01219nas a2200193 4500008004100000022001400041245006400055210006400119260007100183300001400254490000700268520054200275100002500817700002100842700002600863700001900889700002100908856009600929 2013 eng d a0163-386400aAntimycobacterial labdane diterpenes from leucas stelligera0 aAntimycobacterial labdane diterpenes from leucas stelligera a1155 16TH ST, NW, WASHINGTON, DC 20036 USAbAMER CHEMICAL SOCcOCT a1836-18410 v763 a

Phytochemical investigation of the acetone extract of the aerial parts of Leucas stelligera afforded four new compounds (1-4) belonging to the labdane diterpene series as well as two known flavones, velutin (5) and chrysoeriol (6). Structure elucidation of the new compounds was carried out using ID and 2D NMR spectroscopic data and single-crystal X-ray crystallography of compound 1. Compounds 1-4 exhibited selective antimycobacterial activity against Mycobacterium tuberculosis with IC50 values in the range 5.02-9.80 mu g/mL.

1 aKulkarni, Roshan, R.1 aShurpali, Ketaki1 aPuranik, Vedavati, G.1 aSarkar, Dhiman1 aJoshi, Swati, P. uhttps://library.ncl.res.in/content/antimycobacterial-labdane-diterpenes-leucas-stelligera-000813nas a2200205 4500008004100000022001400041245011200055210006900167260007300236300000800309490000800317100002800325700001900353700003100372700002100403700002100424700002100445700001900466856012200485 2014 eng d a0168-165600aAdvanced cell-based high-throughput screening assays targeting active and latent Mycobacterium tuberculosis0 aAdvanced cellbased highthroughput screening assays targeting act aPO BOX 211, 1000 AE AMSTERDAM, NETHERLANDSbELSEVIER SCIENCE BVcSEP aS180 v1851 aShurpali, Ketaki, Dilip1 aSingh, Upasana1 aSarkar, Shamim, Akhtar Sam1 aMishra, Abhishek1 aKulkarni, Roshan1 aJoshi, Swati, P.1 aSarkar, Dhiman uhttps://library.ncl.res.in/content/advanced-cell-based-high-throughput-screening-assays-targeting-active-and-latent-001991nas a2200289 4500008004100000022001400041245008900055210006900144260009200213300001200305490000700317520096500324653002501289653001501314653002101329653002101350653002801371653001401399100002501413700002201438700002401460700003001484700001901514700002601533700002101559856012101580 2014 eng d a1478-641900aAntifungal dimeric chalcone derivative kamalachalcone E from Mallotus philippinensis0 aAntifungal dimeric chalcone derivative kamalachalcone E from Mal a4 PARK SQUARE, MILTON PARK, ABINGDON OX14 4RN, OXON, ENGLANDbTAYLOR & FRANCIS LTDcFEB a245-2500 v283 a

From the red coloured extract (Kamala) prepared through acetone extraction of the fresh whole uncrushed fruits of Mallotus philippinensis, one new dimeric chalcone (1) along with three known compounds 1-(5,7-dihydroxy-2,2,6-trimethyl-2H-1-benzopyran-8-yl)-3-phenyl-2-propen -1-one (2), rottlerin (3) and 4 `-hydroxyrottlerin (4) were isolated. The structure of compound 1 was elucidated by 1D and 2D NMR analyses that included HSQC, HMBC, COSY and ROESY experiments along with the literature comparison. Compounds 1-4 were evaluated for antifungal activity against different human pathogenic yeasts and filamentous fungi. The antiproliferative activity of the compounds was evaluated against Thp-1 cell lines. Compounds 1 and 2 both exhibited IC50 of 8, 4 and 16 mu g/mL against Cryptococcus neoformans PRL518, C. neoformans ATCC32045 and Aspergillus fumigatus, respectively. Compound 4, at 100 mu g/mL, showed 54% growth inhibition of Thp-1 cell lines.

