A comparative study was made on the endogenous digoxin-like activity of sixteen mammalian-type lignan derivatives including enterolactone and enterodiol.
METHODS AND RESULTS:
Cross-reactivity to antidigoxin antibody, inhibition of dog kidney Na+,K+-ATPase, and ouabain displacing activity against [3H]ouabain binding to human erythrocytes on the part of these derivatives were examined and compared in all cases with that of ouabain. meso-2,3-Dibenzylbutane-1,4-diol (meso-HA-1) was found to possess the most potent cross-reactivity to antidigoxin antibody. Several lignans, particularly HA-1 (either meso or dl), dl-2,3-bis(3-methoxybenzyl)butane-1,4-diol(HA-4), dl-2,3-bis(3,4-dimethoxybenzyl)butane-1,4-diol(HA-10), dl-2,3-bis(3,4-dimethoxybenzyl)-1,4-dimethoxybutane(HA-11), and trans-2,3-bis(3,4-dimethoxybenzyl)-gamma-butyrolactone(HA-14) were capable of inhibiting Na+,K+-ATPase activity with IC50 at a concentration less than 5 x 10(-4) M. Meso-HA-1, HA-11 and HA-14 also showed [3H]ouabain displacement activity with IC50 at a concentration of 10(-4)-10(-3) M. These determinations of activity were made at doses 100-1000 times those of ouabain.
CONCLUSIONS:
The synthetic lignans are considered to derive in vivo from plant material usually present in fibrous food. Based on the data obtained, some lignans may possibly be endogenous digitalis-like substances. |
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