IR@IIIM - Indian Institute of Integrative Medicine (CSIR)

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    200 research outputs found

    Flavone Glycoside Based Validated RP-LC Method for Quality Evaluation of Prishniparni (Uraria picta)

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    An LC method is developed for the quantitation of rhoifolin in Uraria picta, a plant of high usage frequency in all Asian traditional systems of medicine. An isocratic RP-LC method using C18 column, UV detection 265 nm and specificity with PDA and MS is speeding up, reliable and comprehensive analysis of rhoifolin in U. picta. Good linearity was obtained in the working range (0.02–0.10 mg mL-1), with correlation coefficients >0.99. LOD and LOQ were 2.33 and 7.69 ng, respectively. The method was validated following international guidelines. The described method can be utilized for assays and stability tests of U. picta extracts as well as Ayurvedic drugs based on Prishniparni

    Quantitative structure–activity relationship (QSAR) of aryl alkenyl amides/imines for bacterial efflux pump inhibitors

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    A quantitative structureeactivity relationship (QSAR) analysis has been performed on a data set of 42 aryl alkenyl amides/imines as bacterial efflux pump inhibitors. Several types of descriptors including topological, spatial, thermodynamic, information content and E-state indices have been used to derive a quantitative relationship between the efflux pump inhibiting activity and structural properties. Algorithm based on genetic function approximation method of variable selection was used to generate the model. Statistically significant model (with r2 ¼ 0.87) was obtained with the descriptors like radius of gyration and heat of formation besides E-state indices, A log P atom types and solvent accessible charged surface area playing an important role in determining the activity of the compounds against bacterial efflux pump. The model was also tested successfully for external validation criteria. The model is not only able to predict the activity of new compounds but also explained the important regions in the molecules in quantitative manner

    Amelioration of adjuvant induced arthritis by apocynin

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    The premise of the study was to investigate the antiarthritic potential of apocynin (APO) in Balb/c mice (in vivo). The experiment showed a dose-dependent decrease in oedema and showed a suppression of proinflammatory cytokines such as TNF-α and IL-1β and mediators such as prostaglandin E2 (PGE2)and LTB4. At oral doses of 0.5, 1.0, 2.0 and 4.0 mg/kg once daily during the course of the experiment,APO induced an inhibition of T cell mediated immune response causing suppression of CD4+ and CD8+ T cells and of intracellular interferon-gamma (IFN-γ ) by flow cytometry in arthritic mice. In parallel there was a dose-dependent inhibition in vascular permeability causing an inhibition in the migration of leucocytes and exudate volume at the site of the inflammatory reaction. These observations validate the immunoregulatory potential of apocynin. Copyright © 2009 John Wiley & Sons, Ltd

    Emodin reverses CCl4induced hepatic cytochrome P450 (CYP) enzymatic and ultrastructural changes: Thein vivoevidence

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    The curative effect of emodin (1,3,8-trihydroxy-6- methyl anthraquinone), an active compound of the plant species Ventilago maderaspatana Gaertn, was evaluated against carbon tetrachloride (CCl4) induced hepatic cytochrome P450 (CYP) enzymatic and ultrastructural alterations in rats. Methods: Female rats were administered CCl4 (1.5 mL/kg, ip) followed by varying doses of emodin (20, 30 and 40 mg/kg, oral po) after 24 h of CCl4 administration. Animals were euthanized after 24 h of last administration to determine liver function tests in serum, hepatic light microscopic and ultrastructural changes, activity of CYP enzymes, microsomal lipid peroxidation and protein contents, hexobarbitone induced sleep time and bromosulphalein retention. Results: The CCl4 induced-toxic effects were observed with sharp elevation in the release of serum transaminases, alkaline phosphatase, lactate dehydrogenase and g-glutamyl transpeptidase. An initial study for an optimum dose of emodin among different dose levels revealed that a 30 mg/kg dose was effective in restoring all the enzymatic variables and liver histoarchitecture in a dose dependent manner. Exposure to CCl4 diminished the activities of CYP enzymes (i.e. aniline hydroxylase and amidopyrine-N-demethylase and microsomal protein contents with concomitant increase in microsomal lipid peroxidation). Emodin at 30 mg/kg effectively reversed the CCl4 induced hepatotoxic events, which was consistent with ultrastructural observations. Hexobarbitoneinduced sleep time and plasma bromosulphalein retention also improved liver functions after emodin therapy. Conclusion: By reversal CYP activity and ultrastructural changes, emodin shows a strong hepatoprotective abilities

    Reaction of carbohydrates with Vilsmeier reagent: a tandem selective chloro O-formylation of sugars

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    A convenient and efficient method for selective replacement of the primary hydroxyl groups of sugars by chlorine with concomitant O-formylation, compatible with the presence of a variety of functional groups, has been developed using the Vilsmeier–Haack reaction. Sugars having free primary hydroxyl groups mostly afforded the chloro-O-formylated product while sugars devoid of primary hydroxyl groups yielded only O-formylated products

    Application of a multiplex PCR assay for the detection of Shigella, Escherichia coli and Shiga toxin-producing Esch. coli in milk.

