Abstract
Triple-negative breast cancer (TNBC) represents the deadliest form of gynecological tumors currently lacking targeted therapies. The ethanol extract of the North Pacific brittle star Ophiura sarsii presented promising anti-TNBC activities. After elimination of the inert material, the active extract was submitted to a bioguided isolation approach using high-resolution semipreparative HPLC-UV, resulting in one-step isolation of an unusual porphyrin derivative possessing strong cytotoxic activity. HRMS and 2D NMR resulted in the structure elucidation of the compound as (3S,4S)-14-Ethyl-9-(hydroxymethyl)-4,8,13,18-tetramethyl-20-oxo-3-phorbinepropanoic acid. Never identified before in Ophiuroidea, porphyrins have found broad applications as photosensitizers in the anticancer photodynamic therapy. The simple isolation of a cytotoxic porphyrin from an abundant brittle star species we describe here may pave the way for novel natural-based developments of targeted anti-cancer therapies.
Highlights
Received: 29 November 2020 Accepted: 24 December 2020 Published: 29 December 2020Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.Despite the enormous effort, cancer remains one of the leading causes of diseaserelated mortality
Brittle stars Ophiura sarsii were collected near the Russky Island in the Peter the Great Gulf, Sea of Japan, in May 2019
A procedure to eliminate them was performed, whereas the extract was submitted to C18 solid-phase extraction (SPE) by elution with water and methanol
Summary
Received: 29 November 2020 Accepted: 24 December 2020 Published: 29 December 2020. Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Cancer remains one of the leading causes of diseaserelated mortality To overcome this persistence, targeted anticancer therapies are in need and are being actively developed. As an example of the former, drugs attacking the oncogenic Wnt signaling pathway are being actively developed by pharma companies and academia [1,2]. In our quest to identify novel Wnt-targeting anti-TNBC compounds, we among other approaches screened extracts from deep-sea invertebrates of the Russian Pacific in a set of assays monitoring Wnt signaling in the cancer cells, identifying Ophiura irrorata and other brittle stars collected at the depths of 2.2–3.3 km as a promising source of a powerful anticancer activity [7,8]. Our findings may have identified a natural photosensitizer for future PDT applications
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