Shrishailappa Badami

Antioxidant activity of the ethanolic extract of Striga orobanchioides.

Plants containing flavonoids have been reported to possess strong antioxidant properties. The ethanolic extract of Striga orobanchioides was screened for in vitro and in vivo antioxidant properties using standard procedures. The ethanol extract exhibited IC(50) values of 18.65+/-1.46 and 11.20+/-0.52 micro g/ml, respectively in DPPH and nitric oxide radical inhibition assays. These values were less than those obtained for ascorbic acid and rutin, used as standards. In the in vivo experiments the extract treatment at 100mg/kg body weight dose caused a significant increase in the level of the catalase in the liver and the kidneys. A significant increase in the level of SOD in the liver was observed. The treatment also caused a significant decrease in the TBA-RS and increase in the ascorbic acid levels. These results suggest strong antioxidant potentials of the ethanolic extract of S. orobanchioides.

Antioxidant and hepatoprotective effect of swertiamarin from Enicostemma axillare against D-galactosamine induced acute liver damage in rats.

ETHNOPHARMACOLOGICAL RELEVANCE The whole plant of Enicostemma axillare Raynal (Family: Gentianaceae) is used in variety of diseases in traditional Indian system of medicine including hepatic ailments. AIM OF THE STUDY Swertiamarin isolated from Enicostemma axillare Raynal was evaluated for antioxidant and hepatoprotective activity. MATERIALS AND METHODS Swertiamarin was isolated from successive ethyl acetate extract of the plant Enicostemma axillare belongs to the family Gentianaceae. The concentration of swertiamarin was determined by high performance thin layer chromatography (HPTLC). The hepatoprotective and antioxidant activity of swertiamarin (100 and 200mg/kg body weight) was carried out against d-Galactosamine (d-GalN) (200mg/kg body weight intraperitoneally i.p.) induced liver injury in rats. RESULTS Swertiamarin a secoiridoid glycoside was found to contain a major constituent of the extract. d-GalN caused significant hepatotoxicity by alteration of several hepatic parameters. It also caused significant lipid peroxidation and reduced the levels of antioxidant defense mechanisms. The treatment with swertiamarin at 100 and 200mg/kg body weight when administered orally for 8 days prior to d-GalN caused a significant restoration of all the altered biochemical parameters due to d-GalN towards the normal, indicating the potent antioxidant and hepatoprotective nature of swertiamarin. CONCLUSIONS Swertiamarin isolated from Enicostemma axillare possesses significant antioxidant and hepatoprotective properties against d-GalN induced hepatotoxicity given at 100 and 200mg/kg body weight orally for 8 days, which might be due to its in vitro antioxidant activity.

Protective effect of embelin against acetic acid induced ulcerative colitis in rats

The aim of the present study is to evaluate the effect of embelin isolated from Embelia ribes on acetic acid induced colitis in rats. Experimental animals received embelin (25 and 50 mg/kg, p.o.) and sulfasalazine (100mg/kg, p.o.) for five consecutive days before induction of colitis by intra-rectal acetic acid (3% v/v) administration and the treatment continued up to 7 days. The colonic mucosal injury was assessed by clinical, macroscopic, biochemical and histopathological examinations. Embelin treatment significantly decreased clinical activity score, gross lesion score, percent affected area and wet colon weight when compared to acetic acid induced controls. The treatment also reduced significantly the colonic myeloperoxidase activity, lipid peroxides and serum lactate dehydrogenase and significantly increased the reduced glutathione. The histopathological studies also confirmed the foregoing findings. The protective effect may be due to its antioxidant and anti-inflammatory activities.

Post-coital antifertility activity of Acalypha indica L.

Four successive solvent extracts of the whole plant Acalypha indica L. (Euphorbiaceae) were tested for post-coital antifertility activity in female albino rats. Of these, the petroleum ether and ethanol extracts were found to be most effective in causing significant anti-implantation activity. The antifertility activity was reversible on withdrawal of the treatment of the extracts. Both the extracts at 600 mg/kg body weight showed estrogenic activity. Histological studies of the uterus were carried out to confirm this estrogenic activity.

Hepatoprotective effect of the total alkaloid fraction of Solanum pseudocapsicum leaves

The total alkaloid fraction of the methanol extract of leaves of Solanum pseudocapsicum was tested for its hepatoprotective activity against CCl 4 induced toxicity in freshly isolated rat hepatocytes, HepG2 cells and animal models. The total alkaloid fraction was able to normalise the levels of aspartate amino transferase (ASAT), alanine aminotransferase (ALAT), alkaline phosphatase (ALP), triglycerides (TGL), total proteins, albumin, total bilirubin and direct bilirubin, which were altered due to CCl 4 intoxication in freshly isolated rat hepatocytes and also in animal models. The antihepatotoxic effect of the total alkaloid fraction was observed at very low concentrations (6–10µg/ml) and was found to be superior to that of the standard used. A dose dependent increase in the percentage viability was observed when CCl 4 exposed HepG2 cells were treated with different concentrations of the total alkaloid fraction. The highest percentage viability of HepG2 was observed at a concentration of 10µg/ml. Its in vivo hepatoprotective effect at 20 mg/kg body weight was comparable with that of the standard at 250mg/kg body weight. The total alkaloid fraction merits further investigation to identify the active principles responsible for the hepatoprotective properties. The results from the present investigation also indicate well correlation between the in vivo and in vitro studies.

