Antitumor activity of 3-indolylmethanamines 31b and ps121912

Margaret L. Guthrie; Preetpal S. Sidhu; Emily K. Hill; Timothy C. Horan; Premchendar Nandhikonda; Kelly A. Teske; Nina Y. Yuan; Marina Sidorko; Revathi Rodali; James M. Cook; Lanlan Han; Nicholas R. Silvaggi; Daniel D. Bikle; Richard G. Moore; Rakesh K. Singh; Leggy A. Arnold

Antitumor activity of 3-indolylmethanamines 31b and ps121912

Margaret L. Guthrie
, Preetpal S. Sidhu
, Emily K. Hill
, Timothy C. Horan
, Premchendar Nandhikonda
, Kelly A. Teske
, Nina Y. Yuan
, Marina Sidorko
, Revathi Rodali
, James M. Cook
, Lanlan Han
, Nicholas R. Silvaggi
, Daniel D. Bikle
, Richard G. Moore
, Rakesh K. Singh
, Leggy A. Arnold^*

^*Corresponding author for this work

Department of Chemistry and Biochemistry
University of Wisconsin-Milwaukee
Brown University
Milwaukee Institute of Drug Discovery
Department of Veterans Affairs

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

Aim: To investigate the in vivo effects of 3-indolylmethanamines 31B and PS121912 in treating ovarian cancer and leukemia, respectively. Materials and Methods: Terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and western blotting were applied to demonstrate the induction of apoptosis. Xenografted mice were investigated to show the antitumor effects of 3-indolylmethanamines. 13CNuclear magnetic resource (NMR) and western blotting were used to demonstrate inhibition of glucose metabolism. Results: 31B inhibited ovarian cancer cell proliferation and activated caspase-3, cleaved poly (ADP-ribose) polymerase 1 (PARP1), and phosphorylated mitogen-activated protein kinases (MAPK), JUN N-terminal kinase/stress-activated protein kinase (JNK/SAPK) and p38. 31B reduced ovarian cancer xenograft tumor growth and PS121912 inhibited the growth of HL-60-derived xenografts without any sign of toxicity. Compound 31B inhibited de novo glycolysis and lipogenesis mediated by the reduction of fatty acid synthase and lactate dehydrogenase-A expression. Conclusion: 3-Indolylmethanamines represent a new class of antitumor agents. We have shown for the first time the in vivo anticancer effects of 3-indolylmethanamines 31B and PS121912.

Original language	English
Pages (from-to)	6001-6007
Number of pages	7
Journal	Anticancer Research
Volume	35
Issue number	11
Publication status	Published - Nov 2015
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

3-Indolylmethanamine
Leukemia
Ovarian cancer

Cite this

@article{fd9ff62a638743df9f817b348e03a3ad,

title = "Antitumor activity of 3-indolylmethanamines 31b and ps121912",

abstract = "Aim: To investigate the in vivo effects of 3-indolylmethanamines 31B and PS121912 in treating ovarian cancer and leukemia, respectively. Materials and Methods: Terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and western blotting were applied to demonstrate the induction of apoptosis. Xenografted mice were investigated to show the antitumor effects of 3-indolylmethanamines. 13CNuclear magnetic resource (NMR) and western blotting were used to demonstrate inhibition of glucose metabolism. Results: 31B inhibited ovarian cancer cell proliferation and activated caspase-3, cleaved poly (ADP-ribose) polymerase 1 (PARP1), and phosphorylated mitogen-activated protein kinases (MAPK), JUN N-terminal kinase/stress-activated protein kinase (JNK/SAPK) and p38. 31B reduced ovarian cancer xenograft tumor growth and PS121912 inhibited the growth of HL-60-derived xenografts without any sign of toxicity. Compound 31B inhibited de novo glycolysis and lipogenesis mediated by the reduction of fatty acid synthase and lactate dehydrogenase-A expression. Conclusion: 3-Indolylmethanamines represent a new class of antitumor agents. We have shown for the first time the in vivo anticancer effects of 3-indolylmethanamines 31B and PS121912.",

