Anti-Hepatocellular-Cancer Activity Exerted by β-Sitosterol and β-Sitosterol-Glucoside from <i>Indigofera zollingeriana</i> Miq

• Published in: Molecules
• Main Authors: Tuong Kha Vo, Qui Thanh Hoai Ta, Quang Truyen Chu, Thuy Trang Nguyen, Van Giau Vo
• Format: Article
• Language: English
• Published: MDPI AG 2020-07-01
• Subjects: <i>Indigofera zollingeriana</i> Miq; β-sitosterol; β-sitosterol-glucoside; anticancer; HepG2; Huh7
• Online Access: https://www.mdpi.com/1420-3049/25/13/3021

<i>Indigofera zollingeriana</i> Miq (<i>I.</i> <i>zollingeriana</i>) is a widely grown tree in Vietnam. It is used to cure various illnesses. The purpose of this study was to investigate the chemical constituents of an <i>I. zollingeriana</i> extract and test its anticancer activity on hepatocellular cells (Huh7 and HepG2). The experimental results of the analysis of the bioactive compounds revealed that β-sitosterol (β-S) and β-sitosterol-glucoside (β-SG) were the main ingredients of the <i>I.</i> <i>zollingeriana</i> extract. Regarding anticancer activity, the β-S and β-SG of <i>I. zollingeriana</i> were found to exhibit cytotoxic effects against HepG2 and Huh7 cells, but not against normal human primary fibroblasts. The β-S was able to inhibit the proliferation of HepG2 and Huh7 cells in a dose-dependent manner with half-maximal inhibitory concentration (IC₅₀) values of 6.85 ± 0.61 µg/mL and 8.71 ± 0.21 µg/mL, respectively (<i>p</i> < 0.01), whereas the β-SG IC₅₀ values were 4.64 ± 0.48 µg/mL for HepG2 and 5.25 ± 0.14 µg/mL for Huh7 cells (<i>p</i> < 0.01). Remarkably, our study also indicated that β-S and β-SG exhibited cytotoxic activities via inducing apoptosis and activating caspase-3 and -9 in these cells. These findings demonstrated that β-S and β-SG from <i>I.</i> <i>zollingeriana</i> could potentially be developed into promising therapeutic agents to treat liver cancer.