6533b82ffe1ef96bd1295156

RESEARCH PRODUCT

Cytotoxic benzylbenzofuran derivatives from Dorstenia kameruniana

Fozia A. AdemVictor KueteArmelle T. MbavengMatthias HeydenreichAbiy YenesewBeatrice IrunguAlbert NdakalaThomas A. Efferth

subject

0301 basic medicineChalconeStereochemistryMoraceaeBergapten03 medical and health sciencesFuranocoumarinchemistry.chemical_compound0302 clinical medicineCell Line TumorDrug DiscoveryHumansCytotoxicityIC50Institut für Biochemie und BiologieBenzofuransPharmacologyMolecular StructurebiologyGeneral MedicineNuclear magnetic resonance spectroscopyMoraceaebiology.organism_classificationAntineoplastic Agents PhytogenicDrug Resistance Multiple030104 developmental biologychemistryDrug Resistance NeoplasmCell culture030220 oncology & carcinogenesisddc:540

description

Abstract Chromatographic separation of the extract of the roots of Dorstenia kameruniana (family Moraceae) led to the isolation of three new benzylbenzofuran derivatives, 2-(p-hydroxybenzyl)benzofuran-6-ol (1), 2-(p-hydroxybenzyl)-7-methoxybenzofuran-6-ol (2) and 2-(p-hydroxy)-3-(3-methylbut-2-en-1-yl)benzyl)benzofuran-6-ol(3) (named dorsmerunin A, B and C, respectively), along with the known furanocoumarin, bergapten (4). The twigs of Dorstenia kameruniana also produced compounds 1–4 as well as the known chalcone licoagrochalcone A (5). The structures were elucidated by NMR spectroscopy and mass spectrometry. The isolated compounds displayed cytotoxicity against the sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells, where compounds 4 and 5 had the highest activities (IC50 values of 7.17 μM and 5.16 μM, respectively) against CCRF-CEM leukemia cells. Compound 5 also showed cytotoxicity against 7 sensitive or drug-resistant solid tumor cell lines (breast carcinoma, colon carcinoma, glioblastoma), with IC50 below 50 μM, whilst 4 showed selective activity.

yearjournalcountryeditionlanguage
2018-04-30Fitoterapia
https://doi.org/10.1016/j.fitote.2018.04.019