Analgesic, anti-inflammatory and antipyretic activities of the petroleum ether fraction from the ethanol extract of Desmodium podocarpum

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DOI: 10.1016/j.jep.2010.11.042 · Source: PubMed
Abstract
Desmodium podocarpum is a plant that has been used in the folk medicine to treat febrile diseases, cough and bleeding wounds. However, there is no scientific basis or reports in the modern literature regarding its effectiveness as an analgesic, anti-inflammatory and antipyretic agent. The objective of this study is to evaluate the analgesic, anti-inflammatory and antipyretic activities of the petroleum ether fraction (PEF) from the ethanol extract of Desmodium podocarpum. PEF (50, 100, 200 mg/kg) was estimated for its pharmacological properties by using the acetic acid-induced writhing test, the hot plate test, the Carrageenan-induced rat paw edema model, the dimethylbenzene-induced mouse inflammation model, and the lipopolysaccharide (LPS)-induced rat fever model. In addition, the acute toxicity of PEF was also studied. PEF significantly and dose-dependently inhibited the writhing responses in mice, increased reaction time of mice in the hot plate test, reduced carrageenan-induced paw edema in rats and the dimethylbenzene-induced ear edema in mice, and attenuated LPS-induced fever in rats. No death of mice was observed when orally administered PEF up to 4.2 g/kg. These findings suggest that PEF possesses evident analgesic, anti-inflammatory and antipyretic activities, and has a favorable safety, which supports the use of Desmodium podocarpum as an analgesic, anti-inflammatory and antipyretic drug in the folk medicine.
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Contents lists available at ScienceDirect
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Ethnopharmacological communication
Analgesic, anti-inflammatory and antipyretic activities of the petroleum ether
fraction from the ethanol extract of Desmodium podocarpum
Zhan-Zhou Zhu
a
, Ke-Jia Ma
a,b
, Xia Ran
a,c
, Hong Zhang
a,
, Cheng-Jian Zheng
a
, Ting Han
a
,
Qiao-Yan Zhang
a
, Lu-Ping Qin
a,∗∗
a
Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, No. 325, Guohe Road, Shanghai 200433, PR China
b
College of Pharmacy, Jiamusi University, Jiamusi 154007, PR China
c
School of Life Science, East China Normal University, Shanghai 200062, PR China
article info
Article history:
Received 10 August 2010
Received in revised form 25 October 2010
Accepted 18 November 2010
Available online 30 November 2010
Keywords:
Desmodium podocarpum
Analgesic
Anti-inflammatory
Antipyretic
Acute toxicity
abstract
Ethnopharmacological relevance: Desmodium podocarpum is a plant that has been used in the folk medicine
to treat febrile diseases, cough and bleeding wounds. However, there is no scientific basis or reports in the
modern literature regarding its effectiveness as an analgesic, anti-inflammatory and antipyretic agent.
Aims of the study: The objective of this study is to evaluate the analgesic, anti-inflammatory and antipyretic
activities of the petroleum ether fraction (PEF) from the ethanol extract of Desmodium podocarpum.
Materials and methods: PEF (50, 100, 200 mg/kg) was estimated for its pharmacological properties by using
the acetic acid-induced writhing test, the hot plate test, the Carrageenan-induced rat paw edema model,
the dimethylbenzene-induced mouse inflammation model, and the lipopolysaccharide (LPS)-induced rat
fever model. In addition, the acute toxicity of PEF was also studied.
Results: PEF significantly and dose-dependently inhibited the writhing responses in mice, increased
reaction time of mice in the hot plate test, reduced carrageenan-induced paw edema in rats and the
dimethylbenzene-induced ear edema in mice, and attenuated LPS-induced fever in rats. No death of
mice was observed when orally administered PEF up to 4.2 g/kg.
Conclusions: These findings suggest that PEF possesses evident analgesic, anti-inflammatory and
antipyretic activities, and has a favorable safety, which supports the use of Desmodium podocarpum as an
analgesic, anti-inflammatory and antipyretic drug in the folk medicine.
© 2010 Elsevier Ireland Ltd. All rights reserved.
