Cytotoxicity of Aromatic Substituted Curcuminoid against Human Lung Cancer Cell Line
Hien Van Nguyen, Van Thi Bich Pham and Hao Minh Hoang* Author for corresponding; e-mail address: haohm@hcmute.edu.vn
Volume: Vol.48 No.5 (September 2021)
Research Article
DOI:
Received: 4 Febuary 2021, Revised: 20 March 2021, Accepted: 25 March 2021, Published: -
Citation: Nguyen H.V., Pham V.T.B. and Hoang H.M., Cytotoxicity of Aromatic Substituted Curcuminoid against Human Lung Cancer Cell Line, Chiang Mai Journal of Science, 2021; 48(5): 1313-1321.
Abstract
We now focus on the synthesis of curcumin analogues (1-8) bearing -OCH3/-OH/-F substituents on the phenyl rings via base-catalyzed aldol condensations between various benzaldehydes with pentane- 2,4-dione. The analogues were subsequently tested for in vitro anticancer capacity against human lung cancer cell line (LU-1) by determining their half-maximal inhibitory concentration (IC50, μM). The presence of methoxy/hydroxy groups at meta-positions in aromatic rings of compounds (3, IC50 = 29.21±2.12 μM; 5, IC50 = 68.69±5.47 μM) exhibited higher anticancer activities, whereas analogues (2, 4) having similar substituents at para-positions displayed very poor activities when compared with curcumin (1, IC50 = 72.88±6.19 μM). Fluorinated curcuminoids (6, 7) showed inactivities. Remarkably, the level of inhibition of (8) containing 3-fluoro aromatic moiety was improved with an IC50 of 56.39±4.26 μM in this assay. The results indicated that the 3-substituted phenyl motifs are responsible for inhibition of LU-1 cell growth.