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Study of Sedative, Anxiolytic, CNS – Depressant and Skeletal Muscle Relaxant Effects of Methanolic Extract of Hibiscus Rosa-Sinensis on Laboratory Animals

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Aim: Methanolic extract of Hibiscus rosasinensis (MEHR) shows sedative, anxiolytic, skeletal muscle relaxant and CNS - depressant effect. Methods: Hibiscus rosasinensis, found in south Asia, was extracted by methanol and the practical yield of extract was found to be 7.2%w/w. Models: 1. Anxiolytic action was studied by the open field behavior model in which it significantly increase in rearing and crossing, elevated plus-maze model in which MEHR significantly increase the entry in both arm, dark & light field model in which MEHR significantly increase the time spent in dark field, compared with control-CMC solution [using diazepam (25 mg/kg, i.p.)]. 2. Sedative effect was seen by Phenobarbital induce sleep model. 3. Skeletal muscle relaxant effect was studied using rota rod model, in which MEHR significantly increase the time of fall, compared with control-CMC solution [using diazepam (25 mg/kg, i.p.)]. 4. CNS - depressant effect was studied using Actophotometer model in which MEHR significantly decrease the number of cut-off, compared with control-CMC solution [using diazepam (25 mg/kg, i.p.)]. Conclusion: The MEHR shows seadative, anxiolytic, skeletal muscle relaxant and CNS - depressant effects.
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Study of Sedative, Anxiolytic, CNS – Depressant and Skeletal Muscle
Relaxant Effects of Methanolic Extract of Hibiscus Rosa-Sinensis on
Laboratory Animals
Ganatra TH*, Joshi UH, Patel MN, , Desai TR Tirgar PR
Department of Pharmacology, R. K. College of Pharmacy, Kasturbadham, Bhavanagar Road, Rajkot, India - 360020
Abstract:
Aim: Methanolic extract of Hibiscus rosasinensis (MEHR) shows sedative, anxiolytic, skeletal muscle relaxant and
CNS – depressant effect.
Methods: Hibiscus rosasinensis, found in south Asia, was extracted by methanol and the practical yield of extract was
found to be 7.2%w/w.
Models:
1. Anxiolytic action was studied by the open field behavior model in which it significantly increase in rearing and
crossing, elevated plus-maze model in which MEHR significantly increase the entry in both arm, dark & light field
model in which MEHR significantly increase the time spent in dark field, compared with control-CMC solution
[using diazepam (25 mg/kg, i.p.)].
2. Sedative effect was seen by Phenobarbital induce sleep model.
3. Skeletal muscle relaxant effect was studied using rota rod model, in which MEHR significantly increase the time of
fall, compared with control-CMC solution [using diazepam (25 mg/kg, i.p.)].
4. CNS - depressant effect was studied using Actophotometer model in which MEHR significantly decrease the
number of cut-off, compared with control-CMC solution [using diazepam (25 mg/kg, i.p.)].
Conclusion: The MEHR shows seadative, anxiolytic, skeletal muscle relaxant and CNS – depressant effects.
Keywords: Hibiscus, sedative, anxiolytic, skeletal muscle relaxant, rota-rod and CNS – depressant effects,
actophotometer, etc.
INTRODUCTION:
[1,2,5]
Biological Name: The dried ripe flowers,
leaves of Hibiscus rosa-sinenis belongs to
family Malvaceae.
[1]
Source: Widely spread all over the world,
majorly in tropical and subtropical areas.
[2]
Description: The leaves are alternate, simple
and ovate to lanceolate, often with a toothed or
lobed margin. The flowers are large,
conspicuous, trumpet-shaped, with five or
more petals, ranging from white to pink, red,
orange, purple or yellow, and from 4–18 cm
broad.
[2, 6]
Synonyms: Aloala [Hawai]; red hibiscus;
China rose [English]; da hong hua (big red
flower) [China]; Jasud [Gujarati], japapushpam
[India]; shoeflower [Jamaica].
[5]
Nomenclature: Hibiscus is taken from the
Greek "hibiscos," a name for mallow.
[6]
Pharmacological Actions: Abortifacient
[5]
;
analgesic
[5]
; antidiarrhoic
[5]
; antiestrogenic
[1]
;
antifungal
[5]
; anti-infectious; anti-inflammatory;
antipyretic; astringent
[5]
; CNS depressant
[1]
;
constipating
[1]
; contraceptive; demulcent
[5]
;
dentifrice
[6]
; diuretic
[6]
; expectorant
[5]
;
hemostat; hypoglycemic
[5]
; hypotensive;
hypothermic; insect attractant
[1]
; promotes hair
growth and color
[1,2,,5,6]
; purgative
[1]
;
refrigerant
[5]
; relaxes spasm
[1]
; soothes irritated
tissue.
