LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 10 of total 6703

Search options

  1. Article ; Online: Cationic Ester Prodrugs of Curcumin with N,N-dimethyl Amino Acid Promoieties Improved Poor Water Solubility and Intestinal Absorption.

    Hirano-Kusuda, Mariko / Setoguchi, Shuichi / Koga, Mitsuhisa / Goto, Shotaro / Yamada, Ayano / Watase, Daisuke / Nagata-Akaho, Nami / Karube, Yoshiharu / Matsunaga, Kazuhisa / Takata, Jiro

    Pharmaceutical research

    2023  Volume 40, Issue 5, Page(s) 1299–1310

    Abstract: ... solubility. The purpose of this study was to confirm whether cationic N,N-dimethyl amino acid esters of Cur ... could act as prodrugs and improve its water solubility and oral bioavailability.: Methods: Two N,N ... Conclusions: The cationic N,N-dimethyl amino acid ester prodrugs of Cur improved the water solubility of Cur ...

    Abstract Purpose: Although curcumin (Cur) has powerful pharmacological effects, its use in medicine has not been established yet. The oral bioavailability (BA) of Cur is limited because of its poor water solubility. The purpose of this study was to confirm whether cationic N,N-dimethyl amino acid esters of Cur could act as prodrugs and improve its water solubility and oral bioavailability.
    Methods: Two N,N-dimethyl amino acid esters of Cur were synthesized. The hydrolysis profile of the esters was evaluated using rat and human microsomes. A pharmacokinetic study after oral administration of the Cur ester derivatives was performed in rats and compared to the administration of suspended or dissolved Cur formulation. The anti-inflammatory effects of the Cur derivatives were evaluated using macrophage RAW 264.7 stimulated with lipopolysaccharide.
    Results: Cur ester derivatives showed  > 200 mM water solubility. The derivatives were reconverted to the parent compound (Cur) after cleavage of the ester bonds by microsomal esterase, indicating that the compounds could act as Cur prodrugs. The Cur prodrugs enhanced the absolute oral bioavailability of Cur by a 9- and threefold increase of suspended and dissolved Cur administration, respectively, thereby improving intestinal absorption. Cur prodrugs strongly attenuated COX2, iNOS, and ERK phosphorylation.
    Conclusions: The cationic N,N-dimethyl amino acid ester prodrugs of Cur improved the water solubility of Cur and enhanced oral bioavailability in rats. These Cur prodrugs may be good candidates for developing medicinal options previously unavailable due to the poor water solubility and oral BA of Cur.
    MeSH term(s) Rats ; Humans ; Animals ; Curcumin ; Solubility ; Prodrugs/chemistry ; Esters/chemistry ; Amino Acids ; Intestinal Absorption ; Water ; Biological Availability ; Administration, Oral
    Chemical Substances Curcumin (IT942ZTH98) ; Prodrugs ; Esters ; Amino Acids ; Water (059QF0KO0R)
    Language English
    Publishing date 2023-04-20
    Publishing country United States
    Document type Journal Article
    ZDB-ID 843063-9
    ISSN 1573-904X ; 0724-8741 ; 0739-0742
    ISSN (online) 1573-904X
    ISSN 0724-8741 ; 0739-0742
    DOI 10.1007/s11095-023-03500-5
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 1937: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  2. Article ; Online: Organocatalyzed Amine-Free O-Phosphorylation of Alcohols with 4-Methylpyridine N-Oxide.

    Yoshida, Keisuke / Hirano, Wataru / Ota, Ryuuki / Kitagaki, Shinji

    Chemical & pharmaceutical bulletin

    2024  Volume 72, Issue 3, Page(s) 303–308

    Abstract: Amine-free phosphorylation of various alcohols was developed with 4-methylpyridine N-oxide ...

    Abstract Amine-free phosphorylation of various alcohols was developed with 4-methylpyridine N-oxide in the presence of 4 Å molecular sieves at room temperature. This mild method gave various phosphorylated products in high yield and could be applied to acid- or base-sensitive substrates. Furthermore, this method was also effective for the chemoselective phosphorylation of diols or polyols.
    MeSH term(s) Alcohols ; Oxides ; Amines ; Phosphorylation ; Catalysis ; Picolines
    Chemical Substances Alcohols ; Oxides ; 4-methylpyridine (TJD6V9SSO7) ; Amines ; Picolines
    Language English
    Publishing date 2024-03-13
    Publishing country Japan
    Document type Journal Article
    ZDB-ID 213307-6
    ISSN 1347-5223 ; 0009-2363
    ISSN (online) 1347-5223
    ISSN 0009-2363
    DOI 10.1248/cpb.c24-00029
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 770: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  3. Article ; Online: N-acetyl amino acid amide solubility in aqueous 1,6-hexanediol solutions: Insights into the protein droplet deformation mechanism.

