Department of Pharmacognosy, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.
Molecules. 2021 Mar 2;26(5):1320. doi: 10.3390/molecules26051320.
Agarwood is known to have a sedative effect and the less studied volatile aromatic constituents it contains may have contribution to the activity. In this study, two grade (highest-grade agarwood in Japan) samples were extracted using headspace-solid phase microextraction (HS-SPME) and analyzed through gas chromatography-mass spectrometry (GC-MS). Six low molecular weight aromatic compounds (LACs) and one structurally simple compound (diethylene glycol monoethyl ether) present in the aromas were individually evaluated for inhalational sedative activity in mice through open field test. Doses of 0.0001 g/L to 1 g/L were prepared for each compound and administered to mice ( = 6/dose/compound). Results revealed all compounds decreased spontaneous motor activity at almost all doses. Strongest sedative activity of each compound reduced total spontaneous motor activity by more than half against control, demonstrating their contribution to agarwood aroma and potential as independent sedating agents. Mixtures of compounds using their most effective dose were made and evaluated again for inhalational sedative effect. Interestingly, the combination of all compounds showed no significant effect and even caused stimulation in mice movements. This result suggests antagonistic-like interaction between the compounds, which is probably due to structural similarities. Consequently, it implies the other constituents present in agarwood, along with LACs, are also important to the overall sedative activity.
沉香素有镇静作用，其含有的挥发性芳香成分可能与其活性有关。本研究采用顶空固相微萃取（HS-SPME）提取两种特级（日本最高级沉香）样品，并用气相色谱-质谱联用（GC-MS）进行分析。通过旷场试验，对香气中存在的 6 种低分子量芳香化合物（LACs）和 1 种结构简单的化合物（二乙二醇单乙醚）进行了单独评估，以评估其在小鼠体内的吸入镇静活性。为每种化合物制备了 0.0001 g/L 至 1 g/L 的剂量（ = 6/剂量/化合物），并对小鼠进行了给药。结果表明，所有化合物在几乎所有剂量下均降低了自发性运动活性。每种化合物的最强镇静活性将总自发运动活性降低了一半以上，与对照组相比，表明它们对沉香香气有贡献，并可能作为独立的镇静剂。使用其最有效剂量的化合物混合物再次进行吸入镇静作用评估。有趣的是，所有化合物的组合没有显示出显著的效果，甚至导致小鼠运动的刺激。该结果表明化合物之间存在拮抗样相互作用，这可能是由于结构相似性所致。因此，这意味着沉香中存在的其他成分以及 LACs 对整体镇静活性也很重要。
