Anti-Tumor Activity of Atractylenolide I in Human Colon Adenocarcinoma In Vitro

• Main Authors: Ka Woon Karen Chan, Hau Yin Chung, Wing Shing Ho
• Format: Article
• Language: English
• Published: MDPI AG 2020-01-01
• Series: Molecules
• Subjects: atractylenolide i; <i>atractylodes macrocephala</i>; colon adenocarcinoma; ht-29; mitochondria-dependent apoptosis; caspase
• Online Access: https://www.mdpi.com/1420-3049/25/1/212

<i>Atractylodes macrocephala</i> is known to exhibit multi-arrays of biologic activity in vitro. However, detail of its anti-tumor activity is lacking. In this study, the effects of atractylenolide I (AT-I), a bio-active compound present in <i>Atractylodes macrocephala</i> rhizome was studied in the human colorectal adenocarcinoma cell line HT-29. The results showed that AT-I induced apoptosis of human colon cancer cells through activation of the mitochondria-dependent pathway. The IC₅₀ of AT-I was 277.6 μM, 95.7 μM and 57.4 μM, after 24, 48 and 72 h of incubation with HT-29, respectively. TUNEL and Annexin V-FITC/PI double stain assays showed HT-29 DNA fragmentation after cell treatment with various AT-I concentrations. Western blotting analysis revealed activation of both initiator and executioner caspases, including caspase 3, caspase 7, and caspase 9, as well as PARP, after HT-29 treatment with AT-I via downregulation of pro-survival Bcl-2, and upregulation of anti-survival Bcl-2 family proteins, including Bax, Bak, Bad, Bim, Bid and Puma. The studies show for the first time that AT-I is an effective drug candidate towards the HT-29 cell.