Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor

Baicalin prevents the production of hydrogen peroxide and oxidative stress induced by Aβ aggregation in SH-SY5Y cells

“…Together with the neuroprotective effects of baicalin reported by others [7,11,12,19,21,30,31], this study provides further supportive evidence for the potential use of baicalin as a therapeutic agent to reduce A␤-induced neuronal cytotoxicity. It is possible that baicalin may be beneficial to prevent or treat AD acting through the aforementioned mechanisms, however, further in vivo studies are needed to determine whether baicalin or its metabolites can indeed be transported across the blood brain barrier to reach brain tissue and accumulate up to a level for performing such functions, as the existing evidence of baicalin absorption and tissue distribution data published to date for baicalin are inconclusive [3,13,18,30,33].…”

“…It is possible that baicalin may be beneficial to prevent or treat AD acting through the aforementioned mechanisms, however, further in vivo studies are needed to determine whether baicalin or its metabolites can indeed be transported across the blood brain barrier to reach brain tissue and accumulate up to a level for performing such functions, as the existing evidence of baicalin absorption and tissue distribution data published to date for baicalin are inconclusive [3,13,18,30,33].…”

Natural compounds from traditional medicinal herbs in the treatment of cerebral ischemia/reperfusion injury

“…However, this problem may be resolved by the development of separation techniques. Recent studies have demonstrated that some of these compounds, such as paeoniflorin [78] , emodin-8-O-β-D-glucoside [79] , baicalin [80] , and curcuma oil [11] , have the ability to penetrate the bloodbrain barrier and achieve wide distribution in the brain, which is critical for CNS effects. It is easy to understand that the highly lipophilic structure of curcuma oil greatly enhances its access to the brain.…”

Adaptive Cellular Stress Pathways as Therapeutic Targets of Dietary Phytochemicals: Focus on the Nervous System

“…Although many phytochemicals were shown to have antidepressant effects, there are few studies of the application of phytochemicals to bipolar disorder. One study proposed that baicalin is a new prodrug inhibitor of prolyl oligopeptidase, which has been associated with schizophrenia, bipolar affective disorder, and related neuropsychiatric disorders (Tarragó et al, 2008). Given the established efficacy of lithium for bipolar disorder, phytochemicals that inhibit GSK-3b …”