研究动态
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新颖的非脂质体包埋2,5-二酮肽酸(BHPPD):合成、配方及其抗乳腺癌活性研究。

Novel Niosome-Encapsulated 2,5-Diketopiperazine (BHPPD): Synthesis, Formulation, and Anti-breast Cancer Activity.

发表日期:2023 Aug 25
作者: Hedieh Ghourchian, Renzon Daniel Cosme Pecho, Maryam Karimi-Dehkordi, Aynaz Mazandarani, Ghazal Ghajari, Tohid Piri-Gharaghie
来源: Genes & Diseases

摘要:

在此研究过程中,我们开发、合成和评估了一种全新的散发臭味的封装的2,5-二酮肽(BHPPD)。利用CCK-8、入侵筛选、MTT试验、流式细胞术和细胞周期分析,我们评估了封装BHPPD的散发体对乳腺癌的抗肿瘤特性。利用定量实时PCR和MTT试验测定了凋亡相关基因的表达和细胞毒性。这个药物结合亲和力的荟萃分析显示对肠道蛋白酶具有显著的结合能力。自由BHPPD、F1散发体BHPPD和F2散发体BHPPD的球形平均直径分别为108.91 ± 4.2 nm,129.13 ± 7.2 nm和149.43 ± 3.2 nm。此外,发现BHPPD散发体的F1制剂的封装效率(EE%)分别为81.01 ± 0.09%和70.22 ± 0.13%。早期、晚期、坏死和存活的MCF-7细胞在F1制剂的细胞中的比例分别为38.24%、34.34%、4.02%和23.40%。与对照组相比,治疗组的基因P57、Prkca、MDM4、Map2k6和FADD的表达显著增加(P < 0.001)。此外,与对照细胞相比,治疗组细胞的BCL2和存活基因表达更低(P < 0.001)。此外,封装在散发体中的BHPPD制剂显示了一种生物相容的纳米传递方法,并在HEK-293标准细胞系中表现出较小的细胞毒性。根据结果,封装在散发体中的BHPPD制剂可能有助于提高抗癌活性。© 2023. 作者,独家许可给Springer Science+Business Media, LLC,Springer Nature的一部分。
In the course of this investigation, a brand-new noisome-encapsulated 2,5-diketopiperazine (BHPPD) was developed, synthesized, and assessed. Utilizing CCK-8, invasion screens, MTT test, flow cytometry, and cell cycle analysis, we evaluated the anti-breast cancer properties of niosome-encapsulated BHPPD. Apoptosis-related gene expression and cytotoxicity was measured using quantitative real-time PCR and MTT assays. This meta-analysis showed a significant drug-binding affinity for intestinal protease. The spherical mean diameters of the free BHPPD, the F1 niosomal-BHPPD, and the F2 niosomal-BHPPD were all determined to be108.91 ± 4.2, 129.13 ± 7.2 nm, and 149.43 ± 3.2 nm, respectively. Also, it was found that the entrapment efficiency (EE%) of the F1 formulations of BHPPD that was niosome-encapsulated was 81.01 0.09% and that it was 70.22 0.13%, respectively. Early, late, necrotic, and viable MCF-7 cells were present in the cells with F1 formulation in proportions of 38.24%, 34.34%, 4.02%, and 23.40%, respectively. Compared to the control group, the treatment group's expression of the genes P57, Prkca, MDM4, Map2k6, and FADD was considerably greater (P < 0.001). Furthermore, compared to control cells, cells in the treatment group expressed less BCL2 and survival genes (P < 0.001). Moreover, formulations of BHPPD encapsulated in niosomes showed a biocompatible nanoscale delivery method and exhibited little cytotoxicity against the HEK-293 standard cell line. According to the findings, formulations of BHPPD with niosome-encapsulation might be viable for boosting anticancer activity.© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.