Anastomotic thrombosis prevalently causes anastomosis failure, accompanied with ischemia and necrosis, the early diagnosis of which is restricted by inherent shortcomings of traditional imaging techniques in clinic and lack of appropriate prodromal biomarkers for thrombosis initiation. Herein, a fresh thrombus-specific molecular event, protein disulfide isomerase (PDI) is innovatively chosen as the activating factor, and a thrombosis targeting and PDI-responsiveturn-on near infrared II (NIR-II) fluorescence nanoprobe is firstly developed. The supramolecular complex-based nanoprobe IR806-PDA@BSA-CREKA is fabricated by assembling NIR-II emitting cyanine derivative IR806-PDA with bovine serum albumin (BSA), which could ameliorate the stability and pharmacokinetics of the nanoprobe, addressing thecontradiction in the balance of brightness and biocompatibility. The NIR-II-off nanoprobe exhibits robust turn-on NIR-II fluorescence upon PDI-specific activation, in vitro and in vivo. Of note, the constructed nanoprobe demonstrates superior photophysical stability, efficient fibrin targeting peptide-derived thrombosis binding and a maximum signal-to-background ratio (SBR) of 9.30 for anastomotic thrombosis in NIR-II fluorescent imaging. In conclusion, the exploited strategy enables positive visualized diagnosis for anastomotic thrombosis and dynamic monitoring for thrombolysis offresh fibrinolytic thrombus, potentially contributes a novel strategy for guiding the therapeutic selection between thrombolysis and thrombectomy for thrombosis treatment in clinic.
We demonstrate that reactions between various 1-indanones and (SS)-N-tert-butanesulfinyl-(3,3,3)-trifluoroacetaldimine, conducted in the presence of catalytic amounts of LDA, occur with virtually complete stereochemical outcome, offering reliable and generalized access to biologically relevant β-trifluoromethyl-β-amino indanone derivatives. The products can be isolated in diastereomerically pure form simply by washing the crude reaction mixture with hexanes, underscoring practicality of the present method.
Semiconducting polymer nanoparticles (SPNs) have been widely applied for phototheranostics. However, the disadvantage of in vivo long-term metabolism greatly suppresses the clinical application of SPNs. To improve the metabolic rate and minimize the long-term toxicity of SPNs, biodegradable semiconducting polymers (BSPs), whose backbones may be degraded under certain conditions, have been designed. This review summarizes recent advances in BSP-constructed nanoparticles (BSPNs) for phototheranostics. BSPs are divided into two categories: conjugated backbone degradable BSPs (CBD-BSPs) and non-conjugated backbone degradable BSPs (NCBD-BSPs), based on the feature of chemical structure. The biological applications, including cancer imaging and combination therapy, of these BSPNs are described. Finally, the conclusion and future perspectives of this field are discussed.
A multifunctional semiconducting nanoagonist with high photothermic conversion efficiency (86.2%) and alkyl radical generation ability was developed. The nanoagonist demonstrated excellent anticancer performance through NIR-II light-triggered photothermic/thermodynamic combinational therapy both in vitro and in vivo.
Abstract The novel cascade strategy for trifunctionalization of an acetylene bond proceeds via a sequence involving iodination, aryl migration, decarboxylation, and a second iodination.
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