1. Introduction
Desmodium podocarpum DC., a type of shrub belonging to the
family Leguminosae, is widely found in Yunnan, Gansu, Guizhou
and other Southwest Provinces in China. In Chinese folk medicine,
the whole plant of Desmodium podocarpum is used in the treatment
of febrile diseases, cough and bleeding wounds for its functions of
clearing away heat and toxic materials and cooling blood (Editorial
committee of Chinese Materia Medica, 1999).
There are many extracts from plants of this genus Desmodium
that have been proven to possess anti-inflammatory, analgesic and
antipyretic activities in many animal models. For example, the
ethanol extract of the leaves of Desmodium adscendens (Sw.) DC. var.
adscendens, a medicinal plant in the African traditional medicine,
could induce hypothermia and had an analgesic effect in mice
∗∗
Corresponding author. Tel.: +86 21 81871300.
Corresponding author. Tel.: +86 21 81871305.
E-mail addresses: lpqin@smmu.edu.cn (L.-P. Qin)
zhanghong@smmu.edu.cn (H. Zhang).
(N’gouemo et al., 1996). The aqueous extract of Desmodium adscen-
dens also had anti-anaphylactic properties in guinea pigs, which
could reduce the lung histamine content in a dose-dependent
manner, elicited a dose-dependent reduction in the amount of
spasmogens released, and inhibited histamine-induced contraction
of ileal muscle (Addy and Dzandu, 1986). The methanol extract
from Desmodium triflorum DC. decreased the acetic acid-induced
writhing responses in mice and the licking time on the late phase in
the formalin test, and inhibited -carrageenan-induced paw edema
in mice. The anti-inflammatory mechanism of Desmodium triflorum
might be related to the decrease in the level of malondialdehyde
(MDA) in the edema paw via increasing the activities of superox-
ide dismutase (SOD) and glutathione reductase (GRd) in the liver,
and the reduction in the nitric oxide (NO) level via regulating the
interleukin-1 (IL-1) production and the level of tumor necrosis
factor- (TNF-) in the inflamed tissues (Lai et al., 2009). The aque-
ous extract of root and aerial parts of Desmodium gangeticum DC.
was also found to have significant anti-inflammatory and analgesic
activities in experimental animals (Rathi et al., 2004).
Although a number of plants belonging to the genus Desmod-
ium have been investigated on their chemical components and
0378-8741/$ see front matter © 2010 Elsevier Ireland Ltd. All rights reserved.
doi:10.1016/j.jep.2010.11.042
Author's personal copy
Z.-Z. Zhu et al. / Journal of Ethnopharmacology 133 (2011) 1126–1131 1127
pharmacological effects, there seems to be no report on the anal-
gesic, antipyretic and anti-inflammatory activities of the plant
Desmodium podocarpum. In this study, the above activities of the
petroleum ether fraction (PEF) from the ethanol extract of Desmod-
ium podocarpum were evaluated in mice and rats to substantiate
and expand its clinical applications. In addition, we determined
acute oral toxicity of PEF which exhibited a good security.
2. Materials and methods
2.1. Plant material and extraction
The whole plant of Desmodium podocarpum was collected in
Jiande of Zhejiang Province in July 2009 and identified by Professor
Lu-Ping Qin, a pharmacognosist from the Department of Pharma-
cognosy, School of Pharmacy, Second Military Medical University
(Shanghai, China). A voucher specimen of Desmodium podocarpum
was deposited with the number SY3245 in the Herbarium of the
Department of Pharmacognosy, School of Pharmacy, Second Mili-
tary Medical University (Shanghai, China). The dried plant (500 g)
was pulverized with a motor-driven grinder to prepare the extract.
After refluxing extraction with 8 L 85% (v/v) aqueous ethanol at
55
C four times for 0.5 h each time, the extract was filtered and
then the solvent was evaporated to get the ethanol extract of
Desmodium podocarpum (DPE, 59.54 g) under reduced pressure in a
rotary evaporator. Further, the crude ethanol extract of the whole
plant was sequentially fractionated into five sub-extracts explicitly,
namely, petroleum ether, dichloromethane, ethyl acetate (EtOAc),
n-butanol, and remaining water extracts. The petroleum ether frac-
tion (PEF) was concentrated under reduced pressure to obtain a
residue (16.24 g) for bioactivity determination.