keywords = "3-Indolylmethanamine, Leukemia, Ovarian cancer",

author = "Guthrie, \{Margaret L.\} and Sidhu, \{Preetpal S.\} and Hill, \{Emily K.\} and Horan, \{Timothy C.\} and Premchendar Nandhikonda and Teske, \{Kelly A.\} and Yuan, \{Nina Y.\} and Marina Sidorko and Revathi Rodali and Cook, \{James M.\} and Lanlan Han and Silvaggi, \{Nicholas R.\} and Bikle, \{Daniel D.\} and Moore, \{Richard G.\} and Singh, \{Rakesh K.\} and Arnold, \{Leggy A.\}",

year = "2015",

month = nov,

language = "English",

volume = "35",

pages = "6001--6007",

journal = "Anticancer Research",

issn = "0250-7005",

number = "11",

}

TY - JOUR

T1 - Antitumor activity of 3-indolylmethanamines 31b and ps121912

AU - Guthrie, Margaret L.

AU - Sidhu, Preetpal S.

AU - Hill, Emily K.

AU - Horan, Timothy C.

AU - Nandhikonda, Premchendar

AU - Teske, Kelly A.

AU - Yuan, Nina Y.

AU - Sidorko, Marina

AU - Rodali, Revathi

AU - Cook, James M.

AU - Han, Lanlan

AU - Silvaggi, Nicholas R.

AU - Bikle, Daniel D.

AU - Moore, Richard G.

AU - Singh, Rakesh K.

AU - Arnold, Leggy A.

PY - 2015/11

Y1 - 2015/11

N2 - Aim: To investigate the in vivo effects of 3-indolylmethanamines 31B and PS121912 in treating ovarian cancer and leukemia, respectively. Materials and Methods: Terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and western blotting were applied to demonstrate the induction of apoptosis. Xenografted mice were investigated to show the antitumor effects of 3-indolylmethanamines. 13CNuclear magnetic resource (NMR) and western blotting were used to demonstrate inhibition of glucose metabolism. Results: 31B inhibited ovarian cancer cell proliferation and activated caspase-3, cleaved poly (ADP-ribose) polymerase 1 (PARP1), and phosphorylated mitogen-activated protein kinases (MAPK), JUN N-terminal kinase/stress-activated protein kinase (JNK/SAPK) and p38. 31B reduced ovarian cancer xenograft tumor growth and PS121912 inhibited the growth of HL-60-derived xenografts without any sign of toxicity. Compound 31B inhibited de novo glycolysis and lipogenesis mediated by the reduction of fatty acid synthase and lactate dehydrogenase-A expression. Conclusion: 3-Indolylmethanamines represent a new class of antitumor agents. We have shown for the first time the in vivo anticancer effects of 3-indolylmethanamines 31B and PS121912.

AB - Aim: To investigate the in vivo effects of 3-indolylmethanamines 31B and PS121912 in treating ovarian cancer and leukemia, respectively. Materials and Methods: Terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and western blotting were applied to demonstrate the induction of apoptosis. Xenografted mice were investigated to show the antitumor effects of 3-indolylmethanamines. 13CNuclear magnetic resource (NMR) and western blotting were used to demonstrate inhibition of glucose metabolism. Results: 31B inhibited ovarian cancer cell proliferation and activated caspase-3, cleaved poly (ADP-ribose) polymerase 1 (PARP1), and phosphorylated mitogen-activated protein kinases (MAPK), JUN N-terminal kinase/stress-activated protein kinase (JNK/SAPK) and p38. 31B reduced ovarian cancer xenograft tumor growth and PS121912 inhibited the growth of HL-60-derived xenografts without any sign of toxicity. Compound 31B inhibited de novo glycolysis and lipogenesis mediated by the reduction of fatty acid synthase and lactate dehydrogenase-A expression. Conclusion: 3-Indolylmethanamines represent a new class of antitumor agents. We have shown for the first time the in vivo anticancer effects of 3-indolylmethanamines 31B and PS121912.

KW - 3-Indolylmethanamine

KW - Leukemia

KW - Ovarian cancer

UR - https://www.scopus.com/pages/publications/84946067038

M3 - Article

C2 - 26504023

AN - SCOPUS:84946067038

SN - 0250-7005

VL - 35

SP - 6001

EP - 6007

JO - Anticancer Research

JF - Anticancer Research

IS - 11

ER -

Antitumor activity of 3-indolylmethanamines 31b and ps121912

Abstract

UN SDGs

Keywords

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