Abstract |
The antihyperplastic activity of beta- retinoic acid (RA) and nine synthetic analogues ( retinoids) was examined in organ cultures of mouse prostate made hyperplastic by treatment with N-methyl-N'-nitro-N-nitrosoguanidine ( MNNG). After 8 or 10 days, when most explants developed hyperplasia, the carcinogen was withdrawn and explants were incubated in control medium and medium containing different concentrations of a retinoid. The antimitotic activity of retinoids was compared with that of RA. Different retinoids produced variable degrees of mitotic inhibition in the hyperplastic prostate epithelium. The methylketo cyclopentenyl and 1-methoxyethyl cyclopentenyl analogues of RA were at least 50-fold more active than RA in reversing MNNG-induced hyperplasia. The trimethylmethoxyphenyl analogue of RA and retinyl methyl ether were significantly more active than RA. Three analogues, N-acetyiretinylamine, retinal acetyl hydrazone, and retinal oxime, were as active as RA. The chlorotrimethylphenyl analogue showed less activity than RA, and alpha- retinyl acetate was completely devoid of mitotic inhibitory activity.
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Authors | D P Chopra, L J Wilkoff |
Journal | Journal of the National Cancer Institute
(J Natl Cancer Inst)
Vol. 58
Issue 4
Pg. 923-30
(Apr 1977)
ISSN: 0027-8874 [Print] United States |
PMID | 557570
(Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
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Chemical References |
- Vitamin A
- Methylnitronitrosoguanidine
- Tretinoin
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Topics |
- Cell Division
(drug effects)
- Epithelium
(drug effects, pathology)
- Hyperplasia
(chemically induced)
- Male
- Methylnitronitrosoguanidine
(antagonists & inhibitors)
- Neoplasms, Experimental
(drug therapy)
- Organ Culture Techniques
- Precancerous Conditions
(drug therapy)
- Prostate
(drug effects, pathology)
- Prostatic Neoplasms
(drug therapy)
- Structure-Activity Relationship
- Tretinoin
(pharmacology)
- Vitamin A
(analogs & derivatives, pharmacology)
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