Fig. 5.

Galloflavin inhibits PDHC. (A) PDHC activity in HeLa cells incubated with 750 µM of galloflavin or vehicle (0.075% DMSO) for 6 h (n = 2; t test, p = 0.011). (B) PDHC activity in mouse livers harvested 6 h after the intraperitoneal injection of a dose of 80 mg/kg of galloflavin compared to vehicle (DMSO 40% in saline) (n = 4 per group; t test, p = 0.041). (C-D) Surface representation of octameric E1 subunit of the PDHC (3exe) with highlighted point of contact with galloflavin (inset). (E) Three hydrogen bonds were observed between galloflavin and Arg19 and Asp20 of chain D of one tetramer and Lys189 of chain H of the other E1 tetramer. PDHC, pyruvate dehydrogenase complex. (This figure appears in colour on the web.)