|
ANTIULCER ACTIVITY OF ROOTS OF ZAPOTECA PORTORICENSIS (FAM. FABIACEAE)
Ukwe C. V.1, Ubaka C. M.1, Adibe M.
O.*1, Okonkwo C. J.1, Akah P. A.2
1Department of Clinical Pharmacy and Pharmacy Management,
Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Nigeria
2Department of Pharmacology and Toxicology, Faculty of Pharmaceutical
Sciences, University of Nigeria, Nsukka 410001, Nigeria.
|
Date of Web Publication
|
15-Aug-2010
|
*Corresponding Author: E-mail: maxolpharmacia@yahoo.com
ABSTRACT
|
|
|
Background:The roots of Zapoteca portricensis is a common remedy in the treatment
gastrointestinal disorders used by tradomedical practitioners in Eastern Nigeria.
Aim:This study was aimed at evaluating the possible antiulcer activity of
the root of this plant in experimental rats.
Methods:A methanolic root extract was prepared by cold maceration. Antiulcer
activity was tested using absolute ethanol and indomethacin induced ulcer models.
Sucralfate (100 mg/kg oral) was used as the reference drug. Different groups of
albino rats of male sex were given three doses (50, 100, 200 mg/kg) of the extract.
Phytochemical analysis of the freshly dried roots was also done.
Results:Phytochemical results revealed presence of alkaloids, terpenoids,
glycosides and flavonoids. The ethanol model produced an average ulceration in rats
with reduction of ulcer (50%, 75% and 90%) seen in all the extract treatment. A
dose dependent inhibition of ulcer was seen in all doses of the extract with doses
100 and 200 mg/kg produced a significant reduction compared with control. In the
indomethacin model, an absolute ulceration was produced in all the animals. Inhibition
of ulcer (57.1%, 65.7% and 80.0%) was seen in the treatments with the extracts in
a dose dependent manner. All the three doses of the extracts produced significant
ulcer protection compared with control.
Conclusion:This study has shown that roots of this plant (Zapoteca portoricensis)
possess potent antiulcer activity.
KEYWORDS:Anti-ulcer, ethanol, indomethacin, ulcer inhibition, Zapoteca portoricensis.
INTRODUCTION
|
|
|
Research into the treatment of ulcer has been intensified after the implication
of Helicobacter pylori in the pathogenesis of most resistant ulcer [1]. The disease has been reported to have high recurrence
and mortality rates especially in complicated cases [2].
Herbal medicine has attracted so much interest in this area especially with herbs
from the tropics. Herbs like the Brazilian “Pau santo” [3], Black pepper [4],
the Indian “Sharpunkha” [5]
etc have been reported to possess potent antiulcer property and so many still to
be investigated. Zapoteca portoricencis, is a perennial shrubby plant with slender
branches, cream colored flowers and flat fruits. It is widely distributed in West
Africa especially in Togo (Misahohe), Gold Coast (Odumase, Aburi), and Southern
Nigeria (Bonny, Oban, Aguku and Lagos). It is also common in the West Indies and
the Atlantic Coast of America. It is popularly called “ELUGELU” in
eastern Nigeria and its leaves are used to treat tonsillitis, spasmodic and other
gastrointestinal disorders. Its roots have been reported to possess anti-inflammatory
activity [6], antifungal and antibacterial
activity [7]. It is often agreed that
agents with antispasmolytic activity may also possess antiulcer activity and this
study however is aimed at evaluating the possible ulcer healing potential of this
plant in experimental rats.
METHODS
|
|
|
Plant Material
The plant was collected in large quantities from the Obukpa and Orba communities
of Nsukka Local Government Area of Enugu State. The plant was then identified by
Mr A.O. Ozioko, taxonomist, of the Bioresources and Development Center Programme
in Nsukka. A voucher specimen of the root was deposited at the hebarium of the Department
of Pharmacognosy, University of Nigeria, Nsukka for future reference (Pcg/SN 89).
