Orazbekov Yerkebulan, Ibrahim Mohamed A, Mombekov Serjan, Srivedavyasasri Radhakrishnan, Datkhayev Ubaidilla, Makhatov Bauyrzhan, Chaurasiya Narayan D, Tekwani Babu L, Ross Samir A
National Center for Natural Products Research, University of Mississippi, University, MS 38677, USA.
South-Kazakhstan State Pharmaceutical Academy, Al-Farabi Square, Shymkent 160019, Kazakhstan.
Evid Based Complement Alternat Med. 2018 Jan 14;2018:1370368. doi: 10.1155/2018/1370368. eCollection 2018.
Phytochemical analysis of the ethanolic extract of fruits yielded four new compounds (-) along with eleven known compounds (-). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with and opioid receptors (-49.7 and -53.8% displacement, resp.). Compound was found to be possibly allosteric for and opioid receptors (-88.4 and -27.2% displacement, resp.) and showed moderate activity (60.5% displacement) towards CB1 receptor. Compound exhibited moderate activity towards cannabinoid receptors CB1 and CB2 (47.9 and 42.3% displacement, resp.). The known compounds (-) exhibited prominent activity towards cannabinoid receptors: pomiferin () (IC of 2.110 and 1.318 M for CB1 and CB2, resp.), auriculasin () (IC of 8.923 M for CB1), warangalone () (IC of 1.670 and 4.438 M for CB1 and CB2, resp.), and osajin () (IC of 3.859 and 7.646 M for CB1 and CB2, resp.). The isolated compounds were also tested for inhibition of human monoamine oxidase-A and monoamine oxidase-B enzymes activities, where all the tested compounds showed fewer inhibitory effects on MAO-A compared to MAO-B activities: auriculasin () (IC of 1.91 and 45.98 M for MAO-B and MAO-A, resp.).
对果实乙醇提取物进行的植物化学分析得到了四种新化合物(-)以及十一种已知化合物(-)。粗提取物对大麻素受体表现出显著活性(CB1:103.4%置换率;CB2:68.8%置换率),并且可能与μ和κ阿片受体存在变构相互作用(分别为-49.7%和-53.8%置换率)。发现化合物对μ和κ阿片受体可能具有变构作用(分别为-88.4%和-27.2%置换率),并且对CB1受体表现出中等活性(60.5%置换率)。化合物对大麻素受体CB1和CB2表现出中等活性(分别为47.9%和42.3%置换率)。已知化合物(-)对大麻素受体表现出显著活性:波米费林()(CB1和CB2的IC分别为2.110和1.318μM)、耳状素()(CB1的IC为8.923μM)、瓦朗戈龙()(CB1和CB2的IC分别为1.670和4.438μM)以及奥沙金()(CB1和CB2的IC分别为3.859和7.646μM)。还测试了分离出的化合物对人单胺氧化酶-A和单胺氧化酶-B酶活性的抑制作用,与MAO-B活性相比,所有测试化合物对MAO-A的抑制作用较小:耳状素()(MAO-B和MAO-A的IC分别为1.91和45.98μM)。