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New low-molecular conjugates of antitumor drugs with derivatives N-acetyl-D-galactosamineтезисы доклада Тезисы
- Авторы: Petrov S.A., Petrov R.A., Yamansarov E.Yu, Beloglazkina E.K., Majouga A.G.
- Сборник: 29th International Carbohydrate Symposium
- Тезисы
- Год издания: 2018
- Первая страница: P-S75
- Последняя страница: P-S75
- Аннотация: Hepatocellular carcinoma is the most common liver tumor, the result of malignant degeneration of hepatocytes. In terms of the number of deaths, hepatocellular carcinoma ranks 2nd in the world among all malignant tumors according to the World Health Organization.[1] Existing drugs for nowadays have several disadvantages, such as: 1) low selectivity 2) a wide range of side effects 3) low efficiency. Therefore, there is an urgent need to find new highly effective antitumor agents for the treatment of liver diseases. The using of targeted delivery strategy would help to avoid these shortcomings.The asialoglycoprotein receptor is an excellent target for targeted delivery to hepatocytes of galactose-based derivatives [2]. In this work, three novel N-acetyl galactosamine ligands which show the highest affinity for ASGP-R have been synthesized. These ligands were also conjugated with antitumor drugs (paclitaxel, doxorubicin, methotrexate), which are used in clinical practice.[3],[4] The reaction of [3 + 2] copper-catalyzed azide-alkyne cycloaddition (CuAAC) was used for the ligand and drug fragments conjugation. Subsequently, all the resulting conjugates were tested for cytotoxicity. Cytotoxicity was determined by the standard MTS method on the HepG2 cell line. Also, the method of fluorescent microscopy was used for the characterization of doxorubicin conjugates. The obtained results indicated the accumulation of free doxorubicin in the cell nucleus. In the case of doxorubicin conjugates, accumulation in the cytoplasm was observed. Some of the synthesised compounds exhibited cytotoxicity comparable to free drugs.
- Добавил в систему: Петров Станислав Александрович
Прикрепленные файлы
| № | Имя | Описание | Имя файла | Размер | Добавлен |
|---|---|---|---|---|---|
| 1. | Первая страница | первая страница | Pervaya_stranitsa.PNG | 250,7 КБ | 26 августа 2021 [stanislavpetrov] |
| 2. | Полный текст | текст тезиса | Tezis.PNG | 92,0 КБ | 26 августа 2021 [stanislavpetrov] |