Siedle Bettina, Hrenn Andrea, Merfort Irmgard
Institute for Pharmaceutical Sciences, Department of Pharmaceutical Biology and Biotechnology, University of Freiburg, Freiburg, Germany.
Planta Med. 2007 May;73(5):401-20. doi: 10.1055/s-2007-967183. Epub 2007 Apr 20.
The imbalance between human neutrophil elastase (HNE) and endogenous serine proteinase inhibitors is considered to cause a variety of HNE-mediated inflammatory disorders. Thus, HNE has been the object of intensive research to find potent inhibitors that target its destructive and pro-inflammatory action. This review focuses on natural compounds which have been demonstrated to inhibit the enzyme itself or its release from neutrophils. Some of the natural compounds discussed here may serve as lead structures suitable to be used for the development of semi-synthetic inhibitors, but up to now none has been found active enough to be directly used in therapy.
人类中性粒细胞弹性蛋白酶（HNE）与内源性丝氨酸蛋白酶抑制剂之间的失衡被认为会引发多种由HNE介导的炎症性疾病。因此，HNE一直是深入研究的对象，旨在寻找能够靶向其破坏作用和促炎作用的有效抑制剂。本综述聚焦于已被证明可抑制该酶本身或其从嗜中性粒细胞释放的天然化合物。这里讨论的一些天然化合物可能作为适合用于开发半合成抑制剂的先导结构，但截至目前，尚未发现有足够活性可直接用于治疗的化合物。
