Synthesis and evaluation of analgesic and anti-inflammatory activities of most active free radical scavenging derivatives of embelin-A structure-activity relationship.

Antioxidant and related properties of the plant Embelia ribes and embelin are well known. In the present study embelin was condensed with various aromatic substituted primary amines to yield ten new and one reported derivatives along with monomethyl embelin. All these compounds along with embelin were evaluated for in vitro antioxidant activity using 2,2'-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) diammonium salt (ABTS) and 2,2'-diphenyl-1-picryl hydrazyl (DPPH) methods. Two para-substituted embelin derivatives showed potent antioxidant activity. These compounds along with embelin were studied for analgesic and anti-inflammatory activities at 10 and 20 mg/kg doses by standard methods. Potent analgesic activity higher than the standard pentazocine was observed. Embelin and both of its derivatives almost completely abolished the acetic acid induced writhing. p-Sulfonylamine phenylamino derivative showed better anti-inflammatory activity than embelin.

Antioxidant and hepatoprotective effect of the ethyl acetate extract of Enicostemma axillare (Lam). Raynal against CCL4-induced liver injury in rats.

Enicostemma axillare is used in Indian traditional medicine as a liver tonic. Its ethyl acetate extract has shown potent in vitro antioxidant activity and found to contain 7.26% of a bitter secoiridoid glycoside, swertiamarin. Hence, in the present study the ethyl acetate extract was screened for hepatoprotective and antioxidant properties against CCl4 induced hepatic injury in rats. The hepatoprotection was assessed in terms of reduction in histological damage and changes in serum enzymes and metabolites. The pretreatment with the extract at 100 and 200 mg/kg body weight doses given orally for eight days prior to CCl4 caused significant restoration of altered biochemical changes due to CCl4 towards the normal in serum, liver and kidney. The extract treatment at 200 mg/kg body weight was found to be more potent than the standard silymarin at 100 mg/kg body weight in reversing most of the biochemical parameters. Histopathological studies complemented the results of biochemical estimations in providing a proof of hepatoprotective and antioxidant actions of the extract. The study provides a support to the ethnomedical use of E. axillare in India.

In vitro antioxidant activity of Argyreia cymosa bark extracts.

The Argyreia cymosa bark extracts were subjected to in vitro antioxidant activity with different methods. The petroleum ether extract has shown antioxidant activity in ABTS, nitric oxide, hydroxyl radical (by p-NDA) and lipid peroxidation methods. The ethyl acetate extract has shown antioxidant activity in DPPH, H(2)O(2) and hydroxyl radical (by deoxyribose) scavenging methods.

Microwave-assisted rapid extraction of red dye from Caesalpinia sappan heartwood.

Since ancient times Caesalpinia sappan heartwood dye has been well-known for its medicinal and dyeing properties. Isolation of the red dye using both conventional and newly developed microwave method was carried out. The conventional heating of 2 h provided 0.656 +/- 0.049 g of the dye and by microwave heating at 540 W for 20 min, the yield obtained was 0.747 +/- 0.047 g. Both the dyes were found to be the same as evidenced by UV, TLC and HPTLC studies. Antioxidant activity of the dyes was also carried out using DPPH and nitric oxide methods to confirm the similarity in their biological activity. The procedure developed can be used for the fast extraction of the red dye of C. sappan without affecting the nature of the product.

Antipsychotic activity of embelin isolated from Embelia ribes: A preliminary study.

BACKGROUND: Embelia ribes is claimed in Indian traditional medical practice to be useful in the treatment of nervous diseases. Embelin, an alkyl substituted hydroxy benzoquinone, is a major active constituent of E. ribes. The present preliminary study was intended to evaluate antipsychotic activity of embelin against apomorphine-induced climbing behaviour in mice and stereotyped behaviour in rats. METHODS: Two doses of embelin (5 and 10mg/kg) were administered once daily for 15days before exposure to apomorphine. On the concluding day of pre-treatment, after apomorphine-injection, the rodents were assessed for climbing and stereotyped behaviours according to the published scoring system. Thereafter, neurotransmitters (dopamine, noradrenaline and serotonin) levels were estimated in rodent brains. RESULTS: Embelin pre-treatment significantly inhibited apomorphine-induced climbing and stereotyped behaviours in mice and rats, respectively. Further, embelin also statistically reversed elevated levels of dopamine, noradrenaline and serotonin neurotransmitters in the brain of mice and rats. Embelin showed more significant results at high dose (10mg/kg) than low dose (5mg/kg) in both the tested models. CONCLUSION: Considering the present pharmacological profile of embelin, it is suggested that embelin possesses antipsychotic activity in the treatment of psychotic disorders. However, further research is warranted for evaluating its exact mechanism of action.

