1.2.5 anti-inflammatory activity in lipopolysaccharide-induced macrophage cells (Shih

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Last updated: December 25, 2019

1.2.5 BIOASSAYSAntibacterialactivityThetriterpenes present in the crude extract of Euphorbiahirta was isolated by silica gel chromatography to test the antimicrobialproperty of the plant extract. The compound taraxerone and25-hydroperoxycycloart-23-en-3?-ol and 24-hydroperoxycycloart-25-en-3?-ol presentin the crude were obtained to dissolve in ethanol that inhibits the growth of P.aeruginosa and S.aureus (Ragasa andCornelio 2013). The Euphorbia hirta extract,have prominent antibacterial effect against Shigelladysenteriae and Shigella flexneri(Ananthan et al.

,1995)  AntioxidantactivityThe flowerextract of E.hirta was obtained to evaluate DPPH free radical scavengingactivity, reducing power assay and other scavenging assay to check theantioxidant activity. The alcoholic extract showed high percentage inhibitionof 66.12±1.

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5 in superoxide anion scavenging assay and 50.2±1.7 in DPPHscavenging activity when compared to the other assays (Kumar et al.,2010) The methanolextract of Euphorbia hirta (L).

has astrong antioxidant property which explores a maximum, DPPH scavenging activityof (72.96±0.78) % whereas BHT has an antioxidant value of (75.

13±0.75) % whichis used as a standard (Basma et al.,2011). The aqueous and ethanol extract ofthis plant proved to have highest antioxidant activity using scavengingbioassays. The high level of phenolics and Flavonoid content presence may beresponsible for this activity (Uppala et al.

,2014).Anti-inflammatorypropertyThe ethanolicextract of E.hirta was showing an anti-inflammatoryeffect, the active component ?-amyrin, was isolated separately from the plant, whichproduces an anti-inflammatory activity in lipopolysaccharide-induced macrophagecells (Shih et al.

,2010). The effect on NO inhibition indicates the plantextract has a potency against inflammation. The triterpenes like ?-amyrin,?-sitosterol and methyl encyloartenol isolated from the n-hexane extract of E.hirta possess a significant anti-inflammatory property in 12-O-tetradecanoylphorbol acetate induced ear model (Vazquez et a.,1999)Anti-tumouractivityA newcyclopentanone derivative from E.hirtaplant was isolated and structurally elucidated.

The cytotoxicity effect of thiscompound has also been studied (Chi et al.,2012). The isolated(1R,5R)-5-(5-carboxymethyl-2-oxocyclopentyl)-3Z-pentenyl acetate compound fromthe ethanolic extract of E.hirta wereevaluated for cytotoxicity in K562, human leukemia and A549 lung cancer celllines which exhibit weak activity against A549 cells. The triterpenes areobtained from E.hirta to check thecytotoxicity effect, were a combination of 25-hydroperoxycycloart-23-en-3?-oland 24-hydroperoxycycloart-25-en-3?-ol was taken as sample 2 which showed apositive result against lung carcinoma A549 cell lines with IC50 value of 4.5µg ml-1 (Ragasa and Cornelio.,2013)AntidiarrhealactivityThelyophilized decoction of Euphorbia hirtacontains a flavonoid glycoside compound, quercitrin that showed a significantanti diarrhoeic effect, at a dosage level of 350mg and 700mg against threemodels of experimentally induced diarrhoea in mice by castor oil, arachidonicacid, and prostaglandin E2 (Galvez et al.

,1992). The antidiarrheal activity ofthis plant extract was performed in mice. The aqueous extract ranging from100-1000mg/kg was given in different dosage forms, followed by 0.5 ml of castoroil to each mouse. The result showed that the leave extract of Euphorbia hirta possibly plays a crucialrole in the anti-diarrhoeic activity (Hore et al.,2006).Diuretic effectThediuretic effect of E.

hirta was analyzedin rats by injecting water and ethanolic extract of the plant. There is asignificant increase in the electrolyte excretion, loss of Na+, K+, and HCO3?ions was enhanced by water extract. Whereas the ethanolic extract of E.hirtaincreases the excretion of HCO3? decreased the loss of K+ and had a littleeffect on the renal removal of Na+.

(Johnson et al.,1999)Anti-anaphylactic activityTheanti-anaphylactic effect of the ethanolic extract of E.hirta was observed against compound 488- induced systemicanaphylaxis in rat and mouse models. EH-A001 when given orally preventedcompound 4880 induced mortality and initiate a suppressive effect on TNF-?(Tumor necrosis factor alpha) by 34%, 55%, and 83% it also lowered the level of(interleuin-6) IL-6 by 38%, 63%, 89% after DNP-HSA challenge.

