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Herein, a multi-functional nanoplatform (PDA-DTC/Cu–MnO2) was established, which has been employed for MR imaging-guided multi-therapy (CDT, PTT and chemotherapy) for cancer treatment. The in vitro and in vivo results confirmed that the biocompatible nanoplatform could significantly induce tumor cell death and inhibit tumor growth. [ABSTRACT FROM AUTHOR]

To overcome the acquired resistance and the significant side-effects of the reported drugs, four new ruthenium(II) complexes with alkynyl (Ru1, Ru2, Ru3, Ru4) were designed and synthesized. Ru1, Ru2, Ru3 and Ru4 were characterized by ESI-MS, 1H NMR, 1H–1H COSY NMR and elemental analysis. Compared with Ru2, Ru3, Ru4 and cisplatin, the anti-tumor experiments in vitro and vivo confirmed that Ru1 could most effectively inhibit tumor growth. In the experiments of safety evaluation in vivo, Ru1 could avoid any detectable side-effects compared with cisplatin. DNA binding experiments and cell cycle experiments showed that Ru1 exhibited the strongest DNA binding ability and interfered with the cell cycle by inserting DNA to inhibit tumor growth. The study demonstrated that Ru1 had the potential to be an exciting new drug candidate for glioblastoma treatment. [ABSTRACT FROM AUTHOR]

Multifunctional nanotheranostic systems with both therapeutic and imaging functions are highly desired for the development of more effective and less toxic anti-tumor drugs. Herein, a simple but effective method is reported to fabricate a novel PCN-CuS-FA-ICG-based nanoplatform for dual-modal imaging-guided synergistic photothermal/photodynamic therapy. Porphyrinic metal–organic frameworks with CuS NPs are obtained in aqueous solution via a simple post-synthesis strategy. Furthermore, to obtain a more effective therapy, indocyanine green (ICG) was incorporated into the multifunctional theranostic platform to promote the photothermal therapeutic effect. The as-prepared PCN-CuS-FA-ICG not only exhibits an excellent 1O2 generation efficiency under 650 nm irradiation to achieve remarkable photodynamic cell killing, but also presents outstanding photothermal conversion under 808 nm irradiation to destroy tumor tissues by hyperthermia. In particular, the nanotherapeutic agent realized fluorescence and thermal imaging dual-modal imaging-guided cancer treatment. Meanwhile, in vivo experiments confirmed the evident accumulation of nanoparticles (NPs) at local tumors, and tumor growth was inhibited obviously via synergistic photothermal/photodynamic therapy with negligible side effects. [ABSTRACT FROM AUTHOR]

Based on the Pt nanozyme modified mesoporous polydopamine in situ, a multi-functional nanoplatform was established, which could overcome tumour hypoxia by catalyzing overexpressed H2O2 in tumour cells to enhance photodynamic therapy. In vivo results confirmed that the tumour growth was inhibited efficiently by synergetic therapy. [ABSTRACT FROM AUTHOR]

Chiral recognition of DNA molecules is important because much evidence has indicated that transformations of chirality and diverse conformations of DNA are involved in a series of key biological events. Among these, enrichment of G-quadruplexes (GQs) in the genome, and the exploration of their multiple structures, has aroused great interest. Herein, we compared nearly 100 different sequences with 3′-tail sequences of variable length or different linkers or diverse loops and mutative ionic concentrations. All sequences were capable of forming stable GQs, with fluorescence signal enhancement upon binding with Δ- and Λ- [Ru(bpy)2(dppz-idzo)]2+ (Δ/Λ-1). Our results show that multiple factors, including the 3′-tail length, linkers, loop length and ionic concentration, regulate the enantioselectivity of GQs. Furthermore, molecular docking simulations revealed that chiral recognition of GQs depends on the binding site. To the best of our knowledge, this is the first systematic study regarding the regulation of multi-factors for GQ selectivity of chiral Ru-complexes. These results will serve as a useful reference for enantioselective recognition of genomic GQs and may facilitate the development of chiral anticancer agents for targeting GQs. [ABSTRACT FROM AUTHOR]

Chiral recognition of DNA molecules is important because much evidence has indicated that transformations of chirality and diverse conformations of DNA are involved in a series of key biological events. Among these, enrichment of G-quadruplexes (GQs) in the genome, and the exploration of their multiple structures, has aroused great interest. Herein, we compared nearly 100 different sequences with 3′-tail sequences of variable length or different linkers or diverse loops and mutative ionic concentrations. All sequences were capable of forming stable GQs, with fluorescence signal enhancement upon binding with Δ- and Λ- [Ru(bpy)2(dppz-idzo)]2+ (Δ/Λ-1). Our results show that multiple factors, including the 3′-tail length, linkers, loop length and ionic concentration, regulate the enantioselectivity of GQs. Furthermore, molecular docking simulations revealed that chiral recognition of GQs depends on the binding site. To the best of our knowledge, this is the first systematic study regarding the regulation of multi-factors for GQ selectivity of chiral Ru-complexes. These results will serve as a useful reference for enantioselective recognition of genomic GQs and may facilitate the development of chiral anticancer agents for targeting GQs. [ABSTRACT FROM AUTHOR]

