壳聚糖谷氨酸涂层尼欧脂质体负载（S）-3-（3,4-二羟基苄基）哌嗪-2,5-二酮（环-Gly-L-DOPA 或 CG-Nio-CGLD）肽的抗结直肠癌活性。

(S)-3-(3,4-Dihydroxybenzyl) piperazine-2,5-dione (cyclo-Gly-L-DOPA or CG-Nio-CGLD) peptide loaded in Chitosan Glutamate-Coated Niosomes as anti-Colorectal cancer activity.

机构信息

Biotechnology Research Center, Faculty of Biological Sciences, Shahrekord Branch, Islamic Azad University, Shahrekord, Iran.

Department of Biology, Faculty of Biological Science, Tehran North Branch, Islamic Azad University, Tehran, Iran.

出版信息

BMC Pharmacol Toxicol. 2024 Aug 1;25(1):44. doi: 10.1186/s40360-024-00766-2.

DOI:10.1186/s40360-024-00766-2

PMID:39090674

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11295349/

Abstract

BACKGROUND

Colorectal cancer (CRC), now the second most prevalent malignant tumor worldwide, is more prevalent in young adults. In recent decades, there has been progress in creating anti-colorectal cancer medications, including cytotoxic compounds.

OBJECTIVES

Novel anticancer drugs are needed to surmount existing obstacles. A recent study investigated the effectiveness of novel formulations in preventing colorectal cancer.

METHODS

During this study, we assessed a new kind of niosome called cyclo-Gly-L-DOPA (CG-Nio-CGLD) made from chitosan glutamate. We evaluated the anti-colorectal cancer properties of CG-Nio-CGLD utilizing CCK-8, invasion assay, MTT assay, flow cytometry, and cell cycle analysis. The transcription of genes associated with apoptosis was analyzed using quantitative real-time PCR. At the same time, the cytotoxicity of nanomaterials on both cancer and normal cell lines was assessed using MTT assays. Novel anticancer drugs are needed to surmount existing obstacles. A recent study investigated the effectiveness of newly developed formulations in preventing colorectal cancer.

RESULTS

The Nio-CGLD and CG-Nio-CGLD were spherical mean diameters of 169.12 ± 1.87 and 179.26 ± 2.17 nm, respectively. Entrapment efficiency (EE%) measurements of the Nio-CGLD and CG-Nio-CGLD were 63.12 ± 0.51 and 76.43 ± 0.34%, respectively. In the CG-Nio-CGLD group, the percentages of early, late, necrotic, and viable CL40 cells were 341.93%, 23.27%, 9.32%, and 25.48%. The transcription of the genes PP53, cas3, and cas8 was noticeably higher in the treatment group compared to the control group (P > 0.001). Additionally, the treatment group had lower BCL2 and survivin gene expression levels than the control group (P < 0.01). Additionally, CG-Nio-CGLD formulations demonstrated a biocompatible nanoscale delivery mechanism and displayed little cytotoxicity toward the CCD 841 CoN reference cell line.

CONCLUSION

These findings indicate that chitosan-based noisome encapsulation may enhance the effectiveness of CG-Nio-CGLD formulations in fighting cancer.

摘要

背景

结直肠癌（CRC）是目前全球第二大常见恶性肿瘤，在年轻人中更为普遍。近几十年来，在开发抗癌药物方面取得了进展，包括细胞毒性化合物。

目的

需要新型抗癌药物来克服现有障碍。最近的一项研究调查了新型制剂预防结直肠癌的效果。

方法

在这项研究中，我们评估了一种由壳聚糖谷氨酸制成的新型囊泡，称为环-Gly-L-DOPA（CG-Nio-CGLD）。我们利用 CCK-8、侵袭实验、MTT 实验、流式细胞术和细胞周期分析评估 CG-Nio-CGLD 的抗结直肠癌特性。使用实时定量 PCR 分析与细胞凋亡相关的基因转录。同时，使用 MTT 实验评估纳米材料对癌细胞和正常细胞系的细胞毒性。需要新型抗癌药物来克服现有障碍。最近的一项研究调查了新型制剂预防结直肠癌的效果。

结果

Nio-CGLD 和 CG-Nio-CGLD 的平均粒径分别为 169.12±1.87nm 和 179.26±2.17nm。Nio-CGLD 和 CG-Nio-CGLD 的包封效率（EE%）分别为 63.12±0.51%和 76.43±0.34%。在 CG-Nio-CGLD 组中，CL40 细胞的早期、晚期、坏死和存活百分比分别为 341.93%、23.27%、9.32%和 25.48%。与对照组相比，治疗组中 PP53、cas3 和 cas8 基因的转录明显更高（P>0.001）。此外，治疗组的 BCL2 和 survivin 基因表达水平低于对照组（P<0.01）。此外，CG-Nio-CGLD 制剂表现出生物相容性的纳米级递药机制，对 CCD 841 CoN 参考细胞系表现出低细胞毒性。