Bioactivities of decoctions from Plectranthus species related to their traditional use on the treatment of digestive problems and alcohol intoxication
Bioactivities of decoctions from Plectranthus species related to their traditional use on the treatment of digestive problems and alcohol intoxication
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DOI：
10.1016/j.jep.2018.04.006
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发表时间：
2018-06-28
影响因子：
5.4
通讯作者：
Serralheiro, Maria Luisa M.
中科院分区：
文献类型：
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作者：
Brito, Elsa;Gomes, Emma;Serralheiro, Maria Luisa M.
民族药理学相关性：传统上，在大餐后食用香茶菜属植物的提取物，用于治疗食物消化和酒精滥用。本研究的目的：本研究旨在将香茶菜属植物提取物的消化相关民族用途与可能解释它们的分子机制相关联：缓解消化（乙酰胆碱酯酶抑制）和治疗宿醉（ADH抑制）材料和方法：分析了香茶属植物的提取物对乙醇脱氢酶（ADH）和乙酰胆碱酯酶（AChE）的抑制作用，分别与酒精代谢和肠动力有关。采用LC-MS/MS鉴定活性成分，并与乙酰胆碱酯酶（AChE）进行对接，检测活性分子。这种抑制作用与迷迭香酸（RA）含量相关，其IC 50值为19 μ g/mL，与参考抑制剂CuCl 2相似。RA的存在也导致大多数抑制剂显示出AChE抑制能力。如分子对接研究所示，具有80 pg/mL的IC 50的祖鲁羊肚菌水煎剂也呈现了美替诺，其是一种甚至更好的AChE抑制剂。此外，所有的测试表明，对两个人的细胞系没有毒性，和高的能力，以淬灭自由基（DPPH），这也发挥了在消化过程中的帮助，相关的RA content.Conclusions：所有的活动提出的RA丰富的香茶属植物支持他们使用在治疗消化障碍和P.香茶属植物可以解释其使用也缓解宿醉症状。存在于P. zuluensis中的美替洛尔表现出显著的AChE抑制作用，并且在未来可能提供生物活性化合物的新的先导。
Ethnopharmacological relevance: Decoctions of Plectranthus species are traditionally ingested after large meals for treatment of food digestion and alcohol abuse.Aim of the study: 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.Results: All decoctions inhibited ADH activity. This inhibition was correlated with their rosmarinic acid (RA) content, which showed an IC50 value of 19 mu g/mL, similar to the reference inhibitor CuCl2. The presence of RA also leads to most decoctions showing AChE inhibiting capacity. P. zuluensis decoction with an IC50 of 80 pg/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.Conclusions: 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.