Unraveling the Antimelanogenic Potential of Poria cocos: Component Characterization, Spatial Distribution, and Inhibitory Mechanisms

  • J Agric Food Chem. 2026 Jun 10;74(22):17165-17184. doi: 10.1021/acs.jafc.6c03500.
Yang Yu  1  2  3 ,  Ting-Ting Li  1 ,  Zi-Yi Deng  1 ,  Si-Qi Ma  1 ,  Jun-Shi Tao  1 ,  Yun-Peng Sun  1  2 ,  Guo-Kai Wang  1  2 ,  De-Ling Wu  1  2 ,  Jin-Song Liu  1  2
Affiliations
  • 1. School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, P. R. China.
  • 2. Anhui Province Key Laboratory of Bioactive Natural Products, Hefei 230012, P. R. China.
  • 3. Functional Activity and Resource Utilization on Edible and Medicinal Fungi Joint Laboratory of Anhui Province, Hefei 230012, P. R. China.
PMID: 42220209 DOI: 10.1021/acs.jafc.6c03500
Abstract

Phytochemical investigation of the edible fungus Poria cocos (Poria cum Radix Pini, PRP) led to the isolation and identification of 40 lanostane-type triterpenoids (LTDs), including seven new LTDs. Six LTDs (2, 5, 14, 17, 23, 36) exhibited antimelanogenic activity in B16F10 cells and zebrafish. Structure-activity relationship analysis revealed that an α-oriented hydroxyl at C-3, absence of C-16 hydroxyl, and free C-3 hydroxyl are critical for high activity. LTD 14 suppressed melanogenesis by inhibiting the ERK pathway, downregulating MITF and Tyrosinase. Molecular docking and dynamics predicted stable binding to Tyrosinase, which was confirmed by SPR (KD = 148 nM). Additionally, MALDI-MSI was employed for the first time to spatially map the distribution of bioactive triterpenoids directly in P. cocos tissue, revealing that whitening-active LTDs 14, 17, and 23 are widely distributed across different anatomical parts. This study establishes an integrated paradigm from structural discovery to spatial mapping for edible bioresource development.

Keywords
Antimelanogenic; ERK/MITF pathway; Lanostane-type triterpenoids; Mass spectrometry imaging; Poria cocos; Poria cum Radix Pini; Structure−activity relationship.
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