Eclipta alba (L.) A review on its phytochemical and pharmacological profile

PHARMACOLOGICAL PROPERTIES:

Crude extract:
The crude extract has been found to have wound healing properties. It been reported to counteract CCl4-induced inhibition of the hepatic microsomal drug metabolizing enzymes. The loss of hepatic lysosomal acid phosphatase and alkaline phosphatase by CCl4 was significantly restored by Eclipta alba. The study shows that hepatoprotective activity of Eclipta alba is by regulating the levels of hepatic microsomal drug metabolizing enzymes21. The fresh plant is used as self medication by AIDS patients in southern Thailand and showed potential as a therapeutic agent against Giardia intestinalis infections22,23. The leaf extract showed hypolipedemic activity in atherogenic diet induced hyperlipedemic rats7. It has antimicrobial and antioxidant properties24. 3% extract of Eclipta alba is used in pilex formulation with other ingredients. It has been reported to decrease bleeding time25. Leaf extract has been used in edema. It is used in the treatment of paronychia26.

Antihepatotoxic properties:
The hepatoprotective effect of the ethanol/water (1:1) extract of Eclipta alba has been studied at subcellular levels in rats against CCl4-induced hepatotoxicity. Eclipta alba significantly counteracted CCl4-induced inhibition of the hepatic microsomal drug metabolizing enzymes. The loss of hepatic lysosomal acid phosphatase and alkaline phosphatase by CCl4 was significantly restored by Eclipta alba. The study shows that hepatoprotective activity of Eclipta alba is by regulating the levels of hepatic microsomal drug metabolizing enzymes21. Bi-herbal ethanolic extract (BHEE) from the leaves of Eclipta alba and seeds of Piper longum at a dose level of 50 mg/kg body weight was administered orally once for 14 days which restored elevated serum marker enzymes such as SGOT, SGPT, ALP, LDH, ACP, GGT and 5' Nucleotidase, due to CCl4 treatment. All the biochemical parameters like total protein, total bilirubin, total cholesterol, triglycerides, and urea were also restored towards normal levels5. Hepatoprotective activity of methanolic extract and sub fractions of leaves and the chloroform extract and sub fractions of roots of Eclipta alba was carried out using carbon tetrachloride- induced liver damage and Lysosomal enzymes level in wistar albino rats. The methanolic extract of leaves and the chloroform extract of roots of Eclipta alba showed significant activities and respectively causing 72.8% & 47.96% reduction of lysosomal enzyme. The triterpenoid eclabasaponin fraction from methanolic extract of leaves produced significant (78.78%) and the alkaloidal fraction (60.65%) reduction of carbon tetra chloride induced increase in lysosomal enzyme in blood. Coumestan fraction and triterpenoidal saponin fraction from the chloroform extract of roots produced very significant (75.6%) and (52.41%) respectively reduction of carbon tetra chloride induced increase in lysosomal enzyme levels in blood6.

Antihyperlipedemic properties:
It has been reported that in the atherogenic diet induced hyperlipedemic model, the aqueous leaf extract of the Eclipta.prostrata was given orally to the rats which significantly reduced total cholesterol, triglycerides, total protein. There was a significant elevation in the high density lipoprotein cholesterol levels. 200mg/kg of extract showed better results compared to 100mg/kg7. Animal model containing Charles River Sprague-Dawley CD rats (specific pathogen-free/viral antibody-free Crj/Bgi male, 180 ± 10 g) were fed experimental diets supplemented with 0 mg (control), 25 mg (E25), 50 mg (E50), or 100 mg (E100) of a freeze-dried butanol fraction of E. prostrata per kilogram of diet for 6 weeks which reported significant reduction of serum triacylglycerol and total cholesterol, low-density lipoprotein-cholesterol levels and elevation in the high-density lipoprotein in the E50 and E100 groups respectively when compared with the untreated control group8.

