Modular Assembly of Heterotrifunctional Molecules Enabled by Iodosulfonylation of Allenes and Subsequent Amination.

Beyond the rapid achievements of therapeutic heterobifunctional molecules, some recent efforts have focused on constructing heterotrifunctional molecules, aiming at developing more potent and selective therapeutic agents or emerging additional functions to heterobifunctional molecules. However, the synthesis of these complex molecules requires a specific design and lengthy steps. We have developed a two-step strategy for the modular construction of heterotrifunctional molecules, enabled by the sustainable and convenient iodosulfonylation of allenes followed by S2'-selective amination.

Temperature-responsive two-dimensional polydopamine hydrogel: Preparation, mechanisms, and applications in cancer treatment.

Temperature-responsive hydrogels are advanced materials that exhibit significant physical or chemical changes in response to temperature variations. When the temperature reaches a specific threshold, these hydrogels alter their properties accordingly. They offer significant advantages in cancer therapy, including precise control over drug release, minimized toxicity, improved therapeutic efficacy, and biodegradability.

Ring Transformation of Cyclopropenes to Benzo-Fused Five-Membered Oxa- and Aza-Heterocycles via a Formal [4+1] Cyclization.

In the context of the growing importance of heterocyclic compounds across various disciplines, numerous strategies for their construction have emerged. Exploiting the distinctive properties of cyclopropenes, this study introduces an innovative approach for the synthesis of benzo-fused five-membered oxa- and aza-heterocycles through a formal [4+1] cyclization and subsequent acid-catalyzed intramolecular O- to N- rearrangement. These transformations exhibit mild reaction conditions and a wide substrate scope.

Homologous polydopamine ameliorates haemolysis of melittin for enhancing its anticancer efficacy.

Despite exhibiting potent anticancer activity, the strong hemolytic properties of melittin (MEL) significantly restrict its delivery efficiency and clinical applications. To address this issue, we have devised a strategy wherein homologous dopamine (DA), an essential component of bee venom, is harnessed as a vehicle for the synthesis of MEL-polydopamine (PDA) nanoparticles (MP NPs). The ingenious approach lies in the fact that MEL is a basic polypeptide, and the polymerization of DA is also conducted under alkaline conditions, indicating the distinctive advantages of PDA in MEL encapsulation.

Oxygen-evolving hollow polydopamine alleviates tumour hypoxia for enhancing photodynamic therapy in cancer treatment.

Hypoxia, a characteristic hallmark of solid tumours, restricts the therapeutic effect of photodynamic therapy (PDT) for cancer treatment. To address this issue, a facile and nanosized oxygen (O) bubble template is established by mixing oxygenated water and water-soluble solvents for guiding hollow polydopamine (HPDA) synthesis, and O is encapsulated in the cavity of HPDA. HPDA with abundant catechol is designed as a carrier for zinc phthalocyanine (ZnPc, a boronic acid modified photosensitizer) borate ester bonds to fabricate nanomedicine (denoted as HZNPs).

Oxyhemoglobin nano-recruiter preparation and its application in biomimetic red blood cells to relieve tumor hypoxia and enhance photodynamic therapy activity.

Photodynamic therapy (PDT) is strongly O2 dependent. Therefore, its therapeutic effects are seriously hindered in hypoxic tumors. Red blood cells are responsible for delivering O2 in the blood.

Multiple Functions Integrated inside a Single Molecule for Amplification of Photodynamic Therapy Activity.

Nitric oxide (NO) can play both prosurvival and prodeath roles in photodynamic therapy (PDT). The generation efficiency of peroxynitrite anions (ONOO), by NO and superoxide anions (O), significantly influenced the outcome. Reports indicated that such efficiency is closely related to the distance between NO and O.

Drug-Controlled Release Based on Complementary Base Pairing Rules for Photodynamic-Photothermal Synergistic Tumor Treatment.

Controlled drug release systems can enhance the safety and availability but avoid the side effect of drugs. Herein, the concept of DNA complementary base pairing rules in biology is used to design and prepare a photothermal-triggered drug release system. Adenine (A) modified polydopamine nanoparticles (A-PDA, photothermal reagent) can effectively bind with thymine (T) modified Zinc phthalocyanine (T-ZnPc, photosensitizer) forming A-PDA = T-ZnPc (PATP) complex based on A = T complementary base pairing rules.

Design and synthesis of thymine modified phthalocyanine for Aβ protofibrils photodegradation and Aβ peptide aggregation inhibition.

The formation and accumulation of toxic amyloid beta (Aβ) protofibrils in brain is recognized as the pathological hallmark of alzheimer's disease (AD). Recent research indicated that photodynamic therapy (PDT) has potential to treat AD because reactive oxygen species (ROS) generated by photosensitizers (PS) could degrades Aβ protofibrils. Al and Fe were found at markedly high levels on and around Aβ protofibrils comparing with the normal part of brain.

Breaking the reduced glutathione-activated antioxidant defence for enhanced photodynamic therapy.

Photodynamic therapy (PDT) has been applied in cancer treatment by utilizing reactive oxygen species (ROSs) to kill cancer cells. However, a high concentration of reduced glutathione (GSH) is present in cancer cells and can consume ROSs and sharply reduce the PDT activity. To address this problem, herein, we synthesized a thymine modified Zn phthalocyanine (ZnPc, a monomer and an active form for PDT) and prepared its nanoparticle form (an aggregator and an inactive form) with Hg providing the driving force for the "thymine-Hg-thymine" interaction.