FLAVONOIDS AND ITS DERIVATIVES FROM CALLISTEPHUS CHINENSIS FLOWERS AND THEIR INHIBITORY ACTIVITIES AGAINST Α-GLUCOSIDASE Xiaoshu Zhang1, Zhenting Liu2, Xiuli Bi3, Jingxin Liu2, Wei Li1, Yuqing Zhao*1
1
School of Traditional Chinese Medicine, Shenyang Pharmaceutical University,
Shenyang 110016, China
2
Chifeng MinYi Natural Anthocyanins Company Limited. Inner Mongolia Autonomous
Region, 024000, China
3
School of Life Science, Liaoning University, Shenyang 110036, China
* Correspondence to: Yuqing Zhao; School of Traditional Chinese Medicine, Shenyang
Pharmaceutical University, Shenyang 110016, People’s Republic of China;
Inhibitors of carbohydrate-hydrolysing enzymes play an important role for the treatment of diabetes. One of the therapeutic methods for decreasing of postprandial hyperglycemia is to retard absorption of glucose by the inhibition of carbohydrate- hydrolysing enzymes, such asα-glucosidase, in the digestive organs. To investigate the therapeutic potential of compounds
from natural sources, Callistephus chinensis flowers (CCF) were tested for inhibition of α-glucosidase, and acarboes was used as the positive control. The 70 % ethanol extract of CCF exhibited significant α-glucosidase inhibitory activities with IC50 value of 8.14 μg/ml. The stepwise polarity fractions of CCF were tested further for in vitro inhibition of α-glucosidase.
The ethyl acetate (EtOAc) fraction exhibited the most significant inhibitory activity. Eight pure compounds, apigenin, apigenin-7-O-β-D- glucoside, kaempferol, hyperin, naringenin, quercetin, luteolin, and kaempferol-7-O-β-D- glucoside, were isolated (using enzyme assayguide fractionation method) from the EtOAc fraction. Among these, quercetin was the most active one (IC50 values 2.04 μg/ml), and it appears that the inhibiting percentages are close to acarbose (IC50 values 2.24 μg/ml), the positive control, on α-glucosidase inhibition.HPLC/UV analysis indicated that the major components of CCF are kaempferol, hyperin and
quercetin. The presented results revealed that CCF containing these eight flavonoids could bena useful natural source in the development of a novel α-glucosidase inhibitory agent against diabetic complications.
Food Funct. 2014 Dec;5(12):3304-10. doi: 10.1039/c4fo00637b.
Effects of Callistephus chinensis flower polyphones on improving metabolic disorders in high-fat diet-induced mice.
Bi X1, Liu W, Xia X, Chen L, Mu T, Liu J, Hou Y, Zhao Y.
The aim of this study was to investigate the effects of Callistephus chinensis flower (CCF) polyphones on symptoms of metabolic syndrome in a newly developed high-fat diet-induced non-alcoholic fatty liver disease (NAFLD) mouse model. C57BL/6J mice were fed a high fat diet (HFD; 50% energy as fat) with normal drinking fluid or HFD with CCF polyphones (50 mg L(-1) or 100 mg L(-1)) in drinking fluid for 12 weeks. As a comparison, mice fed a normal-fat (NFD; 10% energy as fat) and with normal drinking fluid were also included. The HFD group developed more severe symptoms of metabolic syndrome than the NFD group. CCF polyphones treatment significantly reduced fecal lipids compared to the HFD group, suggesting a strong indication of improved lipid metabolism. Liver damage and liver triglyceride levels were also decreased by CCF polyphones treatment. Moreover, both morphologic and histological detections indicated that CCF polyphones significantly reversed HFD-induced hepatic steatosis and liver injury. Furthermore, CCF polyphones significantly ameliorated both HFD-induced metabolic disorders, such as insulin resistance, and inflammatory cytokines, including interlukin-6 (IL-6) and tumor necrosis factor-α (TNF-α). Moreover, hepatic peroxisome proliferator-activated receptor (PPARα) and the gene involved in PPARα, Peroxisomal acyl-CoA oxidase (ACOX), were markedly up-regulated at protein levels by CCF polyphones. Our results demonstrate that the HFD produces metabolic syndrome of NAFLD, and CCF polyphones treatment can alleviate these symptoms. The beneficial effects of CCF polyphones are associated with improved lipid metabolism and reduced levels of inflammatory cytokines.