Comparative HPLC-DAD and UHPLC-ESI(-)-HRMS & MS/MS profiling of Hypericum species and correlation with necrotic cell-death activity in human leukemic cells. (June 2017)

• Record Type: Journal Article
• Authors: Sakavitsi, Maria-Eleni; Christodoulou, Maria-Ioanna; Tchoumtchoua, Job; Fokialakis, Nikolas; Kokkinopoulou, Ioanna K.; Papageorgiou, Efstathia; Argyropoulou, Aikaterini; Skaltsounis, Leandros A.; Halabalaki, Maria; Scorilas, Andreas
• Is Part Of: Phytochemistry letters. Volume 20(2017:Jun.)
• Page Start: 481
• Page End: 490
• Publication Date: 2017-06
• Subjects: Hypericum species -- Leukemia -- HL-60 -- LC-HRMS -- Orbitrap -- Dereplication; Botanical chemistry -- Periodicals; Chimie végétale -- Périodiques; 572.205
• DOI: 10.1016/j.phytol.2017.05.003
• Languages: English
• ISSNs: 1874-3900

Abstract

Graphical abstract: Highlights: A collection of extracts was screened in vitro for possible anti-cancer properties. The HL-60 human promyelocytic leukemia cell line was used as an in vitro model. Three Hypericum species induced necrotic cell death in the HL-60 cells. HPLC-DAD and UHPLC-ESI(−)-HRMS & MS/MS dereplication procedures were used. Naphodianthrones, phloroglucinol derivatives and flavonoids were mainly detected. Abstract: In the search for potential new anti-cancer agents, the possible anti-proliferative effect of various plant extracts from an in-house extract library was investigated in vitro . The cytotoxic, cytostatic and the pro-apoptotic capacity of the extracts was estimated on the HL-60 human promyelocytic leukemia cell line by the trypan-blue exclusion method, the MTT assay and flow-cytometric analysis. Interestingly, out of all extracts screened, three methanol extracts, namely Hypericum perforatum, Hypericum triquetrifolium and Hypericum rumeliacum, exhibited the most significant activity by promoting necrotic cell-death, accompanied by alterations in the mRNA expression levels of the BCL2 and BAX genes. All the three bioactive extracts were subjected to HPLC-DAD and UHPLC-ESI(−)-HRMS & MS/MS dereplication procedures for correlation purposes. Interesting comparative results related to known constituents such as naphodianthrones, phloroglucinol derivatives and flavonoids were elucidated. To our knowledge, this is the first time that H. triquetrifolium and H. rumeliacum are investigated for both their anti-proliferative properties and their detailed composition.