Synthesis of N-acyl derivatives of Pro-Gly-Pro-Leu peptide: Proteolytic stability in vitro and effects on mouse macrophage cells RAW264.7
- Авторы: Shevchenko K.V.1, Bezuglov V.V.2, Akimov M.G.2, Nagaev I.Y.1, Shevchenko V.P.1, Myasoedov N.F.1
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Учреждения:
- Institute of Molecular Genetics
- Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
- Выпуск: Том 476, № 1 (2017)
- Страницы: 333-336
- Раздел: Biochemistry, Biophysics, and Molecular Biology
- URL: https://journals.rcsi.science/1607-6729/article/view/211992
- DOI: https://doi.org/10.1134/S1607672917050118
- ID: 211992
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Аннотация
Acetyl, oleoyl, arachidonoyl, and docosahexaenoyl derivatives of the Pro-Gly-Pro-Leu peptide with a chemical purity of 99.8% were synthesized. The degradation kinetics of the Pro-Gly-Pro-Leu derivatives under the action of leucine aminopeptidase, nasal mucus, and microsomal fraction of the brain and blood of rats was studied. It was shown that the N-acyl derivatives of Pro-Gly-Pro-Leu proved to be more resistant to the action of leucine aminopeptidase and other enzyme systems. The study of the cytotoxic and anti-inflammatory activity of preparations on the mouse macrophage cell line RAW264.7 showed that acylation with oleic and arachidonic acid makes the peptide cytotoxic with LC50 in the range of 70–15 μM and gives it anti-inflammatory properties with EC50 of 32 and 36 μM, respectively.
Об авторах
K. Shevchenko
Institute of Molecular Genetics
Автор, ответственный за переписку.
Email: ATRegister@mail.ru
Россия, Moscow, 123182
V. Bezuglov
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: ATRegister@mail.ru
Россия, Moscow, 117997
M. Akimov
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: ATRegister@mail.ru
Россия, Moscow, 117997
I. Nagaev
Institute of Molecular Genetics
Email: ATRegister@mail.ru
Россия, Moscow, 123182
V. Shevchenko
Institute of Molecular Genetics
Email: ATRegister@mail.ru
Россия, Moscow, 123182
N. Myasoedov
Institute of Molecular Genetics
Email: ATRegister@mail.ru
Россия, Moscow, 123182
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