Early disease diagnosis is very important for the prevention or mitigation of metastasis. Effective and efficient methods are needed to improve the diagnosis and assessment of diseases. Thrombin is a biomarker for diagnosis of some diseases, such as pulmonary metastases and diseases associated with coagulation abnormalities. Lots of methods for detecting thrombin have been reported, however, most of them were based on a single aptamer and needed modification of aptamers, and label free sensors for thrombin detection based on an aptamer pair are challenging. In this work, we present three label free sensing platforms based on [Ru(bpy)2(o-mopip)]2+ (bpy = 2,2-bipyridine; o-mopip = 2-(2-methoxylphenyl)imidazo[4,5-f][1,10]phenanthroline) (OMO) and graphene oxide (GO) for thrombin detection. Thrombin detection using our three label free sensors is accomplished by specific target recognition based on aptamer pair TBA1/TBA2–thrombin, single aptamer TBA1–thrombin or TBA2–thrombin, respectively. Direct readouts of the target recognition is achieved by restoration of the fluorescence of OMO prequenched by GO. All of the three sensing platforms exhibited high sensitivity and selectivity. Furthermore, all sensing platforms were successfully applied to thrombin analysis in diluted bovine serum. According to the thrombin dependent response of the three platforms, the sensing platform based on aptamer pair TBA1 and TBA2 showed the highest sensitivity, widest linearity, best selectivity and recovery in diluted serum to thrombin. These results show that the sensing platform based on an aptamer pair have great potential for clinical diagnosis of disease-related biomarkers. [ABSTRACT FROM AUTHOR]

Herein, a multi-functional nanoplatform (PDA-DTC/Cu-MnO2) was established, which has been employed for MR imaging-guided multi-therapy (CDT, PTT and chemotherapy) for cancer treatment. The in vitro and in vivo results confirmed that the biocompatible nanoplatform could significantly induce tumor cell death and inhibit tumor growth.

To overcome the acquired resistance and the significant side-effects of the reported drugs, four new ruthenium(ii) complexes with alkynyl (Ru1, Ru2, Ru3, Ru4) were designed and synthesized. Ru1, Ru2, Ru3 and Ru4 were characterized by ESI-MS, 1H NMR, 1H-1H COSY NMR and elemental analysis. Compared with Ru2, Ru3, Ru4 and cisplatin, the anti-tumor experiments in vitro and vivo confirmed that Ru1 could most effectively inhibit tumor growth. In the experiments of safety evaluation in vivo, Ru1 could avoid any detectable side-effects compared with cisplatin. DNA binding experiments and cell cycle experiments showed that Ru1 exhibited the strongest DNA binding ability and interfered with the cell cycle by inserting DNA to inhibit tumor growth. The study demonstrated that Ru1 had the potential to be an exciting new drug candidate for glioblastoma treatment.

Chiral recognition of DNA molecules is important because much evidence has indicated that transformations of chirality and diverse conformations of DNA are involved in a series of key biological events. Among these, enrichment of G-quadruplexes (GQs) in the genome, and the exploration of their multiple structures, has aroused great interest. Herein, we compared nearly 100 different sequences with 3'-tail sequences of variable length or different linkers or diverse loops and mutative ionic concentrations. All sequences were capable of forming stable GQs, with fluorescence signal enhancement upon binding with Δ- and Λ- [Ru(bpy)2(dppz-idzo)]2+ (Δ/Λ-1). Our results show that multiple factors, including the 3'-tail length, linkers, loop length and ionic concentration, regulate the enantioselectivity of GQs. Furthermore, molecular docking simulations revealed that chiral recognition of GQs depends on the binding site. To the best of our knowledge, this is the first systematic study regarding the regulation of multi-factors for GQ selectivity of chiral Ru-complexes. These results will serve as a useful reference for enantioselective recognition of genomic GQs and may facilitate the development of chiral anticancer agents for targeting GQs.

Early disease diagnosis is very important for the prevention or mitigation of metastasis. Effective and efficient methods are needed to improve the diagnosis and assessment of diseases. Thrombin is a biomarker for diagnosis of some diseases, such as pulmonary metastases and diseases associated with coagulation abnormalities. Lots of methods for detecting thrombin have been reported, however, most of them were based on a single aptamer and needed modification of aptamers, and label free sensors for thrombin detection based on an aptamer pair are challenging. In this work, we present three label free sensing platforms based on [Ru(bpy) 2 (o-mopip)] 2+ (bpy = 2,2-bipyridine; o-mopip = 2-(2-methoxylphenyl)imidazo[4,5-f][1,10]phenanthroline) (OMO) and graphene oxide (GO) for thrombin detection. Thrombin detection using our three label free sensors is accomplished by specific target recognition based on aptamer pair TBA1/TBA2-thrombin, single aptamer TBA1-thrombin or TBA2-thrombin, respectively. Direct readouts of the target recognition is achieved by restoration of the fluorescence of OMO prequenched by GO. All of the three sensing platforms exhibited high sensitivity and selectivity. Furthermore, all sensing platforms were successfully applied to thrombin analysis in diluted bovine serum. According to the thrombin dependent response of the three platforms, the sensing platform based on aptamer pair TBA1 and TBA2 showed the highest sensitivity, widest linearity, best selectivity and recovery in diluted serum to thrombin. These results show that the sensing platform based on an aptamer pair have great potential for clinical diagnosis of disease-related biomarkers.