ABSTRACT
The ethanol extract of Atractylodes lancea rhizome displayed significant lipase inhibition with an IC50 value of 9.06 µg/mL in a human pancreatic lipase assay from high-throughput screening. Bioassay-guided isolation led to the identification of one new polyacetylene, syn-(5E,11E)-3-acetoxy-4-O-(3-methylbutanoyl)-1,5,11-tridecatriene-7,9-diyne-3,4-diol (7), along with six known compounds (1-6). The structure of compound 7 was determined based on the analysis of NMR and MS data. Among these seven lipase inhibitors, the major compound atractylodin (1) showed the highest lipase inhibitory activity (IC50 = 39.12 µM). The antiobesity effect of the ethanol extract of Atractylodes lancea rhizome was evaluated in a high-fat diet-induced obesity mice model at daily dosages of 250 mg/kg and 500 mg/kg body weight for 4 weeks, and treatment with this extract demonstrated a moderate efficacy at the 500 mg/kg dose level.
Subject(s)
Anti-Obesity Agents/pharmacology , Atractylodes/chemistry , Furans/pharmacology , Lipase/antagonists & inhibitors , Plant Extracts/pharmacology , Polyynes/pharmacology , Animals , Anti-Obesity Agents/chemistry , Anti-Obesity Agents/isolation & purification , Body Weight , Butyrates/chemistry , Butyrates/isolation & purification , Butyrates/pharmacology , Diet, High-Fat/adverse effects , Disease Models, Animal , Furans/chemistry , Furans/isolation & purification , High-Throughput Screening Assays , Humans , Inhibitory Concentration 50 , Mice , Mice, Inbred C57BL , Molecular Structure , Pancreas/enzymology , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Polyynes/chemistry , Polyynes/isolation & purification , Rhizome/chemistryABSTRACT
Anti-inflammatory properties of both baicalin and catechins have been widely reported. However, the reports of analgesic effects of baicalin and catechins are limited. Three commonly used pain-related animal models were employed to evaluate the analgesic activity of UP446, a standardized bioflavonoid composition of baicalin and catechins. Carrageenan-induced paw edema, formalin test, and abdominal constriction assays were used to evaluate antinociceptive activity of 150 mg/kg or 100 mg/kg oral doses of UP446. Ibuprofen was used as a reference compound in each test. Pretreatment of carrageenan-induced hyperalgesic animals with UP446 at 150 mg/kg oral dosage reduced the hypersensitivity of pain by 39.5%. Similarly, a single dose of UP446, given orally at 100 mg/kg, exhibited 58% and 71.9% inhibition in pain sensitivity compared to vehicle-treated control in writhing and formalin tests, respectively. These findings suggest that the standardized anti-inflammatory bioflavonoid composition, UP446, could also be employed to inhibit nociception.
