Exfoliated Nanosheets of a CuII Coordination Polymer Modulate Enzyme Activity of α-Chymotrypsin
Koushik Sarkar1, Parthasarathi Dastidar1
1Department of Organic Chemistry, Indian Association for the Cultivation of Science (IACS), 2A and 2B, Raja S. C. Mullick Road, Jadavpur, Kolkata, 700032, West Bengal, India.
Abstract:
A 2D coordination polymer derived from 5-azidoisophthalic acid (AIA) and Cu(NO3 )2 was designed with the aim of modulating the activity of a digestive enzyme α-chymotrypsin (ChT). The coordination polymer namely {[Cu0.5 (μ-AIA)0.5 (H2 O)]⋅2 H2 O}α (CP1) was successfully synthesized and fully characterized by single-crystal X-ray diffraction (SXRD). An exfoliated nanosheet (ENS) of CP1 was readily produced by overnight stirring of hand-ground CP1 crystals dispersed in DMSO. ENS(CP1) was demonstrated to be acting as an inhibitor of ChT; as much as ≈97 % inhibition of ChT was achieved with 100 μm of ENS(CP1) using N-succinyl-l-phenylalanine-p-nitroanilide (SPNA) as substrate. Enzyme kinetics data revealed that the inhibition of ChT followed a competitive pathway. An enzyme assay under varying ionic strength and varying concentration of free histidine revealed that the active site His-57 participated in coordination with the CuII metal center of ENS(CP1) thereby preventing the substrate (SPNA) from binding with the enzyme resulting in efficient inhibition.
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