Single Nano-Sized Metal-Organic Framework for Bio-Nanoarchitectonics with In Vivo Fluorescence Imaging and Chemo-Photodynamic Therapy.

Theranostics is an emerging technique for cancer treatments due to its safety and high efficiency. However, the stability, efficiency, and convenience of preparation are the main challenges for developing theranostics. Here we describe a one-pot process for biocompatible metal-organic framework (MOF)-based theranostics. The ligand H2L designed for the MOF enables both red fluorescence emission and photodynamic therapy (PDT). The frame and regular channel structure of H2L-MOF empower the theranostics with good drug delivery performance, and the uniform and nano-sized particles facilitate the in vivo imaging/therapy applications. In vivo fluorescence imaging and in vitro chemo-photodynamic therapy were achieved with the MOF without any further modification. Our results reveal an effective strategy to achieve multifunctional theranostics by the synergistic action of the organic ligand, metal node, and channel structure of MOF nanoparticles.

Acute effects of the translocator protein drug ligand FGIN-1-27 on serum testosterone and luteinizing hormone levels in male Sprague-Dawley rats†.

We reported that FGIN-1-27 (N,N-dihexyl-2-(4-fluorophenyl)indole-3-acetamide, FGIN), a synthetic ligand for translocator protein (TSPO, 18 kDa), increased serum testosterone levels in young and aged Brown Norway rats after its administration daily for 10 days. It is not known, however, how soon after treatment with FGIN serum testosterone rises, how long levels remain elevated after cessation of treatment, or whether the drug acts solely through TSPO. Adult Sprague-Dawley male rats received a single ip dose of FGIN (1 mg/kg BW). Serial blood samples were collected, and serum testosterone and luteinizing hormone (LH) were assessed hourly throughout 24 h. Testosterone concentration was maximal by 3 h, remained significantly higher than the controls at 10 h, and returned to the control level by 24 h. Consistent with the in vivo study, culturing isolated Leydig cells with either FGIN (40 µM) or LH (0.1 ng/ml) resulted in significantly increased testosterone production by 30 min, and the stimulatory effects persisted through 48 h. At a very early (15 min) treatment time, however, FGIN significantly increased testosterone production but LH had not yet done so. Surprisingly, in vivo treatment with FGIN not only increased serum testosterone but also serum LH concentration, raising the possibility that FGIN may increase serum testosterone concentration by dual mechanisms.