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Bioorg Med Chem Lett ; 26(2): 306-309, 2016 Jan 15.
Article in English | MEDLINE | ID: mdl-26711890

ABSTRACT

Two novel acridone-quinoline alkaloids, acriquinoline A (1) and acriquinoline B (2), together with twenty-two known compounds were isolated from the methanol extract of the root of Citrus reticulata Blanco. The structures of all compounds were determined by comprehensive analyses of their 1D and 2D NMR and mass spectral (EI and ESI) data. The possible biosynthesis for the formation of above compounds is proposed, based on close examination of their structures. Compounds 1, 2, 6, 10 and 14-17 exhibited strong suppressive effect on phagocytosis response upon activation with serum opsonized zymosan in the range of IC50 0.2-10.5µM, which was tested in vitro for oxidative burst studies of whole blood. However, compounds displayed low cytotoxic activity against the human Caucasian prostate adenocarcinoma cell line PC-3, with IC50 between 30.8 and 60.5µM compared to the standard doxorubicin with IC50 0.9µM. These compounds, tested against bacteria, fungi and plant pathogen oomycetes by the paper disk agar diffusion assay, resulting in missing to low activities corresponding with MICs>1mg/mL.


Subject(s)
Acridones/pharmacology , Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/pharmacology , Respiratory Burst/drug effects , Acridones/blood , Acridones/chemistry , Acridones/isolation & purification , Anti-Bacterial Agents/blood , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Antifungal Agents/blood , Antifungal Agents/chemistry , Antifungal Agents/isolation & purification , Antifungal Agents/pharmacology , Antineoplastic Agents/blood , Antineoplastic Agents/chemistry , Antineoplastic Agents/isolation & purification , Bacillus subtilis/drug effects , Candida albicans/drug effects , Cell Line, Tumor , Citrus , Escherichia coli/drug effects , Humans , Mucor/drug effects , Oomycetes/drug effects , Staphylococcus aureus/drug effects , Zymosan/pharmacology
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