@misc{10481/86127,
year = {2023},
month = {11},
url = {https://hdl.handle.net/10481/86127},
abstract = {Lung cancer is the most commonly diagnosed cancer and the one that causes the most deaths worldwide, so there
is a need for therapies that improve survival rates. Products derived from marine organisms are a source of novel
and potent antitumor compounds, but they present the great obstacle of their obtaining from the natural environment
and the problems associated with the synthesis and biological effects of chemical analogues. In this
work, a Bengamide analogue (Bengamide II) was chemically synthesized and in vitro and in vivo studies were
performed to determine its antitumor activity and mechanisms of action. It was shown to have potent antiproliferative
activity in lung cancer lines in 2D and 3D models. In addition, Bengamide II-treated cells showed
G2/M and G0/G1 cell cycle arrest, together with a decrease in the proliferation marker Ki67. As for the
mechanism of action, the treatment was associated with increased LC3-II expression and production of acidic
vesicles signaling autophagy. In addition, Bengamide II treatment was associated with caspase-3 activation and
DNA fragmentation related to apoptosis. Furthermore, a reduction of VEGFA expression, related to angiogenesis,
was also observed. In vivo studies showed that Bengamide II markedly reduced tumor volume and metastases
increasing survival. Additionally, it revealed no systemic toxicity in in vivo models at the therapeutic doses used,
which is essential for its future clinical use. Taken together, the chemically synthesized bengamide analogue
Bengamide II, is a promising drug for lung cancer treatment showing relevant antitumor activity and significant
safety.},
organization = {Junta de Andalucía through project FP20_00540/FEDER and partially through the Projects A-CTS-666-
UGR20 and RTI2018-098296-BI00 (MINECO and FEDER)},
organization = {CTS-107(Andalusian Government)},
organization = {FPU2020 grant (ref. FPU20/07083) from
the Ministerio de Educación y Formación Profesional (Spain)},
publisher = {Elsevier},
keywords = {Bengamide II},
keywords = {Lung cancer},
keywords = {Antitumor},
keywords = {In vitro},
keywords = {In vivo},
title = {Antitumor activity of bengamide ii in a panel of human and murine tumor cell lines: In vitro and in vivo determination of effectiveness against lung cancer},
doi = {10.1016/j.biopha.2023.115789},
author = {Ortigosa Palomo, Alba and Quiñonero Muñoz, Francisco José and Ortiz Quesada, Raúl and Melguizo Alonso, Consolación and Prados Salazar, José Carlos},
}