On the mechanism of tumor cell entry of aloe-emodin, a natural compound endowed with anticancer activity

被引：2

作者：

Pecere, Teresa ^{[1
]}

Ponterio, Eleonora ^{[1
]}

Di Iorio, Enzo ^{[1
]}

Carli, Modesto ^{[2
]}

Fassan, Matteo ^{[4
]}

Santoro, Luisa ^{[5
]}

Bissaro, Maicol ^{[3
]}

Bernabe, Giulia ^{[1
]}

Moro, Stefano ^{[3
]}

Castagliuolo, Ignazio ^{[1
]}

Palu, Giorgio ^{[1
]}

机构：

[1] Univ Padua, Dept Mol Med, Via A Gabelli 63, I-35121 Padua, Italy

[2] Univ Padua, Dept Womens & Childrens Hlth, Hematol Oncol Div, Padua, Italy

[3] Univ Padua, Dept Pharmaceut & Pharmacol Sci, Mol Modeling Sect MMS, Padua, Italy

[4] Univ Padua, Dept Med, Padua, Italy

[5] Azienda Osped Padova, Padua, Italy

来源：

INTERNATIONAL JOURNAL OF CANCER | 2021年 / 149卷 / 05期

关键词：

aloe-emodin; anticancer activity; somatostatin receptor; SOMATOSTATIN RECEPTOR; EXPRESSION; PROLIFERATION; INHIBITION; CANCER;

D O I：

10.1002/ijc.33686

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Aloe-emodin (1,8-dihydroxy-3-[hydroxymethyl]-anthraquinone), AE, is one of the active constituents of a number of plant species used in traditional medicine. We have previously identified, for the first time, AE as a new antitumor agent and shown that its selective in vitro and in vivo killing of neuroblastoma cells was promoted by a cell-specific drug uptake process. However, the molecular mechanism underlying the cell entry of AE has remained elusive as yet. In this report, we show that AE enters tumor cells via two of the five somatostatin receptors: SSTR2 and SSTR5. This observation was suggested by gene silencing, receptor competition, imaging and molecular modeling experiments. Furthermore, SSTR2 was expressed in all surgical neuroblastoma specimens we analyzed by immunohistochemistry. The above findings have strong implications for the clinical adoption of this natural anthraquinone molecule as an antitumor agent.

引用

页码：1129 / 1136

页数：8

共 25 条

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