Planta Med 2007; 73(3): 241-250
DOI: 10.1055/s-2007-967125
Original Paper
Pharmacology
© Georg Thieme Verlag KG Stuttgart · New York

Hypoglycaemic Constituents of Stachytarpheta cayennensis Leaf

A. C. Adebajo1 , E. O. Olawode1 , O. R. Omobuwajo1 , S. A. Adesanya1 , F. Begrow2 , A. Elkhawad2 , M. A. Akanmu3 , R. Edrada4 , P. Proksch4 , T. J. Schmidt5 , M. Klaes5 , E. J. Verspohl2
  • 1Department of Pharmacognosy, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria
  • 2Department of Pharmacology, Institute of Pharmaceutical and Medicinal Chemistry, Münster, Germany
  • 3Department of Pharmacology, Faculty of Pharmacy, Ile-Ife, Nigeria
  • 4Institute of Pharmaceutical Biology, Düsseldorf, Germany
  • 5Institute of Pharmaceutical Biology and Phytochemistry, Münster, Germany
Further Information

Publication History

Received: April 4, 2006

Accepted: January 15, 2007

Publication Date:
22 February 2007 (online)

Abstract

The aqueous infusion (tea) of Stachytarpheta cayennensis leaves is used ethnomedically in Peru, Nigeria and other tropical countries for the management of diabetes. Oral administration (p. o.) of aqueous (125 mg/kg) and methanolic (2000 mg/kg) extracts of the leaves to alloxan-diabetic rats showed significant blood glucose reductions by 43 and 53 %, respectively, at the end of a 4 hour period similar to the strong effect of glibenclamide (5 mg/kg, p. o.). The methanolic extract was successively partitioned into ethyl acetate, butanol and water fractions, and the same test showed that the butanol fraction (2000 mg/kg) had the highest (50 %) hypoglycaemic activity at 4 hours after oral administration. It was also the most active fraction when tested in vitro [insulin release from an insulin secreting cell line (INS-1)] and was also active in normal rats and rats made hyperglycaemic by a glucose load. Its activity was comparable to that of glibenclamide (positive control) in these models. This active butanol fraction was subjected to chromatographic subfractionation; some subfractions reduced hyperglycaemia in alloxan-diabetic rats to 60 and 78 % and induced insulin release from the INS-1 cells; other subfractions, however, gave hyperglycaemic activities in vivo and inhibition of insulin release from the INS-1 cells. Three major compounds of the butanol fraction were isolated and characterised as 6β-hydroxyipolamide, ipolamide and isoverbascoside; they increased insulin secretion from INS-1 cells to 125, 128 and 127 %, respectively, whereas glibenclamide increased insulin secretion to 157 %. The results justify the ethnomedical use of the plant in the management of diabetes and suggest that the butanol fraction and some of its isolated constituents mediate their actions primarily by stimulating insulin release directly.

Abbreviations

AQ, H2O: aqueous/water extract of the leaf

DNC: diabetic negative control rats given only saline

GLB: diabetic positive control rats given 5 mg/kg of
glibenclamide (a standard antidiabetic agent)

HEPES: N-(2-hydroxylethyl)piperazine-N’-2-ethanesulphonic acid

HPLC: high pressure liquid chromatography

INS-1: rat insulinoma cell line (insulin secreting cell line)