10a4 `-hydroxyrottlerin10aantifungal10adimeric chalcone10akamalachalcone E10aMallotus philippinensis10arottlerin1 aKulkarni, Roshan, R.1 aTupe, Santosh, G.1 aGample, Suvarna, P.1 aChandgude, Macchindra, G.1 aSarkar, Dhiman1 aDeshpande, Mukund, V.1 aJoshi, Swati, P. uhttps://library.ncl.res.in/content/antifungal-dimeric-chalcone-derivative-kamalachalcone-e-mallotus-philippinensis-001843nas a2200181 4500008004100000245010200041210006900143260000800212520117100220100001801391700002501409700002101434700002301455700002001478700001801498700001901516856012601535 2014 eng d00aAptamer functionalized multifunctional fluorescent nanotheranostic platform for pancreatic cancer0 aAptamer functionalized multifunctional fluorescent nanotheranost cDEC3 aThis study explores the potential of aptamer functionalized and fluorescent silver nanoparticles (AgNPs) labeled human serum albumin nanoparticles for drug delivery and bioimaging. Nanotechnology is certainly the most promising research arena in recent years and different fields of biotechnology, medicine and agricultural have been deeply benefited by the enormous advantages of nanotechnology. In recent years, synthesis of nanoparticles via eco-friendly methods has attained a lot of interest and silver nanoparticles are synthesized extensively due to their size tunable properties and vast applicability in different areas. In this study we have explored green synthesized fluorescent silver nanoparticles as a novel bioimaging agent for pancreatic cancer. Capsaicin, a plant phytochemical found in red chilli pepper was encapsulated in aptamer MUC-1 coupled albumin nanoparticles and it was observed that the nanoformulation significantly enhanced the bioavailability and sustained release property of the drug to pancreatic cancer cells in-vitro. Meanwhile AgNPs mediated excellent bioimaging has enhanced the efficacy of our system as drug delivery vehicle.1 aNigam, Preeti1 aWaghmode, Shobha, A.1 aYeware, Amar, M.1 aNawale, Laxman, U.1 aDagde, Priyanka1 aDudhane, Amol1 aSarkar, Dhiman uhttps://library.ncl.res.in/content/aptamer-functionalized-multifunctional-fluorescent-nanotheranostic-platform-pancreatic01578nas a2200169 4500008004100000245011800041210006900159260000800228300000900236490000700245520095900252100001901211700001901230700001901249700001901268856012101287 2015 eng d00aAnalyzing different acetyl co-a metabolizing enzymes as potential drug targets against mycobacterium tuberculosis0 aAnalyzing different acetyl coa metabolizing enzymes as potential cSEP a1-150 v103 a

Mycobacterium tuberculosis, the causative agent of tuberculosis, is responsible for the deaths of million people around the globe. The scenario is worse than ever due to the emergence of drug resistant strains which are widely spread throughout the globe in much faster ways. To control this worst situation, we need to speed up the search for novel drugs which can specifically kill drug resistant bacteria in collaborative ways amongst academic, clinician and industry. Among different metabolic pathways, fatty acid synthesis pathway has always been a very attractive area for the drug target because of its crucial role during the infection and further in long term survival of pathogen inside the human host. In this review article, we analyzed the role of important and crucial enzymes, which are responsible for the influx and efflux of acetyl co-A substrate, a central hub of metabolites, as potential drug targets against M. tuberculosis.

1 aAkhtar, Shamim1 aSingh, Sheetal1 aKumar, Santosh1 aSarkar, Dhiman uhttps://library.ncl.res.in/content/analyzing-different-acetyl-co-metabolizing-enzymes-potential-drug-targets-against01529nas a2200181 4500008004100000245009000041210006900131260000800200300001000208490000600218520089800224100002901122700002101151700002401172700001901196700002101215856011101236 2015 eng d00aAntimycobacterium activity of coumarins from fruit pulp of aegle marmelos (L.) correa0 aAntimycobacterium activity of coumarins from fruit pulp of aegle cJUL a39-440 v53 a

Phytochemical investigation of n-butanol fraction of acetone extract of Aegle marmelos fruit has afforded four compounds coumarins marmelosin (1), marmin (2) and xanthotoxol (3) and flavonoid kaempferol 3- O-rhamnoside, afzelin (4). All the isolated compounds were evaluated for their antimycobacterium activity against Mycobacterium tuberculosis H37Ra and Mycobacterium bovis. Compounds 1 and 2 exhibited antimycobacterium activity against M. tuberculosis H37Ra with an IC50 12.46 µg/mL and 4.31 µg/mL respectively whereas, at 100 µg/mL, 62.5% and 82.4% growth inhibition of M. bovis was observed respectively. Compounds 1 and 2 were also evaluated against two gram positive bacteria Staphylococcus aureus, Bacillus subtilis and one gram negative bacteria Escherichia coli. Compound 1 at 100 µg/mL, showed growth inhibition, 64.6% and 74.9% of E. coli and B. subtilis respectively.