Antioxidant activity of Aporosa lindleyana root.

Four successive and two crude extracts of Aporosa lindleyana Baill. root were tested for antioxidant activity using standard in vitro and in vivo models. The successive methanol and ethyl acetate and crude 50% methanol extracts showed antioxidant activity with IC50 values 3.51+/-0.27, 6.09+/-1.00 and 7.34+/-0.46 microg/ml, respectively, in DPPH method. In the nitric oxide radical inhibition method, the successive ethyl acetate, petroleum ether and methanol extracts showed antioxidant activity. The successive methanol extract at 100 and 200 mg/kg body weight administered for 5 days prior to CCl4 treatment caused a significant increase in the levels of catalase and SOD and a significant decrease in the level of TBARS in liver, kidney and blood, when compared to CCl4 treated control. These results indicate strong antioxidant nature of Aporosa lindleyana root. The in vitro cytotoxicity studies against normal Vero cell lines indicate non-toxic nature of the root extracts. The study provides a proof for the ethnomedical and reported biological activities.

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.

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.

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.

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.

Physico-Phytochemical investigation and Anti-inflammatory screening of Capsicum annum L. and Hemidesmus indicus (Linn.) R. Br.

Capsicum annum L. (Family: Solanaceae) and Hemidesmus indicus (Linn.) R.Br. (Family: Asclepiadaceae) are commonly used in Tamilnadufor treating various ailments in the native system of medicine. The hydroalcoholic extracts of both plants at dose level of 100 mg/kg body weight showed demonstrable anti-inflammatory activity in the carrageenan-induced hind paw model in rats. Nevertheless, the overall anti-inflammatory activity exhibited by the extracts are found to be less as compared with that of standard drug Indometacin. Preliminary physico-phytochemical analysis of the plants in question were attempted. The results are highlighted and discussed.

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.

Antitumor activity of Hypericum hookerianum against DLA induced tumor in mice and its possible mechanism of action.

A large number of plants belonging to the genus Hypericum and their phytoconstituents are known to possess potent anticancer nature. Earlier studies from our laboratories indicated a strong cytotoxic nature of the methanol extract of Hypericum hookerianum stem (MEHH). In the present study, the in vivo antitumor activity of MEHH against the Dalton's lymphoma ascitic (DLA) model was determined at 100 and 200 mg/kg body weight given orally for 10 days. The results indicate that administration of the extract not only increased the survival of animals with ascites tumor, decreased the body weight induced by the tumor burden and reduced the packed cell volume and viable tissue cell count, but also altered many hematological parameters changed during tumor progression indicating the potent antitumor nature of the extract. Hematological and biochemical analysis were carried out to prove the anticancer and antioxidant nature of the extract.

Hepatoprotective and antioxidant activity of methanol extract of Ficus glomerata.

The present study was carried out to evaluate Ficus glomerata extracts for antioxidant and hepatoprotective properties. The methanol extract of the bark of F. glomerata showed potent in vitro antioxidant activity when compared to the root methanol extract. In the in vivo studies, the CCl(4) treated control rats showed a significant alteration in the levels of antioxidant and hepatoprotective parameters. The methanol extract of the bark when given orally along with CCl(4) at the doses of 250 and 500 mg/kg body weight showed a significant reversal of these biochemical changes towards the normal when compared to CCl(4)-treated control rats in serum, liver and kidney. The results were comparable to those observed for standard sylimarin. Histological studies also confirmed the same. The results indicated the potent hepatoprotective and antioxidant nature of the bark extract.

