IR@IIIM - Indian Institute of Integrative Medicine (CSIR)
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Immunomodulation exhibited by piperinic acid through suppression of proinflammatory cytokines
Piper longum (PL) has been reported for its varied pharmacological activities including bio-enhancer and anti-inflammatory activities in traditional medicine. Here the premise of the study was to investigate the immunoregulatory potential of PL and piperinic acid, one of its active constituent, in Balb/C mice (in vivo) and human PBMCs (in vitro) models. Piperinic acid moderated the proinflammatory mediators and cytokines in our experiments. At doses of 10, 20, 40 and 80 mg/kg p.o. PL showed a dose
dependent decrease of lymphocytes (CD4+ and CD8+ T cells) and cytokine levels in sensitized Balb/C mice with a marked
inhibition at 40 mg/kg. At an in vitro dose of 20 μg/ml of PL and 5 μg/ml of piperinic acid, there was a significant inhibition of mitogen induced human PBMC proliferation, mRNA transcripts of IL-2 (ConA) and TNFα, IL-1β and iNOS (LPS) respectively under stimulated conditions in time dependent (6 h, 12 h and 24 h respectively) expression studies. In parallel, induced nitric oxide production was also reduced by stimulated macrophages. Our observations rationalize the traditional use of PL and also validate the
immunoregulatory potential of piperinic acid
Variability and selection on different Argyrolobium roseum accessions for morphological traits and yield
Variability studies were carried out among different accessions of Argyrolobium roseum for 12 metric traits under natural and cultivated conditions.Almost all characters showed higher values in cultivated than natural population. Leaf breadth recorded highest CV (30.59%). Highest percentage of vitexin and D-pinitol (0.208 and 0.773% dwb) was observed in RAR-7 and RAR-6, respectively, under cultivated conditions. Phenotypic coefficient was higher than genotypic coefficient of variation. The association analysis revealed that root yield had positive significant correlation with 100 seed weight (r=0.839) biomass yield (r=0.601), where biomass yield had a
positive significant correlation with leaf length, single
pod weight. High heritability (97.4–99.8%) coupled
with moderate genetic advance ranged between (49–67%) as a percent of mean was observed for leaf breadth, pod length, total foliage biomass yield and total root yield/plant. This suggests that direct selection for these traits is suitable for the improvement of this crop
Anionic Domino C-O-Heterocyclization Approach for the Synthesis of 5-Vinyl Isoxazolines
5-Vinyl isoxazolines were isolated in high yields through
domino nucleophilic addition–anionic C–O-heterocyclization,
when allyl organometallics derived from trans-1,4-dihalobutene were reacted with nitrile oxides
Induction and assessment of morpho-biochemical mutants in Artemisia pallens Bess.
Artemisia pallens Bess. is a low volume and high value essential oil plant used in perfumery, cosmetic and flavouring industries. On account of the failure of conventional procedures to induce variability in species, mutation techniques have been tried in our experiments. Dry
and viable seeds (moisture content 8%) of homozygous pure breeding lines were subjected to 150–500 Gy doses of gamma rays and 0.01–0.1% ethyl methane sulphonate (EMS) for
8 h. Desirable qualitative mutants were recovered from segregating M2 generation (4,283 plants scored) raised as single plant progenies. The spectrum of morphological mutants included late and early flowering types; bushy and high yielding types; tall and more capitula-producing types and high oil and high davanone yielding types. These
were raised through M3 families to evaluate stability
and transmission of mutant characters. As such out of 15 different types selected in M2, only 11 types bred true to their characteristic variability. Based on their performance, the mutants were characterised depending upon their distinguishing features. Davanone, the main component
of oil showed the maximum increase (64.22% against 54.64% in control) in mutant ‘S–5’ recovered from exposure with 250 Gy c-rays. Mutant ‘E-6’ was economically most viable
having increased oil biosynthesis (0.36% against 0.22% in control) and hence yields higher oil per unit area than the parental control (isolated from 0.05% EMS treatment)
Anti-anaphylactic effect of Euphorbia hirta
The Euphorbia hirta ethanolic extract (EH A001) was found to possess a prominent anti-anaphylactic activity. A preventive
