Next Article in Journal
Inhibitory Effects of Bioassay-Guided Isolation of Anti-Glycation Components from Taraxacum coreanum and Simultaneous Quantification
Previous Article in Journal
Synthesis and Biological Evaluation of Novel Alkyl Amine Substituted Icariside II Derivatives as Potential Anticancer Agents
Previous Article in Special Issue
Molecular Dynamics on Wood-Derived Lignans Analyzed by Intermolecular Network Theory
Article Menu
Issue 9 (September) cover image

Export Article

Open AccessArticle
Molecules 2018, 23(9), 2147;

Lignans from Tujia Ethnomedicine Heilaohu: Chemical Characterization and Evaluation of Their Cytotoxicity and Antioxidant Activities

TCM and Ethnomedicine Innovation & Development International Laboratory, Innovative Drug Research Institute, School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan
Hunan Province Key Laboratory of Plant Functional Genomics and Developmental Regulation, College of Biology, Hunan University, Changsha 410082, China
Shaanxi Key Laboratory of Basic and New herbal Medicament Research, Shaanxi Collaborative Innovation Center of Chinese Medicinal Resource Industrialization, Shaanxi University of Chinese Medicine, Xianyang 712046, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 30 July 2018 / Revised: 24 August 2018 / Accepted: 24 August 2018 / Published: 27 August 2018
(This article belongs to the Special Issue Lignans)
Full-Text   |   PDF [642 KB, uploaded 29 August 2018]   |  


Heilaohu, the roots of Kadsura coccinea, has a long history of use in Tujia ethnomedicine for the treatment of rheumatoid arthritis and gastroenteric disorders, and a lot of work has been done in order to know the material basis of its pharmacological activities. The chemical investigation led to the isolation and characterization of three new (13) and twenty known (423) lignans. Three new heilaohulignans A-C (13) and seventeen known (420) lignans possessed dibenzocyclooctadiene skeletons. Similarly, one was a diarylbutane (21) and two were spirobenzofuranoid dibenzocyclooctadiene (2223) lignans. Among the known compounds, 45, 7, 1315 and 1722 were isolated from this species for the first time. The structures were established, using IR, UV, MS and NMR data. The absolute configurations of the new compounds were determined by circular dichroism (CD) spectra. The isolated lignans were further evaluated for their cytotoxicity and antioxidant activities. Compound 3 demonstrated strong cytotoxic activity with an IC50 value of 9.92 µM, compounds 9 and 13 revealed weak cytotoxicity with IC50 values of 21.72 µM and 18.72 µM, respectively in the HepG-2 human liver cancer cell line. Compound 3 also showed weak cytotoxicity against the BGC-823 human gastric cancer cell line and the HCT-116 human colon cancer cell line with IC50 values of 16.75 µM and 16.59 µM, respectively. A chemiluminescence assay for antioxidant status of isolated compounds implied compounds 11 and 20, which showed weak activity with IC50 values of 25.56 µM and 21.20 µM, respectively. View Full-Text
Keywords: lignans; heilaohu; tujia ethnomedicine; chemical characterization; cytotoxicity; antioxidant lignans; heilaohu; tujia ethnomedicine; chemical characterization; cytotoxicity; antioxidant

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Supplementary material


Share & Cite This Article

MDPI and ACS Style

Liu, Y.; Yang, Y.; Tasneem, S.; Hussain, N.; Daniyal, M.; Yuan, H.; Xie, Q.; Liu, B.; Sun, J.; Jian, Y.; Li, B.; Chen, S.; Wang, W. Lignans from Tujia Ethnomedicine Heilaohu: Chemical Characterization and Evaluation of Their Cytotoxicity and Antioxidant Activities. Molecules 2018, 23, 2147.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top