Baker C A, Uno H, Johnson G A
Upjohn Company, Kalamazoo, Mich.
Skin Pharmacol. 1994;7(6):335-9. doi: 10.1159/000211315.
The in vivo model which may be the most accurate for the ability to predict hair growth in humans, and which was utilized in the preclinical development of minoxidil, is the adult stumptailed macaque. Previous reports have suggested that the enzyme activity which accounts for the activation of minoxidil, i.e., minoxidil sulfotransferase, is present in skin. We have demonstrated that scalp skin from the stumptailed macaque contains minoxidil sulfotransferase activity, and further with dissection of that scalp skin into epidermis, dermis and hair follicle, most of sulfotransferase activity was present in the follicle. Sulfotransferase activity in the hair follicle in freeze-dried scalp skin sections from 9 stumptailed macaques ranged from 47 to 84% of the total (mean 61 +/- 12%). Much less minoxidil sulfotransferase activity was measured in the epidermis (mean 18 +/- 11%, with a range of 2-37%) and the dermis (mean 21 +/- 8%, with a range of 4-35%) of these scalp sections. These results indicate that the scalp skin from the stumptailed macaque contains minoxidil sulfotransferase activity and this activity is largely localized in the hair follicle which may account for its ability to stimulate hair growth in this animal model.
成年断尾猕猴体内模型或许是预测人类头发生长能力最准确的模型，米诺地尔临床前开发就采用了该模型。以往报告表明，负责激活米诺地尔的酶活性，即米诺地尔磺基转移酶，存在于皮肤中。我们已证明，断尾猕猴的头皮皮肤含有米诺地尔磺基转移酶活性，进一步将该头皮皮肤解剖为表皮、真皮和毛囊后发现，大部分磺基转移酶活性存在于毛囊中。9只断尾猕猴冻干头皮皮肤切片中毛囊的磺基转移酶活性占总量的47%至84%（平均61±12%）。在这些头皮切片的表皮（平均18±11%，范围为2%至37%）和真皮（平均21±8%，范围为4%至35%）中测得的米诺地尔磺基转移酶活性要低得多。这些结果表明，断尾猕猴的头皮皮肤含有米诺地尔磺基转移酶活性，且该活性主要定位于毛囊，这可能解释了其在该动物模型中刺激头发生长的能力。
