Cytotoxic Activity-Guided Isolation from Achillea monocephala, and Biological Activities of its Different Extracts

Abstract

Background: The genus Achillea is one of the most important genus of the Asteraceae family and many species of Achillea are used in traditional medicine to treat several ailments. Aim: The aim of the current research was to evaluate in vitro cytotoxic activities of n-hexan, chloroform, ethyl acetate and methanol extracts and to isolate the active compounds from the extract showing the strongest cytotoxic activity. In addition to this, it was aimed to evaluate the biological activities (cytotoxic, antioxidant, anti-urease, anticholinesterase, antimicrobial) of different extracts and active compounds from Achillea monocephala. Methods and Materials: The in vitro antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial activities of different extracts from A. monocephala aerial parts were examined. The structures of the active compounds were determined by NMR techniques, UV, IR and LC-MS/MS analysis and their biological potential was examined. Results: The chloroform extract showed strong and selective cytotoxic activity on the cancer cell lines (MDA-MB-231, MCF-7). Besides, this extract exhibited stronger antimicrobial activity than other extracts. Therefore, through activity-guided procedures, luteolin, naringenin and 8-hydroxy-salvigenin compounds were isolated from this extract. The methanol extract showed stronger antioxidant (DPPH, ABTS, CUPRAC) and anticholinesterase activity than other extracts. The n-hexan extract exhibited the highest anti-urease activity. In this study, it was determined that the isolated compounds had a strong biological activity. Naringenin compound had stronger ABTS radical cation scavenging and ferric reducing/antioxidant power, cytotoxic and antimicrobial activity than other compounds. 8-hydroxy-salvigenin compound showed the highest urease and acetylcholinestease enzyme inhibition. Conclusion: The results of this study suggest that the extracts and isolated compounds from the A. monocephala may be used as antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial agents in the future.

Antifungal Activity of Isolated Compounds from the Leaves of Combretum erythrophyllum (Burch.) Sond. and Withania somnifera (L.) Dunal against Fusarium Pathogens

“…In that study, 5-hydroxy-7,4′-dimethoxyflavone exhibited an antifungal activity with a MIC value of 45 µg/mL against Candida albicans [ 47 ]. The antimicrobial activity of 8-hydroxy-salvigenin was also reported with MIC values ranging from 0.098 mg/mL to 0.78 mg/mL against human and animal pathogens such as Escherichia coli , Proteus vulgaris , Pseudomonas aeruginosa , Candida albicans , Candida glabrata , Candida guilliermondii , Candida parapsilosis and Candida krusei [ 48 ].…”

Phytochemistry and Evidence-Based Traditional Uses of the Genus Achillea L.: An Update (2011–2021)

“…Chlorogenic acid ( 81) is one of the most abundant compounds found in A. alpina, A. asiatica, A. biebersteinii, A. coarctata, A. distans, A. kotschyi, A. ligustica, A. lycaonica, A. millefolium, A. multifidi, A. schurii, A. setacea, A. vermicularis and A. wilhelmsii (Table 5). Moreover, isomers of the aforementioned compound were also reported from A. alpina [56], A. biebersteinii [26], A. cretica [28], A. millefolium and A. moschata [42]. Caffeic acid ( 94) is also abundant, as it was found in 17 Achillea spp.…”

“…Two flavones bearing a methoxy group attached to C-7 or C-3 were reported once, namely 7-O-methyl apigenin (3) (from A. ligustica) [35] and chrysoeriol (20) (from A. millefolium) [40], respectively. Moreover, other methylated flavonoids, such as cirsiliol (22) and cirsimaritin (4), were reported for A. fragrantissima [31,33]; salvigenin (5) for A. millefolium [41] and A. wilhelmsi [50]; and 8-hydroxysalvigenin (6) was identified for A. lycaonica A. monocephala and A. vermicularis [36,42,49]. Moreover, eupatorin (21) was reported for A. alpina and A. tenuifolia [17,48], while eupatilin 7-methyl ether (5-demethylsinensetin) (23) for A. wilhelmsii [25].…”