Cimifugin - CAS 37921-38-3
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Not Intended for Therapeutic Use. For research use only.
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Cimifugin is a major components of Yu-ping-feng-san, a Chinese medical formula that is used clinically for allergic diseases and characterized by reducing allergy relapse.
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1.Simultaneous determination of 10 active components in Baizhu Shaoyao San and its single herbs by high-performance liquid chromatography coupled with diode array detection.
Zheng L1, Zhang M1, Qin K2, Cai H3, Cao G4, Cai B2. J Chromatogr Sci. 2015 Apr;53(4):633-40. doi: 10.1093/chromsci/bmu101. Epub 2014 Sep 12.
Baizhu Shaoyao San (BSS) is a famous traditional Chinese medicinal prescription, which is composed of Rhizome atractylodis macrocephalae, Radix Paeoniae Alba, Pericarpium Citri Reticulatae and Radix Saposhnikovia. In this study, a simple and sensitive high-performance liquid chromatography coupled with diode array detection method was established for the simultaneous determination of 10 marker compounds including atractylenolide I, gallic acid, albiflorin, paeoniflorin, narirutin, hesperidin, nobiletin, cimifugin, prim-O-glucosylcimifugin, 4'-O-β-d-glucosyl-5-O-methylvismminol in BSS and its single herbs. The chromatographic separation was performed using a YMC C18 column with a gradient elution system of acetonitrile and 0.1% formic acid aqueous solution at a flow rate of 1 mL/min. The results demonstrated that the validated method was simple, reliable and successfully applied to evaluate the selected compounds in BSS and its single herbs for quality control.
2.[Studies on effects of calycosin-7-O-β-D-glucoside on prim-O-glucosylcimifugin and cimifugin in vivo pharmacokinetics].
Zhao XL, Liu L, Di LQ, Li JS, Kang A. Zhongguo Zhong Yao Za Zhi. 2014 Dec;39(23):4669-74.
Study on the effects of Astragali Radix main active flavone calycosin-7-O-β-D-glucoside on Saposhnikoviae Radix main active ingredients prim-O-glucosylcimifugin and cimifugin, a UPLC-MS/MS method for simultaneous determination of prim-O-glucosylcimifugin and cimifugin in rat plasma was established, and the comparative pharmacokinetics of prim-O-glucosylcimifugin and cimifugin after oral administration of prim-O-glucosylcimifugin and calycosin-7-O-β-D-glucoside-prim-O-glucosylcimifugin to rats were carried out, which might be conductive in exploring the rationality of Astragali Radix - Saposhnikoviae Radix herb couple. Twelve male SD rats were divided into two groups. Prim-O-glucosylcimifugin and cimifugin in rat plasma of different time points after oral administration of prim-O-glucosylcimifugin and calycosin-7-O-β-D-glucoside - prim-O-glucosylcimifugin to rats were determinated. And the main pharmacokinetic parameters were investigated using DAS 3.
3.Metabolism studies on prim-O-glucosylcimifugin and cimifugin in human liver microsomes by ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry.
Jia P1,2, Zhang Y1, Zhang Q1, Sun Y1, Yang H1, Shi H1, Zhang X1, Zhang L1. Biomed Chromatogr. 2016 Feb 23. doi: 10.1002/bmc.3711. [Epub ahead of print]
Prim-O-glucosylcimifugin (PGCN) and cimifugin (CN) are major constituents of Radix Saposhnikoviae which have pharmacological activities of antipyretic, analgesic and anti-inflammatory. However, there were few reports with respect to the metabolism of PGCN and CN in vitro. In this paper, we describe a strategy using ultra- performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) for fast analysis of the metabolic profile of PGCN and CN in human liver microsomes. In total, 5 phase I metabolites of PGCN, 7 phase I metabolites and 2 phase II metabolites of CN were identified in the incubation of human liver microsomes. The results revealed that the main phase I metabolic pathways of PGCN were hydroxylation and hydrolysis reactions. The phase I metabolic pathways of CN were found to be hydroxylation, demethylation, dehydrogenation, and so on. Meanwhile, the results indicated that O-glucuronidation was the major metabolic pathway of CN in phase II metabolism.
4.Biotransformation of prim-O-glucosylcimifugin by human intestinal flora and its inhibition on NO production and DPPH free radical.
Zhao B1, Yang XB, Yang XW, Liu JX. J Asian Nat Prod Res. 2012;14(9):886-96. doi: 10.1080/10286020.2012.702756. Epub 2012 Aug 23.
prim-O-Glucosylcimifugin (PGCN), a highest content chromone in the roots of Saposhnikovia divaricata, was incubated with human intestinal flora (HIF), and two biotransformation products were obtained from the incubated solution by chromatographic methods. The chemical structures of the two biotransformation products were elucidated as cimifugin (CN) and 5-O-methylvisamminol (MVL), respectively, on the basis of NMR and MS data. The biotransformation product CN was formed through a deglucosylation of PGCN by β-glucosidase secreted from the HIF, and then the hydroxymethyl group of CN was reduced to lead to occurrence of MVL. All of these compounds were evaluated for their effect on the inhibition of nitric oxide production induced by lipopolysaccharide in macrophage cell line RAW 264.7 and for 1,1-diphenyl-2-picrylhydrazyl free-radical scavenging activity in cell-free bioassay system.
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CAS 37921-38-3 Cimifugin

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