KRBH: Krebs-Ringer-bicarbonate buffer with HEPES

NGR: normoglycaemic control rats given only saline

RPMI medium: Roswell Park Memorial Institute medium

SCA, EtOAc: ethyl acetate partition fraction of SCM

SCB, BuOH: butanol partition fraction of SCM

SCM, MeOH: methanolic extract of the leaf

SCW, H2O: aqueous/water partition fraction of SCM

TLC: thin layer chromatography

To: Time (0 h) of administration of the extract/fraction/drug

Tt: 1, 2 and 4 h after administration of the extract/fraction/drug

VLC: vacuum liquid chromatography

References

  • 1 Fajan S S. What is diabetes, definition, diagnosis and causes.  Med Clin J N Am. 1971;  55 793-5.
  • 2 Momo C EN, Oben J E, Tazoo D, Dongo E. Antidiabetic and hypolipidemic effects of Laportea ovalifolia (Urticaceae) in alloxan induced diabetic rats.  Afr J Trad CAM. 2006;  3 36-43.
  • 3 Ivorra M D, Payá M, Villar A. A review of natural products and plants as potential antidiabetic drugs.  J Ethnopharmacol. 1989;  27 243-75.
  • 4 Prince S PM, Menon V P, Pari L. Hypoglycaemic activity of Syzygium cumini seed: effect on lipid peroxidation in alloxan-diabetic rats.  J Ethnopharmacol. 1998;  61 1-7.
  • 5 Roman-Ramos R, Flores-Saenz J L, Alarcon-Aquilar F J. Anti-hyperglycaemic effect of some edible plants.  J Ethnopharmacol. 1995;  48 25-32.
  • 6 Verspohl E J. Recommended testing in diabetes research.  Planta Med. 2002;  68 581-90.
  • 7 Ahmad M, Akhtar M S, Malik T, Gilani A H. Hypoglycaemic action of the flavonoid fraction of Cuminum nigrum seeds.  Phytother Res. 2000;  14 103-6.
  • 8 Haselwood E L, Motter G G. Handbook of Hawaiian weeds. Hawaii; University of Hawaii Press, Honolulu 1966: 334
  • 9 Balik M J. Notes on some medicinal and poisonous plants of Amazonian Peru.  Adv Econ Bot. 1985;  1 1-8.
  • 10 Akanmu M A, Olayiwola G, Ukpomwan O E, Honda K. Acute toxicity and sleep-wake EEG analysis of Stachytarpheta cayennensis (Verbenaceae) in rodents.  Afr J Trad CAM. 2005;  2 222-32
  • 11 Schapoval E ES, Winter de Vargas M R, Chaves C G, Bridi R, Zuanazzi J A, Henriques A T. Anti-inflammatory and antinociceptive activities of extracts and isolated compounds from Stachytarpheta cayennensis .  J Ethnopharmacol. 1998;  60 53-9
  • 12 Vela S M, Souccar C, Lima-Landman M T, Lapa A J. Inhibition of gastric acid secretion by the aqueous extract and purified extract of Stachytarpheta cayennensis .  Planta Med. 1997;  63 36-9
  • 13 Robinson R D, Williams L A, Lindo J F, Terry S I, Mansingh A. Inactivation of Strongyloides stercoralis filariform larvae in vitro by six Jamaican plant extracts and three commercial anthelmintics.  W Ind Med J. 1990;  39 213-7.
  • 14 Schmeda-Hirshmann G, Rojas de Arias A. A screening method for natural products on Triatomine bugs.  Phytother Res. 1992;  62 68-73.
  • 15 Duke J A, Vazquez Martrinez R. Amazonian Ethnobotanical Dictionary (Peru). Boca Raton; CRC Press 1994: 210-5
  • 16 Lin S R, Chen A H. Phytochemical study on Stachytarpheta jamaicensis .  Chung-Kuo Nung Yen Hua Hsuehib Hui Chih. 1976;  15 151-3
  • 17 Taoubi K, Fauvel M T, Glieye J, Rouraste I. Caffeic and heteroside esters from Verbenaceae.  Polyphenols. 1992;  16 174-7.
  • 18 Damtoft S, Jensen S R, Nielsen B J. The identity of the iridoid glucoside tarphetalin with Ipolamide.  Phytochemistry. 1984;  23 907-8.
  • 19 De Costa A O. Pharmacognosy of Stachytarpheta jamaicensis .  Rev Bras Farmacol. 1960;  41 135-6.
  • 20 Saha J C, Savini E C, Kasinathan S. Ecbolic properties of Indian medicinal plants, Part 1.  Ind J Med Res. 1961;  49 130-51.
  • 21 Melita R S, Castro O. Pharmacological and chemical evaluation of Stachytarpheta cayennensis .  Rev Biol Trop. 1996;  44 353-9.
  • 22 Bozdag O, Verspohl E J, Ertan R. Synthesis and hypoglycaemic activity of some new flavones derivatives 11(4’-Flavonyl-2,4-thiazolidinediones).  Arzneimittelforschung/Drug Res. 2000;  50 539-43.
  • 23 Verspohl E J, Bauer K, Neddermann E. Antidiabetic effect of Cinnamomum cassia and Cinnamomum zeylanicum in vivo and in vitro .  Phytother Res. 2005;  19 203-6.
  • 24 Goldner M, Gomori G. Alloxan-induced diabetes.  Endocrinology. 1943;  33 297-9.
  • 25 Defronzo R A. Pharmacological therapy for type II diabetes mellitus.  Ann Intern Med. 1999;  131 281-303.
  • 26 Gilman A G, Rall T W, Nies A S, Tayer P. Goodman and Gilman’s: Pharmacological basis of therapeutics, 8th edition. New York; Pergamon Press 1990: 1317-22, 1463 - 95.
  • 27 De Luca C, Guiso M, Martino C. 6β-Hydroxyipolamide, an iridoid glucoside from Stachytarpheta mutabilis .  Phytochemistry. 1983;  22 1185-7.
  • 28 Kanchanapooma T, Kasaia R, Yamasakia K. Phenolic glycosides from Barnettia kerrii .  Phytochemistry. 2002;  59 565-70.
  • 29 Miyase T, Koizumi A, Ueno A, Noro T, Kuroyanagi M, Fukushima S. et al . Studies on the acyl glycosides from Leucoseptrum japonicum .  Chem Pharm Bull. 1982;  30 2732-7.

Dr. Adeleke Clement Adebajo

Department of Pharmacognosy

Faculty of Pharmacy

Obafemi Awolowo University

Ile-Ife

Nigeria

Phone: +80-3367-9390

Fax: +80-5624-4750

Email: caadebajo@yahoo.com

Email: aadebajo@oauife.edu.ng