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Guided by anti-liver cancer activity and guided byLC-MSanalysis, the research team conducted a preliminary study on the anti-liver cancer active ingredients of Artemisia sphaerocephala ,isolated and identified 143 compounds from it, and found 41 sesquiterpene dimers ( Ata Pharmaceutica Sinica B), 2021 , 11, 1648–1666 ;Organic Chemistry Frontiers 2021 , 8, 1249–1256 ; Chinese Journal of Chemistry ; 2021 , doi:10.
1002/cjoc.
202100528 ) .
The discovered sesquiterpene dimers are mainly polymerized by intermolecular Diels-Alder reaction, including 8 types of polymerization , and their anti-liver cancer activity is more significant than that of monomer compounds .
Recently, the research team established a key method for the efficient synthesis of sesquiterpene dimers based on the analysis of the biogenic synthesis pathways of dimers, using arglabin , which has a higher content in Artemisia plants , as a substrate : ( 1)Through trivalent titanium The promoted epoxy isomerization reaction constructs the diene in one step; ( 2) The dimer is obtained with high stereoselectivity through the biomimetic Diels-Alder reaction .
Through 4-6 steps of reaction, the semi-synthesis of natural products of lavandiolides H, I, K and artematrolide F was completed with a yield of up to 60% , and the synthesis can reach a scale of 10g , laying a material foundation for subsequent in-depth biological activity research .
Based on the Diels-Alder reaction between the sub-divisions , the established synthetic methodology was successfully applied to " natural product-like" Sesquiterpene dimers, trimers efficient synthesis, the tetramer were found to have a significant cytotoxic activity against cancer, the study is based on two subsequent synthesis of highly active anti-tumor activity sesquiterpenoids compound The aggregates are provided for reference
Dr.
Tianze Li / Associate Researcher is the first author, and Researcher Chen Jijun is the corresponding author
The Chen Jijun research team at the Kunming Institute of Botany, Chinese Academy of Sciences is committed to finding anti-hepatocarcinoma lead compounds and innovative drugs from Artemisia plants with unique structures and novel mechanisms of action
.
Guided by anti-liver cancer activity and guided byLC-MSanalysis, the research team conducted a preliminary study on the anti-liver cancer active ingredients of Artemisia sphaerocephala ,isolated and identified 143 compounds from it, and found 41 sesquiterpene dimers ( Ata Pharmaceutica Sinica B), 2021 , 11, 1648–1666 ;Organic Chemistry Frontiers 2021 , 8, 1249–1256 ; Chinese Journal of Chemistry ; 2021 , doi:10.
1002/cjoc.
202100528 ) .
The discovered sesquiterpene dimers are mainly polymerized by intermolecular Diels-Alder reaction, including 8 types of polymerization , and their anti-liver cancer activity is more significant than that of monomer compounds .
The biomimetic synthesis of dimers based on high content of sesquiterpenes can not only verify the biogenic pathway of the compound, and quickly obtain the target compound, but also provide a synthetic route for the synthesis of analogs and lay the foundation for the structure-activity relationship study
.
Recently, the research team established a key method for the efficient synthesis of sesquiterpene dimers based on the analysis of the biogenic synthesis pathways of dimers, using arglabin , which has a higher content in Artemisia plants , as a substrate : ( 1)Through trivalent titanium The promoted epoxy isomerization reaction constructs the diene in one step; ( 2) The dimer is obtained with high stereoselectivity through the biomimetic Diels-Alder reaction .
Through 4-6 steps of reaction, the semi-synthesis of natural products of lavandiolides H, I, K and artematrolide F was completed with a yield of up to 60% , and the synthesis can reach a scale of 10g , laying a material foundation for subsequent in-depth biological activity research .
Based on the Diels-Alder reaction between the sub-divisions , the established synthetic methodology was successfully applied to " natural product-like" Sesquiterpene dimers, trimers efficient synthesis, the tetramer were found to have a significant cytotoxic activity against cancer, the study is based on two subsequent synthesis of highly active anti-tumor activity sesquiterpenoids compound The aggregates are provided for reference
Related research recently to "Biomimetic Synthesis of Lavandiolides H, the I, F and K and Artematrolide Via Diels ? Alder Reaction" in the title in Organic Letters published (magazines 2021 , 23 , 8380-8384 )
.
Dr.
Tianze Li / Associate Researcher is the first author, and Researcher Chen Jijun is the corresponding author
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