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    • 6. 发明授权
    • Diarylalkanes as potent inhibitors of binuclear enzymes
    • 二芳基烷烃作为双核酶的有效抑制剂
    • US08729136B2
    • 2014-05-20
    • US13707270
    • 2012-12-06
    • Unigen, Inc.
    • Qi JiaJi-Fu Zhao
    • A61K31/75
    • A61K8/347A61K8/31A61K8/4973A61K8/97A61K31/015A61K31/05A61K31/085A61K31/09A61K31/357A61K31/40A61K31/704A61K2800/782A61Q19/02C07C39/15C07C39/367C07C41/26C07C41/32C07C43/23C07C45/673C07C49/835C07C215/74C07D321/12Y02A50/406Y02A50/411
    • The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.
    • 本发明实现了一种将酶抑制测定与化学去除方法结合以鉴别活性植物提取物和特异性抑制双核酶功能的那些提取物中的二芳基烷烃和/或二芳基链烷醇的策略。 包括在本发明中的是由一种或多种二芳基烷烃和/或二芳基链烷醇组成的物质组合物,其抑制双核酶,特别是酪氨酸酶的活性,并且其防止黑色素过量产生。 本发明还提供了抑制双核酶,特别是酪氨酸酶的活性的方法,以及用于预防和治疗与双核酶功能相关的疾病和病症的方法。 本发明还包括一种预防和治疗与其相关的黑色素过量产生及其疾病和病症的方法。 用于预防和治疗与双核酶功能和黑色素过量产生相关的疾病和病症的方法包括向有需要的宿主施用有效量的包含一种或多种二芳基烷烃和/或二芳基链烷醇的组合物,所述二芳基烷烃和/或二芳基链烷醇合成和/或分离自 更多的植物和药学上可接受的载体。