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<p>A novel compound of isosteviol-12,17-sulfonic ester, <b>4</b>, has been synthesized and structurally characterized by IR, NMR, and MS. Its X-ray crystallographic analysis revealed the <i>β</i>-orientation of the sulfonic ester group at C12. The biological activities of the title compound were further evaluated. The results showed that compound <b>4</b> had better antibacterial, antitumor, antioxidant, and LSD1 inhibitory effects, which indicated that the introduction of the sulfonic ester substructure unit could improve biological activities. In particular, compound <b>4</b> could selectively inhibit <i>B</i>. <i>subtilis</i> and <i>S</i>. <i>aureus</i> with an MIC value of 2 mg/mL. Meanwhile, the inhibitory rate of compound <b>4</b> against LSD1 was 47.82% at a concentration of 10 μM, and the scavenging rate of compound <b>4</b> on ABTS free radicals reached 36.81% at a concentration of 1 mg/mL, whereas, it exhibited poor inhibitory activity against HepG2, HeLa, and SW480 cells, and had no selectivity. Current findings revealed that the title compound had biological activity and may be further investigated.</p>

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Synthesis, Structure, and Biological Activity of a Novel Diterpenoid Isosteviol-12,17-Sulfonic Ester Derivative

  • 期刊论文

  • 发表日期：

    2025年5月17日

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  • Cong-Jun Liu,
  • Ke-Jia Qiang,
  • Ling-Yan Guo,
  • Yong Wang,
  • Wei Wang,
  • Han Chen,
  • Yu-Tao Min,
  • Yu-Ling Li,
  • Yu-Fei Wang

摘要

A novel compound of isosteviol-12,17-sulfonic ester, 4, has been synthesized and structurally characterized by IR, NMR, and MS. Its X-ray crystallographic analysis revealed the β-orientation of the sulfonic ester group at C12. The biological activities of the title compound were further evaluated. The results showed that compound 4 had better antibacterial, antitumor, antioxidant, and LSD1 inhibitory effects, which indicated that the introduction of the sulfonic ester substructure unit could improve biological activities. In particular, compound 4 could selectively inhibit B. subtilis and S. aureus with an MIC value of 2 mg/mL. Meanwhile, the inhibitory rate of compound 4 against LSD1 was 47.82% at a concentration of 10 μM, and the scavenging rate of compound 4 on ABTS free radicals reached 36.81% at a concentration of 1 mg/mL, whereas, it exhibited poor inhibitory activity against HepG2, HeLa, and SW480 cells, and had no selectivity. Current findings revealed that the title compound had biological activity and may be further investigated.