| Description: |
Senkyunolide A is a useful standard compound for the quality evaluation and chemical differentiation between Rhizoma chuanxiong and Angelica sinensis, and suitable for the analysis of a large number of samples. Senkyunolide A has the vasorelaxation activity in contractions to various contractile agents in rat isolated aorta. |
| In vitro: |
| J Ethnopharmacol. 2007 May 22;111(3):677-80. | | Relaxation effects of ligustilide and senkyunolide A, two main constituents of Ligusticum chuanxiong, in rat isolated aorta.[Pubmed: 17222996] | Ligusticum chuanxiong Hort. (Umbelliferae) is a widely prescribed traditional Chinese medicinal herb for cardiovascular diseases in China. However, the cardiovascular actions of ligustilide and senkyunolide A, two of the most abundant Ligusticum chuanxiong constituents, have yet to be examined. The objective of the present study was to investigate the vasorelaxation effects of ligustilide and senkyunolide A and their underlying mechanisms in rat isolated aorta.
METHODS AND RESULTS:
Both constituents had similar relaxation potencies against contractions to 9,11-dideoxy-9alpha,11alpha-methanoepoxyprostaglandin F(2alpha), phenylephrine, 5-hydroxytryptamine and KCl. Their vasorelaxation effects were not affected by endothelium removal, the adenylate cyclase inhibitor 9-(tetrahydro-2-furanyl)-9H-purin-6-amine, the soluble guanylate cyclase inhibitor 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, or the non-selective K+ channel blocker tetraethylammonium.
CONCLUSIONS:
This is the first report to demonstrate the vasorelaxation activities of ligustilide and senkyunolide A in contractions to various contractile agents in rat isolated aorta. The underlying mechanisms await further investigations. |
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| In vivo: |
| Ther Drug Monit. 2007 Feb;29(1):49-56. | | Low oral bioavailability and pharmacokinetics of senkyunolide a, a major bioactive component in Rhizoma Chuanxiong, in the rat.[Pubmed: 17304150] | The pharmacokinetics of Senkyunolide A, one of the major bioactive ingredients in the traditional Chinese medicinal herb Rhizoma Chuanxiong, which is commonly used for the treatment of cardiovascular diseases, was studied in rats.
METHODS AND RESULTS:
After intravenous (IV) administration, Senkyunolide A was extensively distributed (Vd/F: 6.74 +/- 0.73 L/kg) and rapidly eliminated from the plasma (CL/F: 7.20 +/- 0.48 L/h per kilogram and t1/2: 0.65 +/- 0.06 hr). Hepatic metabolism was suggested as the major route of Senkyunolide A elimination as indicated by the results of in vitro S9 fraction study. After intraperitoneal (IP) administration, Senkyunolide A exhibited dose-independent pharmacokinetics. The absorption after IP administration was rapid (Tmax: 0.04 +/- 0.01 hours), and the bioavailability was 75%. After oral administration, Senkyunolide A was also absorbed rapidly (Tmax: 0.21 +/- 0.08 hours); however, its oral bioavailability was low (approximately 8%). The contributing factors were determined to be instability in the gastrointestinal tract (accounting for 67% of the loss) and hepatic first-pass metabolism (accounting for another 25%).
CONCLUSIONS:
Pharmacokinetics of Senkyunolide A were unaltered when Chuanxiong extract was administered, which suggests that components in the extract have insignificant effects on Senkyunolide A pharmacokinetics. |
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