Supervisors info:
Ελένη Σκαλτσά, Καθηγήτρια, Φαρμακευτικής, Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών
Summary:
The genus Achillea L. is comprised of over 100 widely distributed medicinal herbs, known since antiquity. The name Achillea refers to the Greek hero Achilles, who used it to treat the soldiers’ wounds during the literary Trojan War. Achillea spp. have been traditionally used for many ailments, such as wound healing, against bleeding, headaches, inflammations, pains, spasmodic diseases, flatulence and dyspepsia. A. millefolium L. herb and flos are quoted by EMA as traditional herbal medicinal products. A. coarctata Poir., a perennial herb found from sub-montane to montane level in Greece, was collected at Lake Poliphytou (Kozani, Greece), where it is locally used to treat gastrointestinal disorders and as diuretic agent. The aerial parts have been exctracted with a mixture of solvents containing cyclohexane: ether: methanol 1:1:1. The non-polar exctract was prefractionated by VLC on silica gel, using cyclohexane-EtOAc-Me2CO mixtures of increasing polarity as eluents to give several fractions. Further purification by VLC, CC and RP18-HPLC yielded six sesquiterpene lactones: arteludovicinolide A (1), rupicolin A (2), rupicolin B (3), 11,13- dihydrodesacetylmatricarin (4), artecalin (5) and 3-acetylridentin B (6), a nor-isoprenoid: 3S,5R-loliolide (7), three flavonoids: luteolin (8), centaureidin (9), casticin (10) and a phenolic acid: 3,5-di-O-caffeoylquinic acid (11). The structures of the isolated compounds were elucidated by high-field NMR spectroscopy (1H-NMR, 1H-1H COSY, NOESY, HSQC and HMBC). Compounds 1-5 and 8-10 are common metabolites of Achillea L., while (6) and (7) have been reported for the first time in this genus. In addition, the initial extract, as well as the isolated metabolites 1-3, 5 and 7-11 were evaluated for their cytotoxic effects on MCF-7 human breast cancer cells and MCF-7 human cervical cancer cells. According to the results, sesquiterpene lactones seem to have potential cytotoxic activity. Rupicolin A and rupicolin B significally inhibit MCF-7 and HeLa cancer cells while artecalin was the most active compound on MCF-7 with IC50 14.23 ± 4.44 μg/mL.
Keywords:
Achillea coarctata, Asteraceae, sesquiterpene lactones, cytotoxicity, MTT
