Chinese Journal of Organic Chemistry >
Total Synthesis and Anti-inflammatory Evaluation of Dorsmerunin A
Received date: 2021-02-22
Revised date: 2021-03-27
Online published: 2021-05-25
Supported by
Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Chinese Medicine(202001AZ070001-007); Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Chinese Medicine(202001AZ070001-038); Undergraduate Innovation and Entrepreneurship Training Program of Yunnan University of Chinese Medicine(2019066)
Benzofurans have been found to be one of the major sources of drug development for a variety of diseases, and have received increasing attention in the field of synthetic medicinal chemistry. Dorsmerunin A, a natural cytotoxic product of 2-benzylbenzofurans, was isolated from the roots of Dorstenia kameruniana. In this work, Dorsmerunin A was firstly synthesized in 49% total yield from 4-methoxysalicylaldehyde and 2-bromo-4'-methoxyacetophenone through intramolecular condensation, reduction and deprotection. The in vitro anti-inflammatory activity of Dorsomerinein A was initially tested using the murine macrophage RAW264.7 model, and the results showed that it showed good inhibitory effect on NO production at a concentration of 25 μmol/L, as well as proinflammatory factors (IL-6, IL-1β and TNF-α).
Key words： Dorsmerunin A; total synthesis; anti-inflammatory activity; mechanism
Minxin Li , Qiuping Zou , Wenrong Du , Jinchun Gao , Yanping Li , Zewei Mao . Total Synthesis and Anti-inflammatory Evaluation of Dorsmerunin A[J]. Chinese Journal of Organic Chemistry, 2021 , 41(8) : 3292 -3296 . DOI: 10.6023/cjoc202102040
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