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Characterization and Biological Evaluation of Solid Dispersed Nanoparticles of Synthetic Epoksilignan Targeting Pancreatic Cancer Cell as an Anticancer Agent.
Journal of Biomedical Nanotechnology ( IF 2.9 ) Pub Date : 2021-8-28 , DOI: 10.1166/jbn.2021.3127
Yusnita Rifai 1 , Weltiansy Tanggulungan 1 , Latifah Rahman 2 , Deep Jyoti Bhuyan 3
Affiliation  

MMEO (3'-methoxy-3',4″(methylenedioxy)-2,5-epoksilignan-4'ol-6-on) is a derivative of DMEO (3'-methoxy-3″,4″(methylenedioxy)-2,5-epoksilignan-4',6-diol) synthesized through demethylation using dimethylsulfoxide-acetic anhydride reagent. MMEO inhibits Hedgehog signaling at a concentration of 4.1 μM. The current study aimed to formulate MMEO as solid dispersed nanoparticles and determine their physicochemical properties and inhibitory activities. XRD (X-ray diffraction) analysis showed that the crystalline particles of the pure compound MMEO was smaller than MMEO nanoparticles. Image J software showed that at concentrations of 25 mg/mL and 50 mg/mL, the average nanoparticle sizes were 852.26 nm and 178.65 nm, respectively. Therefore, the MMEO solid dispersion system with the PEG 4000 polymer increases the solubility of MMEO. The higher the concentration of PEG 4000 the greater the solubility of MMEO. Treating pancreatic cancer cell lines with MMEO silenced the smoothened function by downregulating mRNA Ptch expression. This study suggests that MMEO may inhibit pancreatic cancer disease.

中文翻译:

靶向胰腺癌细胞的合成 Epoksilignan 固体分散纳米颗粒作为抗癌剂的表征和生物学评价。

MMEO(3'-甲氧基-3',4”(亚甲二氧基)-2,5-epoksilignan-4'ol-6-on)是DMEO(3'-甲氧基-3”,4”(亚甲二氧基)-的衍生物) 2,5-epoksilignan-4',6-diol) 使用二甲亚砜-乙酸酐试剂通过去甲基化合成。MMEO 在 4.1 μ的浓度下抑制 Hedgehog 信号传导M. 目前的研究旨在将 MMEO 配制为固体分散的纳米粒子,并确定它们的理化性质和抑制活性。XRD(X射线衍射)分析表明纯化合物MMEO的结晶颗粒小于MMEO纳米颗粒。Image J 软件显示,在 25 mg/mL 和 50 mg/mL 的浓度下,平均纳米颗粒尺寸分别为 852.26 nm 和 178.65 nm。因此,含有 PEG 4000 聚合物的 MMEO 固体分散体系增加了 MMEO 的溶解度。PEG 4000 的浓度越高,MMEO 的溶解度越大。用 MMEO 治疗胰腺癌细胞系通过下调 mRNA Ptch 表达使平滑功能沉默。这项研究表明 MMEO 可能抑制胰腺癌疾病。
更新日期:2021-08-28
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