[5]
Collection of materials and Method for
extraction:
The herb of Hibiscus was collected from local
region in Rajkot district of Gujarat &
morphological & microscopy of pant was
authentified by pharmarcognosy department of
R.K. College of pharmacy. The leaves were
separated and dried between 55 º to 60º C and
then pulvirized to very fine powder. The
powder was extracted using Soxhlet apparatus
Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155
1146
using methanol as a solvent. The % yield was
found to be 7.2%W/W.
Animals:
Male Swiss albino rat of weighing 220-
280 g were used for the study.
The animals were procured from Animal House
, Department of Pharmacology, R.K.College of
Pharmacy, Rajkot, India. The animals were
place at random and allocated to treatment
groups in polypropylene cages with paddy husk
as bedding. Animals were housed at a
temperature of 24±20˚C and relative humidity
of 30 – 70 %. A light and dark cycle was
followed. All animals were fed on standard
balance diet and provided with water ad
libitum.
Experiments were carried out between 09:00 an
d 14:00 h.
All the experimental procedures and protocols
used in the study were reviewed and
approved by the Institutional AnimalEthical
Committee(IAEC) and care of laboratory
animals was taken as per the guidelines of
Committee for the purpose of control and
supervision of experiments on
animals(CPCSEA), Govt. of India (Registration
No.1131/ac/07/CPCSEA.)
EXPERIMENTAL MODELS AND
STUDIES (METHODS):
The study includes the sedative, anxiolytic,
skeletal muscle relaxant effect and CNS-
depressant effect of Methanolic extract of
Hibiscus rosa-sinensis [MEHR].
A] For Sedative effect:
1. Phenobarbital induced sleep model:
The 18 animals (mice) divided in to 3 groups
containing 6 animals each.
[Normal: 0.5ml 1% CMC solution, i.p.;
standard: Phenobarbital: 5 mg/kg, i.p.; test:
MEHR: 200 mg/kg, p.o.]. Observe the onset of
time and duration of action.
[3,4,9,11]
. From the
given data in table: 1 we can say that drug
possesses sedative effect.[Chart 1]
B] For Anxiolytic effect:
1. Open-field behavior model:
Instrument: The apparatus consisted of a
wooden box (60 Χ 60 Χ 60 cm). The arena of
the open field was divided into 16 squares (15
Χ 15 cm): the four inner squares in the center
and 12 squares in the periphery along the walls.
The experimental room was a sound attenuated,
dark room.
Method: The 18 animals (mice) divided in to 3
groups containing 6 animals each. [Normal:
0.5ml 1% CMC solution, i.p.; standard:
diazepam: 25 mg/kg, i.p.; test: MEHR: 200
mg/kg, p.o.]. Allow the animal to freely move
in the model and note the number of crossing
and number of rearing. From the given data
table 2 the number of crossing increases in test
compare to normal.
[3,4]
[Chart 2]
2. Elevated Plus model:
Instrument: The EPMT apparatus consisted of
four arms elevated 30 cm above the floor, with
each arm positioned at 90° relative to the
adjacent arms. Two of the arms were enclosed
with high walls (30 Χ 7 Χ 20 cm), and the other
arms were connected via a central area (7 Χ 7
cm) to form a plus sign.
Method: The 18 animals (mice) divided in to 3
groups containing 6 animals each. [Normal:
0.5ml 1% CMC solution, i.p.; standard:
diazepam: 25 mg/kg, i.p.; test: MEHR: 200
mg/kg, p.o.]. Allow the animal to freely move
in the model and note the number of entry in
open arm and close arm. From the given data
table 3 the number entry in open arm increases
in test compare to normal.
[3,4]
[Chart 3]
3. Dark and light field model:
Instrument: It consists of open top wooden box.
Two distinct chambers, a black chamber (25 cm
long Χ 35 cm wide Χ 35 cm deep), painted
black and made dark by covering its top with
black plywood, and a bright chamber (25 cm
long Χ 35 cm wide Χ 35 cm deep), painted
white and brightly illuminated with 40-W white
light source, were placed 25 cm above the open
box. The two chambers were connected through
a small open doorway, (7.5 cm long Χ 5 cm
wide) situated on the floor level at the center of
the partition.
