Next Article in Journal
First-Principles Elucidation of the Surface Chemistry of the C2Hx (x = 0–6) Adsorbate Series on Fe(100)
Previous Article in Journal
Cholinesterase Enzymes Inhibitors from the Leaves of Rauvolfia Reflexa and Their Molecular Docking Study
Molecules 2013, 18(4), 3789-3805; doi:10.3390/molecules18043789
Article

Synthesis and Anti-Influenza Virus Activities of a Novel Class of Gastrodin Derivatives

, , , , , , , , * ,  and *
Received: 16 February 2013; in revised form: 19 March 2013 / Accepted: 20 March 2013 / Published: 26 March 2013
(This article belongs to the Section Medicinal Chemistry)
Download PDF [413 KB, uploaded 18 June 2014]
Abstract: A series of substituted aryl glycoside analogues of gastrodin have been identified as potential anti-influenza agents. The most potent inhibitor 1a exhibited moderate inhibitory activity against the A/Hanfang/359/95(H3N2) and A/FM/1/47(H1N1) strains of the influenza A virus (IC50 values of 44.40 and 34.45 μM, respectively) and the oseltamivir-null B/Jifang/13/97 strain of influenza B (IC50 value of 33.01 μM). In this article, multiple doses of compound 1a (80 mg/kg/day, oral administration) were used for the treatment of mice infected with influenza A/FM/1/47-MA (H1N1), and surprisingly we found that compound 1a significantly increased the number of survivors and prolonged the mean survival time. The preliminary studies on the mechanism of antiviral activity showed no interaction between compound 1a and the neuraminidase or the M2 protein. The novel target to overcome drug resistance combined with its good in vivo profile support compound 1a to be a new lead for further development of antiviral agents.
Keywords: gastrodin; aryl glycoside; synthesis; influenza virus inhibitors gastrodin; aryl glycoside; synthesis; influenza virus inhibitors
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.

Export to BibTeX |
EndNote


MDPI and ACS Style

Xue, S.-T.; He, W.-Y.; Ma, L.-L.; Wang, H.-Q.; Wang, B.; Zheng, G.-H.; Ji, X.-Y.; Zhang, T.; Li, Y.-H.; Jiang, J.-D.; Li, Z.-R. Synthesis and Anti-Influenza Virus Activities of a Novel Class of Gastrodin Derivatives. Molecules 2013, 18, 3789-3805.

AMA Style

Xue S-T, He W-Y, Ma L-L, Wang H-Q, Wang B, Zheng G-H, Ji X-Y, Zhang T, Li Y-H, Jiang J-D, Li Z-R. Synthesis and Anti-Influenza Virus Activities of a Novel Class of Gastrodin Derivatives. Molecules. 2013; 18(4):3789-3805.

Chicago/Turabian Style

Xue, Si-Tu; He, Wei-Ying; Ma, Lin-Lin; Wang, Hui-Qiang; Wang, Bo; Zheng, Guang-Hui; Ji, Xing-Yue; Zhang, Tian; Li, Yu-Huan; Jiang, Jian-Dong; Li, Zhuo-Rong. 2013. "Synthesis and Anti-Influenza Virus Activities of a Novel Class of Gastrodin Derivatives." Molecules 18, no. 4: 3789-3805.


Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert