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DIT Lagenaria
DIT Lagenaria
ABSTRACT
Ancient systems of Indian medicines have been known to cure several kinds of health ailments. The traditional systems of
medicines have explored on different parts of the plants for the treatment and cure of various pathophysiological conditions.
One such important plant is Lagenaria siceraria (bottle gourd), whose leaves, fruits, seeds, and flowers are known for the
treatment for several health ailments. This cucurbitaceous vegetable has shown significant activities against hepatotoxicity,
hyperlipidemia, hypertension, and free radicals among others. The aim of this present review is to succinctly compile the
earlier reports on the phytochemical constituents and pharmacological activities exhibited by the extracts of L. siceraria.
KEY WORDS: Antihyperlipidemic, Antioxidant, Bottle gourd, Hepatoprotective, Lagenaria siceraria, Phytochemical
Department of Pharmaceutical Chemistry and Analysis, School of Pharmaceutical Sciences, Vels Institute of Science,
Technology and Advanced Studies (VISTAS), Chennai, Tamil Nadu, India
*Corresponding author: Dr. Sowmyalakshmi Venkataraman, Department of Pharmaceutical Chemistry and Analysis,
School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram,
Chennai - 600 117, Tamil Nadu, India. Phone: +91-44-2266 2500/01/02. E-mail: sowmyamahesh30@gmail.com
triterpenoids like cucurbitacins, fibers, polyphenols, 1000 times) did not show any free radical scavenging
are also seen. Sterols like campesterol, codisterol, effect.[8] The extract also showed a promising effect in
isofucasterol sitosterol etc. have been isolated from the liver damage induced by carbon tetra chloride where
seeds. .The methanolic extract of the fruit, consists of it improved and maintained the levels of superoxide
flavones C glycosides. It also contains flavonoids like dismutase, catalase and glutathione peroxidase,
isovitexin, saponatin, saporarin . The fruit also contains which are the important endogenous enzymes with
a water soluble polysaccharide, which had shown antioxidant properties.
excellent cytotoxic activity against MCF-7 cell lines.[4]
The radical scavenging effect of bottle gourd was
Extract of its leaves showed the presence of sterols, observed by performing different in vitro assays like
polyphenolics, flavonoids, saponin, protein, and radial scavenging assay, superoxide scavenging assay,
carbohydrates. A novel protein, lagenin, has also been MTT reducing assay and lipid peroxidation inhibition
isolated from its seeds, and it possesses antitumor, methods. It was observed that the ethyl acetate
immunoprotective, and antiproliferative properties. extract of the fruit showed the maximum antioxidant
activity.[10] From the above literature, it is shown
In addition, it also contains mono and di caffeoyl- that the ethyl acetate extract of Lagenaria siceraria
quinic acid was seen . The methanol extract of the is found to have maximum anti-oxidant property in
stem consists of D: C-friedooleanane type triterpenes, different in vitro assay methods DPPH assay was
which had shown cytotoxic activity against SK-Hep performed by this method. IC50 value was calculated
1 cell line.[3] and change in absorbance with respect to control was
calculated.[5]
ACTIVITIES IN LAGENARIA
The methanolic extract of Lagenaria siceraria leaves
SICERARIA is a vital source of natural antioxidant and it plays an
Immunomodulatory Activities important role as therapeutic agent by preventing and
slowing the progress of ROS and associated stress
L. siceraria fruit when extracted with methanol
related degenarative disease.[12]
showed notable reactions in rat with increase in white
cells and lymphocyte. HPLC analysis showed presence The acetone extract of Lagenaria siceraria fruit
of lagenin (a ribosome inactivating protein) which is epicarp shows maximum anti-oxidant activity. It was
responsible for the activity. Lagenaria was evaluated found that the ellagitannins that were present in the
for its immunomodulatory activity against pyrogallol acetone extract of L. siceraria fruit is responsible
induced immunosuppression. The results showed an for this radical scavenging activity.[8] Isoquercetin
increase in the humoral and cellular immunity. The was the major constituent which is responsible for
increase in non-specific immunity was indicated by the antioxidant property in Lagenaria siceraria.
