Pharmacological Activity and Chemical Constituents of Eclipta Alba

Table of contents

1.

Ethnopharmacology : Eclipta Alba (L.) has been used in various parts of tropical and sub-tropical regions like south America, Asia, Africa. There are three kinds or Eclipta Alba-the white-flowering, the yellowflowering, and the black-fruiting, but all three grow throughout India by marshes, rivers, and lakes or on the foothills of the Himalayas. It is an active ingredient of many herbal formulations prescribed for liver ailments and shows effect on liver cell generation. It is used as a tonic and diuretic in hepatic and spleen enlargement. It is also used in catarrhal jaundice and for skin diseases (Scott Treadway1998). The alcoholic extract of the plant has shown antiviral activity against Ranikhet disease virus (Sunita Dalal, et al., 2010). The plant is commonly used in hair oil all over India for healthy black and long hair (Roy RK, et al., 2008). The fresh juice of leaves is used for increasing appetite, improving digestion (Cheryl Lans, 2007) and as a mild bowel regulator. It is commonly used in viral hepatitis to promote bile flow and protect the parenchyma and popularly used to enhance memory and learning (Otilia Banji, et al., 2007).

Authors ? ? ?: Chandigarh College of Pharmacy, Landran (Mohali) M.pharmacy (Pharmacology Department). e-mails: [email protected], [email protected], [email protected]

The plant has a reputation as an antiageing agent in Ayurveda (Thakur VD, et al., 2005). It is used as a general tonic for debility. Externally it is used for inflammation (Amritpal singh, et al., 2008; and Mahesh Sawant, et al., 2004), minor cuts and burns and the fresh leaf-juice is considered very effective in stopping bleeding (Mukherjee DR, et al., 1976). Leaf juice mixed with honey is also used for children with upper respiratory infections and also used in eye and ear infections. It is a source of coumestans-type compounds used in phytopharmaceutical formulations of medicines prescribed for treatment of cirrhosis of the liver and infectious hepatitis (Wagner H. et al., 1986). (Tewtrakul S, et al., 2007). Vedic Guard, a polyherbal formulation is a synergistic combination of 16 medicinal plant extracts contains Eclipta Alba as a major ingredient (Rema Razdan, et al., 2008). Charaka advises taking the juice of Eclipta Alba with honey to prevent the onset of senility, and its oil as the best medicated massage oils for rejuvenation therapies.

Phytochemistry: Eclipta Alba (L.) contains wide range of active principles which includes coumestans, alkaloids, flavonoids, glycosides, polyacetylenes, triterpenoids. The leaves contain stigmasterol, ?-terthienylmethanol, wedelolactone, demethylw-edelolactone and 1986).The roots give hentriacontanol and heptacosanol. The roots contain polyacetylene substituted thiophenes.The aerial part is reported to contain a phytosterol, ?-amyrin in the n-hexane extract and luteolin-7-glucoside, ?-glucoside of phytosterol, a glucoside of a triterpenic acid and wedelolactone in polar solvent extract (Jadhav VM, et al., 2009). The polypeptides isolated from the plant yield cystine, glutamic acid, phenyl alanine, tyrosine and methionine on hydrolysis. Nicotine and nicotinic acid are reported to occur in this plant (Jadhav VM, et al., 2009).

Coumestan: Coumestan is an organic compound that is a derivative of coumarin. Coumestan forms the central core of a variety of natural compounds known collectively as coumestans. Coumestans, including a coumestrol and phytoestrogen are found in a variety of plants. Because of the estrogenic activity of some coumestans, a variety of syntheses have been developed that allow the preparation of coumestans so that their pharmacological effects can be explored. The major coumestan isolated from Eclipta Alba includes wedelolactone 0.5-0. Immunomodulator activity : The protection of neuronal tissue may be possible due to the immunomodulatory action of Eclipta Alba. Due to methanol extract of whole plant of Eclipta Alba (1.6% wedelolactone), the phagocytic index antibody titer, phagocytic index and WBC count increased. Due to inhibition of non-specific humoral (lysozyme, antiprotease and complement) and cellular (myelop-eroxidase content), the reactive oxygen and nitrogen species are produced.The dietary intake of Eclipta Alba aqueous leaf extract also enhance the non-specific immune response and disease resistance of o.massambicus against A.Hydrpphila. Eclipta Alba serve as a potential memory modulator also (Ghosh M et al., 1984 And Roitt I et al., 1998, Hudson L et al., 1991). Hair growth and alopecia : Eclipta Alba is a well known Ayurvedic herb for hair growth. Eclipta Alba is used in hair oil preparation since it promotes hair growth and maintains hair black.10%w/v of Eclipta Alba used as a main ingredient in the preparation of herbal formulation for hair growth. Petroleum ether and ethanolic extract were also used in oleaginous cream and applied topically (Roy R, et al., 2008).

