A herbal extract with acetyl-coenzyme A carboxylase inhibitory activity and its potential for treating metabolic syndrome.
Acetyl-coenzyme A carboxylase (ACC) plays a crucial role in fatty acid metabolism, and its inhibition is an effective approach for treating metabolic syndrome. Partially purified ACC from rat liver was used to screen herbs commonly used in Taiwanese folk medicine for ACC inhibitory effects. An ethanol extract of Polygonum hypoleucum Ohwi (EP), the Taiwan tuber fleece flower, was found to have the highest inhibitory activity (half-maximal inhibitory concentration = 30 microg/mL). We then tested the physiologic effects of EP using high-fat (HF) diet-fed C57BL/6J mice. After 4 weeks, body weight and levels of blood glucose, insulin, triacylglycerol, total cholesterol, and leptin were significantly reduced (P < .05) in mice fed a 3% EP-containing HF diet. The EP also improved the glucose tolerance and insulin sensitivity of HF diet-fed mice. In addition, EP at concentrations of 0.0725 and 0.145 mg/mL (2.5- and 5-fold higher than the half-maximal inhibitory concentration) was also effective in decreasing ACC and fatty acid synthase activity and the triacylglycerol content of HepG2 cells incubated in high-glucose (30 mmol/L) medium. These results show that EP, acting by inhibiting ACC activity, is effective in alleviating the symptoms associated with metabolic disease.
Chen
Chi-Hua
CH
Food Industry Research Development Institute, Hsinchu 300, Taiwan.
Chang
Mei-Yui
MY
Lin
Yu-Shen
YS
Lin
Da-Gin
DG
Chen
Shiow-Wen
SW
Chao
Pei-Min
PM
D000103:Acetyl-CoA Carboxylase / Q000037:antagonists & inhibitors*; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002478:Cells, Cultured; D004036:Diet, Atherogenic; D004041:Dietary Fats / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004365:Drugs, Chinese Herbal / Q000494:pharmacology / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D000431:Ethanol / Q000494:pharmacology; D022781:Hepatocytes / Q000187:drug effects / Q000378:metabolism; D050155:Lipogenesis / Q000187:drug effects; D008297:Male; D024821:Metabolic Syndrome / Q000188:drug therapy* / Q000209:etiology; D051379:Mice; D008810:Mice, Inbred C57BL; D010936:Plant Extracts / Q000494:pharmacology* / Q000627:therapeutic use*; D028502:Polygonum / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar
D001786:Blood Glucose; D004041:Dietary Fats; D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D000431:Ethanol; D000103:Acetyl-CoA Carboxylase