Changes in chemical components and antitumor activity during the heating process of Fructus Arctii

Abstract

Context: The dried fruits of Arctium lappa L. have been used in two forms in traditional Chinese medicine; crude and stir-heating Fructus Arctii. However, its processed product possesses better activity.

Objective: In this study, the chemical constituents of both crude and processed Fructus Arctii and their antiproliferative activities were evaluated.

Materials and methods: The seven main active components in crude and various processed Fructus Arctii were quantitatively determined using high-performance liquid chromatography (HPLC). According to the actual amount in crude and five processed samples, seven single components were combined as multi-component combinations with six different proportions. The antiproliferative activities of these compatibility component groups were examined using the CCK-8 assay.

Results: During the heating process, the proportion of the seven main components changed dynamically. The contents of 3-caffeoylquinic acid (3-CQA), 3,5-dicaffeoylquinic acid (3,5-diCQA), and arctiin (ARC) declined, while the contents of 4-caffeoylquinic acid (4-CQA), 3,4-dicaffeoylquinic acid (3,4-diCQA), 4,5-dicaffeoylquinic acid (4,5-diCQA), and arctigenin (ARG) increased very significantly.

Discussion and conclusions: The results also indicated that seven components in the processed samples had higher cytotoxic profiles against HL-60 cells than those in the crude sample. Therefore, the heating process may enhance the antitumor activity of Fructus Arctii by changing the proportion of active components.

Keywords:

• Traditional Chinese medicine
• stir-heating
• multi-component
• compatibility

Disclosure statement

All the authors have read and approved present manuscript, and declared that they have no conflicts of interest.

Additional information

Funding

The authors gratefully acknowledge the financial support of this study by the National Natural Science Foundation of China [No. 81603297], the Opening Project of Zhejiang Provincial First-rate Subject (Chinese Traditional Medicine), Zhejiang Chinese Medical University [No. Ya2017003], and Jiangsu Province 333 High-level Talents Training Program [2016-3-0277].