| Форма представления | Статьи в российских журналах и сборниках |
| Год публикации | 2023 |
| Язык | английский |
|
Аймалетдинов Александр Маазович, автор
Бондарь Оксана Викторовна, автор
Каюмов Айрат Рашитович, автор
Павельев Роман Сергеевич, автор
Пугачев Михаил Владимирович, автор
Штырлин Юрий Григорьевич, автор
|
|
Карут Рауда , автор
|
|
Мохаммад Тараа , автор
Ыгайев Бексултан Бактыбекович, автор
|
| Библиографическое описание на языке оригинала |
.V. Bondar, R. Karwt, T. Mohammad, R.S. Pavelyev, M.V. Pugachev, Be.B. Ygaiev, A.R. Kayumov, A.M. Aimaletdinov, and Y.G. Shtyrlin. Structural Analogs of Dehydrozingerone Containing a Pyridoxine Fragment Exhibit Membrane-Modulating Properties and Synergistically Enhance the Antitumor Activity of Cytostatics // Russian Journal of Bioorganic Chemistry, 2023, 49 (4), P. 797-814. ISSN 1068-1620. DOI: 10.1134/S106816202304009X |
| Аннотация |
Previously we synthesized 10 novel structural analogs of dehydrozingerone based on the pyridoxine
(vitamin B6) scaffold. Two lead compounds (compound (I) and compound (II)) expressed good cytotoxic
activity against tumor cells and have shown higher selectivity than doxorubicin. In the present study, the
mechanism of action of the leading analogues of dehydrozingerone, as well as the efficiency of their combinations
with known cytostatics, was studied in more detail. We revealed a synergistic effect of leader dehydrozingerone
analogs combinations with known cytostatics—doxorubicin, vinblastine and paclitaxel. It was
established, that test compounds (I) and (II), as well as curcumin and dehydrozingerone, possess membranedamaging
activity: cause cytoplasmic membrane depolarization and reduction in its microviscosity, which
can explain the increase in toxicity of cytostatics. In addition, the test compounds were found to increase the
ATPase activity of P-glycoproteins, likely acting as their substrates. It was also revealed that the test compounds
increase the expression of BAX and E-cadherin, decrease the expression of Bcl-2 in cancer cells.
Compound (I) does not cause blood cells hemolysis, does not possess DNA-damaging and mutagenic activity,
and when administered intravenously to mice, the LD50 was 65 mg/kg. The investigated compounds are
promising drug candidates to be further tested on animals with grafted tumors. |
| Ключевые слова |
pyridoxine, dehydrozingerone, curcumin, compositions with cytostatics, membrane-damaging activity |
| Название журнала |
Биоорганическая химия
|
| URL |
https://link.springer.com/article/10.1134/S106816202304009X |
| Пожалуйста, используйте этот идентификатор, чтобы цитировать или ссылаться на эту карточку |
https://repository.kpfu.ru/?p_id=292856 |
| Файлы ресурса | |
|
|
Полная запись метаданных  |
| Поле DC |
Значение |
Язык |
| dc.contributor.author |
Аймалетдинов Александр Маазович |
ru_RU |
| dc.contributor.author |
Бондарь Оксана Викторовна |
ru_RU |
| dc.contributor.author |
Каюмов Айрат Рашитович |
ru_RU |
| dc.contributor.author |
Павельев Роман Сергеевич |
ru_RU |
| dc.contributor.author |
Пугачев Михаил Владимирович |
ru_RU |
| dc.contributor.author |
Штырлин Юрий Григорьевич |
ru_RU |
| dc.contributor.author |
Мохаммад Тараа |
ru_RU |
| dc.contributor.author |
Ыгайев Бексултан Бактыбекович |
ru_RU |
| dc.contributor.author |
Карут Рауда |
ru_RU |
| dc.date.accessioned |
2023-01-01T00:00:00Z |
ru_RU |
| dc.date.available |
2023-01-01T00:00:00Z |
ru_RU |
| dc.date.issued |
2023 |
ru_RU |
| dc.identifier.citation |
.V. Bondar, R. Karwt, T. Mohammad, R.S. Pavelyev, M.V. Pugachev, Be.B. Ygaiev, A.R. Kayumov, A.M. Aimaletdinov, and Y.G. Shtyrlin. Structural Analogs of Dehydrozingerone Containing a Pyridoxine Fragment Exhibit Membrane-Modulating Properties and Synergistically Enhance the Antitumor Activity of Cytostatics // Russian Journal of Bioorganic Chemistry, 2023, 49 (4), P. 797-814. ISSN 1068-1620. DOI: 10.1134/S106816202304009X |
ru_RU |
| dc.identifier.uri |
https://repository.kpfu.ru/?p_id=292856 |
ru_RU |
| dc.description.abstract |
Биоорганическая химия |
ru_RU |
| dc.description.abstract |
Previously we synthesized 10 novel structural analogs of dehydrozingerone based on the pyridoxine
(vitamin B6) scaffold. Two lead compounds (compound (I) and compound (II)) expressed good cytotoxic
activity against tumor cells and have shown higher selectivity than doxorubicin. In the present study, the
mechanism of action of the leading analogues of dehydrozingerone, as well as the efficiency of their combinations
with known cytostatics, was studied in more detail. We revealed a synergistic effect of leader dehydrozingerone
analogs combinations with known cytostatics—doxorubicin, vinblastine and paclitaxel. It was
established, that test compounds (I) and (II), as well as curcumin and dehydrozingerone, possess membranedamaging
activity: cause cytoplasmic membrane depolarization and reduction in its microviscosity, which
can explain the increase in toxicity of cytostatics. In addition, the test compounds were found to increase the
ATPase activity of P-glycoproteins, likely acting as their substrates. It was also revealed that the test compounds
increase the expression of BAX and E-cadherin, decrease the expression of Bcl-2 in cancer cells.
Compound (I) does not cause blood cells hemolysis, does not possess DNA-damaging and mutagenic activity,
and when administered intravenously to mice, the LD50 was 65 mg/kg. The investigated compounds are
promising drug candidates to be further tested on animals with grafted tumors. |
ru_RU |
| dc.language.iso |
ru |
ru_RU |
| dc.subject |
pyridoxine |
ru_RU |
| dc.subject |
dehydrozingerone |
ru_RU |
| dc.subject |
curcumin |
ru_RU |
| dc.subject |
compositions with cytostatics |
ru_RU |
| dc.subject |
membrane-damaging activity |
ru_RU |
| dc.title |
Structural Analogs of Dehydrozingerone Containing a Pyridoxine Fragment Exhibit Membrane-Modulating Properties and Synergistically Enhance the Antitumor Activity of Cytostatics |
ru_RU |
| dc.type |
Статьи в российских журналах и сборниках |
ru_RU |
|
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