Vaiyapuri Sivajothi1, Shruthi Shirur Dakappa2. 1. Department of Pharmaceutical Chemistry, The Oxford College of Pharmacy, Bangalore -68, Karnataka, India. 2. Microbiology and Cell Biology Department, Indian Institute of Science, Bangalore-560012, Karnataka, India.
Abstract
OBJECTIVE: To investigate the in vitro antidiabetic effects of isolated 4-Oxo-4H-pyran-2,6-dicarboxylic acid bis-[6-methyl-heptyl] ester from the chloroform extract of root of Tragia cannabina (T. cannabina) and AMP kinase activation property of the isolated compound. METHODS: The roots of T. cannabina were collected and extracted with ethanol [95% v/v] then chromatographed over silica gel 60-120 mesh of column length 100 cm and diameter 3 cm. Elution was carried out with solvents and solvent mixtures of increasing polarities. Then the chloroform extract was used for isolation. In vitro antidiabetic activity was performed with fertile eggs of White Leghorn chicks by induction of diabetes by streptozotocin. RESULTS: The isolated pyran ester binds very efficiently within the active pocket of AMPK with the formation of hydrogen bond and consuming less binding energy, which is good when compared to orientation of standard drug metformin. In in vitro antidiabetic evaluation by streptozotocin treated chick embryo the administration of isolated compound at a doses of 0.5 mg/egg and 1 mg/egg produced a significant reduction in the blood glucose levels in a dose dependant manner (P<0.01). The blood glucose level of diabetic control was (244.20±12.64) mg/dL, whereas it was (207.40±2.43) mg/dL (P<0.001) for isolated compound 0.5 mg/egg and 174.800±2.410 mg/dL (P<0.001) for 1 mg/ egg of the isolated compound. CONCLUSIONS: The significant glucose levels were reduced (P<0.01) after administration of the pyran ester isolated from T. cannabina to streptozotocin treated chick embryo.
OBJECTIVE: To investigate the in vitro antidiabetic effects of isolated 4-Oxo-4H-pyran-2,6-dicarboxylic acid bis-[6-methyl-heptyl] ester from the chloroform extract of root of Tragia cannabina (T. cannabina) and AMP kinase activation property of the isolated compound. METHODS: The roots of T. cannabina were collected and extracted with ethanol [95% v/v] then chromatographed over silica gel 60-120 mesh of column length 100 cm and diameter 3 cm. Elution was carried out with solvents and solvent mixtures of increasing polarities. Then the chloroform extract was used for isolation. In vitro antidiabetic activity was performed with fertile eggs of White Leghorn chicks by induction of diabetes by streptozotocin. RESULTS: The isolated pyran ester binds very efficiently within the active pocket of AMPK with the formation of hydrogen bond and consuming less binding energy, which is good when compared to orientation of standard drug metformin. In in vitro antidiabetic evaluation by streptozotocin treated chick embryo the administration of isolated compound at a doses of 0.5 mg/egg and 1 mg/egg produced a significant reduction in the blood glucose levels in a dose dependant manner (P<0.01). The blood glucose level of diabetic control was (244.20±12.64) mg/dL, whereas it was (207.40±2.43) mg/dL (P<0.001) for isolated compound 0.5 mg/egg and 174.800±2.410 mg/dL (P<0.001) for 1 mg/ egg of the isolated compound. CONCLUSIONS: The significant glucose levels were reduced (P<0.01) after administration of the pyran ester isolated from T. cannabina to streptozotocin treated chick embryo.
Authors: Christian Frøsig; Christian Pehmøller; Jesper B Birk; Erik A Richter; Jørgen F P Wojtaszewski Journal: J Physiol Date: 2010-09-13 Impact factor: 5.182