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Chemotherapeutic evaluation of 4-hydroxybenzylretinone (4-HBR), a nonhydrolyzable C-linked analog of N-(4-hydroxyphenyl) retinamide (4-HPR) against mammary carcinogenesis.

Abstract
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.
AuthorsH Abou-Issa, R W Curley Jr, G A Alshafie, K L Weiss, M Clagett-Dame, J S Chapman, S M Mershon
JournalAnticancer research (Anticancer Res) 2001 Nov-Dec Vol. 21 Issue 6A Pg. 3839-44 ISSN: 0250-7005 [Print] Greece
PMID11911255 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • 4-hydroxybenzylretinone
  • Anticarcinogenic Agents
  • Antineoplastic Agents
  • Carcinogens
  • Receptors, Retinoic Acid
  • Vitamin A
  • Fenretinide
  • 9,10-Dimethyl-1,2-benzanthracene
Topics
  • 9,10-Dimethyl-1,2-benzanthracene
  • Animals
  • Anticarcinogenic Agents (metabolism, pharmacology)
  • Antineoplastic Agents (metabolism, pharmacology)
  • Carcinogens
  • Female
  • Fenretinide (analogs & derivatives, metabolism, pharmacology)
  • Mammary Neoplasms, Experimental (chemically induced, drug therapy, metabolism)
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Retinoic Acid (metabolism)
  • Vitamin A (analogs & derivatives, blood, metabolism, pharmacology)

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