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Novel ANO1 Inhibitor from Mallotus apelta Extract Exerts Anticancer Activity through Downregulation of ANO1

Yohan Seo1,2,3, Nguyen Hoang Anh4, Yunkyung Heo1

  • 1College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 85 Songdogwahak-ro, Yeonsu-gu, Incheon 21983, Korea.

International Journal of Molecular Sciences
|September 9, 2020
PubMed

Insights

Researchers identified Ani-D2, a novel compound from Mallotus apelta, as a potent inhibitor of Anoctamin1 (ANO1) channels. This discovery shows therapeutic potential for treating cancers like prostate and oral squamous cell carcinoma that overexpress ANO1.

Area of Science:

  • Biochemistry and Molecular Biology
  • Cancer Biology
  • Pharmacology

Background:

  • Anoctamin1 (ANO1) is a calcium-activated chloride channel overexpressed in prostate and oral cancers, crucial for tumor growth.
  • Identifying novel ANO1 inhibitors is vital for developing targeted cancer therapies.

Purpose of the Study:

  • To isolate and characterize compounds from Mallotus apelta with inhibitory effects on ANO1 channel activity.
  • To evaluate the therapeutic potential of these compounds against prostate and oral cancer cells.

Main Methods:

  • Isolation and identification of six compounds from Mallotus apelta.
  • Electrophysiological studies to assess ANO1 channel inhibition (IC50 determination).
  • Cell viability assays, Western blotting, cell migration assays, and apoptosis marker analysis (caspase-3, PARP).

Main Results:

  • Two new compounds (1 and 2) and four known compounds (3-6) were isolated. Compound 2 (Ani-D2) demonstrated potent and selective ANO1 inhibition (IC50 = 2.64 μM) with minimal off-target effects.
  • Ani-D2 significantly reduced ANO1 protein expression, cell viability, and migration in PC-3 and CAL-27 cancer cells.
  • Ani-D2 induced apoptosis via caspase-3 activation and PARP cleavage in a manner dependent on ANO1 expression.

Conclusions:

  • Ani-D2 is a novel, potent, and selective ANO1 inhibitor with significant anti-cancer effects.
  • Ani-D2 exhibits therapeutic potential for treating ANO1-overexpressing cancers, including prostate and oral squamous cell carcinoma.
Keywords:
Mallotus apeltaanoctamin 1apoptosiscytotoxicityinhibitor

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