title: Evaluation of hypoglycemic activity of total lignans from Fructus Arctii in the spontaneously diabetic Goto-Kakizaki rats.
abstract: BACKGROUND
  Fructus Arctii, called "Niubangzi" in China (Great burdock achene in English), is a well-known Chinese Materia Medica. It is the dried ripe fruit of Arctium lappa L. (family Asteraceae) and was included in the Chinese pharmacopoeia for its traditional therapeutic actions. Meanwhile it has been utilized extensively in a number of classical drug formulas as a major component for the treatment of noninsulin-dependent diabetes mellitus. It has also been reported recently that the clinical use of Fructus Arctii resulted in a satisfactory hypoglycemic effect in diabetic patients. The aim of this study was to investigate hypoglycemic activity of total lignans from Fructus Arctii (TLFA) in Goto-Kakizaki (GK) rats, a spontaneous type 2 diabetic animal model, and the mechanism of its hypoglycemic activity.
  
  
  METHODS
  Male GK rats and normal Wistar rats were used in this study, GK rats fed twice daily were given TLFA (300 mg/kg) or nateglinide (50mg/kg) orally before each meal for 12 weeks. Besides common evaluation indexes of hypoglycemic activity such as blood glucose level, oral glucose tolerance test (OGTT), glycated hemoglobin, as well as lipid metabolism parameters such as cholesterol (CHOL), triglycerides (TG), et al., in rat serum. The effects of TLFA on insulin secretion and pancreas tissue sections, the levels of serum glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), and the α-glucosidase inhibitory activity of TLFA in vitro were investigated.
  
  
  RESULTS
  TLFA demonstrated stable and long-lasting hypoglycemic activity in GK rats and showed significant improvement in glucose tolerance in glucose fed hyperglycemic GK rats. Both TLFA and nateglinide controlled the glycosylated hemoglobin levels of the experimental animals very well. Stimulation of insulin secretion was proved to be one of the hypoglycemic mechanism of TLFA, promoting the release of GLP-1 should be another one, and ɑ-glucosidase inhibitory activity of TLFA also contributes to its hypoglycemic activity. In this study, we didn't found that TLFA could effect the body weight of GK rats, which was also verified by the changes of biochemical parameters of blood in experimental rats.
  
  
  CONCLUSIONS
  The results of this study indicates that TLFA has significant hypoglycemic potential in GK rats, and it may be acting through stimulating insulin secretion, promoting the release of GLP-1, and decreasing intestinal absorption of glucose.
authors.affiliation: Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine, Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address: zhhxu1970@gmail.com.
authors.forename: Zhaohui
authors.initials: Z
authors.lastname: Xu
authors.affiliation: Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine, Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Jiaxing
authors.initials: J
authors.lastname: Ju
authors.affiliation: Center for Drug Safety Evaluation, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Wang
authors.affiliation: Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine, Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Chenchen
authors.initials: C
authors.lastname: Gu
authors.affiliation: Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine, Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Feng
mesh_terms: D000818:Animals; D031170:Arctium / Q000737:chemistry*; D001786:Blood Glucose / Q000187:drug effects; D002097:C-Reactive Protein / Q000378:metabolism; D002940:Circadian Rhythm; D003920:Diabetes Mellitus / Q000188:drug therapy*; D004334:Drug Administration Schedule; D005638:Fruit / Q000737:chemistry*; D005749:Gastric Inhibitory Polypeptide / Q000235:genetics / Q000378:metabolism; D005786:Gene Expression Regulation; D052216:Glucagon-Like Peptide 1 / Q000235:genetics / Q000378:metabolism; D005951:Glucose Tolerance Test; D007328:Insulin / Q000097:blood; D017705:Lignans / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017208:Rats, Wistar
chemical_list: D001786:Blood Glucose; D007328:Insulin; D017705:Lignans; D005749:Gastric Inhibitory Polypeptide; D052216:Glucagon-Like Peptide 1; D002097:C-Reactive Protein
keywords: CHOL; DM; Diabetes; ELISA; FBG; Fructus Arctii; GIP; GK rats; GLP-1; Goto-Kakizaki rats; HDL-C; Hypoglycemic activity; Insulin secretion; LDL-C; OGTT; PBG; TG; TLFA; cholesterol; diabetes mellitus; enzyme-linked immunosorbent assay; fasting blood glucose; glucagon-like peptide-1; glucose-dependent insulinotropic polypeptide; high density lipoprotein cholesterol; low density lipoprotein cholesterol; oral glucose tolerance test; postprandial blood glucose; total lignans from Fructus Arctii.; triglycerides