RESUMEN
In this study, a series of nitric oxide (NO) -releasing 5-cyano-6-phenyl-2, 4-disubstituted pyrimidine derivatives were designed and synthesized. In the in vitro biological evaluation, compound 24l exhibited optimal antiproliferative activity against MGC-803 cells with the IC50 value of 0.95 µM, significantly better than that of the positive control 5-FU. In addition, preliminary mechanistic studies indicated that 24l inhibited colony formation and blocked MGC-803 cells in the G0/G1 phase. DAPI staining, reactive oxygen species and apoptosis assays demonstrated that 24l induced apoptosis of MGC-803 cells. Particularly, the most potent compound 24l produced the highest level of NO, and the antiproliferative activity was significantly reduced after preincubation with NO scavengers. In conclusion, compound 24l may be considered as a potential candidate antitumor agent.
Asunto(s)
Antineoplásicos , Óxido Nítrico , Óxido Nítrico/farmacología , Relación Estructura-Actividad , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Proliferación Celular , Antineoplásicos/farmacología , Apoptosis , Pirimidinas/farmacología , Diseño de Fármacos , Estructura MolecularRESUMEN
Halide perovskites have emerged as a type of extremely promising material for their diverse chemical and electronic structures along with their brilliant optoelectronic properties. The introduction of chirality into perovskite scaffolds, generating a novel concept of chiral perovskite materials, offers an immense step forward toward the development of smart optoelectronic and spintronic materials and devices. The present Review summarizes recent advances in such an emerging field regarding the design and construction of chiral perovskite materials, along with their optoelectronic performances. In addition, an outlook of future challenges as well as the potential significance of the chiral perovskite family on the optical communication is proposed.
RESUMEN
Random walks including non-nearest-neighbor jumps appear in many real situations such as the diffusion of adatoms and have found numerous applications including PageRank search algorithm; however, related theoretical results are much less for this dynamical process. In this paper, we present a study of mixed random walks in a family of fractal scale-free networks, where both nearest-neighbor and next-nearest-neighbor jumps are included. We focus on trapping problem in the network family, which is a particular case of random walks with a perfect trap fixed at the central high-degree node. We derive analytical expressions for the average trapping time (ATT), a quantitative indicator measuring the efficiency of the trapping process, by using two different methods, the results of which are consistent with each other. Furthermore, we analytically determine all the eigenvalues and their multiplicities for the fundamental matrix characterizing the dynamical process. Our results show that although next-nearest-neighbor jumps have no effect on the leading scaling of the trapping efficiency, they can strongly affect the prefactor of ATT, providing insight into better understanding of random-walk process in complex systems.
RESUMEN
Helicobacter pylori (H. pylori) infection is closely associated with the development of various gastric diseases. The effectiveness of current clinical antibiotic therapy is hampered by the rise of drug-resistant strains and the formation of H. pylori biofilm. This paper reports a sonodynamic nanocomposite PtCu3-PDA@AIPH@Fucoidan (PPAF), which consists of dopamine-modified inorganic sonosensitizers PtCu3, alkyl radicals (Râ¢) generator AIPH and fucoidan, can penetrate the mucus layer, target H. pylori, disrupt biofilms, and exhibit excellent bactericidal ability. In vitro experiments demonstrate that PPAF exhibits excellent acoustic kinetic properties, generating a significant amount of reactive oxygen species and oxygen-independent R⢠for sterilization under ultrasound stimulation. Simultaneously, the produced N2 can enhance the cavitation effect, aiding PPAF nanoparticles in penetrating the gastric mucus layer and disrupting biofilm integrity. This disruption allows more PPAF nanoparticles to bind to biofilm bacteria, facilitating the eradication of H. pylori. In vivo experiments demonstrate that ultrasound-stimulated PPAF exhibited significant antibacterial efficacy against H. pylori. Moreover, it effectively modulated the expression levels of inflammatory factors and maintained gastrointestinal microbiota stability when compared to the antibiotic treatment group. In summary, PPAF nanoparticles present a potential alternative to antibiotics, offering an effective and healthy option for treating H. pylori infection.