2.2. GC–MS analysis
GC–MS analysis was performed for determination of PEF com-
position with a Finnigan Voyager gas chromatograph fitted with
a fused silica VF-5 ms capillary column (3 m × 0.25 mm; coating
thickness 0.25 m, VARIAN, USA) using the following tempera-
ture program. The initial temperature was 50
C, raised to 180
C
at 15
C/min, and then it was raised to 300
Cat5
C/min and held
for 15 min. The injector temperature was 240
C and the MS source
Helium was used as the carrier gas at a flow rate of 1.0 ml/min with
a split ratio of 50:1 (v/v). The gas chromatograph was coupled to
a Finnigan Voyager mass selective detector. The ionization source
temperature was 250
C.
2.3. Animals
ICR mice (20–25 g), male Sprague-Dawley (SD) rats (200–220 g)
and male Wistar rats (200–220 g), obtained from the Experimental
Animal Center of the Second Military Medical University (Shang-
hai, China), were housed in a regulated environment (20 ± 2
C),
with a 12 h light/dark cycle (08:00––20:00, light). The animals
were deprived of food for 15 h before the experiment, with free
access to drinking water. Each animal was used only once in the
experiment. All animal treatments were strictly in accordance with
international ethical guidelines concerning the care and use of lab-
oratory animals, and all the experiments were carried out under
the approval of the Committee of Experimental Animal Adminis-
tration of the University. Each experimental group consisted of 10
animals.
2.4. Drugs and reagents
The following reagents and drugs were used: ethanol (AR),
dimethylbenzene (AR) and acetic acid (AR) (Sinopharm chem-
ical reagent Co. Ltd., China), aspirin, ibuprofen, indomethacin,
dexamethasone, paracetamol (Chengdu Pharmaceutical Factory,
Chengdu, China), lipopolysaccharide, and carrageenan (Sigma, St.
Louis, MO, USA).
2.5. Treatment
PEF, aspirin, ibuprofen, indomethacin, dexamethasone and
paracetamol were respectively dissolved in distilled water prior to
administration. Four groups of animals (n = 10) were orally admin-
istered 50, 100, 200 mg/kg PEF and 350 mg/kg DPE, respectively, by
intubation. The positive group of animals (n = 10) were respectively
given aspirin (100 mg/kg), ibuprofen (200 mg/kg), indomethacin
(5 mg/kg), dexamethasone (5 mg/kg) and paracetamol (100 mg/kg)
in different experiments. Another group of animals (negative con-
trol group, n = 10) were given distilled water, and it was run
concurrently with the drug-treated groups, all of which were given
in a volume of 10 ml/kg body weight irrespective of dose.
2.6. Analgesic test
The peripheral analgesic activity of PEF was evaluated in male
mice using the acetic acid-induced writhing test (Garcia et al.,
2004), while central analgesic activity of PEF against thermal stim-
uli was studied in female mice using the hot plate test (Franzotti
et al., 2000).
In the writhing test, male mice (n = 10) were orally adminis-
tered DPE, PEF or aspirin (100 mg/kg), respectively, before 1 h of
intraperitoneal injection of acetic acid (1%, 10 ml/kg). The number
of writhing reflexes was counted during the following 15 min and
the experiment was repeated twice.
In the hot plate test, a transparent glass cylinder with 23 cm high
and 23 cm diameter was used to keep the mouse on the heated
surface of the plate. The temperature of the hot plate was main-
tained at 55 ± 0.5
C by using a thermo-adjustable water-circulating
pump. The reaction time was noted by observing either the lick-
ing of the hind paws or the jumping movements to avoid thermal
pain. After pre-treatment latencies were determined before one
day of the experiment, only mice that showed initial nociceptive
responses between 5 and 30 s were selected for the experiment.
The post-treatment reaction time of each animal was recorded after
30, 60, 90 and 120 min of administration of DPE, PEF or ibuprofen
(200 mg/kg), respectively.
2.7. Anti-inflammatory test
The anti-inflammatory activity of PEF was evaluated with both
carrageenan-induced rat paw edema model (Winter et al., 1962)
and dimethylbenzene-induced mouse inflammation model (Zheng
et al., 2009).
