Center from Malaria and Other Tropical Diseases (CMDT), Institute of Hygiene and Tropical Medicine (IHMT), New University of Lisbon, Lisbon, Portugal.
In Vivo. 2013 Sep-Oct;27(5):605-10.
Chlorpromazine (CPZ) was exposed to a 266 nm laser beam for different periods of time ranging from minutes to 24 h. At intervals, the products from irradiation were evaluated by thin-layer chromatography (TLC) and evaluated for their activity against mycobacteria of human interest (Mycobacterium tuberculosis, M. avium, M. intracellulare and their corresponding reference strains or clinical isolates). With the exception of the M. avium 47/07 clinical strain, the products produced from the irradiation of CPZ for 4 h had greater activity against M. intracellulare ATCC, M. avium ATCC, H37Rv and the Multidrug-resistant tuberculosis (MDR-TB) strains as opposed to that produced by the unirradiated control. The level of products from the 4-h exposure of CPZ remained the same throughout the next 20 h of irradiation. Of significant note is that the irradiation products of CPZ had lower in vitro cytotoxicity against human cells, suggesting that this approach may be useful for the development of compounds more bioactive than the parental species.
氯丙嗪（CPZ）暴露于 266nm 激光束下不同的时间段，从几分钟到 24 小时不等。在照射过程中，每隔一段时间通过薄层色谱法（TLC）评估产物，并评估其对人类感兴趣的分枝杆菌（结核分枝杆菌、鸟分枝杆菌、胞内分枝杆菌及其相应的参考菌株或临床分离株）的活性。除了鸟分枝杆菌 47/07 临床株外，CPZ 照射 4 小时产生的产物对 ATCC 胞内分枝杆菌、ATCC 鸟分枝杆菌、H37Rv 和耐多药结核分枝杆菌（MDR-TB）菌株的活性大于未照射对照产物。CPZ 照射 4 小时产生的产物水平在接下来的 20 小时照射过程中保持不变。值得注意的是，CPZ 的辐照产物对人细胞的体外细胞毒性较低，这表明这种方法可能有助于开发比母体化合物更具生物活性的化合物。
