Department of Organic Chemistry, Faculty of Science, The University of Yaounde I, Yaounde 812, Cameroon.
Department of Chemical Engineering, School of Chemical Engineering and Mineral Industries, University of Ngaoundere, Ngaoundere 454, Cameroon.
Molecules. 2023 Jun 16;28(12):4802. doi: 10.3390/molecules28124802.
is a tropical plant noticeable for its variegated leaves and exploited for various medicinal purposes. In this study, seven compounds, including three furanolabdane diterpenoids, i.e., Hypopurin E, Hypopurin A and Hypopurin B, as well as with Lupeol, β-sitosterol 3--β-d-glucopyranoside, stigmasterol 3--β-d-glucopyranoside and a mixture of β-sitosterol and stigmasterol, were isolated from , and their structures were deduced from ESI-TOF-MS, HR-ESI-TOF-MS, 1D and 2D NMR experiments. The compounds were evaluated for their anticholinesterase activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BchE), as well as their antidiabetic potential through inhibition of α-glucosidase and α-amylase. For AChE inhibition, no sample had IC50 within tested concentrations, though the most potent was Hypopurin A, which had a percentage inhibition of 40.18 ± 0.75%, compared to 85.91 ± 0.58% for galantamine, at 100 µg/mL. BChE was more susceptible to the leaves extract (IC = 58.21 ± 0.65 µg/mL), stem extract (IC = 67.05 ± 0.82 µg/mL), Hypopurin A (IC = 58.00 ± 0.90 µg/mL), Hypopurin B (IC = 67.05 ± 0.92 µg/mL) and Hypopurin E (IC = 86.90 ± 0.76 µg/mL). In the antidiabetic assay, the furanolabdane diterpenoids, lupeol and the extracts had moderate to good activities. Against α-glucosidase, lupeol, Hypopurin E, Hypopurin A and Hypopurin B had appreciable activities but the leaves (IC = 48.90 ± 0.17 µg/mL) and stem (IC = 45.61 ± 0.56 µg/mL) extracts were more active than the pure compounds. In the α-amylase assay, stem extract (IC = 64.47 ± 0.78 µg/mL), Hypopurin A (IC = 60.68 ± 0.55 µg/mL) and Hypopurin B (IC = 69.51 ± 1.30 µg/mL) had moderate activities compared to the standard acarbose (IC = 32.25 ± 0.36 µg/mL). Molecular docking was performed to determine the binding modes and free binding energies of Hypopurin E, Hypopurin A and Hypopurin B in relation to the enzymes and decipher the structure-activity relationship. The results indicated that and its compounds could, in general, be used in the development of therapies for Alzheimer's disease and diabetes.
是一种热带植物，因其斑驳的叶子而引人注目，并被用于各种药用目的。在这项研究中，从 中分离出了 7 种化合物，包括 3 种呋喃 labdane 二萜类化合物，即 Hypopurin E、Hypopurin A 和 Hypopurin B，以及羽扇豆醇、β-谷甾醇 3--β-d-吡喃葡萄糖苷、豆甾醇 3--β-d-吡喃葡萄糖苷和 β-谷甾醇和豆甾醇的混合物，它们的结构是通过 ESI-TOF-MS、HR-ESI-TOF-MS、1D 和 2D NMR 实验推断出来的。评估了这些化合物对乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BchE) 的抗胆碱酯酶活性，以及通过抑制α-葡萄糖苷酶和α-淀粉酶抑制的抗糖尿病潜力。对于 AChE 抑制，没有样品在测试浓度内具有 IC50，尽管最有效的是 Hypopurin A，在 100 µg/mL 时，其抑制率为 40.18 ± 0.75%，而加兰他敏为 85.91 ± 0.58%。BChE 对叶片提取物（IC = 58.21 ± 0.65 µg/mL）、茎提取物（IC = 67.05 ± 0.82 µg/mL）、Hypopurin A（IC = 58.00 ± 0.90 µg/mL）、Hypopurin B（IC = 67.05 ± 0.92 µg/mL）和 Hypopurin E（IC = 86.90 ± 0.76 µg/mL）更为敏感。在抗糖尿病测定中，呋喃 labdane 二萜类化合物、羽扇豆醇和提取物具有中等至良好的活性。对于 α-葡萄糖苷酶，羽扇豆醇、Hypopurin E、Hypopurin A 和 Hypopurin B 具有可观的活性，但叶片（IC = 48.90 ± 0.17 µg/mL）和茎（IC = 45.61 ± 0.56 µg/mL）提取物比纯化合物更活跃。在 α-淀粉酶测定中，与标准阿卡波糖（IC = 32.25 ± 0.36 µg/mL）相比，茎提取物（IC = 64.47 ± 0.78 µg/mL）、Hypopurin A（IC = 60.68 ± 0.55 µg/mL）和 Hypopurin B（IC = 69.51 ± 1.30 µg/mL）具有中等活性。进行了分子对接以确定 Hypopurin E、Hypopurin A 和 Hypopurin B 与酶的结合模式和自由结合能，并破译结构-活性关系。结果表明， 和其化合物一般可用于治疗阿尔茨海默病和糖尿病的药物开发。
