Tetra-O-methyl nordihydroguaiaretic acid, an inhibitor of Sp1-mediated survivin transcription, induces apoptosis and acts synergistically with chemo-radiotherapy in glioblastoma cells

Castro‐Gamero, Angel Mauricio; Borges, Kleiton Silva; Moreno, Daniel Antunes; Suazo, Veridiana Kill; Fujinami, Mayara Missono; Queiroz, Rosane Pg; Oliveira, Harley Francisco de; Carlotti, Carlos Gilberto; Scrideli, Carlos Alberto; Tone, Luíz Gonzaga

doi:10.1186/1753-6561-7-s2-p8

Cited by 2 publications

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“…Apoptosis has been suggested as one of the mechanisms underlying the inhibition of NDGA and its derivatives in multiple tumors. 4,16,17,35,36 However, we found that similar to Nordy, NDGA-P21 had little effects on apoptosis. The results suggest different structure modification of NDGA leads an alternative mechanism for inhibition of tumor cells.…”

Section: Discussionmentioning

confidence: 50%

NDGA-P21, a novel derivative of nordihydroguaiaretic acid, inhibits glioma cell proliferation and stemness

Zhao

Lin

et al. 2017

Laboratory Investigation

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Nordihydroguaiaretic acid (NDGA) and its synthetic chiral analog dl-nordihydroguaiaretic acid (Nordy) show collective benefits in anti-tumor, and defending against viral and bacterial infections. Here, we synthetized a new derivative-NDGA-P21 based on NDGA structure. Regardless of the structural similarity, NDGA-P21 exhibited stronger capability in suppression of glioblastoma (GBM) cell growth as compared to Nordy. Mechanically, NDGA-P21 is able to arrest cell cycle of GBM cells in G0/G1 phase, and to block cell proliferation sequentially. It is important to note that NDGA-P21 is able to impair the stemness of glioma stem-like cells (GSLCs) via measurement of colony formation and sphere formation. Taken together, the novel NDGA-based compound NDGA-P21 exhibits potential therty -20 apeutic implications through inhibiting proliferation of glioma cells and self-renewal capability of GSLCs.

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Section: Discussionmentioning

confidence: 50%

NDGA-P21, a novel derivative of nordihydroguaiaretic acid, inhibits glioma cell proliferation and stemness

Zhao

Lin

et al. 2017

Laboratory Investigation

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“…; Castro‐Gamero et al. ), concentrations that produce a significant activation of TRPA1. By contrast to the inhibitory effects of Sp1 inhibition on cell growth, recent findings indicate that activation of TRPA1 may promote the survival of small cell lung cancer cells (SCLC, Schaefer et al.…”

Section: Discussionmentioning

confidence: 99%

Nordihydroguaiaretic acid activates hTRPA1 and modulates behavioral responses to noxious cold in mice

Redmond

Camo

Mitchell

et al. 2014

Pharmacology Res & Perspec

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Nordihydroguaiaretic acid (NDGA) is a major biologically active component of the creosote bush, Larrea tridentate, widely used in unregulated therapies. NDGA is a lipoxygenase inhibitor while a derivative, terameprocol, has been trialed as a chemotherapeutic agent. When investigating fatty acid activation of the human transient receptor potential cation channel subfamily A, member 1 (hTRPA1), we found that NDGA activated the channel. Here we investigate the actions of NDGA and terameprocol at hTRPA1 and the consequences of this for noxious cold sensitivity in mice. hTRPA1 was stably expressed in HEK 293 cells (HEK 293-TRPA1) and channel activity examined by measuring changes in intracellular calcium ([Ca]i) using a fluorescent dye and activation of membrane currents using patch clamp electrophysiology. The effects of local NDGA and terameprocol application on acetone-induced paw flinching were examined in mice. NDGA (pEC50 of 5.4 ± 0.1, maximum change in fluorescence of 385 ± 30%) and terameprocol (pEC50 4.5 ± 0.2, maximum 550 ± 75%) increased [Ca]i in HEK 293-hTRPA1 cells. NDGA also induced an increase in membrane conductance in HEK 293-hTRPA1 cells. These effects were prevented by the TRPA1 antagonist HC-030031, and were dependent on the presence of Cys621, Cys 641, and Cys 665 in hTRPA1. Neither NDGA nor terameprocol alone produced spontaneous pain behaviors in mice after hind paw injection, but both enhanced responses to acetone. NDGA and terameprocol are efficacious activators of TRPA1. NDGA should be used with care to probe lipoxygenase involvement in nociception while TRPA1 activity should be considered when considering use of these drugs in humans.

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Tetra-O-methyl nordihydroguaiaretic acid, an inhibitor of Sp1-mediated survivin transcription, induces apoptosis and acts synergistically with chemo-radiotherapy in glioblastoma cells

Cited by 2 publications

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NDGA-P21, a novel derivative of nordihydroguaiaretic acid, inhibits glioma cell proliferation and stemness

NDGA-P21, a novel derivative of nordihydroguaiaretic acid, inhibits glioma cell proliferation and stemness

Nordihydroguaiaretic acid activates hTRPA1 and modulates behavioral responses to noxious cold in mice

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