Anticancer activity : The methanolic extract of Eclipta Alba has the inhibitory effect against colon cancer due to inhibition of proliferation of cancer cells in a concentration dependent manner (Ruddon R. W, et al., 1995 and St. Luke, et al., 2007). 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 models (Malaya Gupta, et al., 2005). 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 cancer (Neerja Kaushik-Basu, et al., 2008). Dasyscyphin-C (saponins) a newer isolated compound from Eclipta prostrata reported to have anticancercytotoxic activity. It was tested under invitro conditions in HeLa (Human cervical carcinoma) & vero cell lines. At the concentration of 50µg/ml it showed a good anticancer-cytotoxic activity on HeLa cells (Khanna, 2008). 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 proliferation (Mi Kyeong .

Hepatoprotective effect : Eclipta Alba is considered a powerful liver tonic. The hepatoprotective potential of Eclipta Alba was studied by assessing the biochemical parameters like lipid peroxide (LPO), superoxide dismutase (SOD), Catalase (CAT), glutathione peroxide (GPx), glutathione reductase (GR), ascorbic acid and ?-tocopherol. Oral administration of the Eclipta Alba significantly decreased levels of LPO and elevated the activity of antioxidant enzymes SOD, CAT, GPx, and GR as well as endogenous levels of ascorbic acid and ?-tocopherol. Eclipta Alba has show protective effect on experimental liver damage in rats and mice and also used for the treatment of liver cirrhosis and infective hepatitis by reducing centrilobular necrosis, hydropic degeneration and fatty change of the hepatic parenchymal cells (Singh B et al., 1993). The coumestans constituents of the Eclipta Alba plant, wedelolactone and demethylwedelolactone, are responsible for the potent antihepatotoxic activities in CCL 4 -galactosamine and phalloidin induced liver damage in rats (Chopra R et al., 1996). The ethyl acetate fraction of Eclipta Alba improves the both enzymatic and non enzymatic antioxidant status in rat liver (Singh B et al., 1993). Hepatoprotective activity also expressed by Eclipta Alba by regulating hepatic lysosomal enzymes (Saxena A, et al., 1993).

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 blood (Lal V.K, et al., 2010 Antioxidant properties: The antioxidant effects of Eclipta prostrata was reported when the level of serum hydroxyl radical (nmol/mg protein per minute) and serum lipid peroxide (nmol/mg protein) levels reduced as 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 was determined by ferric thiocynate (FTC) (Karthikumar S, et al., 2007).

Anthelmintic activity: The methanolic extract of whole plant of Eclipta Alba (L.) have the anthelmintic activity.

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 activity (Mi Kyeong . 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 aureus (Karthikumar S, et al., 2007).

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 Thailand (Sawangjaroen N, et al., 2005 andCheryl Lans. 2007). 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 diseases (Bensky Dan, et al., 1986).