Antifertility and hormonal properties of flavones of Striga orobanchioides

The two flavones, apigenin and luteolin, isolated from Striga orobanchioides, were investigated for endocrine and contraceptive properties. Graded doses of these compounds (5-25 mg/kg body weight/day) when administered from day 1 to day 4 of pregnancy showed dose-dependent and significant anti-implantation activity. The mean effective Dose 100% (MED(100)) for both compounds was found to be 25 mg/kg body weight. Oral administration of these compounds caused a significant increase in uterine weight in immature ovariectomised rats. It also caused a significant increase in uterine diameter, thickness of the endometrium and its epithelial cell height when compared with those of control rats. The uterotrophic potency was less than that of ethinyl estradiol. Simultaneous administration of these compounds with ethinyl estradiol caused a significant increase in uterine weight, uterine diameter, thickness of the endometrium and height of endometrial epithelium. The extent of these changes was also less than that in only ethinyl estradiol-treated rats. Hence the compounds exhibited estrogenic properties at their contraceptive dose level when given alone. However, along with ethinyl estradiol, they exhibited slight anti-estrogenic activity.

Antifertility activity of Derris brevipes variety coriacea.

Traditional physicians in and around Kotagiri village near Ootacamund, use a mixture of powdered roots of Cassia occidentalis, Derris brevipes variety coriacea and Justicia simplex to control female fertility. A mixture of powdered roots of these three plants, powdered root of Derris brevipes variety coriacea and its ethanolic extract were screened for antifertility activity in proven fertile female rats at 200 and 600 mg/kg body weight, respectively and given orally on D(1-7) of pregnancy. Both doses of the root powder of Derris brevipes variety coriacea showed 50% anti-implantation activity and also a significant reduction in the number of litters born. The ethanolic extract exhibited 40% anti-implantation activity when given orally at 600 mg/kg body weight. The rats, which continued their pregnancy, did not deliver any litters after their full term. Hence, the combined antifertility (anti-implantation and abortifacient) activity of the ethanolic extract was 100%. The results suggest that the ethanolic extract possesses more abortifacient type effect than the anti-implantation activity. The ethanolic extract also exhibited weak estrogenic activity when given alone and tested in immature ovariectomised female albino rats. But, when given along with ethinyl estradiol, it exhibited slight antiestrogenic activity. Histological and biochemical estimations were carried out to confirm this.

Antiedematogenic and free radical scavenging activity of swertiamarin isolated from Enicostemma axillare.

Swertiamarin, a secoiridoid isolated from the ethyl acetate extract of Enicostemma axillare, was evaluated for antiedematogenic activity using carrageenan-, formalin-, and histamine-induced paw edema methods in rats. In the carrageenan-induced method, the percentages of edema inhibition obtained after 5 h induction were 38.60, 52.50, and 45.44, respectively, for 100 and 200 mg/kg bw swertiamarin and 100 mg/kg bw of standard diclofenac sodium given orally. The activity of swertiamarin at 200 mg/kg bw was found to be superior to that of standard diclofenac sodium in all these methods. Swertiamarin was also screened for IN VITRO antioxidant activity using seven different methods: good activity was observed in ABTS and hydrogen peroxide methods, and moderate activity was observed in hydroxyl radical by deoxyribose and lipid peroxidation methods, with IC50 values of 2.83, 5.70, 52.56, and 78.33 microg/mL, respectively. The total antioxidant capacity was found to be 4.51 mM of ascorbic acid per gram of swertiamarin. Swertiamarin possesses antiedematogenic and in vitro antioxidant activities, and it may be the active constituent responsible for the anti-inflammatory activity of E. AXILLARE.

Antihistaminic and mast cell stabilizing activity of Striga orobanchioides

The ethanolic and aqueous extracts of the whole plant of S. orobanchioides were evaluated for antihistaminic and mast cell stabilizing activities. Both extracts inhibited histamine-induced contractions of the guinea-pig ileum at the concentration range of 2.5-25 microg/ml in a dose-related manner. At 25 microg/ml, both extracts inhibited the response of histamine (0.5 microg/ml) almost completely. The effect of these two extracts on the degranulation rate of sensitized peritoneal cells of albino rats when challenged with antigen (horse serum) was studied. Triple vaccine was used as adjuvant. Ketotifen and prednisolone were used for comparison. The ethanolic extract at 100 and 200 mg/kg body weight was found to significantly inhibit degranulation of mast cells to an extent of 52.14+/-3.24 and 67.96+/-3.70%, respectively. At the same doses, the aqueous extract showed 42.09+/-2.91 and 60.67+/-3.50% reduction in degranulation of mast cells, respectively. Hence, both extracts markedly protected the rats against antigen-induced challenge of mast cells.

In Vitro Cytotoxicity and Anti-tumor Properties of the Total Alkaloid Fraction of Unripe Fruits of Solanum pseudocapsicum

The total alkaloid fraction of the methanol extract of unripe fruits of Solanum pseudocapsicum was tested for in vitro cytotoxicity on HEp-2, RD and Vero cell lines and anti-tumor activity using DLA and HEp-2 cell lines. Cell viability and morphological changes were assessed. The total alkaloid fraction exhibited strong cytotoxic activity against all the cell lines tested. The CTC 50 (50 % of cytotoxicity inhibition) was found to be 1.65 µg/ml for the RD cell line, 6.32 µg/ml for the HEp-2 cell line and 12.01 µg/ml for the Vero cell line. In the clonogenic assay, no colony formation was observed even up to a concentration of 25 µg/ml. In the short term, antitumor, studies using DLA cells, the total alkaloid fraction was associated with 50 % viability in the concentration range of 6.25-12.5 µg/ml. In long term, anti-tumor activity using the HEp-2 cell line, no colony formation was observed up to a concentration of 20 µg/ml. Hence, there is a correlation between the results obtained in the cytotoxicity and antitumor studies carried out. Morphological observation by phase contrast microscopy revealed intense damage on all the cell lines. The total alkaloid fraction has the potential for further investigation in animal models.