14117
2011
eng
1682-1697
10
9
article
1
2016-11-30
--
--
New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
Four new tetromycin derivatives, tetromycins 1-4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001(T) 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 M(pro), and PL(pro). The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with K(i) values in the low micromolar range.
Marine drugs
10.3390/md9101682
urn:nbn:de:bvb:20-opus-141171
Mar. Drugs 2011, 9, 1682-1697; doi:10.3390/md9101682
Sheila M. Pimentel-Elardo
Verena Buback
Tobias A. M. Gulder
Tim S. Bugni
Jason Reppart
Gerhard Bringmann
Chris M. Ireland
Tanja Schirmeister
Ute Hentschel
eng
uncontrolled
cysteine protease
eng
uncontrolled
drugs
eng
uncontrolled
streptomyces
eng
uncontrolled
discovery
eng
uncontrolled
anti-trypanosomal
eng
uncontrolled
protease inhibition
eng
uncontrolled
Streptomyces axinellae
eng
uncontrolled
marine sponge
eng
uncontrolled
tetromycin
Organische Chemie
open_access
Julius-von-Sachs-Institut für Biowissenschaften
Institut für Organische Chemie
Institut für Pharmazie und Lebensmittelchemie
Universität Würzburg
https://opus.bibliothek.uni-wuerzburg.de/files/14117/098_Pimentel-Elardo_MARINE-DRUGS.pdf
6386
2011
eng
article
1
2013-01-29
--
--
New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
Four new tetromycin derivatives, tetromycins 1–4 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.
urn:nbn:de:bvb:20-opus-75465
7546
In: Marine Drugs (2011) 9, 1682-1697; doi:10.3390/md9101682
Sheila M. Pimentel-Elardo
Verena Buback
Tobias A. M. Gulder
Tim S. Bugni
Jason Reppart
Gerhard Bringmann
Chris M. Ireland
Tanja Schirmeister
Ute Hentschel
deu
swd
Biologie
eng
uncontrolled
tetromycin
eng
uncontrolled
anti-trypanosomal
eng
uncontrolled
protease inhibition
eng
uncontrolled
Streptomyces axinellae
eng
uncontrolled
marine sponge
Medizin und Gesundheit
open_access
Julius-von-Sachs-Institut für Biowissenschaften
Universität Würzburg
https://opus.bibliothek.uni-wuerzburg.de/files/6386/Pimentel_Elardo_marinedrugs_09_01682_v3.pdf
6226
2010
eng
article
1
2012-10-30
--
--
Anti-Parasitic Compounds from Streptomyces sp. Strains Isolated from Mediterranean Sponges
Actinomycetes are prolific producers of pharmacologically important compounds accounting for about 70% of the naturally derived antibiotics that are currently in clinical use. In this study, we report on the isolation of Streptomyces sp. strains from Mediterranean sponges, on their secondary metabolite production and on their screening for anti-infective activities. Bioassay-guided isolation and purification yielded three previously known compounds namely, cyclic depsipeptide valinomycin, indolocarbazole alkaloid staurosporine and butenolide. This is the first report of the isolation of valinomycin from a marine source. These compounds exhibited novel anti-parasitic activities specifically against Leishmania major (valinomycin IC50 < 0.11 μM; staurosporine IC50 5.30 μM) and Trypanosoma brucei brucei (valinomycin IC50 0.0032 μM; staurosporine IC50 0.022 μM; butenolide IC50 31.77 μM). These results underscore the potential of marine actinomycetes to produce bioactive compounds as well as the re-evaluation of previously known compounds for novel anti-infective activities.
urn:nbn:de:bvb:20-opus-68312
6831
In: Marine Drugs (2010) 8, 2, 373-380, DOI: 10.3390/md8020373
Sheila Marie Pimentel-Elardo
Svitlana Kozytska
Tim S. Bugni
Chris M. Ireland
Heidrun Moll
Ute Hentschel
deu
swd
Biologie
eng
uncontrolled
marine sponges
eng
uncontrolled
Streptomyces
eng
uncontrolled
valinomycin
eng
uncontrolled
staurosporine
eng
uncontrolled
butenolide
eng
uncontrolled
anti-parasitic
Biowissenschaften; Biologie
open_access
Julius-von-Sachs-Institut für Biowissenschaften
Universität Würzburg
https://opus.bibliothek.uni-wuerzburg.de/files/6226/Elardo056_marinedrugs_08_00373.pdf