New hybrid bromopyridine-chalcones as in vivo phase II enzyme inducers: potential chemopreventive agents

MedChemComm ◽  
2016 ◽  
Vol 7 (12) ◽  
pp. 2395-2409 ◽  
Author(s):  
Mauricio Cabrera ◽  
Hugo Cerecetto ◽  
Mercedes González
Keyword(s):  
Phase Ii ◽  
Chemopreventive Agents ◽  
Phase Ii Enzyme ◽  
Potential Cancer ◽  
Enzyme Inducers

We report the synthesis of eighteen new potential cancer chemopreventive agents, structurally designed to combine (naphtho)chalcone and (bromo)pyridine skeletons.

scholarly journals In Vitro and in Vivo Regulation of Antioxidant Response Element-Dependent Gene Expression by Estrogens

Endocrinology ◽  
2004 ◽  
Vol 145 (1) ◽  
pp. 311-317 ◽  
Author(s):  
P. J. Ansell ◽  
C. Espinosa-Nicholas ◽  
E. M. Curran ◽  
B. M. Judy ◽  
B. J. Philips ◽  
...  
Keyword(s):  
Gene Expression ◽  
Phase Ii ◽  
Enzyme Activities ◽  
Antioxidant Response ◽  
Quinone Reductase ◽  
Antioxidant Response Element ◽  
Phase Ii Enzyme ◽  
17Β Estradiol

Abstract Understanding estrogen’s regulation of phase II detoxification enzymes is important in explaining how estrogen exposure increases the risk of developing certain cancers. Phase II enzymes such as glutathione-S-transferases (GST) and quinone reductase protect against developing chemically induced cancers by metabolizing reactive oxygen species. Phase II enzyme expression is regulated by a cis-acting DNA sequence, the antioxidant response element (ARE). It has previously been reported that several antiestrogens, but not 17β-estradiol, could regulate ARE-mediated gene transcription. Our goal was to determine whether additional estrogenic compounds could regulate ARE-mediated gene expression both in vitro and in vivo. We discovered that physiological concentrations (10 nm) of 17β-estradiol repressed GST Ya ARE-dependent gene expression in vitro. Treatment with other endogenous and anti-, xeno-, and phytoestrogens showed that estrogen receptor/ARE signaling is ligand, receptor subtype, and cell type specific. Additionally, GST and quinone reductase activities were significantly lowered in a dose-dependent manner after 17β-estradiol exposure in the uteri of mice. In conclusion, we have shown that 17β-estradiol, and other estrogens, down-regulate phase II enzyme activities. We propose estrogen-mediated repression of phase II enzyme activities may increase cellular oxidative DNA damage that ultimately can result in the formation of cancer in some estrogen-responsive tissues.

In vivo phase II-enzymes inducers, as potential chemopreventive agents, based on the chalcone and furoxan skeletons

2016 ◽  
Vol 24 (8) ◽  
pp. 1665-1674 ◽  
Author(s):  
Mauricio Cabrera ◽  
Ignacio Mastandrea ◽  
Gabriel Otero ◽  
Hugo Cerecetto ◽  
Mercedes González
Keyword(s):  
Phase Ii ◽  
Chemopreventive Agents ◽  
Phase Ii Enzymes

Virtual Reality and In Vivo Exposure for Fear of Flying: A Phase II Replication Study

2006 ◽  
Author(s):  
Ken Graap ◽  
Barbara O. Rothbaum ◽  
Page Anderson ◽  
Elana Zimand ◽  
Larry Hodges ◽  
...  
Keyword(s):  
Virtual Reality ◽  
Phase Ii ◽  
Replication Study ◽  
Fear Of Flying

Pleiotropic Effect of Mahanine and Girinimbine Analogs: Anticancer Mechanism and its Therapeutic Versatility

