TY  - JOUR
AU  - Daletos, Georgios
AU  - Kalscheuer, Rainer
AU  - Koliwer-Brandl, Hendrik
AU  - Hartmann, Rudolf
AU  - de Voogd, Nicole J.
AU  - Wray, Victor
AU  - Lin, Wenhan
AU  - Proksch, Peter
TI  - Callyaerins from the Marine Sponge Callyspongia aerizusa : Cyclic Peptides with Antitubercular Activity
JO  - Journal of natural products
VL  - 78
IS  - 8
SN  - 1520-6025
CY  - Washington, DC
PB  - Soc.
M1  - FZJ-2016-05390
SP  - 1910 - 1925
PY  - 2015
AB  - Chemical investigation of the Indonesian sponge Callyspongia aerizusa afforded five new cyclic peptides, callyaerins I−M (1−5), along with the known callyaerins A−G (6−12). The structures of the new compounds were unambiguously elucidated on the basis of one- and twodimensional NMR spectroscopy and mass spectrometry. In addition, the structures of callyaerins D (9), F (11), and G (12), previously available in only small amounts, have been reinvestigated and revised. All compounds were tested in vitro against Mycobacterium tuberculosis, as well as against THP-1 (human acute monocytic leukemia) and MRC-5 (human fetal lung fibroblast) cell lines, in order to assess their general cytotoxicity. Callyaerins A (6) and B (7) showed potent anti-TB activity with MIC90 values of 2 and 5 μM, respectively. Callyaerin C (8) was found to be less active, with an MIC90 value of 40 μM. Callyaerin A (6), which showed the strongest anti- TB activity, was not cytotoxic to THP-1 or MRC-5 cells (IC50 > 10 μM), which highlights the potential of these compounds as promising anti-TB agents.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000360773700014
C6  - pmid:26213786
DO  - DOI:10.1021/acs.jnatprod.5b00266
UR  - https://juser.fz-juelich.de/record/819795
ER  -