Antiulcer Pterspermum Plant

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Journal of Pharmacy Research Vol.2.I ssue 5.May 2009

A.K. M anna et al. / Jour nal of Pharmacy Research 2009, 2(5),785-788 Research Article

ISSN: 0974-6943

The antiulcer activity of Ptero sperm um acer i fo l iu m bark extract in experimental animal

A.K. Manna**, AK Behera, J Jena, S Manna, S Karmakar*, Dr.S Kar**, B.R.Panda**, S. Maity***Dept. of pharm Tech. Jadavpur University, kolkata -700032.**Seemanta Institute of pharmaceutical sciences, Jharpokharia, Orissa. 757086.

Received on: 27-09-2008; Accepted on: 28-03-2009

ABSTRACT

The role of ethanolic fraction of Pterospermum acerifolium bark extract on different experimental ulcer models in rats was investigated.Th

extract demonstrated significant antiulcer activity against aspirin, indomethacin & ethanol induced ulcerations, significant inhibition o

gastric secretary volume, and total acidity in pylorus ligated rats were observed to occur with the extract.

Keyw ord s: Pterospermum acerifolium, ulcer , Leukotrienes

*Corresponding author.

E-mail: [email protected]

INTRODUCTION

Pterospermum acerifolium wild (Sterculiaceae) commonly

known as ‘Kanak champa’ is a shurbs distributed in tropical Asia. It

has been traditionally used for blood troubles, inflammation, ulcer,

tumors, leprosy and for small pox eruptions (wealth of India).In an

earlier study in our laboratory, the ethanolic extract of P. acerifolium

was found to possess anti-inflammatory activity.The work was aimed

at the scientific validation of the ethnopharmacological calim about

anti ulcer properties of the bark extract.Earlier studies in our labora-

tory have revealed that the ethanolic fraction of Pterospermum

acerifolium bark extract possesses a significant anti-inflammatory and

analgesic property.6

According to Shay and Sun,21 the genesis of peptic ulcer

mechanism is related to the balance between the defensive and ag-

gressive factors. Gastric mucosa is an active area of arachidonic acid

metabolism (where both cyclo oxygenase and lipoxygenase enzyme

are involved) the integrity of gastric mucosal barrier is influenced by

mucus secretion, acid secretion, and gastric blood flow.18 The gastric

irritance of non-steroidal anti-inflammatory drugs (NSAIDs) on the

gastric mucosa is one of the major disadvantage of their using inflam-

matory. It is well established that NSAIDs causes inhibition of the

synthesis of cytoprotective prostaglandin.

However, according to Cohn4 NSAIDs increase the suscepti-

bility of gastric mucosa to injury by gastric acid bile salt and ethanol.As it is essential to evaluate the ulcerogenic potential of any anti-

inflammatory agent, the same was evaluated with ethanolic fraction

of Pterospermum acerifolium bark extract and it is found that

Pterospermum acerifolium did not possesses ulcerogenic activity.

However, our studies revealed that Pterospermum acerifolium po

sess significant antiulcer activity against various experimental model

of gastro intestinal ulceration in rat. The present study was under

taken to evaluate the effect of Pterospermum acerifolium on differen

experimental models of gastro intestinal ulceration.

MATERIALS & METHODS:

Plants materials P. acerifolium bark were collected from Ea

Midnapur (West Bengal, India) in July 2007 and authenticated by com

parison with a voucher. Specimen in Botanical Survey of Indi

Kolkata.One kg. of the air dried barks were blended to a fine powde

and extracted with Pet. Ether, chloroform and ethanol for 6 day(144hours). The extract was concentrated using a rotavapor. The ex

tract was dissolved in normal saline before orally administrating 15

and 300 mg /kg of the extract to the rats. The preliminary investigatio

for the antiulcer activity

Phytochemical screening:

The extract and its fraction were tested by the librman Burchar

Ferric chlorides, Magnesium tracings and Vanillin sulphuric acid teste

to determine the presence of sterols phenolic compound, flavonoid

and saponins respectively.

Chemicals:

Indomethacin (sigma), aspirine (sigma) and all the chemical collecte

from Sisco laboratory Mumbai.

