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<p>Polycyclic polyprenylated acylphloroglucinols (PPAPs) represent a structurally diverse class of natural products with reported biological activities, yet their effects on oral squamous cell carcinoma (OSCC) remain insufficiently characterized. In this study, fourteen tertiary alcohol-containing PPAPs, including seven previously undescribed compounds, were isolated from <i>Hypericum scabrum</i> Linn and structurally elucidated by spectroscopic methods. Their antiproliferative activities were evaluated in CAL-27 human OSCC cells. PPAPs were isolated and purified by means of column chromatography combined with semi-preparative techniques, then chemical structures were characterized using nuclear magnetic resonance (NMR) spectroscopy. The half-maximal inhibitory concentration (IC₅₀) values of these phloroglucinol compounds against CAL-27 cells were determined via the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyl tetrazolium bromide (MTT) assay. Furthermore, the in vitro mechanism underlying the action of these compounds on CAL-27 cells was elucidated through an integrated approach involving RNA sequencing (RNA-Seq), quantitative real-time polymerase chain reaction (qRT-PCR), and Western blot analysis. Fourteen tertiary alcohol-containing PPAPs were isolated and structurally characterized, including seven new analogs (<b>1</b>–<b>7</b>). Among these, compound <b>13</b> was found to be the potential cytotoxic active compound against CAL-27 during in-vitro tests, with IC<sub>50</sub> 8.96 µM. Cell viability assays demonstrated that compound <b>13</b> exerted significant growth inhibitory effects in a dose-dependent manner. Flow cytometric analysis revealed cell cycle arrest at the G2/M phase and a marked increase in apoptotic cell population following treatment at the IC₅₀ concentration. Further investigation showed that intracellular reactive oxygen species (ROS) levels were significantly elevated in treated cells, and co-treatment with the antioxidant cysteine partially attenuated ROS accumulation. These findings indicate that different cell death mechanisms may contribute to the cytotoxic effects of compounds. These findings demonstrate that compound <b>13</b> suppresses proliferation and induces apoptosis in CAL-27 cells, with ROS accumulation potentially contributing to its cytotoxic effects.</p>

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Tertiary alcohol-containing polycyclic polyprenylated acylphloroglucinols from Hypericum scabrum inhibit the proliferation of oral squamous cell carcinoma CAL-27 cells

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年4月17日

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  • Hong Zeng,
  • Peng-Yun Mou,
  • Sheng-Qiang Yang,
  • Yik-Ling Chew,
  • Li-Ping Teng,
  • Zhong-Bo Zhou

摘要

Polycyclic polyprenylated acylphloroglucinols (PPAPs) represent a structurally diverse class of natural products with reported biological activities, yet their effects on oral squamous cell carcinoma (OSCC) remain insufficiently characterized. In this study, fourteen tertiary alcohol-containing PPAPs, including seven previously undescribed compounds, were isolated from Hypericum scabrum Linn and structurally elucidated by spectroscopic methods. Their antiproliferative activities were evaluated in CAL-27 human OSCC cells. PPAPs were isolated and purified by means of column chromatography combined with semi-preparative techniques, then chemical structures were characterized using nuclear magnetic resonance (NMR) spectroscopy. The half-maximal inhibitory concentration (IC₅₀) values of these phloroglucinol compounds against CAL-27 cells were determined via the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyl tetrazolium bromide (MTT) assay. Furthermore, the in vitro mechanism underlying the action of these compounds on CAL-27 cells was elucidated through an integrated approach involving RNA sequencing (RNA-Seq), quantitative real-time polymerase chain reaction (qRT-PCR), and Western blot analysis. Fourteen tertiary alcohol-containing PPAPs were isolated and structurally characterized, including seven new analogs (1–7). Among these, compound 13 was found to be the potential cytotoxic active compound against CAL-27 during in-vitro tests, with IC50 8.96 µM. Cell viability assays demonstrated that compound 13 exerted significant growth inhibitory effects in a dose-dependent manner. Flow cytometric analysis revealed cell cycle arrest at the G2/M phase and a marked increase in apoptotic cell population following treatment at the IC₅₀ concentration. Further investigation showed that intracellular reactive oxygen species (ROS) levels were significantly elevated in treated cells, and co-treatment with the antioxidant cysteine partially attenuated ROS accumulation. These findings indicate that different cell death mechanisms may contribute to the cytotoxic effects of compounds. These findings demonstrate that compound 13 suppresses proliferation and induces apoptosis in CAL-27 cells, with ROS accumulation potentially contributing to its cytotoxic effects.