Scutellarin is a flavonoid with multiple biological activities[1]. Scutellarin can prevent endothelial dysfunction and prevent atherosclerosis through antioxidant activity[2]. Scutellarin has anti-HIV-1IIIB, HIV-1(74V) and HIV-1KM018 activities with EC50 of 26μM, 253μM and 136μM, respectively[3].
In vitro, Scutellarin (0-210μM) treated human renal cancer cells (ACHN and 786-O cells) for 24-72h inhibited cell proliferation in a dose- and time-dependent manner, induced cell apoptosis and cell cycle arrest at the G0/G1 phase, and increased the expression of phosphatase and tensin homolog (PTEN)[4]. Scutellarin (50μM) pre-treated BV-2 cells for 30min inhibited the production of NO, TNFα, IL-1β and ROS induced by lipopolysaccharide (LPS), and inhibited LPS-induced nuclear translocation and DNA binding activity of nuclear factor κB (NF-κB)[5].
In vivo, Scutellarin (30, 60mg/kg/day) was orally treated for 3 weeks in mice with H1975-Luciferase cell xenografts, which significantly inhibited the growth of transplanted tumors in mice, upregulated the levels of LC3-II and p-ERK1/2 in mouse lung tissue, and downregulated the level of p-AKT[6]. Scutellarin (5mg/kg) was intravenously injected to treat doxorubicin (DOX)-induced cardiac toxicity in rats, significantly reducing serum lactate dehydrogenase (LDH) activity, lipid peroxide (MDA) levels, and cardiac troponin T (cTnT) concentrations, and significantly reducing cardiac tissue damage[7].
References:
[1] Wang Z L, Wang S, Kuang Y, et al. A comprehensive review on phytochemistry, pharmacology, and flavonoid biosynthesis of Scutellaria baicalensis[J]. Pharmaceutical biology, 2018, 56(1): 465-484.
[2] Mo J, Yang R, Li F, et al. Scutellarin protects against vascular endothelial dysfunction and prevents atherosclerosis via antioxidation[J]. Phytomedicine, 2018, 42: 66-74.
[3] Zhang G H, Wang Q, Chen J J, et al. The anti-HIV-1 effect of scutellarin[J]. Biochemical and Biophysical Research Communications, 2005, 334(3): 812-816.
[4] Deng W, Han W, Fan T, et al. Scutellarin inhibits human renal cancer cell proliferation and migration via upregulation of PTEN[J]. Biomedicine & Pharmacotherapy, 2018, 107: 1505-1513.
[5] Wang S, Wang H, Guo H, et al. Neuroprotection of Scutellarin is mediated by inhibition of microglial inflammatory activation[J]. Neuroscience, 2011, 185: 150-160.
[6] Sun C Y, Li C Y, Li X F, et al. Scutellarin induces apoptosis and autophagy in NSCLC cells through ERK1/2 and AKT Signaling Pathways in vitro and in vivo[J]. Journal of Cancer, 2018, 9(18): 3247.
[7] Sun X P, Wan L L, Yang Q J, et al. Scutellarin protects against doxorubicin-induced acute cardiotoxicity and regulates its accumulation in the heart[J]. Archives of pharmacal research, 2017, 40: 875-883.
Scutellarin是一种具有多种生物活性的黄酮[1]。Scutellarin能够防止血管内皮功能障碍，并通过抗氧化来预防动脉粥样硬化[2]。Scutellarin具有抗HIV-1IIIB，HIV-1(74V)和 HIV-1KM018的活性，EC50分别为26μM，253μM和136μM[3]。
在体外，Scutellarin（0-210μM）处理人肾癌细胞（ACHN和786-O细胞）24-72h，以剂量和时间依赖性方式抑制了细胞增殖，诱导了细胞凋亡和细胞周期停滞在 G0/G1期，增加了磷酸酶和张力蛋白同源物（PTEN）的表达[4]。Scutellarin（50μM）预处理BV-2细胞30min，抑制了脂多糖（LPS）诱导的NO、TNFα、IL-1β和ROS的产生，抑制了LPS诱导的核转位和核因子κB（NF-κB）的DNA结合活性[5]。
在体内，Scutellarin（30, 60mg/kg/day）通过口服治疗H1975-Luciferase细胞异种移植小鼠3周，显著抑制了小鼠体内移植瘤的生长，上调了小鼠肺组织中LC3-II和p-ERK1/2的水平，下调了p-AKT水平[6]。Scutellarin（5mg/kg）通过静脉注射治疗阿霉素（DOX）诱导的大鼠心脏毒性，显著降低了血清中乳酸脱氢酶（LDH）活性、脂质过氧化物（MDA）水平、心肌肌钙蛋白T（cTnT）浓度，显著减少了心脏组织的损伤[7]。