In the rat paw edema test, male Wistar rats were used and acute
inflammation was produced by subplantar injection of 0.1 ml of
freshly prepared 1% (w/v) carrageenan in normal saline into the
right hind paws of rats. Paw volume was measured plethysmomet-
rically using a paw edema calcimeter (YLS-7A Shandong Academy
of Medical Science device station, Shandong) at 0, 0.5, 1, 2, 3, 4 and
6 h after carrageenin injection. Animals were orally premedicated
with DPE, PEF or indomethacin (5 mg/kg) before 0.5 h of injection.
The mean increase in paw volume was measured and inhibitory
percentage was calculated. The edema rate of rats was calculated
as follows:
Edema rate (%) =
V
t
V
0
V
0
× 100
where V
0
is the volume before carrageenan injection (ml); V
t
is the
volume at t h after carrageenan injection (ml).
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1128 Z.-Z. Zhu et al. / Journal of Ethnopharmacology 133 (2011) 1126–1131
Fig. 1. Fingerprint of PEF analyzed by GC–MS. (A) 2,6,10,14,18,22-tetracosahexaene-2,6,10,15,19,23-hexamethyl, (B) -sitostero and (C) -tocopherol--d-mannoside.
In the dimethylbenzene-induced ear edema test, DPE, PEF or
dexamethasone (5 mg/kg) was orally administered before 1 h of
topical application of dimethylbenene (40 l/ear) to the right ears
of mice. The ear swelling was measured by subtracting the weight
of the left ear from that of the right after 1 h of dimethylbenzene
treatment as reported in the literature (Zheng et al., 2009).
2.8. Antipyretic test
The antipyretic activity of DPE and PEF was evaluated accord-
ing to the method reported (Santos and Rao, 1998a). SD rats were
trained previously to be kept quiet under minimal restraint in a
special rat stock for half an hour at a time. The animals were free
to move their limbs and necks and remained in an alert condi-
tion. The temperature in external auditory meatus was measured
in a temperature-controlled room (ambient temperature 20 ± 2
C)
using an electronic temperature recorder (DT-IDB, Shanghai Med-
ical Instruments Factory, Shanghai). The animals were randomly
divided into six groups based on their basal temperature measured
before experiment. Rat fever can be induced by intraperitoneal
injection of LPS (1 mg/kg). SD rats were pretreated with LPS
after 0.5 h of the oral administration of DPE, PEF or paracetamol
(100 mg/kg). The temperature was measured every 30 min from 9
a.m to 17 p.m.
2.9. Acute toxicity
The acute toxicity test for PEF was carried out to evaluate any
possible toxicity. ICR mice of either sex were tested by orally admin-
istering different doses of the extract by increasing or decreasing
the dose according to the responses of animals (Bruce, 1985). The
given maximum dose was 4.2 g/kg, while the control group only
received distilled water. All animals were observed for any gross
effect or mortality within 7 days.
2.10. Statistical analysis
The data were analyzed using a SPSS 13.0 statistical package.
Data for multiple comparisons were performed by one-way ANOVA
followed by LSD t-test. A value of P < 0.05 was considered statisti-
cally significant and all results are presented as mean ± SD.
3. Results
3.1. Chemical compounds in PEF
GC–MS analysis showed that dozens of compounds
were detected from the petroleum ether fraction (PEF)
and the major components were 2,6,10,14,18,22-tetracosa
hexaene-2,6,10,15,19,23-hexamethyl, -sitostero, -tocopherol-
-d-mannoside, 3,7,11,15-tetramethyl-2-hexadecen-1-ol,
Bis(2-ethylhexyl)-phthalate, phytol, 2,4-bis(1, 1-dimethylethyl)-
phenol with relative contents of 10.48%, 7.89%, 7.88%, 5.64%, 4.98%,
2.49% and 1.23%, respectively (Fig. 1).
3.2. Effects of PEF on writhing reflex of mice
In the writhing test, intraperitoneal injection of acetic acid evi-
dently resulted in writhing reflexes of mice. The ethanol extract
of Desmodium podocarpum (DPE) reduced the number of writhing
responses, while PEF much more significantly inhibited the number
of writhing responses in a dose-dependent manner within 15 min
of injection of acetic acid. The writhing number of the mice given
high dose of PEF (200 mg/kg) was even lower than that of the mice
received aspirin (Fig. 2).
