China News Service, Kunming, February 21 (Reporter Hu Yuanhang) The Kunming Institute of Botany, Chinese Academy of Sciences announced on the 21st that the research team of Chen Jijun of the Institute discovered a series of novel sesquicides with anti-liver cancer activity from the medicinal plant Artemisia annua. Terpene dimers.
Relevant research results were recently published in the internationally renowned journal Signal Transduction and Targeted Therapy.
Liver cancer is a malignant tumor that seriously threatens human health.
There are more than 840,000 new cases of liver cancer every year in the world, and 780,000 deaths due to liver cancer, and about 50% of the new cases occur in China.
There are currently four tyrosine kinase inhibitors sorafenib, regorafenib, lenvatinib, and cabozantinib, one vascular endothelial growth factor receptor 2 antagonist ramucirumab, and two PD-1 inhibitors nivolumab and pembrolizumab are used in the clinical treatment of liver cancer, but their structural types are relatively single, and drug resistance is easy to develop.
In recent years, Chen Jijun's research team has been committed to searching for anti-hepatoma lead compounds and innovative drugs with unique structures and novel mechanisms of action from Artemisia plants, and successfully established the directional identification and anti-hepatoma activity tracking of sesquiterpene dimers in Artemisia plants combined separation methods.
This study found for the first time that the extract of Artemisia annua had strong inhibitory activity on three liver cancer cell lines, and isolated 36 novel sesquiterpene dimers of 9 structural types from the active part of Artemisia miltiorrhiza for the first time, namely, artemisinin A1-A3, B1-B2, C1-C4, D, E, F1-F15, G1-G8, H and I.
Further studies have shown that among the 36 novel sesquiterpene dimers, genteemin G5 and G7 have the best activity, which is comparable to the clinical first-line anti-liver cancer drug Sorafenib; Cell THLE-2 showed better selectivity than Sorafenib, and its safety was better than Sorafenib; at the same time, nanhaosu G7 can also inhibit liver cancer cell invasion, migration, induce cell apoptosis and block Arrest the G2/M cell cycle to inhibit the proliferation of HepG2 cells.
This study revealed for the first time a series of sesquiterpene dimers with novel skeletons and diverse structures in Artemisia annua. Structurally diverse candidate molecules and important pharmacological basis.
So far, Chen Jijun’s research team has isolated and identified 122 novel sesquiterpene dimers with anti-liver cancer activity from plants such as Artemisia annua, Artemisia annua, Artemisia Zhongdian, Artemisia oxtail, and Artemisia mongolica, accounting for 122 novel sesquiterpene dimers with anti-liver cancer activity, accounting for 12% of the world’s genus Artemisia. 52% of the total number of 234 sesquiterpene dimers reported in plants.
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