Pharmacological Activity of Eclipta Alba Linn

Abstract

The Bhringraj plant, scientifically known as Eclipta alba L., has many uses in Ayurvedic medicine. Common names for this plant include bhringaraj and fake daisy. Its distribution is global, with a concentration in the tropics and subtropics. It also highlights the short pharmacological profile of the chemicals or compounds derived from plant components and their characteristics. Anti-diabetic, anti-inflammatory, hair rejuvenator, antibacterial, analgesic, antiviral, hepatoprotective, immunomodulatory activity, etc., qualities of Bhringraj plant extracts are well-known among many medicinal uses for this plant. The herb Eclipta alba L. is ironic in bioactive compounds, including triterpenes, flavonoids, steroids, polypeptides, polyacetylenes, thiophene derivatives, and coumestans (wedelolactone and demethylwedelolactone). The pharmacological actions of this plant are thought to include anticancer, antioxidant, neuroprotective, analgesic, diuretic, hypolipidemic, antifungal, antimalarial, neuroprotective, and memory boosting properties. Eclipta alba L.'s taxonomy, phytochemistry, traditional use, medicinal value, and pharmacological activity are all topics that will be covered in this review.

Keywords

Introduction

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Figure1: Bhringaraj Plant

Table 1: Botanical Information

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Table 2: Vernacular Name

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MATERIAL AND METHOD

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Figure 2: Structures Of Major Cumestans

Steroidal Alkaloids

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Figure 3: Structure of Verazine

Flavonoids

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Figure 4: Major Structure of Flavonoids

Triterpenoids

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Figure 5: Structure of Eclipta saponin A

Volatile compounds

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Figure 7: Structure of Eclipta saponin A

Pharmacological Activities:

Neuroprotective effects

Eclipta alba has been the subject of numerous investigations on its potential neuropsychiatric effects in various animal models. The flavonoid luteolin, which is present in this plant, has shown promising results in the treatment of many neurological disorders. In a mouse model of acute pentylenetetrazole-induced convulsions, luteolin isolated from E. alba in methanolic solution had anticonvulsant effects. The treatment of epilepsy is another area that this chemical is being considered for. It also helps with traumatic brain injury, diabetes-related cognitive disease[41].

Antivenom properties

The chemical components extracted from Eclipta alba have demonstrated remarkable efficacy in counteracting a range of snake bite venoms. Research by Pithayanukul et al. on this plant's butanolic and pure butanolic extracts revealed its antivenom, hemorrhagic, and phospholipase A2 properties on the Calloselasmarhodostoma snake, a species native to Thailand. Another chemical in Eclipta alba called wedelolactone has shown anti-venom effects against the venoms of South American crotalids and Agkistrodon contortrix in a number of other investigations.

Antibacterial effect

There many bacteria that have been shown to be susceptible to the antibacterial effects of chemical components of E. alba.   Among the compounds isolated from E. alba, the two with the strongest antibacterial action were ethanol and ethyl acetate.  

Antifungal effect

The saponin fraction, an active component of E.alba leaves, has antifungal effects.  The antifungal effects against Candida albicans were also demonstrated by another chemical, 25-betahydroxyverazine.  Candida tropicalis, Trichophyton spp., Rhodotorulaglutinis, and Candida albicans were all inactivated in vitro by E. alba extracts[8].

Antimalarial effect

Mice infected with the Plasmodium berghei ANKA type of malaria showed encouraging responses to E. alba leaf extract, according to an investigation. At 200 ppm, the methanol extract was lethal.   This plant may be useful in the battle against malaria due to its larvicidal and ovicidal actions[30]. The methanol extract was lethal to larvae when it was at its peak effectiveness.   When tested against Aedes aegypti, the methanol extract showed the most effective ovicidal efficacy.   The methanol extract was lethal to all organisms (unhatchable) at 300 ppm.   All of the extracts had mild adulticide effects.   As the concentration of the extracts changed, so did their capacity to ward off mosquitoes.  

Hepatoprotective effect

It has been reported that the plant can protect against acute liver damage caused by carbon tetrachloride[3].  Wedelolactone and demethylwedelolactone are examples of coumestans that may contribute to the protective impact on the liver and the prevention of liver diseases.  In tests including CCl4 (carbon tetrachloride), GalN (galactosamine), and phalloidin-cytotoxicity, both chemicals demonstrated antihepatotoxic effects on rat hepatocytes.   They also significantly enhanced the regeneration of liver cells.   The alcoholic extract of E. alba showed good antihepatotoxic activity, as measured by the ratio of albino rats' livers to their body weights, the amount of time pentobarbitone was administered during sleep, the levels of glutamate pyruvate transaminase (GPT) and glutamic oxaloacetic transaminase (GOT) in their serum, alkaline phosphatase (ALP), and bilirubin.   Blood bilirubin, GOT, GPT, and SALP levels were all elevated in CCl4-treated rats, along with abnormalities in pentobarbitone sleep duration, liver weight, and overall health[2].   When given at a dosage of 200 mg/kg, the alcoholic extract significantly reduced these effects.   It may regulate liver microsomal drug metabolising enzyme levels, which in turn exerts its hepatoprotective properties.  Through phytochemical analysis, three substances were found in the extract: wedelolactone, luteolin, and apigenin.   These compounds inhibited HCV replication in vitro and in cell cultures in a dose-dependent manner.   Research suggests that this plant or one of its components may have anti-HCV properties.  An ethanol extract of the entire plant was tested in a mouse model of paracetamol-induced hepatotoxicity to determine its hepatoprotective effectiveness.  

