6533b86dfe1ef96bd12ca181
RESEARCH PRODUCT
Cyclic heptapeptides from the soil-derived fungus Clonostachys rosea
Zhen LiuMostafa A. FouadPeter ProkschNada M. Abdel-wahabWeaam EbrahimWeaam EbrahimWerner E. G. M�llerMatthias U. KassackAlexandra HamacherWenhan LinMohamed KamelHarwoko Harwokosubject
Cell SurvivalStereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsFungusPeptides Cyclic01 natural sciencesBiochemistryMiceStructure-Activity RelationshipCell Line TumorDrug DiscoveryIc50 valuesAnimalsHumansCytotoxicityMolecular BiologyIC50Cell ProliferationDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistryChemistryOrganic ChemistryGliocladiumbiology.organism_classification0104 chemical sciences010404 medicinal & biomolecular chemistryCell cultureFermentationClonostachys roseaMolecular MedicineFermentationDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopydescription
Abstract Three new cyclic heptapeptides (1–3) together with three known compounds (4–6) were isolated from a solid rice culture of the soil-derived fungus Clonostachys rosea. Fermentation of the fungus on white beans instead of rice afforded a new γ-lactam (7) and a known γ-lactone (8) that were not detected in the former extracts. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR spectra as well as by HRESIMS data. Compounds 1 and 4 exhibited significant cytotoxicity against the L5178Y mouse lymphoma cell line with IC50 values of 4.1 and 0.1 µM, respectively. Compound 4 also displayed cytotoxicity against the A2780 human ovarian cancer cell line with an IC50 value of 3.5 µM. The preliminary structure-activity relationships are discussed.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2019-02-24 | Bioorganic & Medicinal Chemistry |