TY - JOUR
T1 - Anticancer activity of a novel methylated analogue of L-mimosine against an in vitro model of human malignant melanoma
AU - Kyriakou, Sotiris
AU - Mitsiogianni, Melina
AU - Mantso, Theodora
AU - Cheung, William
AU - Todryk, Stephen
AU - Veuger, Stephany
AU - Pappa, Aglaia
AU - Tetard, David
AU - Panagiotidis, Mihalis
N1 - Funding Information:
Funding This work was supported by start-up funds (MIP) including PhD studentships (SK & MM) provided by the Multi-Disciplinary Research Theme in “Bio-economy” of Northumbria University.
Publisher Copyright:
© 2019, The Author(s).
Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.
PY - 2020/6/1
Y1 - 2020/6/1
N2 - 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.
AB - 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.
KW - Anticancer activity
KW - L-mimosine analogues
KW - Melanoma
KW - Metal chelators
KW - Skin cancer
UR - https://www.scopus.com/pages/publications/85068110900
U2 - 10.1007/s10637-019-00809-0
DO - 10.1007/s10637-019-00809-0
M3 - Article
C2 - 31240512
SN - 0167-6997
VL - 38
SP - 621
EP - 633
JO - Investigational New Drugs
JF - Investigational New Drugs
IS - 3
ER -
