Presence of Antispasmodic, Antidiarrheal, Antisecretory, Calcium Antagonist and Acetylcholinesterase Inhibitory Steroidal Alkaloids inSarcococca saligna

Abstract

The aim of this investigation was to see if the crude extract of Sarcococca saligna (Ss.Cr) contains chemicals with gut function inhibitory activity by using in vitro and in vivo assays. Ss.Cr caused a dose-dependent (0.03 - 3 mg/mL) inhibitory effect on K+-induced contractions in rat stomach fundus, guinea-pig ileum and rabbit jejunum preparations. The calcium channel blocking(CCB) activity was confirmed when Ss.Cr caused a rightward shift in the Ca++ dose-response curves. It also potentiated, at lower do-ses (0.001 - 0.03 mg/mL), the contractile effect of a fixed dose of acetylcholine (ACh), similar to physostigmine, and suppressed the effect of ACh at higher doses (0.3 - 1.0 mg/mL). Both Ss.Cr and physostigmine inhibited acetylcholinesterase (AChE), in the in vitro assay, confirming the AChE inhibitory activity. In the in vivo studies, Ss.Cr exhibited antidiarrheal and antisecretory activities against castor oil-induced diarrhea and intestinal fluid accumulation in mice. Characteristic steroidal compounds of the plant (saracocine, saracodine, saracorine and alkaloid-C), exhibited a similar combination of AChE inhibitory and CCB activities. Thus this study provides a sound mechanistic base for some of the traditional uses of the plant in hyperactive gut states, in addition to providing the first evidence for verapamil to possess additional AChE inhibitory activity. Furthermore, these characteristic compounds with dual activity may be good candidates for further studies on their usefulness in Alzheimer's disease.

Studies to determine antidiarrhoeal and spasmolytic activities of extract of Aegle marmelos. L fruit

“…The vasorelaxant activity of the Am.Cr was examined in isolated mice ileum 20 . Mice (25-30 g) was fasted for 12 hr prior to experiments.…”

“…A preload of 1.0 g was exercised and the tissues were allowed to equilibrate for 1hr prior to the addition of test sample or drug. Under these experimental conditions, mice ileum exhibits spontaneous rhythmic contractions, allowing to test the relaxant (spasmolytic) effect directly, without adding some agonist 20 . The control responses to submaximal concentration of acetylcholine (0.3 µM) were recorded.…”

Antidiarrheal and antispasmodic activities of <i>Vitex negundo</i> are mediated through calcium channel blockade

“…Spontaneously beating isolated rabbit jejunum preparation is used to test possible inhibitory (spasmolytic) effect of test substances without use of a spasmogen (Gilani et al, 2005). When tested in isolated rabbit jejunum preparations, cumulative addition of the Vn.Cr, diltiazem and loperamide, caused concentrationdependent inhibition of the spontaneous contractions (Figure 1), with respective EC50 values of 0.36 mg/mL (0.22-0.61), 2.62 µM (0.57-11.95; n=5) and 25.80 µM (18.80-29.33; n=4) (Figure 2), thus, showing smooth muscle relaxant activity.…”

“…The isolated tissue experiments were carried out as previously described (Gilani et al, 2005;Shah et al, 2011b). The animals had free access to water but were fasted for 24 h before the experiment.…”

“…Under these experimental conditions, rabbit jejunum exhibits spontaneous rhythmic contractions, allowing testing the relaxant (spasmolytic) activity directly without the use of an agonist (Gilani et al, 2005).…”