Fig. 2. Effects of PEF on writhing reflex of mice in the writhing test. When mice were
intraperitoneally injected with 1% acetic acid (10 ml/kg), the writhing times were
counted immediately for 15 min. The experiment was repeated two times. Data are
presented as mean ± SD, n = 10. *P < 0.05, **P < 0.01, significance versus control.
Author's personal copy
Z.-Z. Zhu et al. / Journal of Ethnopharmacology 133 (2011) 1126–1131 1129
Fig. 3. Effects of PEF on hot-stimulated mice in the hot plate test. The latency period was recorded when female mice were putted on the hot plate maintained at 55 ± 0.5
C.
Data are presented as mean ± SD, n = 10. *P < 0.05, **P < 0.01, significance versus control.
3.3. Effects of PEF in hot-stimulated mice
In the hot plate test, the antinociceptive activity of PEF was also
significantly revealed, of which the duration of action was more
than 120 min. PEF markedly prolonged the latency period of mice,
when compared with negative group of animals given distilled
water (Fig. 3).
3.4. Effects of PEF on carrageenan-induced paw edema in rats
As shown in Fig. 4, subplantar injection of carrageenan notice-
ably induced paw edema in rats, which persisted for over 6 h.
However, PEF was found to be effective as an anti-inflammatory
agent at a higher dose (200 mg/kg). The percentage of paw edema
in rats was significantly reduced by administration of 200 mg/kg
PEF, which lasted for 6 h, when compared with the model group of
rats given distilled water.
3.5. Effects of PEF on dimethylbenzene-induced ear edema in mice
Effects of pre-treatment with PEF on mouse ear edema induced
by dimethylbenzene are shown in Fig. 5. Dimethylbenzene evi-
dently increased ear edema in mice, but PEF significantly inhibited
ear edema, when compared with the control group. These results
revealed that PEF possesses a good activity against acute inflam-
mation induced by dimethylbenzene.
Fig. 4. Effects of PEF on carrageenan-induced paw edema in rats. When 0.1 ml of
freshly prepared 1% (w/v) carrageenan was injected subplantarly into the right
hind paws of male rats, acute inflammation was induced. Data are presented as
mean ± SD, n = 10. *P < 0.05, **P < 0.01, significance versus control.
Fig. 5. Influence of PEF on dimethylbenzene-induced ear edema in mice. Mice were
orally given PEF or dexamethasone before 1 h of topical application of dimethyl-
benene (40 l/ear) to the right ears of mice. Data are presented as mean ± SD, n = 10.
*P < 0.05, **P < 0.01, significance versus control.
3.6. Effects of PEF on fever in rats
As shown in Fig. 6, lipopolysaccharide (LPS) evidently elevated
the temperature in rats from 9 a.m. to 17 p.m. In contrast to the
control group of animals given distilled water, the temperature in
the rats received PEF significantly decreased in a time- and dose-
Fig. 6. Time course of the effects of PEF on the change of the temperature in exter-
nal auditory meatus of rats. The rats were injected with LPS after 0.5 h of the oral
administration of PEF or paracetamol. The temperature was measured every 30 min
from 9 a.m. to 17 p.m. Data are presented as mean ± SD, n = 10. *P < 0.05, **P < 0.01,
significance versus control.
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1130 Z.-Z. Zhu et al. / Journal of Ethnopharmacology 133 (2011) 1126–1131
dependent manner from 9 a.m to 17 p.m. These results exhibited
that oral administration of PEF inhibited pyrexia induced by LPS.
3.7. Acute toxicity
Although the mice were given 4.2 g/kg of PEF, no mortality was
observed during the assessment period (7 days). So we can draw
a conclusion that the minimum lethal dose of PEF is more than
4.2 g/kg, which is equivalent to approximately 500 times of clinical
dose.
