Kongpol Kantapich, Chaihao Preenapan, Shuapan Parichat, Kongduk Ploypailin, Chunglok Warangkana, Yusakul Gorawit
School of Allied Health Sciences, Walailak University Nakhon Si Thammarat Thailand.
Research Excellence Center for Innovation and Health Product, Walailak University Nakhon Si Thammarat Thailand.
RSC Adv. 2022 Jun 13;12(27):17443-17453. doi: 10.1039/d2ra01782b. eCollection 2022 Jun 7.
Owing to their water insolubility, low stability, and poor absorption, anti-inflammatory curcuminoids (CUN) are difficult to be extracted and delivered to the action site. As a result, therapeutic hydrophobic deep eutectic solvents (HDESs), containing menthol and fatty acids (capric, caprylic, and oleic acids), are being developed for CUN solubilization and delivery. In this study, the anti-inflammatory effects of various combinations of HDESs with CUN and curcumin (CUR) were investigated on RAW264.7 macrophage cells. The results showed that CUN can be solubilized using the HDESs. The HDESs of oleic acid (OLA) : menthol (1 : 2, 1 : 1, and 2 : 1 molar ratios) exhibited anti-inflammatory effects, and OLA : menthol (1 : 1 molar ratio) increased the anti-inflammatory effects of CUR. The cytotoxicity of CUN and CUR was also lowered when combined with some OLA : menthol HDESs. The combination of OLA, menthol, and CUR entirely suppressed NO secretion without significant cytotoxicity. These results clearly indicate the potential of HDESs to solubilize CUN and impart anti-inflammatory properties. Furthermore, these solvents could replace organic solvents for CUN extraction, with the added benefit of being therapeutic, biodegradable, and safe for human consumption.
由于其水不溶性、低稳定性和较差的吸收性，抗炎类姜黄素（CUN）难以提取并输送到作用部位。因此，正在开发含有薄荷醇和脂肪酸（癸酸、辛酸和油酸）的治疗性疏水低共熔溶剂（HDESs）用于CUN的增溶和递送。在本研究中，研究了HDESs与CUN和姜黄素（CUR）的各种组合对RAW264.7巨噬细胞的抗炎作用。结果表明，CUN可用HDESs增溶。油酸（OLA）与薄荷醇（摩尔比为1∶2、1∶1和2∶1）的HDESs具有抗炎作用，且OLA∶薄荷醇（摩尔比为1∶1）增强了CUR的抗炎作用。当与某些OLA∶薄荷醇HDESs联合使用时，CUN和CUR的细胞毒性也降低了。OLA、薄荷醇和CUR的组合完全抑制了NO分泌，且无明显细胞毒性。这些结果清楚地表明了HDESs增溶CUN并赋予其抗炎特性的潜力。此外，这些溶剂可替代有机溶剂用于CUN的提取，还具有治疗性、可生物降解且对人体食用安全的额外优势。