Plant material:

Authenticated bark of Pterospermum acerifolium were a

dried powdered and subsequently extracted with petroleum ether, chl

roform and ethyl alcohol in a soxhlet extractor. The ethanol extract wa

dried in vacuum and yellowish brown residue was obtained. Just pri

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A.K. M anna et al. / J ournal of Pharmacy Research 2009, 2(5),785-788

to testing, the extract was dissolved in distil water which serve as the

vehicle in our experiments.

Animals used:

Adult Charles Foster rats (of male 140-160g) house and nor-

mal laboratory condition (24 + 20C) were used. They were suppliedwith standard food pellets (water ad libitum). The animal were fasted

for 24 hours prior to experimentation, however they were supplied

with water adlibitum till 1 hour before commencement of the experi-

mentation, how ever they were supplied with water ad libitum till one

hour before commencement of experimentation.

Aspirin induced gastric ulcer:

Animals were divided into three groups (n = 6) Pterospermum

acerifolium(150, 300mg/kg) inter peritoneal and control vehicle were

administered 30 min. before the administration of aspirin (400mg/kg)

per oral [PO]. The animals were scarified, after 6 hours following the

administration of aspirin, stomachs were removed and 2% formalin

was injected into the stomach. The stomach was open along with

greater curvature and immersed in 2% formalin solution. The length of

each lesion was measured under the dissecting microscope (X 10).

The sum of the length (mm) of all lesions for each rat were used in

lesion index.1, 12

Indomethacin induced ulceration:

Male rats tested for 24 hours administered with

Pterospermum acerifolium (150mg/kg) [PO] or the control vehicle and

30min. later, indomethacin (20mg/kg) [PO] was administered. The ani-

mals were sacrificed 18 hours later of the ulcer index was determinedmicroscopically. 17,10

Ethanol induced ulceration:

Male Albino rats were divided into three groups (n = 6)

Pterospermum acerifolium (150, 300mg/kg) and control vehicle was

administered [PO] after 30 min., ethanol (50%, 5ml/kg) was adminis-

tered orally. The animals was sacrificed after one hour and the lesion

index was determined microscopically.18

Gastric secretory study in Pylorus ligated rats:

The effect of Pterospermum acerifolium (150, 300mg/kg) ongastric secretion (volume, pH, total acidity and peptic activity) was

studied in Pylorus ligated rats, Pterospermum acerifolium was ad-

ministered orally 30 min. pyloric ligation. The animals were sacrificed

after 4 hours following pyloric ligation,1 gastric content were con-

trolled and analyzed for volume, acidity ,pH and peptic activity. For

determination of acidity, 0.2ml of gastric juice was taken and diluted to

2ml with distil water in small conical flask; 1 drop of 1% phenopthalin

was then added to it. The total acidity was determined by tritrating

with 0.01N NaOH and was expressed in meq/L/hr .Peptic activity was

determined by the modified Anson method2 as described by Debnath

et al.5 Gastric juice was diluted (1:250) with 0.01N HCL and 1 ml o

diluted gastric juice was taken for further estimation, which was adde

to 2.5ml of 2% haemoglobin solution in 0.06M HCL. The minture wa

incubated at 370C for 20min. and thereafter 0.6m trichloro acitic aci

added. The tubes were kept in an ice bath for 15min. and then centr

Table-1. Effect of Pterospermum aceri fol ium extract on Aspirin inducegastric ulceration (values are expressed as mean + S.E.; n = 6) (Dose Pterospermum aceri foli um extract (T

1– 150 mg/kg and T

2= 300 mg/kg)

standard drug omeprazole = S = 10 mg/kg)

Animal No. Ulcer IndexControl T

1T

2S

1 3.5 1.9 0.4 0.12 3.2 1.7 0.2 0.23 3.1 1.2 0.8 0.34 4.2 1.5 0.4 0.25 4.5 1.3 0.5 0.26 3.8 1.4 0.3 0.3Mean 3.71 1.5 0.43 0.21+ S.E. ±0.095 ±0.047* ±0.008* ±0.007*

