Rationally designed Ru(II) metallacycles with tunable imidazole ligands for synergistical chemo-phototherapy of cancer.

Herein, we construct a series of Ru(II) metallacycles with multimodal chemo-phototherapeutic properties, which exhibited much higher anticancer activity and better cancer-cell selectivity than cisplatin. The antitumor mechanism could be ascribed to the activation of caspase 3/7 and the resulting apoptosis. These results open new possibilities for Ru(II) metallacycles in biomedicine.

NIR-II Emissive Ru(II) Metallacycle Assisting Fluorescence Imaging and Cancer Therapy.

Despite the success of emissive Ruthenium (Ru) agents in biomedicine, problems such as the visible-light excitation/emission and single chemo- or phototherapy modality still hamper their applications in deep-tissue imaging and efficient cancer therapy. Herein, an second nearinfrared window (NIR-II) emissive Ru(II) metallacycle (Ru1000, λem  = 1000 nm) via coordination-driven self-assembly is reported, which holds remarkable deep-tissue imaging capability (≈6 mm) and satisfactory chemo-phototherapeutic performance. In vitro results indicate Ru1000 displays promising cellular uptake, good cancer-cell selectivity, attractive anti-metastasis properties, and remarkable anticancer activity against various cancer cells, including cisplatin-resistant A549 cells (IC50  = 3.4 × 10-6  m vs 92.8 × 10-6  m for cisplatin). The antitumor mechanism could be attributed to Ru1000-induced lysosomal membrane damage and mitochondrial-mediated apoptotic cell death. Furthermore, Ru1000 also allows the high-performance in vivo NIR-II fluorescence imaging-guided chemo-phototherapy against A549 tumors. This work may provide a paradigm for the development of long-wavelength emissive metallacycle-based agents for future biomedicine.

Structural elucidation and α­glucosidase inhibitory activity of a new xanthone glycoside from Lomatogonium rotatum (L.) Fries es Nym.

A new xanthone glycoside, 1,8-dihydroxyl-2,5-dimethoxy-xanthone-6-O-ß-D-glucoside (1), along with two known xanthone glycosides and two flavonoid glycosides were isolated from the aerial parts of Lomatogonium rotatum (L.) Fries es Nym. The structure of 1 was elucidated by analysis of its spectroscopic data, including UV, IR, HR-ESI-MS and extensive 1 D and 2 D NMR techniques. In vitro test, compound 1 behaved similarity to swertianolin against α­glucosidase and more potent inhibitory effects than the positive control, acarbose.

NIR-II emissive multifunctional AIEgen with single laser-activated synergistic photodynamic/photothermal therapy of cancers and pathogens.

Despite the wide application of the traditional NIR-I phototheranostic platforms in basic research and clinical studies, problems such as tissue scattering, auto-fluorescence combined with aggregation caused quenching hamper precise image-guided phototherapy. Herein, we developed a multifunctional NIR-II phototheranostic platform using a novel AIE-based dye (ZSY-TPE) for single laser-activated imaging-guided combined photothermal and photodynamic therapies of tumors and pathogens. As confirmed through in vivo studies, the ZSY-TPE dots displayed precise and efficient high-performance NIR-II imaging-guided combination phototherapy against 4T1 tumor as well as S. aureus-infected mice models without any noticeable side effects. The current study demonstrates ZSY-TPE as a powerful phototheranostic platform for precise NIR-II fluorescence/PA imaging and synergistic photodynamic/photothermal therapy of tumors and bacterial infections.

Fabrication of a Tyrosine-Responsive Liquid Quantum Dots Based Biosensor through Host-Guest Chemistry.

Design and fabrication of smart liquid quantum dots (LQDs) with high biomolecule selectivity and specificity remains a challenge. Herein, a multifunctional calix[4]arene derivative (PCAD) was rationally designed and applied to fabricate a Tyr-responsive CdSe-LQD system through host-guest chemistry. Such a biosensor displays an outstanding fluorescence/macroscopic response for Tyr and reversible fluidic features due to the hydrogen interaction between the PCAD of CdSe-LQDs and Tyr. These excellent results highlighted CdSe-LQDs as a promising platform for biological molecule recognition and separation in the future.