<p><i>Uvaria valderramensis</i>, an endemic Philippine species, has not previously been evaluated for antidiabetic activity. This study evaluated the antidiabetic-relevant and Nrf2-modulatory activities of its leaf extracts using in vitro assays for α-glucosidase and α-amylase inhibition, antiglycation activity, and Nrf2 reporter modulation. Petroleum ether (UvP), dichloromethane (UvD), and methanol (UvM) extracts were obtained by cold percolation. UvM exhibited significant α-glucosidase inhibition (IC<sub>50</sub> = 44.21&#xa0;µg/mL), whereas none of the extracts inhibited α-amylase. UvP demonstrated moderate inhibition of advanced glycation end-product formation (IC<sub>50</sub> = 333.6&#xa0;µg/mL). In luciferase reporter assays, UvP increased Nrf2 activity in HaCaT keratinocytes (111.22% vs. DMSO control; <i>p</i> &lt; 0.05), while UvP and UvM reduced Nrf2 activity in Huh7 hepatocellular carcinoma cells (24.7% and 67.6%, respectively; <i>p</i> &lt; 0.05). The extracts also did not promote cytotoxicity. These findings demonstrate extract-specific bioactivities involving carbohydrate-digestive enzyme inhibition, antiglycation activity, and context-dependent Nrf2 modulation. This study provides the first in vitro evidence of antidiabetic-relevant and Nrf2-modulatory bioactivities of <i>U. valderramensis</i> leaf extracts and supports further chemical, mechanistic, cellular, and in vivo investigations.</p>

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Antidiabetic-relevant and differential Nrf2-modulatory activities of Uvaria valderramensis leaf extracts

  • Mia Lynelle R. Ang-Santo,
  • Gaea Felize Anne M. Asilo,
  • Beatrice Alexa N. Fuentes,
  • Meriel Frangelea L. Lalican,
  • Sheanne Audrey R. Sanchez,
  • Elian Abellanosa,
  • Porferio S. Bangcaya,
  • Joe Anthony H. Manzano,
  • Chia-Hung Yen,
  • Allan Patrick G. Macabeo,
  • Grecebio Jonathan D. Alejandro

摘要

Uvaria valderramensis, an endemic Philippine species, has not previously been evaluated for antidiabetic activity. This study evaluated the antidiabetic-relevant and Nrf2-modulatory activities of its leaf extracts using in vitro assays for α-glucosidase and α-amylase inhibition, antiglycation activity, and Nrf2 reporter modulation. Petroleum ether (UvP), dichloromethane (UvD), and methanol (UvM) extracts were obtained by cold percolation. UvM exhibited significant α-glucosidase inhibition (IC50 = 44.21 µg/mL), whereas none of the extracts inhibited α-amylase. UvP demonstrated moderate inhibition of advanced glycation end-product formation (IC50 = 333.6 µg/mL). In luciferase reporter assays, UvP increased Nrf2 activity in HaCaT keratinocytes (111.22% vs. DMSO control; p < 0.05), while UvP and UvM reduced Nrf2 activity in Huh7 hepatocellular carcinoma cells (24.7% and 67.6%, respectively; p < 0.05). The extracts also did not promote cytotoxicity. These findings demonstrate extract-specific bioactivities involving carbohydrate-digestive enzyme inhibition, antiglycation activity, and context-dependent Nrf2 modulation. This study provides the first in vitro evidence of antidiabetic-relevant and Nrf2-modulatory bioactivities of U. valderramensis leaf extracts and supports further chemical, mechanistic, cellular, and in vivo investigations.