Comparison of the Blood–Brain Barrier Penetration Ability and Anti-Neuroinflammatory Activity of Chromones in Two Types of Agarwood DOI Creative Commons
Mengyuan Yang, Yanan Yuan,

Jingfan Wei

et al.

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(4), P. 510 - 510

Published: March 31, 2025

Background/Objectives: Agarwood has a good neuroprotective effect and is often used to relieve anxiety treat insomnia. This study compared the similarities differences in chromone components of two types agarwood. It further investigated absorption brain distribution characteristics these rats their effects mediated through anti-neuroinflammatory pathways. Methods: confirmed, ITS2 barcoding chloroplast genome analysis, that both ordinary Qi-Nan agarwood are derived from Aquilaria sinensis. A comparative analysis chromones ethanol extracts agarwood, as well those capable penetrating blood-brain barrier vivo, was conducted using UPLC-Q-TOF-MS. Subsequently, an vitro neuroinflammatory model established via lipopolysaccharide (LPS)-stimulated BV-2 cells evaluate activity differential chromones. Results: UPLC-Q-TOF-MS characterization revealed agarwood: total 81 compounds were identified (OAE) (20 THPECs, 42 FTPECs, 19 BI), while 41 (QNE) (11 THPECs 30 FTPECs). Pharmacokinetic showed 14 OAE (eight six FTPECs) penetrated rat serum, 10 blood–brain (BBB). Twelve FTPECs QNE all which BBB. The peak area ion current (TIC) calculated for samples, TIC serum tissue same roughly estimate ratio. results demonstrated capability traverse substantially superior THPECs. Correspondingly, only detected DESI-MS imaging; no tissue, imaging localized neuroanatomic regions (cerebral cortex, thalamus, hippocampus). In assays anti-inflammatory efficacy over (IL-6/TNF-α suppression, p < 0.05), correlating with its FTPEC-rich composition. Conclusions: Structure–activity relationships potent inhibitors pro-inflammatory cytokines, exhibiting enhanced BBB penetration (blood–brain relative abundance > 1). These findings establish prioritized candidates CNS-targeted therapeutics, QNE’s pharmacological superiority attributed FTPEC dominance optimized transit capacity.

Language: Английский

Comparison of the Blood–Brain Barrier Penetration Ability and Anti-Neuroinflammatory Activity of Chromones in Two Types of Agarwood DOI Creative Commons
Mengyuan Yang, Yanan Yuan,

Jingfan Wei

et al.

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(4), P. 510 - 510

Published: March 31, 2025

Background/Objectives: Agarwood has a good neuroprotective effect and is often used to relieve anxiety treat insomnia. This study compared the similarities differences in chromone components of two types agarwood. It further investigated absorption brain distribution characteristics these rats their effects mediated through anti-neuroinflammatory pathways. Methods: confirmed, ITS2 barcoding chloroplast genome analysis, that both ordinary Qi-Nan agarwood are derived from Aquilaria sinensis. A comparative analysis chromones ethanol extracts agarwood, as well those capable penetrating blood-brain barrier vivo, was conducted using UPLC-Q-TOF-MS. Subsequently, an vitro neuroinflammatory model established via lipopolysaccharide (LPS)-stimulated BV-2 cells evaluate activity differential chromones. Results: UPLC-Q-TOF-MS characterization revealed agarwood: total 81 compounds were identified (OAE) (20 THPECs, 42 FTPECs, 19 BI), while 41 (QNE) (11 THPECs 30 FTPECs). Pharmacokinetic showed 14 OAE (eight six FTPECs) penetrated rat serum, 10 blood–brain (BBB). Twelve FTPECs QNE all which BBB. The peak area ion current (TIC) calculated for samples, TIC serum tissue same roughly estimate ratio. results demonstrated capability traverse substantially superior THPECs. Correspondingly, only detected DESI-MS imaging; no tissue, imaging localized neuroanatomic regions (cerebral cortex, thalamus, hippocampus). In assays anti-inflammatory efficacy over (IL-6/TNF-α suppression, p < 0.05), correlating with its FTPEC-rich composition. Conclusions: Structure–activity relationships potent inhibitors pro-inflammatory cytokines, exhibiting enhanced BBB penetration (blood–brain relative abundance > 1). These findings establish prioritized candidates CNS-targeted therapeutics, QNE’s pharmacological superiority attributed FTPEC dominance optimized transit capacity.

Language: Английский

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