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Mar. Drugs 2018, 16(10), 383; https://doi.org/10.3390/md16100383

Anticancer Activity of Fascaplysin against Lung Cancer Cell and Small Cell Lung Cancer Circulating Tumor Cell Lines

Department of Surgery, Medical University of Vienna, A-1090 Vienna, Austria
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Received: 15 September 2018 / Revised: 4 October 2018 / Accepted: 10 October 2018 / Published: 14 October 2018
(This article belongs to the Collection Marine Compounds and Cancer)
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Abstract

Lung cancer is a leading cause of tumor-associated mortality. Fascaplysin, a bis-indole of a marine sponge, exhibit broad anticancer activity as specific CDK4 inhibitor among several other mechanisms, and is investigated as a drug to overcome chemoresistance after the failure of targeted agents or immunotherapy. The cytotoxic activity of fascaplysin was studied using lung cancer cell lines, primary Non-Small Cell Lung Cancer (NSCLC) and Small Cell Lung Cancer (SCLC) cells, as well as SCLC circulating tumor cell lines (CTCs). This compound exhibited high activity against SCLC cell lines (mean IC50 0.89 µM), as well as SCLC CTCs as single cells and in the form of tumorospheres (mean IC50 0.57 µM). NSCLC lines showed a mean IC50 of 1.15 µM for fascaplysin. Analysis of signal transduction mediators point to an ATM-triggered signaling cascade provoked by drug-induced DNA damage. Fascaplysin reveals at least an additive cytotoxic effect with cisplatin, which is the mainstay of lung cancer chemotherapy. In conclusion, fascaplysin shows high activity against lung cancer cell lines and spheroids of SCLC CTCs which are linked to the dismal prognosis of this tumor type. Derivatives of fascaplysin may constitute valuable new agents for the treatment of lung cancer. View Full-Text
Keywords: fascaplysin; lung cancer; circulating tumor cells; signal transduction; cytotoxicity; cisplatin fascaplysin; lung cancer; circulating tumor cells; signal transduction; cytotoxicity; cisplatin
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Rath, B.; Hochmair, M.; Plangger, A.; Hamilton, G. Anticancer Activity of Fascaplysin against Lung Cancer Cell and Small Cell Lung Cancer Circulating Tumor Cell Lines. Mar. Drugs 2018, 16, 383.

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