Abstract
Angoroside C is a phenylpropanoid glycoside compound isolated from the dried root of Scrophularia ningpoensis Hemsl., which possesses the effects of preventing ventricular remodeling, reducing pulmonary oedema, and reducing blood pressure, as well as having the properties of anti-platelet aggregation, hepatoprotection and anti-nephritis, etc. However, few investigations have been conducted on the absorption, distribution, metabolism, and excretion (ADME) study of angoroside C. Thus, a fast ultra-high performance liquid chromatography-tandem quadrupole mass spectrometry (UPLC-MS/MS) method was established for the determination of angoroside C and its metabolite ferulic acid in rat plasma and tissue homogenate. The two analytes were extracted from the biosamples using a simple protein precipitation with acetonitrile. The developed method was validated and successfully applied to the pharmacokinetics, bioavailability and tissue distribution study after the intragastric administration of angoroside C (100 mg/kg) or the intravenous administration of angoroside C (5 mg/kg), respectively. The results showed that angoroside C can be absorbed extremely quickly (Tmax = 15 min), can be eliminated very rapidly (t1/2 = 1.26 h), and its oral bioavailability is only about 2.1%. Furthermore, angoroside C was extensively distributed in all main organs (liver, heart, spleen, lung, kidney, and brain), and the highest concentration was detected in the lung 15 min after oral administration. This paper also indicated that angoroside C could be converted to the active metabolite ferulic acid in vivo. The maximum concentrations of ferulic acid in the kidney occurred at 6 h after oral administration. In summary, this study explored some of the pharmacokinetic characteristics of angoroside C in vivo, and the data produced could provide a basis for the further investigation of angoroside C.
Highlights
Radix Scrophulariae is the name for the dried roots of Scrophularia ningpoensis Hemsl. (National Pharmacopoeia Committee, 2015), and is a famous botanical medicine used widely in Asian populations
We found that angoroside C can be metabolized to ferulic acid in rats, which is one of the functional phenolic acids that commonly exist in a variety of plants, and multiple biological and pharmacological properties such as anti-oxidant (Perezternero et al, 2017), anti-inflammatory (Salazar-López et al, 2017), anti-obesity (Salazar-López et al, 2017), and anti-depression (Liu et al, 2017b) have been reported for this compound
The purpose of this paper is to develop a sensitive and reproducible ultra performance liquid chromatography (UPLC)– MS/MS methods to simultaneous quantify angoroside C and its metabolite ferulic acid and apply the method to rat pharmacokinetics, bioavailability, and tissue distribution studies
Summary
Radix Scrophulariae is the name for the dried roots of Scrophularia ningpoensis Hemsl. (National Pharmacopoeia Committee, 2015), and is a famous botanical medicine used widely in Asian populations. Modern pharmacological researches have shown that Radix Scrophulariae possesses antiinflammatory effects, and is able to protect the cardiovascular system, and enhance immunity, among other properties (Qian et al, 1991). Angoroside C (Figure 1) is a representative phenylpropanoid glycoside (PhG) compound isolated from Scrophularia ningpoensis Hemsl (Li et al, 2000; Wagner et al, 2011). According to the continuous series of in-depth studies by Gu Weiliang on Radix Scrophulariae (Gu et al, 2010; Huang et al, 2012), the results showed that angoroside C has beneficial effects against ventricular remodeling, and the mechanism is likely to be related to decreasing the level of Ang II, attenuating the mRNA expressions of endothelin 1 (ET-1) and transforming growth factor β1 (TGF-β1) (Gu et al, 2015), which is effective in postponing heart failure for patients with cardiovascular illness
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