Sareen Rashmi, Jain Nitin, Dhar K L
a School of Pharmacy, Bharat Institute of Technology , Meerut , Uttar Pradesh , India and.
b I.S.F. College of Pharmacy , Moga , Punjab , India.
Pharm Dev Technol. 2016 Aug;21(5):630-5. doi: 10.3109/10837450.2015.1041042. Epub 2015 Apr 29.
The aim of present investigation was to prepare Curcumin-Zn(II) complex in a view to enhance solubility, stability and pharmacodynamic effect in experimentally induced ulcerative colitis.
Curcumin-Zn(II) complex was prepared by stirring curcumin with anhydrous zinc chloride at a molar ratio of 1:1. The prepared curcumin metallocomplex was characterized by TLC, FTIR, UV spectroscopy and (1)H NMR. In vitro kinetic degradation and solubility of Curcumin and Curcumin-Zn(II) complex was analyzed spectrophotometrically. Pharmacodynamic evaluation of curcumin and its metal complex was assessed in ulcerative colitis in mice.
Curcumin showed chelation with zinc ion as confirmed by the TLC, FTIR, UV spectroscopy and (1)H NMR. The results of TLC [Rf value], IR Spectroscopy [shifting of stretching vibrations of υ(C=C) and υ(C=O)], UV spectra [deconvoluted with absorption band at 432-466.4 nm] of Curcumin-Zn(II) complex compared to curcumin confirmed the formation of metallocomplex. (1)HNMR spectra of Curcumin-Zn(II) showed the upfield shift of Ha and Hb. Kinetic stability studies showed metallocomplex with zinc exhibited good stability. In vivo study revealed significant reduction in severity and extent of colonic damage with Curcumin-Zn(II) which were further confirmed by histopathological study.
This study recognizes higher solubility and stability of Curcumin-Zn(II) complex and suggested better pharmacodynamic effects.
本研究旨在制备姜黄素 - 锌(II)配合物,以提高其在实验性诱导的溃疡性结肠炎中的溶解度、稳定性和药效学作用。
通过将姜黄素与无水氯化锌以1:1的摩尔比搅拌制备姜黄素 - 锌(II)配合物。制备的姜黄素金属配合物通过薄层色谱法(TLC)、傅里叶变换红外光谱法(FTIR)、紫外光谱法和核磁共振氢谱(¹H NMR)进行表征。用分光光度法分析姜黄素和姜黄素 - 锌(II)配合物的体外动力学降解和溶解度。在小鼠溃疡性结肠炎模型中评估姜黄素及其金属配合物的药效学。
通过TLC、FTIR、紫外光谱法和¹H NMR证实姜黄素与锌离子发生螯合。与姜黄素相比,姜黄素 - 锌(II)配合物的TLC[比移值(Rf值)]、红外光谱[υ(C = C)和υ(C = O)伸缩振动的位移]、紫外光谱[在432 - 466.4 nm处有解卷积吸收带]结果证实了金属配合物的形成。姜黄素 - 锌(II)的¹H NMR光谱显示Ha和Hb的高场位移。动力学稳定性研究表明与锌形成的金属配合物具有良好的稳定性。体内研究显示姜黄素 - 锌(II)可使结肠损伤的严重程度和范围显著降低,组织病理学研究进一步证实了这一点。
本研究证实了姜黄素 - 锌(II)配合物具有更高的溶解度和稳定性,并表明其具有更好的药效学作用。