Effect of Embelin Against Lipopolysaccharide-induced Sickness Behaviour in Mice.

Sickness behaviour is a coordinated set of adaptive behavioural changes that develop in ill individuals during the course of an infection. It is relevant to understanding depression and some aspects of the suffering that in cancer. Embelin has been reported to possess antiinflammatory, neuroprotective and anxiolytic assets and has been shown to inhibit nuclear factor κB pathway and cytokine production. The present study was undertaken to investigate the effect of embelin isolated from Embelia ribes Burm in lipopolysaccharide (LPS)-induced sickness behaviour in mice. Adult male Swiss albino mice were pre-treated with embelin (10 and 20 mg/kg, p.o.) or dexamethasone (1 mg/kg, i.p.) for 3 days and then challenged with LPS (400 µg/kg, i.p.). At different time intervals of post-LPS challenge, sickness behaviour was evaluated in the animals by battery of behavioural tests (plus maze, open field, light-dark box, forced swim, social behaviour assessment, sucrose preference and food and water intake). Levels of oxidative stress makers (reduced glutathione and lipid peroxidation) in mice brain were also analysed. LPS induced behavioural alterations, anhedonia and anorexia, in mice. Pre-treatment with embelin attenuated behavioural changes induced by LPS. In addition, embelin prevented anhedonia, anorexia and ameliorated brain oxidative stress markers. The experimental outcomes of the present study demonstrated protective effect of embelin in LPS-induced sickness behaviour in mice. Copyright © 2016 John Wiley & Sons, Ltd.

Effect of embelin against 3-nitropropionic acid-induced Huntington's disease in rats.

3-Nitropropionic acid (3-NP) causes severe neurotoxicity in animals, which depicts Huntington's disease (HD) in humans. Embelin, the main active constituent of Embelia ribes, has been reported to possess various pharmacological actions, mainly anti-inflammatory, antioxidant, anticonvulsant and neuroprotective. The aim of the present study was to evaluate the neuroprotective effect of embelin against 3-NP induced experimental HD in rats. Adult Wistar rats were pretreated with vehicle/embelin (10 and 20mg/kg p.o.) for 7 days. From 8th day onwards, embelin was co-treated with 3-NP (15mg/kg, i.p.) for 7 days. At the end of the treatment schedule, animals were evaluated for behavioral alterations and brain homogenates were used for estimation of oxidative stress parameters (lipid peroxidation, reduced glutathione, catalase and glutathione-S-transferase). 2,3,5-Triphenyl tetrazolium chloride (TTC) stained brain slices were used for lesion size measurement. Administration of 3-NP significantly altered the behavioral and neuronal antioxidant status and caused significant neuronal damage in striatal region. Embelin, at both the tested doses, caused a significant reversal of behavioral and antioxidant status alterations and reversed the striatal neuronal damage induced by 3-NP. These findings suggest the neuroprotective effect of embelin against HD. The observed protective effect might be attributed to the antioxidant properties of embelin.

Anti-diabetic and anti-cataract effects of Chromolaena odorata Linn., in streptozotocin-induced diabetic rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Chromolaena odorata Linn., is used in traditional Indian medicine in the treatment of diabetes and eye problems. AIM OF THE STUDY: The present study was designed to investigate the effect of the ethanol extract Chromolaena odorata leaves (ACO) in streptozotocin (STZ; 45 mg/kg, i.v) induced diabetes and cataract in rats. MATERIALS AND METHODS: Different doses of ACO (200 and 400mg/kg) was administered once daily for eight weeks to STZ-induced diabetic rats. To know the mechanism of action of title plant, AUC(glucose), AUC(insulin), Homeostatic Model Assessment (HOMA), insulin tolerance test (ITT) and glucose uptake by rat hemi-diaphragms were carried out. Further, cataract score was taken once in a week upto eight weeks and opacity index was measured. HPLC fingerprinting profiling of ACO was also carried out. RESULTS: Administration of ACO exhibited significant reduction in glucose, HOMA, lipid profiles and significantly improved glucose and insulin tolerance, glycogen content, glucose uptake by skeletal muscle, serum insulin and HDL-c levels. In addition, ACO also decreased oxidative stress by improving endogenous antioxidants. Further, treatment of ACO showed significantly reduced onset and extent of cataract. CONCLUSION: The present data suggested that the treatment of ACO reversed the STZ-induced diabetes and cataract in rats. The observed beneficial effects may be mediated by interacting with multiple targets operating in diabetes mellitus and its complication. Taken together, this study provided the scientific evidence for the traditional use of Chromolaena odorata.

Protective effect of embelin from Embelia ribes Burm. against transient global ischemia-induced brain damage in rats.

