Bak Eun-Jung, Kim Jinmoon, Choi Yun Hui, Kim Ji-Hye, Lee Dong-Eun, Woo Gye-Hyeong, Cha Jeong-Heon, Yoo Yun-Jung
Oral Cancer Research Institute, Yonsei University College of Dentistry, Seoul, Republic of Korea.
Research Center for Orofacial Hard Tissue Regeneration, College of Dentistry, Yonsei University, Seoul, Republic of Korea; Department of Applied Life Science, Yonsei University Graduate School, Seoul, Republic of Korea; Department of Oral Biology, Yonsei University College of Dentistry, Seoul, Republic of Korea.
Clin Nutr. 2014 Feb;33(1):156-63. doi: 10.1016/j.clnu.2013.03.013. Epub 2013 Mar 26.
BACKGROUND & AIMS: Wogonin is a flavonoid extracted from the root of Scutellaria baicalensis Gerogi. We evaluated the therapeutic effects of wogonin using db/db mice.
Mice received wogonin or vehicle by oral gavage for 2 weeks. Blood glucose, insulin, and cholesterol levels were measured, and liver morphology was observed with histopathological analysis. The mRNA expression levels of PPARα, PPARγ, and adiponectin in the liver and white adipose tissue (WAT) were determined by real-time PCR. Immunoblotting for AMPK and PPARγ, and adipocyte differentiation were investigated in vitro using 3T3-L1 cells. A luciferase assay was used to measure PPARα and PPARγ binding activity.
The wogonin group showed decreased weight gain without a change in food intake and improved glucose tolerance. Serum insulin and cholesterol levels in the wogonin group were significantly decreased compared to those in the control group. The wogonin group also showed less accumulation of lipid droplets and glycogen in the liver. PPARα and PPARγ expression levels in the liver and WAT and adiponectin expression level in WAT in the wogonin group were higher than those in the control group. In 3T3-L1 cells, wogonin was shown to stimulate AMPK activation in a dose-dependent manner. The presence of wogonin did not affect adipocyte differentiation or PPARγ protein level during adipogenesis. Notably, wogonin enhanced PPARα but not PPARγ transactivation.
These indicate that wogonin may have beneficial effects on glucose and lipid metabolism related to enhanced PPARα and adiponectin expression via AMPK activation. Importantly, wogonin did not cause deleterious effects, such as weight gain and fatty liver. Wogonin might be a useful therapeutic agent to treat type 2 diabetes.
汉黄芩素是从黄芩根中提取的一种黄酮类化合物。我们使用db/db小鼠评估了汉黄芩素的治疗效果。
小鼠通过口服灌胃接受汉黄芩素或赋形剂，持续2周。测量血糖、胰岛素和胆固醇水平，并通过组织病理学分析观察肝脏形态。通过实时PCR测定肝脏和白色脂肪组织（WAT）中PPARα、PPARγ和脂联素的mRNA表达水平。使用3T3-L1细胞在体外研究AMPK和PPARγ的免疫印迹以及脂肪细胞分化。使用荧光素酶测定法测量PPARα和PPARγ的结合活性。
汉黄芩素组体重增加减少，食物摄入量无变化，葡萄糖耐量得到改善。与对照组相比，汉黄芩素组的血清胰岛素和胆固醇水平显著降低。汉黄芩素组肝脏中脂滴和糖原的积累也较少。汉黄芩素组肝脏和WAT中PPARα和PPARγ的表达水平以及WAT中脂联素的表达水平均高于对照组。在3T3-L1细胞中，汉黄芩素以剂量依赖的方式刺激AMPK激活。在脂肪生成过程中，汉黄芩素的存在不影响脂肪细胞分化或PPARγ蛋白水平。值得注意的是，汉黄芩素增强了PPARα的反式激活，但没有增强PPARγ的反式激活。
这些结果表明，汉黄芩素可能通过激活AMPK增强PPARα和脂联素的表达，从而对葡萄糖和脂质代谢产生有益影响。重要的是，汉黄芩素不会引起体重增加和脂肪肝等有害影响。汉黄芩素可能是治疗2型糖尿病的一种有用的治疗药物。
