23 research outputs found

    Phytochemical Screening for Active Compounds in Pedalium murex L.

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    AbstractPedalium murex (Pedaliceae) has been traditionally used for the treatment of puerperal diseases, digestive tonics, ulcers, fevers, wounds other ailments and general debility. The present investigation was intented to evaluate the preliminary phytochemical characters of this plant. Phytochemical studies facilitate new discovery for the synthesis of more potent drugs. Keywords: Pedalium murex, leaves, fruits, solvents and active compound

    Molecular Dynamics Simulation Study and Hybrid Pharmacophore Model Development in Human LTA4H Inhibitor Design

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    Human leukotriene A4 hydrolase (hLTA4H) is a bi-functional enzyme catalyzes the hydrolase and aminopeptidase functions upon the fatty acid and peptide substrates, respectively, utilizing the same but overlapping binding site. Particularly the hydrolase function of this enzyme catalyzes the rate-limiting step of the leukotriene (LT) cascade that converts the LTA4 to LTB4. This product is a potent pro-inflammatory activator of inflammatory responses and thus blocking this conversion provides a valuable means to design anti-inflammatory agents. Four structurally very similar chemical compounds with highly different inhibitory profile towards the hydrolase function of hLTA4H were selected from the literature. Molecular dynamics (MD) simulations of the complexes of hLTA4H with these inhibitors were performed and the results have provided valuable information explaining the reasons for the differences in their biological activities. Binding mode analysis revealed that the additional thiophene moiety of most active inhibitor helps the pyrrolidine moiety to interact the most important R563 and K565 residues. The hLTA4H complexes with the most active compound and substrate were utilized in the development of hybrid pharmacophore models. These developed pharmacophore models were used in screening chemical databases in order to identify lead candidates to design potent hLTA4H inhibitors. Final evaluation based on molecular docking and electronic parameters has identified three compounds of diverse chemical scaffolds as potential leads to be used in novel and potent hLTA4H inhibitor design

    Characterization of Actinomycetes Antagonist Fusariumoxysporum f.sp.passiflora Isolated from Rhizosphere Soil ofPurple Passion Fruit Plants, South Sulawesi, Indonesia

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    To survey rhizosphere actinomycetes as potential biocontrol against fungal diseaseof passion fruits, rhizosphere soil of the plant were used as an isolation sources. Twenty fivestrains were assigned to Streptomyces-like strain based on morphological properties of sporechain. Four strain with distinguishing characteristic based on the macroscopic appearance ofcolonies on different media, were recovery from rhizosphere soil of passion fruits plantsuggesting that various Streptomyces spp. grow surrounding of plant roots. On an agarmedium, four strains (11.43%) commonly formed a clear growth-inhibition zone against fungal pathogen of passion fruits, Fusarium oxysporum f.sp. radicalix passiflori (FORP), indicatingthat this strains can produce antifungal substances. The present results indicate that four strainare a suitable candidate for the biocontrol of fusarium wilt. Keywords: Actinomycetes, AntifungalFusarium oxysporum f.sp.passiflora Rhizosphere, Purple Passion Fruit Plants, South Sulawesi, Indonesi

    Production, Purification and Characterization of Chicken Egg Yolk Immunoglobulin against Cryptococcus neoformans Capsular Antigen

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    Cryptococcus neoformans is an encapsulated yeast that can live in both plants and animals which cause Cryptococcal meningitis in human. Objectives: The aim of the present investigation is to produce anti-capsular egg yolk antibody in adult White Leghorn hen to promote immunodiagnosis and immunotherapy. Methods: The capsular antigen was prepared and administered to chickens. After immunization, the egg yolk antibodies were purified by Polyethylene and Ammonium sulphate precipitate method. IgY produced were titrated against killed whole cell antigen by micro-titer plate agglutination method and Growth inhibition assay was also carried out against live C. neoformans. Results: After 35 days of immunization, the antibody titer raised at high level. The intramuscular route of inoculation stimulates better IgY production than any other routes tried. The growth inhibition assay was directly proportional to the concentration of IgY added to the test medium. Conclusion: These findings suggest that the IgY is less invasive and not harm the experimental animals. It could be an alternate to IgG serum antibodies for both diagnosis as well as therapy

    Wild habits of Kolli Hills being staple food of inhabitant tribes of eastern Ghats, Tamil Nadu, India

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    432-437There is a proverb in Tamil that “Foods are medicines” “Medicines are foods”. Still it is being maintained by the folks, whose food habits depends on wild habits. Hence, the present study emphasis the documentation of traditional knowledge of Malayalis folks pertaining to their food habits which is necessary for the benefit of mankind. A survey has been made and identified 38 wild species belonging to 21 families. The roots, rhizomes and tubers of these plants are not only used as foods but are also consumed to maintain their health status. Thus these plants are used for general medicinal purposes also. Most of the tubers and roots are consumed after cooking, while some of them are eaten raw. Botanical name, family, vernacular name, life form/habit, parts used for food and medicine, mode of preparation and consumption are recorded for each species

