COX2-Inhibitory and Cytotoxic Activities of Phytoconstituents of Matricaria chamomilla L.

Abstract

Chamomile tea is a popular beverage and herbal remedy with various health benefits, including antioxidant and antimicrobial activities and beneficial effects on metabolism. In this study, we investigated the inhibitory activities of secondary metabolites from Matricaria chamomile L. against COX2, an enzyme involved in inflammation and linked to cancer development. The cytotoxicity of the compounds was also evaluated on a panel of 60 cancer cell lines. Myricetin, one of the COX2-inhibiting and cytotoxic compounds in chamomile tea, was further studied to determine a proteomic expression profile that predicts the sensitivity or resistance of tumor cell lines to this compound. The expression of classical mechanisms of anticancer drug resistance did not affect the responsiveness of cancer cells to myricetin, e.g., ATP-binding cassette (ABC) transporters (ABCB, ABCB5, ABCC1, ABCG2), tumor suppressors (p53, WT1), and oncogenes (EGFR, RAS), whereas significant correlations between myricetin responsiveness and GSTP expression and cellular proliferation rates were observed. Additionally, Kaplan–Meier survival time analyses revealed that high COX2 expression is associated with a worse survival prognosis in renal clear cell carcinoma patients, suggesting a potential utility for COX2 inhibition by myricetin in this tumor type. Overall, this study provides insight into the molecular modes of action of chamomile secondary metabolites and their potential as cancer-preventive or therapeutic agents.

Impact of Fermentation on the Phytochemical Profile and Bioactivity Characteristics of Aqueous Matricaria recutita L. Root Extracts

“…2-Hydroxy-3-methylbutyric acid 10.3 262.5 247 ( 6), [a] 219 (12), 147 (71), [b] 145 (100), 73 (87) [b] N,N-Dimethylamino-methylidene-trifluoroacetamide [c] 11.0 168.1 168 (2), 99 (100), 69 (24) 2-Hydroxyisocaproic acid 12.1 276.5 159 (81), 147 (55), [b] 103 (100), 73 (96) [b] Ethylsuccinic acid 12.7 218.3 203 (34), [a] 175 (41), 157 (19), 129 (21), 75 (100), 73 (92), [b] 55 (37) Glycerol 13.1 308.6 218 (25), 205 (59), 147 (84), [b] 133 (20), 117 (33), 103 (33), 73 (100) [b] Butanedioic acid 14.5 262.4 247 ( 13), [a] 147 (100), [b] 73 (49) [b] 2-Hydroxyglutaric acid 22.1 364.2 349 (4), [a] 247 (66), 147 (70), [b] 129 (81), 73 (100) [b] 4-Hydroxy-phenylethanol 22.3 282.4 282 (17), 267 ( 12), [a] 193 (14), 179 (100), 103 (12), 73 (53) [b] β-Phenyllactic acid 22.6 310.5 267 (6), 220 (14), 193 (69), 147 (59), [b] 73 (100) [b] Methylmaleic acid 22.9 274.5 247 (7), 184 (29), 147 (100), [b] 73 (98) [b] p-Hydroxybenzoic acid 23.7 282.5 282 (28), 267 ( 53), [a] 268 (10), 193 (24), 73 (100) [b] Cyclooctene diol 25.1 286.2 286 (35), 260 (22), 217…”

“…This is of particular interest since cytotoxic effects on various cell lines have been determined for aqueous chamomile flower extracts in concentrations < 100 μg/mL. [20,59] Subsequently, potential immunomodulating effects of LF extracts were evaluated. The transcription factor NF-kB plays a key role in regulating immune responses upon stimulation.…”