(Youssouf etal.,2007) The anti-allergic effect & immunosuppressive property of theethanolic extract of E.hirta weretested against various animal models. The nonspecific anaphylactic reactioninduced by compound 4880 where prevented by EH-A001, inhibiting RPMCdegranulation. Also, inhibit dextran-induced rat paw edema and suppress theCD4CD8 cell ratio in peripheral blood (Singh et al.,2006).

Sedative propertyThelyophilized aqueous extract of E.hirtapossesses a sedative property, which was confirmed by the decreased behaviouralactivity of mice when induced with a high dose of 100mg of dried whole plant/kg(Lanhers et al.,1990)Anti-venom activityThewhole plant decoction or paste was used to treat snakebite by ancientpractitioners. The phenolic compounds present in the extract are responsiblefor inhibiting the venom enzymes under in-vitro conditions (Gopi et al., 2015)A major constituent, pyrogallol present in the methanolic extract of E. hirta was found to have theanti-venom activity which is identified by GCMS, it significantly inhibitsprotease but not phospholipase A2 even at higher concentrationsproving the specificity in venom detoxification. The present study (Gopiet al.,2016) reveals that the compound Quercetin-3-O-rhamnoside isolated fromthe methanolic extract of E.

hirtainhibit the protease as well as metalloproteases present in the snake venom.Larvicidal activity Thereport of (Panneerselvam et al.,2013) reveals the larval and pupal activity of E.hirta leaf against An.

Stephensi at differentconcentrations ranging from 75 to 375 ppm. The mortality percent increases withthe concentration, the larvae found in the drinking water body was reduced by13.17%, 37.64% and 84.

00% at 24, 48 and 72 h after the treatment. Similarly,the combined effect of E.hirta and B.sphaericus showed a 100% reduction inlarval density which proves that the leaf extract has a potential control onthe malarial vector.

Different solvent extract of this plant was acquired toshow the larvicidal potential against Anopheles vector, in which the Petroleumether and methanol extract showed an effective toxicity to the vector (Sharmaet al.,2009). The methanol extract and the synthesized AgNPs from E. hirta leaf were analysed for toxicityeffect against An. Stephensiat. Thesynthesized AgNPs were more potent than crude extract, in inhibiting the larvalvector (Priyadharshini et al.,2012).

The study of (Rahman et al.,2010) addedthe predominant adult emergence inhibition and adulticidal activity of thisplant. 1.2.5 BIOASSAYSAntibacterialactivityThetriterpenes present in the crude extract of Euphorbiahirta was isolated by silica gel chromatography to test the antimicrobialproperty of the plant extract. The compound taraxerone and25-hydroperoxycycloart-23-en-3?-ol and 24-hydroperoxycycloart-25-en-3?-ol presentin the crude were obtained to dissolve in ethanol that inhibits the growth of P.aeruginosa and S.aureus (Ragasa andCornelio 2013).

The Euphorbia hirta extract,have prominent antibacterial effect against Shigelladysenteriae and Shigella flexneri(Ananthan et al.,1995)  AntioxidantactivityThe flowerextract of E.hirta was obtained to evaluate DPPH free radical scavengingactivity, reducing power assay and other scavenging assay to check theantioxidant activity. The alcoholic extract showed high percentage inhibitionof 66.12±1.

5 in superoxide anion scavenging assay and 50.2±1.7 in DPPHscavenging activity when compared to the other assays (Kumar et al.,2010) The methanolextract of Euphorbia hirta (L). has astrong antioxidant property which explores a maximum, DPPH scavenging activityof (72.

96±0.78) % whereas BHT has an antioxidant value of (75.13±0.75) % whichis used as a standard (Basma et al.

,2011). The aqueous and ethanol extract ofthis plant proved to have highest antioxidant activity using scavengingbioassays. The high level of phenolics and Flavonoid content presence may beresponsible for this activity (Uppala et al.,2014).Anti-inflammatorypropertyThe ethanolicextract of E.

hirta was showing an anti-inflammatoryeffect, the active component ?-amyrin, was isolated separately from the plant, whichproduces an anti-inflammatory activity in lipopolysaccharide-induced macrophagecells (Shih et al.,2010). The effect on NO inhibition indicates the plantextract has a potency against inflammation. The triterpenes like ?-amyrin,?-sitosterol and methyl encyloartenol isolated from the n-hexane extract of E.

hirta possess a significant anti-inflammatory property in 12-O-tetradecanoylphorbol acetate induced ear model (Vazquez et a.,1999)Anti-tumouractivityA newcyclopentanone derivative from E.hirtaplant was isolated and structurally elucidated. The cytotoxicity effect of thiscompound has also been studied (Chi et al.