Antidiabetic effect

In order to determine if an ethanolic extract of E. alba could alleviate hyperglycemia and diabetic nephropathy, researchers examined its possible anti-diabetic properties in rats with STZ diabetes.   The results demonstrated a 17.6% decrease in blood glucose levels compared to pre-treatment levels following 5 hours of oral administration of 250 mg/kg of the extract[17].   The eye-specific aldose reductase inhibitory activity of the extract was found to be roughly 4.5 μg per mL, while its noncompetitive inhibitory effect on α-glucosidase was approximately 54 μg per mL.Eleclalbasaponin VI was the most effective, having an IC50 value of 54.2 ± 1.3 microM.

Analgesic and anti-inflammatory effect

Experimental studies using albino mice using traditional models of pain response (tail flick, acetic acid-induced writhing reaction, and tail clip) proved that an ethanol extract of E. alba whole plants, together with a total alkaloid fraction, had analgesic effects.   The ethanol extract and whole alkaloids were determined to have good analgesic efficacy across all pain models in this investigation[7,26].   The entire alkaloid fraction had a stronger analgesic effect than the ethanolic extract. Tests assessing the effects of histamine and serotonin on inflammation, the cotton pellet generated granuloma test, and carrageenan-induced paw oedema were among the models used to evaluate the plant's anti-inflammatory potential in rats[6].   The plant had a robust anti-inflammatory impact.   It's potential as a peripheral and central nervous system analgesic is becoming more apparent.

Cardiovascular effect

Mildly hypertensive individuals have been studied to determine the effects of daily administration of 3 g of dried E. alba leaf powder.  Over the course of 60 days, subjects took three doses of six capsules containing 500 mg of powder daily.  Serum vitamin C levels (17%) and tocopherols (23%), as well as urine volume (34% increase), were significantly higher in the Eclipta group.  Research showed that leaf powder helped hypertensives deal with oxidative stress-related complications and had diuretic, hypotensive, and hypocholesterolemic effects.  Isolated frog hearts were tested for cardiac inhibitory activity with an ethanolic extract of E. alba leaves and leaf calluses[34].  The extracts reduced cardiac output and exhibited negative ionotropic and chronotropic effects.  At 20 mg doses, the inhibitory effect on the heart was greater in the callus extract compared to the leaf extract.  Researchers also discovered that the callus extract counteracted adrenaline's effects.

Immunomodulatory effect

Research on the immunostimulatory effects of tilapia (Oreochromis mossambicus) fish feeding on an aqueous extract of E. alba leaves has been conducted.  The fish were given diets containing extract at concentrations of 0.01, 0.1, and 1%.  Every week, we checked for disease resistance and nonspecific humoral and cellular responses to Aeromonas hydrophila[6,7]. After one, two, or three weeks of feeding fish an aqueous extract, lysozyme activity skyrocketed.  Myeloperoxidase concentration and reactive oxygen species generation were both markedly improved following one week of aqueous extract feeding.  When exposed to the infection, the percentage of fish that died after consuming the extract also dropped dramatically. 

Antiepilepsy effect

The antiepileptic efficacy of E. alba leaf powder, which was extracted using methanol, was studied in rats using the Maximal Electroshock Test (MES).   One hour after the last treatment, rats were shocked with a 150-mA shock for 0.2 seconds using ear clip electrodes by means of an electroconvulsiometer in order to induce seizures.   As a measure of anticonvulsant action, the time of hind leg extension was measured to be decreased.   Extensor phase duration was dramatically shortened in rats administered extract at several doses as compared to controls; the magnitude of this impact was dose-dependent.   The extract was found to include wedelolactone, luteolin, and β-amyrin, which were found to have antiepileptic properties.   Using guinea pigs and mice subjected to pentylenetetrazole and picrotoxin seizure models, researchers investigated the anticonvulsant properties of an ethanol extract from E. alba leaves.  Research on the extract's ability to modulate GABAA receptors and its impact on γ-amino butyric acid (GABA) levels in the brains of mice helped to better clarify the process.  Researchers believe that the anticonvulsant effect was caused by modulatory actions on GABAA receptors.  It was thought that the extract's wedelolactone and luteolin were responsible for the impact.  The malfunctioning of GABAA receptors is an important factor in the development of epilepsy.  Benzodiazepine (BZD) binding site on GABAA receptors is the one that wedelolactone is said to have a high affinity and selectivity for.  Additionally, luteolin binds to the GABAA receptors at the BZD location and has neuroprotective effects.