Method: The 18 animals (mice) divided in to 3
groups containing 6 animals each. [Normal:
0.5ml 1% CMC solution, i.p.; standard:
diazepam: 25 mg/kg, i.p.; test: MEHR: 200
mg/kg, p.o.]. Allow the animal to freely move
Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155
1147
in the model and note the number of entry in
light field as well as count the time spent in
light field. From the given data table 4a & 4b
the number entry as well as time spent in light
field increases in test compare to normal.
[7]
[Chart 4 a & b]
C] For CNS-depressant effect:
1. Actophotometer:
The 18 animals (mice) divided in to 3 groups
containing 6 animals each. [Normal: 0.5ml 1%
CMC solution, i.p.; standard: diazepam: 25
mg/kg, i.p.; test: MEHR: 250 mg/kg, p.o.].
Allow the animal to freely move in the model
and note the number of cut off (crossing) of
lesser for 2 minutes. From the given data in
table 5 the number of cut off decreases in test
compare to normal.
[3,4,10]
[Chart 5]
D] For Skeletal muscle relaxant effect:
1. Rota rod model:
Instrument: Rota rod apparatus consisted of a
base platform and an iron rod of 3 cm diameter
and 30 cm length, with a non-slippery surface.
This rod was divided into two equal sections by
two disks, thus enabling two mice to walk on
the rod at the same time at the speed of 25 rpm.
Method: The 18 animals (mice) divided in to 3
groups containing 6 animals each. [Normal:
0.5ml 1% CMC solution, i.p.; standard:
diazepam: 25 mg/kg, i.p.; test: MEHR: 200
mg/kg, p.o.].
The animal is put on the rotating rod and the
time required to fall down from the rod is
measured. From the given data, in table 6 the
time required to fall down is lesser in test
compared to normal.
[3,4,11]
[Chart 6]
Statistical Analysis: Results were expressed as
mean ± SEM. Difference in means were
compared using one way analysis of variance
(ANOVA) followed by Tukey’s test. P<0.001
were considered statistically significant.
Result:
Activity and
Model
Parameters
Control Standard Test
Before
Reading
±SEM
After
Reading
±SEM
Before
Reading
±SEM
After
Reading
±SEM
Before
Reading
±SEM
After
Reading
±SEM
Sedative
(Phenobarbital
induce sleep)
Onset of action
(Minutes)
--- --- --- 26.5±0.84 --- 33.16±1.25
Duration of action
(Minutes)
--- --- --- 187.66±4.75 --- 159±3.41
Anxiolytic
(open field model)
Number of crossing
18.75±1.1 21.5±1.5 19±1.04 48.5±1.73 16±1.42 35.83±0.97
Anxiolytic
(Elevated plus
model)
Entries in open arm
8.16±0.49 8.5±0.27 7.5±0.52 18.33±2.12 8±0.44 14±0.89
Anxiolytic
(Light/Dark
model)
Number of Entry in
light area
10.5±0.64 11±0.70 9±0.40 20.5±0.6 10.66±0.4 18±0.40
Time spent in light
area (seconds)
25±0.70 24±0.70 24±0.70 112±0.9 22±0.70 72.5±0.93
CNS-depressant
(Actophotometer)
Number of cut-off
52.5±0.76 53±0.63 51.5±0.8 9.5±0.62 51±0.96 20±0.36
SKM-relaxant
(Rota-rod model)
Time of fall
(Seconds)
--- 246.6±3.3 --- 5.83±0.60 --- 17.5±0.80
Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155
1148
Images of Models used in work:
Table 1: Sedative effect of MEHR on rat using Phenobarbital induced sleep model
For Sedative: phenobarbiatal induced sleep model
Sr. No. Group
Control (Seconds) Standard (Seconds) Test (Seconds)
Onset of
time
Duration
of action
Onset of
time
Duration of
action
Onset of
time
Duration of
action
1 Head --- --- 26 190 30 155
2 Tail --- --- 27 180 34 154
3 Back --- --- 24 189 29 148
4 Head back --- --- 30 200 35 167
5 Back tail --- --- 27 169 34 160
6 No mark --- --- 25 198 37 170
Average --- --- 26.5 187.66 33.16 159
SD --- --- 2.073 11.60 3.06 8.34
SEM --- --- 0.84 4.75 1.25 3.41
variance --- --- 6.25 66.91 8.66 63.33
ACTOPHOTOMETER
ROTAROD
OPEN FIELD MODE
L
ELEVATED PLUS MODE
L
LIGHT DARK MODE
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1149
Table 2: Anxiolytic effect of MEHR on rat using Open field model
For Anxiolytic action: Open field model (number of crossing in 5 minutes)
Sr. No. Group
Control Standard Test
Before After Before After Before After
1 Head 15 17 22 51 20 39
2 Tail 18 21 20 54 18 36
3 Back 22 26 16 46 12 33
4 Head back 18 20 18 45 16 36
5 Back tail 19 23 20 49 15 36
6 No mark 20 22 18 46 14 35
Average 18.667 21.5 19 48.5 15.833 35.833
SD 2.3381 3.0166 2.0976 3.5071 2.8577 1.9408
SEM 1.169 1.5083 1.0488 1.7536 1.4289 0.9704
variance 5.46 9.1 4.4 12.3 8.16 3.76
Table 3: Anxiolytic effect of MEHR on rat using Elevated plus model
For Anxiolytic action: Elevated Plus method (number of entry in open arm 5 minutes)
Sr. No.
