OBJECTIVETo investigate the role of ATP-binding cassette transporter G1 (ABCG1) in endothelial dysfunction induced by high glucose.

METHODSHuman aortic endothelial cells (HAECs) were incubated in the presence of 5.6 or 30 mmol/L glucose for 24-72 h with or without a 2-h pretreatment with the LXR agonist 22(R)-hydroxycholesterol. Real-time PCR and Western blotting were used to measure the mRNA and protein expressions of ABCG1; the intracellular cholesterol efflux and endothelial nitric oxide synthase (eNOS) activity were measured by scintillation counting.

RESULTSHigh glucose time-dependently suppressed ABCG1 expression and cholesterol efflux to HDL in HAECs. High glucose also decreased eNOS activity. ABCG1 down-regulation induced by high glucose, along with decreased cholesterol efflux and eNOS activity, was abolished by treatment of the cells with the LXR agonist.

CONCLUSIONEndothelial dysfunction induced by high glucose is associated with decreased ABCG1 expression.

ATP Binding Cassette Transporter, Sub-Family G, Member 1 ; ATP-Binding Cassette Transporters ; genetics ; metabolism ; Aorta ; cytology ; Cell Line ; Down-Regulation ; drug effects ; Endothelial Cells ; cytology ; metabolism ; physiology ; Glucose ; pharmacology ; Humans

OBJECTIVE： To establish the fingerprint of Mahai zhitan capsule， to determine the contents of main components， and to provide scientific basis for the stability and quality control of the preparation technology. METHODS： The determination was performed on Inertsil ODS-3 column with acetonitrile-0.1％ phosphoric acid as mobile phase （gradient elution） at the flow rate of 1.0 mL/min. The detection wavelength was set at 250 nm （0-23 min and 31-120 min） and 230 nm （23-31 min）. The column temperature was set at 30 ℃. HPLC fingerprint for 10 batches of Mahai zhitan capsule was established by using “similarity evaluation software for chromatographic fingerprint of traditional chinese medicine” （2012 edition） and the similarity was evaluated. The chromatographic peaks were assigned and identified with reference substance， negative samples without ingredient and substance control respectively， and the identified main components were quantitatively analyzed. RESULTS： The similarity of 10 batches of sample was more than 0.99； 20 common peaks were found， and 10 common peaks were identified. Among them， No. 1，13，14，15，16，17，18，19，20 chromatographic peaks originated from Rheum palmatum； No. 3，4，6，7 chromatographic peaks originated from processed Strychnos nuxvomica； No. 8 chromatographic peaks originated from Angelica sinensis； the corresponding source of medicinal materials was not found in No. 2，5，9，10，11，12 chromatographic peaks. By comparing the reference substances， No. 1，4，6，7，8，16，17，18，19 and 20 chromatographic peaks were identified as gallic acid， loganin acid， strychnine， brucine， ferulic acid， aloe-emodin， rhein， emodin， chrysophanol and emodin methyl ether， respectively. In the determination of identified five main components （loganin， strychnine， brucine， emodin and chrysophanol）， the methodological investigation met the relevant standards. In 10 batches of samples， the contents of loganin， strychnine， brucine， emodin and chrysophanol were 2.477 1-2.785 9， 1.746 1-1.946 0， 1.374 6-1.505 8， 1.573 2-1.824 1 and 0.232 1-0.261 7 mg/g， respectively. CONCLUSIONS： The established method is reliable， accurate， stable and simple， which could provide reference for the preparation technology and quality control of Mahai zhitan capsule.