Belaabed Soumia, Khalfaoui Ayoub, Parisi Valentina, Santoro Valentina, Russo Daniela, Ponticelli Maria, Monné Magnus, Rebbas Khellaf, Milella Luigi, Donadio Giuliana
Department of Chemistry, Research Unit, Development of Natural Resources, Bioactive Molecules, Physicochemical and Biological Analysis, University Mentouri, Route Ain ElBey, Constantine 25000, Algeria.
Dipartimento di Farmacia, Università Degli Studi di Salerno, via Giovanni Paolo II 132, Fisciano, 84084 Salerno, Italy.
Plants (Basel). 2023 Jan 9;12(2):301. doi: 10.3390/plants12020301.
Several specialized plant metabolites are reported to be enzyme inhibitors. In this investigation, the phytochemical composition and the biological activity of Desf. were studied. One new lignan (rhanteriol 1) and seven known secondary metabolites were isolated from the aerial parts of by using different chromatographic procedures. The biological properties of the extracts and the new compound were evaluated by measuring their ability to inhibit the cholinesterase and carbohydrate-hydrolyzing enzymes, using cell-free in vitro methods. The new lignan, rhanteriol, was shown to inhibit -amylase and -glucosidase (IC = 46.42 3.25 μM and 26.76 ± 3.29 μM, respectively), as well as butyrylcholinesterase (IC = 10.41 ± 0.03 μM), with an effect comparable to that of the respective standards, acarbose and galantamine. Furthermore, docking studies were performed suggesting the interaction mode of rhanteriol with the active sites of the investigated enzymes. The obtained data demonstrated that the aerial part of could represent a source of active molecules, such as rhanteriol, usable in the development of treatments for preventing or treating type 2 diabetes mellitus and neurodegeneration.
据报道，几种特殊的植物代谢产物是酶抑制剂。在本研究中，对Desf.的植物化学成分和生物活性进行了研究。通过不同的色谱方法，从Desf.的地上部分分离出一种新的木脂素（rhanteriol 1）和七种已知的次生代谢产物。采用无细胞体外方法，通过测量提取物和新化合物抑制胆碱酯酶和碳水化合物水解酶的能力，对其生物学特性进行了评估。新木脂素rhanteriol被证明能抑制α-淀粉酶和α-葡萄糖苷酶（IC分别为46.42±3.25μM和26.76±3.29μM），以及丁酰胆碱酯酶（IC为10.41±0.03μM），其效果与相应标准品阿卡波糖和加兰他敏相当。此外，进行了对接研究，表明rhanteriol与所研究酶的活性位点的相互作用模式。获得的数据表明，Desf.的地上部分可能是活性分子的来源，如rhanteriol，可用于开发预防或治疗2型糖尿病和神经退行性疾病的治疗方法。
