Université de Limoges, PEIRENE EA 7500, 87060 Limoges, France.
Université de Limoges, PEIRENE EA 7500, 87060 Limoges, France.
Bioorg Med Chem Lett. 2021 Jun 1;41:128024. doi: 10.1016/j.bmcl.2021.128024. Epub 2021 Apr 9.
Two protoporphyrin IX (PpIX) adamantane derivatives were synthesized and then metallated with zinc. The Zn-PpIX derivatives, exhibiting a high singlet oxygen quantum yield, were tested for their photodynamic activity against the HT-29 cell line. In order to enhance their water-solubility and their cellular bioavailability, these photosensitizers were encapsulated into the hydrophobic cavity of cyclodextrins (CD) previously attached to cellulose nanocrystals (CNCs) via electrostatic interactions. Under illumination, the encapsulated adamantanyl-porphyrins exerted an enhanced in vitro cytotoxicity, as compared with the corresponding free photosensitizers.
合成了两种原卟啉 IX（PpIX）金刚烷衍生物，然后用锌进行金属化。具有高单线态氧量子产率的 Zn-PpIX 衍生物被测试其对 HT-29 细胞系的光动力活性。为了提高它们的水溶性和细胞生物利用度，这些光敏剂被包封到先前通过静电相互作用附着在纤维素纳米晶体（CNC）上的环糊精（CD）的疏水性空腔中。在光照下，与相应的游离光敏剂相比，包封的金刚烷基卟啉在体外表现出增强的细胞毒性。
