RESUMO
Metal complexes that exhibit both near-infrared (NIR) phosphorescence imaging and chemotherapeutic activity would represent a novel class of anticancer drugs in clinical tumor treatment. In this work, a series of novel rodlike nanomicelles have been fabricated in water by coupling poly(ethylene oxide)-block-poly(sodium acrylate) and [Rh(C≡N-2,6-xylyl)4]+(1/2SO4)-. These nanomicelles exhibit intense NIR phosphorescence and excellent stability. As revealed by in vivo NIR phosphorescence imaging data, the rodlike nanomicelle can selectively stain tumor sites with a long retention time. Moreover, the nanorods demonstrate effective anticancer activity by precisely killing tumor tissues without damaging healthy organs in vivo. To the best of our knowledge, this research provides the first example of metal-based complexes showing simultaneous NIR luminescence imaging and antitumor activity in vivo.
Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Micelas , Nanoestruturas , Polímeros/química , Ródio/química , Espectroscopia de Luz Próxima ao Infravermelho/métodos , Animais , Luminescência , Camundongos , Camundongos Nus , Água/química , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
The electrostatic combination of anionic block copolymers with cationic gold(i) complexes leads to the formation of spherical micelles, where gold(i)-containing ionic cores were formed with anionic blocks and further stabilized by neutral blocks of polystyrene or poly(ethylene oxide). This self-assembled strategy induces remarkable phosphorescence enhancement of the gold(i) complexes in solution. The emissive intensity increases unexpectedly with increasing molecular weight of the anionic block that is not coordinated onto the gold(i) complexes. The intensely phosphorescent micelles formed in water can be utilized as a luminescence bioimaging probe in living cells.
RESUMO
Ganoderpetchoids A-E and (-)-dayaolingzhiol H, six undescribed meroterpenoids, were isolated from Ganoderma petchii. Their structures including the relative configurations were identified by means of spectroscopic methods and 13C NMR calculations. Chiral separation of the new racemics was performed to afford their respective enantiomers. The absolute configurations of the new isolates were clarified by computational approaches, CD comparisons and X-ray diffraction analysis. Biological studies toward triple negative breast cancer indicated that (+)-6 and (-)-6 significantly inhibit the migration of MDA-MB-231 cell line.
Assuntos
Ganoderma , Neoplasias de Mama Triplo Negativas , Humanos , Terpenos/farmacologia , Terpenos/química , Estrutura Molecular , Ganoderma/química , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Linhagem CelularRESUMO
Petchienes A-E (1-5), five new meroterpenoids, were isolated from the fruiting bodies of Ganoderma petchii. Their structures, including absolute configurations, were elucidated by means of spectroscopic and computational methods. Compound 4 was isolated as a racemic mixture, which was finally purified by chiral HPLC to yield individual (-) and (+)-antipodes. Biological evaluation showed that compounds 2 and (-)-4 could increase intracellular free calcium concentration at 10 µM in HEK-293 cells.
Assuntos
Carpóforos/química , Ganoderma/química , Terpenos/química , Terpenos/isolamento & purificação , Estrutura MolecularRESUMO
The fungal species of the genus Ganoderma attracted great interest in the last decades. Our recent investigation on Ganoderma petchii afforded five new compounds, (-)-petchioics A and B (1 and 2), petchiates A and B (3 and 4), petchine (5), and a known compound. The structures of the new compounds were elucidated on the basis of spectroscopic data. The absolute configurations of 1 and 2 were assigned by computational methods. Biological activities of these isolates towards human cancer cells, COX-1/2, and influenza virus were evaluated.