- The effect of unsaturation on the formation of self-assembled gels from fatty acid L-serine amides and their cytotoxicity towards caco-2 cancer cells
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A series of saturated and unsaturated fatty acid l-serines 3 were synthesized and their ability to form self-assembled gels was investigated. The saturated (lauroyl 3a and steraoyl 3b) and monounsaturated (oleoyl 3c) fatty acid l-serines form gels in both water and organic solvent, whereas the diunsaturated linoleyl-l-serine 3d does not form gels in these solvents, indicating that unsaturation adversely affects the gelation process. Cytotoxicity studies on these compounds with Caco-2 cancer cells in vitro show that these gels are only moderately cytotoxic at concentrations up to 0.5 mM, making them a promising candidate for applications such as drug delivery. CSIRO 2009.
- Lim, Li Yun Grace,Su, Yingying,Braet, Filip,Thordarson, Pall
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Read Online
- N-Linoleyltyrosine protects against transient cerebral ischemia in gerbil via CB2 receptor involvement in PI3K/Akt signaling pathway
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Anandamide (AEA) played potent neuroprotective activities via cannabinoid type 1 (CB1) and 2 (CB2) receptor. N-Linoleyltyrosine (NITyr), as an AEA analogue, was synthesized in our laboratory and evaluated the neuroprotective effects and mechanisms for the
- Cheng, Lin,Li, Jinsi,Zhou, Yi,Zheng, Qixue,Ming, Xin,Liu, Sha
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Read Online
- CARRIERS FOR EFFICIENT NUCLEIC ACID DELIVERY
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Nanoparticle compositions for delivery of nucleic acids to subjects including carriers comprising polyester (PE) dendrimers or dendrons, and therapeutic or immunogenic nucleic acid agents enclosed within the PE are described. Methods for treating or preve
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Paragraph 00157
(2021/10/15)
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- Preparation method and application of compound with beta amyloid protein resisting activity
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The present invention provides a compound represented by formula I, or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method of the compound. Experimental results show that the compound is suitable for industrial pro
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Page/Page column 9
(2019/12/29)
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- PERSONAL CARE COMPOSITIONS COMPRISING FATTY ACID AMIDE DERIVATIVES
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In one embodiment, the present invention provides a personal care composition, comprising: (i) a compound of Formula (1) at a concentration from 0.0001 wt % to 20 wt % of the composition; wherein R is selected from the group consisting of C15-C23 conjugated dienes, C15-C23 hydroxylated mono unsaturated alkenes, and C15-C23 hydroxylated alkanes; wherein R1 is selected from the group consisting of H, C1-C4 alkyl, - CH2OH, -CH2(CH3)-OH,-[CH2]4-NH2, -CH2-CO2H, -[CH2]2-CO2H, (I), (II) and (III); wherein R3 is -CO2H; -CH2CO2H; -CH2CH2CO2H;; and (ii) a cosmetically acceptable carrier.
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Page/Page column 48-49
(2018/02/28)
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- Α - galactose ceramide new isomer and its synthetic method
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The invention provides an alpha-galactosyl ceramide new isomer and its synthetic method. Configuration of sphingosine chain is changed to 4,5-cis double bond sphingosine chain. According to the invention, reaction steps are shortened, yield is raised, and aftertreatment and purification steps are omitted. The synthetic method can be used for total synthesis of similar glycosyl ceramide and satisfies wide range of development, research and application of different glycosyl ceramide.
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Paragraph 0065; 0066
(2017/10/31)
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- 4,5-Cis Unsaturated α-GalCer Analogues Distinctly Lead to CD1d-Mediated Th1-Biased NKT Cell Responses
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The total synthesis of 4,5-cis unsaturated α-GalCer analogues was achieved, and their immune-response altering activity was assessed in vitro as well as in vivo in mice. Using glycosyl iodide as a glycosyl donor, construction of the sphingosine unit was shortened by four steps and single α-stereoselectivity was achieved in good yield (67%). With regard to the therapeutic use of α-GalCer, the novel analogues (1b and 1c) distinctly induced a Th1-biased cytokine response, avoiding induction of a contradictory response and overstimulation.
- Cui, Yanli,Li, Zhiyuan,Cheng, Zhaodong,Xia, Chengfeng,Zhang, Yongmin
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p. 1209 - 1215
(2015/06/25)
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- Unsaturated acyl chains dramatically enhanced cellular uptake by direct translocation of a minimalist oligo-arginine lipopeptide
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The recurring issue with cell penetrating peptides is how to increase direct translocation vs. endocytosis, to avoid premature degradation. Acylation by a cis unsaturated chain (C22:6) of a short cationic peptide provides a new rational design to favour diffuse cytosolic and dense Golgi localisations.
- Swiecicki,Di Pisa,Lippi,Chwetzoff,Mansuy,Trugnan,Chassaing,Lavielle,Burlina
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supporting information
p. 14656 - 14659
(2015/09/28)
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- COMPOUNDS AND METHODS OF TREATING OBESITY
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The present invention relates to novel fatty acid derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as agents for the treatment of obesity and related disorders, and for improving cognition.
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Page/Page column 59-60
(2009/10/22)
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- Chemoselective acylation of fully deprotected hydrazino acetyl peptides. Application to the synthesis of lipopeptides
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Fully deprotected N-terminal α-hydrazino acetyl peptides were synthesized and chemoselectively acylated on the hydrazine moiety with various fatty acid succinimidyl esters or N-(cholesterylcarbonyloxy) succinimide to give lipopeptides of high purity. The buffer and pH were adjusted in order to minimize the oxidation of the hydrazine moiety and to achieve the best conversion and selectivity. The acylation was performed in a citrate - Phosphate buffer/2-methylpropan-2-ol mixture of pH 5.1. The pKa of the α-hydrazino acetyl group on our model peptide was found to be 6.45, i.e., about 2 units lower than the pKa of a glycyl residue. The reaction was subsequently applied to the synthesis of a 38AA peptide derivatized by a palmitoyl group.
- Bonnet,Ollivier,Gras-Masse,Melnyk
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p. 443 - 449
(2007/10/03)
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- Synthesis and Biological Activities of N-Acetylglucosaminyl-&β(1->4)-N-Acetylmuramyl Tri- and Tetrapeptide Derivatives
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The acylated, amidated and esterified derivatives of N-acetylglucosaminyl-β(1->4)-N-acetylmuramyl tri- and tetrapeptide were synthesized and examined as to their protective effect on pseudomonal infection in the mouse and pyrogenicity in the rabbit.Modifications of the terminal end function of the peptide moieties in their molecules caused enhancement of resistance to pseudomonal infection and reduction of pyrogenicity.Among the compounds tested, sodium N-acetylglucosaminyl-β(1->4)-N-acetylmuramyl-L-alanyl-D-isoglutaminyl-(L)-stearoyl-(D)-meso-2,6-diaminopimelic acid-(D)-amide and sodium N-acetylglucosaminyl-β(1->4)-N-acetylmuramyl-L-alanyl-D-isoglutaminyl-(L)-stearoyl-(D)-meso-2,6-diaminopimelic acid-(D)-amide-(L)-D-alanine were found to be advantageous and conceivably worthwhile for further investigation as immunobiologically active compounds.
- Furuta, Rhyuji,Kawata, Shigeo,Naruto, Shunsuke,Minami, Akira,Kotani, Shozo
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p. 2561 - 2572
(2007/10/02)
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