作者机构:
[赵小芳; 刘清茹; 徐博] School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China;Hunan Province Engineering Research Center of Bioactive Substance Discovery of Chinese Medicine, Changsha, 410208, China;[彭文达] Pharmaceutical Department, Hunan Provincial Mawangdui Hospital, Changsha, 410001, China;[李顺祥; 李娟] School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China, Hunan Province Engineering Research Center of Bioactive Substance Discovery of Chinese Medicine, Changsha, 410208, China
通讯机构:
[Li, S.-X.] S;School of Pharmacy, Hunan University of Chinese Medicine, Changsha, China
摘要:
BACKGROUND: Angelica sinensis and Aurantii fructu used in a pair, named Danggui-Zhiqiao herb-pair (DZHP), which was rich in essential oil and has been adopted to promote blood circulation, dispel blood stasis, and relieve pain in traditional Chinese medicine (TCM). OBJECTIVE: To analyze the composition and pharmacological effects of essential oil from DZHP. MATERIALS AND METHODS: The composition of the essential oil from DZHP was analyzed by gas chromatography/mass spectrometry (GC/MS). Its analgesic activity was evaluated by acetic acid-induced writhing test and hot plate test. The hemorheology test was carried out to evaluate the effect on hemorheology in rats with blood stasis syndrome. RESULTS: Twenty-eight components were identified and the main components were alpha-pinene (3.07%), beta-pinene (2.0%), beta-myrcene (3.71%), D-limonene (49.28%), gamma-terpinen (9.53%), alpha-terpinolene (1.80%), alpha-terpineol (2.02%), beta-bisabolene (1.13%), butylidenephthalide (1.43%), and Z-ligustilide (16.08%). The pharmacology test showed that the essential oil significantly inhibited the number of writhes induced by acetic acid with inhibition rate of 44.64% and significantly increased hot-plate latency compared with control group from 30 to 90 min after oral administration of drugs in mice. It could significantly decrease plasma viscosity, whole blood relative index at high and low shear rate, whole blood reduced viscosity at high and low shear rate, and erythrocyte rigidity index in hemorheology test. CONCLUSION: The composition of the essential oil of DZHP was determined successfully and it had analgesic and promoting blood circulation activities. SUMMARY: Angelica sinensis and Aurantii fructu used in a pair, named Danggui-Zhiqiao herb-pair (DZHP), which was rich in Essential oil and has been adopted to promote blood circulation, dispel blood stasis and relieve pain in traditional Chinese medicine (TCM).Twenty-eight components were identified and the main components were alpha-pinene (3.07%), beta-pinene (2.0%), beta-myrcene (3.71%), D-limonene (49.28%), gamma-terpinen (9.53%), alpha-terpinolene (1.80%), alpha-terpineol (2.02%), beta-bisabolene (1.13%), butylidenephthalide (1.43%), and Z-ligustilide (16.08%).The essential oil significantly inhibited the number of writhes induced by acetic acid and increased hot-plate latency compared with control group from 30 min to 90 min after oral administration of drugs in mice.The essential oil could significantly decrease plasma viscosity (PV), whole blood relative index (WBRI) at high and low shear rate, whole blood reduced viscosity (WBRV) at high and low shear rate, and erythrocyte rigidity index (ERI) in hemorheology test. Abbreviations used: DZHP: Danggui-Zhiqiao herb-pair; TCM: traditional Chinese medicine; GC/MS: gas chromatography /mass spectrometry; PV: plasma viscosity; WBRI: whole blood relative index; WBRV: whole blood reduced viscosity; ERI: erythrocyte rigidity index.
摘要:
Ezetimibe, a selective inhibitor of intestinal cholesterol absorption, effectively reduces plasma cholesterol, but its effect on atherosclerosis is unclear. Foam cell formation has been implicated as a key mediator during the development of atherosclerosis. The purpose of this study was to investigate the effects of ezetimibe on foam cell formation and explore the underlying mechanism. Our results showed that ezetimibe reduced atherosclerotic lesions in apolipoprotein E deficient (apoE-/-) mice by lowering cholesterol levels. Treatment of macrophages with Chol:MβCD resulted in foam cell formation, which was concentration-dependently inhibited by the presence of ezetimibe. Mechanically, ezetimibe treatment downregulated the expression of CD36 and scavenger receptor class B1 (SR-B1), but upregulated the expression of apoE and caveolin-1 in macrophage-derived foam cells, which kept consistent with our microarray results. Moreover, treatment with ezetimibe abrogated the increase of phospho-extracellular signal regulated kinase (ERK) 1/2 and their nuclear accumulation in foam cells. Inhibition of the MAPK pathway by the MEK inhibitor PD98059 attenuated the inhibitory effect of ezetimibe on the expression of p-ERK1/2 and caveolin-1. Taken together, our results showed that ezetimibe suppressed foam cell formation via the caveolin-1/MAPK signaling pathway, suggesting that inhibition of foam cell formation might be a novel mechanism underlying the anti-atherosclerotic effect of ezetimibe. This article is protected by copyright. All rights reserved.