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article · Phytotherapy Research

Isolates from <scp><i>Alpinia officinarum</i></scp> Hance attenuate LPS‐induced inflammation in HepG2: Evidence from <i>in silico</i> and <i>in vitro</i> studies

In plain language

Virtual screening of a Traditional Chinese Medicine database against p38 alpha mitogen-activated protein kinase identified anti-inflammatory candidates present in Alpinia officinarum, commonly known as Lesser galangal. Chromatographic separation of the plant rhizomes yielded five distinct compounds: galangin, kaempferide, isorhamnetin, and two diarylheptanoids. The biological activity of these isolates was evaluated in vitro using HepG2 liver cells exposed to lipopolysaccharide, an agent that triggers the expression of pro-inflammatory cytokines including interleukin-1 beta, interleukin-6, and tumour necrosis factor alpha. Treatment with each of the five isolated compounds suppressed this elevated cytokine gene expression in a dose-dependent manner. These findings confirm the bioactivity predicted by molecular modelling and demonstrate that specific chemical constituents of Alpinia officinarum rhizomes have functional properties relevant to the management of inflammatory conditions.

Key takeaways

  • Structure-based virtual screening against p38 alpha MAPK identified potential anti-inflammatory compounds within Alpinia officinarum.
  • Five active constituents, comprising galangin, kaempferide, isorhamnetin, and two diarylheptanoids, were isolated from the plant rhizomes.
  • Lipopolysaccharide stimulation of HepG2 cells induced gene expression of interleukin-1 beta, interleukin-6, and tumour necrosis factor alpha.
  • All five isolated compounds downregulated the expression of these pro-inflammatory cytokines in a dose-dependent manner.

Why it matters

Inflammatory diseases require effective therapeutic strategies with minimal adverse effects. By combining computational screening with laboratory cell models, this research demonstrates how constituents from traditional botanical sources can modulate inflammatory signalling pathways. Validating the ability of specific plant compounds to lower cytokine gene expression provides foundational scientific evidence supporting their potential relevance in managing inflammation-related disorders.

Commercialisation angle

This work represents early-stage research that could interest pharmaceutical and nutraceutical developers seeking natural anti-inflammatory leads. The findings demonstrate that five specific isolates from Lesser galangal rhizomes suppress inflammatory markers in cultured liver cells. However, practical application remains distant, requiring in vivo validation, pharmacokinetic evaluation, safety testing, and formulation development before these compounds can be translated into preventative or therapeutic healthcare products.

AI-generated from the published abstract. Always read the original work before citing.

Abstract

In an attempt to connect the legacy of centuries of invaluable knowledge from traditional medicine and the current understanding to the molecular mechanism of diseases, we took the advantage of the emergence of in silico screening as a promising tool for identification of potential leads from libraries of natural products. Traditional Chinese Medicine database was subjected to structure based virtual screening for identification of anti-inflammatory compounds using the 3D crystal structure of p38 alpha mitogen activated protein kinase. The molecular docking studies revealed the potential activity of several classes of compounds known to be the constituents of the rhizomes of Alpinia officinarum Hance (Lesser galangal). Five compounds, galangin, kaempferide, isorhamnetin, and two diarylheptanoids, were isolated from the rhizomes of the plant using vacuum liquid chromatography and flash chromatography techniques. The anti-inflammatory activity of these compounds was investigated on HepG2 cells stimulated by lipopolysaccharide. The latter induced the gene expression of proinflammatory cytokines; interleukin-1β, interleukin-6, tumor necrosis factor alpha. Addition of the 5 isolated compounds downregulated this increased gene expression in a dose dependent manner. Thus, these results indicate that the isolated compounds from A. officinarum could be used as a beneficial source for preventing and treating inflammatory diseases.

Research topics

  • Ginger and Zingiberaceae research
  • Piperaceae Chemical and Biological Studies
  • Drug-Induced Hepatotoxicity and Protection

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DOI: 10.1002/ptr.6056

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