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<p><i>Kaempferia parviflora</i>, well-known as Thai ginseng (Krachaidum), has been used as a medicinal plant and food source for centuries. Its rhizome contains several flavonoids, particularly poly-<i>O</i>-methylated flavones (also known as polymethoxyflavones). We previously found that <i>K. parviflora</i> extract had a strong stimulatory effect on melanogenesis in B16F10 mouse melanoma cells. The aim of this study was to investigate the melanogenic stimulation exerted by various <i>O</i>-methylated flavonoids from <i>K. parviflora</i> in human melanoma cells and elucidate the mechanism of action of the most active compound. MNT-1 cells were used to screen for the most potent <i>O</i>-methylated flavonoid, and its effects on some key steps in melanin biosynthesis would subsequently be investigated. The poly-<i>O</i>-methylated flavone 3,5,7,3′,4′-pentamethoxyflavone (PMF) exhibited the strongest melanogenesis-stimulating activity among the 13 <i>O</i>-methylated flavones isolated from <i>K. parviflora</i>. It was shown to enhance tyrosinase (TYR) activity by upregulating the levels of TYR and TYR-related protein 1 (TRP-1) via its inhibitory effect on two-pore channel 2 (TPC2). In conclusion, poly-<i>O</i>-methylated flavones, especially PMF, were suggested as a potential group of flavonoids that could stimulate melanin production by inhibiting the activity of the TPC2 channel, leading to increased TYR and TRP-1 activities.</p>

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Polymethoxyflavones from Kaempferia parviflora stimulate melanogenesis by blocking the TPC2 channel

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年11月18日

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  • Pattara Poungcho,
  • Rachel Tang,
  • Rita Hairani,
  • Carla Abrahamian,
  • Ponsawan Netcharoensirisuk,
  • Warinthorn Chavasiri,
  • Chatchai Chaotham,
  • Christian Grimm,
  • Wanchai De‑Eknamkul

摘要

Kaempferia parviflora, well-known as Thai ginseng (Krachaidum), has been used as a medicinal plant and food source for centuries. Its rhizome contains several flavonoids, particularly poly-O-methylated flavones (also known as polymethoxyflavones). We previously found that K. parviflora extract had a strong stimulatory effect on melanogenesis in B16F10 mouse melanoma cells. The aim of this study was to investigate the melanogenic stimulation exerted by various O-methylated flavonoids from K. parviflora in human melanoma cells and elucidate the mechanism of action of the most active compound. MNT-1 cells were used to screen for the most potent O-methylated flavonoid, and its effects on some key steps in melanin biosynthesis would subsequently be investigated. The poly-O-methylated flavone 3,5,7,3′,4′-pentamethoxyflavone (PMF) exhibited the strongest melanogenesis-stimulating activity among the 13 O-methylated flavones isolated from K. parviflora. It was shown to enhance tyrosinase (TYR) activity by upregulating the levels of TYR and TYR-related protein 1 (TRP-1) via its inhibitory effect on two-pore channel 2 (TPC2). In conclusion, poly-O-methylated flavones, especially PMF, were suggested as a potential group of flavonoids that could stimulate melanin production by inhibiting the activity of the TPC2 channel, leading to increased TYR and TRP-1 activities.