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Molecules 2018, 23(9), 2147; https://doi.org/10.3390/molecules23092147

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

1
TCM and Ethnomedicine Innovation & Development International Laboratory, Innovative Drug Research Institute, School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China
2
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan
3
Hunan Province Key Laboratory of Plant Functional Genomics and Developmental Regulation, College of Biology, Hunan University, Changsha 410082, China
4
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)
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Abstract

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
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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.

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