Laboratory of Pharmacognosy, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece.
Dipartimento NEUROFARBA, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Polo Scientifico, Sesto Fiorentino (Firenze), Italy.
Nat Prod Res. 2022 Mar;36(6):1558-1564. doi: 10.1080/14786419.2021.1880406. Epub 2021 Feb 3.
spp. are lipophilic fungi that are part of the normal flora of the human skin and are the etiological agents of dandruff and seborrheic dermatitis. β-Carbonic Anhydrases (CAs; EC 4.2.1.1) expressed from the pathogenic fungi are an alternative/complementary drug target. Previous work by our groups demonstrated that flavonoids and depsides can effectively inhibit β-CA (MgCA). In continuation of this study herein we report the inhibitory activity of a variety of phenols from L. and L. against β-MgCA, among them I4-II7-di-carvacrol, a new natural product. Structure elucidation of the compounds was performed by 1 D, 2 D NMR and spectrometric analyses. Xanthomicrol and rosmarinic acid were active in the (sub)micromolar range (K 0.6 and 2.2 μM, respectively 40.0 μM of the standard inhibitor acetazolamide). Finally, the compounds were not cytotoxic, but showed no activity against .
spp. 是亲脂性真菌，是人体皮肤正常菌群的一部分，是头皮屑和脂溢性皮炎的病因。来自致病性真菌的β-碳酸酐酶（CA；EC 4.2.1.1）是替代/互补的药物靶点。我们小组的先前工作表明，类黄酮和地衣酸可以有效抑制β-CA（MgCA）。在此研究中，我们报告了来自 L. 和 L. 的各种酚类化合物对β-MgCA 的抑制活性，其中包括 I4-II7-二香豆素，一种新的天然产物。通过 1D、2D NMR 和光谱分析进行了化合物的结构阐明。黄烷酮和迷迭香酸在亚微摩尔范围内具有活性（K0.6 和 2.2μM，分别为标准抑制剂乙酰唑胺的 40.0μM）。最后，这些化合物没有细胞毒性，但对 没有活性。