    In vitro propagation of a rare succulent medicinal plant Caralluma diffusa (Wight) N.E.Br

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    Caralluma diffusa (Wight) N.E.Br is rare and an endemic medicinally important plantbelonging to the family Asclepiadaceae. A cost effective and efficient protocol has beendescribed in the present work for large scale and rapid propagation through in vitro organogenesis using nodal explants cultured on Murashige and Skoog’s (MS) media fortifiedwith BAP, 2,4-D, NAA and Kn. The highest frequency ( 83.3%) of callus was observed in MSmedium containing NAA (2mg/L) in combination with BAP (0.5mg/L) + Kn (0.25mg/L).Development of highest percentage of shoot organogenesis (82.4%) occurred when the calliwere sub cultured in MS medium supplemented with combination of BAP + NAA + Kn (2.0+ 0.5 + 0.25mg/L). Multiple shoots were induced from the nodal segments cultured onmedium containing BAP or Kn alone or in combination. Highest number of shoots(6.40±0.34) and maximum length of shoots (6.61±1.01cm) were obtained on MS mediumcontaining BAP (2.5mg/L). These shoots were then cultured on half strength MS mediumsupplemented with various concentrations of IBA and NAA. Highest percentage of rooting(78.4%) and mean length of rootlets was observed on IBA (0.5mg/L) in combination withNAA (0.5mg/L). In vitro derived plantlets were hardened and acclimatized. About 98% ofplantlets survived in field condition. The method described here can be successfully employed for large scale multiplication, long term in vitro conservation. This is the firstreport on indirect organogenesis of universally threatened cacti C. diffusa

    Micropropagation prospective of cotyledonary explants of <i>Decalepis hamiltonii</i> Wight & Arn.—An endangered edible species

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    256-260The study was undertaken to standardize the development of callus, shoot and root regeneration from cotyledonary explant of Decalepis hamiltonii Wight & Arn. through the tissue culture techniques. The MS medium supplemented with 6-benzyl amino purine (BA), 2,4-dichlorophenoxy acetic acid (2,4-D), kinetin (Kn), gibberelic acid (GA3), indole acetic acid (IAA), indole butyric acid (IBA) and 1-naphthalene acetic acid (NAA) was used for callus, shoot and root regeneration. The maximum percentage (82.0%)of callus formation was achieved on 0.5 mg/L BA in combination with 0.05 mg/L Kn, followed by 78.5% of callus formation on 0.5 mg/L 2,4-D fortified with 0.05 mg/L Kn. The highest shoot proliferation (4.6 shoots/callus) and shoot length (6.9 cm) was achieved on 1.0 mg/L BA combined with 0.1 mg/L GA3, followed by 3.8 shoots per callus and 5.8 cm shoot length on 1.0 mg/L IAA combined with 0.1 mg/L GA3. The highest root formation (38.2 roots/shoot) and root length (11.8cm) was achieved on ½ strength MS medium fortified with 0.4 mg/L IBA, followed by 36.5 roots per shoot and root length of 10.7 cm on 0.4 mg/L NAA. The well-developed rooted plantlets were hardened in the mixtures of forest soil, soil and vermiculite (1:1:1) and 97.5% plantlets survived after hardening

    A lazy learning-based QSAR classification study for screening potential histone deacetylase 8 (HDAC8) inhibitors

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    © 2015 Taylor & Francis. Histone deacetylases 8 (HDAC8) is an enzyme repressing the transcription of various genes including tumour suppressor gene and has already become a target of human cancer treatment. In an effort to facilitate the discovery of HDAC8 inhibitors, two quantitative structure–activity relationship (QSAR) classification models were developed using K nearest neighbours (KNN) and neighbourhood classifier (NEC). Molecular descriptors were calculated for the data set and database compounds using ADRIANA.Code of Molecular Networks. Principal components analysis (PCA) was used to select the descriptors. The developed models were validated by leave-one-out cross validation (LOO CV). The performances of the developed models were evaluated with an external test set. Highly predictive models were used for database virtual screening. Furthermore, hit compounds were subsequently subject to molecular docking. Five hits were obtained based on consensus scoring function and binding affinity as potential HDAC8 inhibitors. Finally, HDAC8 structures in complex with five hits were also subjected to 5 ns molecular dynamics (MD) simulations to evaluate the complex structure stability. To the best of our knowledge, the NEC classification model used in this study is the first application of NEC to virtual screening for drug discovery
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