Yang Jiali, Chen Mengyu, Zhang Wan, Liu Jia, Zhao Jing, Ping Xin, Lu Ye, He Pei, Pei Lin
School of Integrated Traditional Chinese and Western Medicine, Hebei University of Chinese Medicine, Shijiazhuang, Hebei, China.
Key Research Laboratory of Phlegm Stagnation Syndrome and Treatment in Hebei Province, Hebei Academy of Chinese Medicine Sciences, Shijiazhuang, Hebei, China.
Front Pharmacol. 2025 Aug 21;16:1607919. doi: 10.3389/fphar.2025.1607919. eCollection 2025.
Baicalin, an extract derived from the dried root of Scutellaria baicalensis Georgi (Huang Qin), has demonstrated neuroprotective properties. Nonetheless, the safety profile of baicalin has not yet been fully elucidated.
The objective was to characterize the acute and subacute toxicity profiles of baicalin across various organ systems, thereby establishing safe therapeutic windows for its clinical application in the treatment of chronic neurodegenerative disorders.
Acute toxicity was assessed at 4,000 mg/kg (OECD 423), while subacute toxicity evaluated escalating doses (1,000-4,000 mg/kg; OECD 407). Endpoints included survival, general behaviours, behavioral alterations, hematological/biochemical parameters, organ coefficients, and histopathology of brain, liver, and kidney.
Acute exposure showed no mortality (LD50 > 4,000 mg/kg) or lasting physiological effects, with only transient gastrointestinal symptoms in one subject. Subacute administration caused temporary gastrointestinal issues and occasional compulsive behaviors, all resolving within 24 h. Behavioral assessments indicated intact neurocognitive function and emotional stability. Hematological profiles revealed sex-specific responses, with males showing higher lymphocyte percentages and females demonstrating renal changes. Biochemical analyses indicated liver metabolic changes, including alkaline phosphatase suppression and reduced triglycerides, along with mild nephrotoxic signs. Histopathological evaluations confirmed non-necrotic liver stress and unchanged hippocampal structure.
Baicalin showed high acute safety with an LD50 over 4,000 mg/kg in mice, and a subacute no-observed-adverse-effect level (NOAEL) of 2,000 mg/kg, indicating its potential as a neuroprotective agent. However, 4,000 mg/kg doses led to reversible hepatorenal toxicity and biochemical alterations, highlighting the need to monitor organ function during extended high-dose use.
黄芩苷是从黄芩（Huang Qin）干燥根中提取的一种提取物，已显示出神经保护特性。尽管如此，黄芩苷的安全性尚未完全阐明。
目的是描述黄芩苷在各个器官系统中的急性和亚急性毒性特征，从而为其在治疗慢性神经退行性疾病中的临床应用建立安全治疗窗口。
按照经合组织423号准则，以4000mg/kg评估急性毒性；按照经合组织407号准则，以递增剂量（1000 - 4000mg/kg）评估亚急性毒性。观察指标包括存活率、一般行为、行为改变、血液学/生化参数、器官系数以及脑、肝和肾的组织病理学。
急性暴露未显示死亡率（半数致死量>4000mg/kg）或持久的生理影响，仅一名受试者出现短暂的胃肠道症状。亚急性给药导致暂时性胃肠道问题和偶尔的强迫行为，所有这些在24小时内均得到缓解。行为评估表明神经认知功能和情绪稳定性完好。血液学分析显示出性别特异性反应，男性淋巴细胞百分比更高，女性出现肾脏变化。生化分析表明肝脏代谢发生变化，包括碱性磷酸酶受抑制和甘油三酯降低，同时伴有轻度肾毒性迹象。组织病理学评估证实肝脏存在非坏死性应激，海马结构未改变。
黄芩苷在小鼠中显示出高急性安全性，半数致死量超过4000mg/kg，亚急性无观察到有害作用水平（NOAEL）为2000mg/kg，表明其作为神经保护剂的潜力。然而，40