1 aChinchansure, Ashish, A.1 aShamnani, Neelam1 aArkile, Manisha, A.1 aSarkar, Dhiman1 aJoshi, Swati, P. uhttps://library.ncl.res.in/content/antimycobacterium-activity-coumarins-fruit-pulp-aegle-marmelos-l-correa02007nas a2200181 4500008004100000245012400041210006900165260000800234300001300242490000800255520133400263100001901597700001701616700002301633700001901656700002101675856012901696 2017 eng d00aAnti-proliferative effect of novel primary cetyl alcohol derived sophorolipids against human cervical cancer cells HeLa0 aAntiproliferative effect of novel primary cetyl alcohol derived  cAPR ae01742410 v12 3 aSophorolipids (SLs) are glycolipid biosurfactants that have been shown to display anticancer activity. In the present study, we report anti-proliferative studies on purified forms of novel SLs synthesized using cetyl alcohol as the substrate (referred as SLCA) and their anticancer mechanism in human cervical cancer cells. Antiproliferative effect of column purified SLCA fractions (A, B, C, D, E and F) was examined in panel of human cancer cell lines as well as primary cells. Among these fractions, SLCA B and C significantly inhibited the survival of HeLa and HCT 116 cells without affecting the viability of normal human umbilical vein endothelial cells (HUVEC). The two fractions were identified as cetyl alcohol sophorolipids with non-hydroxylated tail differing in the degree of acetylation on sophorose head group. At an IC50 concentration SLCA B (16.32 mu g ml(-1)) and SLCA C (14.14 mu g ml(-1)) blocked the cell cycle progression of HeLa cells at G1/S phase in time-dependent manner. Moreover, SLCA B and SLCA C induced apoptosis in HeLa cells through an increase in intracellular Ca2+ leading to depolarization of mitochondrial membrane potential and increase in the caspase-3, -8 and -9 activity. All these findings suggest that these SLCAs could be explored for their chemopreventive potential in cervical cancer.1 aNawale, Laxman1 aDubey, Parul1 aChaudhari, Bhushan1 aSarkar, Dhiman1 aPrabhune, Asmita uhttps://library.ncl.res.in/content/anti-proliferative-effect-novel-primary-cetyl-alcohol-derived-sophorolipids-against-human01695nas a2200181 4500008004100000245008700041210006900128260000800197300001200205490000800217520106500225100002301290700001901313700002101332700001901353700002401372856011701396 2018 eng d00aAntibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life0 aAntibacterial and antiTB tatpeptidomimetics with improved effica cMAY a358-3690 v1523 aNon-natural antimicrobial peptides are ideal as next-generation antibiotics because of their ability to circumvent the problems of drug resistance and in vivo instability. We report novel all-alpha- and alpha,gamma-mixed Tat peptide analogues as potential antibacterial and anti-TB agents. These peptides have broad spectrum antibacterial activities against Gram-positive (MICs 0.61 +/- 0.03 to 1.35 +/- 0.21 mu M with the peptide gamma TatM4) and Gram-negative (MICs 0.71 +/- 0.005 to 1.26 +/- 0.02 M with gamma TatM4) bacteria and are also effective against active and dormant forms of Mycobacterium tuberculosis, including strains that are resistant to rifampicin and isoniazid. The introduction of the non-natural amino acids of the study in the Tat peptide analogues results in increased resistance to degradation by proteolysis, significantly increasing their half-life. The peptides appear to inhibit bacteria by a membrane disruption mechanism, and have only a low cytotoxic effect on mammalian cells. (C) 2018 Elsevier Masson SAS. All rights reserved.1 aBhosle, Govind, S.1 aNawale, Laxman1 aYeware, Amar, M.1 aSarkar, Dhiman1 aFernandes, Moneesha uhttps://library.ncl.res.in/content/antibacterial-and-anti-tb-tat-peptidomimetics-improved-efficacy-and-half-life02851nas a2200277 4500008004100000022001400041245013700055210006900192260000800261300001100269490000700280520193000287653002202217653001002239653001502249653002202264653001502286653001002301100002402311700002502335700001902360700002202379700001902401700002202420856013102442 2020 eng d a0946-672X00aAnticancer potential of AgNPs synthesized using acinetobacter sp. and curcuma aromatica against HeLa cell lines: a comparative study0 aAnticancer potential of AgNPs synthesized using acinetobacter sp cDEC a1266300 v623 a

