Study on E-6-O-p-coumaroyl Scandoside Methyl Ester from Hedyotis Diffusa
|School||Shenyang Pharmaceutical University|
|Keywords||Hedyotis diffusa Trans- 6-O- coumaroyl Paederia vine glycoside methyl ester Coumarate Pharmacokinetics|
According to statistics, currently used anticancer effects of traditional Chinese medicine experience Fang, Hedyotis diffusa highest utilization rate, the drug is widely used to treat a variety of tumors, especially for the digestive system tumors, such as esophageal cancer, stomach cancer, liver cancer, rectal cancer treatment. In research diffusa injection fingerprinting process, we isolated from medicinal obtained p-coumaric acid, this component is a phenolic-based compound, as an anti-oxidant having a pharmacological activity of anti-colon cancer and cardiovascular disease, and non-toxic to the human body. Phenolic compounds including ferulic acid, coumaric acid, caffeic acid and other antioxidant components plants worldwide has become research hotspot. From diffusa, extraction and separation has been active compounds trans-6-O-the coumaroyl Paederia vine glycoside methyl ester (the compound is p-coumaric acid prodrug); HPLC method was established for the first time determined Radix trans-6-O-coumaroyl chicken shit vine glycosides methyl ester content; HPLC-UV method in rat plasma trans-6-O-glycosides methyl coumaroyl chicken shit vine chicken shit vine glycoside methyl ester after trans-6-O-coumaric acid and coumaric acid content and Rats were given prototype drugs and their metabolites in vivo drug coumarate dynamic process . 1. Trans-6-O-coumaric the acyloxy Paederia vine glycoside methyl ester Preparation of trans-6-O-coumaric the acyloxy Paederia vine glycosides methyl iridoid glycosides, the compound may be provided in the body through ester enzymatic degradation of p-coumaric acid, extracted from Hedyotis diffusa herbs prepared trans-6-O-coumaroyl the chicken droppings vine glycosides methyl, and their structures were confirmed. 2. HPLC determination of trans-6-O-Radix coumaroyl chicken shit vine glycoside content of methyl HPLC method for determination of 12 different Radix trans-6-O-coumaroyl Paederia vine glycosides the content of methyl column C18 column, a mobile phase of methanol - water (45:55, v / v), the detection wavelength was 310nm, the flow rate was 1.0mL · min -1 sup> column greenhouse temperature. Orthogonal design effects of trans-6-O-coumaroyl the the chicken droppings vine glycosides methyl ester extraction process to determine the optimum extraction conditions. 3. Rats were given 6-O-trans pharmacokinetic study of the coumaroyl Paederia rattan glycosides methyl after prototype and metabolites amended and perfected first conventional literature search ideas. For the first time established a HPLC-UV method in rat plasma trans-6-O-coumaroyl chicken shit vine glycosides methyl content, chromatographic conditions to: DiamonsilTM the ODS (250mm × 4.6 mm, 5 μm) column, methanol - acetonitrile - water (30:15:55, v / v) as the mobile phase, detection wavelength was 310 nm, column temperature at room temperature. The law to chloramphenicol as internal standard, the linear range of 0.2-20μg · mL -1 sup>, and the limit of quantification was 0.2μg · mL -1 sup>. HPLC-UV method coumaric acid content of rat plasma, chromatographic conditions: DiamonsilTMODS (250 mm × 4.6 mm, 5μm) column, acetonitrile - water (21:79, v / v / v) containing 1% glacial acetic acid as the mobile phase, detection wavelength of 310 nm, the column temperature at room temperature. The Act tinidazole as the internal standard, the linear range of 0.02-5.0μg · mL -1 sup>, and the lower limit of quantification 0.02μg · mL -1 sup>. Rats were given 20 mg / kg trans-6-O-coumaric acid the the chicken droppings vine glycosides methyl ester, a prototype drug is rapidly metabolized in the body, four rats only one in the administration 5,10,20 min three points of time is able to detect the component. Metabolites in rat plasma coumarate time to peak the T max, 1.2 ± 0.3 h, the peak concentration C max 0.236 ± 0.047μg/mL, elimination half-life T 1/2 1.3 ± 0.5 h, the peak area of ??the plasma concentration - time curve AUC 0-t 23.8 ± 5.1μg min for / mL.