Anticancer effect

Researchers looked for anticancer effects in a hydroalcoholic E. alba extract.   The extract inhibited cell growth in a way that was dose-dependent, as shown by the IC50 values of 22 ± 2.9, 25 ± 3.6, and 50 ± 8.7 μg/mL for the HepG2, A498, and C6 glioma cell lines, respectively.   Extremely low amounts of matrix metalloproteinase 2 and 9 were detected.   Additionally, nuclear factor κB (NFκB) expression was shown to be decreased.   After 72 hours of extract treatment, DNA damage was identified, leading to apoptosis.Also, the drug-resistant hepatocellular cancer cell line DR-HepG2 demonstrated antiproliferative properties in response to the hydroalcoholic extract of the plant.   Researchers discovered that E. alba juice prevented the migration of hepatocellular carcinoma S102 (HCC-S102) cells.   The migration of all the cell lines that were tested—liver, lung, and breast cancer cells—was decreased by the juice, with IC50 values ranging from 31-70 μg/mL.   It appears that the plant could have potential as a tool in the battle against the spread of cancer.   Additionally, the antiangiogenic effects of the juice were demonstrated.  

Antiulcer effect

The antiulcer action of the methanolic extract of E. alba was further demonstrated by its successful treatment of ulcers caused by aspirin, ethanol, or pylorus ligation + aspirin in Sprague Dawley rats that had been fasted for 36 hours.   Oral E. alba groups showed a markedly decreased rate of gastric ulcer and inflammation compared to control groups in all three studies, even after 4 hours of therapy.  Rabeprazole, a medicine that blocks the proton pump, has activity levels similar to those of the extract.

Antihelmintic effect

The anthelmintic potential of a methanol extract of the entire E. alba plant was tested at doses ranging from 25 to 100 mg/mL against the earthworm Pheretimaposthuma.  Antihelmintic action against P. posthuma was likewise demonstrated by the water and ethanol extracts.

Hair growth promoting effect

The telogen hair growth phase was also used to select pigmented C57/BL6 mice, and the plant extract's capacity to stimulate hair growth during this phase was assessed.   The truncal epidermis does not include melanin-producing melanocytes, and melanin synthesis is closely associated with the anagen phase of hair growth in these species.  

Anti-hyperlipidemic effect

The albino mice, who are prone to hyperlipidaemia due to dietary fat, were utilised to study the hepatoprotective and antihyperlipidemic effects of E. alba.  After being administered E. alba, hypercholesterolemic mice showed a substantial decrease in serum levels of both LDL & VLDL cholesterol.   E. alba significantly improved the markers of SGOT, SGPT, and ALP, which are elevated in high-fat diets.

Antioxidant effect

In various extract solutions, Eclipta alba demonstrates antioxidant properties. Research conducted by Karthikumar, S. et al. indicated that the antioxidant activity of hexane, ethyl acetate, ethanol, and water extract varied with concentration, as assessed by ferric thiocynate (FTC)[11].  The researchers also found that the activity of polyphenols, flavonoids, and flavanone increased strongly with increasing polarity.

Antidepressant effect

This study shows that Eclipta alba leaf extract has an antidepressant effect in animal models of depression that is comparable to Imipramine and Fluoxetine.  To determine its medicinal value, phytochemical analysis, active ingredient separation, and additional research in this area are crucial.

CONCLUSION

The little, branching annual medicinal plant Eclipta alba (L) offers vital characteristics against a number of diseases.  Due to the presence of important chemical components for management of numerous infections and diseases, plant has garnered a lot of interest.  There may be a treatment for every ailment, but unfortunately, most of them come with worrying side effects.  Metabolite treatments derived from Eclipta alba, on the other hand, are completely safe because they are all-natural.  Various pharmacological activities, such as those with anti-diabetic, anti-proliferative, hypolipidemic, hepatoprotective, antioxidant, anti-epilepsy, anti-cancer, anti-malarial, and other potential medical uses, have been the subject of clinical trials.  Additionally, this plant may be able to prevent the growth of fungi and bacteria to a higher extent.  Finally, protecting the planet from economic and environmental losses can be achieved through additional research into the plant, which can pave way for modern medicine by allowing for isolation of novel bioactive molecules. These molecules will aid in investigation of various pharmacological activities aimed at curing incurable human diseases.

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