Centro de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.
Centro de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal; Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal; BioISI - Biosystems & Integrative Sciences Institute, Faculty of Sciences, University of Lisboa, Campo Grande C8, 1749-016 Lisboa, Portugal.
J Ethnopharmacol. 2018 Jun 28;220:147-154. doi: 10.1016/j.jep.2018.04.006. Epub 2018 Apr 4.
Decoctions of Plectranthus species are traditionally ingested after large meals for treatment of food digestion and alcohol abuse.
This study aims at associating the digestion-related ethno-uses of Plectranthus species decoctions to molecular mechanism that might explain them: easing digestion (AChE inhibition) and treating hangover (ADH inhibition) MATERIAL AND METHODS: Decoctions from Plectranthus species were analysed for their alcohol dehydrogenase (ADH) inhibition and acetylcholinesterase (AChE) inhibition, related with alcohol metabolism and intestinal motility, respectively. Identification of the active components was carried out by LC-MS/MS and the docking studies were performed with AChE and the bioactive molecules detected.
All decoctions inhibited ADH activity. This inhibition was correlated with their rosmarinic acid (RA) content, which showed an IC value of 19 μg/mL, similar to the reference inhibitor CuCl. The presence of RA also leads to most decoctions showing AChE inhibiting capacity. P. zuluensis decoction with an IC of 80 μg/mL presented also medioresinol, an even better inhibitor of AChE, as indicated by molecular docking studies. Furthermore, all decoctions tested showed no toxicity towards two human cell lines, and a high capacity to quench free radicals (DPPH), which also play a helpful in the digestive process, related with their RA content.
All activities presented by the RA-rich Plectranthus decoctions support their use in treating digestion disorders and P. barbatus could explain its use also for alleviating hangover symptoms. Medioresinol, which is present in P. zuluensis, exhibited a significant AChE inhibition and may provide, in the future, a new lead for bioactive compounds.
传统上，唇形科假糙苏属植物的煎剂在大餐后服用，用于治疗消化不良和酗酒。
本研究旨在将唇形科假糙苏属植物煎剂的相关消化用途与可能解释这些用途的分子机制联系起来：促进消化（乙酰胆碱酯酶抑制）和治疗宿醉（乙醇脱氢酶抑制）。
分析了唇形科假糙苏属植物的煎剂，以研究其对乙醇脱氢酶（ADH）的抑制作用和乙酰胆碱酯酶（AChE）的抑制作用，分别与酒精代谢和肠道蠕动有关。通过 LC-MS/MS 对活性成分进行鉴定，并对 AChE 进行对接研究，检测到生物活性分子。
所有煎剂均抑制 ADH 活性。这种抑制作用与它们的迷迭香酸（RA）含量有关，RA 的 IC 值为 19μg/mL，与参考抑制剂 CuCl 相似。RA 的存在也导致大多数煎剂具有 AChE 抑制能力。IC 值为 80μg/mL 的 P. zuluensis 煎剂还含有介体醇，这是一种更好的 AChE 抑制剂，这一点通过分子对接研究得到了证实。此外，所有测试的煎剂对两种人类细胞系均无毒性，并且具有很高的清除自由基（DPPH）的能力，这也有助于消化过程，这与它们的 RA 含量有关。
富含 RA 的唇形科假糙苏属植物煎剂所呈现的所有活性均支持其用于治疗消化紊乱，而 P. barbatus 也可用于缓解宿醉症状。存在于 P. zuluensis 中的介体醇表现出显著的 AChE 抑制作用，可能为生物活性化合物提供新的研究方向。
