Planta Med 2005; 71(2): 120-125
DOI: 10.1055/s-2005-837777
Original Paper
Pharmacology
© Georg Thieme Verlag KG Stuttgart · New York

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

Anwar-ul Hassan Gilani1 , Mohammad Nabeel Ghayur1 , Asaad Khalid2 ,  Zaheer-ul-Haq2 , Muhammad Iqbal Choudhary2 ,  Atta-ur-Rahman2
  • 1Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi, Pakistan
  • 2Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical Sciences, University of Karachi, Karachi, Pakistan
Further Information

Publication History

Received: May 17, 2004

Accepted: August 29, 2004

Publication Date:
24 February 2005 (online)

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 doses (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.