Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Selangor, 43400 Serdang, Malaysia.
Evid Based Complement Alternat Med. 2012;2012:829814. doi: 10.1155/2012/829814. Epub 2012 May 28.
The in vitro antitumour-promoting, cytotoxic, and antioxidant activities of two ester derivatives of garcinia acid, that is, 2-(butoxycarbonylmethyl)-3-butoxycarbonyl-2-hydroxy-3-propanolide (1) and 1',1''-dibutyl methyl hydroxycitrate (2), that had been previously isolated from the fruits of Garcinia atroviridis Griff. ex T. Anders (Guttiferae), were examined. Based on the inhibition of Epstein-Barr virus early antigen (EBV-EA) activation, compound 1 (IC(50): 70 μM) showed much higher (8-fold) antitumour-promoting activity than compound 2 (IC(50): 560 μM). In addition, both compounds were nontoxic towards CEM-SS (human T-lymphoblastic leukemia) cells (CD(50): >100 μM), Raji (human B-lymphoblastoid) cells (CD(50): >600 μM), and brine shrimp (LD(50): >300 μM). Although the antitumour-promoting activity of compound 1 is moderate compared with the known antitumour promoter genistein, its non-toxicity suggests the potential of compound 1 and related structures as chemopreventive agents. The weak antioxidant activity displayed by both compounds also suggested that the primary antitumour-promoting mechanism of compound 1 did not involve oxidative-stress quenching.
先前从藤黄科藤黄属植物山竹子（Garcinia atroviridis Griff. ex T. Anders）的果实中分离得到的两种藤黄酸酯衍生物，2-(丁氧基羰基甲基）-3-丁氧基羰基-2-羟基-3-丙内酯（1）和 1',1''-二丁基甲基羟基柠檬酸酯（2），其体外抗肿瘤促进、细胞毒性和抗氧化活性已被检测。基于对 Epstein-Barr 病毒早期抗原（EBV-EA）激活的抑制作用，化合物 1（IC（50）：70μM）显示出比化合物 2（IC（50）：560μM）更高（8 倍）的抗肿瘤促进活性。此外，两种化合物对 CEM-SS（人 T 淋巴细胞白血病）细胞（CD（50）：>100μM）、Raji（人 B 淋巴细胞白血病）细胞（CD（50）：>600μM）和卤虫（LD（50）：>300μM）均无毒性。虽然与已知的抗肿瘤促进剂染料木黄酮相比，化合物 1 的抗肿瘤促进活性适中，但它的无毒性表明化合物 1 及其相关结构具有作为化学预防剂的潜力。两种化合物显示出的弱抗氧化活性也表明，化合物 1 的主要抗肿瘤促进机制不涉及氧化应激抑制。