    Hirano, Atsushi / Wada, Momoyo / Sato, Takehiro K / Kameda, Tomoshi

    International journal of biological macromolecules

    2024  Volume 261, Issue Pt 1, Page(s) 129724

    Abstract: ... droplet deformation remains unknown. In this study, the solubilities of N-acetyl amino acid amides ...

    Abstract Proteinaceous liquid droplets, generated by liquid-liquid phase separation, function as membraneless compartments that are essential for diverse biological functions. Studies addressing droplet generation have used 1,6-hexanediol (1,6-HD) as a droplet-discerning agent owing to its capacity to induce droplet deformation. Despite the empirical utility of 1,6-HD, the mechanism underlying 1,6-HD-induced droplet deformation remains unknown. In this study, the solubilities of N-acetyl amino acid amides, which correspond to proteinogenic amino acid residues, were examined in the presence of 1,6-HD at 25 °C. Other solvents included ethanol, 1-propanol, and amides. Remarkably, 1,6-HD effectively solubilized hydrophobic species (particularly aromatic species) and exhibited reduced efficacy in solubilizing hydrophilic species and peptide bond moieties. These solubilizing effects are reflected in changes in protein solubility and structure. Specifically, 1,6-HD primarily targets the hydrophobic regions of a protein, increasing protein solubility without causing substantial structural changes. This solubilization mechanism is essential for elucidating the role of 1,6-HD as a droplet-discerning agent and recognizing its potential limitations.
    MeSH term(s) Solubility ; Amino Acids ; Amides/chemistry ; Solvents/chemistry ; Water ; Proteins ; Glycols
    Chemical Substances Amino Acids ; hexamethylene glycol (ZIA319275I) ; Amides ; Solvents ; Water (059QF0KO0R) ; Proteins ; Glycols
    Language English
    Publishing date 2024-01-24
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 282732-3
    ISSN 1879-0003 ; 0141-8130
    ISSN (online) 1879-0003
    ISSN 0141-8130
    DOI 10.1016/j.ijbiomac.2024.129724
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 2374: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  4. Article ; Online: Synaptic N

    Merkurjev, Daria / Hong, Wan-Ting / Iida, Kei / Oomoto, Ikumi / Goldie, Belinda J / Yamaguti, Hitoshi / Ohara, Takayuki / Kawaguchi, Shin-Ya / Hirano, Tomoo / Martin, Kelsey C / Pellegrini, Matteo / Wang, Dan Ohtan

    Nature neuroscience

    2018  Volume 21, Issue 7, Page(s) 1004–1014

    Abstract: A localized transcriptome at the synapse facilitates synapse-, stimulus- and transcript-specific local protein synthesis in response to neuronal activity. While enzyme-mediated mRNA modifications are known to regulate cellular mRNA turnover, the role of ... ...

    Abstract A localized transcriptome at the synapse facilitates synapse-, stimulus- and transcript-specific local protein synthesis in response to neuronal activity. While enzyme-mediated mRNA modifications are known to regulate cellular mRNA turnover, the role of these modifications in regulating synaptic RNA has not been studied. We established low-input m
    MeSH term(s) Adenosine/analogs & derivatives ; Adenosine/genetics ; Adenosine/metabolism ; Animals ; Mice ; Prosencephalon/metabolism ; Synapses/physiology ; Synaptic Transmission/physiology ; Transcriptome
    Chemical Substances N-methyladenosine (CLE6G00625) ; Adenosine (K72T3FS567)
    Language English
    Publishing date 2018-06-27
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1420596-8
    ISSN 1546-1726 ; 1097-6256
    ISSN (online) 1546-1726
    ISSN 1097-6256
    DOI 10.1038/s41593-018-0173-6
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 4891: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)
    Zs.MG 67: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  5. Article ; Online: Practical N-to-C peptide synthesis with minimal protecting groups.

