Structure-related enhancing activity of escins Ia, Ib, IIa and IIb on magnesium absorption in mice.


Li Y, Matsuda H, Wen S, Yamahara J




Bioorg Med Chem Lett


We examined the effects of the saponin fraction and its principal saponins, escins Ia (1), Ib (2), IIa (3) and IIb (4), obtained from European horse chestnut, and their hydrolyzed products, desacylescins I (5) and II (6) on magnesium absorption from the gastrointestinal tract in mice. Test samples were given orally to fasted mice before loading of 0.5 or 1.67 M MgSO4 (10 mL/kg, p.o.). The saponin fraction (12.5-100 mg/kg) significantly enhanced the Mg2+ absorption 30, 60, 120 and 240 min after administration, with maximum enhancement by 48.3% at 50 mg/kg. Escins Ib (2) and IIb (4) (12.5 and 25 mg/kg) also enhanced the absorption, whereas escins Ia (1) and IIa (3) (12.5 and 25 mg/kg) and desacylescins I(5) and II (6) (25 mg/kg) showed no activity. These results suggested that the 21-O-tigloyl and/or 22-O- acetyl group(s) is essential for such activity. The saponin fraction, 2 and 4 (50 mg/kg) also affected the activity, but their effects were attenuated in streptozotocin-induced diabetic mice. Furthermore, pretreatment with insulin or indomethacin did not reduce the effect of 2 and 4. These results also implied that neither the sympathetic nervous system nor endogenous prostaglandins were involved. The involvement of parathyroid hormone, and/or the metabolism of vitamin D should be considered.