4. Discussion
The present study investigated the scientific reasons for
the folkloric use of Desmodium podocarpum in the manage-
ment of febrile diseases and painful conditions. GC–MS analysis
revealed the presence of five major families of compounds in this
plant, viz. 2,4-bis(1,1-dimethylethyl)-phenol (phenols), -sitostero
(phytosterols); bis(2-ethylhexyl)-phthalate (arylpropionic acids),
-tocopherol--d-mannoside (saponins), 3,7,11,15-tetramethyl-
2-hexadecen-1-ol (enols) and phytol (enols), which may play a key
role in the anti-inflammatory, analgesic and antipyretic activities of
PEF (Cocco et al., 2003; Kang et al., 2008; Chen et al., 2009; Nsonde
Ntandou et al., 2010).
The carrageenan rat paw edema test is suitable for evaluation of
anti-inflammatory drugs and is used frequently to assess the anti-
edematous effect of natural products (Basu and Nag Chaudhuri,
1991). As we know, prostaglandins play an important role in
pain progress in chemical nociception models (Santos and Vedana,
1998b; Zheng et al., 2009) and are the target of action of commonly
used anti-inflammatory drugs. Several inflammatory mediators,
such as sympathomimetic amines, tumor necrosis factor- (TNF-
), interleukin-1 (IL-1) and interleukin-8 (IL-8), are also involved
in the nociceptive response to chemical stimulus in mice (Santos
and Vedana, 1998b; Ribeiro et al., 2000). There are two phases of
carrageenan-induced inflammatory reaction: early phase (0–2.5 h
after injection of carrageenan) results from serotonin, brady-kinin
and histamine liberation, while late phase is associated with the
release of prostaglandins (Antonisamy and Ignacimuthu, 2010). As
shown in Fig. 4, the petroleum ether fraction (PEF) significantly
inhibited each phase of edema in rats, suggesting that the extract
had a non-selective inhibitory effect on the release or actions of
these mediators. In order to further evaluate the anti-inflammatory
activity of the extract, the dimethyl benzene-induced ear edema
test was employed. In the process of inflammation, activated neu-
trophils release mediators such as platelet-activating factor and
lysozyme, which can lead to vasodilatation and increase vascu-
lar permeability (Saeed et al., 2010). In the present study, it was
also shown that PEF significantly inhibited ear edema of mice.
These findings indicated that the extract possesses a significant
anti-inflammatory activity.
Lipopolysaccharide (LPS) can stimulate myeloid cells, which
further synthesize many cytokines such as interleukin-1 (IL-1),
interleukin-6 (IL-6) and TNF-, inducing a general homeostatic
reaction, serving as the organism’s first line of defense against
infection and causing fever finally (Hart, 1988). In the present
study, the rat hyperthermia induced by LPS was employed to inves-
tigate the antipyretic activity of PEF. The results exhibited that
PEF attenuated pyrexia, supporting the view that PEF has some
influence on prostaglandin-biosynthesis, because the synthesis of
prostaglandins plays a crucial role in the febrile response to endoge-
nous pyrogens (such as the cytokines) or to exogenous pyrogens
(such as LPS).
The acetic acid writhing test is known as a non-selective anti-
nociceptive model. When animals are intraperitoneally injected
with acetic acid, a painful reaction and acute inflammation emerge
in the peritoneal area. The stimulation of peritoneal nociceptors
is indirect and occurs with the release of endogenous substances,
which stimulate nervous endings (Gyires and Torna, 1984). After
acetic acid injection, a great increase occurs in prostaglandins E
2
and F
2
levels in peritoneal fluid (Daud and Habib, 2006) and the
analgesic effect of PEF may be due to inhibition of the local level of
prostaglandins. However, the result of this writhing test alone does
not substantiate whether the anti-nociceptive effect is associated
with central analgesia substances.
