School of Computing, Engineering & Physical Sciences, University of the West of Scotland, Paisley PA1 2BE, Scotland, UK.
Leicester School of Pharmacy, De Montfort University, Leicester LE1 9BH, UK.
Fitoterapia. 2020 Jan;140:104420. doi: 10.1016/j.fitote.2019.104420. Epub 2019 Nov 14.
We report for the first time the isolation of 2-furyl(phenyl)methanol (5) from the chloroform extracts of the Atractylis gummifera roots. A. gummifera is a thistle belonging to the Asteraceae family that produces the ent-kaurane diterpenoid glycoside atractyloside (ATR). ATR (1) was isolated and chemically modified to obtain its aglycone atractyligenin (2) and the methylated derivatives ATR-OMe (3) and genine-OMe (4). The compounds 1-5 were structurally characterised and evaluated against the intracellular amastigote, cultured within macrophages, and the extracellular promastigote of Leishmania donovani, the protozoan parasite responsible for the highly infective disease visceral leishmaniasis, which is fatal if untreated. The 2-furyl(phenyl)methanol 5 exhibited notable activity against the promastigote.
我们首次从苍术根的氯仿提取物中分离出 2-呋喃（苯基）甲醇（5）。苍术是菊科的一种蓟，它产生的 ent-贝壳杉二萜糖苷苍术苷（ATR）。ATR（1）被分离出来并进行化学修饰，以获得其苷元苍术烯醇（2）和甲基化衍生物 ATR-OME（3）和金烯醇-OME（4）。对化合物 1-5 进行了结构表征，并对巨噬细胞内的内阿米巴、利什曼原虫（导致高度传染性疾病内脏利什曼病的原生动物寄生虫）的外生前鞭毛体进行了评估，如果不治疗，该病是致命的。2-呋喃（苯基）甲醇 5 对前鞭毛体表现出显著的活性。