the subsequent increase in the total leucocyte and Polyphenolic compounds were isloated from extracts
neutrophils count. From the studies it was clear that of Lagenaria siceraria. Flavones C glycosides
the fruit has both specific and non-specific immunity such as isovitexin, isoorientin saponarin, saponarin
modulating activity.[5] 4-o-glucosidase was obtained in the methanol and
water extracts of L. siceraria. Flavonoids such as
Analgesic Activity
isoquercetin, kaempferol was isolated from the
Lagenaria siceraria was evaluated for its analgesic ethylacetate and n-butanol extracts of dried fruit
property using Tail immersion method to determine the sample.phenolic acid such as gallic acid were also
pain treshold capacity of rats by using analgesiometer. isolated. UPLC chromatography studies were carried
It was found that the methanolic extract of Lagenaria out (at 280nm) by Mohan et al. method and was
siceraria fruit showed nominal activity (3.97 ± 0.01) found that peak ‘7’ is similar to that of derivative of
and the aqueous extract showed more activity at 180 caffeic acid. The levels of these compounds was found
min (5.81 ± 0,006).[6] to be maximum in fruit extracts. Catechol moiety
of isoquercetin was found to have the maximum
Antioxidant Activity antioxidant activity. From this study, it was found to
The fruit epicarp was extracted using acetone and that gallic acid is present in low content in the fruit.
evaluated for the in vitro antioxidant activity using Isoquercetin present in Lagenaria siceraria can be
DPPH (1, 1- diphenyl-2-picryl hydrazyl) as the used as α-glucosidase inhibitor.[13] Between the fresh
reagent and it was found that the extract showed a high and dried fruit extracts (like ethyl acetate, n-butanol
antioxidant activity.[7] Interestingly, the fresh juice of extracts) of Lagenaria siceraria, there is a negligible
bottle gourd had an effective antioxidant effect. The difference in antioxidant and chemical properties. So
juice had shown a significant effect even when diluted both type of fruits either fresh or dried exhibit similar
to ten times, whereas when diluted further (up to anti-oxidant properties.[14]
It has been proven that the epicarp is the best source of induced myocardial infarction and found a significant
antioxidant than the mesocarp, and it was found that cardioprotective effect. Vishal et.al evaluated the L.
the ethyl acetate fractions of both epicarp and mesocarp siceraria fruit powder against isoprenalin induced
have higher content of antioxidant. The total flavonoid cardiotoxicity in rats for cardioprotective activity. It
content of the fruit was found to be 17.9 mg/g, which was found that the pretreatment of Lagenaria siceraria
was measured by Sharma and coworkers.[7] powder (500 mg/kg) for about 51 days provides
cardioprotective effect in the heart of rats. Hence, it
Free radical scavenging method was studied which has cardioprotective activity was confirmed.[14]
shown that the ethanolic extract of the bottle gourd
seeds has maximum scavenging activity (75.19%) by The ethanolic extract of Lagenaria siceraria fruit
1,1-diphenyl-2-picryl hydrazyl free radical scavenging (EELSF) shows cardioprotective activity based on
method.[7] The antioxidant activity of the fruit juice lipid profile in myocardial infarction induced by
was studied using pyrogallol-induced oxidative stress. isoproterenol in albino rat model. It was reported
It was found that stimulation of humoral and cellular that the EELSF contain cardioprotective property
response was observed in immunosuppressed patients and considered helpful in the treatment of various
and thus showed a significant protection against the cardiovascular disorders.[19]
oxidative stress.[11]
Immunosuppressive Activity
Antihyperglycemic Activity
The aqueous extract of LS fruit shows preferential
The hyperglycemic condition possibly helps in the suppression on cell-mediated immunity and but had
generation of free radicals, which in turn can reduce not shown effect on humoral immunity. The extract
the natural antioxidant defensive properties of the suppresses the important contents of cell-mediated
cell and thus results in various complications like immunity. It was found that the extract could supress
disruption of cellular functions, oxidative damage to the non-specific immune system.[18]
cellular membranes and increased lipid peroxidation.
