THE STRUCTURE-ACTIVITY RELATIONSHIP BETWEEN SYNTHETIC BUTYLIDENEPHTHALIDE DERIVATIVES REGARDING THE COMPETENCE AND PROGRESSION OF INHIBITION IN PRIMARY CULTURES PROLIFERATION OF MOUSE AORTA SMOOTH-MUSCLE CELLS

Citation
Y. Mimura et al., THE STRUCTURE-ACTIVITY RELATIONSHIP BETWEEN SYNTHETIC BUTYLIDENEPHTHALIDE DERIVATIVES REGARDING THE COMPETENCE AND PROGRESSION OF INHIBITION IN PRIMARY CULTURES PROLIFERATION OF MOUSE AORTA SMOOTH-MUSCLE CELLS, Biological & pharmaceutical bulletin, 18(9), 1995, pp. 1203-1206
Citations number
17
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
0918-6158
Volume
18
Issue
9
Year of publication
1995
Pages
1203 - 1206
Database
ISI
SICI code
0918-6158(1995)18:9<1203:TSRBSB>2.0.ZU;2-0
Abstract
The inhibitory effects of synthetic butylidenephthalide (BP) derivativ es on 10% fetal bovine serum-stimulated proliferation were assayed by measuring the proliferative cell number at an interval of 12 h in prim ary cultures of mouse aorta smooth muscle cells (SMC). Their potencies for the anti-proliferation effect were in the order BP-42 (4,5-dihydr oxy BP) > BP-92 (4,5-dihydroxy butylphthalide) > BP-97 (6,7-dihydroxy- 3-(3-bromo-1-octenyl)-phthalide) > BP-82 (6,7-dihydroxy BP) > BP-86 (5 ,6-dihydroxy BP) > BP-87 (4,5,6-trihydroxy BP) > BP-85 (4,7-dihydroxy BP) > BP-84 (5,7-dihydroxy BP) > BP-4C(3) (4-methoxy propylphthalide) > BP-7 (4-hydroxy BP) > BP-40 (4,5-dimethoxy butylphthalide) > BP-5C(3 ) (4-hydroxy propylphthalide). We divided these anti-proliferative eff ects into anti-competence and anti-progression effects by using a conv enient assay. BP-42 had the greatest potency in used phthalides for co mpetence inhibition of the SMC proliferation. BP-92 had small potency for competence inhibition. BP-97 had greater potency for competence in hibition than BP-82. These results demonstrated that the anti-prolifer ative effect of BP-42 was greatest in used phthalides in primary cultu res of vascular SMC. The 4,5-dihydroxy group and 3-butylidene or 3-(3- bromo-1-octenyl) group in these synthetic BP derivatives contributed t o the anti-competence effect on SMC. BP-42 may become a prototype of a n anti-atherosclerotic drug.