Preparation of the Extract
The roots were dried under the sun for 7 days and pulverized into coarse powders.
The coarse powders (weighing 460 g) were subjected to maceration extraction using
2 L analytical methanol with intermittent shaking. The mixture was filtered and
the methanolic extract of Zapoteca portoricensis (MEZP) dried under the shade at
room temperature (yield of 4.13%).
Animals
Healthy adult albino rats of male sex weighing between 100–180 g obtained
from the animal house Department of Pharmacology and Toxicology, University of Nigeria,
Nsukka were used. The animals were housed under standard conditions of light/dark
at 12/12 hr cycle. They were fed with standard animal feed (Nigerfeed, Nigeria)
and allowed free access to clean drinking water. The rats were fasted eighteen hours
before the experiment but were given water ad libitum. Animal experiments were done
in compliance with the National Institute of Health Guide for Care and Use of Laboratory
Animal (Pub No. 85–23, revised 1985).
Preliminary Phytochemical Tests
These tests were carried out according to methods described by Habourne [8].
Antiulcer
Activity
|
|
|
Ethanol Induced Ulcer [9]
Thirty over-night fasted rats were divided into five groups of six rats each. All
the groups of rats were given treatments as follows: group 1 received 5 ml/kg of
3% Tween 80 (control group), group 2 received 100 mg/kg sucralfate (Antepsin®,
Chugai Pharma UK), group 3 received 50 mg/kg, group 4 received 100 mg/kg and group
5 received 200 mg/kg of MEZP. Thirty minutes later, ulcers were induced by administering
1 ml absolute ethanol (99%) to each rat. All administrations were by per oral route.
One hour later all the rats were cuthanized with chloroform. The stomach were excised,
cut along the greater curvature and gently rinsed under tap water. The stomachs
were stretched on a corkboard and a magnifying glass (X10 magnification) used to
spot and count the craters using a severity scale described by. The ulcer index
was obtained by the sum of a group’s crater score and divided by magnification
[10]. Ulcer inhibition (UI) was calculated
using the formula below;

Indomethacin Induced Ulcer [11]
Thirty over-night fasted rats were divided into five groups of six rats each. All
the groups of rats received treatments as follows; group 1 received 5 ml/kg of 3%
Tween 80 (control group), group 2 received 100 mg/kg sucralfate (Antepsin®,
Chugai Pharma UK), group 3 received 50 mg/kg, group 4 received 100 mg/kg and group
5 received 200 mg/kg of MEZP. Thirty minutes later, ulcer was induced with indomethacin
(40 mg/kg) p.o in all the rats. Eight hours later, the rats were sacrificed as above
and their stomachs isolated and cut along the greater curvature. The excised stomachs
were rinsed under tap water and viewed for ulcer craters as described above.
Statistical Analysis
The results of ulcer indices were expressed as mean ± SEM while ulcer inhibition
expressed as a percentage. Differences in mean ulcer index in comparison with control
was done using the one way ANOVA followed by the Dunnett’s multiple comparison
with statistical significance considered at P>0.05 and P>0.01.
RESULTS
|
|
|
Phytochemical Tests
Phtytochemical tests showed abundant presence of alkaloids, terpenoids, steroids,
resins, tannins, saponins and flavonoids.
Effect of MEZP on Ethanol Induced Gastric Models
Antiulcer activity results for the ethanol model are displayed in
Table 1. Ulcer was not produced in all the rats in the treatment group but
with only control group having absolute (100%) ulceration. Ulcer inhibition was
highest with 200 mg/kg of MEZP (93%, p>0.05) which was significant compared with
control. Sucralfate produced the lowest and a non significant ulcer protection (25%).
The extracts produced a dose dependent ulcer inhibition.