2019 ◽  
Vol 18 (14) ◽  
pp. 1983-1990 ◽  
Author(s):  
V. Lenin Maruthanila ◽  
Ramakrishnan Elancheran ◽  
Ajaikumar B. Kunnumakkar ◽  
Senthamaraikannan Kabilan ◽  
Jibon Kotoky
Keyword(s):  
Biological Effects ◽  
Pleiotropic Effect ◽  
In Vivo Evaluation ◽  
Chemopreventive Agents ◽  
Cycle Arrest ◽  
Wide Range ◽  
Anticancer Mechanism ◽  
Metastasis Development

Emerging evidence present credible support in favour of the potential role of mahanine and girinimbine. Non-toxic herbal carbazole alkaloids occur in the edible part of Murraya koenigii, Micromelum minutum, M. zeylanicum, and M. euchrestiolia. Mahanine and girinimbine are the major potent compounds from these species. In fact, they interfered with tumour expansion and metastasis development through down-regulation of apoptotic and antiapoptotic protein, also involved in the stimulation of cell cycle arrest. Consequently, these compounds were well proven for the in-vitro and in vivo evaluation that could be developed as novel agents either alone or as an adjuvant to conventional therapeutics. Therefore, mahanine and girinimbine analogs have the potential to be the promising chemopreventive agents for the tumour recurrence and the treatment of human malignancies. In this review, an updated wide-range of pleiotropic anticancer and biological effects induction by mahanine and girinimbine against cancer cells were deeply summarized.

scholarly journals Phase I/II and Phase II Studies of Targeted Gene Delivery In Vivo: Intravenous Rexin-G for Chemotherapy-resistant Sarcoma and Osteosarcoma

2009 ◽  
Vol 17 (9) ◽  
pp. 1651-1657 ◽  
Author(s):  
Sant P Chawla ◽  
Victoria S Chua ◽  
Lita Fernandez ◽  
Doris Quon ◽  
Andreh Saralou ◽  
...  
Keyword(s):  
Gene Delivery ◽  
Phase I ◽  
Phase Ii ◽  
Targeted Gene Delivery ◽  
Phase Ii Studies

Effects of Ofloxacin Administration on the Reliability of Urine Glucose Testing

1996 ◽  
Vol 30 (5) ◽  
pp. 469-472
Author(s):  
Tsong-Mei Tsai ◽  
Brian F Shea ◽  
Paul F Souney ◽  
Fred G Volinsky ◽  
Joseph M Scavone ◽  
...  
Keyword(s):  
Phase I ◽  
Phase Ii ◽  
Tertiary Care ◽  
Urine Samples ◽  
Care Hospital ◽  
Open Label ◽  
Urine Glucose ◽  
Glucose Testing

OBJECTIVE: TO study the effects of ofloxacin on the reliability of urine glucose testing. DESIGN: Open-label, nonrandomized. SETTING: A university-affiliated tertiary care hospital, ambulatory clinic. PARTICIPANTS: Ten healthy volunteers (8 men and 2 women) aged 22-39 years. MAIN OUTCOME MEASURES: Phase I (in vitro) involved the addition of selected amounts of ofloxacin to a set of standard 50-mL urine samples prepared to simulate glycosuria. Phase II (in vivo) involved the oral administration of ofloxacin 400 mg to 10 subjects. Urine was collected: (1) immediately predose, (2) pooled 0–4 hours postdose, and (3) pooled 4–8 hours postdose. Known glucose concentrations were then added to these samples. Clinitest and Diastix tests were performed on all samples. The accuracy of these tests in determining glucose concentrations was compared among urine samples taken before and after ofloxacin dosing. RESULTS: None of the ofloxacin concentrations in phase I (0,25,50, 100, 200,400, and 800 μg/mL) influenced these testing methods at the urine glucose concentrations of 0.0%, 0.5%, 1%, and 2%. Likewise, the accuracy of these two tests was unaffected by ofloxacin administration in phase II. CONCLUSIONS: In single-dose administration, ofloxacin does not interfere with Clinitest or Diastix for determining urine glucose concentrations. Supported by a grant from the RW Johnson Pharmaceutical Research Institute. Presented in abstract form at the American College of Clinical Pharmacy 1994 Winter Practice and Research Forum, February 6–9, 1994, San Diego. CA.

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