Comparison of the Blood–Brain Barrier Penetration Ability and Anti-Neuroinflammatory Activity of Chromones in Two Types of Agarwood

Pharmaceuticals, Год журнала: 2025, Номер 18(4), С. 510 - 510

Опубликована: Март 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.

Язык: Английский

Drug-loaded nanoparticles induce immunogenic cell death and efficiently target cells from glioblastoma patients

Nanomedicine, Год журнала: 2025, Номер unknown, С. 1 - 12

Опубликована: Май 6, 2025

Glioblastoma multiforme (GBM) is characterized by a highly immunosuppressive tumor microenvironment (TME), posing significant challenges for efficient therapy's outcomes. Nanomedicine combined with immunotherapy holds the potential to modulate TME and reactivate immune responses. This study proposes polymeric nanosystem (NPs) encapsulating diaminocyclohexane-platinum II (DACHPt), an oxaliplatin derivative, induce immunogenic cell death (ICD) in GBM cells. An ionic-gelation technique was employed generate nanoparticles approximate size of 200 nm. NPs internalization analyzed lines, vitro-derived macrophages, leukocytes cells from patient via flow cytometry confocal imaging. ICD assessed measuring two its main markers: adenosine triphosphate (ATP) high-mobility group box 1 (HMGB1). were efficiently incorporated myeloid cells, but not lymphocytes. DACHPt-loaded demonstrated enhanced cytotoxicity compared free drug, increased ATP HMGB1 release confirming induction. Our findings suggest that represent promising therapeutic strategy capable targeting both tumor-promoting while inducing ICD.

Язык: Английский

Recent advances in nanomaterial-based brain-targeted delivery systems for glioblastoma therapy

Nanomedicine, Год журнала: 2025, Номер unknown, С. 1 - 17

Опубликована: Май 12, 2025

Glioblastoma (GBM) poses a formidable challenge because of its high morbidity and mortality. The therapeutic efficacy GBM is significantly hampered by the intricate blood-brain barrier (BBB) tumor (BBTB). Nanomaterial-based brain-targeted delivery systems have shown great potential for effectively delivering agents treatment overcoming limitations conventional drugs, such as poor BBB penetration, short half-life, low bioavailability. This review focuses on an in-depth analysis interplay between BBB/BBTB drug transport kinetics while analyzing innovative nanoparticle-mediated strategies enhanced treatment. Moreover, nanoparticle-based are emphasized, with particular attention given to biomimetic nanoparticles (BMNPs), whose unique advantages. current challenges, translational potential, future research directions in this rapidly evolving field comprehensively discussed, highlighting advances nanomaterial applications. aims stimulate further into systems, offering promising avenues maximizing effects gene drugs or chemotherapeutic practical

Язык: Английский