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| Synthesis of acylated triterpenes of Inonotus obliquus and their antitumor activities |
| Hits 1325 Download times 990 Received:May 30, 2018 |
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| DOI
10.11656/j.issn.1672-1519.2018.11.18 |
| Key Words
Inonotus obliquus;triterpene;acylation;antitumor |
| Author Name | Affiliation | E-mail | | DENG Liying | People's Hospital of Huixian City, Huixian 453600, China | | | YANG Canyu | People's Hospital of Huixian City, Huixian 453600, China | | | YAN Yahui | College of Pharmacy, Henan University, Kaifeng 475004, China | | | LI Jiawei | College of Pharmacy, Henan University, Kaifeng 475004, China | | | CEN Ruyue | College of Pharmacy, Henan University, Kaifeng 475004, China | | | ZHAO Hui | College of Pharmacy, Henan University, Kaifeng 475004, China | tzz1113@163.com |
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| Abstract
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| [Objective] To synthesize acylated triterpenes of Inonotus obliquus and study the effect of acylation on antitumor activity.[Methods] The triterpenes were separated from the 95% ethanol extracts of I. obliquus by silica gel, ODS column chromatograph and preparative HPLC. The compounds were then acylated with succinic anhydride. The antitumor activities of the triterpenes and their acetylation products against A549, Hela, MCF-7 and 4T1 cancer cells were tested by MTT method.[Results] Inotodiol (1), trametenolic acid (2) and inonotusane A (3) were isolated and identified from I. obliquus. They were acylated to inotodiol-3-mono succinate (1a), inotodiol-22-mono succinate (1b), inotodiol-3,22-di succinate (1c), trametenolic acid-3-mono succinate (2a) and inonotusane A-3-mono succinate (3a) respectively. MTT tests showed that the antitumor activities of 1a, 1b and 1c against A549 and 4T1 were stronger than 1. Furthermore, the antitumor activity of 1a against MCF-7 was stronger than 1. The antitumor activities of 3 against A549, MCF-7 and 4T1 were all enhanced after acylation. Activity of 3a against A549 was the strongest (with IC50=9.53 μM). While neither 2 or 2a was inactive.[Conclusion] Acylation on 3-position or 22-position in 1 and 22-position in 3 enhance the anti-tumor activity. This provides valuable reference for their further structure modification. |
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