% Inhibition 59.66 88.40 94.33

‘P’ values vs. control (by student‘t’ test) * p <0.05

0

2

4

c o T

*

Fig.1.Effect of Pterospermum aceri fol ium extract on Aspirin induce

gastric ulceration (values a*re expressed as mean + S.E.; n =

(Dose of Pterospermum aceri foli um extract (T1

– 150 mg/kg and T

= 300 mg/kg) = standard drug omeprazole = S = 10 mg/kg

‘P’ values vs. control (by student‘t’ test) * p <0.05

Table-2. Effect of Pterospermum aceri fol ium extract on Alcohol induce

gastric ulceration (values are expressed as mean + S.E.; n = 6) (Dose

Pterospermum aceri foli um extract (T1

– 150 mg/kg and T2

= 300 mg/kg)

standard drug omeprazole = S = 10 mg/kg


1T

2S

1 8.1 5.1 2.2 1.22 8.3 6.8 2.8 1.83 8.2 6.1 3.6 1.44 7.6 5.6 3.1 1.35 7.2 5.4 3.8 1.76 8.4 6.2 2.7 1.1Mean 7.9 5.86 3.03 1.41± S.E. ±0.481 ±0.066** ±0.099* ±0.038*% Inhibition 25.82 61.65‘ 82.15

‘P’ values vs. control (by student‘t’ test)* p <0.01),** p <0.05

fuged. 1ml of supernatant was used to determine the concentration

liberated amino acids by the lowry et al9.

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A.K. M anna et al. / Jour nal of Pharmacy Research 2009, 2(5),785-788

0

2

4

6

8

10

c o n t r o l

T 1

T 2

S t d .

U l c e r i n d e x

*

*

**

‘P’ values vs. control (by student ‘t’ test)* p <0.01),** p<0.05

Fig.2. Effect of Pterospermum aceri fol ium extract on Alcohol induced

gastric ulceration (values are expressed as mean + S.E.; n = 6) (Dose of

Pterospermum aceri foli um extract (T1

– 150 mg/kg and T2

= 300 mg/kg) =

standard drug omeprazole = S = 10 mg/kg)


1T

2S

1 2.6 2.1 0.8 0.42 2.8 2.2 0.9 0.23 2.1 1.4 0.5 0.24 2.2 1.3 1.1 0.95 2.3 1.9 0.8 0.66 2.7 1.7 1.2 0.4Mean 2.4 1.7 0.88 0.45±S.E. ±0.118 ±0.15** ±0.101* ±0.074*

% Inhibition 28.97 64.08 81.63

Table-3. Effect of Pterospermum aceri foli um extract on Indometha-

cin (20mg/kg) induced gastric ulceration (values are expressed as

mean + S.E.; n = 6) (Dose of Pterospermum aceri foli um extract (T1–

150 mg/kg and T2= 300 mg/kg) = standard drug omeprazole = S = 10

mg/kg)01

23

C o n

t r o l

T 1 T 2 S t d . U

l c e r i n d e x ( i n

m m

‘P’ values vs. control (by student ‘t’ test)* p <0.01),** p<0

Fig.3.Effect of Pterospermum aceri foli um extract on Indomethac

(20mg/kg) induced gastric ulceration (values are expressed as mea

+ S.E.; n = 6) (Dose of Pterospermum aceri foli um extract (T1

– 15

mg/kg and T2= 300 mg/kg) = standard drug omeprazole = S = 10 m

kg

Animal no Volume (ml/100gm) PH Total acidity Peptic activity mg of

(Meq/lit/hr) tyrosine/mlC T

1T

2S C T

1T

2S C T

1T

2S C T

1T

2

1. 1.8 1.7 1.4 1.3 4 5 5 5 42 37 31 28 16.42 11.13 8.712. 1.7 1.6 1.4 1.2 4 5 6 6 42 30 28 27 16.67 14.23 6.123. 1.6 1.5 1.3 1.3 4 4 6 5 39 31 30 26 17.64 14.18 9.524. 1.9 1.7 1.3 1.2 5 5 5 5 38 33 29 29 15.12 15.54 10.65. 2.1 1.8 1.4 1.4 6 5 5 5 39 30 28 28 16.47 14.16 8.726. 2.1 1.6 1.4 1.3 4 5 6 5 36 33 29 27 17.12 13.61 9.22Mean 1.87 1.65 1.37 1.28 4.5 4.83 5.5 5.1 39.7 32.7 29.1 27.6 16.57 13.64 8.8±S.E.M ±.08 ±.04 ±.02 ±.03 ±.34 ±.17 ±.23 ±.17 ±.93 ±.59 ±.30 ±.34 ±.35 ±.51 ±.61

%inhibition 13.15 36.58 45.52 6.89 18.2 12.9 21.3 36.4 43.5 21.5 88.1

Table 4. Effect of Pterospermum aceri foli um extract on Gastric secretion following Administra-tion of 50% V/v alcohol (5 ml/kg; P.O

pylorus ligated rats [Dose of Pterospermum aceri foli um extract T1 – 150 mg/kg; T2 – 300mg/kg; S-10mg/kg P.o]

Remarks: * Signif icant decrease of volume, total acidi ty, and peptic activity. The PH of gastri c content r emained unaffected in pylorus ligated rats.

