Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A2 activity

Palle Jacob Pedersen; Helene Marie-France Viart; Fredrik Melander; Thomas Lars Andresen; Robert Madsen; Mads Hartvig Clausen

doi:10.1016/j.bmc.2012.05.024

Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A₂activity

Palle Jacob Pedersen
, Helene Marie-France Viart
, Fredrik Melander
, Thomas Lars Andresen
, Robert Madsen
, Mads Hartvig Clausen

Research output: Contribution to journal › Journal article › Research › peer-review

Abstract

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.

Original language	English
Journal	Bioorganic & Medicinal Chemistry
Volume	20
Issue number	13
Pages (from-to)	3972-3978
ISSN	0968-0896
DOIs	https://doi.org/10.1016/j.bmc.2012.05.024
Publication status	Published - 2012

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Drug delivery
Liposomes
Vitamin E
Phospholipase

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10.1016/j.bmc.2012.05.024

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Cite this

@article{9e039b32a0fd48229be36b34a411adc8,

title = "Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A2 activity",

abstract = "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.",

keywords = "Drug delivery, Liposomes, Vitamin E, Phospholipase",

author = "Pedersen, \{Palle Jacob\} and Viart, \{Helene Marie-France\} and Fredrik Melander and Andresen, \{Thomas Lars\} and Robert Madsen and Clausen, \{Mads Hartvig\}",

year = "2012",

doi = "10.1016/j.bmc.2012.05.024",

language = "English",

volume = "20",

pages = "3972--3978",

journal = "Bioorganic \& Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier",

number = "13",

}

TY - JOUR

T1 - Synthesis of tocopheryl succinate phospholipid conjugates and monitoring of phospholipase A2 activity

AU - Pedersen, Palle Jacob

AU - Viart, Helene Marie-France

AU - Melander, Fredrik

AU - Andresen, Thomas Lars

AU - Madsen, Robert

AU - Clausen, Mads Hartvig

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

M3 - Journal article

SN - 0968-0896

VL - 20

SP - 3972

EP - 3978

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 13

ER -