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Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1
Cheng-Jian Tan1,2, Shi-Fei Li1,3, Ning Huang4,5
1State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650204, Yunnan, People's Republic of China.
Natural products yielded six daphnane diterpenoids from Trigonostemon lii with potent anti-HIV activity. These compounds inhibit HIV-1 replication and cell fusion, offering potential as entry inhibitors, especially against drug-resistant strains.
Area of Science:
- Natural Product Chemistry
- Virology
- Medicinal Chemistry
Background:
- Natural products are a vital source for discovering novel anti-HIV therapeutics.
- Trigonostemon lii is a plant species with potential medicinal properties.
Purpose of the Study:
- To isolate and characterize daphnane diterpenoids from Trigonostemon lii.
- To evaluate the anti-HIV activity of these isolated compounds, focusing on replication and entry inhibition.
Main Methods:
- Isolation and structural elucidation of six daphnane diterpenoids from Trigonostemon lii.
- In vitro assays to assess inhibition of HIV-1 replication.
- Cell-cell fusion assays to evaluate HIV entry inhibition.
- Testing against wild-type and T20-resistant HIV-1 strains.
Main Results:
- Three new daphnane diterpenoid structures were identified.
- The isolated compounds exhibited potent anti-HIV-1 activity in the nanomolar/picomolar range.
- Significant inhibition of HIV-1/H9 cell fusion was observed, with EC50 values between 1.06-8.73 ng/mL.
- Compounds showed activity against T20-resistant HIV-1 strains but no inhibition of HIV-1 reverse transcriptase.
Conclusions:
- The six daphnane diterpenoids are potential lead candidates for developing new HIV entry inhibitors.
- These compounds are particularly promising for treating infections caused by T20-resistant HIV-1 variants.