The hot plate test is a classical approach widely applied in the
analgesic investigations for several decades. When male mature
animals touch the heated plate, they will lick their scrotums against
thermal injury. In this case, we often record a false reaction time
of licking the hind paws. Therefore, only female animals are used
in the hot plate test. The hot plate test, when associated with
the writhing test, can usually distinguish central from periph-
eral effects (Srinivasan et al., 2003). Some analgesic drugs such as
aspirin usually have few effects in the hot plated test, indicating
their peripheral analgesic activities. But some other analgesic drugs
such as ibuprofen and morphine can decrease prostaglandin syn-
thesis via central inhibition of cyclooxygenase (Biorkman, 1995;
Dolezal and Krsiak, 2002) or bind to specific opioid receptors in the
central nervous system, exhibiting their both peripheral and cen-
tral analgesic activities. Our results showed that PEF significantly
prolonged latency period of mice in the hot plate test, suggesting
that this antinociceptive effect is carried out mainly via the partici-
pation of central nerve. In addition, we also evaluated the acute oral
toxicity of PEF, which did not cause any death of mice at the dose
of 4.2 g/kg, which is equal to approximately 500 times of clinical
dose, showing a favorable safety.
In conclusion, our findings demonstrate that the petroleum
ether fraction (PEF) from the ethanol extract of Desmodium
podocarpum has the favorable antinociceptive, anti-inflammatory
and antipyretic activities, which are involved in possible inhibition
of the central synthesis of prostaglandins, and affirm the claim by
traditional medicine practitioners that Desmodium podocarpum can
be used to treat febrile diseases, cough and bleeding wounds. How-
ever, further studies are necessary to fully elucidate the mechanism
of action of the plant.
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    • "Carrageenan induced edema formation consist of two phases, that is, an early or first phase (0–2.5 h after carrageenan injection) and a late or second phase (6–12 h postinjection). The early phase results from the release of inflammatory mediators such as serotonin, histamine, and bradykinins, whereas the late phase is associated with the release of PGs. [30] The n‑hexane extract at the test dose of 100 mg/kg body weight reduced the edema by 80% after 3 h which suggest the inhibitory activity on the release of protaglandins. Chronic inflammation is produced when the body fails to respond against anti‑inflammatory agents that further leads to fibroblast proliferation and formation of granulomatous tissues. "
    [Show abstract] [Hide abstract] ABSTRACT: Background: Bergia suffruticosa (Delile) Fenzl (Syn. Bergia odorata Edgew) (Elatinaceae family) is used traditionally to repair bones and is applied as a poultice on sores. It is also used for stomach troubles and as an antidote to scorpion stings. So far, very little scientific work has been reported to validate its ethnomedical uses in the alleviation of pain, bone repair, etc. Objective: This study was designed to explore the anti-inflammatory and anti-implantation potential of n-hexane extract of B. suffruticosa whole plant in mice along with identification of its chemical constituents. Materials and methods: n-Hexane extract of B. suffruticosa whole plant was screened for acute and chronic anti-inflammatory activity followed by an anti-estrogenic activity. Eventually, n-hexane extract was tested for anti-implantation activity by exploiting markers of uterine receptivity, lipid peroxidation, and superoxide enzyme activity. The extract was administered orally at a dose of 100 mg/kg body weight in each study. Results: Thin layer chromatography fingerprint profile of n-hexane extract revealed the presence of lupeol and β-sitosterol. The n-hexane extract reduced the edema by 80% in acute inflammation, whereas it reduced edema to 75% on the 5(th) day in chronic inflammation. The n-hexane extract reduced elevated malonaldehyde level from 6 to 2.5 nmol/g × 10(-5) and increased superoxide dismutase enzyme activity from 0 to 350 units/g in treated animals on the 5(th) day of pregnancy. Moreover, extract decreased uterine weight from 0.33 to 0.2 g in estradiol treated animals. Conclusion: These results indicate that n-hexane extract of B. suffruticosa is having potent anti-inflammatory, anti-estrogenic, and anti-implantation activity. This is the first report of all the pharmacological activities of B. suffruticosa mentioned above. Summary: TLC fingerprint profile of n-hexane extract of Bergia suffruticosa whole plant revealed the presence of lupeol and β-sitosteroln-Hexane extract showed in vivo anti-inflammatory activity in both acute and chronic model of inflammation in ratsn-Hexane extract possess significant anti-estrogenic activityn-Hexane extract altered the levels superoxide anion radical and superoxide dismutase enzyme activity during the blastocyst implantationAnti-implantation activity of n-hexane extract is attributed to its anti-inflammatory and anti-estrogenic potential. Abbreviations used: TLC: Thin layer chromatography; LPO: Lipid peroxidation; SOD: Superoxide dismutase; B. suffruticosa: Bergia suffruticosa; TNF-α: Tumor necrosis factor-α; NO: Nitric oxide; IL-1: Interleukin-1; LIF: Leukemia inhibitory factor; CSF-1: Colony-stimulating factor; COX: Cyclooxygenase; SDS: Sodium dodecyl sulfate; IAEC: Animal House Ethics Committee; CPCSEA: Committee for the Purpose of Control and Supervision of Experiments on Animals; HBSS: Hank's balanced salt solution; MDA: Malonaldehyde; and TBA: Thiobarbituric acid.