2. Global Journal of Medical Research

Volume XIII Issue VII Version I Year ( ) B

Figure 1.
Introduction amily : Asteraceae Eclipta Alba (Asteraceae) is an annual herbaceous plant, commonly known as false daisy. It is an erect or prostrate, much branched, roughly hairy, annual, rooting at the nodes; the leaves are opposite, sessile and lanceolate. It is also known as Bhringaraj and Karisilakanni, which is found a common weed throughout India ascending up to 6000 ft. The specific Eclipta Alba means white which refers to the colour of the flowers. Main active principles consist of coumestans like wedelolactone, desmethylwedelolactone (Wagner H. et al., 1986), furanocoumarins, oleanane & taraxastane glycosides (Amritpal Singh.et al., 2010).
Figure 2. Figure :
:Figure : Eclipta Alba with White flower It is widely used in India as a chologuague and deobstruent in hepatic enlargement, for jaundice and other ailments of the liver and gall bladder (Scott Treadway, 1998). The water extract of Eclipta prostrata (whole plant) exhibited the most potent inhibitory activity against HIV-1 integrase (HIV-1 IN) (Tewtrakul S, et al.,
Figure 3. Table 1 :
1
).
Note: Volatile oils: The volatile components were isolated from the aerial parts of this plant by hydrodistillation and analysed by GC-MS. A total of 55 compounds, which were the major part (91.7%) of the volatiles, were identified by matching mass spectra with a mass spectrum library (NIST 05.L) (Xiong-HaoLin,et al., 2010).Saponins: From the whole plant of Eclipta Alba, a new triterpene saponin, named eclalbatin, together with alpha-amyrin, ursolic acid and oleanolic acid were isolated. Dasyscyphin C was isolated from Eclipta prostrate which were studied on the HeLa cells for the anticancer activity(Khanna, et al., 2008).Crude extract : The crude extract has wound healing properties. The loss of hepatic lysosomal acid phosphatase and alkaline phosphatase by CCl4 was significantly restored by Eclipta Alba. The previous studies shows that hepatoprotective activity of Eclipta Alba is by regulating the levels of hepatic microsomal drug metabolizing enzymes(Saxena AK, et al., 1993).The fresh plant is used as self medication by AIDS patients in
Figure 4. Table 2 :
2
Sl.No Chemical constituents Pharmacological activites
1 Wedelolactone Antihepatotoxic (Nazim Uddin, et al., 2010), Antibacterial (Karthikumar S, et al., 2007),
Trypsin Inhibitor, Antivenom (Vianna-da-silva NM, et al., 2003)
2 Eclalbosaponins hair revitalizing (Rupali thorat, et al., 2009), Antiproleferative (Khanna, et al., 2008 and
Neerja Kaushik-Basu, et al., 2008), Antigiardial (Sawangjaroen N, et al., 2005)
3 Demethylwedelolactone Antihepatotoxic (Wagner H. et al. 1986), Antihaemorrhage (Mukherjee DR, et al., 1976),
Antivenom (Vianna-da-silva NM, et al., 2003), Dye (cosmetic) (Meena AK, et al., 2010)
4 Dasyscyphin C Antiviral, Anticancer (Khanna, et al., 2008)
5 Eclalbatin Antioxidant(Tewtrakul S, et al., 2007)
6 Ecliptalbine Verazine Lipid lowering, Analgesic(Maged S. Abdel-Kader et al., 1998)
Anti -Ulcer Activity : Eclipta Alba has the anti-
ulcer activity. There are different type of herbal plants
which are used to treat anti-ulcer such as The
Polyherbal Formulation -RO7D consists of eleven
medicinal plants namely Centella asiatica, Cassia
auriculata, Cynadon dactylon, Rosa damascene,
Myristica fragrans, Nelumbo nucifera, Hibiscus rosa-
sinensis, Hemidesmus indicus, Glycyrrhiza glabra,
Eclipta alba and Phyllanthus niruri. The Polyherbal
Formulation -RO7D exhibited (P<0.001) significant
decrease in ulcer index in both the model and significant
decrease in the gastric volume in pyloric ligation rat
ulcer model. The study indicates that extract RO7D has
anti-ulcer activity and its anti-ulcer potential may be due
to anti -secretary and cyto-protective activity.
(Srinivasan D et al., 2008)
Figure 5.
improvement in parameters like body weight and lipid
profile by enhancing antioxidant defenses to protect
against oxidative damage (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 (Dae-Ik Kima, et al.,
2008).
Anti-inflammatory and Analgesic activity : The
extract of Eclipta Alba was administered orally to
investigate anti-inflammatory activity (Amritpal singh, et
al., 2008). The anti-inflammatory activity which estimated
by using carragenan induced paw oedema
model.Inflammation occures due to activation of platelet
activation factors and release of pro-inflammatory
mediators such as prostaglandins, kinins, tumor
necrosis factors and nitric acid. The extract of Eclipta
Alba has the potent inhibitor of the pro-inflammatory
transcription factors and a promising agent for the
treatment of the inflammatory cascade of cardio-
vascular diseases (Kaileh et al., 2007).
Antidiabetic Activity : Extracts of various plant
materials capable of decreasing blood sugar (Bopanna
K et al., 1982). The chloroform extract of Eclipta Alba
exhibited significant anitidiabetic activity in alloxan
induced diabetic rats. This extract has showed
1

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Notes
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Date: 2013-01-15