Zhang Hui, Jiang Qian, Gong Guojin, Li Mingzhen, Alotaibi Saad H
Department of Gastroenterology, Inner Mongolia People's Hospital, Hohhot city, Inner Mongolia, China.
Department of Oncological Radiotherapy, The Affiliated Huai'an Hospital of Xuzhou Medical University, Huai'an, Jiangsu, China.
Arch Med Sci. 2021 Jul 2;19(5):1479-1486. doi: 10.5114/aoms/138832. eCollection 2023.
Alpinetin is the bioactive component of a traditional Chinese medicine. This compound, one of the main constituents of the seeds of Hayata, is a member of the flavonoids, with anti-inflammatory, antibacterial, and other significant therapeutic activities of important potency and low systemic toxicity.
In our study, the inhibitory effect of isoliquiritigenin on HMG-CoA reductase showed a lower value of IC = 21.86 ±1.44 μg/ml. A molecular docking study was performed as a complementary study to provide additional data about the biological activities of alpinetin in the presence of urease. The docking calculations revealed that alpinetin with a docking score of -5.097 (kcal/mol) has an acceptable binding affinity to the enzyme, and because of various hydrophobic contacts and hydrogen bonds created by this chemical compound, alpinetin could be considered as an adequate inhibitor of urease.
In the cellular and molecular part of the study, the cells treated with alpinetin were assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay for 48 h as regards the cytotoxicity and anti-human gastric carcinoma properties towards normal (human umbilical vein endothelial cells (HUVECs)) and gastric carcinoma cell lines, i.e. SNU-1, Hs 746T, and KATO III. The IC values of alpinetin were 426, 586, and 424 μg/ml against SNU-1, Hs 746T, and KATO III cell lines, respectively. The viability of the malignant gastric cell line decreased dose-dependently in the presence of alpinetin.
It seems that the anti-human gastric carcinoma effect of the investigated molecule is due to its antioxidant effects.
高山黄芩素是一种中药的生物活性成分。该化合物是玉山柯种子的主要成分之一，属于黄酮类，具有抗炎、抗菌等重要的显著治疗活性且全身毒性低。
在我们的研究中，异甘草素对HMG-CoA还原酶的抑制作用显示出较低的IC值 = 21.86 ±1.44 μg/ml。进行了分子对接研究作为补充研究，以提供关于高山黄芩素在脲酶存在下生物活性的额外数据。对接计算表明，对接分数为 -5.097（千卡/摩尔）的高山黄芩素与该酶具有可接受的结合亲和力，并且由于该化合物形成的各种疏水接触和氢键，高山黄芩素可被视为脲酶的合适抑制剂。
在研究的细胞和分子部分，用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基-2H-四唑溴盐（MTT）法评估用高山黄芩素处理48小时的细胞对正常（人脐静脉内皮细胞（HUVECs））和胃癌细胞系（即SNU-1、Hs 746T和KATO III）的细胞毒性和抗人胃癌特性。高山黄芩素对SNU-1、Hs 746T和KATO III细胞系的IC值分别为426、586和424 μg/ml。在存在高山黄芩素的情况下，恶性胃癌细胞系的活力呈剂量依赖性下降。
似乎所研究分子的抗人胃癌作用归因于其抗氧化作用。