Group
Control Standard Test
Before After Before After Before After
1 Head 9 8 7 15 7 14
2 Tail 8 9 6 14 8 13
3 Back 9 9 9 19 9 15
4 head back 7 8 8 19 9 15
5 back tail 9 9 7 17 8 14
6 No mark 7 8 8 26 7 13
Average 8.16 8.5 7.5 18.33 8 14
SD 0.98 0.54 1.04 4.274 0.89 0.89
SEM 0.49 0.27 0.52 2.137 0.44 0.44
variance 0.96 0.3 1.1 18.26 0.8 0.8
Table 4 a: Anxiolytic effect of MEHR on rat using Light Dark model
For Anxiolytic action: Light Dark model (number of entry in light field 5 minutes)
Sr. No. Group
Control Standard Test
Before After Before After Before After
1 Head 11 10 10 22 10 18
2 Tail 12 13 9 20 12 18
3 Back 10 11 9 21 11 19
4 No mark 9 10 8 19 10 17
5 back tail 11 12 8 21 10 16
6 No mark 10 10 10 20 11 20
Average 10.5 11 9 20.5 10.66 18
SD 1.048 1.26 0.89 1.04 0.81 1.41
SEM 0.52 0.63 0.44 0.52 0.40 0.70
variance 1.66 2 0.66 1.66 0.91 0.66
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Table 4 b: Anxiolytic effect of MEHR on rat using Light Dark model
For Anxiolytic action: Light Dark model (Time spent in light field 5 minutes)
Sr. No. Group
Control Standard Test
Before After Before After Before After
1 Head 25 23 24 115 21 73
2 Tail 26 22 23 113 22 75
3 Back 24 25 22 112 23 74
4 No mark 23 24 25 110 22 71
5 back tail 27 26 26 110 20 72
6 No mark 25 24 24 112 24 70
Average 25 24 24 112 22 72.5
SD 1.41 1.41 1.41 1.89 1.41 1.87
SEM 0.70 0.70 0.70 0.94 0.70 0.93
variance 1.66 1.66 1.66 4.33 0.66 2.91
Table 5: CNS -depressant effect of MEHR on rat using Actophotometer model
For CNS-Depressant: Actophometer model (number of cut-off in 2 minutes)
Sr. No. Group
Control Standard Test
Before After Before After Before After
1 Head 50 51 49 9 51 19
2 Tail 52 52 52 10 55 20
3 Back 55 54 51 8 50 21
4 head back 51 52 50 8 50 19
5 back tail 53 54 52 10 52 21
6 No mark 54 55 55 12 48 20
Average 52.5 53 51.5 9.5 51 20
SD 1.87 1.54 2.07 1.51 2.36 0.89
SEM 0.76 0.63 0.84 0.62 0.96 0.36
variance 3.5 2.4 4.3 2.3 5.6 0.8
Table 6: Skeletal Muscle Relaxant effect of MEHR on rat using Rota-rod model
For Skelatal muscle relaxant: Rota rod model (time required to fall down)
Sr. No. Group Control (seconds) Standard (seconds) Test (seconds)
1 Head 240 5 17
2 Tail 250 6 15
3 Back 260 8 21
4 head tail 250 5 17
5 back tail 240 7 18
6 No mark 240 4 17
Average 246.66 5.83 17.5
SD 8.16 1.47 1.97
SEM 3.34 0.60 0.80
variance 66.66 2.16 3.9
Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155
1151
Chart 1: Sedative effect of MEHR on rat using Phenobarbital induced sleep model
* indicate significant difference from control (p<0.001)
Chart 2: Anxiolytic effect of MEHR on rat using Open field model
* indicate significant difference from control (p<0.001)
Chart 3: Anxiolytic effect of MEHR on rat using Elevated plus model
* indicate significant difference from control (p<0.001)
Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155
1152
Chart 4 a: Anxiolytic effect of MEHR on rat using Light Dark Field model
* indicate significant difference from control (p<0.001)
Chart 4 b: Anxiolytic effect of MEHR on rat using Light Dark Field model
*
indicate significant difference from control (p<0.001)
Chart 5: CNS -depressant effect of MEHR on rat using Actophotometer model
* indicate significant difference from control (p<0.001)
Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155
1153
Chart 6: Skeletal Muscle Relaxant effect of MEHR on rat using Rota-rod model
* indicate significant difference from control (p<0.001)
DISCUSSION:
The result of our study shows methanolic
extract of flower of Hibiscus rosa-sinensis can
markedly reduce fall of time (in Rota-rod
model), decrease in onset of time as well as
increase in duration of action (in phenobarbital
induced sleep model), decrease number of cut-
off (in Actophotometer) and increase in number
of crossing (in open-field behavior model),
