Intestinal transport of 5-methyltetrahydrofolate

The mechanism of intestinal absorption of 5-methyltetrahydrofolate (5- CH3THF ) has been the topic of some controversy. In the present study, we have used enzymatically prepared 5- CH3THF to characterize transport by rat intestinal loops in vivo and everted jejunal sacs in vitro. Transport of 5- CH3THF is saturable (Km = 5.2 microM) and highly pH dependent, with the rate of maximal transport occurring at pH 5.8. Transport is competitively inhibited by folic acid (Ki = 4.2 microM) and methotrexate (Ki = 4.65 microM). Metabolic poisons and anaerobiosis greatly reduce 5- CH3THF transport. We conclude that 5- CH3THF transport in the rat intestine occurs by the same structure-specific mechanism responsible for the transport of unreduced folic acid and other monoglutamyl folates.