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Sci Rep. 2018 Feb 19;8(1):3307. doi: 10.1038/s41598-018-21722-1.

Experimental study of the anti-tumour activity and pharmacokinetics of arctigenin and its valine ester derivative.

Author information

1
College of Chinese Medicinal Material, Jilin Agricultural University, Xincheng Street No. 2888, Changchun Shi, Jilin province, 130118, China.
2
College of Chinese Medicinal Material, Jilin Agricultural University, Xincheng Street No. 2888, Changchun Shi, Jilin province, 130118, China. hanmei126621@126.com.
3
College of Chinese Medicinal Material, Jilin Agricultural University, Xincheng Street No. 2888, Changchun Shi, Jilin province, 130118, China. sqcg126621@126.com.

Abstract

Arctigenin (ARG) is a functional active component that has important physiological and pharmacological activities. The anti-tumour and anti-inflammatory activities of ARG show good potential for application and development, but this material has the defect of low water solubility. In this experiment, the valine derivative of ARG (ARG-V) was designed and synthesized to overcome this disadvantage. The ARG amino acid, EDCI and DMAP were raw materials in the addition reaction, with a molar ratio of 1:2:2:0.5. The yield of ARG-V was up to 80%. ARG-V has strong anti-tumour activity in vivo and in vitro. The inhibitory rate of ARG-V was 69.2%, with less damage to the immune organs and different degrees of increased serum cytotoxicity. Moreover, the pharmacokinetics of ARG following oral administration and ARG-V following oral administration in rats were also studied. The Cmax and AUC values of ARG-V showed significant differences compared to ARG. The relative bioavailabilities of three doses of ARG-V compared to ARG were 664.7%, 741.5% and 812.9%. These pharmacokinetic results may be useful for further studies of the bioactive mechanism of ARG and provide a theoretical basic for clinical use.

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