Rho-kinase inhibitors from adlay seeds

Abstract

Rho-kinase enzymes are one of the most important targets recently identified in our bodies. Several lines of evidence indicate that these enzymes are involved in many diseases and cellular disorders. ROCK inhibitors may have clinical applications for cancer, hypertension, glaucoma, etc. Our study aims to identify the possible involvement of Rho-kinase inhibition to the multiple biological activities of adlay seeds and provide a rationale for their folkloric medicines. Hence, we evaluated Rho-kinase I and II inhibitory activity of the ethanol extract and 28 compounds derived from the seeds. A molecular docking assay was designed to estimate the binding affinity of the tested compounds with the target enzymes. The results of our study suggest a possible involvement of Rho-kinase inhibition to the multiple biological activities of the seeds. Furthermore, the results obtained with the tested compounds revealed some interesting skeletons as a scaffold for design and development of natural Rho-kinase inhibitors.

Keywords:

• Adlay
• Coix lacryma-jobi
• Rho-kinase
• docking

Acknowledgements

The Egyptian Ministry of Higher Education is acknowledged for the fellowship support to Yhiya Amen. The authors wish to thank Shinnihonseiyaku Co Ltd (Japan) for providing the extract material. We express our deep thanks and appreciate the technical assistance from The Research Support Center, Research Center for Human Disease Modelling, Kyushu University Graduate School of Medical Sciences.