,2012). The isolated(1R,5R)-5-(5-carboxymethyl-2-oxocyclopentyl)-3Z-pentenyl acetate compound fromthe ethanolic extract of E.hirta wereevaluated for cytotoxicity in K562, human leukemia and A549 lung cancer celllines which exhibit weak activity against A549 cells.

The triterpenes areobtained from E.hirta to check thecytotoxicity effect, were a combination of 25-hydroperoxycycloart-23-en-3?-oland 24-hydroperoxycycloart-25-en-3?-ol was taken as sample 2 which showed apositive result against lung carcinoma A549 cell lines with IC50 value of 4.5µg ml-1 (Ragasa and Cornelio.,2013)AntidiarrhealactivityThelyophilized decoction of Euphorbia hirtacontains a flavonoid glycoside compound, quercitrin that showed a significantanti diarrhoeic effect, at a dosage level of 350mg and 700mg against threemodels of experimentally induced diarrhoea in mice by castor oil, arachidonicacid, and prostaglandin E2 (Galvez et al.,1992). The antidiarrheal activity ofthis plant extract was performed in mice. The aqueous extract ranging from100-1000mg/kg was given in different dosage forms, followed by 0.5 ml of castoroil to each mouse.

The result showed that the leave extract of Euphorbia hirta possibly plays a crucialrole in the anti-diarrhoeic activity (Hore et al.,2006).Diuretic effectThediuretic effect of E.hirta was analyzedin rats by injecting water and ethanolic extract of the plant. There is asignificant increase in the electrolyte excretion, loss of Na+, K+, and HCO3?ions was enhanced by water extract. Whereas the ethanolic extract of E.

hirtaincreases the excretion of HCO3? decreased the loss of K+ and had a littleeffect on the renal removal of Na+. (Johnson et al.,1999)Anti-anaphylactic activityTheanti-anaphylactic effect of the ethanolic extract of E.hirta was observed against compound 488- induced systemicanaphylaxis in rat and mouse models. EH-A001 when given orally preventedcompound 4880 induced mortality and initiate a suppressive effect on TNF-?(Tumor necrosis factor alpha) by 34%, 55%, and 83% it also lowered the level of(interleuin-6) IL-6 by 38%, 63%, 89% after DNP-HSA challenge. (Youssouf etal.,2007) The anti-allergic effect & immunosuppressive property of theethanolic extract of E.

hirta weretested against various animal models. The nonspecific anaphylactic reactioninduced by compound 4880 where prevented by EH-A001, inhibiting RPMCdegranulation. Also, inhibit dextran-induced rat paw edema and suppress theCD4CD8 cell ratio in peripheral blood (Singh et al.,2006).Sedative propertyThelyophilized aqueous extract of E.hirtapossesses a sedative property, which was confirmed by the decreased behaviouralactivity of mice when induced with a high dose of 100mg of dried whole plant/kg(Lanhers et al.

,1990)Anti-venom activityThewhole plant decoction or paste was used to treat snakebite by ancientpractitioners. The phenolic compounds present in the extract are responsiblefor inhibiting the venom enzymes under in-vitro conditions (Gopi et al., 2015)A major constituent, pyrogallol present in the methanolic extract of E.

hirta was found to have theanti-venom activity which is identified by GCMS, it significantly inhibitsprotease but not phospholipase A2 even at higher concentrationsproving the specificity in venom detoxification. The present study (Gopiet al.,2016) reveals that the compound Quercetin-3-O-rhamnoside isolated fromthe methanolic extract of E.hirtainhibit the protease as well as metalloproteases present in the snake venom.Larvicidal activity Thereport of (Panneerselvam et al.,2013) reveals the larval and pupal activity of E.hirta leaf against An.

Stephensi at differentconcentrations ranging from 75 to 375 ppm. The mortality percent increases withthe concentration, the larvae found in the drinking water body was reduced by13.17%, 37.64% and 84.00% at 24, 48 and 72 h after the treatment.

Similarly,the combined effect of E.hirta and B.sphaericus showed a 100% reduction inlarval density which proves that the leaf extract has a potential control onthe malarial vector. Different solvent extract of this plant was acquired toshow the larvicidal potential against Anopheles vector, in which the Petroleumether and methanol extract showed an effective toxicity to the vector (Sharmaet al.,2009). The methanol extract and the synthesized AgNPs from E.

hirta leaf were analysed for toxicityeffect against An. Stephensiat. Thesynthesized AgNPs were more potent than crude extract, in inhibiting the larvalvector (Priyadharshini et al.

,2012). The study of (Rahman et al.,2010) addedthe predominant adult emergence inhibition and adulticidal activity of thisplant. 

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