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<p>Hemorrhoids are characterized by inflammation, vascular dilation, and abnormal angiogenesis, and currently available therapies often provide only limited and temporary relief. The present study aimed to evaluate the anti-hemorrhoidal potential of <i>Tagetes erecta</i> L., Asteraceae (African marigold), through molecular docking, topical formulation development, <i>in vivo</i> efficacy studies, and mechanistic investigation focusing on inflammatory mediators and vascular endothelial growth factor expression. A total of 142 phytoconstituents reported from <i>T. erecta</i> were screened through molecular docking against vascular endothelial growth factor receptor 2 and cyclooxygenase-2. To conduct an in-depth interaction analysis of vascular endothelial growth factor receptor 2 and cyclooxygenase-2, the 10 top compounds with the lowest binding energies were chosen. A hydroethanolic extract of the plant was incorporated into ointment formulations and evaluated for rectal permeation using Franz diffusion cells. Hemorrhoids were experimentally induced in rats using a croton oil preparation. Following treatment with the formulated ointments for 5 days, rectoanal coefficient and severity score were assessed. Serum levels of pro-inflammatory markers including tumor necrosis factor-α, interleukin-6, prostaglandin E2, and cyclooxygenase-2, along with the anti-inflammatory cytokine interleukin-10, were determined. Immunohistochemistry was performed to evaluate vascular endothelial growth factor expression, and histopathological analysis was conducted to examine tissue morphology. The 20% <i>T. erecta</i> ointment showed favorable rectal permeation and significantly reduced rectoanal coefficient and severity scores. Treatment normalized inflammatory cytokine levels in a dose-dependent manner, reduced vascular endothelial growth factor expression, and improved tissue architecture. <i>Tagetes erecta</i> ointment demonstrated significant anti-hemorrhoidal activity.</p> Graphical Abstract <p></p>

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Anti-hemorrhoidal Efficacy of Hydroethanolic Extract of Tagetes erecta Flower-Based Ointment in Croton Oil-Induced Hemorrhoids: Role of VEGF and COX-2 Inhibition

  • 期刊论文

  • 发表日期：

    2026年7月29日

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  • Padmaja Kore,
  • Abhijit Deshmukh,
  • Ujwala Desai,
  • Rohini Pujari,
  • Anuradha More,
  • Sonali Nipate,
  • Somdatta Chaudhari,
  • Mohini Kuchekar,
  • Minal Harde,
  • Aarti Shingan

摘要

Hemorrhoids are characterized by inflammation, vascular dilation, and abnormal angiogenesis, and currently available therapies often provide only limited and temporary relief. The present study aimed to evaluate the anti-hemorrhoidal potential of Tagetes erecta L., Asteraceae (African marigold), through molecular docking, topical formulation development, in vivo efficacy studies, and mechanistic investigation focusing on inflammatory mediators and vascular endothelial growth factor expression. A total of 142 phytoconstituents reported from T. erecta were screened through molecular docking against vascular endothelial growth factor receptor 2 and cyclooxygenase-2. To conduct an in-depth interaction analysis of vascular endothelial growth factor receptor 2 and cyclooxygenase-2, the 10 top compounds with the lowest binding energies were chosen. A hydroethanolic extract of the plant was incorporated into ointment formulations and evaluated for rectal permeation using Franz diffusion cells. Hemorrhoids were experimentally induced in rats using a croton oil preparation. Following treatment with the formulated ointments for 5 days, rectoanal coefficient and severity score were assessed. Serum levels of pro-inflammatory markers including tumor necrosis factor-α, interleukin-6, prostaglandin E2, and cyclooxygenase-2, along with the anti-inflammatory cytokine interleukin-10, were determined. Immunohistochemistry was performed to evaluate vascular endothelial growth factor expression, and histopathological analysis was conducted to examine tissue morphology. The 20% T. erecta ointment showed favorable rectal permeation and significantly reduced rectoanal coefficient and severity scores. Treatment normalized inflammatory cytokine levels in a dose-dependent manner, reduced vascular endothelial growth factor expression, and improved tissue architecture. Tagetes erecta ointment demonstrated significant anti-hemorrhoidal activity.

Graphical Abstract