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

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

Keywords

3-Indolylmethanamine
Leukemia
Ovarian cancer

UN SDGs

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

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@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 - http://www.scopus.com/inward/record.url?scp=84946067038&partnerID=8YFLogxK

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

Keywords

UN SDGs

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