Background: Biogenic nanoparticles are gaining attention due to their low toxicity and numerous biomedical applications. Present study aimed to compare the potential anticancer activity of two biogenic silver nanoparticles (bAgNPs and pAgNPs) against human cervical cancer cell lines (HeLa). Methods: bAgNPs were synthesized using Acinetobacter sp. whereas pAgNPs were synthesized using aqueous root extract of Curcuma aromatica. Effect of these nanoparticles on HeLa cells viability was studied using MTT assay and colony formation assay. Anticancer potential was determined using fluorescence microscopy and flow cytometry studies. Bio-compatibility studies were performed against peripheral blood mononuclear cells (PBMCs). Results: Both the nanoparticles showed 50 % viability of peripheral blood mononuclear cells (PBMCs) when used at high concentration (200 mu g/mL). IC50 for bAgNPs and pAgNPs against HeLa cells were 17.4 and 14 mu g/mL respectively. Colony formation ability of Hela cells was reduced on treatment with both nanoparticles. Acridine orange and ethidium bromide staining demonstrated that bAgNPs were cytostatic whereas pAgNPs were apoptotic. JC-1 dye staining revealed that the mitochondrial membrane potential was affected on treatment with pAgNPs while it remained unchanged on bAgNPs treatment. Flow cytometry confirmed cell cycle arrest in HeLa cells on treatment with nanoparticles further leading to apoptosis in case of pAgNPs. About 77 and 58 % HeLa cells were found in subG1 phase on treatment with bAgNPs and pAgNPs respectively. bAgNPs showed cytostatic effect on HeLa cells arresting the cell growth in subG1 phase, whereas, pAgNPs triggered death of HeLa cells through mitochondrial membrane potential impairment and apoptosis. Conclusion: Overall, bAgNPs and pAgNPs could be safe and showed potential to be used as anticancer nanoantibiotics against human cervical cancer cells.

10aAcinetobacter sp.10aAgNPs10aAnticancer10aCurcuma aromatica10aHeLa cells10aPBMCs1 aNadhe, Shradhda, B.1 aTawre, Madhumita, S.1 aAgrawal, Sonia1 aChopade, Balu, A.1 aSarkar, Dhiman1 aPardesi, Karishma uhttps://library.ncl.res.in/content/anticancer-potential-agnps-synthesized-using-acinetobacter-sp-and-curcuma-aromatica-against02067nas a2200277 4500008004100000022001400041245012300055210006900178260000800247300001400255490000700269520108700276653003101363653003401394653001701428653001701445653002801462100003001490700002401520700002401544700002001568700002401588700001901612700002601631856013201657 2022 eng d a1040-663800aAmide-linked monocarbonyl curcumin analogues: efficient synthesis, antitubercular activity and molecular docking study0 aAmidelinked monocarbonyl curcumin analogues efficient synthesis  cMAY a2655-26710 v453 a

An approach toward the synthesis of novel conjugates of 3,5-bis (arylidene)-4-piperidones (DAP) pharmacophore with amide-linkage has been developed via one-pot multicomponent reaction of aryl aldehydes, piperidinone and 2-chloro-N-phenylacetamide using [Et3NH][HSO4] as a catalyst/medium. Both substitutions on arylidene rings and piperidinone nitrogen (substituted 2-chloro-N-phenylacetamide) were varied. The synthesized conjugates were evaluated for their in vitro antitubercular activity against M. tuberculosis H37Ra (MTB) and M. bovis BCG strains. Among the series, compounds 4f, 4g, 4i and 4j showed remarkable broad spectrum antitubercular activity with low IC50 values. Furthermore, computer docking simulations, for the most active conjugates were performed with the active site of mycobacterial enoyl-acyl carrier protein reductase (InhA) support the antitubercular activity. Lower cytotoxicity, high potency and promising activity against MTB and M. Bovis BCG suggest that amide linked DAP could serve as good leads for further modifications and development.

10aantimycobacterial activity10aBis (arylidene)-4-piperidones10aCytotoxicity10aIonic liquid10aMolecular docking Study1 aSubhedar, Dnyaneshwar, D.1 aShaikh, Mubarak, H.1 aNagargoje, Amol, A.1 aAkolkar, Satish1 aBhansali, Sujit, G.1 aSarkar, Dhiman1 aShingate, Bapurao, B. uhttps://library.ncl.res.in/content/amide-linked-monocarbonyl-curcumin-analogues-efficient-synthesis-antitubercular-activity-and