| Autor: |
Abou-Issa H; Department of Surgery, College of Medicine, The Ohio State University, Columbus 43210, USA. Abou-Issa.1@osu.edu, Curley RW Jr, Alshafie GA, Weiss KL, Clagett-Dame M, Chapman JS, Mershon SM |
| Jazyk: |
angličtina |
| Zdroj: |
Anticancer research [Anticancer Res] 2001 Nov-Dec; Vol. 21 (6A), pp. 3839-44. |
| Abstrakt: |
The antitumor effects of N-(4-hydroxyphenyl)retinamide (4-HPR), and its stable C-linked analog, 4-hydroxybenzylretinone (4-HBR) on the regression of established 7,12-dimethylbenz(a)anthracene(DMBA)-induced rat mammary tumors were compared. 4-HBR is a stable and nonhydroyzable derivative which cannot be converted in vivo to retinoic acid (RA). The results indicate that 4-HBR decreased mammary tumor volumes to the same extent as equimolar concentration (2 mmol/kg diet) of 4-HPR (-45% for 4-HBR vs. -42% for 4-HPR, p<0.01). Both 4-HPR and 4-HBR bind very poorly to nuclear retinoid receptors RARs and RXRs. The similarity of physicochemical properties of 4-HPR and 4-HBR as well as their equal antitumor potency suggests that 4-HPR like 4-HBR, is acting directly rather than through hydrolysis to free RA. Treatment with 4-HPR caused an almost 65% decrease in serum retinol levels. These results suggest that 4-HBR may have a significant chemotherapeutic advantage over 4-HPR, as the nonhydrolyzable analog may not cause night blindness which occurs as a significant side effect of 4-HPR usage. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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