Metal organic frameworks (MOFs) are widely used in drug carrier research due to their tunability.

Cucurbit[10]uril (Q[10] or CB[10]), with the largest rigid cavity (ca. 1.0 nm) yet characterized in the cucurbiturils family, and indeed among all artificial macrocyclic receptors to date, has been successfully exploited to construct a novel Q[10]-[CdCl]-based pillared diamond porous supramolecular framework. Single-crystal X-ray diffraction analysis revealed that the three-dimensional open-nanotube-type porous framework is constructed from free Q[10] molecules and [CdCl] cluster anions through the outer surface interactions of Q[10]. Notably, the Q[10]-based porous framework host can accommodate guest dyes, such as rhodamine B (G1), pyrenemethanamine hydrochloride (G2), and bathocuproine hydrochloride (G3), to form solid materials with efficient red-green-blue (RGB) fluorescence. This work not only exemplifies a facile approach for the construction of macrocycle-based porous frameworks but also offers a simple, lower cost, yet still highly efficient means of preparing multi-emitting, including white-light-emitting, solid luminescent materials.

Crystal structure of compound 1 (CIF) Crystal structure of compound 2 (CIF) Crystal structure of compound 3 (CIF) Crystal structure of compound 4 (CIF) Crystal structure of compound 5 (CIF) Crystal structure of compound 6 (CIF) Experimental procedure, Crystal data, PXRD patterns, EDS data (PDF)

Combination of antiangiogenesis and chemotherapy holds vast promise for effective inhibition of tumor proliferation and invasion. Herein, a multifunctional self-assembled nanosystem consisting of amphiphilic c(RGDyK)-functionalized low-molecular-weight heparin-gambogic acid conjugate (cRHG) is developed, using c(RGDyK) peptide as αv β3 integrin targeting moiety to realize a double-targeted delivery to both tumor cells and angiogenic vasculature. cRHG with a markedly decreased anticoagulant activity can self-assemble into nanosized particles (around 150 nm). cRHG nanoparticles effectively inhibit vascular endothelial growth factor (VEGF)-triggered tube-like formation of HUVEC and neovascularization of subcutaneous Matrigel plugs. More importantly, the targeting ability of cRHG nanoparticles is revealed by their efficient internalization by αv β3 integrin-positive cells (U87MG and HUVEC) in vitro and obvious accumulation of Cy7/cRHG in the tumor site with strong fluorescence signals in both cancer cells and neovasculature. Besides, cRHG maintains the in vitro cytotoxic activity of gambogic acid, while achieving the highest in vivo antitumor activity in U87MG mouse xenograft model and displaying better safety profile than free drugs solutions. Mechanistic investigations reveal the substantial inhibition of hypoxia-inducible factor-1 alpha, VEGF, and CD31 expression by cRHG nanoparticles with remarkable down-regulation of VEGFR2 phosphorylation. These results suggest that cRHG nanoparticles provide a versatile nanoplatform for efficacious combinatorial tumor therapy.

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