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Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: Synthesis, structure-activity relationships, and X-ray crystallographic studies

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Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: Synthesis, structure-activity relationships, and X-ray crystallographic studies
Cheng, Keguang
Zhang, Liying
Οικονομάκος, Νίκος Γ.
Alexacou, Kyra-Melinda
Hao, Jia
Gimisis, Thanasis
Hayes, Joseph M.
Wen, Xiaoan
Zhang, Luyong
Sun, Hongbin
Ni, Peizhou
Ζωγράφος, Σπύρος Ε.
Λεωνίδας, Δημήτρης Δ.
Liu, Jun
Zhang, Pu
Άρθρο σε επιστημονικό περιοδικό
2008-06-26
WASHINGTON
Twenty-five naturally occurring pentacyclic triterpenes, 15 of which were synthesized in this study, were biologically evaluated as inhibitors of rabbit muscle glycogen phosphorylase a (GPa). From SAR studies, the presence of a sugar moiety in triterpene saponins resulted in a markedly decreased activity (7, 18-20) or no activity (21, 22). These saponins, however, might find their value as potential natural prodrugs which are much more water-soluble than their corresponding aglycones. To elucidate the mechanism of GP inhibition, we have determined the crystal structures of the GPb-asiatic acid and GPb-maslinic acid complexes. The X-ray analysis indicates that the inhibitors bind at the allosteric activator site, where the physiological activator AMP binds. Pentacyclic triterpenes represent a promising class of multiple-target antidiabetic agents that exert hypoglycemic effects, at least in part, through GP inhibition.
Χημεία (Γενικά) (EL)
Φαρμακευτική (EL)
Pharmacy and materia medica (EN)
Chemistry (General) (EN)
Chemistry, Medicinal
English
American Chemical Society
Journal of Medicinal Chemistry
© AMER CHEMICAL SOC
https://rightsstatements.org/page/InC/1.0/?language=en
© AMER CHEMICAL SOC (EN)
National Hellenic Research Foundation (NHRF)
Helios - Repository of the National Hellenic Research Foundation (NHRF)



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