    Full-text · Article · Oct 2015
    • "Av-EtOH (25, 50 and 100 mg/kg, p.o) administered 1 h before carrageenan injection, inhibited significantly (P < 0.01) the increase in the edema volume at 1 and 2 h, initial phase. This phase has been induced due to the action of mediators such as histamine, serotonin and bradykinin on vascular permeability [40], which is subsequently sustained by the release of prostaglandins and nitric oxide (second-phase) with peak at 3 h. The histamine induced paw edema model was used to confirm the involvement of histamine in the anti-inflammatory effect of Av-EtOH, since the extract showed anti-inflammatory effect in the early hours of the carrageenan induced paw edema induced test. "
    [Show abstract] [Hide abstract] ABSTRACT: Annona vepretorum Mart. (Annonaceae) is a native tree from Caatinga (Brazilian Northeastern savanna biome), popularly known as "araticum" and "pinha da Caatinga". In this study, we investigated the effects of the crude ethanolic extract (Av-EtOH) in models of pain and inflammation in rodents. The evaluation of antinociceptive activity was carried out by the acetic acid-induced writhing, formalin, hot plate and tail flick tests, while paw edema induced by carrageenan or histamine, and leukocyte migration to the peritoneal cavity were used for anti-inflammatory profile. Histological analyses also were carried out. Av-EtOH (25, 50 and 100 mg/kg, p.o) significantly reduced the number of writhing (P < 0.01) and decreased (P < 0.01) the paw licking time in both phases of the formalin test. In the hot plate and tail flick tests, this extract increased the reaction time, consequently reduced painful behavior. The effects in the formalin and hot plate tests were antagonized by naloxone. Av-EtOH inhibited significantly (P < 0.01) the increase in the edema volume after administration of carrageenan and histamine. In the peritonitis test, acute pre-treatment with Av-EtOH inhibited leukocyte migration. Histological analysis showed less inflammation in the groups treated with the extract when the inflammation was induced by carrageenan or histamine. Thus, Av-EtOH has significant antinociceptive and anti-inflammatory properties, which are related probably with the activation of opioid receptors and inhibition of release of mediators of the inflammatory process. This specie is a potential target for drug discovery.
    Full-text · Article · Jun 2015
    • "p.o. were selected for the present study [12]. The Eddy's hot plate test is useful for the evaluation of centrally acting analgesics which elevate the pain threshold of animals towards heat [19]. It is thought to be responsive to opioids and measures the complex response to a non-inflammatory, acute nociceptive stim- ulus [20]. "
    [Show abstract] [Hide abstract] ABSTRACT: Albizia lebbeck Benth. is extensively used in Indian traditional medicine for treating several painful and inflammatory disorders. The possible central analgesic activity and the underlying mechanism of action of the aqueous (AE) and ethanolic extracts (EE) of the leaves of A. lebbeck were investigated in Wistar rats using Eddy's hot plate and the tail flick tests. In order to investigate the underlying mechanism of action, rats were pretreated with naloxone, bicuculline or methysergide and then were administered a per os (p.o.) dose of AE or EE. AE and EE caused a significant (p<0.05) elevation in the mean basal reaction time in the hot plate method and an increase in the latency time in the tail flick method. In rats pretreated with bicuculline and methysergide, a significant (p<0.05) reduction in the analgesic activity was observed in comparison to AE and EE. Thus, AE and EE exhibited significant central analgesic activity and act possibly via the GABAergic and serotonergic pathways. The flavonoids and saponins found in the leaves could be responsible for the observed effect.
    Full-text · Article · Apr 2015
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