Department of Endocrinology & Metabolism, School of Medicine, Kyung Hee University, 1, Hoegi-dong, Dongdaemun-gu, Seoul 02447, Republic of Korea.
Department of Biomedical Laboratory Science, College of Health Sciences, Cheongju University, Cheongju, Chungbuk 28503, Republic of Korea.
Toxicol In Vitro. 2019 Dec;61:104613. doi: 10.1016/j.tiv.2019.104613. Epub 2019 Jul 29.
Methylglyoxal (MG), a highly reactive dicarbonyl compound, is a major precursor in the formation of advanced glycation end products, which are associated with diabetes-related diseases. Bergenin, an active constituent of plants of the genus Bergenia, exhibits multiple biological activities. This study evaluated the effect of bergenin on osteoclast differentiation and determined its mechanism of action. Bergenin reversed MG-inhibited tartrate-resistant acid phosphatase (TRAP) activity and decreased the bone resorption activity of osteoclasts. Quantitative RT-PCR revealed that bergenin decreased the expression of ERK1, Akt2, MMP-9, and OSTM1 genes in the presence of MG. Bergenin pretreatment yielded significant increases in intracellular calcium concentration, mitochondrial mass, mitochondrial membrane potential, and glyoxalase I reduced by MG. Additionally, bergenin decreased the formation of mitochondrial superoxide induced by MG. Detoxification of MG by bergenin may be a viable treatment for bone disorders in patients with diabetes.
甲基乙二醛（MG）是一种高度反应性的二羰基化合物，是形成与糖尿病相关疾病有关的晚期糖基化终产物的主要前体。小檗堿是小檗属植物的一种活性成分，具有多种生物学活性。本研究评估了小檗堿对破骨细胞分化的影响，并确定了其作用机制。小檗堿逆转了 MG 抑制的抗酒石酸酸性磷酸酶（TRAP）活性，并降低了破骨细胞的骨吸收活性。定量 RT-PCR 显示，小檗堿降低了 MG 存在时 ERK1、Akt2、MMP-9 和 OSTM1 基因的表达。MG 诱导的细胞内钙浓度、线粒体质量、线粒体膜电位和还原型谷胱甘肽的增加，以及由 MG 诱导的线粒体超氧化物的形成减少。小檗堿对 MG 的解毒作用可能是糖尿病患者骨骼疾病的一种可行治疗方法。
