Augmenting Anti-Cancer Natural Products with a Small Molecule Adjuvant

Marine Drugs

Paul G. Wahome²  Kevin R. Beauchesne²  Anna C. Pedone²  John Cavanagh⁵  Christian Melander⁴  Paul Zimba¹  Peter D. R. Moeller³ 

[1] Department of Life Sciences, Texas A&M Corpus Christi, 6300 Ocean Drive, Corpus Christi, TX 78412, USA; E-Mail:;Biosortia Pharmaceuticals, 565 Metro Place South, Suite 300, Dublin, OH 43017, USA; E-Mails:;Toxin/Natural Products Chemistry, National Ocean Service/NOAA, Hollings Marine Lab, 331 Fort Johnson Road, Charleston, SC 29412, USA;Department Chemistry, North Carolina State University, 2620 Yarbrough Drive, Box 8204, Raleigh, North Carolina 27695, USA; E-Mail:;Department of Molecular & Structural Biochemistry, North Carolina State University, Campus Box 7622, 128 Polk Hall, Raleigh, NC 27695, USA; E-Mail:

关键词: anti-cancer agents;    cytotoxicity;    natural products;    toxins;    adjuvant;    small molecule;   

DOI  :  10.3390/md13010065

来源: mdpi

【 摘 要 】

Aquatic microbes produce diverse secondary metabolites with interesting biological activities. Cytotoxic metabolites have the potential to become lead compounds or drugs for cancer treatment. Many cytotoxic compounds, however, show undesirable toxicity at higher concentrations. Such undesirable activity may be reduced or eliminated by using lower doses of the cytotoxic compound in combination with another compound that modulates its activity. Here, we have examined the cytotoxicity of four microbial metabolites [ethyl N-(2-phenethyl) carbamate (NP-1), Euglenophycin, Anabaenopeptin, and Glycolipid 652] using three in vitro cell lines [human breast cancer cells (MCF-7), mouse neuroblastoma cells (N2a), and rat pituitary epithelial cells (GH4C1)]. The compounds showed variable cytotoxicity, with Euglenophycin displaying specificity for N2a cells. We have also examined the modulatory power of NP-1 on the cytotoxicity of the other three compounds and found that at a permissible concentration (125 µg/mL), NP-1 sensitized N2a and MCF-7 cells to Euglenophycin and Glycolipid 652 induced cytotoxicity.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.