effect of EH-A001 given by oral route at dose from 100 to 1000 mg/kg was observed against compound 48/80-induced systemic anaphylaxis. At the same range of dose, EH-A001 inhibited passive cutaneous anaphylaxis (PCA) in rat and active paw anaphylaxis in mice. A suppressive effect of EH-A001 was observed on the release of TNF-α and IL-6 from anti-DNP-HSA activated rat peritoneal mast cells
Purification of 3 monomeric monocot mannose-binding lectins and their evaluation for antipoxviral activity: potential applications in multiple viral diseases caused by enveloped viruses
Three monomeric monocot lectins from Zephyranthes carinata, Zephyranthes candida, and Gloriosa superba with carbohydrate specificity towards mannose derivatives and (or) oligomannose have been isolated and purified from their storage tissues. The lectins were purified by anion-exchange chromatography on DEAE-Sephacyl and by gel filtration chromatography on Biogel P-200 followed by high-performance liquid chromatography. The purified lectins, Z. carinata, Z. candida, and G. superba had molecular masses of 12, 11.5, and 12.5 kDa, respectively, as determined by gel filtration and SDS-PAGE, indicating that they are monomers. In a hapten inhibition assay, methyl-alpha-D-mannopyranoside inhibited agglutination of both Z. candida and Z. carinata; the latter was also inhibited by Man(alpha1-2)Man and Man(alpha1-3)Man. Gloriosa superba showed inhibition only with Man(alpha1-4)Man of all of the sugars and glycoproteins tested. All purified lectins agglutinated red blood cells from rabbit, whereas G. superba was also reactive towards erythrocytes from guinea pig. All of the lectins were nonglycosylated and did not require metal ions for their activity. They were labile above 60 degrees C and were affected by denaturing agents such as urea, thiourea, and guanidine-HCl. The lectins were virtually nonmitogenic, like other members of Amaryllidaceae and Liliaceae. Of the 3 lectins, G. superba was found to be highly toxic to the BSC-1 cell line (African green monkey kidney epithelial cells), while both of the Zephyranthes species showed significant in vitro inhibition of poxvirus replication in BSC-1 cells without any toxic effects to the cells. In addition, Z. candida also exhibited significant anticancer activity against SNB-78, a CNS human cancer cell line
A chemo-enzymatic route to diastereoisomers of 2-methyl-1-phenyl-1,3-butanediol: the dual role of microorganisms
Diastereoisomers (1S,2R,3S)-, (1R,2R,3S)-, (1R,2S,3S)- and (1S,2S,3S)-2-methyl-1-phenyl-1,3-butanediols were prepared by simple and convenient strategies using two different chemo-enzymatic approaches for the reduction of racemic 2-methyl-1-phenyl-1,3-butanedione,both involving in situ racemization. The first method comprised a one-pot microbial reduction coupled with a chemical reduction, while
in the second method, stepwise chemo-enzymatic reductions were performed
Anti-tubercular agents. Part IV: Synthesis and antimycobacterial evaluation of nitroheterocyclic-based 1,2,4-benzothiadiazines
In continuation of our earlier work on benzothiadiazines, we have prepared a series of nitrofuran, nitrothiophene and
arylfuran coupled benzothiadiazines and evaluated them for antimycobacterial and antibacterial activities. One of the compounds 2f has shown good in vitro antimycobacterial activity. All the synthesized compounds have shown moderate to good antibacterial
activity
The formation of novel 1,3-dioxolanes: atypical Baylis–Hillman reaction of a sesquiterpene lactone parthenin
The Baylis–Hillman reaction of a sesquiterpene lactone parthenin with various aldehydes gave unexpected products containing a 1,3-dioxolane moiety. Both small aliphatic and aromatic aldehydes produced 1,3-dioxolanes, whereas higher aliphatic aldehydes produced normal Baylis–Hillman products
Macroporous Beads for Lipase Immobilization: Kinetic Resolution of a Racemic Drug Intermediate
Lipase isolated from Arthrobacter sp. (RRLJ-1, MTCC No. 5125,named ABL), is effective in resolving a wide range of racemic drug intermediates.In this study, ABL was immobilized on a series of synthetic macroporous epoxy copolymers beads with varying pore sizes, surface area and hydrophobicity.Poly(glycidyl methacrylate-co-ethylene dimethacrylate) beads, with 75% crosslink density and 10% of epoxy groups modified with dibutyl amine[GMA-EGDM-75 (10% DBA)] had a pore volume of 0.77 mL/g and a surface
area of 86.05m2/g; these beads were optimally suitable for ABL immobilization.The covalent binding of the lipase was optimized by varying the ionic strength, buffers, pH, temperature and time. The optimal binding was achieved in 100 mM phosphate buffer at