Publications by authors named "Tse-Kai Fu"

3 Publications

  • Page 1 of 1

Synthesis of α-1,2- and α-1,3-linked di-rhamnolipids for biological studies.

Carbohydr Res 2020 Oct 25;496:108102. Epub 2020 Jul 25.

Department of Pharmaceutical Chemistry, University of Debrecen, H-4032, Debrecen, Egyetem tér 1, Hungary. Electronic address:

For a detailed examination of the interaction of rhamnose containing derivatives with recombinant horseshoe crab plasma lectin (rHPL), two di-rhamno-di-lipids (an α-1,2- and an α-1,3-linked) were synthesized via a new simple method. The N-iodosuccinimide/triflic acid mediated glycosylation of the methyl (R)-3-hydroxydecanoate with phenyl-1-thio-rhamnobioside donors afforded the mono-lipid disaccharides. Removal of the methyl ester group followed by esterification of the mono-lipids with a second (R)-3-hydroxydecanoate unit resulted in fully protected di-lipid derivatives, transformation of which into the target compounds was accomplished in two steps. This method allows the synthesis of both regioisomers in only 6 steps starting from the corresponding free disaccharides. Both synthetic di-rhamnolipids were biologically active for lectin binding differential binding preference between two isomeric di-rhamno-di-lipids. The rHPL lectin favours the α-1,3-linked di-rhamno-di-lipids over its α-1,2-linked regioisomer.
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http://dx.doi.org/10.1016/j.carres.2020.108102DOI Listing
October 2020

Cell Penetrating Peptide as a High Safety Anti-Inflammation Ingredient for Cosmetic Applications.

Biomolecules 2020 01 7;10(1). Epub 2020 Jan 7.

Institute of Molecular and Cellular Biology, National Tsing Hua University, Hsinchu 30013, Taiwan.

Cosmeceutical peptides have become an important topic in recent decades in both academic and industrial fields. Many natural or synthetic peptides with different biological functions including anti-ageing, anti-oxidation, anti-infection and anti-pigmentation have been developed and commercialized. Current cosmeceutical peptides have already satisfied most market demand, remaining: "cargos carrying skin penetrating peptide with high safety" still an un-met need. To this aim, a cell-penetrating peptide, CPP, which efficiently transported cargos into epithelial cells was exanimated. CPP was evaluated with cell model and 3D skin model following OECD guidelines without using animal models. As a highly stable peptide, CPP neither irritated nor sensitized skin, also did not disrupt skin barrier. In addition, such high safety peptide had anti-inflammation activity without allergic effect. Moreover, cargo carrying activity of CPP was assayed using HaCaT cell model and rapid CPP penetration was observed within 30 min. Finally, CPP possessed transepidermal activity in water in oil formulation without disruption of skin barrier. All evidences indicated that CPP was an ideal choice for skin penetrating and its anti-inflammatory activity could improve skin condition, which made CPP suitable and attractive for novel cosmeceutical product development.
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http://dx.doi.org/10.3390/biom10010101DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7023394PMC
January 2020

Rhamnose Binding Protein as an Anti-Bacterial Agent-Targeting Biofilm of .

Mar Drugs 2019 Jun 14;17(6). Epub 2019 Jun 14.

Institute of Molecular and Cellular Biology, National Tsing Hua University, Hsinchu 30013, Taiwan.

More than 80% of infectious bacteria form biofilm, which is a bacterial cell community surrounded by secreted polysaccharides, proteins and glycolipids. Such bacterial superstructure increases resistance to antimicrobials and host defenses. Thus, to control these biofilm-forming pathogenic bacteria requires antimicrobial agents with novel mechanisms or properties. , a Gram-negative opportunistic nosocomial pathogen, is a model strain to study biofilm development and correlation between biofilm formation and infection. In this study, a recombinant hemolymph plasma lectin (rHPL) cloned from Taiwanese was expressed in an system. This rHPL was shown to have the following properties: (1) Binding to PA14 biofilm through a unique molecular interaction with rhamnose-containing moieties on bacteria, leading to reduction of extracellular di-rhamnolipid (a biofilm regulator); (2) decreasing downstream quorum sensing factors, and inhibiting biofilm formation; (3) dispersing the mature biofilm of PA14 to improve the efficacies of antibiotics; (4) reducing PA14 cytotoxicity to human lung epithelial cells in vitro and (5) inhibiting PA14 infection of zebrafish embryos in vivo. Taken together, rHPL serves as an anti-biofilm agent with a novel mechanism of recognizing rhamnose moieties in lipopolysaccharides, di-rhamnolipid and structural polysaccharides (Psl) in biofilms. Thus rHPL links glycan-recognition to novel anti-biofilm strategies against pathogenic bacteria.
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http://dx.doi.org/10.3390/md17060355DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6628293PMC
June 2019