TY  - JOUR
AB  - Lung cancer is the most deadly type of cancer in humans, with non-small-cell lung cancer (NSCLC) being the most frequent and aggressive type of lung cancer showing high resistance to radiation and chemotherapy. Despite the outstanding progress made in anti-tumor therapy, discovering effective anti-tumor drugs is still a challenging task. Here we describe a new semisynthetic derivative of cucurbitacin B (DACE) as a potent inhibitor of NSCLC cell proliferation. DACE arrested the cell cycle of lung epithelial cells at the G2/M phase and induced cell apoptosis by interfering with EGFR activation and its downstream signaling, including AKT, ERK, and STAT3. Consistent with our in vitro studies, intraperitoneal application of DACE significantly suppressed the growth of mouse NSCLC that arises from type II alveolar pneumocytes due to constitutive expression of a human oncogenic c-RAF kinase (c-RAF-1-BxB) transgene in these cells. Taken together, these findings suggest that DACE is a promising lead compound for the development of an anti-lung-cancer drug.
AU  - Silva, Izabella T.
AU  - Carvalho, Annelise
AU  - Lang, Karen L.
AU  - Dudek, Sabine Eva
AU  - Masemann, Dörthe
AU  - Durán, Fernando J.
AU  - Balparda Caro, Miguel Soriano
AU  - Rapp, Ulf Rüdiger
AU  - Rapp, Ulf R.
AU  - Rapp, U. R.
AU  - Rapp, Ulf
AU  - Rapp, U.
AU  - Wixler, Viktor
AU  - Schenkel, Eloir P.
AU  - Simões, Cláudia M. O.
AU  - Ludwig, Stephan
DA  - 2015-02-12
DO  - 10.1371/journal.pone.0117794
LA  - eng
N1  - PLoS ONE 10 (2015) 2, e0117794, 1-19
N1  - Finanziert durch den Open-Access-Publikationsfonds 2014/2015 der Deutschen Forschungsgemeinschaft (DFG) und der Westfälischen Wilhelms-Universität Münster (WWU Münster).
PY  - 2015-02-12
SN  - 1932-6203
TI  - In Vitro and In Vivo Antitumor Activity of a Novel Semisynthetic Derivative of Cucurbitacin B
UR  - https://nbn-resolving.org/urn:nbn:de:hbz:6-39299643678
Y2  - 2024-11-21T23:19:53
ER  -