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Molecules 2017, 22(12), 2119; doi:10.3390/molecules22122119

Anti-Proliferative Activity of Triterpenoids and Sterols Isolated from Alstonia scholaris against Non-Small-Cell Lung Carcinoma Cells

1
Research Center for Biodiversity, China Medical University, Taichung 40402, Taiwan
2
Department of Laboratory, Chang Bing Show Chwan Memorial Hospital, Changhua 500, Taiwan
3
Department of Biological Science and Technology, China Medical University, Taichung 40402, Taiwan
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 31 October 2017 / Revised: 28 November 2017 / Accepted: 30 November 2017 / Published: 1 December 2017
(This article belongs to the Special Issue Diversity of Terpenoids)
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Abstract

(1) Background: In China and South Asia, Alstonia scholaris (Apocynaceae) is an important medicinal plant that has been historically used in traditional ethnopharmacy to treat infectious diseases. Although various pharmacological activities have been reported, the anti-lung cancer components of A. scholaris have not yet been identified. The objective of this study is to evaluate the active components of the leaf extract of A. scholaris, and assess the anti-proliferation effects of isolated compounds against non-small-cell lung carcinoma cells; (2) Methods: NMR was used to identify the chemical constitutes isolated from the leaf extract of A. scholaris. The anti-proliferative activity of compounds against non-small-cell lung carcinoma cells was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay; (3) Results: Eight triterpenoids and five sterols were isolated from the hexane portion of A. scholaris, and structurally identified as: (1) ursolic acid, (2) oleanolic acid, (3) betulinic acid, (4) betulin, (5) 2β,3β,28-lup-20(29)-ene-triol, (6) lupeol, (7) β-amyrin, (8) α-amyrin, (9) poriferasterol, (10) epicampesterol, (11) β-sitosterol, (12) 6β-hydroxy-4-stigmasten-3-one, and (13) ergosta-7,22-diene-3β,5α,6β-triol. Compound 5 was isolated from a plant source for the first time. In addition, compounds 9, 10, 12, and 13 were also isolated from A. scholaris for the first time. Ursolic acid, betulinic acid, betulin, and 2β,3β,28-lup-20(29)-ene-triol showed anti-proliferative activity against NSCLC, with IC50 of 39.8, 40.1, 240.5 and 172.6 μM, respectively.; (4) Conclusion: These findings reflect that pentacyclic triterpenoids are the anti-lung cancer chemicals in A. scholaris. The ability of ursolic acid, betulinic acid, betulin, and 2β,3β,28-lup-20(29)-ene-triol to inhibit the proliferative activity of NSCLC can constitute a valuable group of therapeutic agents in the future. View Full-Text
Keywords: Alstonia scholaris; triterpenoid; sterol; non-small-cell lung carcinoma cells (NSCLC); ursolic acid; betulinic acid; betulin; 2β,3β,28-lup-20(29)-ene-triol Alstonia scholaris; triterpenoid; sterol; non-small-cell lung carcinoma cells (NSCLC); ursolic acid; betulinic acid; betulin; 2β,3β,28-lup-20(29)-ene-triol
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MDPI and ACS Style

Wang, C.-M.; Tsai, S.-J.; Jhan, Y.-L.; Yeh, K.-L.; Chou, C.-H. Anti-Proliferative Activity of Triterpenoids and Sterols Isolated from Alstonia scholaris against Non-Small-Cell Lung Carcinoma Cells. Molecules 2017, 22, 2119.

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