112661-85-5Relevant articles and documents
PDT (photodynamics therapy) prodrug based on carbonylated polycaprolactone as well as preparation method and application of PDT prodrug
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Paragraph 0040-0043, (2020/06/20)
The invention discloses a PDT (photodynamics therapy) prodrug based on carbonylated polycaprolactone. The structure of the PDT prodrug is represented in the description, wherein x is equal to 10-40, and y is equal to 10-40. The PDT prodrug based on carbonylated polycaprolactone is an amphiphilic polymer and can be prepared into micelles. A cell experiment proves that compared with pure 5-aminolevulinic acid, the content of the prodrug micelles converted into protoporphyrin is higher, and the prodrug has better destruction property on tumor cells. 5-aminolevulinic acid is introduced into functionalized polycaprolactone with a chemical grafting method, esterification of the 5-aminolevulinic acid is realized, lipid solubility and stability of 5-aminolevulinic acid are improved, and the prodrug has better targeting performance, higher conversion rate and better photodynamic effect.
Hydroxypyridinone and 5-Aminolaevulinic Acid Conjugates for Photodynamic Therapy
Battah, Sinan,Hider, Robert C.,MacRobert, Alexander J.,Dobbin, Paul S.,Zhou, Tao
, p. 3498 - 3510 (2017/05/05)
Photodynamic therapy (PDT) is a promising treatment strategy for malignant and nonmalignant lesions. 5-Aminolaevulinic acid (ALA) is used as a precursor of the photosensitizer, protoporphyrin IX (PpIX), in dermatology and urology. However, the effectiveness of ALA-PDT is limited by the relatively poor bioavailability of ALA and rapid conversion of PpIX to haem. The main goal of this study was to prepare and investigate a library of single conjugates designed to coadminister the bioactive agents ALA and hydroxypyridinone (HPO) iron chelators. A significant increase in intracellular PpIX levels was observed in all cell lines tested when compared to the administration of ALA alone. The higher PpIX levels observed using the conjugates correlated well with the observed phototoxicity following exposure of cells to light. Passive diffusion appears to be the main mechanism for the majority of ALA-HPOs investigated. This study demonstrates that ALA-HPOs significantly enhance phototherapeutic metabolite formation and phototoxicity.
PYRIDINONE COMPOUNDS FOR USE IN PHOTODYNAMIC THERAPY
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Paragraph 0094, (2015/08/04)
A compound which is a compound of formula (I) or any salt thereof: wherein R1 is a Ci-C6 alkyl group, R2 is H or a Ci-C6 alkyl group, R3 is H or a Ci-C6 alkyl group, and n is an integer from 0 to 5.