TY - JOUR
T1 - Synthesis, α-glucosidase inhibition, α-amylase inhibition, and molecular docking studies of 3,3-di(indolyl)indolin-2-ones
AU - Santoso, Mardi
AU - Ong, Li Lin
AU - Aijijiyah, Nur Pasca
AU - Wati, First Ambar
AU - Azminah, Azminah
AU - Annuur, Rose Malina
AU - Fadlan, Arif
AU - Judeh, Zaher M.A.
N1 - Publisher Copyright:
© 2022 The Author(s)
PY - 2022/3
Y1 - 2022/3
N2 - The synthesized 3,3-di(indolyl)indolin-2-ones 1a-p showed desired higher α-glucosidase inhibitory activities and lower α-amylase inhibitory activities than standard drug acarbose. Particularly, compound 1i showed favorable higher α-glucosidase % inhibition of 67 ± 13 and lower α-amylase % inhibition of 51 ± 4 in comparison to acarbose with % inhibition activities of 19 ± 5 and 90 ± 2, respectively. Docking studies of selected 3,3-di(indolyl)indolin-2-ones revealed key interactions with the active sites of both α-glucosidase and α-amylase, further supporting the observed % inhibitory activities. Furthermore, the binding energies are consistent with the % inhibition values. The results suggest that 3,3-di(indolyl)indolin-2-ones may be developed as suitable Alpha Glucosidase Inhibitors (AGIs) and the lower α-amylase activities should be advantageous to reduce the side effects exhibited by commercial AGIs.
AB - The synthesized 3,3-di(indolyl)indolin-2-ones 1a-p showed desired higher α-glucosidase inhibitory activities and lower α-amylase inhibitory activities than standard drug acarbose. Particularly, compound 1i showed favorable higher α-glucosidase % inhibition of 67 ± 13 and lower α-amylase % inhibition of 51 ± 4 in comparison to acarbose with % inhibition activities of 19 ± 5 and 90 ± 2, respectively. Docking studies of selected 3,3-di(indolyl)indolin-2-ones revealed key interactions with the active sites of both α-glucosidase and α-amylase, further supporting the observed % inhibitory activities. Furthermore, the binding energies are consistent with the % inhibition values. The results suggest that 3,3-di(indolyl)indolin-2-ones may be developed as suitable Alpha Glucosidase Inhibitors (AGIs) and the lower α-amylase activities should be advantageous to reduce the side effects exhibited by commercial AGIs.
KW - 3,3-Di(indolyl)indolin-2-ones
KW - Diabetes
KW - Docking studies
KW - α-amylase inhibition
KW - α-glucosidase inhibition
UR - http://www.scopus.com/inward/record.url?scp=85125943659&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85125943659&partnerID=8YFLogxK
U2 - 10.1016/j.heliyon.2022.e09045
DO - 10.1016/j.heliyon.2022.e09045
M3 - Article
AN - SCOPUS:85125943659
SN - 2405-8440
VL - 8
JO - Heliyon
JF - Heliyon
IS - 3
M1 - e09045
ER -