increase time spent in light field as well as
increase number of entry in close and open arm
(in elevated plus model).
In conclusion, our data indicates that MEHR
can possess Sedative, anxiolytic, CNS -
depressant and skeletal muscle relaxant
activities.
The MEHR contains flavanoids (hibiscitin),
phenolic content as well as terpenoid
compounds like β – sitosterol, caemphesterol,
etc, which are probably responsible for the
actions.
[5]
CONCLUSION:
The methanolic extract of Hibiscus rosa-
sinensis can increase the duration of action so it
possesses sedative effect.It can also increase the
number of crossing in open field model,
increase the time spent in open arm, entry in
open arm (in elevated plus model) as well as
increase the time spent in light field (in Light
Dark field) thus we can conclude that it can also
possesses anxiolytic action.
The decrease in number of cut-off in
actophotometer model indicates that it can
possess CNS-depressant.It can also decrease the
time of fall from the rotating rod in rota-rod
model, thus it can possesses skeletal muscle
relaxant action.
ACKNOWLEDGEMENT
On the occasion of presenting this paper in
internet journal, I take this as a unique
opportunity to record my deep sense of
gratitude to my esteemed research guide Tirgar
PR, Professor and Head, Department of
Pharmacology, R. K. College of Pharmacy,
Rajkot and also to Dr. Desai TR, Principal, R.
K. College of Pharmacy, Rajkot.
I am also thankful to Pandiya DJ and Sheth DB
for his kind support for authentication and
identification of this plant.
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... After 2 more minutes of maze exploration, the mouse was put back in its home cage. 24 hours after the first day of trial (the eighth day of medication treatment), participants were tested on their ability to recall the steps of this newly learnt activity[20]. level in the middle of the divider united the two rooms.The procedure involves letting the animal roam freely within the model while keeping track of how many times it enters and exits the light field and how long it stays there ...
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Hibiscus Rosa Sinensis Linn. (Malvaceae) is a popular medicinal plant found in tropical and sub-tropical region of world. All plant parts of Hibiscus Rosa Sinensis Linn are most widely used to treat several ailments like anti-Tumor, anti-fertility, anti-ovultory, anti-implantation, anti-Inflammatory, analgesic, anti-estrogenic, anti-pyretic, anti-spasmodic, anti-viral, anti-fungal, anti-bacterial, hypoglycemic, spasmolytic, CNS depressant, hypertensive and juvenoid Activity. Due to its multidimensional pharmacological approach it is certain to emerge as a effficient player in the flourising field of herbal supplements, medicines and health care system. This review aims to present recent details on botany, ethnomedicinal uses, photochemistry, pharmacological effects, toxic effects, with the purpose to find research gaps demanding for upcoming research and investigation of Hibiscus Rosa Sinensis Linn. Principal constituents reported in Hibiscus Rosa Sinensis Linn are flavones, containing quercetin-3-sophorotrioside, kaempferol-3xylosylglucoside,quercetin-3-diglucoside, quercetin-3,7-diglucoside, cyaniding-3,5-diglucoside, cyaniding-3-sophoroside-5-glucoside and other constituent are cyanidin chloride, cyclopeptide alkaloid, ascorbic acid, riboflavin, thiamine, hentriacontane, taraxeryl acetate, ß-sitosterol, malvalic acids and cyclic acids sterculic. Complete literature was probed via websites,online databases, thesis and texts. The available reports was portray physicochemical parameters, nutritional aspects and phytochemical analysis of bioactive plant parts. Friendly holistic conservation approaches offered by plant biotechnology applications are also discussed.
