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The structure of a new crystalline base (melting point (mp) 167-169 degrees C) obtained from Fritillaria imperialis was elucidated as (20R, 25R)-5alpha,17beta-cevanine-3beta,6beta-diol, X-ray diffraction analysis of the mono-hydrate. The base was found to be identical with persicanidine B and also with harepermine.
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The extraction procedure and quantitative determination by HPLC-evaporative light scattering detection (ELSD) of the main bioactive components, namely, imperialine (1) and imperialine-3 beta-glucoside (2), of bulbs of Fritillaria pallidiflora Schrenk have been investigated. The most efficient method for the simultaneous extraction of 1 and 2 involved pre-treatment of the bulb powder with ammonia, followed by reflux with dichloromethane:methanol at 90 degrees C for 4 h. Simultaneous determination of non-chromophoric 1 and 2 by HPLC-ELSD employed a Kromasil C18 column eluted with acetonitrile:water:diethylamine. The assay was accurate and reproducible with an overall variation lower than 4% and a sample recovery higher than 98%. The methods described have been successfully used to evaluate the quality of three batches of the crude traditional Chinese medicinal herb derived from the bulbs of F. pallidiflora.
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The presence of M(1)-M(4) receptors in guinea-pig gallbladder smooth muscle cells has been reported recently. The majority of these receptors are said to be of M(2) subtype. However, there are controversial reports about the functional muscarinic receptors that mediate contraction in this tissue. Similar to gallbladder, it was claimed that M(4) receptors mediate guinea-pig uterine contractions, but these receptors have appeared to be of M(2) subtypes later. Therefore, the antagonistic affinities of three M(2)-selective muscarinic antagonists were determined in contraction and radioligand binding experiments in guinea-pig gallbladder in the present study. The antagonistic affinity values (p K(i)) of gallamine, tripitramine and imperialine were as follows, respectively: 6.28+/-0.15, 8.65+/-0.10 and 6.55+/-0.07 against 0.250 n m [(3)H]QNB binding. All three antagonists displaced the concentration- response curves to carbachol to the right in parallel without affecting the maximum responses. The p A(2) values obtained from constrained Schild plots (-log K(B)) were 4.14+/-0.18 for gallamine, 6.79+/-0.09 for tripitramine, and 7.02+/-0.09 for imperialine. The antagonistic affinity values of gallamine, tripitramine and imperialine for M(2) receptors are reported to be 6. 3, 9.6, 7.7, respectively. The p A(2) values obtained in this study clearly indicate that the primary muscarinic receptors involved in carbachol-induced guinea-pig gallbladder contraction are not of M(2) subtype. The poor correlation between the antagonistic affinity values of these antagonists obtained at radioligand binding (p K(i)) and contraction (p A(2)) experiments also support the conclusion that the majority of muscarinic receptors which have been reported to be of M(2) do not mediate the contractile responses.
The action of the cervane alkaloid, imperialine, has been assessed at M1, M2 and M3 receptors in functional assays and at M1, M2, M3 and putative M4 sites in binding studies. In functional studies, imperialine acted as a selective surmountable antagonist at M2 receptors in guinea-pig isolated atria and uterus (-log KB = 7.7 and 7.4, respectively), in comparison to M1 receptors in canine isolated saphenous vein (-log KB = 6.9) or M3 receptors in a range of guinea-pig isolated smooth muscles including ileum, trachea, fundus, seminal vesicle or oesophagus (-log KB = 6.6-6.8). In rat aorta, the -log KB value at the M3 receptor (5.9) was slightly, but significantly, lower. In competition radioligand binding studies, imperialine was also selective toward to M2 sites in rat myocardium (-log Ki = 7.2) with respect to M1 and M3 sites (rat cerebral cortex, rat submaxillary gland; -log Ki = 6.1 and 5.7, respectively). However, it did not significantly discriminate between rat cardiac M2 sites and putative M4 sites in rabbit lung (-log Ki = 6.9). Imperialine resembles the alkaloid himbacine in terms of its pharmacological profile at muscarinic receptor subtypes in that it acts as an M2 selective antagonist with respect to M1 or M3 sites. It may also provide a second, commercially available, antagonist with which to discriminate between M1 and M4 receptors.
Rat cortical synaptosomes were incubated in a saline medium. On the addition of pentobarbital, chloralhydrate, ether and protoveratrine a redistribution of synaptic vesicles was revealed by electron microscopy. The anaesthetics decreased the number of synaptic vesicles attached to the presynaptic membrane while protoveratrine increased them. It is assumed that these agents affect the mechanism of vesicle reformation from the synaptosomal membrane and/or vesicle migration towards the synaptic cleft.
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The effect of protoveratrine A and germine-3-acetate (GMA) on the release mechanism of acetylcholine from the nerve terminals of the Auerbach plexus in the longitudinal muscle layer of the guinea-pig ileum was studied. Protoveratrine A, GMA and germine potentiated neuroeffector transmission in Auerbach's plexus in the longitudinal muscle preparation provided the neurons were stimulated at low frequencies (less than 10 Hz). Protoveratrine A and GMA enhanced the release of acetylcholine from the nerve terminals during the resting period and at low frequency of stimulation (less than 10 Hz). At continous stimulation with high frequency they were ineffective (greater than 10 Hz). When trains of 20 stimuli, with a pulse interval of 0.1 s (10 Hz) were repeatedly applied with intervals of 0.1 to 20 s between trains, the effect of GMA to increase ACh release depended on the length of the train interval; the longer the resting period between trains the higher was the output of ACh. This fact indicates that the release of ACh increased primarily during the resting periods following single stimuli or trains. The effect of GMA on ACh release proved to be highly temperature-dependent: in the presence of GMA Q10 increasing from 3.25 to 4.92. A high Ca concentration, removal of Mg or lowering of the Na concentration abolished the effect of GMA to enhance ACh release.
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