التفاصيل البيبلوغرافية
| العنوان: |
Hierarchical Self‐Assembly of BODIPY Dyes as a Tool to Improve the Antitumor Activity of Capsaicin in Prostate Cancer. |
| المؤلفون: |
Sampedro, Angel, Ramos‐Torres, Ágata, Schwöppe, Christian, Mück‐Lichtenfeld, Christian, Helmers, Ingo, Bort, Alicia, Díaz‐Laviada, Inés, Fernández, Gustavo |
| المصدر: |
Angewandte Chemie International Edition; Dec2018, Vol. 57 Issue 52, p17235-17239, 5p |
| مصطلحات موضوعية: |
ANTINEOPLASTIC agents, CAPSAICIN, PROSTATE cancer, CANCER treatment, ANALGESICS |
| مستخلص: |
Capsaicin (CAP) has been long known for its analgesic properties and more recently for its antitumor activity in various cell types. However, its pungency and the high doses needed to achieve a significant activity have precluded its application in cancer therapy. Herein, we propose a straightforward novel strategy to improve the antitumor effect of CAP based on the enhancement of its aggregation propensity in aqueous media by covalent attachment of a BODIPY (BDP) dye. The target CAP‐BDP 1 self‐assembles in aqueous solutions into weakly fluorescent globular assemblies that become highly emissive upon cell uptake‐induced disassembly. Remarkably, due to the improved delivery to the tumour tissue upon aggregation, we have succeeded in reducing the doses of CAP‐based drugs in vivo in prostate cancer by two orders of magnitude while maintaining a substantial antitumor activity. Spice up your life! Covalent attachment of a fluorescent BODIPY dye has been exploited to enhance the aggregation propensity of capsaicin—the major active component of chili peppers—in aqueous media. Due to the improved delivery of active capsaicin‐based molecules to the tumour tissue upon aggregation, the effective doses for prostate cancer treatment could be successfully reduced by two orders of magnitude. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
