Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer

被引：3

作者：

Sharma, Mani ^{[1
,3
]}

Ambadipudi, S. S. S. S. Sudha ^{[1
]}

Chouhan, Neeraj Kumar ^{[2
,3
]}

Nayak, V. Lakshma ^{[1
]}

Pabbaraja, Srihari ^{[2
,3
]}

Andugulapati, Sai Balaji ^{[1
,3
]}

Sistla, Ramakrishna ^{[1
,3
]}

机构：

[1] CSIR Indian Inst Chem Technol IICT, Dept Appl Biol, Hyderabad 500007, India

[2] CSIR Indian Inst Chem Technol CSIR IICT, Dept Organ Synth & Proc Chem, Hyderabad 500007, India

[3] Acad Sci & Innovat Res AcSIR, Ghaziabad 201002, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2024年 / 97卷

关键词：

Cationic lipid; Amphiphile; Melphalan; Liposome; Drug delivery; Anti-cancer; DNA-DAMAGE; CELL-CYCLE;

D O I：

10.1016/j.bmcl.2023.129549

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Therapeutically active lipids in drug delivery systems offer customization for enhanced pharmaceutical and biological effects, improving safety and efficacy. Biologically active N, N-didodecyl-3,4-dimethoxy-N-methyl-benzenaminium lipid (Q) was synthesized and employed to create a liposome formulation (FQ) encapsulating melphalan (M) through a thin film hydration method. Synthesized cationic lipids and their liposomal formulation underwent characterization and assessment for additive anti-cancer effects on myeloma and melanoma cancer cell lines. These effects were evaluated through various studies, including cytotoxicity assessments, cell cycle arrest analysis, apoptosis measurements, mitochondrial membrane potential depolarization, DNA fragmentation, and a significant reduction in tumorigenic potential, as evidenced by a decrease in both the number and percentage area of cancer spheroids.

引用

页数：9

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