Design of Soymetide-4 Derivatives to Potentiate the Anti-alopecia Effect
Design of Soymetide-4 Derivatives to Potentiate the Anti-alopecia Effect
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Soymetide-4 衍生物的设计以增强抗脱发效果
DOI：
10.1271/bbb.68.1139
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
M. Yoshikawa
中科院分区：
文献类型：
--
作者：
T. Tsuruki;M. Yoshikawa
大豆蛋白肽-4（soymetide-4，MITL）是一种来源于大豆β-伴大豆球蛋白α′亚基的N-甲酰-甲硫氨酰-亮氨酰-苯丙氨酸（fMLP）激动肽，经口给药后，可刺激人多形核白细胞的吞噬功能，并抑制抗癌药物依托泊苷诱导的新生大鼠脱发。我们发现，fMLP受体的亲和力和吞噬刺激活性的soymetide-4增强Thr 3与疏水残基的替代。在所合成的衍生物中，[Trp]3-soymetide-4（MIWL）是最有效的，在受体亲和力和吞噬刺激活性方面分别比soymetide-4强180和130倍。口服给药后，[Trp]3-soymetide-4的抗脱发作用比soymetide-4大约3倍。
Previously, we found that soymetide-4 (MITL), an N-formyl-methionyl-leucyl-phenylalanine (fMLP) agonist peptide derived from soybean β-conglycinin α′ subunit, stimulated phagocytosis of human polymorphonuclear leukocytes, and inhibited alopecia induced by etoposide, an anticancer drug, in neonatal rats after oral administration. We found that the fMLP receptor affinity and phagocytosis-stimulating activity of soymetide-4 was potentiated by replacement of Thr3 with hydrophobic residues. Among the derivatives synthesized, [Trp]3-soymetide-4 (MIWL) was the most potent, stronger by 180 and 130 times than soymetide-4 in receptor affinity and phagocytosis-stimulating activity, respectively. The anti-alopecia effect of [Trp]3-soymetide-4 was about 3 times larger than that of soymetide-4 after oral administration.
影响因子：
56.9
作者：
STEINKAMP, JA;WILSON, JS;STEWART, CC
通讯作者：
STEWART, CC