The presence of several flavonol glycosides and Antigiardial Activity
flavonoid containing extracts of numerous plants have Earlier, the petroleum ether and methanolic extracts of
shown promising anti-diabetic activity. certain cucurbitaceous vegetables were tested against
The extract of aerial parts against fruit showed activity Giardia lamblia. It was found that the petroleum ether
in diabetes. The antihyperglycemic activity is due to extract of C. maxima seeds shows highest activity
the presence of good flavonoid content in fruit. In the against Giardia lambelia.[20]
study, streptozotocin (50 mg/kg, i.p.) was administered
Hepatoprotective Activity
in rats to induce hyperglycemia. The methanolic
extract of the fruit was given orally (200 and The extract was prepared using soxhlet extraction using
400 mg/kg) for about 14 days MELS at doses of The petroleum ether and methanol and it was found that
standard drug used for the assay was Glibenclamide the methanolic extract exhibited highest mortality
(500 μg/kg) and the antidiabetic property was assessed (100%) within 96 hours with IC50 35.6 ppm.[20]
using different biochemical parameters at different
Cytotoxic Activity
time intervals (0, 4, 8 and 15 days).
Cancer is the leading cause of mortality. Cucurbitaceae
Administration of phytosterols at a dose of 30 mg/kg family showed antitumor activity. It has been proved that
has significantly decreased the blood glucose level the activity is due to cytotoxic and antioxidant property.
and also has a significant increase in the oral glucose
tolerance test animals in glucose tolerance.[12] For the study, healthy mice were selected and
Ehrlich’s ascites carcinoma (EAC) was inoculated,
Diuretic Activity and it is treated with methanolic extract of L. siceraria
The methanolic extract showed diuretic potential. It was (200 and 400 mg kg-1) and 5-Flurouracil (20 mg k-1) as
assayedbydifferentparameterssuchasurineconcentration, reference drug up to 9 days. Multiple parameters like
determination of electrolyte concentration of sodium, haematological parameter, biochemical estimations,
potassium and chlorides. Vacccum dried extract and were determined. The experimental results showed
methanolic extract of fruit were subjected for the that the antineoplastic activity was due to cell toxicity
activity and it was found that both the extracts shows and antioxidant effects. The experimental results had
increased urine volume (diuretic) and increased shown a notable increase in the levels of peroxide in
excretion of electrolytes.[16] the liver especially in EAC treated mice. In this study
viable cell count had shown a remarkable increase
Cardioprotective Activity (2.20 to 31.99%) in treated groups and the mean
Lagenaria siceraria showed excellent cardioprotective survival time had increased up to 61.54% and thus
effect.The fruit juice when given in rats with isoproterenol revealed the anti-tumor property of L. siceraria .[19]
Triterpenoids present in fruit shows cytotoxic activity lipoprotein component, which is known to protect
compounds like 3-o-coumaroyl D; C-friedooleana-7, against atheroscelerosis. Thus, the phytosterols from
9(11)-dien-29oic acid and 20-epibryonolic acid bottle gourd fruit can be used as an antihyperlipidemic
showed remarkable cell toxicity against SK-Hep1 agent and can be effectively used in the treatment of
cell line.. The cell toxicity studies for the compounds hyperlipidemia. The ethanolic extract of Lagenaria
were assayed by colorimetric method using MTT [3- siceraria fruit contain antiatherosclerotic potential.
(4,5- dimethylthiazol- 2-yl)-2,5- Diphenyl tetrazolium Thus, it reduces the risk of atherosclerosis. The extract
bromide] as the reagent. The compounds -O-(E)- induces the activity of the enzyme lipoprotein lipase
coumaroyl-D: C-friedooleana-7, 9 (11)-dien-29- oic and thus reduces the HMG COA reductase action in
acids (IC50 value: 4.8 mg/mL) and 20-epibryonolic hyperlipidemic rats. In addition, it also decreases the
acid (IC50 value: 2.1 mg/mL) showed remarkable cholesterogenesis in the liver.
cytotoxic activity against the SK-Hep 1 cell line.[25]
The methanolic extract of L. siceraria contained four The studies revealed that plant Lagenaria siceraria
new D:C-friedooleanane-type triterpenes, 3 beta-O- gave a positive Libermann-Burchard test for sterols.