    Tatsumi, Toshifumi / Sasamoto, Koki / Matsumoto, Takuya / Hirano, Ryo / Oikawa, Kazuki / Nakano, Masato / Yoshida, Masaru / Oisaki, Kounosuke / Kanai, Motomu

    Communications chemistry

    2023  Volume 6, Issue 1, Page(s) 231

    Abstract: ... peptide synthesis using chain-elongation from C- to N-terminus is reliable, it produces large quantities ... on the environment. Here we report an alternative N-to-C elongation strategy utilizing catalytic peptide thioacid ... without requiring elaborate condensation reagents and protecting group manipulations. A recyclable N-hydroxy ...

    Abstract Accessible drug modalities have continued to increase in number in recent years. Peptides play a central role as pharmaceuticals and biomaterials in these new drug modalities. Although traditional peptide synthesis using chain-elongation from C- to N-terminus is reliable, it produces large quantities of chemical waste derived from protecting groups and condensation reagents, which place a heavy burden on the environment. Here we report an alternative N-to-C elongation strategy utilizing catalytic peptide thioacid formation and oxidative peptide bond formation with main chain-unprotected amino acids under aerobic conditions. This method is applicable to both iterative peptide couplings and convergent fragment couplings without requiring elaborate condensation reagents and protecting group manipulations. A recyclable N-hydroxy pyridone additive effectively suppresses epimerization at the elongating chain. We demonstrate the practicality of this method by showcasing a straightforward synthesis of the nonapeptide DSIP. This method further opens the door to clean and atom-efficient peptide synthesis.
    Language English
    Publishing date 2023-10-26
    Publishing country England
    Document type Journal Article
    ZDB-ID 2929562-2
    ISSN 2399-3669 ; 2399-3669
    ISSN (online) 2399-3669
    ISSN 2399-3669
    DOI 10.1038/s42004-023-01030-0
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  6. Article ; Online: Combination of Copper Ions and Nucleotide Generates Aggregates from Prion Protein Fragments in the N-Terminal Domain.

    Shiraishi, Noriyuki / Hirano, Yoshiaki

    Protein and peptide letters

    2020  Volume 27, Issue 8, Page(s) 782–792

    Abstract: ... experiment using N-acetylated and Camidated PrP fragments of the N-terminal domain, Octa1, Octa2, Octa3 ...

    Abstract Background: It has been previously found that PrP
    Objective: We aimed to determine the requirements for the formation of these aggregates.
    Methods: In this study, we performed an aggregation experiment using N-acetylated and Camidated PrP fragments of the N-terminal domain, Octa1, Octa2, Octa3, Octa4, PrP
    Results: Among these PrP fragments, Octa4, containing four copper-binding sites, was particularly effective in forming aggregates. We also tested the effect of other pyridine nucleotides and adenine nucleotides on the aggregation of Octa4. ATP was equally effective, but NADH, NADP, ADP, and AMP had no effect.
    Conclusion: The phosphate group on the adenine-linked ribose moiety of adenine nucleotides and pyridine nucleotides is presumed to be essential for the observed effect on aggregation. Efficient aggregation requires the presence of the four octarepeats. These insights may be helpful in the eventual development of therapeutic agents against prion-related disorders.
    MeSH term(s) Copper/chemistry ; Endopeptidase K/chemistry ; Humans ; Peptide Fragments/chemistry ; Prion Proteins/chemistry ; Purine Nucleotides/chemistry
    Chemical Substances Peptide Fragments ; Prion Proteins ; Purine Nucleotides ; Copper (789U1901C5) ; Endopeptidase K (EC 3.4.21.64)
    Language English
    Publishing date 2020-02-24
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1280776-x
    ISSN 1875-5305 ; 0929-8665
    ISSN (online) 1875-5305
    ISSN 0929-8665
    DOI 10.2174/0929866527666200225124829
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 4452: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  7. Article ; Online: Author Correction: Synaptic N

    Merkurjev, Daria / Hong, Wan-Ting / Iida, Kei / Oomoto, Ikumi / Goldie, Belinda J / Yamaguti, Hitoshi / Ohara, Takayuki / Kawaguchi, Shin-Ya / Hirano, Tomoo / Martin, Kelsey C / Pellegrini, Matteo / Wang, Dan Ohtan

    Nature neuroscience

    2018  Volume 21, Issue 10, Page(s) 1493

    Abstract: In the version of this article initially published, a Supplementary Fig. 6f was cited in the last paragraph of the Results. No such panel exists; the citation has been deleted. The error has been corrected in the HTML and PDF versions of the article. ...

