Mar. Drugs 2011, 9(10), 1682-1697; doi:10.3390/md9101682

New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities

1,‡,* email, 2email, 3,§email, 4,||email, 4email, 3email, 4email, 2,¶email and 1email
Received: 25 July 2011; in revised form: 9 September 2011 / Accepted: 16 September 2011 / Published: 26 September 2011
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: Four new tetromycin derivatives, tetromycins 14 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001T cultivated from the Mediterranean sponge Axinella polypoides. Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei, and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV Mpro, and PLpro. The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with Ki values in the low micromolar range.
Keywords: tetromycin; anti-trypanosomal; protease inhibition; Streptomyces axinellae; marine sponge
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MDPI and ACS Style

Pimentel-Elardo, S.M.; Buback, V.; Gulder, T.A.; Bugni, T.S.; Reppart, J.; Bringmann, G.; Ireland, C.M.; Schirmeister, T.; Hentschel, U. New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities. Mar. Drugs 2011, 9, 1682-1697.

AMA Style

Pimentel-Elardo SM, Buback V, Gulder TA, Bugni TS, Reppart J, Bringmann G, Ireland CM, Schirmeister T, Hentschel U. New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities. Marine Drugs. 2011; 9(10):1682-1697.

Chicago/Turabian Style

Pimentel-Elardo, Sheila M.; Buback, Verena; Gulder, Tobias A.M.; Bugni, Tim S.; Reppart, Jason; Bringmann, Gerhard; Ireland, Chris M.; Schirmeister, Tanja; Hentschel, Ute. 2011. "New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities." Mar. Drugs 9, no. 10: 1682-1697.

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