TY - JOUR
T1 - Rho-kinase inhibitors from adlay seeds
AU - Amen, Yhiya
AU - Zhu, Qinchang
AU - Tran, Hai Bang
AU - Afifi, Mohamed S.
AU - Halim, Ahmed F.
AU - Ashour, Ahmed
AU - Fujimoto, Ryoji
AU - Goto, Takahiro
AU - Shimizu, Kuniyoshi
N1 - Publisher Copyright:
© 2017, © 2017 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2018/8/18
Y1 - 2018/8/18
N2 - 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.
AB - 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.
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U2 - 10.1080/14786419.2017.1354183
DO - 10.1080/14786419.2017.1354183
M3 - Article
C2 - 28722478
AN - SCOPUS:85025114712
SN - 1478-6419
VL - 32
SP - 1955
EP - 1959
JO - Natural Product Research
JF - Natural Product Research
IS - 16
ER -