- Synthesis, characterization, and saccharide binding studies of bile acid - Porphyrin conjugates
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Synthesis and characterization of bile acid-porphyrin conjugates (BAPs) are reported. Binding of saccharides with BAPs in aqueous methanol was studied by monitoring changes in the visible absorption spectral of the porphyrin-moieties. Although these studi
- Koivukorpi, Juha,Sievaenen, Elina,Kolehmainen, Erkki,Kral, Vladimir
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- ANTI-CANCER AGENT LOADED HYDROPHOBIC BILE ACID CONJUGATED HYDROPHILIC CHITOSAN OLIGOSACCHARIDE NANOPARTICLES AND PREPARATION METHOD THEREOF
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Disclosed herein are hydrophobic bile acid- conjugated hydrophilic chitosan oligosaccharide nanoparticles with anticancer agent loaded therein and a method for preparing the same. The hydrophobic bile acid- conjugated hydrophilic chitosan oligosaccharide nanoparticles form self-aggregates in aqueous phases. With a high load of anticancer agents, the hydrophobic bile acid-conjugated chitosan oligosaccharide nanoparticles with anticancer agents loaded therein exhibit excellent cytotoxicity against cancer cells. Also, the nanoparticles release the anticancer agent in a sustained manner therefrom, thereby exhibiting anticancer activity for a prolong period of time. Therefore, the nanoparticles are very useful in cancer chemotherapy.
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Page/Page column 25-26
(2008/06/13)
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- SOLUBLE STEROIDAL PEPTIDES FOR NUCLEIC ACID DELIVERY
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Amphiphilic lipopeptide compositions for gene delivery are disclosed. An illustrative amphiphilic lipopeptide composition includes a human protamine 2 peptide conjugated to a hydrophobic moiety. Illustrative hydrophobic moieties include sterols, bile acid
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Page/Page column 4
(2010/02/10)
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- Antimicrobial activities of squalamine mimics
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We investigated the antimicrobial properties of compounds with structural features that were designed to mimic those of squalamine, an antibiotic isolated from the stomach of the dogfish shark. The mimics, like squalamine, are sterol-polyamine conjugates. Unlike squalamine, the mimics were simple to prepare, at high yield, from readily available starting materials. Several squalamine mimics showed activity against gram-negative rods, gram-positive cocci including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and fungi. Some had little or no hemolytic activity. The hydrophobicity of the sterol backbone and the length and the cationic charge of the side chains appeared to be critical determinants of activity. One of the squalamine mimics, SM-7, was bactericidal against Escherichia coli, Pseudomonas aeruginosa, and S. aureus; its activity was decreased by divalent or monovalent cations and by bovine serum albumin. Subinhibitory concentrations of SM-7 markedly enhanced the antimicrobial activity of rifampin against gram-negative rods. These results suggest that the compounds may disrupt an outer membrane of gram-negative rods. Squalamine mimics are a new class of broad-spectrum antimicrobial agents. The antagonism of their activity by serum and albumin and their hemolytic properties may limit their use as systemic agents. The squalamine mimics, because of their potencies, broad spectra of antimicrobial activity, and potential for systemic toxicity, appear to be good candidates for development as topical antimicrobial agents.
- Kikuchi, Ken,Bernard, Edward M.,Sadownik, Andrzej,Regen, Steven L.,Armstrong, Donald
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p. 1433 - 1438
(2007/10/03)
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