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Abstract #17648 Published in IGR 9-2
Synthesis and ocular hypotensive activity of magnolol
Huang W-H; Lin I-H; Tan K-I; Chiang C-H; Lee A-RChinese Pharmaceutical Journal 2006; 58: 115-122
A facile one-step synthesis of naturally occurring magnolol under a mild condition was attainable by mixing 2,2'-biphenol and allyl bromide in the presence of copper(II) chloride and an appropriate amount of water. After being vigorously stirred and heated to reflux for 10 hr, the crude product was purified by column chromatography and recrystallization. The physico-chemical properties of synthetic magnolol were identical to those of the natural compound isolated from the cortex of Magnolia officinali. This method, the yield improving up to 50%, proved to be superior for the pilot-plant purpose. Synthetic magnolol was investigated in normal tensive rabbit eyes for determining the potential intraocular pressure (IOP) lowering effect. Our results showed that aftter topical administration of aqueous 0.5% magnolol in rabbit eyes, it demonstrated a significant activity to depress IOP with a potency comparable to timolol and the duration of the effect could last for more than 4 hr for single instillation. Thus, magnolol, for the fist time, was shown to possess potential application in the treatment of glaucoma.
Dr. A.-R. Lee, School of Pharmacy, National Defense Medical Center, Taipei, Taiwan
Classification:
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
