Efficacy of Biologically Active Food Supplements for People with Atherosclerotic Vascular Changes

The current paper deals with the development of a new biologically active food supplement (BAFS) aimed at treating atherosclerosis. Since atherosclerosis is considered to be a disease of aging, the composition of the supplement includes such essential minerals as magnesium and potassium, which are commonly used to prevent atherosclerosis, as well as vitamins C, E and the B-group vitamins in order to address the needs of the elderly. The authors outline the supplement-manufacturing technology and discuss the clinical trial undertaken by patients, aged about 60 years, with peripheral atherosclerosis. The research methodology focuses on studying the effectiveness of the developed supplement by assessing the influence of the active ingredients on treating metabolic disorders. To establish the efficacy of the supplement, blood tests, ultrasound and physical examinations were applied. The combination therapy resulted in improved metabolism and an overall better performance of the cardiovascular system; therefore, the BASF can be recommended as part of combination therapy to prevent and treat atherosclerotic and age-related changes in blood vessels.     

Application of Cleavable Linkers to Improve Therapeutic Index of Radioligand Therapies

Radioligand therapy (RLT) is an emergent drug class for cancer treatment. The dose administered to cancer patients is constrained by the radiation exposure to normal tissues to maintain an appropriate therapeutic index. When a radiopharmaceutical or its radiometabolite is retained in the kidneys, radiation dose deposition in the kidneys can become a dose-limiting factor. A good exemplar is [¹⁷⁷Lu]Lu-DOTATATE, where patients receive a co-infusion of basic amino acids for nephroprotection. Besides peptides, there are other classes of targeting vectors like antibody fragments, antibody mimetics, peptidomimetics, and small molecules that clear through the renal pathway. In this review, we will review established and emerging strategies that can be used to mitigate radiation-induced nephrotoxicity, with a focus on the development and incorporation of cleavable linkers for radiopharmaceutical designs. Finally, we offer our perspectives on cleavable linkers for RLT, highlighting future areas of research that will help advance the technology.     

自由电子激光的医学应用

自由电子激光这种新型光源非常适合于医学应用。通过对医用自由电子激光器的简要介绍,探讨了自由电子激光与人体组织的相互作用及其在医学上的应用前景。     

Detection and recognition of cancer cells in vivo

A fundamentally new recognition method of bio-objects (e.g., cancer cells as the most important case of them) that escape the immune system supervision control is suggested. It is proposed to use a unified complex consisting of several molecular groups (e.g., antibodies or their fragments) bound with each other. Binding targets are localized on the surface of this bio-object. The choice of the targets is determined by antigen profiling being expressed on the surface of these bio-objects. The recognition efficiency appears to be notably higher than in a situation when molecular groups do not form a unified complex and act separately.     

Synthesis of Cationic Dumbbell-shaped Fullerene Nanostructures as Potential Photodynamic Sensitizers

A design of novel hydrophilic tetracationic dumbbell-shaped [60]fullerene nanostructures was made by balancing the hydrophilicity and hydrophobicity characteristics of the fullerene adduct for their potential application as photodynamic sensitizers in the PDT treatment. A sequential protection-deprotection reaction pathway was applied for the functional differentiation between primary and secondary amine moieties of pentaethylene hexamine. Synthesis of the target molecule involves two key steps of unsymmetrical esterification and amidation of malonic acid and subsequent fullerenation. The synthetic strategy was accomplished using mild reaction conditions in the intermediate molecule preparation and led a moderate overall product yield.     

Synthesis and photophysical evaluations of β-fused uracil-porphyrin derivatives

New β-fused uracil-porphyrin conjugates were synthesized by the tetramerization of uracil-pyrroles under acidic conditions. Two different synthetic approaches were systematically studied in order to evaluate their efficiency, as well as the possibility to obtain a single regioisomer. Metallation effects were studied for aggregation in solution, and preliminary photophysical experiments were also performed in order to evaluate the potential of these new compounds.     

Red/Near‐Infrared Emissive Metalloporphyrin‐Based Nanodots for Magnetic Resonance Imaging‐Guided Photodynamic Therapy In Vivo

Near‐infrared emissive (NIR) porphyrin‐implanted carbon nanodots (PCNDs or MPCNDs) are prepared by selectively carbonization of free base or metal complexes [M = Zn(II) or Mn(III)] of tetra‐(meso‐aminophenyl)porphyrin in the presence of citric acid. The as‐prepared nanodots exhibit spontaneously NIR emission, small size, good aqueous dispersibility, and favorable biocompatibility characteristic of both porphyrins and pristine carbon nanodots. The subcellular localization experiment of nanodots indicates a lysosome‐targeting feature. And the in vitro photodynamic therapy (PDT) results on HeLa cells indicate the nanodots alone have no adverse effect on tumor cells, but display remarkable photodynamic efficacy upon irradiation. Moreover, MnPCNDs containing paramagnetic Mn(III) ions, which possesses good biocompatibility, NIR luminescence, and magnetic resonance imaging and efficient singlet oxygen production, are further studied in magnetic resonance imaging‐guided photodynamic therapy in vivo.