Senkyunolide A

Relaxation effects of ligustilide and senkyunolide A, two main constituents of Ligusticum chuanxiong, in rat isolated aorta.[Pubmed: 17222996]

J Ethnopharmacol. 2007 May 22;111(3):677-80.

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.

Low oral bioavailability and pharmacokinetics of senkyunolide a, a major bioactive component in Rhizoma Chuanxiong, in the rat.[Pubmed: 17304150]

Ther Drug Monit. 2007 Feb;29(1):49-56.

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.

Zhongguo Zhong Yao Za Zhi. 2014 May;39(9):1650-5.

[Quantitative determination of 5 active ingredients in different harvest periods of Ligusticum chuanxiong by HPLC].[Pubmed: 25095378]

A simple and quick method is described for the determination of ferulic acid, senkyunolide I, senkyunolide H, Senkyunolide A and ligustilide in rhizomes of Ligusticum chuanxiong.
METHODS AND RESULTS:
The 5 active ingredients in the sample was extracted using 40% ethanol and analyzed by reversed-phase high performance liquid chromatography (HPLC). Chromatography separation was performed using Agilent 1100 series HPLC system with a Symmetry C18 column and gradient elution with a mixture of three solvents : solvent A, acetonitrile, solvent B, methanol and solvent C, 1% aqueous acetic acid, 0 min to 5 min A: B: C 20: 40: 40, 5 min to 30 min A: B: C 60 to 100 : 0 : 40 to 0. The effluent was monitored using a VWD detector set at 321 nm (0-4.3 min) and 275 nm (4.31-30 min). The flow rate was set at 1 mL x min(-1) and the injection volume was 10 microL. The column temperature was maintained at 35 degrees C. The calibration curve was linear (r > or = 0.99) over the tested ranges. The average recovery was 94.44%-103.1% (n = 6). The method has been successfully applied to the analysis in different harvest periods of L. chuanxiong samples.
CONCLUSIONS:
In this paper, single-factor randomized block design to study the 5 components content of L. chuanxiong on ten collecting stages. For the L. chuanxiong collected from April 15th to May 30rd, the content of 5 ingredients increased primarily, and then decreased. Determine the appropriate harvest time has important significance to the promotion of the quality of L. chuanxiong.

Chem Pharm Bull (Tokyo). 2005 Nov;53(11):1480-3.

Identification and comparative determination of senkyunolide A in traditional Chinese medicinal plants Ligusticum chuanxiong and Angelica sinensis by HPLC coupled with DAD and ESI-MS.[Pubmed: 16272738]

METHODS AND RESULTS:
Using the HPLC/DAD/ESI/MS method, the qualitative and quantitative analysis of Senkyunolide A (SA) in the rhizomes of Ligusticum chuanxiong (Rhizoma chuanxiong; CX) and roots of Angelica sinensis (DG) was established. As a result, it was found that Senkyunolide A is a characteristic standard compound for the quality evaluation and chemical differentiation between CX and DG. Methanol was chosen in the preparation of standard solutions and extraction of samples based on the stability data. The identity of Senkyunolide A in CX and DG was unambiguously determined based on the quasimolecular ions in ESI-MS. A comprehensive validation of the method, including sensitivity, linearity, reproducibility and recovery, was conducted using the optimized chromatographic conditions. The linear calibration curve was acquired with R2>0.999 and limit of detection (S/N=3) was estimated to be 12.5 mug/g. The reproducibility was evaluated by repeated sample injection and replicated analysis of samples with the relative standard deviation (RSD) value found within 0.68%. The recovery rates of Senkyunolide A varied within the range of 96.91-101.50% with RSD less than 2.38%. In the present work, the contents of Senkyunolide A were quantified within 3.94-9.14 mg/g and 0.108-0.588 mg/g for 12 batches each of CX and DG.
CONCLUSIONS:
The results demonstrated that Senkyunolide A is a useful standard compound for the quality evaluation and chemical differentiation between CX and DG. The analytical procedure is precise and reproducible and thus suitable for the analysis of a large number of samples.