ABSTRACT
Background: The oleo-gum resin of Boswellia serrata contains pentacyclic triterpenic acids known as Boswellic acids (BAs) that are responsible for the anti-inflammatory and anti-arthritic activities by inhibition of 5-lipoxygenase. Methods: Soylecithin based tablet formulation of an enriched extract of BAs were formulated and evaluated comparatively with the unformulated extract for bioavailability on rabbits and therapeutic efficacy against arthritis on rats targeting two primary constituent 11-keto ?-boswellic acid (KBA) and 3-O-acetyl 11-keto ?-boswellic acid (AKBA). Total BAs content in the enriched fraction was measured and characterized by HPLC analysis. Soy lecithin based tablet of BAs enriched extract was prepared and evaluated for different parameters. Tablets at 160 and 320 mg/kg, and unformulated extract 160 mg/kg was assessed on CFA-induced arthritic rat model and bioavailability was evaluated on the rabbit. Results: Tablet formulation showed two times higher efficacy in increasing hot plate reaction time, reduction in paw volume, and TNF-? levels compared to unformulated extract signifying enhanced systemic absorption and availability of the BAs at the site of action. The tablet at 320 mg/kg dose showed repair of articular surfaces with small areas of erosion and irregularities in the connective tissue. Plasma samples of rabbit showed identified peaks only for KBA. Conclusion: The soy lecithin based tablet of BAs enriched extract at both doses showed higher peak plasma concentration and AUC compared to unformulated enriched extract. The results of the study substantiated higher efficacy and bioavailability of B. serrata gum resin enriched extract in the form of lecithin based tablet formulation.
ABSTRACT
Free radicals play an important role in stomach ulcer formation. The present investigation validates the anti ulcer activity of hesperidin, isolated from Citrus sinensis (L.) Osbeck, Rutaceae, through the assessment of its antioxidant potential over stomach mucosal tissue by histological examination. Hesperidin was isolated from the dried peel of C. sinensis, and authenticated by TLC, IR and HPLC. The anti-ulcerogenic potential of this fruit was assessed using indomethacin and hypothermic restrain stress-induced ulceration models on rats at 150, 300 and 450 mg/kg dose orally. The parameters measured were gastric pH, volume, free and total acidity, ulcer index, and mucin, glutathione, super oxide dismutase, catalase and protein content. Hesperidin at 300 and 450 mg/kg dose showed significant (p < 0.01-0.001) increase in pH, decrease in acidity and ulcer index against indomethacin and hypothermic restrain stress, along with histological evidence of cytoprotection. Glutathione, super oxide dismutase, catalase and mucin levels increased significantly at 450 mg/kg (p < 0.05-0.001) after indomethacin ulceration, whereas hypothermic restrain stress only increased glutathione and mucin levels. Hesperidin prevents oxidative cell injury by significant rise of super oxide dismutase, glutathione and catalase levels in gastric mucosa. Hesperidin allowed the regeneration of ulcerated tissue, and prevented hemorrhagic injury of gastric mucosa. The potential anti-ulcer effect of hesperidin may be due to antioxidant, mucoprotective and cytoprotective activities.
ABSTRACT
The effects of aqueous (PnAq) and alcoholic (PnAl) extract (50-250 mg/kg) of P. niruri on in vivo gamma radiation induced chromosome aberration and in vitro antioxidant activity (50-500 µg/ml) were studied. The antioxidant activity was studied by measuring inhibition of hydroxyl radicals generated by the fenton reaction along with pro-oxidant and iron chelating ability. PnAl showed highly significant in vitro free radical scavenging ability when compared to DMSO above 250 µg/ml concentration. PnAq showed significant pro-oxidant activity while PnAl was devoid of it at the tested concentrations. Exposure to gamma radiation (4 Gy) caused 29.10 % increase in the frequency of chromosomal aberrations. Administration of PnAl (250 mg/kg) showed highly significant decrease in chromosomal aberrations compared to radiation treated group. Radioprotective potential of alcoholic extract was found to be more effective than the aqueous extract. Qualitative phytochemical investigation of PnAq and PnAl revealed the presence of sugars, flavonoids, alkaloid, lignans, polyphenols, tannins, coumarins and saponins. Higher radioprotective effect of the alcoholic extract may be attributed to rich presence of antioxidant polyphenolic compounds.
ABSTRACT
The leaf extract of E. neriifolia significantly reduced apomorphine-induced stereotypy in mice at all doses (100, 200, 400 mg/kg body weight) in mice and rats and was devoid of catalepsic effect thereby, suggesting specific dopaminergic receptor modulating activity. The extract (400 mg/kg) potentiated pentobarbitone-induced hypnosis. It showed protection against maximal electro-shock-induced convulsion at 400 mg/kg. E. neriifolia leaf extract had anxiolytic action at 400 mg/kg by increasing the percentage of time spent in open arm in elevated plus-maze. The extract did not reverse scopolamine-induced amnesia on elevated plus-maze. It increased transfer latency at 200 and 400 mg/kg and also in combination with scopolamine. These results indicated anti-anxiety, anti-psychotic and anti-convulsant activity of E. neriifolia leaf extract in mice and rats. Phytochemical study showed the presence of steroidal saponin, reducing sugar, tannins, flavonoids in the crude leaf extract