title: The anti-obesity potential of sigmoidin A.
abstract: BACKGROUND
  During the last few decades, the prevalence of obesity in the western world has dramatically increased with epidemic proportions. Hand in hand with this statistic, the incidences of obesity-linked diseases such as diabetes are increasing with pandemic rate. The search for novel drugs and nutritional intervention approaches for obesity is now of significant importance.
  
  
  OBJECTIVE
  The anti-obesity potential of eriodictyol (ERD) and its close structural analogue, sigmoidin A (SGN), were evaluated. SGN was isolated from Erythrina abyssinica Lam. ex DC. (Fabaceae).
  
  
  METHODS
  Concentrations between 300 and 0.1 µM of test samples and reference drugs made in three-fold dilutions were tested for enzyme inhibitory effects. The major obesity target, pancreatic lipase, was used to test the anti-obesity potential while the selective effects of the compounds were determined through assessments of effects on α-glucosidase.
  
  
  RESULTS
  The inhibitory effect of SGN on pancreatic lipase (IC₅₀, 4.5 ± 0.87 µM) was 30-times greater than that of ERD (IC₅₀, 134 ± 19.39 µM) while their effect on α-glucosidase enzyme was comparable (IC₅₀ value of 62.5 ± 9.47 and 57.5 ± 13.15 µM). The anti-obesity drug, orlistat, inhibited pancreatic lipase with an IC₅₀ value of 0.3 ± 0.04 µM, while the anti-diabetic drug, acarbose, inhibited α-glucosidase with an IC₅₀ value of 190.6 ± 16.05 µM.
  
  
  CONCLUSIONS
  Although less active than the standard anti-obesity drug, orlistat, the observed activity indicated that prenylation of the flavonoid skeleton potently enhances anti-lipase activity.
  
  
  CONCLUSIONS
  Such groups of flavonoids need to be further investigated for their therapeutic and nutritional benefit in combating obesity problems.
authors.affiliation: Pharmacognosy Research Laboratories, Medway School of Science, University of Greenwich , Chatham-Maritime, Kent, UK. s.habtemariam@gre.ac.uk
authors.forename: Solomon
authors.initials: S
authors.lastname: Habtemariam
mesh_terms: D020909:Acarbose / Q000494:pharmacology; D019440:Anti-Obesity Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004895:Erythrina / Q000737:chemistry; D044950:Flavanones / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D007783:Lactones / Q000494:pharmacology; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015394:Molecular Structure; D000077403:Orlistat; D024301:Plant Bark; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal; D054876:Prenylation; D013329:Structure-Activity Relationship; D000520:alpha-Glucosidases / Q000378:metabolism
chemical_list: D019440:Anti-Obesity Agents; D004791:Enzyme Inhibitors; D044950:Flavanones; D005419:Flavonoids; D065089:Glycoside Hydrolase Inhibitors; D007783:Lactones; D010936:Plant Extracts; C064221:sigmoidin A; D000077403:Orlistat; D008049:Lipase; D000520:alpha-Glucosidases; C007619:eriodictyol; D020909:Acarbose