Amphiphilic Triazine-Phosphorus Metallodendrons Possessing Anti-Cancer Stem Cell Activity

Amphiphilic Triazine-Phosphorus Metallodendrons Possessing Anti-Cancer Stem Cell Activity Научная публикация

Журнал

Pharmaceutics
ISSN: 1999-4923

Вых. Данные

Год: 2022, Том: 14, Номер: 2, Номер статьи : 393, Страниц : DOI: 10.3390/pharmaceutics14020393

Ключевые слова

dendrons; phosphorus; supramolecular associates; metallodrugs; copper; gold; tumor stem cells; cytotoxicity; nanomedicine

Авторы

Apartsin Evgeny K. ^1,2,3,4 , Knauer Nadezhda ^3,5,6,7 , Kahlert Ulf Dietrich ^8,9 , Caminade Anne-Marie ^1,2

Организации

1	(Данные Web of science) CNRS, Lab Chim Coordinat, 205 Route Narbonne, F-31077 Toulouse 04, France
2	(Данные Web of science) Univ Toulouse, LCC, CNRS, F-31077 Toulouse, France
3	(Данные Web of science) RAS, Inst Chem Biol & Fundamental Med SB, Novosibirsk 630090, Russia
4	(Данные Web of science) Novosibirsk State Univ, Dept Nat Sci, Novosibirsk 630090, Russia
5	(Данные Web of science) Res Inst Fundamental & Clin Immunol, Novosibirsk 630099, Russia
6	(Данные Web of science) Heinrich Heine Univ, Med Ctr Dusseldorf, Fac Med, Clin Neurosurg, D-40225 Dusseldorf, Germany
7	(Данные Web of science) Heinrich Heine Univ, Med Ctr Dusseldorf, D-40225 Dusseldorf, Germany
8	(Данные Web of science) Univ Hosp Magdeburg, Clin Gen Visceral Vasc & Transplant Surg, Mol & Expt Surg, Fac Med, D-39120 Magdeburg, Germany
9	(Данные Web of science) Univ Hosp Magdeburg, D-39120 Magdeburg, Germany

Dendritic molecules bearing metal complexes in their structure (metallodendrimers and metallodendrons) are considered prospective therapeutic entities. In particular, metallodendrons raise interest as antitumor agents for the treatment of poorly curable or drug-resistant tumors. Herein, we have synthesized amphiphilic triazine-phosphorus dendrons bearing multiple copper (II) or gold (III) complexes on the periphery and a branched hydrophobic fragment at the focal point. Due to their amphiphilic nature, metallodendrons formed single micelles (mean diameter ~9 nm) or multi-micellar aggregates (mean diameter ~60 nm) in a water solution. We have tested the antitumor activity of amphiphilic metallodendrons towards glioblastoma, a malignant brain tumor with a notoriously high level of therapy resistance, as a model disease. The metallodendrons exhibit higher cytotoxic activity towards glioblastoma stem cells (BTSC233, JHH520, NCH644, and SF188 cell lines) and U87 glioblastoma cells (IC50 was 3-6 mu M for copper-containing dendron and 11-15 mu M for gold-containing dendron) in comparison with temozolomide (IC50 >100 mu M)-the clinical standard of care for glioblastoma. Our findings show the potential of metallodendron-based nanoformulations as antitumor entities.

Apartsin E.K. , Knauer N. , Kahlert U.D. , Caminade A-M.
Amphiphilic Triazine-Phosphorus Metallodendrons Possessing Anti-Cancer Stem Cell Activity
Pharmaceutics. 2022. V.14. N2. 393 . DOI: 10.3390/pharmaceutics14020393 WOS Scopus OpenAlex

Опубликована в печати:

10 февр. 2022 г.

Web of science:	WOS:000764644400001
Scopus:	2-s2.0-85124670053
OpenAlex:	W4211119460

БД	Цитирований
Web of science	10
Scopus	8
OpenAlex	10