Степень Проникновения Тиролиберина В Кровь И Отделы Головного Мозга При Интраназальном Или Внутривенном Введении

Шевченко, К. В.; Вьюнова, Т. В.; Радилов, А. С.; Андреева, Л. А.; Нагаев, И. Ю.; Шевченко, В. П.; Рембовский, В. Р.; Мясоедов, Н. Ф.

doi:10.7868/s0869565215360268

Cited by 3 publications

(2 citation statements)

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“…Получены новые данные, касающиеся фармакодинамики H-Pyr-His-Pro-NH 2 и его взаимодействия с другими фармакологически активными пептидами. Эти результаты помогут оптимизировать способы его доставки в целевые ткани для достижения наиболее сильного и пролонгированного действия [16,17].…”

Section: Introductionunclassified

Oxoprolinic short peptides – potential pharmacological means of hypolidemic and antitrombotic actions

Lyapina

et al. 2017

BIOMED KHIM

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One of the most urgent and important tasks of modern biological and medical research is the search and research of pharmacological agents that combine lipid-lowering and antithrombotic effects in the organism. The unique effects of the regulatory peptides of the oxoproline series (5-oхo-Pro-His-Pro-NH2, 5-oxo-Pro-Trp-Pro and 5-oxo-Pro-Arg-Pro or 5-oхo-Pro-His-Pro-NH2, Pyr-Trp-Pro and Pyr-Arg-Pro) have been found in rats with hypercholesterolemia (metabolic syndrome). Multiple intranasal of these peptides to animals with developed hypercholesterolemia increased anticoagulant, fibrinolytic and antiplatelet potential of the blood and simultaneously lowered increased concentrations of total cholesterol, low-density lipoprotein cholesterol and triglycerides. In addition, they contributed to the normalization of blood glucose levels. A week after the last admistration of these peptides, the hypocholesterolemic, normoglycemic and anticoagulant effects persisted. The relationship between the structure of peptides of the oxoproline series and their functional properties is discussed. A conclusion is made about the prospects of further studies of oxoproline peptides as drugs that combine antithrombotic effects with the improvement of fat metabolism in the body.

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Section: Introductionunclassified

Oxoprolinic short peptides – potential pharmacological means of hypolidemic and antitrombotic actions

Lyapina

et al. 2017

BIOMED KHIM

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“…Сначала, при интраназальном введении пептида, из-за диффузии 5-охо-Pro-Arg-Pro и продуктов его деградации из носовой полости крыс в кровоток радиоактивность проб в крови крыс растёт. [52,53] Перед определением включения 5-охо-Pro-His-ProNH 2 в различные органы и ткани организма, как и в предыдущих случаях, оценивали деградацию 5-охо-Pro-His-ProNH 2 за счёт гидролиза и за счёт разрушения аминокислотных остатков в пептиде и его метаболитах. Определяли радиоактивность проб из крови и мозга крыс до и после упаривания экстрактов, полученных при интраназальном и внутривенном введении 5-охо-Pro-His-ProNH 2 .…”

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Stability of prolin-containing peptides in biological media

et al. 2019

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New data on peptide drugs have been summarized; their high stability is due to both the introduction of Pro-Gly-Pro in various amino acid sequences and the modification of the glyproline fragment itself. Pro-Gly-Pro-Leu, ACTH(6-9)Pro-Gly-Pro, 5-oxo-Pro-Arg-Pro and 5-oxo-Pro-His-Pro-NH2 were used as proline-containing peptides. Tritiated peptides were obtained: Pro-Gly-Pro-Leu with specific radioactivity of 135 Ci/mmol, ACTH(6-9)Pro-Gly-Pro – 26 Ci/mmol, 5-oxo-Pro-Arg-Pro – 60 Ci/mmol and 5-oxo-Pro-His-Pro-NH2 – 75 Ci/mmol. The concentration of Pro-Gly-Pro-Leu, ACTH(6-9)Pro-Gly-Pro, 5-oxo-Pro-Arg-Pro and 5-oxo-Pro-His-Pro-NH2 in the blood was found to be about 200 times more than in the brain for intranasal administration, and in average 600 times more for intravenous administration. The stability of proline-containing peptides in vitro experiments was determined using different commercially available peptidases (leucine aminopeptidases, dipeptidases, carboxypeptidases B and Y), and using nasal mucus, microsomal fraction of the rat brain (IMPC) and rat blood plasma. During peptidase hydrolysis of Pro-Gly-Pro-Leu, the main metabolites were Gly-Pro-Leu, Pro-Gly-Pro, Gly-Pro and Pro-Gly. For ACTH(6-9)Pro-Gly-Pro, the main metabolites were Phe-Arg-Trp-Pro-Gly-Pro and Trp-Pro-Gly-Pro. In peptidase hydrolysis of 5-oxo-Pro-His-Pro-NH2, the major metabolite was 5-oxo-Pro-His-Pro. It was shown that with different methods of peptides administration the composition of the metabolites formed is different. Based on the data obtained, resistance to enzymatic cleavage of peptides and their metabolic pathways were evaluated. Thus, these new data have shown that the above approaches can be used to prolong the action of glyprolines in living objects. In this case, the degradation of proline-containing peptides occurs mainly not due to the action of proteases, but due to other ways of degradation. In general, the data presented in the review indicate the promise of intranasal way of introducing biologically active peptides into the brain of living organisms.

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Проникновение 5-Охо-Pro-Arg-Pro В Головной Мозг И Основные Пути Его Метаболизма В Мозге И Крови Крыс При Интраназальном И Внутривенном Введении

Шевченко¹,

Нагаев²,

Шевченко³

et al. 2017

Доклады Академии наук

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Степень Проникновения Тиролиберина В Кровь И Отделы Головного Мозга При Интраназальном Или Внутривенном Введении

Cited by 3 publications

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Oxoprolinic short peptides – potential pharmacological means of hypolidemic and antitrombotic actions

Oxoprolinic short peptides – potential pharmacological means of hypolidemic and antitrombotic actions

Stability of prolin-containing peptides in biological media

Проникновение 5-Охо-Pro-Arg-Pro В Головной Мозг И Основные Пути Его Метаболизма В Мозге И Крови Крыс При Интраназальном И Внутривенном Введении

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