Effects of novel chalcone derivatives on α-glucosidase, dipeptidyl peptidase-4, and adipocyte differentiation in vitro
Effects of novel chalcone derivatives on α-glucosidase, dipeptidyl peptidase-4, and adipocyte differentiation in vitro
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DOI：
10.5483/bmbrep.2011.44.6.410
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发表时间：
2011-06-30
期刊：
影响因子：
3.8
通讯作者：
Cha, Jeong-Heon
中科院分区：
文献类型：
--
作者：
Bak, Eun Jung;Park, Hong Gyu;Cha, Jeong-Heon
Chana系列是新的查尔酮衍生物。为了评价Chana系列作为2型糖尿病治疗药物的可能性，利用体外酶测定研究了Chana系列对α-葡萄糖苷酶和DPP-4活性的抑制作用，并在C3H10T1/2细胞中研究了它们对脂肪细胞分化的影响。 Chana 系列中的 Chana 1 和 Chana 7 显示出对 α-葡萄糖苷酶活性的显着抑制。在DPP-4酶测定中，Chana 1表现出最高的抑制活性，而Chana 7则没有。在MU测定中，Chana 1在浓度高达250μM时未显示出显着的细胞毒性，而Chana 7在浓度为300μM时观察到细胞毒性。此外，Chana 1诱导脂肪细胞分化。因此，Chana 1 显示出对 α-葡萄糖苷酶和 DPP-4 的抑制作用以及对脂肪细胞分化的刺激作用，表明 Chana 1 可能是治疗 2 型糖尿病的潜在有益药物。 [BMB 2011 年报告； 44（6）：410-414]
Chana series are new chalcone derivatives. To evaluate the possibility of Chana series as therapeutic agents of type 2 diabetes, the inhibitory effects of Chana series on the activities of alpha-glucosidase and DPP-4 were investigated using in vitro enzyme assays, and their effects on adipocyte differentiation were investigated in C3H10T1/2 cells. Chana 1 and Chana 7 among the Chana series showed significant inhibition of alpha-glucosidase activity. In DPP-4 enzyme assay, Chana 1 exhibited the highest inhibitory activity while Chana 7 did not. In MU assay, Chana 1 did not show significant cytotoxicity up to a concentration of 250 mu M, whereas cytotoxicity was observed with Chana 7 at a concentration of 300 mu M. In addition, Chana 1 induced adipocyte differentiation. Therefore, Chana 1 showed inhibitory effects on alpha-glucosidase and DPP-4 as well as a stimulatory effect on adipocyte differentiation, suggesting that Chana 1 may be a potential beneficial agent for the treatment of type 2 diabetes. [BMB reports 2011; 44(6): 410-414]