... The use of Hibiscus rosa-sinensis in parturition could be explained by its smooth muscle spasmogenic and spasmolytic activities found in extracts of the flowers (Agarwal and Shinde, 1967;Ganatra et al., 2011) and aerial parts (Gilani et al., 2005). The in-vivo analgesic effect demonstrated in extracts of the flowers (Sawarkar et al., 2009), roots (Soni and Gupta, 2011) and leaves (Tomar et al., 2010) of Hibiscus rosa-sinensis could explain its traditional use in treating dysmenorrhea and migraine. ...
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This is an extensive review of plants used traditionally for women's healthcare in Southeast Asia and surrounding countries. Medicinal plants have a significant role in women's healthcare in many rural areas of the world. Plants with numerous efficacious observations have historically been used as a starting point in the development of new drugs, and a large percentage of modern pharmaceuticals have been derived from medicinal plants. A review was conducted of all plant use mentioned specifically for female healthcare, such as medicine to increase fertility, induce menstruation or abortion, ease pregnancy and parturition, reduce menstrual bleeding and postpartum hemorrhage, alleviate menstrual, parturition and postpartum pain, increase or inhibit lactation, and treat mastitis and uterine prolapse, in 200 studies focusing on medicinal plant use, either general studies or studies focusing specifically on women's healthcare. Nearly 2000 different plant species are reported to be used in over 5000 combinations. Most common are Achyranthes aspera, Artemisia vulgaris, Blumea balsamifera, Carica papaya, Curcuma longa, Hibiscus rosa-sinensis, Leonurus japonicus, Psidium guajava and Ricinus communis, and each of these species had been reported in more than 10 different scientific articles. This review provides a basis for traditional plant use in women's healthcare, and these species can be used as the starting point in the discovery of new drugs.
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Ayurveda suggests that decoction of leaves of Hibiscus rosa-sinensis could be beneficial to reduce cough. Codeine and other synthetic antitussive agents shows number of side-effects and thus to find better and safer alternate Hibiscus rosa-sinensis was evaluated for its antitussive activity.Dried powder of flower part of Hibiscus rosa-sinensis was extracted with methanol and the practical yield of methanolicextract was found to be 1% W/W.Anti-tussive effect of methanolic extract of Hibiscus rosa-sinensis was studied in Histamine chamber using citric acid (7.5%W/V) induced cough model, in which the methanolic extract of Hibiscus rosa-sinensis significantly decreased the number of coughing. From this we concluded that methanolic extract of Hibiscus rosa-sinensis possess antitussive activity.
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Ayurveda suggests that decoction of leaves of Hibiscus rosa-sinensis could be beneficial to reduce cough. Codeine and other synthetic antitussive agents shows number of side-effects and thus to find better and safer alternate Hibiscus rosa-sinensis was evaluated for its antitussive activity.Dried powder of flower part of Hibiscus rosa-sinensis was extracted with methanol and the practical yield of methanolicextract was found to be 1% W/W.Anti-tussive effect of methanolic extract of Hibiscus rosa-sinensis was studied in Histamine chamber using citric acid (7.5%W/V) induced cough model, in which the methanolic extract of Hibiscus rosa-sinensis significantly decreased the number of coughing. From this we concluded that methanolic extract of Hibiscus rosa-sinensis possess antitussive activity. INTRODUCTION Cough is a reflex of pulmonary irritant receptor, found in the epithelium of the respiratory tract, which are sensitive to both chemical and mechanical stimuli 1 . Cough is a useful physiological mechanism that serves to clear the respiratory passages of foreign material and excess secretions and should not be suppressed indiscriminately 1,2 . Anti-tussive drugs are the most relieving class for cough suppressants. They are the drugs that act in the CNS to raise the threshold of cough centre or act peripherally