Abstract

Background Semen Euphorbiae (SE) and Semen Euphorbiae Pulveratum (SEP) have a long history of medicinal use. SEP is the processed product of SE; both ancient and modern studies have shown that SEP has a lower toxicity compared to SE. To clarify the influence of processing on the pharmacological properties of SE and SEP, a study was carried out to compare the pharmacokinetics and distribution characteristics of three active compounds after oral administration of SE and SEP extracts. Methods A UPLC-MS/MS method was established to simultaneously determine the contents of Euphorbia factors L1, L2, and L3 in rat plasma and mouse tissues after an oral administration of crude and processed SE with approximately the same dosage. Plasma and heart, liver, spleen, lung, kidney, and colon tissue samples were treated with ethyl acetate and separated by gradient elution on a C18 column with a mobile phase of 0.1% formic acid and methanol. Results The established method had good selectivity, linear range, accuracy, precision, stability, matrix effect, and extraction recovery. The area under the concentration time curve, time to maximum concentration, maximum concentration, half-life of elimination, and mean retention time of plasma samples in SEP-treated group decreased, and the clearance in SEP-treated group increased. Moreover, the active component concentrations in colon, liver, and kidney tissues were more followed by those in the heart, lungs, and spleen. Conclusion These results indicate that the processing could influence the pharmacokinetics and tissue distribution of Euphorbia factors L1, L2, and L3 after oral administration of crude and processed SE. The data obtained may lay a foundation for the clinical use of SE and for further study on the processing mechanism of SE.

Highlights

  • Semen Euphorbiae (SE) is the dried mature seed of Euphorbia lathyris L., which is a kind of traditional Chinese medicine (TCM) that is widely used in the treatment of hydroncus, ascites, anuria, astriction, menostasis, and scabies [1, 2]

  • Our study reports a rapid and sensitive UPLC-mass spectrometer (MS)/MS method to simultaneously determine the contents of Euphorbia factors L1, L2, and L3 in rat plasma and heart, liver, spleen, lung, kidney, and intestinal tissues of mice. is method has been applied to determine the pharmacokinetics and tissue distribution characteristics of crude SE and its processed products in order to clarify the influence of processing on the pharmacological properties of SE and to lay a foundation for further study of SE

  • Healthy Sprague-Dawley (SD) rats weighing 250 ± 20 g and Kunming mice (KM) weighing 20 ± 2 g were bought from SPF Biotechnology Company Ltd., in Beijing, China (Lot No 2016-0002). e animals have free access to water and food. e animal experiment was carried out strictly according to the Provisions on the Administration of Experimental Animals issued by the Ministry of Science and Technology of the People’s Republic of China. e program was authorized by the Experimental Animal Ethics Committee of Beijing University of Chinese Medicine, and this study was carried out in strict compliance with the ARRIVE guidelines [19]

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Summary

Introduction

Semen Euphorbiae (SE) is the dried mature seed of Euphorbia lathyris L., which is a kind of traditional Chinese medicine (TCM) that is widely used in the treatment of hydroncus, ascites, anuria, astriction, menostasis, and scabies [1, 2]. Semen Euphorbiae Pulveratum (SEP) is the processed product of SE, prepared by removing the oil from the SE; both ancient and modern studies have shown that SEP has a lower toxicity compared to SE [6, 7]. SEP is the processed product of SE; both ancient and modern studies have shown that SEP has a lower toxicity compared to SE. To clarify the influence of processing on the pharmacological properties of SE and SEP, a study was carried out to compare the pharmacokinetics and distribution characteristics of three active compounds after oral administration of SE and SEP extracts. A UPLC-MS/MS method was established to simultaneously determine the contents of Euphorbia factors L1, L2, and L3 in rat plasma and mouse tissues after an oral administration of crude and processed SE with approximately the same dosage. Conclusion. ese results indicate that the processing could influence the pharmacokinetics and tissue distribution of Euphorbia factors L1, L2, and L3 after oral administration of crude and processed SE. e data obtained may lay a foundation for the clinical use of SE and for further study on the processing mechanism of SE

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