Faculty of Bioresources and Environmental Science, Ishikawa Prefectural University, 1-308 Suematsu, Nonoichi, Ishikawa, 921-8836, Japan.
Graduate School of Science and Technology, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki, 305-8572, Japan.
J Nat Med. 2023 Jun;77(3):508-515. doi: 10.1007/s11418-023-01693-y. Epub 2023 Mar 18.
Amyloid β (Aβ) is thought to be involved in the pathogenesis of Alzheimer's disease (AD). Aβ aggregation in the brain is considered the cause of AD. Therefore, inhibiting Aβ aggregation and degrading existing Aβ aggregates is a promising approach for the treatment and prevention of the disease. In searching for inhibitors of Aβ42 aggregation, we found that meroterpenoids isolated from Sargassum macrocarpum possess potent inhibitory activities. Therefore, we searched for active compounds from this brown alga and isolated 16 meroterpenoids, which contain three new compounds. The structures of these new compounds were elucidated using two-dimensional nuclear magnetic resonance techniques. Thioflavin-T assay and transmission electron microscopy were used to reveal the inhibitory activity of these compounds against Aβ42 aggregation. All the isolated meroterpenoids were found to be active, and compounds with a hydroquinone structure tended to have stronger activity than those with a quinone structure.
淀粉样蛋白β（Aβ）被认为与阿尔茨海默病（AD）的发病机制有关。大脑中的 Aβ聚集被认为是 AD 的原因。因此，抑制 Aβ聚集和降解现有的 Aβ聚集体是治疗和预防该疾病的有前途的方法。在寻找 Aβ42 聚集抑制剂时，我们发现来自马尾藻的生源二萜具有很强的抑制活性。因此，我们从这种褐藻中寻找活性化合物，并分离出 16 种生源二萜，其中包含 3 种新化合物。这些新化合物的结构通过二维核磁共振技术阐明。噻唑蓝（Thioflavin-T） assay 和透射电子显微镜用于揭示这些化合物对 Aβ42 聚集的抑制活性。所有分离出的生源二萜都具有活性，并且具有氢醌结构的化合物比具有醌结构的化合物具有更强的活性。
