<p>This study led to the isolation of 17 triterpenoids, including two lanostane-type (<b>1</b> and <b>2</b>), two dammarane-type (<b>3</b> and <b>7</b>), ten tirucallane-type (<b>4</b> and <b>8</b>−<b>16</b>), and three oleanane-type (<b>17</b>−<b>19</b>) triterpenoids, as well as nine sterols (<b>5</b>, <b>6</b>, and <b>20</b>−<b>26</b>) from <i>Cotinus coggygria</i> var. cinereus Engl, which were first discovered from the genus <i>Cotinus</i>. Among them, coggygrenoids A−D (<b>1</b>−<b>4</b>), coggygrerol A (<b>5</b>), and coggygrerol B (<b>6</b>) are undescribed compounds. Additionally, seven flavonoids (<b>27</b>−<b>33</b>) were also isolated from this plant<i>.</i> Compound <b>15</b> displayed inhibitory activities in LPS-induced RAW 264.7 cells with an IC<sub>50</sub> value 6.81 ± 0.15&#xa0;μM. Molecular docking demonstrated that <b>15</b> exhibited favorable affinity for NLRP3 and iNOS. In vitro and in vivo antibacterial evaluations indicated that coggygrnoid C (<b>3</b>) exhibited significant inhibitory activity against methicillin-resistant <i>Staphylococcus aureus</i> ATCC BAA-1717 (USA300), with An MIC of 8&#xa0;μg/mL. Further mechanistic investigations demonstrated that <b>3</b> exerted antibacterial activity by compromising the integrity of the cell wall and membrane. Notably, the combination of <b>3</b> with ampicillin exhibited an additive antibacterial effect. In the <i>Galleria mellonella</i> infection model, compound <b>3</b> exhibited comparable activity to that of the positive control at 20&#xa0;mg/kg. These findings suggest that triterpenoids of <i>C. coggygria</i> are potential antibacterial lead agents.</p> Graphical Abstract <p></p>

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First discovery of triterpenoids and sterols from Cotinus coggygria var. cinereus Engl. with anti-inflammatory and antibacterial activities

  • Yue-Tong Zhu,
  • Ze-Rui Li,
  • Ren-Hao Chen,
  • Jin-Hao Li,
  • Wei Wang,
  • Yu-Qi Gao,
  • Chun-Huan Li,
  • Jin-Ming Gao

摘要

This study led to the isolation of 17 triterpenoids, including two lanostane-type (1 and 2), two dammarane-type (3 and 7), ten tirucallane-type (4 and 816), and three oleanane-type (1719) triterpenoids, as well as nine sterols (5, 6, and 2026) from Cotinus coggygria var. cinereus Engl, which were first discovered from the genus Cotinus. Among them, coggygrenoids A−D (14), coggygrerol A (5), and coggygrerol B (6) are undescribed compounds. Additionally, seven flavonoids (2733) were also isolated from this plant. Compound 15 displayed inhibitory activities in LPS-induced RAW 264.7 cells with an IC50 value 6.81 ± 0.15 μM. Molecular docking demonstrated that 15 exhibited favorable affinity for NLRP3 and iNOS. In vitro and in vivo antibacterial evaluations indicated that coggygrnoid C (3) exhibited significant inhibitory activity against methicillin-resistant Staphylococcus aureus ATCC BAA-1717 (USA300), with An MIC of 8 μg/mL. Further mechanistic investigations demonstrated that 3 exerted antibacterial activity by compromising the integrity of the cell wall and membrane. Notably, the combination of 3 with ampicillin exhibited an additive antibacterial effect. In the Galleria mellonella infection model, compound 3 exhibited comparable activity to that of the positive control at 20 mg/kg. These findings suggest that triterpenoids of C. coggygria are potential antibacterial lead agents.

Graphical Abstract