Asunto(s)
Antibacterianos , Biopelículas , Infecciones por Helicobacter , Helicobacter pylori , Moco , Biopelículas/efectos de los fármacos , Helicobacter pylori/efectos de los fármacos , Infecciones por Helicobacter/tratamiento farmacológico , Infecciones por Helicobacter/terapia , Animales , Antibacterianos/farmacología , Antibacterianos/química , Moco/metabolismo , Ratones , Radicales Libres/química , Nanopartículas/química , Ondas UltrasónicasRESUMEN
Multimodal therapies have been regarded as promising strategies for cancer treatment as compared to conventional drug delivery systems that have various drawbacks in either low loading content, uncontrolled release, non-targeting or biotoxicity. We have developed a multifunctional three-dimensional tumor-targeting drug delivery system, Fe3O4@UIO-66-NH2/graphdiyne (FUGY), based on the hybridization of a novel two-dimensional material, graphdiyne (GDY), with a metal organic framework (MOFs) structure, Fe3O4@UIO-66-NH2 (FU). The FU MOF structure has superior ability for magnetic targeting, and was constructed by an in situ growth method in which it was surface-installed with GDY via amide bonds, as a carrier of anticancer drugs. The anticancer drug doxorubicin (DOX) was loaded onto FUGY and served as both an anticancer drug to treat the tumor and a fluorescence probe to ascertain the location of FUGY. The results show that FUGY exhibits a high drug loading content of 43.8% and an effective drug release around the tumor cells at pH 5.0. In particular, fluorescence imaging demonstrates that FUGY can deliver more anticancer drugs to tumor tissue than conventional drug delivery systems. Furthermore, FUGY exhibits superior therapeutic efficiencies with negligible side effects as compared to the direct administration of free DOX, both in vitro and in vivo. The obtained FUGY drug delivery system possesses ideal biocompatibility, sustained drug release, effective chemotherapeutic efficacy, and specific targeting abilities. Such a multimodal therapeutic system can facilitate new possibilities for multifunctional drug delivery systems.
Asunto(s)
Antibióticos Antineoplásicos , Doxorrubicina , Portadores de Fármacos , Nanopartículas de Magnetita , Neoplasias Experimentales , Imagen Óptica , Animales , Antibióticos Antineoplásicos/química , Antibióticos Antineoplásicos/farmacocinética , Antibióticos Antineoplásicos/farmacología , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Preparaciones de Acción Retardada/farmacología , Doxorrubicina/química , Doxorrubicina/farmacocinética , Doxorrubicina/farmacología , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacología , Células HeLa , Humanos , Concentración de Iones de Hidrógeno , Nanopartículas de Magnetita/química , Nanopartículas de Magnetita/uso terapéutico , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Neoplasias Experimentales/diagnóstico por imagen , Neoplasias Experimentales/tratamiento farmacológico , Neoplasias Experimentales/metabolismo , Neoplasias Experimentales/patologíaRESUMEN
Graphdiyne is a new carbon allotrope comprising sp- and sp2 -hybridized carbon atoms arranged in a 2D layered structure. In this contribution, 2D graphdiyne is demonstrated to exhibit a strong light-matter interaction with high stability to achieve a broadband Kerr nonlinear optical response, which is useful for nonreciprocal light propagation in passive photonic diodes. Furthermore, advantage of the unique Kerr nonlinearity of 2D graphdiyne is taken and a nonreciprocal light propagation device is proposed based on the novel similarity comparison method. Graphdiyne has demonstrated a large nonlinear refractive index in the order of ≈10-5 cm2 W-1 , comparing favorably to that of graphene. Based on the strong Kerr nonlinearity of 2D graphdiyne, a nonlinear photonic diode that breaks time-reversal symmetry is demonstrated to realize the unidirectional excitation of Kerr nonlinearity, which can be regarded as a significant demonstration of a graphdiyne-based prototypical application in nonlinear photonics and might suggest an important step toward versatile graphdiyne-based advanced passive photonics devices in the future.