Gouda Mohamed, Ibrahim Hairul-Islam Mohamed, Negm Amr
Department of Chemistry, College of Science, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Biological Science Department, College of Science, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Polymers (Basel). 2022 Mar 22;14(7):1276. doi: 10.3390/polym14071276.
A biologically active agent based on a Zn-1,3,5-benzen tricarboxylic acid (Zn-BTC) framework incorporated into a chitosan (CS) biopolymer (Zn-BTC@CS) was successfully synthesized using a microwave irradiation technique. The synthesized Zn-BTC@CS was characterized using a scanning electron microscope (SEM) and the obtained data indicated a highly smooth surface morphology of the synthesized Zn-BTC and no morphological changes when the Zn-BTC covered the CS. In addition, the particle size diameter varied from 20 to 40 nm. XRD displayed a well-maintained Zn-BTC structure, and the crystal structure of Zn-BTC was not distorted by the composition of Zn-BTC and chitosan in the nanocomposite. Data from BET analysis revealed that the specific surface area of the Zn-BTC was reduced from 995.15 m/g to 15.16 m/g after coating with chitosan. The pore size distribution and pore volume of the Zn-BTC, Zn-BTC@CS were centered at 37.26 nm and at 22.5 nm, respectively. Zn-BTC@CS exhibited anticancer efficacy against lung and colon cancer cell lines. Zn-BTC@CS inhibited the proliferation of A549 and DLD-1 cancer cell lines in a dose-dependent manner with IC values of 13.2 and 19.8 µg/mL for the colon and lung cancer cell lines, respectively. Zn-BTC@CS stimulated the apoptotic process through up-regulating P53 expression and down-regulating Bcl-2 expression. Moreover, Zn-BTC@CS induced in vitro DNA fragmentation in both cancer cell lines with significantly different affinity by 66% (A549) and 20% (DLD-1) versus 52% reduction by Cisplatin. Zn-BTC@CS (IC50) exhibited anti-invasive activity and dramatically inhibited the migration of lung and colon cancer cell lines. This study provides evidence that Zn-BTC@CS targets the essential proteins involved in proliferation, metastasis, and apoptosis. Thus, Zn-BTC@CS has chemotherapeutic potential for inhibiting lung and colon cancer viability and growth.
采用微波辐射技术成功合成了一种基于掺入壳聚糖（CS）生物聚合物（Zn-BTC@CS）的Zn-1,3,5-苯三甲酸（Zn-BTC）骨架的生物活性剂。使用扫描电子显微镜（SEM）对合成的Zn-BTC@CS进行表征，所得数据表明合成的Zn-BTC表面形态高度光滑，且Zn-BTC覆盖CS时无形态变化。此外，粒径直径在20至40nm之间变化。XRD显示Zn-BTC结构保持良好，纳米复合材料中Zn-BTC与壳聚糖的组成未使Zn-BTC的晶体结构变形。BET分析数据表明，壳聚糖包覆后Zn-BTC的比表面积从995.15m²/g降至15.16m²/g。Zn-BTC、Zn-BTC@CS的孔径分布和孔体积分别集中在37.26nm和22.5nm。Zn-BTC@CS对肺癌和结肠癌细胞系具有抗癌功效。Zn-BTC@CS以剂量依赖性方式抑制A549和DLD-1癌细胞系的增殖，对结肠癌细胞系和肺癌细胞系的IC值分别为13.2和19.8μg/mL。Zn-BTC@CS通过上调P53表达和下调Bcl-2表达刺激凋亡过程。此外，Zn-BTC@CS在两种癌细胞系中均诱导体外DNA片段化，与顺铂使DNA片段化减少52%相比，其亲和力显著不同，分别为66%（A549）和20%（DLD-1）。Zn-BTC@CS（IC50）表现出抗侵袭活性，并显著抑制肺癌和结肠癌细胞系的迁移。本研究提供了证据表明Zn-BTC@CS靶向参与增殖、转移和凋亡的关键蛋白。因此，Zn-BTC@CS具有抑制肺癌和结肠癌细胞活力及生长的化疗潜力。
