Cytotoxic Activity of Opopanax hispidus (Friv.) Griseb.: Characterization of a New Chalcone‐type Compound

TL;DR

This study identifies a new chalcone-type compound from Opopanax hispidus that shows cytotoxic activity against lung cancer cells.

Contribution

The discovery of a novel chalcone-type compound with cytotoxic properties against lung cancer cells.

Findings

A new chalcone-type compound (compound 3) was isolated from Opopanax hispidus.

Compound 3 showed significant cytotoxicity against lung cancer cells (A549) with an IC50 of 13.72 ± 0.80 µM.

Three known coumarins were also identified from the active fractions of the plant.

Abstract

The present study aimed to investigate cytotoxic compounds of Opopanax hispidus (Friv.) Griseb. through in vitro, in silico, and phytochemical analyses. The cytotoxic activity of O. hispidus was evaluated against four different cancer cell lines – lung (A549), breast (MCF‐7), liver (HepG2), and cervix (HeLa) – as well as one healthy cell line (Beas‐2B), using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide colorimetric assay. n‐Hexane and dichloromethane sub‐extracts with the IC50 values of 9.77 ± 0.57 and 7.10 ± 0.78 mg/mL on A549, respectively, were fractionated through chromatographic techniques, and the structures of the isolated compounds were elucidated using various spectroscopic methods. A novel compound, 2',6'‐dihydroxy‐4'‐methoxy‐3''‐(ɤ,ɤ‐dimethylallyl)‐4''‐hydroxy β‐hydroxydihydrochalcone (3), along with three known coumarins – umbelliferone 6‐carboxylic acid (1), umbelliferone (2), and nodakenetin (4) – were isolated from the active fractions. Compound 3, which possesses a chalcone structure, exhibited notable cytotoxicity against lung cancer cells with an IC50 value of 13.72 ± 0.80 µM.

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