Sodium-linked glucose transporters (SGLTs) is a class of membrane-associated carrier protein that carry glucose into cells. Phloridzin is an inhibitor against human SGLT1 (hSGLT1) and human SGLT2 (hSGLT2), two isoforms of SGLTs, with IC50 values of 400 and 65 nM, respectively. Also for phloridzin, the Ki values were 140 and 11 nM for hSGLT1 and hSGLT2, respectively. In hSGLT2 experiment, the half-time inhibition of 1 μM phloridzin of 100 mM glucose Na+/sugar current was 9s, and the recovery time from imbibition was 30s. In hSGLT1 experiment, 10 μM phloridzin inhibited 0.5 mM D-glucose-induced current with an on time course of 2s and a recovery time from inhibition of 10s[1]. In rats, intravenous injection of phloridzin (10 mg/kg) increased the excretion of Me-4FDG into the urinary bladder 60 min after the injection. Also, a bolus of phloridzin, which was injected 20 minutes after F-Dapa, resulted in a rapid displacement of F-Dapa to a new steady state in vivo[2].
作用机制
The sugar moiety of phloridzin interacts with the glucose binding site of SGLT1 and SGLT2. The aglycone of phloridzin is also responsible for selectivity of phloridzin for SGLTs[1].
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