Antioxidant properties:
The antioxidant effects of Eclipta prostrata was reported when 50mg/kg and 100mg/kg dose were fed orally into Charles River Sprague-Dawley CD rats which reduced serum hydroxyl radical (nmol/mg protein per minute) and serum lipid peroxide (nmol/mg protein) levels compared to untreated group. 100mg/kg dose significantly reduced Carbonyl content of oxidatively modified proteins8. Antioxidant activity of Eclipta prostrata was determined by FRAP, radical scavenging activity, reducing activity, and DPPH assay. The antioxidant capacity was increased by increasing the concentration of the extracts from 25 to 100mg/ml27. The antioxidant activity of the hexane, ethyl acetate, ethanol and water extracts of E. prostrata were determined by ferric thiocynate (FTC). FTC method was used to determine the amount of peroxide formed and that react with ferrous chloride (FeCl2) to form a reddish ferric chloride (FeCl3) pigment. In this method, the concentration of peroxide decreases as the antioxidant activity increases. Hexane, ethyl acetate, ethanol and water extract at various concentration (50, 100, 250 and 500 in µg/mL), showed antioxidant activities in a concentration dependent manner. Ethanolic extract at the concentration of 500 µg/mL showed (77.62%), which is close to the reference compound α-tocopherol (80.06%)24.

Immunomodulatory activities:
It has been reported that protection of neuronal tissues may be possibly due to the immunomodulatory action of Eclipta alba. Therefore, Eclipta alba can serve as a potential memory modulator28. Experimentation made to assess the immunomodulatory activity of methanol extracts of whole plant of E. alba (1.6% wedelolactone) at five dose levels (dose-response relationship) ranging from 100 to 500 mg/kg using carbon clearance, antibody titer and cyclophosphamide immunosuppression parameters significantly increased phagocytic index and antibody titer and the F ratios of the phagocytic index and WBC count were also significant30. The aqueous leaf extract Eclipta alba was fed into a fish (tilapia, Oreochromis mossambicus) at 0, 0.01, 0.1 or 1% levels as a diet for 3 weeks. After each week, non-specific humoral (lysozyme, antiprotease and complement) and cellular (myeloperoxidase content, production of reactive oxygen and nitrogen species) responses and disease resistance against Aeromonas hydrophila were noted which resulted in increased activity of non-specific immune parameters. The results indicate that dietary intake of E. alba aqueous leaf extract enhances the non-specific immune responses and disease resistance of O. mossambicus against A. hydrophila29.

Analgesic and Anti-inflammatory activity:
Albino wistar rats was used to investigate anti-inflammatory activity in which methanolic extract was administered orally. 100 and 200 mg/kg showed significant anti-inflammatory activity in carrageenin and egg white induced hind paw edema in rats which was compared with indomethacin (10 mg/kg) and cyproheptadine (8 mg/kg)31. Analgesic effect was studied on albino mice using ethanolic and alkaloidal extract of Eclipta alba. Standard experimental models such as the tail clip method, the tail flick method and the acetic acid induced writhing response were used which showed both the ethanol extract as well as the total alkaloids produced good analgesic activity in all the different models of analgesia used. The total alkaloidal fraction was the most efficacious in all models tested10,11.

Antidiabetic activity:
Leaf suspension of Eclipta alba (2 & 4g/kg) orally in alloxan induced diabetic rats resulted in reduction in blood glucose level, glycosylated hemoglobin. There was decreased activity of glucose-6 phosphatase and fructose1,6-bisphosphatase, and an increase in the activity of liver hexokinase. Thus oral administration of Eclipta alba suspension possess potent antihypergylcemic activity32. Eclipta alba as an ingredient in polyherbal formulation Pan-five were scientifically and clinically proved to possess Antidiabetic and diuretic activity by acting upon pancreas by restoration and regeneration of pancreatic β-cell activity33.

Hair growth & Alopecia:
Eclipta alba is used in hair oil preparations since it promotes hair growth and maintains hair black. 10%w/v of Eclipta alba was an main ingredient in the preparation of herbal formulation for hair growth35. Alopecia is a dermatological disorder with psychosocial implications on patients with hair loss. Eclipta alba is a well-known Ayurvedic herb for hair growth. In the reported work Petroleum ether & ethanolic extracts were incorporated into oleaginous cream (water in oil cream base) and applied topically on shaved denuded skin of albino rats. The time (in days) required for hair growth initiation as well as completion of hair growth cycle was recorded. Minoxidil 2% solution was applied topically and served as positive control for comparison. The result of treatment with 2 and 5% petroleum ether extracts were better than the positive control minoxidil 2% treatment .34

Anticancer activity:
Methanolic extract of Eclipta alba was evaluated for its anticancer activity against Ehrlich Ascites Carcinoma (EAC) in Swiss albino mice. On day 1, the extract of Eclipta alba at a dose of 250 and 500 mg/kg body weight were administered orally and continued for 9 consecutive days. The anticancer activity was examined by determining the tumor volume, tumor cell count, viable tumor cell count, nonviable tumor cell count, mean survival time and increase in life span in experimental animal models. The extract increased the life span of EAC treated mice and restored the hematological parameters as compared with the EAC bearing mice. Thus, study revealed that the methanolic extract of Eclipta alba showed anticancer activity in the tested animal models13. Coumestans are also known to act as phytoestrogens. These compounds are present in soyabeans and clover. In many countries it is used as diet which act as chemopreventive agent in breast and prostate cancer14.

