Pharmacokinetics of Arctigenin and Fructus Arctii Powder in Piglets

Abstract

Fructus arctii, also known as great power seed, is the dried fruit of Arctium lappa of the family Compositae. It is a commonly used veterinary herbal medicine, and arctigenin is the main active ingredient. The aim of this study was to characterize the absorption, distribution, metabolism, and excretion of arctigenin and Fructus arctii powder in piglets. These data were used to provide a theoretical reference for the development and clinical use of new veterinary drugs. Sixteen healthy piglets (mean weight 30.0 ± 5.0 kg) were divided into two groups. One group was administered 2.0 mg/kg body weight (bw) arctigenin intravenously, and the other was administered 1.0 g/kg . bw Fructus arctii powder by gavage. Blood samples were collected from the anterior vena cava at different time points, and the concentration of arctigenin in the plasma of the piglets was determined using high-performance liquid chromatography (HPLC). Arctigenin conformed to a two-compartment model with no absorption, and the main pharmacokinetic parameters were as follows: distribution half-life ( t 1/2α )−0.166 ± 0.022 h; elimination half-life ( t 1/2β )−3.161 ± 0.296 h; apparent volume of distribution ( V d )−0.231 ± 0.033 L/kg; clearance rate (CL b )−0.057 ± 0.003 L/(h.kg); and area under the curve (AUC)−1.189 ± 0.057 g . h/mL. The pharmacokinetic parameters of arctigenin following oral administration of the Fructus arctii powder were as follows: absorption half-life ( t 1/2ka )−0.274 ± 0.102 h, t 1/2α −1.435 ± 0.725 h, t 1/2β −63.467 ± 29.115 h, V d −1.680 ± 0.402 L/kg, CL b −0.076 ± 0.028 L/(h kg), peak time ( t max )−0.853 ± 0.211 h, peak concentration ( C max )−0.430 ± 0.035 g/mL, and AUC−14.672 ± 4.813 g/mL. These results indicated that intravenous arctigenin was sparingly distributed in tissues. In contrast, orally administered Fructus arctii powder was rapidly absorbed, more widely distributed, and more slowly eliminated than the intravenous arctigenin, which may indicate its sustained pharmacological effects.

Lignans as multi‐targeted natural products in neurodegenerative diseases and depression: Recent perspectives

“…This suggested that the metabolic stability of ATG showed differences in the liver microsomes of different species. Respectively, another study using 2 mg/kg of ATG administered intravenously to piglets compared with gavage at a dose of 1000 mg/kg revealed that intravenous ATG had limited distribution in tissues, while oral ATG was more rapidly absorbed, more widely distributed, and more slowly eliminated to achieve longer‐lasting pharmacological effects (He et al, 2019). The results of in vitro microsomal culture experiments in rats by Gao et al (2014).…”

Optimisation of the Conversion and Extraction of Arctigenin From Fructus arctii Into Arctiin Using Fungi

“…The injection volume was 10 µL. The column temperature was maintained at 30 • C, and the detection wavelength was 280 nm (Ju, 2008;He et al, 2019).…”

“…The main active components are lignans, including arctiin and arctigenin. Arctiin has low bioavailability but can be converted into arctigenin by gastrointestinal microorganisms (Hu et al, 2004;Yu, 2007;He et al, 2019). Modern science has demonstrated that arctigenin is beneficial for the treatment of viruses (Swarup et al, 2008;Hayashi et al, 2010), tumours (Matsumoto et al, 2006;Kim et al, 2010), inflammation (Zhao et al, 2009), allergy (Lee and Kim, 2010), shock (Ishihara et al, 2006), bacteria (Liu, 2008), and parasites (Wang et al, 2009).…”

Chinese Traditional Medicine NiuBeiXiaoHe (NBXH) Extracts Have the Function of Antituberculosis and Immune Recovery in BALB/c Mice

“…Bulbus Fritillariae Cirrhosae and Rhizoma Bletillae are the main components of NBXH, which have the functions of heat clearing, lung moistening, phlegm resolving, cough relieving, hemostasis, and detumescence [ 8 – 10 ]. Herba Houttuyniae , Radix Platycodonis , and Fructus Arctii are the auxiliary elements of NBXH, which have the beneficial effects of acting as an anti-inflammatory, reducing phlegm, and relieving cough as well as sore throat [ 11 – 13 ]. Glutinous rice is used as the adjuvant to invigorate the spleen, stomach, and lung [ 14 ].…”