Background: HIV-1 Reverse Transcriptase inhibitors (RTI) are a primary resource for AIDS treatment, but the rapid selection of drug resistance strains requires the identification of novel powerful antiviral agents. Modern studies have correlated different categories of phenolic compounds, bioactive constituents Rhubarb, with anti-inflammatory, antioxidant and anticancer activities. Rhubarb, originated from Rheum tanguticm, R. palmatum and R. officinalis, is one of the earliest and also most commonly used medicinal plant in practice of Traditional Chinese Medicine (TCM), belonging to Rheum L. that counts more than 60 species distributed worldwide, with 39 species in the Western and Northern part of China. Methods: 22 different Rheum Chinese species were tested against HIV-1 RT. After determination of content of chemical components in Rheum samples, the effect of the sole components were evaluated on the HIV-1 RT-associated activities (DNA polymerase and ribonuclease H), the most active were tested for inhibition of HIV-1 replication in cell-based assays. Results: Among the Rheum constituents, we determined that anthraquinones are present in all the Rhubarb samples, while rhein and sennoside (sennoside A and sennoside B) are only present in the official Rhubarbs. Sennoside A inhibited both RT-associated functions in the low micromolar range and targeting the early phases of viral replication. Conclusion: Starting from the traditional Traditional Chinese Medicine knowledge, we successfully identified in the Rhubarb component, sennoside A, a new promising HIV-1 inhibitor.
Sennoside A, from the Traditional Chinese Medicine plant Rheum L., is a new reverse transcriptase inhibitor effective against HIV-1 replication
CORONA, ANGELA;GRANDI, NICOLE;PIANO, DARIO;ESPOSITO, FRANCESCA;
2014-01-01
Abstract
Background: HIV-1 Reverse Transcriptase inhibitors (RTI) are a primary resource for AIDS treatment, but the rapid selection of drug resistance strains requires the identification of novel powerful antiviral agents. Modern studies have correlated different categories of phenolic compounds, bioactive constituents Rhubarb, with anti-inflammatory, antioxidant and anticancer activities. Rhubarb, originated from Rheum tanguticm, R. palmatum and R. officinalis, is one of the earliest and also most commonly used medicinal plant in practice of Traditional Chinese Medicine (TCM), belonging to Rheum L. that counts more than 60 species distributed worldwide, with 39 species in the Western and Northern part of China. Methods: 22 different Rheum Chinese species were tested against HIV-1 RT. After determination of content of chemical components in Rheum samples, the effect of the sole components were evaluated on the HIV-1 RT-associated activities (DNA polymerase and ribonuclease H), the most active were tested for inhibition of HIV-1 replication in cell-based assays. Results: Among the Rheum constituents, we determined that anthraquinones are present in all the Rhubarb samples, while rhein and sennoside (sennoside A and sennoside B) are only present in the official Rhubarbs. Sennoside A inhibited both RT-associated functions in the low micromolar range and targeting the early phases of viral replication. Conclusion: Starting from the traditional Traditional Chinese Medicine knowledge, we successfully identified in the Rhubarb component, sennoside A, a new promising HIV-1 inhibitor.
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