Nugrahani Ilma, Sartinah Ari, Uekusa Hidehiro, Abekura Yuto, Ibrahim Slamet, Anggadiredja Kusnandar
School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia.
Center of Halal Studies, Bandung Institute of Technology, Bandung 40132, Indonesia.
Molecules. 2024 Nov 28;29(23):5631. doi: 10.3390/molecules29235631.
Piperine (PPN) is a natural compound with an anti-inflammation effect and low solubility. Hence, some molecular modifications have improved its solid-state character, including cocrystal formation. However, the salt structure has yet to be widely studied. In this research, PPN was reacted with toluene sulfonic acid (TSA), which was expected to increase its solubility and anti-inflammatory effects. This experiment used solid-state reactions and analysis, including thermal analysis, infrared spectroscopy, and powder X-ray diffractometry, to characterize the new multicomponent solid phase. Next, single crystal R-ray diffractometry was used to determine the final three-dimensional conformation structure. After that, the salt, which can be reproduced by wet grinding, was tested for improved stability and anti-inflammatory effects. As a result, the PPN-TSA multicomponent solid was confirmed as a solid salt with monoclinic packing, exhibiting better solubility and anti-inflammation effects. Thus, this new organic salt has the potential for further phytochemical compound development.
胡椒碱（PPN）是一种具有抗炎作用且溶解度低的天然化合物。因此，一些分子修饰改善了其固态性质，包括形成共晶体。然而，盐结构尚未得到广泛研究。在本研究中，PPN与甲苯磺酸（TSA）反应，预期可提高其溶解度和抗炎效果。本实验采用固态反应和分析方法，包括热分析、红外光谱和粉末X射线衍射法，对新的多组分固相进行表征。接下来，使用单晶R射线衍射法确定最终的三维构象结构。之后，对通过湿磨可重现的盐进行稳定性和抗炎效果测试。结果，PPN-TSA多组分固体被确认为具有单斜堆积的固体盐，表现出更好的溶解度和抗炎效果。因此，这种新型有机盐具有进一步开发植物化学化合物的潜力。
