01956nas a2200205 4500008004100000022001400041245009600055210006900151260008800220300001200308490000700320520116600327100002201493700001801515700002001533700002701553700002001580700002901600856012101629 2011 eng d a1044-549800aEnhanced DNA binding of 9-omega-amino alkyl ether analogs from the plant alkaloid berberine0 aEnhanced DNA binding of 9omegaamino alkyl ether analogs from the a140 HUGUENOT STREET, 3RD FL, NEW ROCHELLE, NY 10801 USAbMARY ANN LIEBERT, INCcFEB a123-1330 v303 a

To understand the structure-activity relationship of isoquinoline alkaloids, absorption, fluorescence, circular dichroism, and thermodynamics were employed to study the interaction of five C-9-omega-amino alkyl ether analogs from the plant alkaloid berberine with double-stranded calf thymus DNA. The C-9 derivatization resulted in dramatic enhancements in the fluorescence emission of these compounds. The most remarkable changes in the spectral and binding properties were in the BC4 and BC5 derivatives. Interactions of these analogs, which have an additional recognition motif with DNA, were evaluated through different spectroscopic and calorimetric titration experiments. The analogs remarkably enhanced the DNA binding affinity and the same was directly dependent on the alkyl chain length. The analog with six alkyl chains enhanced the DNA binding affinity by about 33 times compared with berberine. The binding became more entropically driven with increasing chain length. These results may be of potential use in the design of berberine derivatives and understanding of the structure-activity relationship for improved therapeutic applications.

1 aIslam, Md, Maidul1 aBasu, Anirban1 aHossain, Maidul1 aSureshkumar, Gopalsamy1 aHotha, Srinivas1 aKumar, Gopinatha, Suresh uhttps://library.ncl.res.in/content/enhanced-dna-binding-9-omega-amino-alkyl-ether-analogs-plant-alkaloid-berberine-001357nas a2200253 4500008004100000022001400041245013200055210006900187260007100256300001400327490000600341520041500347653003300762653002200795653002000817653001700837653002000854100002400874700002400898700002100922700001800943700002100961856012100982 2015 eng d a1948-587500aTotal syntheses and biological evaluation of (+/-)-botryosphaeridione, (+/-)-pleodendione, 4-epi-periconianone B, and analogues0 aTotal syntheses and biological evaluation of botryosphaeridione  a1155 16TH ST, NW, WASHINGTON, DC 20036 USAbAMER CHEMICAL SOCcNOV a1117-11210 v63 a

The total syntheses of (+/-)-botryosphaeridione, (+/-)-pleodendione, (+/-)-hoaensieremodione, 4-epi-periconianone B, and their analogues have been accomplished for the first time. All the synthesized target compounds were screened in neural anti-inflammatory assays using LPS induced microglia cells (N9). Among them, compounds 1 and 21 were identified as potential lead compounds for further profiling.

