Department of Medical Microbiology and Parasitology, Universiti Putra Malaysia, 43400 UPM, Serdang Selangor, Malaysia.
Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai, 625 021, Tamil Nadu, India.
Sci Rep. 2017 Sep 8;7(1):10962. doi: 10.1038/s41598-017-09140-1.
Camptothecin (CPT) is an anti-cancer drug that effectively treats various cancers, including colon cancer. However, poor solubility and other drawbacks have restricted its chemotherapeutic potential. To overcome these restrictions, CPT was encapsulated in CEF (cyclodextrin-EDTA-FEO), a composite nanoparticle of magnetic iron oxide (FeO), and β-cyclodextrin was cross-linked with ethylenediaminetetraacetic acid (EDTA). This formulation improved CPT's solubility and bioavailability for cancer cells. The use of magnetically responsive anti-cancer formulation is highly advantageous in cancer chemotherapy. The chemical characterisation of CPT-CEF was studied here. The ability of this nano-compound to induce apoptosis in HT29 colon cancer cells and A549 lung cancer cells was evaluated. The dose-dependent cytotoxicity of CPT-CEF was shown using MTT. Propidium iodide and Annexin V staining, mitochondrial membrane depolarisation (JC-1 dye), and caspase-3 activity were assayed to detect apoptosis in CPT-CEF-treated cancer cells. Cell cycle analysis also showed G1 phase arrest, which indicated possible synergistic effects of the nano-carrier. These study results show that CPT-CEF causes a dose-dependent cell viability reduction in HT29 and A549 cells and induces apoptosis in colon cancer cells via caspase-3 activation. These data strongly suggest that CPT could be used as a major nanocarrier for CPT to effectively treat colon cancer.
喜树碱(CPT)是一种有效的抗癌药物,可有效治疗多种癌症,包括结肠癌。然而,较差的溶解性和其他缺点限制了其化疗潜力。为了克服这些限制,将 CPT 封装在 CEF(环糊精-EDTA-FEO)中,CEF 是磁性氧化铁(FeO)的复合纳米粒子,β-环糊精与乙二胺四乙酸(EDTA)交联。这种制剂提高了 CPT 对癌细胞的溶解性和生物利用度。使用磁性响应性抗癌制剂在癌症化疗中具有很高的优势。本研究对 CPT-CEF 的化学特性进行了研究。评估了这种纳米复合物在 HT29 结肠癌和 A549 肺癌细胞中诱导细胞凋亡的能力。通过 MTT 评估了 CPT-CEF 的剂量依赖性细胞毒性。通过碘化丙啶和 Annexin V 染色、线粒体膜去极化(JC-1 染料)和 caspase-3 活性测定,检测 CPT-CEF 处理的癌细胞中的细胞凋亡。细胞周期分析还显示 G1 期阻滞,这表明纳米载体可能具有协同作用。这些研究结果表明,CPT-CEF 可导致 HT29 和 A549 细胞中细胞活力呈剂量依赖性降低,并通过 caspase-3 激活诱导结肠癌细胞凋亡。这些数据强烈表明,CPT 可用作 CPT 的主要纳米载体,以有效治疗结肠癌。