Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
J Photochem Photobiol B. 2023 Aug;245:112748. doi: 10.1016/j.jphotobiol.2023.112748. Epub 2023 Jun 16.
A novel croconic acid-bisindole dye CR-630 with a morpholine ring showed good water-solubility and obvious lysosome-targeting. The protonation of the nitrogen atom in the indole and lysosome-targeting of morpholine ring let it exhibit stronger pH-responsive NIR/PA imaging and photothermal effect in the lysosome acidic microenvironment (pH 4.0-5.5) than in the tumor acidic microenvironment. In the animal study, compound CR-630 could NIRF/PA image in the tumor tissues in 1.5-2.0 h, effectively inhibit the growth of the tumor, and even ablate the tumor at the drug dose of 1 mg/kg. It also demonstrated good biosafety. This study gives a new idea to develop water-solubility organic dyes with lysosome targeting, stronger pH-responsive NIRF/PA imaging and PTT for breast cancer.
一种具有吗啉环的新型克罗酮双吲哚染料 CR-630 具有良好的水溶性和明显的溶酶体靶向性。吲哚氮原子的质子化和吗啉环的溶酶体靶向性使其在溶酶体酸性微环境（pH 4.0-5.5）中表现出比肿瘤酸性微环境更强的 pH 响应近红外/光声成像和光热效应。在动物研究中，化合物 CR-630 可以在 1.5-2.0 小时内在肿瘤组织中进行 NIRF/PA 成像，有效抑制肿瘤生长，甚至在 1mg/kg 的药物剂量下消融肿瘤。它还表现出良好的生物安全性。本研究为开发具有溶酶体靶向性、更强 pH 响应性近红外/光声成像和 PTT 的水溶性有机染料用于乳腺癌提供了新的思路。
