For many years, studies focused on developing new natural or synthetic compounds with antineoplastic activity have attracted the attention of researchers. An interesting group of such compounds seem to be those with both lactone moiety and an aromatic ring which, in addition to antimicrobial or antiviral activity, also exhibit antitumor properties. The study shows antitumor activity of two enantiomeric trans isomers of 5-(1-iodoethyl)-4-(2′,5′-dimethylphenyl)dihydrofuran-2-one. Our aim was to determine their antitumor activity manifested as an ability to induce apoptosis in selected canine cancer cell lines as well as to evaluate differences in their strength depending on the configuration of their stereogenic centers. The enantiomers (+)-(4R,5S,6R)-1 and (−)-(4S,5R,6S)-2 were found to induce classical caspase-dependent apoptosis through downregulation of the expression of anti-apoptotic proteins Bcl-xL and Bcl-2. Although the mechanism of apoptosis induction was the same for both enantiomers, they differed in their strength, as stronger antineoplastic activity in vitro was exhibited by isomer (+)-(4R,5S,6R)-1.

多年来，致力于开发具有抗肿瘤活性的新型天然或合成化合物的研究吸引了研究人员的注意力。这类化合物的有趣的一类似乎是既具有内酯部分又具有芳香环的化合物，它们除了具有抗微生物或抗病毒活性外，还具有抗肿瘤特性。研究显示了5-（1-碘乙基）-4-（2'，5'-二甲基苯基）二氢呋喃-2-酮的两个对映异构体反式异构体的抗肿瘤活性。我们的目标是确定其抗肿瘤活性，表现为在所选犬癌细胞系中诱导凋亡的能力，以及根据其立体生成中心的构型评估其强度差异的能力。对映体（+）-（4 R，5 S，6发现R）-1和（-）-（4 S，5 R，6 S）-2通过下调抗凋亡蛋白Bcl-xL和Bcl-2的表达诱导经典的caspase依赖性凋亡。尽管两种对映异构体的凋亡诱导机理相同，但是它们的强度不同，因为异构体（+）-（4 R，5 S，6 R）-1表现出更强的体外抗肿瘤活性。