Effect of MEZP on indomethacin induced gastric ulcers
Results for indomethacin model can be viewed in Table 2.There
was an absolute production of severe ulcers in all the rats using this model and
ulcer inhibition was seen in all the treatment groups. Ulcer inhibition was highest
with 200 mg/kg MEZP (80%, p>0.01) and lowest with Sucralfate (51.4%) and there
was a dose dependent protection after pre-treatment with the extracts.
DISCUSSION
|
|
|
This study revealed a significant antiulcer activity of the methanolic root extract
of Zapoteca portoricensis using standard ethanol and indomethacin models in rats.
The pathogenesis of ulcer remains controversial but its cause is known to be aggravated
by an imbalance between the aggressive factors (i.e. acid and pepsin) and factors
that maintain mucosal integrity (i.e. mucus, bicarbonate and prostagladins) [12]. The use of sucralfate in this study was due
to its increasing prescription in ulcer patients in this country and specifically
due to its non antisecretory but mucoprotective nature [1]. It is known to act by several mechanisms which include
physical protection of stomach, synthesis of prostaglandins and stimulate mucus
and bicarbonate secretion [13]. It
has been documented to be effective in uncomplicated NSAID induced ulcers [14, 15,
16] but it does not cure ulcers. Ethanol
has been shown to increase the risk of ulcer in humans [13] but produces potent ulceration in rats [9]. It is believed to produce reactive species responsible
for mucosal injury [17] and lipid peroxidation,
a free radical mediated process that ultimately destroys lipids membrane [18]. The extracts produced a relatively potent
antiulcer activity against ethanol induced ulcer which may suggest that the plant
possesses some cytoprotective actions against ethanol induced ulcer. The dose dependent
ulcer inhibition of MEZP further corroborates its possible cytoprotective actions
in this model. The effect was more pronounced that those of sucralfate which may
suggest a different mechanism of action or probably pronounced cytoprotection at
higher doses.
Indomethacin model produces its ulceration by mechanism well understood. It causes
an inhibition of the production of endogenous cytoprotective prostaglandins [19]. However with the inhibition of ulcer in this
model by the extract, it is possible that the plant produces a cytoprotection similar
to those of sucralfate in the indomethacin model. The smallest dose produced activity
higher than sucralfate which shows its effectiveness in ulcer inhibition at low
doses. Its dose dependent effect proves it has a sustained and increased antiulcer
activity. The secondary metabolites identified may also have been responsible for
the antiulcer activity of this plant as flavonoids have been reported to possess
antiulcer activity in various experimental models of ulcers [20]. The exact mechanism cannot be emphasized and further
studies are undergoing to analyze its exact gastro protective activity.
CONCLUSION
|
|
|
This study had shown that roots of Zapoteca portoricensis possess antiulcer activity
against alcohol and indomethacin ulcers in rats.
ACKNOWLEDGEMENT
|
|
|
Special appreciation goes to Mr. S.O Igboeme of the Science Laboratory Department,
University of Nigeria for his technical assistance in this study.
REFERENCES
|
|
|
|
1.
|
Siepler JK and Smith-Scott C. Upper gastrointestinal disorders. In: Koda-Kimble
MA, Young LY, Kradjan WA and Guglielmo BJ. Applied therapeutics: The clinical use
of drugs. 8th ed. Lippincott Williams and Wilkins. 2005; 27–30.
|
|
2.
|
Ojewole EB. Peptic ulcer disease. In. Aguwa CN (ed). Therapeutic basis of Clinical
Pharmacy in the tropics. 3rd edn. SNAAP Press, Enugu. 2004; 541–564.
|
|
3.
|
Goulart YCF, Sela VR, Obici S, Vanessa J, Martins C, Otorbone F, Cortez DA, et al.