Embelia ribes is being used in Indian traditional herbal medicine for the treatment of mental disorders and as brain tonic. The present study was designed to investigate the protective effects of embelin from E. ribes on global ischemia/reperfusion-induced brain injury in rats. Transient global ischemia was induced by occluding bilateral common carotid arteries for 30 min followed by 24-h reperfusion. Neurological functions were measured using sensorimotor tests. Ischemia/reperfusion-induced neuronal injury was assessed by cerebral infarct area, biochemical and histopathological examination. Pretreatment of embelin (25 and 50 mg/kg, p.o.) significantly increased locomotor activity and hanging latency time and decreased beam walking latency when compared with ischemic control. The treatment also reduced significantly the lipid peroxidation and increased the total thiol content and glutathione-S-transferase activity in brain homogenates. The decreased cerebral infarction area in embelin-treated groups and histopathological observations confirmed the above findings. These observations suggested that embelin is a neuroprotective agent and may prove to be useful adjunct in the treatment of stroke.

Anticonvulsant activity of embelin isolated from Embelia ribes.

Anticonvulsant activity of embelin (2.5, 5 and 10mg/kg, i.p.) was studied. It showed a significant inhibition of the seizures induced by electroshock and pentylenetetrazole in a dose dependent manner and the activity was comparable to phenytoin and diazepam. Significant decrease in locomotion revealing its CNS depressant activity was observed. The findings suggest that embelin possess anticonvulsant activity against both grand mal and petit mal epilepsy.

WITHDRAWN: Evaluation of antidiabetic effect of embelin from Embelia ribes in alloxan induced diabetes in rats.

The Publisher regrets that this article is an accidental duplication of an article that has already been published, http://dx.doi.org/10.1016/j.bionut.2010.08.002. The duplicate article has therefore been withdrawn.

Antinociceptive activity of swertiamarin isolated from Enicostemma axillare.

Many traditional Indian medicinal plants which contain large quantity of a secoiridoid, swertiamarin are being used to relieve pain. Iridoids present in a wide variety of medicinal plants possess a large number of medicinal properties. In the present study in vivo antinociceptive activity of swertiamarin isolated from E. axillare was carried out using three different methods in mice. In the hot plate method, a significant increase in the latency period was observed for the treatment with swertiamarin at 100 and 200 mg/kg bw after 30 and 45 min. The percent protection observed after 45 min was 109.42, 147.42 and 157.14, respectively, for the standard paracetamol and swertiamarin at 100 and 200 mg/kg bw treatments. A significant increase in the tail withdrawal reflex was observed for the swertiamarin treatment at both the doses with percent protections of 150 and 200, respectively. In both these methods, swertiamarin produced potent activity than that of standard paracetamol. In the acetic acid induced writhing, swertiamarin at 100 and 200 mg/kg bw reduced the number of writhes significantly. Dose dependent results were observed in all the three methods and among the two doses, swertiamarin at 200 mg/kg bw showed potent activity. These results prove that swertiamarin possess both peripheral and central antinociceptive activity.

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.

Potential transition state phosphoramidate inhibitors of beta-tubulin as antifilarial agents.

Transition state phosphoramidate inhibitors of beta-tubulin were designed as potential antifilarial agents. The reaction of 2-aminobenzimidazole with diisopropyl phosphite and carbon tetrachloride at a low temperature gave the unexpected 1-diisopropoxyphosphoryl-2-aminobenzimidazole, which on heating gave the novel benzimidazole derivative, 2-(diisopropoxyphosphoryl)aminobenzimidazole. Both products were fully characterized and the synthetic procedure to both compounds was optimized. The procedure was used to prepare the related 5-benzoyl-2-(diisopropoxyphosphoryl)aminobenzimidazole and 5-benzoyl-2-(diethoxyphosphoryl)aminobenzimidazole (1d). In a preliminary trial against Brugia pahangi compound 1d was found to have no antifilarial activity. This lack of activity may be attributed to its extreme insolubility and thus low bioavailability. The synthesis of analogous, more soluble, phosphorothioate-substituted benzimidazoles using the same methods may yield compounds with greater antifilarial activity.

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.

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.

Antiandrogenic effect of Striga orobanchioides.

The ethanolic extract of the whole plant of Striga orobanchioides given for 7 days to immature male rats at a dose level of 200 mg/kg body weight caused a significant decrease in the weight of the testes, epididymis, seminal vesicles and the ventral prostate. It also produced degenerative changes of Leydig cells, their nucleus, the seminiferous tubules and a significant decrease in the number of spermatocytes and spermatids. The seminiferous tubules of the treated rats are shrunken and compactly arranged. The antiandrogenic or antispermatogenic effect of the extract is discussed.

Antifertility activity of Striga orobanchioides.

Four successive solvent extracts of the whole plant Striga orobanchioides have been screened for antifertility activity in albino rats. Of these the ethanolic extract was found to be most effective in causing significant anti-implantation activity. The antifertility activity was reversible on withdrawal of treatment with the extract. The ethanolic extract at 200 mg/kg showed estrogenic activity. Histological studies of the uterus were carried out to confirm this estrogenic activity.