in respiratory tract to reduce the tussal impulses or both these actions 3 . This class has aim to control the cough rather than to eliminate. Anti-tussive should be used only in dry unproductive cough 3 . Opioids, nonopioids, antihistaminic and bronchodilators are different class of anti-tussives 1,3,4,5 . Codeine is the widely used anti-tussive agent from opioid class. It is more selective for cough centres and treated as standard anti-tussive. Codeine exerts effects through opioid receptors present in neurons in the CNS and peripheral tissues. Opioid receptors are of three types identified as μ, κ and δ 3 . These receptors are distributed throughout the brain, spinal cord and peripheral tissues. Mu receptors are primarily found in brainstem and medial thalamus. Kappa receptors are primarily found in limbic system, brainstem and spinalcords. Delta receptors are generally found in limbic and spinal cord area 3, 6 . Even though the codeine is having narcotic effect so it is having abuses and drug dependence 2, 3 . Constipation is also seen as a chief drawback of codeine 1,2,3 . At higher doses the drowsiness and respiratory depression can occur 1,2,3 . It is contraindicated in asthma and in patients who have diminished respiratory reserve 2,3 . Looking at the dire need to find better and safer herbal alternate of codeine and other synthetic antitussive agents, this experiment was done to prove anti-tussive effect of the Hibiscus rosa-sinensis. These are the dried petals of Hibiscus rosa-sinensis belongs to family Malvaceae. Commonly it is known as Shoeflower [Jamaica] or Jasud [Gujarati] 7 . The leaves were alternate, simple and ovate to lanceolate, often with a toothed or lobed margin. The flowers are large, conspicuous, trumpet-shaped, with five or more petals, ranging from white to pink, red, orange, purple or yellow, and from 4–18cm broad 8,10 . Pharmacological actions of Hibiscus rosa-sinensisincludes Pharmacological Actions: color 6,8,9,10 , bortifacient 9 , analgesic 9 , antidiarrhoic 9 , antiestrogenic 9 , antifungal 9 , anti-infectious 9 ; anti-inflammatory 9 ; Antipyretic 9 ; astringent 9 , CNS depressant 7 , constipating 7 , Contraceptive 9 ; demulcent 9 , dentifrice 10 , diuretic 10 , expectorant 9 , hemostat 9 ; hypoglycemic 9 , hypotensive 7 ; hypothermic 7 ; insect attractant 7 ; promotes hair growth and ; purgative 7 ; refrigerant 9 ; relaxes spasm 7 ; soothes irritated tissue 9 .
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Objective: To study Locomotor activity of aqueous and alcoholic extracts of leaves of Pithecellobium dulce Benth. Materials and methods: CNS depressant activity of leaf extracts of P. dulce was evaluated using actophotometer in albino mice. The potency of alcoholic and aqueous extracts of leaf was compared with that of chlorpromazine at a dose of 100 mg/kg. The acute toxicity was determined using albino mice. Results: Both extracts caused significant CNS depression action in albino mice. The activity of alcoholic extract was more, when compared to chlorpromazine. Conclusion: CNS depression action of extracts may be due to increase in the concentration of GABA in brain.
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The central nervous system (CNS) depressant and anticonvulsant activities of the methanol leaf extract of Ficus hispida Linn (FH) were investigated on various animal models including pentobarbitone sleeping time and hole-board exploratory behaviour for sedation tests, and strychnine, picrotoxin, and pentylenetetrazole-induced convulsions in mice. FH (200 and 400mg/kg, p.o.), like chlorpromazine HCl (1mg/kg, i.m.), produced a dose-dependent prolongation of pentobarbitone sleeping time and suppression of exploratory behaviour. FH (200 and 400mg/kg) produced dose-dependent and significant (P < 0.05) increases in onset to clonic and tonic convulsions, and at 400mg/kg, showed complete protection against seizures induced by strychnine and picrotoxin but not with pentylenetetrazole. Acute oral toxicity test, up to 14 days, did not produce any visible signs of toxicity. These results suggest that potencially antiepileptic compounds are present in leaf extract of FH that deserve the study of their identity and mechanism of action.
