Department of Pharmacognosy, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.
Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Mahidol University, Bangkok, Thailand.
Pharm Biol. 2020 Dec;58(1):490-497. doi: 10.1080/13880209.2020.1765813.
Weeras., Chalermglin & R.M.K. Saunders (Annonaceae) is a plant endemic to Thailand. Its constituents and their biological activities are unknown. Isolation and identification of the compounds in the leaves and stems of and determination of their cytotoxicity. Methanol extracts of the leaves and stems of were separated by chromatography, and spectroscopic methods were used to determine the structures of the components. The cytotoxicity of the extracts and pure compounds was evaluated using the sulforhodamine B assay with several cell lines. The cells were treated with the compounds at concentrations of 0.16-20 µg/mL for 48 or 72 h. The investigation of the extracts of leaves and stems resulted in the isolation of a new lignan, mitrephoran, and 15 known compounds. Among these compounds, 2-(3,4-dimethoxyphenyl)-6-(3,5-dimethoxyphenyl)-3,7-dioxabicyclo[3.3.0]octane, ciliaric acid, 6-methoxymarcanine A, and stepharanine were isolated from this genus for the first time. The alkaloids liriodenine and oxoputerine exhibited strong cytotoxicity against all tested cells (IC values of 6.59-11.02 µM). In contrast, magnone A, 3',4--dimethylcedrusin, and 6-methoxymarcanine A inhibited the growth of some of the tested cells (IC values of 2.03-19.73 µM). Magnone A and 6-methoxymarcanine A showed low toxicity for Hek 293 cells (IC >20 µM). is a source of cytotoxic lignans and alkaloids. Among the cytotoxic compounds, magnone A and 6-methoxymarcanine A are potentially useful lead compounds for the further development of anticancer agents because of their selective inhibitory effects on cancer cell lines.
我们拉耶拉杰、查勒姆格林和 R.M.K. 桑德斯（野牡丹科）是一种植物，仅产于泰国。其组成成分及其生物活性尚不清楚。本研究从该植物的叶和茎中分离化合物，并鉴定其结构，同时评价其细胞毒性。采用色谱法对该植物的叶和茎的甲醇提取物进行分离，并用光谱法确定各成分的结构。采用磺酰罗丹明 B 法，以几种细胞系为对象，评价提取物和纯化合物的细胞毒性。将细胞用化合物在 0.16-20 μg/ml 浓度下处理 48 或 72 h。研究该植物叶和茎的提取物，得到一个新的木脂素——mitrephoran 和 15 个已知化合物。在所分离的化合物中，2-(3,4-二甲氧基苯基)-6-(3,5-二甲氧基苯基)-3,7-二氧杂双环[3.3.0]辛烷、ciliaric 酸、6-甲氧基马卡宁 A 和 stepharanine 为该属首次分离得到。生物碱 liriodenine 和 oxoputerine 对所有测试细胞均表现出很强的细胞毒性（IC 值为 6.59-11.02 μM）。相反，magnone A、3',4--二甲氧基杜松素和 6-甲氧基马卡宁 A 抑制了一些测试细胞的生长（IC 值为 2.03-19.73 μM）。Magnone A 和 6-甲氧基马卡宁 A 对 Hek 293 细胞的毒性较低（IC >20 μM）。该植物是细胞毒性木脂素和生物碱的来源。在具有细胞毒性的化合物中，magnone A 和 6-甲氧基马卡宁 A 对癌细胞系具有选择性抑制作用，可能是进一步开发抗癌药物的有用先导化合物。