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    A multiplex PCR (mPCR) assay using previously known genetic markers of Shigella, Escherichia coli and Shiga-toxic Esch. coli was standardized. uidA gene was targeted for the common detection of Esch. coli and Shigella, whereas ipaH and stx1 genes were used as markers for the detection of Shigella and shiga-toxin producing strains, respectively. The standardized assays detected the target organism specifically and selectively. The mPCR developed by combining all the three reactions generated specific products. The inclusivity and exclusivity tests depicted the precise specificity of the mPCR assay. Results were interpreted on the basis of the pattern of amplicons generated: amplifications of the ipaH and uidA gene fragments indicated the presence of Shigella spp., amplification of uidA alone revealed the presence of Esch. coli and additional presence of verotoxin gene amplicon indicated verotoxinogenic nature of the strain. Specific patterns of bands were obtained when different strains of Esch. coli and Shigella spp. were subjected to this assay. The reactions, individually as well as in the mPCR, could detect approximately 1 cell per 20-microl PCR assay. The protocols were validated by analyzing the coded samples of full fat milk spiked with different pathogens. In naturally contaminated raw milk samples (n=100), Esch. coli were detected in all samples and verotoxinogenic Esch. coli in 15 samples. Shigella, however, was not detected in any of the samples. When DNA purified from the samples found positive for Shiga-toxic Esch. coli was directly used as template for the mPCR, the results showed agreement with the enrichment based detection. The mPCR assay, standardized in this study, may be used for rapid microbiological evaluation of milk samples. Further, the study emphasizes the need for better hygienic conditions in dairies

    Anti-histaminic, anti-inflammatory and bronchorelaxant activities of 2, 7-dimethyl-3-nitro-4H pyrido [1,2-a] pyrimidine-4-one

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    An immunopharmacological profile of 2, 7-dimethyl-3-nitro-4H pyrido [1,2-a] pyrimidine-4-one(P-I) has been investigated using in vitro and in vivo models representing various features of Type I allergy. P-I prevented compound 48/80-mediated histamine release from rat peritoneal mast cells. A promising anti-inflammatory activity of P-I was evident in active paw anaphylaxis (mice)and carragenan-induced paw edema (rat). P-I inhibited eosonophil accumulation and eosinophil peroxidase activity in bronchoalveolar lavage fluid from ovalbumin challenged balb/c mice: in these animals blood levels of IL-5, and CD4+ T cells also remained attenuated. A promising bronchorelaxant effect of P-I was observed in histamine-contracted guinea pig tracheal chain via its antagonism to H1 receptor. These findings were compared with some known compounds(ketotifen, cetirizine and promethazine). The anti-histaminic, anti-inflammatory and bronchorelaxant activities of P-I has been discussed in context with its potential profile as an anti-allergic and anti-asthmatic agent

    The gastric ulcer protective effect of boswellic acids, a leukotriene inhibitor from Boswellia serrata, in rats

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    Aim of the study is to evaluate the anti-ulcer efficacy of the boswellic acids (BA), a triterpenoid known as antiinflammatory/anti-arthritic agent, which is in clinical use. The reason for the study is that, the known non-steroidal anti-inflammatory drugs (NSAIDs) are full of side effects especially ulceration which is at the top. BA, although, used as an anti-arthritic agent yet it is not only devoid of ulcer production but protective also. The activity evaluation was done by the following universally accepted animal models viz., pyloric ligation, ethanol–HCl, acetylsalicylic acid,indomethacin and cold restrained stress-induced ulceration in rats. Results of the present study revealed that BA possess a dose dependent antiulcer effect against different experimental models. It showed different degree of inhibition of the ulcer score towards different ulcerogenic agents. The ulcer score against various ulcer inducing agents viz.,pyloric ligation, ethanol/HCl, (acute and chronic) acetylsalicylic acid, indomethacin and cold restraint stress, was inhibited by 39%, 38%, 51%, 31%, 37% and 42% respectively at 250 mg/kg. From the data it is concluded that BA inhibited ulcer production non-specifically in all the experimental models, whereby, it is not possible to propose a single specific mechanism. Nevertheless it is possible that BA might be acting by increasing the gastric mucosal resistance and local synthesis of cytoprotective prostaglandins and inhibiting the leukotriene synthesis

    Boswellic acids: A leukotriene inhibitor also effective through topical application in inflammatory disorders

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    Boswellic acids (BA), a natural mixture isolated from oleo gum resin of Boswellia serrata comprised of four major pentacyclic triterpene acids: b-boswellic acid (the most abundant), 3-acteyl-b-boswellic acid, 11-keto-b-boswellic acid,and 3-acetyl-11-keto-b-boswellic acid, is reported to be effective as anti-inflammatory, immunomodulatory, antitumor,anti-asthmatic and in Chron’s disease. It inhibits pro-inflammatory mediators in the body, specifically leukotrienes via inhibition of 5-lipoxygenase, the key enzyme of leukotriene synthesis, is the scientifically proved mechanism for its anti-inflammatory/anti-arthritic activity. All previous work on BA for its biological activity has been done through the systemic application but no pre-clinical data reported for its anti-inflammatory activity by topical application. We here by report anti-inflammatory activity of BA through this route by applying different acute and chronic models of inflammation i.e., arachidonic acid and croton oil-induced mouse ear edema, carrageenan-induced rats paw edema and adjuvant-induced developing arthritis in rats. The results of the study revealed that the effect observed through this route is in accordance to the study conducted with the systemic route, thus establishing that BA when used through topical application is as effective as through the systemic route

    One-pot synthesis of α-aminophosphonates catalyzed by antimony trichloride adsorbed on alumina

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    SbCl3 adsorbed on Al2O3 is found to be an efficient and recyclable catalyst in promoting three-component coupling reactions of aldehydes (aromatic and aliphatic), amines (aryl amines, aliphatic amines and esters of S-a-amino acids) and dialkylphosphites to afford the corresponding a-aminophosphonates in high yields. The ethyl ester of S-phenylalanine was observed to yield the corresponding a-aminophosphonate with S,S-diastereoisomer formed in dominance over the S,R-diastereoisomer

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