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Antitumor Activity of 3-Indolylmethanamines 31B and PS121912

Margaret L Guthrie1, Preetpal S Sidhu1, Emily K Hill2

  • 1Department of Chemistry and Biochemistry, University of Wisconsin, Milwaukee, WI, U.S.A. Milwaukee Institute of Drug Discovery, University of Wisconsin, Milwaukee, WI, U.S.A.

Anticancer Research
|October 28, 2015
PubMed
Abstract

Insights

3-Indolylmethanamines 31B and PS121912 show in vivo anticancer effects. These compounds inhibit tumor growth in ovarian cancer and leukemia models by inducing apoptosis and reducing glucose metabolism.

Area of Science:

  • Oncology
  • Pharmacology
  • Biochemistry

Background:

  • Ovarian cancer and leukemia pose significant therapeutic challenges.
  • Novel therapeutic strategies are urgently needed to combat these malignancies.

Purpose of the Study:

  • To evaluate the in vivo antitumor efficacy of 3-indolylmethanamines 31B and PS121912.
  • To elucidate the underlying mechanisms of their anticancer activity.

Main Methods:

  • Terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and Western blotting assessed apoptosis.
  • Xenograft models were used to evaluate in vivo antitumor effects.
  • (13)C-Nuclear magnetic resonance ((13)C-NMR) and Western blotting investigated glucose metabolism inhibition.

Main Results:

  • Compound 31B induced apoptosis in ovarian cancer cells by activating caspase-3, PARP1 cleavage, and phosphorylating MAPK, JNK/SAPK, and p38.
  • 31B significantly reduced ovarian cancer xenograft tumor growth.
  • PS121912 inhibited leukemia xenograft growth without observable toxicity.
  • 31B suppressed de novo glycolysis and lipogenesis via reduced fatty acid synthase and lactate dehydrogenase-A expression.

Conclusions:

  • 3-Indolylmethanamines represent a promising new class of antitumor agents.
  • This study provides the first in vivo evidence of anticancer effects for 3-indolylmethanamines 31B and PS121912.
Keywords:
3-Indolylmethanamineleukemiaovarian cancer

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