococcus pneumoniae. The structures were elucidated by a combination of X-ray diffraction and mass and 2D NMR spectroscopic analyses, together with chemical degradation.
Assuntos
Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Bacillus/química , Depsipeptídeos/isolamento & purificação , Depsipeptídeos/farmacologia , Animais , Antineoplásicos/química , Cristalografia por Raios X , Depsipeptídeos/química , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Masculino , Biologia Marinha , Camundongos , Testes de Sensibilidade Microbiana , Modelos Moleculares , Conformação Molecular , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , EstereoisomerismoRESUMO
An investigation of the Phillippine Ampelocissus sp. roots for cancer cell growth inhibitory components led to the isolation of a new acetogenin characterized as 22-epicalamistrin (1) employing primarily 2D NMR and high-resolution mass spectral analysis. Two other antineoplastic constituents proved to be the known acetogenin uvaribonin (2) and chalcone 3. Constituents 1-3 were all found to show significant cancer cell growth inhibitory activity against a panel of human cancer cell lines.
Assuntos
Acetogeninas/isolamento & purificação , Acetogeninas/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Vitaceae/química , Acetogeninas/química , Animais , Antineoplásicos Fitogênicos/química , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Masculino , Conformação Molecular , Estrutura Molecular , Ressonância Magnética Nuclear BiomolecularRESUMO
A Streptomyces sp. isolated from riverbank soil in Manitoba, Canada, was found to contain two cancer cell growth inhibitories: diazaanthraquinone 1 and 3-(hydroxyacetyl)indole (8). The structures were determined by interpretation of data from HRMS, UV, and high-field (400 MHz) NMR experiments. The red-colored diazaanthraquinone 1 and 3-(hydroxyacetyl)indole (8) were found to inhibit (0.1-3 microg/mL) growth of a minipanel of human cancer cell lines and P388 lymphocytic leukemia cells. Diazaanthraquinone 1 was also found to inhibit growth of the bacteria Streptococcus pneumoniae and Neisseria gonorrheae. However, three companion constituents, cyclo-Pro-Leu (5), cyclo-Pro-Phe (6), and cyclo-Pro-Val (7), did not inhibit cancer cell growth.
Assuntos
Antibacterianos/isolamento & purificação , Compostos Aza/isolamento & purificação , Indóis/isolamento & purificação , Quinonas/isolamento & purificação , Streptomyces/química , Sequência de Aminoácidos , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Compostos Aza/química , Compostos Aza/farmacologia , Dipeptídeos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Indóis/química , Indóis/farmacologia , Leucemia P388 , Manitoba , Camundongos , Estrutura Molecular , Peptídeos Cíclicos/isolamento & purificação , Quinonas/química , Quinonas/farmacologia , Streptococcus/efeitos dos fármacos , Streptomyces/isolamento & purificação , Células Tumorais CultivadasRESUMO
Three new sesquiterpene quinols (1, 2, and 5) and two known ones (3 and 4) were isolated along with halistanol sulfate (6) from a marine sponge of the genus Aka collected from Yap Island, Federated States of Micronesia. Their structures were determined from spectral data, and the structure of siphonodictyal C (3) was revised. Sulfates 3 and 6 inhibit CDK4/cyclin D1 complexation, whereas 1 and 4 do not.
