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Synthesis, Characterizations, and Use of O-Stearoyl Mannose Ligand-Engineered Lipid Nanoarchitectonics for Alveolar Macrophage Targeting.
ASSAY and Drug Development Technologies ( IF 1.6 ) Pub Date : 2020-09-16 , DOI: 10.1089/adt.2020.999
Maharshi Thalla 1 , Jagadeeshkumar Gangasani 2 , Pritam Saha 2 , Srikanth Ponneganti 3 , Roshan M Borkar 3 , Vgm Naidu 2 , Usn Murty 4 , Subham Banerjee 1
Affiliation  

The main challenging aspect in the management of tuberculosis (TB) diseases is effective alveolar macrophages targeting. Macrophage mannose receptor plays a predominant role in stimulating immune systems by TB pathogen. Our earlier in silico computational studies revealed that O-stearoyl mannose (OSM) possesses a higher affinity with macrophage mannose receptors. Therefore, keeping this in view, we developed OSM with the association of stearic acid and d-mannose as initial reactants by the esterification process. Preliminary confirmation of reaction was assessed with thin-layer chromatography experimentation, whereas further confirmation followed by in vitro characterization with several analytical experimental tools such as fourier transform near-infrared, differential scanning calorimetry, and electrospray ionization-assisted mass spectrometry confirms the formation of the OSM. This synthesized and well-characterized OSM as a ligand was further incubated with surface-engineered lipid nanoarchitectonics to achieve OSM ligand-engineered lipid nanoarchitectonics and earlier explored for its safety study through hemolysis assay and potential in vitro triggering efficiency in human alveolar macrophages (THP-1 cells) to validate its active targeting efficiency.

中文翻译:

O-硬脂酰甘露糖配体工程脂质纳米结构的合成、表征和用于肺泡巨噬细胞靶向的用途。

结核病 (TB) 疾病管理的主要挑战是有效靶向肺泡巨噬细胞。巨噬细胞甘露糖受体在 TB 病原体刺激免疫系统中起主要作用。我们早期的计算机计算研究表明,O-硬脂酰甘露糖 (OSM) 与巨噬细胞甘露糖受体具有更高的亲和力。因此,考虑到这一点,我们开发了通过酯化过程将硬脂酸和d-甘露糖结合作为初始反应物的OSM 。反应的初步确认是通过薄层色谱实验评估的,而进一步的确认随后是体外使用傅立叶变换近红外、差示扫描量热法和电喷雾电离辅助质谱法等几种分析实验工具进行表征证实了 OSM 的形成。此合成并充分表征OSM作为配体具有表面设计的脂质nanoarchitectonics再保温至达到OSM配体工程化脂质nanoarchitectonics和更早探索通过溶血试验和潜在的其安全性的研究在体外在人肺泡巨噬细胞的触发效率(THP- 1 个细胞)以验证其主动靶向效率。
更新日期:2020-09-17
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