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Overcoming Solubility Challenges: Liposomal Isocoq-Carbazole As a Promising Anti-Tumor Agent for Inoperable and Radiation-Insensitive Cancers.

CHEMBIOCHEM(2024)

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摘要
This study evaluated the potential of isoCoQ-Carbazole, a diheterocyclic analog of isoCA-4, as an anti-tumor agent. To overcome its low aqueous solubility, liposomes were developed as a delivery system for the compound. In vitro experiments showed that loaded liposomes exhibited similar activity to the free form on multiple human tumor cell lines. In vivo experiments using a palliative intratumoral injection chemotherapy approach further demonstrated that isoCoQ-Carbazole loaded liposomes significantly reduced tumor growth in a CA-4-resistant HT29 cell model, without inducing any observable toxicity or weight loss in the treated mice. These findings suggest that liposomal isoCoQ-Carbazole may hold promise as a potential therapeutic agent for the treatment of inoperable, radiation-insensitive cancers. IsoCoQ-Carbazole, an analog of isoCA-4 anti-tumor agent, is encapsulated into liposomes to overcome its low solubility. In vitro experiments show that loaded liposomes exhibit similar activity to the free form on several human tumor cell lines. In vivo experiments using a palliative intratumoral injection chemotherapy approach demonstrate that isoCoQ-Carbazole loaded liposomes significantly reduce tumor growth in a CA-4-resistant HT29 model. image
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关键词
cancer,combretastatins,heterocyclic compounds,cytotoxicity,liposomes
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