Evalaution of gastric antiulcer activity in a hydro-ethanolic extract from Kielmeyera
coriacea. Brazilian Archives of Biology and Technology. 2005; 48 (1): 211–216.
|
|
4.
|
Singh R., Madan J., Rao S.H. Antiulcer activity of black pepper against absolute
ethanol induced gastric mucosal damage in mice. Pharmacognosy magazine 2008; 4(15):
232–235.
|
|
5.
|
Deshpande SS, Shah GB and Parmar. Antiulcer activity of Tephrosia Purpurea. Indian
Journal of Pharmacology. 2003; 35: 168–172.
|
|
6.
|
Nwodo NJ and Uzochukwu CI. Studies on anti-inflammatory and antimicrobial activities
of crude methanol extracts of Zapoteca portoricensis Jacq. H. Hernanadez. Recent
progress in Medicinal Plants. 2008; 19 (7): 61–69.
|
|
7.
|
Esimone CO, Onuh PU, Obitte NC, Egege MK and Ugoeze KC. In vitro evaluation of lozenges
containing extracts of roots of Zapoteca portoricensis (FAM: Fabaceae). Journal
of Pharmacology and Toxicology. 2009; 4(3): 132–137.
|
|
8.
|
Evans WC. Trease and Evan’s Textbook of Pharmacognosy. 13 edn. Bailliere
Tindall, London. 1989: 315–679.
|
|
9.
|
Robert A, Nezamis JE, Lancaster C and Hanchar AJ. Cytoprotection by prostaglandins
in rats: Prevention of gastric necrosis produced by alcohol, HCl, NaOH, Hypertonic
NaCl and thermal injury. Gastroentrology. 1979; 17: 433–443.
|
|
10.
|
Tan PV, Dimo T and Dongo E. Effects of methanol cyclohexane and methylene chloride
extracts of Bidens pilosa on various gastric ulcer models in rats. J. Ethnopharmacol.
2000; 73: 415–421.
|
|
11.
|
Urushidani T, Kashuya Y and Okabe S. The mechanism of aggravation of indomethacin
induced gastric ulcer by adrenalectomy in rats. Journal of Pharmacology. 1979; 29:
715–780.
|
|
12.
|
Berardi RR and Welage SL. Peptic Ulcer Disease. In: Dipiro TJ, Talbert RL, Yees
GC, Matzke GR, Wells GB and Posey ML. Pharmacotherapy: a pathophysiologic approach.
6 edn. McGraw-Hill. Pp 632–648.
|
|
13.
|
Del Valle J. Peptic ulcer disease and related disorders. In: Kasper DL, Braunwald
E, Fauci AS, Hauser SL, Longo DL and Jameson JL (eds). Harrison’s Principles
of Internal of Medicine. 16th ed. McGraw-Hill. pp 1746–1762.
|
|
14.
|
Del Valle J, Chey WD., Scheiman JM, et al. Acid peptic disorders. In: Yamada T,
Aplers DH, Kaplowitz N, et al, (eds). Textbook of Gastroenterology. 4th ed. Philadelphia,
Lippincott Williams & Wilkins. 2003: 1321–1376.
|
|
15.
|
Laine L. Approaches to nonsteroidal anti-inflammatory drug use in the high-risk
patient. Gastroenterology. 2001; 120: 594–606.
|
|
16.
|
Wolfe MM, Lichtenstein DR and Singh G. Gastrointestinal toxicity of nonsteroidal
anti-inflammatory drugs. N Engl J Med. 1999; 340: 1888–1899.
|
|
17.
|
Pihan G, Regillo C, and Szabo S. Free radicals and lipid peroxidation in ethanol-or
aspirin-induced gastric mucosal injury. Digestive Diseases Sciences. 1987; 32: 1395–1401.
|
|
18.
|
Cheesman KH. Lipid peroxidation in biological systems. Ellis Horwood, London. 1993;
12–17.
|
|
19.
|
Lanza FL. A guideline for the treatment and prevention of NSAID-induced ulcers.
Am J Gastroenterol. 1998; 90: 2037–45.
|
|
20.
|
Parmar NS and Parmar S. Antiulcer potential of flavonoids. Indian J Physiol Pharmacol.
1998; 42: 343–51.
|


|