title: Determination of bioactive markers in Cleome droserifolia using cell-based bioassays for antidiabetic activity and isolation of two novel active compounds.
abstract: The antidiabetic activities of the aqueous (AqEx) and ethanolic (AlEx) extracts of Cleome droserifolia (Forssk.) Del., were tested in cultured C2C12 skeletal muscle cells and 3T3-L1 adipocytes. An 18-h treatment with the AqEx increased basal glucose uptake by 33% [insulin equivalent (IE)=1.3±0.04] in muscle cells comparable to a 25.5% increase caused by 100 nM insulin (IE=1±0.03). Fractionation of the tested AqEx yielded hexane (HxFr), chloroform (ClFr) and ethyl acetate (EtFr) fractions which exerted 38, 52 and 35% increase in the glucose uptake corresponding to an IE of 1.5±0.06, 2.0±0.04 and 1.4±0.04, respectively. Only the ClFr and EtFr accelerated the triglyceride accumulation [rosiglitazone equivalent (RE) was 0.9±0.13 and 0.63±0.12, respectively] in pre-adipocytes undergoing differentiation comparably with 10 μM rosiglitazone. Six terpenoids (C1-C6) and three flavonol glycosides (F1-F3) were isolated from the active ClFr and EtFr, respectively, and identified. C5, C2 and C4 had an IE of 0.86±0.05, 1.01±0.04 and 0.9±0.08, while F1, F2 and F3 gave an IE of 1.3±0.05, 2.3±0.05 and 2.0±0.04, respectively. We could conclude that the reported antihyperglycemic activity of Cleome droserifolia is attributed to significant insulin-like effects in peripheral tissues, and that compounds F2 and F3, being highly active, could be used as bioactive markers to standardize the C. droserifolia herbal extract.
authors: Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Kasr-El-Ainy St., Cairo 11562, Egypt. a motaal@hotmail.com
authors: A Abdel
authors: AA
authors: Motaal
authors: S M
authors: SM
authors: Ezzat
authors: P S
authors: PS
authors: Haddad
mesh_terms: D041721:3T3-L1 Cells; D017667:Adipocytes / Q000187:drug effects / Q000378:metabolism; D050156:Adipogenesis / Q000187:drug effects; D000818:Animals; D015415:Biomarkers / Q000032:analysis; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D031485:Cleome / Q000737:chemistry*; D003920:Diabetes Mellitus / Q000188:drug therapy* / Q000378:metabolism; D004534:Egypt; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology; D005947:Glucose / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000302:isolation & purification* / Q000494:pharmacology*; D007328:Insulin / Q000096:biosynthesis; D016488:Medicine, African Traditional; D051379:Mice; D018482:Muscle, Skeletal / Q000187:drug effects / Q000378:metabolism; D008517:Phytotherapy; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal / Q000737:chemistry; D013729:Terpenes / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D015415:Biomarkers; D005419:Flavonoids; D007004:Hypoglycemic Agents; D007328:Insulin; D010936:Plant Extracts; D013729:Terpenes; D005947:Glucose