Antiproliferative activity against leukemia cells of sesquiterpene lactones from the Turkish endemic plant Centaurea drabifolia subsp. detonsa

6533b7d1fe1ef96bd125c347

RESEARCH PRODUCT

Antiproliferative activity against leukemia cells of sesquiterpene lactones from the Turkish endemic plant Centaurea drabifolia subsp. detonsa

Orazio Taglialatela-scafati Carmen Formisano Giuseppina Chianese Gokhan Zengin Carmina Sirignano Thomas Efferth Ean-jeong Seo Daniela Rigano

subject

Turkey Centaurea drabifolia Stereochemistry Cynaropicrin Centaurea Multidrug-resistant cell line Secondary metabolite Biology Sesquiterpene 01 natural sciences Lactones Sesquiterpenes Guaiane Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Drug Discovery medicine Humans Derivatization Pharmacology chemistry.chemical_classification Leukemia Molecular Structure Plant Extracts 010405 organic chemistry Fatty acid General Medicine Plant Components Aerial Antineoplastic Agents Phytogenic Cynaropicrin 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry Drug Resistance Neoplasm Antileukemic activity Drug Screening Assays Antitumor Sesquiterpene lactones Sesquiterpenes Two-dimensional nuclear magnetic resonance spectroscopy Derivative (chemistry)Lactone medicine.drug

description

The apolar organic extract obtained from aerial parts of Centaurea drabifolia Sibth. & Sm. subsp. detonsa (Bornm.) Wagenitz, growing wild in Turkey, was investigated for the first time for its secondary metabolite composition. Seven sesquiterpene lactones belonging to the guaiane class (1-7), including the new compound 4, along with a fatty acid lactone derivative (8), were isolated. The structures of these compounds were established by spectroscopic analysis, including 2D NMR spectroscopic techniques, with the stereostructure of the new guaiane 4 determined with the help of MTPA derivatization. Cytotoxic activities of compounds 1-7 were evaluated against two cancer cell lines, namely acute lymphoblastic leukemia (CCRF-CEM) and its multidrug-resistant subline CEM/ADR5000. Results showed that aguerin B (1) and cynaropicrin (2) showed a potent activity on both cell lines revealing interesting details about the structure-activity relationships in the class of acylated guaiane sesquiterpenes.

year	journal	country	edition	language
2017-04-07	Fitoterapia

https://doi.org/10.1016/j.fitote.2017.05.016