Anticancer activity of a novel methylated analogue of L-mimosine against an in vitro model of human malignant melanoma

被引：9

作者：

Kyriakou, Sotiris ^{[1
]}

Mitsiogianni, Melina ^{[1
]}

Mantso, Theodora ^{[1
]}

Cheung, William ^{[1
]}

Todryk, Stephen ^{[1
]}

Veuger, Stephany ^{[1
]}

Pappa, Aglaia ^{[2
]}

Tetard, David ^{[1
]}

Panayiotidis, Mihalis, I ^{[1
]}

机构：

[1] Northumbria Univ, Dept Appl Sci, Newcastle Upon Tyne, Tyne & Wear, England

[2] Democritus Univ Thrace, Dept Mol Biol & Genet, Alexandroupolis, Greece

来源：

INVESTIGATIONAL NEW DRUGS | 2020年 / 38卷 / 03期

关键词：

Metal chelators; L-mimosine analogues; Skin cancer; Anticancer activity; Melanoma; OXIDATIVE STRESS; METASTATIC MELANOMA; MEDIATED ACTIVATION; FENTON REACTION; IRON CHELATION; DNA-SYNTHESIS; CANCER-CELLS; APOPTOSIS; INHIBITION; BINDING;

D O I：

10.1007/s10637-019-00809-0

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

The anticancer activity of a series of novel synthesized, hydroxypyridone-based metal chelators (analogues of L-mimosine) was evaluated in an in vitro model of melanoma consisting of malignant melanoma (A375), non-melanoma epidermoid carcinoma (A431) and immortalized non-malignant keratinocyte (HaCaT) cells. More specifically, we have demonstrated that the L-enantiomer of a methylated analogue of L-mimosine (compound 22) can exert a potent anticancer effect in A375 cells when compared to either A431 or HaCaT cells. Moreover, we have demonstrated that this analogue has the ability to i) promote increased generation of reactive oxygen species (ROS), ii) activate both intrinsic and extrinsic apoptosis and iii) induce perturbations in cell cycle growth arrest. Our data highlights the potential of compound 22 to act as a promising therapeutic agent against an in vitro model of human malignant melanoma.

引用

页码：621 / 633

页数：13

共 80 条

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