在体外皮肤透的5α-降解酶抑制剂从Tectona grandis L.f. 叶子提取物 叶子提取物
Kamonlak Insumrong1, Neti Waranuch2,3, Kornkanok Ingkaninan4
1Department of Chemistry, Faculty of Science, Naresuan University, Phitsanulok 65000, Thailand.
Molecules (Basel, Switzerland)
|March 13, 2025
概括
Tectona grandis 叶片提取物含有 1 和 2 种化合物,这些化合物对脱发治疗有效. 化合物1显示出更好的皮肤透,表明其潜在的局部配方.
科学领域:
- 药理学和皮肤病学
- 自然产品化学 自然产品化学
背景情况:
- 德克托纳格兰迪斯 (Tectona grandis) 树叶提取物显示出作为5α-还原酶抑制剂的潜力.
- 两种生物活性化合物, (+) -eperua-8,13-dien-15-oic 酸 (1) 和 (+) -eperua-7,13-dien-15-oic 酸 (2),用于标准化T. grandis提取物.
研究的目的:
- 为了研究来自T. grandis叶子提取物中的化合物1和2在体外透到皮肤中的情况.
- 确定化合物1和2的物理化学性质 (分割系数,可溶性).
- 评估不同车辆在皮肤透研究中的适用性.
主要方法:
- 车辆评估的震动瓶法.
- 弗朗茨扩散细胞模型用于体外皮肤透研究.
- 高性能液体染色学 (HPLC) 用于量化化合物1和2.
主要成果:
- 化合物1和2具有较差的水溶性,但在Tween 20的HEPES缓冲器中具有增强的溶性.
- 这两种化合物都是疏水的,分割系数 (log P o/w) 为5.77 ± 0.07对于1和5.66 ± 0.02对于2.
- 在24小时后,化合物1的累积皮肤透率明显高于化合物2.
- 作为增强剂的二醇 (PG) 在受体区中显示了这两种化合物的高累积量.
结论:
- 化合物1的更高的疏水性表明它能透到较高的角层.
- T. grandis 叶子提取物,特别是化合物1,在局部抗脱发产品开发方面表现有前途.
- 这项研究为制定基于T. grandis的脱发疗法提供了关键数据.
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