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293-296,1996
© 1996 by Gustav Fischer Verlag, Stuttgart· Jena . New York
Department of Pharmacology and Toxicology, NationalInstitute for Pharmaceutical Reserarch and Devel-
opment, P.M.B. 21, Abuja, Nigeria.
Summary
Aqueous extract of the stem of Gongronema latifolium was screened for effects on the gas-
trointestinal tract of rats and mice. On the isolated rat intestine, the extract (5-80 ug) evoked re-
producible and concentration-related relaxation which were attenuated by yohimbine and
phenoxybenzamine. Intraperitoneal (i. p.) administration of the extract in mice significantly re-
duced small intestinal transit dose-dependently. This effect was also attenuated by yohimbine and
phenoxybenzamine, but not prazosin and propranolol. Phytochemical analysis revealed the pres-
ence of some bioactive constituents, while the i. p. LDso value of the extract in mice was estab-
lished as 1678.63 ± 78 mg/kg. The results suggest the involvement of the alphaj-adrenoceptors in
the effect of the extract on the intestinal function.
al Institute for Pharmaceutical Reserarch and Development nist was tested on a separate preparation, and there were 5
Herbaria. determinations for each experiment.
Phytochemical tests The preliminary acute toxicity test in mice established the
i. p. LDso of the extract to be 1678.63 ± 78 rug/kg. Phyto-
The freshly prepared extract was subjected to phyto- chemical analysis revealed the presence of alkaloids, carbo-
chemical analysis as described by Trease and Evans (1983). hydrates, tannins, saponins, flavonoids and glycosides (ex-
cept cynogenetic glycosides).
Studies on isolated rat intestine
Effect on the isolated rat intestine
Segments of rat ileum (2 em long) removed from freshly
killed animals were suspended in a 20 ml organ bath con- The extract (5-80 ug) produced a concentration-depend-
taining aerated Tyrode solution maintained at 37°C. The ent and sustained relaxation of the intestine (Tab. 1). It was
composition of the Tyrode solution was (mmollL) NaCI possible to construct three dose-response-curves with the
137; KCI2.7; csci, 1.0; NaHC0 3 12; NaHzP0 4 0.2 and extract within 60 min without remarkable change in sensi-
glucose 5.6. The tension on the tissues was 1 g. The tissues tivity. Acetylcholine (5.5 x lO-SM)-induced contraction and
were equilibrated for 60 min during which the bathing so- noradrenaline (3.0 x 1O-7M)-induced relaxation of the
lution was replaced every 10 min. At the end of the equili- preparation were also recorded for comparison (Fig. 1).
bration period responses were established non-cumulative-
ly for the extract acting for 45 sec. The responses were re-
Effect of antagonists
corded on Ugo Basile Microdynamometer 7050, through
isometric transducer 7004. A 3 min time cycle was found to Prazosin (2.4 x 10-6M) and propranolol (3.4 x 1O-6M)
be adequate. The effect of yohimbine, phenoxybenzamine, did not influence the extract-induced response (Fig.2). Phe-
prazosin and propranolol on the responses of the submaxi- noxybenzamine (3.6 x 1O-7M) attenuated the relaxant ef-
mal concentration of the extract (20llg) was investigated. fect of the extract (Fig.3 a). Yohimbine (3.2 x 10- 7 - 1.3 x
The antagonists were incubated with the tissue 2 min be- 10-6M) caused a dose-dependent block of the relaxant ef-
fore re-establishing responses to the extract. Each antago- fect of the extract (Fig.3 b).
Analysis of th e Gas tro inte stinal Rela xin g Effect of the stern extract of Gongronema latifolium 295
though we have proferred evidence implicating alpha.- Deighton, E C.: Vernacular botanical vocabulary for Sierra Leone.
adrenoceptors in this action, the exact mechanism(s) in- Crown Agent for Overseas Government and Administration,
volved is difficult to determine due to many bioactive con- London,p. 681, 1957.
Di Carlo, G., Mascolo, N., Izzo, A. A., Capasso, E and Autore, G.:
stituents in the extract, and as already stated (Bennett, Effects of quercetin on the gastrointestinal transit in mice. Phy-
1992, Binder, 1992) there are many mechanisms that con- tother. Res. 8: 42-45, 1994.
trol intestinal functions, such as intrinsic and extrinsic Ford, A. P.D. W., Williams, T.]., Blue, D. R. and Clarke, D. E.: AI-
nerves, autacoids and hormones. In view of the wide appli- pha.-adrenocepror classification: sharpening Occam's razor.
cation of this vegetable plant, the health implications of Trends Pharmacal. Sc. 15: 167-170, 1994.
these results are yet to be ascertained. The identification Hoffman, B.B. and Lefkowitz, P.].: Adrenergic receptor antago-
nists. In the Pharmacological Basis for Therapeutics (Gilman, A.
and isolation of the active substance(s) and the mechanism
A., Rall, T. W., Nies, A. S. and Taylor, P. edn.) Pergamon Press,
underlying the action are also subjetcs of further investiga- N. Y., pp.221-243, 1990.
tion. Hsu, W.H.: Xylazine-induced delay of small intestinal transit in
mice. Eur. J. Pharmacal. 83: 55-60, 1982.
Mekean,]. and MacDonald, A.: Analysis of the propranolol-sensi-
Acknowledgement tive relaxation to isoprenaline in rat distal colon. Br. J. Pharma-
The authors are grateful to Mr. A. Ozioko of the Department of cal. 112: p.470, 1994.
Botany, University of Nigeria, Nsukka (UNN) for the identifica- Meli, R., Autore, G., Di Carlo, G. and Capasso, E: Inhibitory ac-
tion of the plants and Mr. David C. Akanwa of National Institute tion of quercetin on intestinal transit in mice. Phytother. Res. 4:
for Pharmaceutical Research and Development (NIPRD) for secre- 201-202,1990.
tarial assistance. Miller, L. C. and Tainter, M. L.: Estimation of ECso and its error by
means of Log-probit graph paper. Proc. Soc. Exp. Biol. Med. 57:
261-269,1944.
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