目的研究盾叶木Macaranga adenantha枝的化学成分并进行蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性和人肿瘤细胞毒活性筛选。方法用硅胶和凝胶色谱分离化合物,用波谱学等方法鉴定结构;分别以体外酶学方法和MTT法测定化合物PTP1B抑制活性和细胞毒活性。结果从盾叶木乙醇提取物中分离得到8个化合物,分别鉴定为:齐墩果酸(Ⅰ)、3β-乙酰基齐墩果酸(Ⅱ)、3β-乙酰基齐墩果酸甲酯(Ⅲ)、3β,28-二羟基-12-烯-齐墩果烷(Ⅳ)、2α,3β-二羟基齐墩果酸(Ⅴ)、3β-乙酰氧基-11-烯-齐墩果烷-28,13-内酯(Ⅵ)、3β-乙酰氧基-11α,12α-环氧-齐墩果烷-28,13-内酯(Ⅶ)、3β-O-乙酰基木油醇酸(Ⅷ)。化合物Ⅰ, Ⅳ, Ⅴ抑制PTP1B酶的IC50分别为(7.2±0.3)、(12.4±5.5)、(6.2±0.9)、(7.6±1.7)μg/mL,所有化合物抑制几种肿瘤细胞的IC50均大于10μg/mL。结论8个化合物均为首次从该属植物中得到。化合物、、、为PTP1B酶抑制剂,所有化合物均无细胞毒活性。

Objective To investigate the chemical constituents of Macaranga adenantha, and assay protein tyrosine phosphotase 1B (PTP1B) inhibitory activity and cytotoxicity to human cancer cell lines. Methods Column and preparative TLC techniques over silica gel and Sephadex LH-20 column chro- matography were used to separate and purify the chemical constituents. The structures were elucidated by spectroscopic methods. PTP1B and several human cancer cell lines were used to evaluate bioactivities of the compounds by enzymology methods and MTT methods, respectively. Results Eight compounds were obtained and their structures were identified as: oleanolic acid (Ⅰ), 3β-acetoxy-olean-12-en-oic acid (Ⅱ), 3β-acetoxy-olean-12-en-28-oic acid methyl ester (Ⅲ), 3β, 28-dihydroxy-12-en-olean (Ⅳ), 2α, 3β-dihydroxy-12-en-28-oic acid (Ⅴ), 3β-acetoxy-11-en-olean-28, 13-olide (Ⅵ), 3β, 28-dihydroxy-12-en-olean, 12α-epoxy-olean-28, 13-olide (Ⅶ), 3β-[WTBX]-O-acetyl aleuritolic acid (Ⅷ). Compounds Ⅰ, Ⅳ, Ⅴ, and Ⅷ showed PTP1B inhibitory activities with IC₅₀(7.2±0.3), (12.4±5.5), (6.2±0.9), (7.6±1.7) μg/mL. respectively. IC₅₀ of all compounds against several human cancer cell lines were larger than 10 μg/mL. Conclusion [WT5BZ]All compunds are isolated from plants of Macaranga Thou. for the first time