IR@IIIM - Indian Institute of Integrative Medicine (CSIR)
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In silico identification of viper phospholipaseA2 inhibitors: validation by in vitro, in vivo studies
No full text2,3-Unsaturated Allyl Glycosides as Glycosyl Donors for Selective α-Glycosylation
No full textIn the presence of NBS and a catalytic amount of a
Lewis acid, 2,3-unsaturated allyl glycosides [6-(allyloxy)-3,6-dihydro-2-(hydroxymethyl)-2H-pyran-3-ol] have been successfully used as versatile glycosyl donors for the stereoselective R-glycosylation of a variety of alcohols comprising sensitive functions such as acetonide, keto, nitro, and ester in 50�90% yields. The methodology offers an equally facile alternative to 4-pentenyl replacement in unsaturated sugars
Protective efficacy of mitochondrial targeted antioxidant MitoQ against dichlorvos induced oxidative stress and cell death in rat brain
No full textDichlorvos is a synthetic insecticide that belongs to the family of chemically related organophosphate(OP) pesticides. It can be released into the environment as a major degradation product of other OPs, such as trichlorfon, naled, and metrifonate. Dichlorvos exerts its toxic effects in humans and animals by inhibiting neural acetylcholinesterase. Chronic low-level exposure to dichlorvos has been shown to result in inhibition of the mitochondrial complex I and cytochrome oxidase in rat brain, resulting in generation of reactive oxygen species (ROS). Enhanced ROS production leads to disruption of cellular antioxidant defense systems and release of cytochrome c (cyt c) from mitochondria to cytosol resulting in apoptotic cell death. MitoQ is an antioxidant, selectively targeted to mitochondria and protects it from oxidative damage and has been shown to decrease mitochondrial damage in various animal models of oxidative
stress. We hypothesized that if oxidative damage to mitochondria does play a significant role in dichlorvos induced neurodegeneration, then MitoQ should ameliorate neuronal apoptosis. Administration of MitoQ (100 mmol/kg body wt/day) reduced dichlorvos (6 mg/kg body wt/day) induced oxidative stress (decreased ROS production, increased MnSOD activity and glutathione levels) with decreased lipid peroxidation, protein and DNA oxidation. In addition, MitoQ also suppressed DNA fragmentation, cyt c
release and caspase-3 activity in dichlorvos treated rats compared to the control group. Further electron
microscopic studies revealed that MitoQ attenuates dichlorvos induced mitochondrial swelling, loss of
cristae and chromatin condensation. These results indicate that MitoQ may be beneficial against OP (dichlorvos) induced neurodegeneration
4-epi-Pimaric acid: a phytomolecule as a potent antibacterial and anti-biofilm agent for oral cavity pathogens
No full textThe present study focused on the antibacterial
and biofilm inhibitory potential of 4-epi-pimaric acid
isolated from aerial parts (stem and leaves) of Aralia
cachemirica L. (Araliaceae) against oral cavity pathogens.
4-epi-Pimaric acid exhibited minimum inhibitory concentration
(MIC) in the range of 4–16 μg/ml and minimum
bactericidal concentration (MBC) two- to four-folds higher
than MIC. There was significant inhibition in the biofilm
formation by Streptococcus mutans on the saliva coated
surface (P<0.05), and confocal microscopy revealed that
4-epi-pimaric acid inhibited the clumping and attachment of
S. mutans. At 8×MIC concentration, it significantly
prevented the pH drop and reduced S. mutans biofilms
(P<0.05). Increased propidium iodide staining and leakage
of 260- and 280-nm absorbing material by 4-epi-pimari
A unique immuno-stimulant steroidal sapogenin acid from the roots of Asparagus racemosus
No full textA new steroidal sapogenin molecule 1 having unique characteristics, 21-nor and unusual C19 carboxylic
acid has been isolated from the roots of Asparagus racemosus. On the basis of chemical evidence, extensive
spectroscopic analysis including two dimensional (2D) NMR and X-ray studies of single crystal,the structure of 1 was determined as(1S,2R,3S,8S,9S,10S,13S,14S,16S,17R,22R,25R)-21-nor-18�,27�-
dimethyl-1�,2�,3�-trihydroxy-25-spirost-4-en-19�-oic acid. 1 crystallizes in monoclinic space group P21 with a = 9.295(2), b = 11.238(2), c = 11.376(2)A˚ ; ˇ = 91.993(4)◦, Z = 2, Dcal = 1.344Mg/m3. The structure was solved by direct methods and refined by full-matrix least-squares procedure to a final R-value of 0.0561 for 4064 observed reflections. 1 was tested against the type of immune responses generated during treatment in normal and immune-suppressed animals and detailed biological activity evaluation suggests it to be a potent immunostimulator
