Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A2 activity
Publication: Research - peer-review › Journal article – Annual report year: 2012
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Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A2 activity. / Pedersen, Palle Jacob; Viart, Helene Marie-France; Melander, Fredrik; Andresen, Thomas Lars; Madsen, Robert; Clausen, Mads Hartvig.
In: Bioorganic & Medicinal Chemistry, Vol. 20, No. 13, 2012, p. 3972-3978.Publication: Research - peer-review › Journal article – Annual report year: 2012
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TY - JOUR
T1 - Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A<sub>2 </sub>activity
A1 - Pedersen,Palle Jacob
A1 - Viart,Helene Marie-France
A1 - Melander,Fredrik
A1 - Andresen,Thomas Lars
A1 - Madsen,Robert
A1 - Clausen,Mads Hartvig
AU - Pedersen,Palle Jacob
AU - Viart,Helene Marie-France
AU - Melander,Fredrik
AU - Andresen,Thomas Lars
AU - Madsen,Robert
AU - Clausen,Mads Hartvig
PB - Pergamon
PY - 2012
Y1 - 2012
N2 - Tocopheryl succinates (TOSs) are, in contrast to tocopherols, highly cytotoxic against many cancer cells. In this study the enzyme activity of secretory phospholipase A2 towards various succinate-phospholipid conjugates has been investigated. The synthesis of six novel phospholipids is described, including two TOS phospholipids conjugates. The studies revealed that the TOS conjugates are poor substrates for the enzyme whereas the phospholipids with alkyl and phenyl succinate moieties were hydrolyzed by the enzyme to a high extent.
AB - Tocopheryl succinates (TOSs) are, in contrast to tocopherols, highly cytotoxic against many cancer cells. In this study the enzyme activity of secretory phospholipase A2 towards various succinate-phospholipid conjugates has been investigated. The synthesis of six novel phospholipids is described, including two TOS phospholipids conjugates. The studies revealed that the TOS conjugates are poor substrates for the enzyme whereas the phospholipids with alkyl and phenyl succinate moieties were hydrolyzed by the enzyme to a high extent.
KW - Drug delivery
KW - Liposomes
KW - Vitamin E
KW - Phospholipase
U2 - 10.1016/j.bmc.2012.05.024
DO - 10.1016/j.bmc.2012.05.024
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
SN - 0968-0896
IS - 13
VL - 20
SP - 3972
EP - 3978
ER -