Book
Safety aspects have become an outstanding issue in the process of drug discovery and development. Until 15 years ago safety aspects were addressed by pharmacological testing of the selected compound in high doses in tests directed at indications other than the intended indication of the new compound. These tests were followed by pharmacokinetic studies, which were mainly aimed at confirming of a suitable half-life time and at oral activity. Safety aspects relied mostly on toxicity studies, which however gave information on changes of organ structure rather than on organ function. Toxicological and pharmacokinetic studies were adapted to the progress of studies in clinical pharmacology and clinical trails. But the success rate in the pharmaceutical industry and the introduction of new chemical entities to the market per year dropped dramatically, whereas the development time for a new compound increased, sometimes exceeding the patent protection. A change of strategy was therefore adopted, involving the following changes: - Parallel instead of sequential involvement of the various disciplines (multidimensional compound optimization). - The term "Safety Pharmacology" was coined. The International Conference on Harmonization (ICH) founded a Safety Pharmacology Working Group. Easily accessible and the most informative tests now have to be selected. - Exposure of a drug to the body by pharmacokinetic studies on absorption, distribution, metabolism and excretion has to be investigated at an early stage of development and can contribute to the selection of a compound for development. Toxicology experienced major achievements by the introduction of new methods, e.g., in silico methods, toxicogenomics and toxicoproteomics. The book is a landmark in the continuously changing world of drugs. As such it is important reading for many groups: not only for all students of pharmacology and toxicology but also for physicians, especially those involved in clinical trials of drugs, and for pharmacists who have to know the safety requirements of drugs. The book is absolutely essential for scientists and managers in the pharmaceutical industry who are involved in drug finding, drug development and decision making in the development process. In particular, the book will be of use for government institutions and committees working on official guidelines for drug evaluation worldwide.
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Objective: The objective of the study was to investigate the anxiolytic activity of petroleum ether, alcohol and water extracts, obtained from the flowers ofSphaeranthus indicus Linn, in mice. Materials and Methods: Elevated plus maze (EPM), open field test (OFT) and foot-shock induced aggression (FSIA) were the screening tests used to assess the anxiolytic activity of the extracts on mice. Diazepam (1 mg/kg) served as the standard anxiolytic agent. Results: The animals receiving extracts or diazepam (1 mg/kg) showed an increase in the time spent, percent entries and total entries in the open arm of the EPM; increased ambulation, activity at centre and total locomotion in the OFT; and decreased fighting bouts in the FSIA, suggesting anxiolytic activity. Petroleum ether extract (10 mg/kg), alcoholic extract (10 mg/kg) and water extract (30 mg/kg) resulted in prominent activity in the mice. Petroleum ether extract (10 mg/kg) resulted in more prominent anxiolytic activity in the EPM and OFT than ethanolic or water extracts, but was less than that produced by diazepam (1 mg/kg). Conclusion: Petroleum ether extract of S. indicus flowers produces prominent anxiolytic activity in mice.
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Pretreatment of rats and mice with clonidine (0.5-5 mg/kg, intraperitoneally) protected the animals against tonic convulsions induced by picrotoxin, strychnine and maximal electroshock, respectively. The time of onset of convulsions as well as mortality due to picrotoxin and strychnine were delayed in the clonidine pretreated groups as compared to controls. Clonidine (1 mg/kg) blocked the extensor phase of the electroshock convulsion. In reserpinized animals the severity of electroshock-induced seizures was reduced by clonidine pretreatment. Clonidine also caused an increase in the food consumption behaviour in mice subjected to novel situation and food. Its effects were comparable to diazepam, an antianxiety agent. In another experiment, clonidine (0.5-5 mg/kg) counteracted the perphenazine-induced catatonia in rats. It is possible that the observed anticatatonic effect of clonidine may be due to its presynaptic activity, but the actual mechanism of this action is not yet understood.
Practicals in pharmacology; 6th edition, Ahmadabad; BS Shah prakashan; 135-138
  • Goyal
Goyal RK ,Practicals in pharmacology; 6th edition, Ahmadabad; BS Shah prakashan; 135-138; 2007 Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155 1154
Drug discovery and Evaluation: Safety & Pharmacokinetic Assays, 3rd edition
  • Hg Vogel
  • Springer
  • No
Vogel HG, Drug discovery and Evaluation: Safety & Pharmacokinetic Assays, 3rd edition, Germany, Springer, Page No.: 24, 27. Ganatra TH et al /J. Pharm. Sci. & Res. Vol.3(4), 2011,1146-1155 1155
Practicals in pharmacology
  • Rk Goyal
Goyal RK,Practicals in pharmacology; 6 th edition, Ahmadabad; BS Shah prakashan; 135-138; 2007
Indian metrica medica,volume one, Bombay,popular prakashan
  • Ak Nandkarni
Nandkarni AK.; Indian metrica medica,volume one, Bombay,popular prakashan; Vol I: Pg: 634-651; Edition: 3 rd, 2005.
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Crawley, Neurosci Biobehav Rev. 9:37-44, 1985