Sun Shasha, Hamezah Hamizah Shahirah, Jin Chuanshan, Han Rongchun, Tong Xiaohui
School of Pharmacy, Anhui University of Chinese Medicine, Hefei, China.
Institute of Systems Biology, Universiti Kebangsaan Malaysia, Bangi, Malaysia.
CNS Neurosci Ther. 2025 Jul;31(7):e70535. doi: 10.1111/cns.70535.
Albiflorin, a key compound from Paeonia lactiflora, has shown therapeutic potential in neuropsychiatric and neurodegenerative disorders (NPDs and NDDs), especially depression and Alzheimer's disease (AD). This review aimed to summarize its pharmacological effects, mechanisms, pharmacokinetics, and therapeutic prospects.
Albiflorin exhibits multi-target actions, including modulation of monoamine neurotransmitters, inhibition of neuroinflammation, and enhancement of neuroplasticity. In AD, it reduces Aβ accumulation, improves mitochondrial function, and activates MAPK/ERK and Nrf2/HO-1 signaling pathways. In depression, it restores phospholipid and tryptophan metabolism, regulates HPA axis function, and increases BDNF expression. Albiflorin crosses the blood-brain barrier (BBB) and may act indirectly via the gut-brain axis through its metabolite benzoic acid. Though brain concentrations are low, its pharmacological effects remain significant. Albiflorin also shows potential benefits in conditions like cerebral ischemia and hypoxic-ischemic brain injury. Toxicological data indicate low systemic toxicity and good safety margins in vivo and in vitro.
Albiflorin demonstrates promising therapeutic potential for NPDs and NDDs via multi-pathway regulation. However, further studies are needed to optimize brain delivery, understand gut microbiota interactions, and confirm efficacy through clinical trials. The advancement of formulation strategies and pharmacokinetic research will be considered key to achieving clinical translation.
芍药苷是芍药中的一种关键化合物，已显示出在神经精神疾病和神经退行性疾病（NPDs和NDDs），特别是抑郁症和阿尔茨海默病（AD）中的治疗潜力。本综述旨在总结其药理作用、机制、药代动力学和治疗前景。
芍药苷具有多靶点作用，包括调节单胺类神经递质、抑制神经炎症和增强神经可塑性。在AD中，它可减少β-淀粉样蛋白（Aβ）积累，改善线粒体功能，并激活丝裂原活化蛋白激酶/细胞外信号调节激酶（MAPK/ERK）和核因子E2相关因子2/血红素加氧酶-1（Nrf2/HO-1）信号通路。在抑郁症中，它可恢复磷脂和色氨酸代谢，调节下丘脑-垂体-肾上腺（HPA）轴功能，并增加脑源性神经营养因子（BDNF）表达。芍药苷可穿过血脑屏障（BBB），并可能通过其代谢产物苯甲酸经肠脑轴间接发挥作用。尽管脑内浓度较低，但其药理作用仍然显著。芍药苷在脑缺血和缺氧缺血性脑损伤等病症中也显示出潜在益处。毒理学数据表明其在体内和体外的全身毒性较低，安全边际良好。
芍药苷通过多途径调节对NPDs和NDDs显示出有前景的治疗潜力。然而，需要进一步研究以优化脑内递送，了解肠道微生物群的相互作用，并通过临床试验确认疗效。制剂策略和药代动力学研究的进展将被视为实现临床转化的关键。