RESULTS:

Aspirin induced gastric ulcer:

Pterospermum acerifolium (150, 300mg/kg) significantly in-

hibited gastric ulceration in rats (table –1).There was significant inhi-

bition of ulcer formation with bark extract gastric mucosa retained

almost normal appearance with the higher dose of Pterospermum

acerifolium (300 & 400mg/kg).

Indomethacin induced gastric ulceration:

Significant inhibition of ulceration was observed with bark

extract (150, 300 & 400mg/kg). However at lower dose of Pterospermum

acerifoliumwas very little protection of gastric mucosa (Table-3).

Ethanol induced gastric ulceration:

Pterospermum acerifolium (150, 300 & 400mg/kg) showe

significant inhibitory activity against ethanol induced gastric ulce

ation. Pterospermum acerifolium at a dose of 150mg/kg showed ver

little protective activity and there was considerable damage of th

mucosal layer accompanied with diffused hyperaemia and glandul

disruption (Table-2).

Gastric secretory study following pylorus ligation in rats:

The bark extract at the dose of(300mg /kg) significantly dcreased gastric volume and total acid contain pH remain unchange

(Table-4).However, no significant change could be observed on th

peptic activity in the groups pretreated with Pterospermum acerifoliu

(300mg/kg).

DISCUSSION:

The risk of gastric ulceration is a predominant factor which r

stricts the use of NSAIDs in a variety of inflammatory condition. Studie

with several neutral products in our laboratory reveals that plan

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A.K. M anna et al. / J ournal of Pharmacy Research 2009, 2(5),785-788

such as Brophyllumpinatum,14 P. indica19,20 etc. possess significant

anti – inflammatory and antiulcer activity.

Studies with ethanolic fraction of Pterospermum acerifolium

root extract initially reveals that anti-inflammatory activity may be

due to inhibition of arachidonic acid metabolism. Aspirin and in-

domethacin causes gastro intestinal ulceration by inhibition of gas-tric mucosal biosynthesis of cytoprotective prostaglandin PGE2and

PGI2.16 It may also be mentioned that the inhibition of prostaglandin

biosynthesis may lead to gastric hyper secretion, the damage of gas-

tric mucosa may occur due to the direct action of these drug and

thereby leading to mast cell degranulation and release of histamine

NSAIDs cause shifting of arachidonic acid metabolism to the 5-LO

pathway thereby leading to over production of leucotrienes.18 Our

studies with Pterospermum acerifolium showed that it was capable of

inhibiting aspirin and indomethacin induced gastric ulceration in rats.

Ethanol causes extensive ulceration in fasted animals. Such

ulceration may be attributed to stasis of gastric blood flow, thereby

leading to haemorrhage and necrosis. Early studies reveals that 5-lo product gastric mucosa from ethanol induced ulceration.10 Thus stud-

ies have also shown that intragastric administration of ethanol causes

increased generation of LTC4

resulting in mucosal and sub-mucosal

vasoconstriction of sub-mucosal micro-vessels and tissue necrosis.15

LTD4

has been found to decrese trans gastric potential.16 All these

factors effectively contribute to gastric ulceration and damage.

Further investigation on gastric secretion in pylorus ligated rat, p

acerifolium extract produce significant decrease in gastric volume,

total acidity and peptic activity of gastric juice in animal treated with

alcohol after pylorus ligation. And pH of gastric juice was found to be

unaffected in this contest it may mentioned that ethanol administra-

tion probably induces LTD4 production their by leading to increasesgastric protein contained and decreases transgastric potential (Sen

et al 2002).

Thus the possible reasons of the antiulcer effect of P.acerifolium

may be due to (i) the inihibition of 5-LO enzyme (ii) blockade of LTC4,

LTD4 synthesis (iii) generation of free radicals; and/or (iv) inhibition

of histamine release following mast cell degranulation. One or more

of the mentioned reasons may be responsible for the antiulcer activ-

ity P.acerifolium. Further work in this regard may be done.

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Antiulcer Pterspermum Plant