Surya Sukumaran, Geethanandan Krishnan, Sadasivan Chittalakkottu, Haridas Madhathilkovilakathu
Inter University Centre for Bioscience and Department of Biotechnology and Microbiology, Kannur University, Thalassery Campus, Kannur 670661, India.
Inter University Centre for Bioscience and Department of Biotechnology and Microbiology, Kannur University, Thalassery Campus, Kannur 670661, India.
Int J Biol Macromol. 2016 Oct;91:696-702. doi: 10.1016/j.ijbiomac.2016.06.010. Epub 2016 Jun 6.
Therapeutic effects of gallic acid (GA) have already been extensively studied. However, its interaction with lectins has not gained much attention. It is of interest to validate the binding profile of GA with Spatholobus parviflorus seed lectin. A combination of Isothermal Titration Calorimetry (ITC), haemagglutination assay and molecular docking was applied on SPL-GA interaction. ITC results showed four binding sites, stoichiometry, n=4, irrespective of the ratio of SPL:GA taken for titration. Difference among the four binding sites of a single molecule of SPL with regard to GA binding kinetic parameters was consistently varying. Similarly, the glide scores obtained for GA in the four different binding clefts of SPL were also conformed to the ITC. The binding of GA on SPL without affecting its sugar binding property could be considered as a boon for glycobiological research. From the presented studies, it could be proposed that the SPL-GA interactions may facilitate drug delivery by specific targeting/attachment by profiling of cell-surface glycans, followed by controlled release of drugs.
没食子酸（GA）的治疗作用已得到广泛研究。然而，其与凝集素的相互作用尚未受到太多关注。验证GA与小花血藤种子凝集素的结合情况很有意义。采用等温滴定量热法（ITC）、血细胞凝集试验和分子对接相结合的方法研究SPL-GA相互作用。ITC结果显示有四个结合位点，化学计量比n = 4，与滴定所用的SPL:GA比例无关。单个SPL分子的四个结合位点在GA结合动力学参数方面的差异持续变化。同样，GA在SPL四个不同结合裂隙中获得的Glide评分也与ITC结果相符。GA与SPL的结合不影响其糖结合特性，这对糖生物学研究来说可谓是一大幸事。从目前的研究来看，可以推测SPL-GA相互作用可能通过对细胞表面聚糖进行分析实现特异性靶向/附着，进而促进药物递送，随后实现药物的控释。
