Phenolics of Achillea fragrantissima growing in Egypt and its cytotoxic activity

Abstract

Achillea fragrantissima Sch. Bip. (Asteraceae) has been reputed in folk medicine of the Arabia region and Egypt for the treatment of many diseases. Air dried aerial parts of A. fragrantissima were extracted with 70% aqueous ethanol and fractionated with petroleum ether, dichloromethane, n-butanol and ethyl acetate fractions. Among them, dichloromethane showed the highest activity and was subjected to separation and purification by various chromatographic techniques. Five flavones and one phenolic acid were isolated and identified as acerosin (1), cirsimaritin (2), cirsiliol (3), luteolin (4), apigenin (5) and caffeic acid (6), respectively. Acerosin, the flavone of higher concentration isolated for the first time in genus Achillea, showed promising cytotoxic and radical scavenging activity. Molecular modeling of acerosin indicated its ability to bind in a co-crystallized ligand-like manner with kinase enzyme (FAK), namely with Cys502, alongside extra binding interactions with Glu430, Lys454 and Asp564. Total protein profiling of A. fragrantissima DNA was performed using polyacrylamide gel electrophoresis (PAGE) for characterization of plant where the total number of bands recovered was 4.

Antitumor activity of methoxylated flavonoids separated from Achillea fragrantissima extract in Ehrlich’s ascites carcinoma model in mice

“…In addition, isolated cirsiliol from A. fragrantissima (7,9). Isolation and identification of cirsimaritin and eupatilin 7-methyl ether from A. fragrantissima herb were also reported, previously (6). Similarly, chrysosplenol D was separated and identified in many previous studies (16,17).…”

“…Chromatographic separation and purification procedures led to the isolation of four methoxylated flavonoids, namely cirsiliol, chrysosplenol D, eupatilin 7-methyl ether and cirsimaritin. Cirsiliol was previously isolated from A. fragrantissima and showed cytotoxic activity against HepG2 cell lines (6). In addition, isolated cirsiliol from A. fragrantissima (7,9).…”

“…A. fragrantissima, also known in Arabic countries as lavender cotton or in many cases as Qaysūm, is a desert plant. In addition, A. fragrantissima was reported to be a potent differentiation inducer and in the same time apoptosis and cell cycle arrest activator in both chronic myeloid leukemia and T cell lymphoma (5,6). It was therefore thought worthwhile to investigate the antitumor effects of A. fragrantissima extract and its methoxylated flavonoid compounds on Ehrlich's Ascites Carcinoma model in mice, the effects that have not been studied to date.…”

“…The methoxylated flavonoids have been used as a dietary supplement in cancer prevention (7). In addition, the antiproliferative activities of these flavonoids have been reported and can be considered a promising target for new researches (6)(7)(8)(9)). The present study described the antitumor activities of the extract and the flavonoid compounds and attempted to explain the mechanisms underlying these activities.…”

Sesquiterpene Lactones from Achillea fragrantissima

“…Many phytochemical and pharmacological studies have been performed to reveal the importance of A. fragrantissima [9]. Essential oils, flavonoids, terpenoids and glucosides were investigated from A. fragrantissima [15][16][17][18][19][20][21][22][23][24][25][26].…”