Effect of altitude on picroside content in core collections of Picrorhiza kurrooa from the north western Himalayas
No full textPicrorhiza kurrooa Royle ex Benth (Scrophulariaceae),
commonly known as Kutki, is a major ingredient of many ayurvedic preparations prescribed in the treatment of various diseases. Picrosides I and II are the active agents responsible for the medicinal effects of Kutki,and the variation in content of these compounds in plants at
different altitudes is a major question to be addressed. The
picroside I and II content in various plant parts of P. kurrooa collected from different altitudes, viz. Sonemarg
(2,740 m a.s.l.), Tangmarg (2,690 m a.s.l.), and Pulwama
(1,630 m a.s.l.) in the north-western Kashmir Himalayas
was analyzed by HPLC. A considerable degree of variation
in picroside content was observed. Picroside I and II was
highest in populations collected from Sonemarg followed
by Tangmarg, suggesting that picroside accumulation is
directly correlated with altitudinal change. More picroside
I was found in the rhizome and roots of the Pulwama
population as compared to Tangmarg samples, whereas the
quantity of Picroside II was reduced in plants from Pulwama
compared to the Tangmarg population, suggesting that
cultivation of P. kurroa at lower altitude reduces the
picroside content. The quantities of picrosides also varied
spatially, being highest in rhizome followed by roots,
inflorescence and leaves in the populations from all three
locations. The study concludes that picroside I and II
accumulation depends on altitude, which could help in the
selection and collection of superior genotypes with uniform
effects for utilization by the pharmaceutical industry
Tandem Catalysis by Lipase in a Vinyl Acetate-Mediated Cross-Aldol Reaction
No full textThe lipase Novozym435 (0.6% w/w) was used in tandem with organocatalysts in a first vinyl/isopropenyl acetate-mediated aldol reaction. The reaction was facilitated through the lipase-catalyzed in situ generation of acetaldehyde/acetone. The importantfeatures of the present methodology include the mild and facile reaction conditions, regenerability of the lipase, comparatively high yields and minimal side product formation
Evaluation of antioxidant and antimicrobial activities of Bergenin and its derivatives obtained by chemoenzymatic synthesis
No full textBergenin pentacetate (2), a peracetate derivative of biologically active lead compound Bergenin (1) isolated from Bergenia stracheyi was subjected to lipase catalyzed regioselective alcoholysis to obtain 3,4,10,11-tetracetate of Bergenin (3). The free hydroxyl group of 3 was derivatised using higher carboxylic acids to obtain acyl derivatives (4–7). These compounds synthesized via chemoenzymatic route were characterized using 1H NMR, 13C NMR and mass spectral data and evaluated for DPPH radical scavenging, antimicrobial and xanthine oxidase inhibitory activities. The studies revealed that biological activity of Bergenin can be optimized by selective modification of its structure
Alcoholic extract of Cicer microphyllum augments Th1 immune response in normal and chronically stressed Swiss albino mice
No full textObjective The purpose of this study was to observe the effect of an alcoholic extract of Cicer microphyllum (I3M/38/A001) (whole plant without seeds and flowers) on the immunological
parameters of sheep red blood cell immunized normal and chronically stressed
Swiss albino mice
Novel bisstyryl derivatives of bakuchiol: Targeting oral cavity pathogens
No full textNovel bisstyryl derivatives of bakuchiol using Heck coupling reaction as the key step were synthesized
and screened against a panel of six oral cavity pathogens for their antimicrobial activity. Four compounds (9e12) showed two to fourfold and four to eightfold better activity (MIC 0.25e16 mg/ml)than bakuchiol and triclosan respectively. These compounds effectively inhibit the biofilm formation of single and multiple species at 2 e 8 � MICs. 4- and 40-Hydroxy/methoxy styryl moieties of the
bakuchiol derivatives play a pivotal role towards the activity as established in the SAR studies.Mechanism of action studies revealed microbial membrane structure disruption as the probable mode of action of these compounds