    Abstract In the version of this article initially published, a Supplementary Fig. 6f was cited in the last paragraph of the Results. No such panel exists; the citation has been deleted. The error has been corrected in the HTML and PDF versions of the article.
    Language English
    Publishing date 2018-08-07
    Publishing country United States
    Document type Published Erratum
    ZDB-ID 1420596-8
    ISSN 1546-1726 ; 1097-6256
    ISSN (online) 1546-1726
    ISSN 1097-6256
    DOI 10.1038/s41593-018-0219-9
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 4891: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)
    Zs.MG 67: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  8. Article ; Online: Copper-catalyzed amination of arylboronates with N,N-dialkylhydroxylamines.

    Matsuda, Naoki / Hirano, Koji / Satoh, Tetsuya / Miura, Masahiro

    Angewandte Chemie (International ed. in English)

    2012  Volume 51, Issue 15, Page(s) 3642–3645

    MeSH term(s) Amination ; Aniline Compounds/chemical synthesis ; Boronic Acids/chemistry ; Catalysis ; Copper/chemistry ; Hydroxylamines/chemistry
    Chemical Substances Aniline Compounds ; Boronic Acids ; Hydroxylamines ; Copper (789U1901C5)
    Language English
    Publishing date 2012-04-10
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.201108773
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  9. Article ; Online: Practical N-to-C peptide synthesis with minimal protecting groups

    Toshifumi Tatsumi / Koki Sasamoto / Takuya Matsumoto / Ryo Hirano / Kazuki Oikawa / Masato Nakano / Masaru Yoshida / Kounosuke Oisaki / Motomu Kanai

    Communications Chemistry, Vol 6, Iss 1, Pp 1-

    2023  Volume 10

    Abstract: ... Although traditional peptide synthesis using chain-elongation from C- to N-terminus is reliable, it produces large ... burden on the environment. Here we report an alternative N-to-C elongation strategy utilizing catalytic ... A recyclable N-hydroxy pyridone additive effectively suppresses epimerization at the elongating chain ...

    Abstract Abstract Accessible drug modalities have continued to increase in number in recent years. Peptides play a central role as pharmaceuticals and biomaterials in these new drug modalities. Although traditional peptide synthesis using chain-elongation from C- to N-terminus is reliable, it produces large quantities of chemical waste derived from protecting groups and condensation reagents, which place a heavy burden on the environment. Here we report an alternative N-to-C elongation strategy utilizing catalytic peptide thioacid formation and oxidative peptide bond formation with main chain-unprotected amino acids under aerobic conditions. This method is applicable to both iterative peptide couplings and convergent fragment couplings without requiring elaborate condensation reagents and protecting group manipulations. A recyclable N-hydroxy pyridone additive effectively suppresses epimerization at the elongating chain. We demonstrate the practicality of this method by showcasing a straightforward synthesis of the nonapeptide DSIP. This method further opens the door to clean and atom-efficient peptide synthesis.
    Keywords Chemistry ; QD1-999
    Subject code 540
    Language English
    Publishing date 2023-10-01T00:00:00Z
    Publisher Nature Portfolio
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

    More links

    Kategorien

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  10. Article ; Online: Role of the N- and C-terminal regions of FliF, the MS ring component in

    Kojima, Seiji / Kajino, Hiroki / Hirano, Keiichi / Inoue, Yuna / Terashima, Hiroyuki / Homma, Michio

    Journal of bacteriology

    2021  Volume 203, Issue 9

    Abstract: ... of a large periplasmic region and two transmembrane segments connected to the N- and C-terminal regions ...

    Abstract The MS ring is a part of the flagellar basal body and formed by 34 subunits of FliF, which consists of a large periplasmic region and two transmembrane segments connected to the N- and C-terminal regions facing the cytoplasm. A cytoplasmic protein, FlhF, which determines the position and number of the basal body, supports MS ring formation in the membrane in
    Language English
    Publishing date 2021-02-22
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2968-3
    ISSN 1098-5530 ; 0021-9193
    ISSN (online) 1098-5530
    ISSN 0021-9193
    DOI 10.1128/JB.00009-21
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Ud II Zs.50: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top