Two substances identified as ((3β, 4α, 16β, 21β, 22α)-21-tigloxy-16, 22, 23, 28-tetrahydroxyolean-12-en-3-yl-β-D-glucopyranosiduronic acid) (GA
1) and ((3β, 4α, 16β, 21β, 22α)-21-(2-methylbutyroxy)-16, 22, 23, 28-tetrahydroxyolean-12-en-3-yl-β-D-glucopyranosiduronic acid) (GA
2) identified among the gymnemic acids are triterpene glycosides extracted from Gymnema sylvestre leaves. We examined the effects of GA1 or GA2 on high K
+-induced contraction in the guinea-pig longitudinal muscle. A sustained muscle contraction induced by hyperosmotically added 65.4mM KCl (H-65K
+) was suppressed by GA
1 or GA
2 (7.7×10
-5M). Simultaneous measurements of reduced pyridine nucleotide (PNred) or oxidized flavin protein (FPox) by the fluorescence technique and of contractile force revealed that GA
1 and GA
2 reduced the increase of PNred fluorescence and contractile force induced by H-65K
+, whereas FPox fluorescence induced by it further increased. Reduced muscle contraction induced by GA
1 or GA
2 was restored by 5.5mM pyruvate. Simultaneous measurements of intracellular Ca
2+ [Ca
2+] i level and contractile force indicated that [Ca
2+] i level, which increased by H-65K+, hardly changed with GA
1 and GA
2. In summary, both GA
1 and GA
2, which are among the gymnemic acids, suppressed high K
+-induced contraction in the guinea-pig ileal longitudinal muscle. The difference between these two gymnemic acids was not significant. The inhibitory effect of GA
1 and GA
2 on smooth muscle were assumed to be a result of inhibiting glucose uptake, which is an energy source of the muscle, whereas the inhibitory mechanisms were probably not mediated by Ca
2+.
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