Antioxidant and hepatoprotective activity of the methanol extract of Careya arborea bark in Ehrlich ascites carcinoma-bearing mice.

The methanol extract of Careya arborea bark (MECA) was tested for antioxidant and hepatoprotective activity in Ehrlich ascites carcinoma (EAC) tumor-bearing mice. Tumor control animals inoculated with EAC showed a significant alteration in the levels of antioxidant and hepatoprotective parameters. The extract treatment at 50, 100 and 200 mg/kg body weight doses given orally caused a significant reversal of these biochemical changes towards the normal in serum, liver and kidney when compared to tumor control animals indicating the potent antioxidant and hepatoprotective nature of the standardized extract.

Antitumor activity and antioxidant status of the methanol extract of Careya arborea bark against Dalton's lymphoma ascites-induced ascitic and solid tumor in mice.

Based on the ethnomedical use of Careya arborea Roxb bark in the treatment of tumors, the present study was carried out to evaluate the anticancer potentials against Dalton's lymphoma ascites (DLA)-induced ascitic and solid tumors. The methanol extract of its bark given orally to mice at the dose of 250 or 500 mg/kg body weight for 10 days caused significant reduction in percent increase in body weight, packed cell volume, and viable tumor cell count when compared to the mice of the DLA control group. Restoration of hematological and biochemical parameters towards normal was also observed. Histological observations of liver and kidney also indicated repair of tissue damage caused by tumor inoculation. The extract at the dose of 5 or 25 mg/kg body weight given i.p. daily for 14 days significantly reduced the solid tumor volume induced by DLA cells.

Potent in vitro cytotoxic and antioxidant activity of Careya arborea bark extracts.

Careya arborea is used in traditional medicine for the treatment of tumors and other ailments. The successive chloroform and ethyl acetate extracts and crude 50% methanol extract exhibited potent cytotoxicity against cancerous RD, HEp-2 and HeLa cell lines. They were found to be safe against the normal Vero cell line. The methanol and aqueous extracts possessed strong antioxidant activity against many oxidants in the in vitro antioxidant screening. The total phenol content of these extracts was found to be high. The results suggest strong cytotoxic and antioxidant properties and support the ethnomedical claims for the plant.

Antitumor Activity of the Methanol Extract of Hypericum hookerianum Stem Against Ehrlich Ascites Carcinoma in Swiss Albino Mice.

A large number of plants belonging to the Hypericum family are known to possess strong antitumor properties. The methanol extract of H. hookerianum Wight and Arnott stem (MEHH) exhibited potent in vitro cytotoxic activity against various cancerous cell lines. In the present study, the high performance liquid chromatography (HPLC) standardized MEHH was tested for in vivo antitumor properties against Ehrlich ascites carcinoma (EAC) tumor bearing mice at 100, 200, and 400 mg/kg body weight doses given orally once daily for 14 days. The results indicate that administration of the extract not only increased the survival of animals with ascites tumor, decreased the body weight induced by the tumor burden, and reduced packed cell volume and viable tissue cell count, but also altered many hematological parameters changed during tumor progression, indicating the potent antitumor nature of the extract. Among the three doses tested, the 200 mg/kg body weight dose was found to be the most potent.

Pharmacognostical Evaluation of Caesalpinia sappan Heartwood.

Caesalpinia span heartwood is used in folklore in India. The present work attempts to summarize the pharmacognostical characters of the heartwood of this plant. Ash and extractive values, phytochemical tests, HPTLC and fluorescence analysis were carried out. The present work contributes for the standardization of this medicinal heat wood.

Antitumor activity of total alkaloid fraction of solanum pseudocapsicum leaves.

The total alkaloid fraction of the methanolic extract of Solanum pseudocapsicum leaves was tested for its in-vivo antitumor activity against Dalton's Lymphoma Ascites model in mice. The total alkaloid fraction at 2.5 and 5.0 mg/kg body weight doses exhibited antitumor activity as revealed by the significant increase in the mean survival time and the percentage increase in life span of tumor bearing mice. The antitumor activity observed may be due to its cytotoxic properties. However the treatment caused a significant decrease in the body weight below the normal indicating the toxicity of the treatment.