Vascular Biology Laboratory, Department of Biotechnology and AU-KBC Research Centre, Anna University, MIT Campus, Chromepet, Chennai 600 044, India.
Chemical Biology and Nanobiotechnology Laboratory, AU-KBC Research centre, Anna University, MIT Campus, Chromepet, Chennai 600 044, India.
Colloids Surf B Biointerfaces. 2018 Jul 1;167:134-143. doi: 10.1016/j.colsurfb.2018.04.007. Epub 2018 Apr 4.
Zinc silibinin complex [Zn(sil)(HO)] and mixed ligand zinc complexes such as Zn(silibinin)(phenanthroline) [Zn(sil)(phen)], and Zn(silibinin)(neocuproine) [Zn(sil)(neo)] have been synthesized and characterized. The UV-vis spectra of the Zn(II) complexes showed a considerable shift in the intra-ligand transition. From the IR spectra, it is clear that carbonyl group in the C-ring is involved in the metal chelation besides A/C-ring hydroxyl group. Thermal gravimetric analysis showed that [Zn(sil)(neo)] has higher thermal stability compared to the other two Zn(II) complexes. The potential biological activities of the synthesized complexes were studied systematically. In osteoblast differentiation, silibinin and Zn-silibinin complexes enhanced osteoblast differentiation at the cellular level by increasing calcium deposition and ALP activity, and at molecular level increased osteoblast markers include Runx2, type 1 col, ALP and OC mRNAs expression. Additionally, Zn-silibinin complexes showed promising effects on osteoblast differentiation by regulating miR-590/Smad7 signaling pathway. Among the complexes, Zn(sil)(phen) showed more stimulatory effect on osteoblastic differentiation. These complexes also exhibited angiogenic property by increasing VEGF and Ang 1 expression in mouse MSCs and antibacterial activity against E. coli (Gram-negative) and S. aureus (Gram-positive) strains. Thus, the present study demonstrated that the Zn-silibinin complexes exhibit great potential as a pharmacological agent for bone tissue engineering.
锌白藜芦醇复合物[Zn(sil)(HO)]和混合配体锌配合物，如 Zn(silibinin)(phenanthroline)[Zn(sil)(phen)]和 Zn(silibinin)(neocuproine)[Zn(sil)(neo)]已被合成并进行了表征。Zn(II)配合物的紫外可见光谱显示出内配体跃迁的相当大的位移。从红外光谱可以清楚地看出，C 环中的羰基除了 A/C 环上的羟基外，还参与了金属螯合。热重分析表明，[Zn(sil)(neo)]与其他两种 Zn(II)配合物相比具有更高的热稳定性。系统研究了合成配合物的潜在生物学活性。在成骨细胞分化中，白藜芦醇和 Zn-白藜芦醇复合物通过增加钙沉积和 ALP 活性在细胞水平上增强成骨细胞分化，在分子水平上增加成骨细胞标志物，包括 Runx2、type 1 col、ALP 和 OC mRNA 的表达。此外，Zn-白藜芦醇复合物通过调节 miR-590/Smad7 信号通路对成骨细胞分化表现出良好的效果。在这些复合物中，Zn(sil)(phen)对成骨细胞分化表现出更强的刺激作用。这些复合物还通过增加小鼠 MSCs 中 VEGF 和 Ang 1 的表达以及对革兰氏阴性的大肠杆菌和革兰氏阳性的金黄色葡萄球菌的抗菌活性表现出血管生成特性。因此，本研究表明，Zn-白藜芦醇复合物作为骨组织工程的药理学制剂具有很大的潜力。