Dasyscyphin-C (saponins) a newer isolated compound from Eclipta prostrata reported to have anticancer-cytotoxic activity12. It was tested under invitro conditions in HeLa (Human cervical carcinoma) & vero cell lines. At the concentration of 50^g/ml it showed a good anticancer-cytotoxic activity on HeLa cells12. A rat hepatic stellate cell line (HSCs) was used as in-vitro assay system, the methanolic extract of aerial parts of Eclipta prostrata showed significant inhibitory activity on HSCs proliferation9.

Combination therapy:
Eclipta alba (whole plant), Mimosa pudica (whole plant), Vitex negundo (whole plant), and Solanum nigrum (aerial parts) possessed styptic and anti-inflammatory properties and help in regeneration of the vascular endothelium36. Combination of Herbs like Anethum sowa (Shatapushpa), Piper longum (Pippali mool), Valeriana wallichii (Tagar), Cassia fistula (Aragvadh), Withania somnifera (Ashwagandha) and Triphala (A herbal combination of three fruits) with Eclipta alba (Bhringaraj) pacify the aggravated Vata dosha and combination with Elaeocarpus ganitrus (Rudraksha), Herpestris monniera (Brahmi) showed a tranquilizer effect37. Herbal mixture containing Phyllanthus nigrum Picrorrhiza kurroa, Zingiber officinale,Boerhaavia diffusa, Andrographis paniculata, Cichorium intybus, Emblica officinalis, Embelia ribes, Terminalia chebula, Terminalia arjuna, Piper longum with Eclipta alba is used as a good digestive tonic38. Galactin Vet Bolus a polyherbal ingredient containing Eclipta alba increased the yield of milk in the Holstein and jersey crossbred cows2. Eclipta alba with Acacia catechu leaves reduced severe hepatotoxicity3.

Other pharmacological activities:
It has been reported that the importance of free carboxylic acid at C-28 position in echinocystic acid derivatives from the methanolic extract Eclipta prostrata showed antifibrotic activity9. Ethanolic and ethyl acetate fractions of Eclipta prostrata were tested for its antibacterial activities against Escherichia coli, Klebsiella pneumoniae, Shigella dysenteriae, Salmonella typhi, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus24. Eclipta prostrata is combined with a non-plant material which is used to bath children suffering from malnutrition for 9 days and used as self medication by AIDS patients in southern Thailand22'40. 16 parts of Eclipta prostrata (bhringaraj), 1 part of Triphala formula {Emblica officinalis (amalaki), Terminalia chebula, (haritaki), Terminalia belerica (bibhitaki)}, 1 part of Caltropis gigantean (arka) and 1 part of Smilax officinalis (sariva) mixed with 80 parts of sesame oil and boiled to make a medicated oil which is reported to be used in skin diseases39.

Table.no:2

Pharmacological activities of the chemical constituents:

Sl.No

Chemical constituents

Pharmacological activites

1

Wedelolactone

Antihepatotoxic48, Antibacterial24, Trypsin Inhibitor, Antivenom50

2

Eclalbosaponins

hair revitalizing35, Antiproleferative12,14, Antigiardial22

3

Demethylwedelolactone

Antihepatotoxic43, Antihaemorrhage25, Antivenom50, Dye (cosmetic)51

4

Dasyscyphin C

Antiviral,Anticancer12

5

Eclalbatin

Antioxidant47

6

Ecliptalbine, verazine

Lipid lowering, Analgesic18

CONCLUDING REMARKS:
Eclipta alba offers a remarkable activities for curing of many diseases. It has a wide range of chemical constituents. Clinical investigations have been done on pharmacological activities like hepatotoxicity, proliferative, diabetic, hypolipedemic etc. It has an greater potential to inhibit the growth of the bacteria and fungus. Further investigation of the plant can increase the isolation of the newer molecules which will be helpful for the study of the pharmacological activities and to discover from the plant thus preventing the human and the economic losses in the environment.

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