阿基瑞林(Argireline),又被称为类肉毒杆菌素,是模仿SNAP-25蛋白N端6个氨基酸的寡肽一。阿基瑞林为高端化妆品常用的原料之一,功效主要是减少由面部表情肌收缩造成的皱纹,对额头或眼睛周围的皱纹有理想的祛除效果。 阿基瑞林是一种更安全、更廉价、温和的肉毒杆菌毒素替代品。阿基瑞林参与竞争SNAP-25在融泡复合体的位点,从而影响融泡复合体的形成,导致囊泡不能有效释放神经递质,使肌肉收缩减弱,进而可以放松肌肉、舒缓细纹使肌肤呈现清透无暇,也可以促使细胞再生使肌肤恢复柔软弹性,因此被广泛应用于制备化妆品和保健品。
阿基瑞林(Argireline),又被称为类肉毒杆菌素,是模仿SNAP-25蛋白N端6个氨基酸的寡肽一。阿基瑞林为高端化妆品常用的原料之一,功效主要是减少由面部表情肌收缩造成的皱纹,对额头或眼睛周围的皱纹有理想的祛除效果。另外,它还能促进胶原蛋白的生成,有助于肌肤组织重建。
一种阿基瑞林的制备方法,包括以下步骤:
步骤1:取树脂,活化,得氨基树脂;
步骤2:取步骤1所得氨基树脂,第一逐步偶联胍基保护的L-精氨酸、 胍基保护的L-精氨酸、侧链氨基保护的L-谷氨酰胺,得三肽树脂;
步骤3:取步骤2所得三肽树脂,第二逐步偶联L-甲硫氨酸、侧链羧基 保护的L-谷氨酸、侧链羧基保护的N-乙酰-L-谷氨酸,得六肽树脂;
步骤4:裂解步骤3所得六肽树脂,得第一产品;
步骤5:取步骤4所得第一产品,纯化,即得。
The incubation of Argireline solution in different concentrations with human embryonic kidney HEK-293 (IC 50 of 34.862 μM) and neuroblastoma IMR-32 cells (IC 50 of 68.458 μM)) for 48 h have dose dependent antiproliferative effect. Argireline solution incubated in different concentrations with HSF has a dose-dependent antiproliferative effect on those cells. Cellular proliferation is not effected in Argireline low concentration.
Argireline is applied to the aged mice twice daily for 6 weeks. There is an improvement in the histological structure of skin tissue in the aged mice; the amount of type I collagen fibers increased, while that of type III collagen fibers decreased. Argireline could improve the histological structure of skin tissue and rejuvenate the aging skin.