(E)-feruloyl-D:C-friedooleana-7,9(11)-dien-29-ol (1), These sterol crystals showed reduction in cholesterol
3 beta-O-(E)-coumaroyl-D:C-friedooleana-7,9(11)- level, triglycerides, LDL, VLDL levels whileHDL
dien-29-ol (2), 3 beta-O-(E)-coumaroyl-D:C- cholesterol which is called as a good cholesterol that
friedooleana-7,9(11)-dien-29-oic acid (3), and protects the heart from coronary artery disease is
methyl 2 beta,3 beta-dihydroxy-D:C-friedoolean- also significantly increased by the ‘white sterols’ in
8-en-29-oate (6), along with known triterpenes with Lagenaria siceraria. Anti-hyperlipidemic activity was
the same skeleton, 3-epikarounidiol (4), 3-oxo-D:C- observed at a dose of 30 mg/kg.[20]
friedoolena-7,9(11)-dien-29-oic acid (5), bryonolol
(7), bryononic acid (8), and 20-epibryonolic acid The methanolic extracts of Lagenaria siceraria
(9). Using different spectroscopic methods, these fruits possess high antihyperlipidemic activity. It was
compounds were characterised. Among them, confirmed by performing test against experimentally
compounds 3 and 9 exhibited remarkable cytotoxic induced hyperlipidemia in rats. It is cleared at the end
activity against the SK-Hep 1 cell line with IC50 values of the 30th day, the lipid levels were much reduced
of 4.8 and 2.1 µg/ml, respectively.[25] and there is a notable elevation in the excretion of bile
acids.[30] It was found that the presence of phytosterols
In another study, a water-soluble polysaccharide was in bottle guard fruit having antihyperlipidemic property
extracted from Lagenaria siceraria fruit and identified as which helps to treat hyperlipidemia.[29] Thus, it reduces
methyl-alpha-d-galacturonate, 3-O-acetyl methyl-alpha- the lipid level (TC, LDL cholesterol, TG level in the
d-galacturonate, and beta-d-galactose in a ratio of 1:1:1. serum) and it increases the HDL cholesterol level
Various experimental analysis showed the presence of and thus established as a traditional medicine for
the repeated units in the polysaccharide, which exhibited the treatment of coronary artery diseases in India.[31]
excellent in vitro anticancer activity against human breast Lagenaria siceraria has shown inhibit the activity of
adenocarcinoma cell line (MCF-7).[4,26]
pancreatic lipase and thus suppresses the digestion of
Antihyperlipidemic Activity lipids. It also inhibits the entry of lipids inside the body.
The results indicate that the regular consumption of the
The oral administration of the aqueous extract of L.
fruit reduces the occurrence of obesity.[21]
siceraria reduced the elevated levels of triglycerides,
cholesterol and low density lipoprotein while it CNS Activity
enhanced the levels of high density lipoprotein. The
The CNS activity was performed using the petroleum
dietary fibre present in the fruit lowers the cholesterol
ether, methanol, chloroform extracts of L. siceraria.
level. Saponins present in this fruit increase the
Petroleum ether extract showed maximum analgesic
lipoprotein activity and fast removal of fatty acids in
the blood.[27] activity and at high doses the methanolic extract
showed a reduced motor activity. In addition, the
The methanol extract showed the presence of motor coordination was also found to be reduced.
phytosterols and were found to be a mixture of four These effects could be due to the presence of
different sterols namely, fucosterol, racemosol, various phytoconstituents present in the bottle
stigmasterol and stigmasta-7, 22-dien-3β, 4β-diol. gourd fruit.[33] Prajapati et al. suggested that the
These compounds were identified by various antidepressant activity of bottle gourd could be due
analytical techniques like FTIR, NMR and mass to the flavonoids, saponins, sterols that were found in
spectral studies. The sterol crystals (30 mg/kg) the methanolic extract of Lagenaria siceraria standley
showed remarkable decrease in the levels of different fruits (MESF). In addition, the other phytoconstituents
lipoproteins in the lipid profiles. On the other hand, the that were identified in the methanolic extract were
extract tend to show an increase in the high density carbohydrates, tannins, protein and amino acids.[34].