Abstract:
:The interaction of a series of amphiphilic 2-alkyl aminoacids (lipoamino acids, LAAs) with different cell cultures and biomembrane models was investigated. LAAs can be useful promoieties to modify the physico-chemical properties of many drugs, and in particular their lipophilicity. Tests were performed in vitro on mammalian cells (murine astrocytes) and human red blood cells (haemolysis), and in vivo on rabbit eye as alternative models to assess the tolerability or the potential damaging effects of these compounds on different biological systems. The mode of interaction of LAAs with pure phospholipid multilamellar liposomes, taken as a biomembrane model, was also analysed by differential scanning calorimetry experiments. Different tolerability/toxicity patterns were obtained in the various models; in particular, the most lipophilic terms of the series, methyl 2-aminohexadecanoate (LAA16), displayed haemolytic activity and toxicity for mouse astrocyte cultures. A specific assay confirmed that LAA16 acted at level of cell membranes, while neither any damaging effects on nucleus or apoptotic induction were observed. The shorter-chain LAAs and the tetradecyl homologue (LAA14) showed the best compatibility with the various cell models.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
Pignatello R,Noce C,Campisi A,Acquaviva R,Bucolo C,Puglisi G,Toth Idoi
10.2174/156720107780362348subject
Has Abstractpub_date
2007-04-01 00:00:00pages
109-21issue
2eissn
1567-2018issn
1875-5704journal_volume
4pub_type
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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更新日期:2017-01-01 00:00:00
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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journal_title:Current drug delivery
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