Effects of novel chalcone derivatives on α-glucosidase, dipeptidyl peptidase-4, and adipocyte differentiation in vitro

被引：23

作者：

Bak, Eun Jung ^{[4
]}

Park, Hong Gyu ^{[5
]}

Lee, ChoongHwan ^{[6
]}

Lee, Tong-Il ^{[6
]}

Woo, Gye-Hyeong ^{[7
]}

Na, Younghwa ^{[3
]}

Yoo, Yun-Jung ^{[1
,2
]}

Cha, Jeong-Heon ^{[1
,2
,4
]}

机构：

[1] Yonsei Univ, Res Ctr Orofacial Hard Tissue Regenerat, Dept Oral Biol, Oral Sci Res Ctr,Coll Dent,Project BK21, Seoul 120749, South Korea

[2] Yonsei Univ, Grad Sch, Dept Appl Life Sci, Seoul 120749, South Korea

[3] CHA Univ, Coll Pharm, Pochon 487801, South Korea

[4] Yonsei Univ, Coll Dent, Oral Canc Res Inst, Seoul 120749, South Korea

[5] Atgc Biotechnol Co Ltd, Songnam 461713, South Korea

[6] ATGen Co Ltd, Songnam 463070, South Korea

[7] Semyung Univ, Dept Clin Lab Sci, Jecheon 390711, South Korea

来源：

BMB REPORTS | 2011年 / 44卷 / 06期

关键词：

Adipocyte differentiation; alpha-Glucosidase; Chalcone derivates; DPP-4; GLUCAGON-LIKE PEPTIDE-1; GLYCYRRHIZA-INFLATA; RECEPTOR AGONISTS; INHIBITOR; RETROCHALCONES; OBESITY; GROWTH;

D O I：

10.5483/BMBRep.2011.44.6.410

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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]

引用

页码：410 / 414

页数：5

共 24 条

[1]

Astrup A, 2000, Obes Rev, V1, P57, DOI 10.1046/j.1467-789x.2000.00013.x

[2] Inhibitory effect of evodiamine alone and in combination with rosiglitazone on in vitro adipocyte differentiation and in vivo obesity related to diabetes [J].

Bak, E. J. ;

Park, H. G. ;

Kim, J. M. ;

Yoo, Y-J ;

Cha, J-H .

INTERNATIONAL JOURNAL OF OBESITY, 2010, 34 (02) :250-260

[3]

CASPARY WF, 1978, LANCET, V1, P1231

[4] Daidzein and the daidzein metabolite, equol, enhance adipocyte differentiation and PPARγ transcriptional activity [J].

Cho, Kae Won ;

Lee, Ok-Hwan ;

Banz, William J. ;

Moustaid-Moussa, Naima ;

Shay, Neil F. ;

Kim, Young-Cheul .

JOURNAL OF NUTRITIONAL BIOCHEMISTRY, 2010, 21 (09) :841-847

[5] NEW DEVELOPMENTS IN THE INCRETIN CONCEPT [J].

CREUTZFELDT, W ;

EBERT, R .

DIABETOLOGIA, 1985, 28 (08) :565-573

[6] Dipeptidyl peptidase IV inhibition reduces the degradation and clearance of GIP and potentiates its insulinotropic and antihyperglycemic effects in anesthetized pigs [J].

Deacon, CF ;

Danielson, P ;

Klarskov, L ;

Olesen, M ;

Holst, JJ .

DIABETES, 2001, 50 (07) :1588-1597

[7] BOTH SUBCUTANEOUSLY AND INTRAVENOUSLY ADMINISTERED GLUCAGON-LIKE PEPTIDE-I ARE RAPIDLY DEGRADED FROM THE NH2-TERMINUS IN TYPE-II DIABETIC-PATIENTS AND IN HEALTHY-SUBJECTS [J].

DEACON, CF ;

NAUCK, MA ;

TOFTNIELSEN, M ;

PRIDAL, L ;

WILLMS, B ;

HOLST, JJ .

DIABETES, 1995, 44 (09) :1126-1131

[8] The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes [J].

Drucker, Daniel J. ;

Nauck, Michael A. .

LANCET, 2006, 368 (9548) :1696-1705

[9] Antioxidative and superoxide scavenging activities of retrochalcones in Glycyrrhiza inflata [J].

Haraguchi, H ;

Ishikawa, H ;

Mizutani, K ;

Tamura, Y ;

Kinoshita, T .

BIOORGANIC & MEDICINAL CHEMISTRY, 1998, 6 (03) :339-347

[10] Mode of antibacterial action of retrochalcones from Glycyrrhiza inflata [J].

Haraguchi, H ;

Tanimoto, K ;

Tamura, Y ;

Mizutani, K ;

Kinoshita, T .

PHYTOCHEMISTRY, 1998, 48 (01) :125-129

← 1 2 3 →