10aantineuroinflammatoty agents10abohyosphaeridione10aNatural product10apleodendione10aTotal synthesis1 aHandore, Kishor, L.1 aJadhav, Prakash, D.1 aHazra, Bibhabasu1 aBasu, Anirban1 aReddy, Srinivasa uhttps://library.ncl.res.in/content/total-syntheses-and-biological-evaluation-botryosphaeridione-pleodendione-4-epi-002000nas a2200193 4500008004100000245011000041210006900151260000800220300001100228490000800239520128500247100003101532700002701563700002701590700002101617700001801638700002101656856012901677 2017 eng d00aIdentification of new anti-inflammatory agents based on nitrosporeusine natural products of marine origin0 aIdentification of new antiinflammatory agents based on nitrospor cJUL a89-1090 v1353 aNitrosporeusines A and B are two recently isolated marine natural products with novel skeleton and exceptional biological profile. Interesting antiviral activity of nitrosporeusines and promising potential in curing various diseases, evident from positive data from various animal models, led us to investigate their anti-inflammatory potential. Accordingly, we planned and synthesized nitrosporeusines A and B in racemic as well as enantiopure forms. The natural product synthesis was followed by preparation of several analogues, and all the synthesized compounds were evaluated for in vitro and in vivo anti-inflammatory potential. Among them, compounds 25, 29 and 40 significantly reduced levels of nitric oxide (NO), reactive oxygen species (ROS) and pro-inflammatory cytokines. In addition, these compounds suppressed several pro-inflammatory mediators including inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), nuclear factor-kappa B (NF -kappa B), and thereby can be emerged as potent anti-inflammatory compounds. Furthermore, all possible isomers of lead compound 25 were synthesized, characterized and profiled in same set of assays and found that one of the enantiomer (-)-25a was superior among them. (C) 2017 Elsevier Masson SAS. All rights reserved.1 aPhilkhana, Satish, Chandra1 aVerma, Abhishek, Kumar1 aJachak, Gorakhnath, R.1 aHazra, Bibhabasu1 aBasu, Anirban1 aReddy, Srinivasa uhttps://library.ncl.res.in/content/identification-new-anti-inflammatory-agents-based-nitrosporeusine-natural-products-marine02161nas a2200193 4500008004100000022001400041245013700055210006900192260000800261490000700269520141000276100002701686700002701713700002701740700003101767700002101798700001801819856013001837 2018 eng d a1935-273500a Nitrosporeusine analogue ameliorates Chandipura virus induced inflammatory response in CNS via NF kappa b inactivation in microglia0 aNitrosporeusine analogue ameliorates Chandipura virus induced in cJUL0 v123 aChandipura Virus (CHPV), a negative-stranded RNA virus belonging to the Rhabdoviridae family, has been previously reported to bring neuronal apoptosis by activating several factors leading to neurodegeneration. Following virus infection of the central nervous system, microglia, the ontogenetic and functional equivalents of macrophages in somatic tissues gets activated and starts secreting chemokines, thereby recruiting peripheral leukocytes into the brain parenchyma. In the present study, we have systemically examined the effect of CHPV on microglia and the activation of cellular signalling pathways leading to chemokine expression upon CHPV infection. Protein and mRNA expression profiles of chemokine genes revealed that CHPV infection strongly induces the expression of CXC chemokine ligand 10 (CXCL10) and CC chemokine ligand 5 (CCL5) in microglia. CHPV infection triggered the activation of signalling pathways mediated by mitogen-activated protein kinases, including p38, JNK 1 and 2, and nuclear factor kappa B (NF-kappaB). CHPV-induced expression of CXCL10 and CCL5 was achieved by the activation of p38 and NF-kappaB pathways. Considering the important role of inflammation in neurodegeneration, we have targeted NF-kappaB using a newly synthesised natural product nitrosporeusine analogue and showed incapability of microglial supernatant of inducing apoptosis in neurons after treatment.1 aVerma, Abhishek, Kumar1 aWaghmare, Trushnal, S.1 aJachak, Gorakhnath, R.1 aPhilkhana, Satish, Chandra1 aReddy, Srinivasa1 aBasu, Anirban uhttps://library.ncl.res.in/content/nitrosporeusine-analogue-ameliorates-chandipura-virus-induced-inflammatory-response-cns-nf01626nas a2200289 4500008004100000022001400041245010400055210006900159260000900228300001400237520066700251653001000918653002200928653002600950653001700976653001600993653002001009100002501029700002101054700002401075700002501099700002101124700002701145700001801172700002101190856012501211 2019 eng d a1434-193X00aNeural anti-inflammatory natural product periconianone A: total synthesis and biological evaluation0 aNeural antiinflammatory natural product periconianone A total sy cAPR  a2376-23813 a

Total synthesis of periconianone A, an eremophilane-type sesquiterpenoid with impressive neural anti-inflammatory potential, has been accomplished. Diels-Alder/aldol strategy to construct tetrahydro-naphthalene-2,6-dione scaffold, allylic oxidation of dienone using DBU/O-2 and postulated biomimetic aldol reaction to construct 6/6/6 tricyclic system are the highlights of the present synthesis. Furthermore, the synthesized (+/-)-periconianone A and two close analogs were tested for their neural anti-inflammatory activity using various assays. In the course of our study we found a structurally simplified analog is superior to (+/-)-periconianone A.

10aAldol10aAllylic oxidation10aBiological evaluation10aCytotoxicity10aDiels-Alder10aPericonianone A1 aKalmode, Hanuman, P.1 aPatil, Suhag, S.1 aHandore, Kishor, L.1 aAthawale, Paresh, R.1 aDandela, Rambabu1 aVerma, Abhishek, Kumar1 aBasu, Anirban1 aReddy, Srinivasa uhttps://library.ncl.res.in/content/neural-anti-inflammatory-natural-product-periconianone-total-synthesis-and-biological