Baicalin Magnesium Salt Exerts an Antitumor Effect in HepG2 Hepatoma Cells

IF 0.6 4区 医学 Q4 CHEMISTRY, MEDICINAL Pharmacognosy Magazine Pub Date : 2023-04-25 DOI:10.1177/09731296231158698
Xia Dongshuai, You Yong, Gao Yaxian, Wang Shuo, Gu YaChun, Jiang Tao, Liu Cuizhe, Song Hongru
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Abstract

Background Scutellaria baicalensis is an important medicinal plant used in China. Several compounds have been extracted from S. baicalensis using modern techniques. Baicalin, an active ingredient of S. baicalensis, is widely used clinically. However, its clinical use is limited owing to poor oral bioavailability and intestinal absorption. Objectives To evaluate the anti-tumor effect of baicalin magnesium salt (BA-MG, a novel magnesium salt form of baicalin with superior water solubility) on the human hepatocellular carcinoma cell line, HepG2. Materials and Methods Seven groups were established, including three dosages of BA-MG (200, 250, and 300 µg/mL), baicalin, dimethyl sulfoxide (DMSO) (negative control), magnesium sulfate (negative control), and control groups. Cell proliferation was determined using the cell counting kit-8 (CCK-8) assay. Cell cycle and apoptosis were detected by flow cytometry. Cell migration was determined using a cell scratch assay. Protein expression was determined using western blotting. Results In vitro, BA-MG inhibited proliferation, reduced cell cloning and migration abilities, induced cell cycle arrest, and promoted apoptosis of HepG2 cells (all p < 0.05). The effects of baicalin and BA-MG on proliferation and migration, cell cycle, and apoptosis may be attributed to decreasing the expression of Bcl-2, ROCK-1, proliferating cell nuclear antigen (PCNA), and cyclin E, as well as increasing the expression of Bax and caspase-9. The efficacy of BA-MG is superior to that of baicalin at the same dose. Conclusion BA-MG showed superior effects on inhibiting cell proliferation and inducing apoptosis in liver cancer cells.
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黄芩苷镁盐对HepG2肝癌细胞的抗肿瘤作用
背景黄芩是我国重要的药用植物。利用现代技术从黄芩中提取了几种化合物。黄芩苷是黄芩的有效成分,临床应用广泛。然而,由于口服生物利用度和肠道吸收率低,其临床应用受到限制。目的评价黄芩苷镁盐(BA-MG,一种新型的水溶性黄芩素镁盐形式)对人肝癌细胞株HepG2的抗肿瘤作用。材料与方法建立7组,分别为BA-MG(200、250和300µg/mL)、黄芩苷、二甲基亚砜(DMSO)(阴性对照)、硫酸镁(阴性对照组)和对照组。使用细胞计数试剂盒-8(CCK-8)测定法测定细胞增殖。流式细胞仪检测细胞周期和细胞凋亡。使用细胞划痕测定法测定细胞迁移。使用蛋白质印迹法测定蛋白质表达。结果在体外,BA-MG抑制HepG2细胞增殖,降低细胞克隆和迁移能力,诱导细胞周期停滞,促进细胞凋亡(均p<0.05)。黄芩苷和BA-MG对细胞增殖和迁移、细胞周期和细胞凋亡的影响可能与降低Bcl-2、ROCK-1、增殖细胞核抗原(PCNA)和细胞周期蛋白E的表达有关,以及增加Bax和胱天蛋白酶-9的表达。BA-MG的药效优于相同剂量的黄芩苷。结论BA-MG在抑制癌症细胞增殖和诱导细胞凋亡方面具有较好的作用。
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来源期刊
Pharmacognosy Magazine
Pharmacognosy Magazine CHEMISTRY, MEDICINAL-
CiteScore
1.87
自引率
0.00%
发文量
37
审稿时长
3 months
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