Preclinical factors influencing the relative contributions of Phase I and II enzymes to the metabolism of the experimental anti-cancer drug 5,6-dimethylxanthenone-4-acetic acid

2003 ◽  
Vol 65 (1) ◽  
pp. 109-120 ◽  
Author(s):  
Shufeng Zhou ◽  
Philip Kestell ◽  
Bruce C Baguley ◽  
James W Paxton
Keyword(s):  
Acetic Acid ◽  
Phase I ◽  
Cancer Drug ◽  
Factors Influencing ◽  
Anti Cancer ◽  
Phase I And Ii

scholarly journals Protective Effects of Myricetin on Benzo[a]pyrene-Induced 8-Hydroxy-2′-Deoxyguanosine and BPDE-DNA Adduct

Antioxidants ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 446
Author(s):  
Seung-Cheol Jee ◽  
Min Kim ◽  
Kyeong Seok Kim ◽  
Hyung-Sik Kim ◽  
Jung-Suk Sung
Keyword(s):  
Phase I ◽  
Oxidative Dna Damage ◽  
Biological Activities ◽  
Adduct Formation ◽  
Dna Adduct ◽  
Protective Effects ◽  
Glutathione S Transferase ◽  
Anti Cancer ◽  
Natural Foods ◽  
Phase I And Ii

Benzo[a]pyrene (B[a]P), a group 1 carcinogen, induces mutagenic DNA adducts. Myricetin is present in many natural foods with diverse biological activities, such as anti-oxidative and anti-cancer activities. The aim of this study was to investigate the protective effects of myricetin against B[a]P-induced toxicity. Treatment of B[a]P induced cytotoxicity on HepG2 cells, whereas co-treatment of myricetin with B[a]P reduced the formation of the B[a]P-7,8-dihydrodiol-9,10-epoxide (BPDE)-DNA adduct, which recovered cell viability. Furthermore, we found a protective effect of myricetin against B[a]P-induced genotoxicity in rats, via myricetin-induced inhibition of 8-hydroxy-2′-deoxyguanosine (8-OHdG) and BPDE-DNA adduct formation in the liver, kidney, colon, and stomach tissue. This inhibition was more prominent in the liver than in other tissues. Correspondingly, myricetin regulated the phase I and II enzymes that inhibit B[a]P metabolism and B[a]P metabolites conjugated with DNA by reducing and inducing CYP1A1 and glutathione S-transferase (GST) expression, respectively. Taken together, this showed that myricetin attenuated B[a]P-induced genotoxicity via regulation of phase I and II enzymes. Our results suggest that myricetin is anti-genotoxic, and prevents oxidative DNA damage and BPDE-DNA adduct formation via regulation of phase I and II enzymes.

Transport of the investigational anti-cancer drug 5,6-dimethylxanthenone-4-acetic acid and its acyl glucuronide by human intestinal Caco-2 cells

2005 ◽  
Vol 24 (5) ◽  
pp. 513-524 ◽  
Author(s):  
Shufeng Zhou ◽  
Xia Feng ◽  
Philip Kestell ◽  
James W. Paxton ◽  
Bruce C. Baguley ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Cancer Drug ◽  
Acyl Glucuronide ◽  
Anti Cancer

Phase I dose escalating study of PEG-PGA and DON (GlutaDON): A new amino acid depleting anti cancer drug approach

2004 ◽  
Vol 22 (14_suppl) ◽  
pp. 3175-3175
Author(s):  
C. Unger ◽  
F. Baas ◽  
S. Wiessner ◽  
S. Steinbild ◽  
M. Medinger ◽  
...  
Keyword(s):  
Amino Acid ◽  
Phase I ◽  
Cancer Drug ◽  
Anti Cancer ◽  
Dose Escalating

Phase I dose escalating study of PEG-PGA and DON (GlutaDON): A new amino acid depleting anti cancer drug approach

2004 ◽  
Vol 22 (14_suppl) ◽  
pp. 3175-3175 ◽  
Author(s):  
C. Unger ◽  
F. Baas ◽  
S. Wiessner ◽  
S. Steinbild ◽  
M. Medinger ◽  
...  
Keyword(s):  
Amino Acid ◽  
Phase I ◽  
Cancer Drug ◽  
Anti Cancer ◽  
Dose Escalating
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