Evaluation of antinociceptive and anti-inflammatory activities of extract and fractions of Eugenia jambolana root bark and isolation of phytoconstituents

Eugenia jambolana Lam., Myrtaceae, is a widely distributed and traditionally well known plant in India. The root bark of the plant was extracted with ethanol and then successively fractionated into petroleum ether fraction, chloroform fraction, n-butanol fraction and methanol fraction. The extract and fractions of the plant material were evaluated for the antinociceptive activity by acetic acid-induced writhing test and formalin-induced nociception test, and anti-inflammatory activity was screened by carrageenan-induced rat paw edema, cotton pellet induced granuloma formation and adjuvant induced arthritis in rat models. The test materials showed the antinociceptive and anti-inflammatory effect in dose dependent manner and the petroleum ether fraction was found to be most potent among the test materials. At 400 mg/kg b.w., p.o. dose petroleum ether fraction significantly inhibited 54.28% writhing response and 73.77% formalin induced nociception in mice. The fraction with same dose showed significant 79.31% inhibition of carrageenan-induced rat paw edema, 57.78% anti-proliferative effect and 77.93% inhibition of adjuvant induced arthritis. The bioactive petroleum ether fraction was then subjected to column chromatography which led to isolate three compounds, namely, β-sitosterol, stigmasterol and lupeol. These compounds were characterized and identified by IR, ¹H NMR, 13C NMR and mass spectroscopy.

Attenuation of carbon tetrachloride-induced hepatotoxicity by cow urine distillate in rats.

OBJECTIVE: To study the carbon tetrachloride-induced hepatoprotective activity in cow urine. METHODS: Effect of cow urine distillate on liver function was studied in vivo in rats intoxicated with carbon tetrachloride (CCl4). Hepatotoxicity was induced by a 1:1 (v/v) mixture of CCl4 in olive oil (5 mL/kg i.p). Protective effect of cow urine distillate (in three dose levels) and standard drug Silymarin (100 mg/kg, p.o) on liver function were studied in intoxicated rats. Parameters in the study included liver function tests and histological observations. RESULTS: The cow urine distillate decreased the levels of SGOT, SGPT, ALP, GGT, and total bilirubin in a dose-dependent manner (P < 0.05) as sylimarin. CONCLUSION: The observed protective effects of cow urine distillate on liver function might be due to the presence of antioxidants in cow urine.

Formulation and in vitro evaluation of in situ gels containing secnidazole for vaginitis.

Gel dosage forms are successfully used as drug delivery systems considering their ability to prolong the drug release. The main objective is to formulate and evaluate in situ vaginal gels of secnidazole, based on ion activated systems. The system utilizes polymers that exhibit sol-to-gel phase transition due to change in specific physico chemical parameters. Ion triggered system using gellan gum (0.1-0.75% w/v) along with sodium carboxymethylcelluose was used to prolong the release of secnidazole (1% w/v). Formulations were evaluated for gelling capacity, viscosity, gel strength, mucoadhesive force, spreadability, microbiological studies and in vitro release studies. The transformation of sols occur in the presence of monovalent/divalent cations in the dissolution medium. Effect of calcium carbonate and other process parameters were optimized and found that increase in calcium ions produce stronger gels. The drug content, clarity, and pH of formulation were found to be satisfactory. The viscosity was found to be in the range of 0.005 to 0.085 for sols, whereas for the gels 16 Pa.s. Formulation showed pseudoplastic flow with thixotrophy. The gel strength (using texture analyzer) and mucoadhesion was found to be up to 6.5 g and 4 g respectively. The optimized formulations were able to release the drug for 360 min. The gels are expected to improve the administration at the site of infection and decrease frequency.

Formulation and Evaluation of in situ Gels Containing Clotrimazole for Oral Candidiasis.

Gel dosage forms are successfully used as drug delivery systems to control drug release and protect the medicaments from a hostile environment. The main objective is to formulate and evaluate in situ oral topical gels of clotrimazole based on the concept of pH triggered and ion activated systems. The system utilizes polymers that exhibit sol-to-gel phase transition due to change in specific physico-chemical parameters. A pH triggered system consisting of carbopol 934P (0.2-1.4% w/v) and ion triggered system using gellan gum (0.1-0.75% w/v) along with hydroxylpropylmethylcelluose E50LV was used to prolong the release of clotrimazole (0.1% w/v). Formulations were evaluated for gelling capacity, viscosity, gel strength, bioadhesive force, spreadability, microbiological studies and in vitro release. The use of carbopol as in situ gel forming system was substantiated by the property to transform into stiff gels when the pH was raised, whereas in gellan gum this transformation occurred in the presence of monovalent/divalent cations. Effect of calcium carbonate and other process parameters optimized and found that increase in calcium ions produced stronger gels. The drug content, clarity, and pH of the formulation were found to be satisfactory. The viscosity was found to be in the range 5 to 85 centipoise for the sol, whereas for the gels it was up to 16000 centipoise. The formulation showed pseudoplastic flow with thixotrophy. The maximum gel strength (using texture analyzer) and bioadhesion was found to be up to 6.5 g and 4 g, respectively. The optimized formulations were able to release the drug up to 6 h. The formulation containing gellan gum showed better sustained release compared to carbopol based gels.

Evaluation of estrogenic activity of alcoholic extract of rhizomes of Curculigo orchioides.

The rhizomes of Curculigo orchioides Gaertn. (Amaryllidacea) is an important Ayurvedic as well as Unani drug. It is present in several drug formulations used in the treatment of menorrhagia and other gynecological problems. In this study, we conducted a comparative study of estrogenic activity of alcoholic extract of Curculigo orchioides with diethylstilbestrol in bilaterally ovariectomized young albino rats. Bilaterally ovariectomized albino rats were divided into five groups (n=9) receiving different treatments, consisting of vehicle (0.6% w/v sodium carboxy methyl cellulose), ethanolic extract of rhizomes of Curculigo orchioides at three different doses (viz., 300, 600, 1200 mg/kg body weight) and standard drug diethylstilbestrol (DES) at a dose of 2 mg/kg body weight. All these were administered orally daily for 7 days. Estrogenic activity was assessed by taking percentage vaginal cornification, uterine wet weight, uterine glycogen content and uterine histology as parameters of assessment. Alcoholic extract of Curculigo orchioides showed a significant increase in percentage vaginal cornification, uterine wet weight (P<0.001), uterine glycogen content (P<0.001) and a proliferative changes in uterine endometrium compared to the control.

Synthesis and biological activity of a novel series of 4-[2'-(6'-nitro)benzimidazolyl]benzoyl amino acids and peptides.

A series of new 4-[2'-(6'-nitro)benzimidazolyl]benzoyl amino acids and peptides have been synthesized by coupling the 4-[2'-(6'-nitro)benzimidazolyl]benzoic acid with amino acid methyl esters/dipeptides using DCC as the coupling agent. All the synthesized compounds were found to exhibit potent anthelmintic activity along with moderate antimicrobial activity.

Studies on the synthesis and biological activity of 3-arylaminomethyl-5-(3-pyridyl)-1,3,4-oxadiazole-2-thione derivatives.

3-arylaminomethyl-5-(3-pyridyl)-1,3,4-oxadiazole-2-thiones were prepared by reaction of 5-(3-pyridyl)-1,3,4-oxadiazole-2-thione with formaldehyde and appropriate alky and aryl amines in ethanol, as potential biological active agents. These new synthesized Mannich bases were screened for their antimicrobial, antifungal and antiinflammatory activities.