Pantoja-Romero Wenndy, Lavín-Flores Alexis, Morell Gerardo, Martínez-Ferrer Magaly, Weiner Brad R, Coronas Joaquín
Department of Chemistry, University of Puerto Rico at Rio Piedras Campus, 601 Av. Universidad, San Juan, San Juan, Puerto Rico.
Molecular Sciences Research Center, University of Puerto Rico at Rio Piedras Campus, 1390 C. Juan Ponce de León, San Juan, 00926, Puerto Rico.
Chemistry. 2025 Jun 17;31(34):e202500655. doi: 10.1002/chem.202500655. Epub 2025 May 12.
Andrographolide (ADG) was conjugated with MIL-53(Al), ZIF-8, carbon-based quantum dots (CBQDs) and doped carbon-based quantum dots (D-CBQDs) using high-pressure (0.3 GPa) contact. This solvent-free approach is environmentally friendly, energy-efficient, and time-saving, resulting in ADG-MOFs-CBQDs/D-CBQDs with physical properties comparable to those produced by traditional liquid phase encapsulation. The resulting nanocomposites were characterized using SEM, XRD, TGA, FT-IR, and H NMR. The results indicate that ADG was partly encapsulated within the metal-organic framework (MOF) pores, while another portion was bound externally to CBQD/D-CBQDs, as evidenced by distinct drug signals in each analysis. This green synthesis approach simplifies the conjugation process. It significantly enhances the drug solubility, as indicated by changes in hydrophobicity observed via H NMR, surpassing the improvements achieved by ADG encapsulation within MOFs alone. Additionally, in preliminary tests, the materials exhibited significant cytotoxicity against PC3 cells compared to ADG (25.05 ± 0.06 µg/mL) after 48 hours of exposure.
穿心莲内酯(ADG)通过高压(0.3 GPa)接触与MIL-53(Al)、ZIF-8、碳基量子点(CBQDs)和掺杂碳基量子点(D-CBQDs)进行共轭。这种无溶剂方法环保、节能且省时,得到的ADG-MOFs-CBQDs/D-CBQDs的物理性质与传统液相封装法制备的相当。使用扫描电子显微镜(SEM)、X射线衍射(XRD)、热重分析(TGA)、傅里叶变换红外光谱(FT-IR)和核磁共振氢谱(H NMR)对所得纳米复合材料进行了表征。结果表明,穿心莲内酯部分包封在金属有机框架(MOF)孔内,而另一部分则在外部与CBQD/D-CBQDs结合,每次分析中不同的药物信号证明了这一点。这种绿色合成方法简化了共轭过程。正如通过核磁共振氢谱观察到的疏水性变化所示,它显著提高了药物溶解度,超过了单独将穿心莲内酯封装在MOF中的改善效果。此外,在初步测试中,与穿心莲内酯(25.05±0.06 μg/mL)相比,这些材料在暴露48小时后对PC3细胞表现出显著的细胞毒性。