Evangelakou Zoi, Schwaiger Stefan, Gianniou Despoina D, Trougakos Ioannis P, Stuppner Hermann
Department of Cell Biology and Biophysics, Faculty of Biology, National and Kapodistrian University of Athens, Athens, 15784, Greece.
Institute of Pharmacy/Pharmacognosy, University of Innsbruck, CCB, Innrain 80-82, 6020, Innsbruck, Austria.
Chem Biodivers. 2025 Mar;22(3):e202401848. doi: 10.1002/cbdv.202401848. Epub 2024 Nov 23.
Kadsurenin F, a natural neolignan-type compound, has been described as a constituent of various members of the Lauraceae family such as Aniba spp. or Nectandra spp., but can also be found in various Piper species such as Piper kadsura Ohwi (Piperaceae). This species is traditionally used to treat asthma, rheumatic pain, arthritis, and digestive problems. Recently, several studies have highlighted the significant anti-inflammatory potential of P. kadsura extracts and secondary metabolites. Here, we report the isolation of kadsurenin F as an active component of P. kadsura. We found that kadsurenin F increases oxidative load and suppresses proteasome functionality in normal diploid human fibroblasts, and after administration in Drosophila flies. Moreover, kadsurenin F likely possesses anti-inflammatory properties, as apart from suppressing proteasome activity, it reversed inflammatory phenotypes and inhibited NO production in RAW 264.7 macrophage cells when administered in parallel with LPS. Our findings suggest that the kadsurenin F scaffold can be used for the development of novel highly bioactive proteasome inhibitors and/or anti-inflammatory compounds.
海风藤素F是一种天然新木脂素类化合物，已被描述为樟科各种植物的成分，如秘鲁香脂属或莲叶桐属植物，但也可以在各种胡椒属植物中找到，如海风藤（胡椒科）。该物种传统上用于治疗哮喘、风湿性疼痛、关节炎和消化问题。最近，几项研究强调了海风藤提取物和次生代谢产物具有显著的抗炎潜力。在此，我们报告了从海风藤中分离出海风藤素F作为其活性成分。我们发现，海风藤素F在正常二倍体人成纤维细胞以及果蝇体内给药后，会增加氧化负荷并抑制蛋白酶体功能。此外，海风藤素F可能具有抗炎特性，因为除了抑制蛋白酶体活性外，当与脂多糖同时给药时，它能逆转RAW 264.7巨噬细胞中的炎症表型并抑制一氧化氮的产生。我们的研究结果表明，海风藤素F骨架可用于开发新型高生物活性蛋白酶体抑制剂和/或抗炎化合物。
