Among the isolated constituents, Sennoside A and B were effective on both RDDP and RNase H RT-associated functions in biochemical assays.
Conclusion: Sennoside A is a new scaffold for the development of HIV-1 dual RT inhibitors.
The reference compounds AloeEmodin, Rhein, Emodin, Chrysophanol, Physcion were purchased from the National Institute for Control of Pharmaceuticals and Biological Products (Beijing, China), and Sennoside A and Sennoside B from the Mansite Pharmaceutical Co.
1 [micro]M, Sennoside A at 20 [micro]M, Sennoside B at 20 [micro]M and RDS1760 at 25 [micro]M).
Specifically, these components included anthraquinone derivatives such as Emodin, Crysophanol, Aloe-Emodin, Physcion, Rhein and Sennoside (both Sennoside A and Sennoside B).
Evaluation of the effects of Sennoside A and B on mutated RT
Thus, we firstly tested the effect of Sennoside A and B on three known single RT mutants involved in NNRTI resistance such as K103N, Y181C and Y188L RTs, using Efavirenz as positive control (Table 3).
Subsequently, considering the results obtained with Sennoside A on the NNRTI resistant RT mutants, we wanted to better characterize its behavior in the presence of Efavirenz in order to explore the possibility that the two compounds may interact with the same RT binding site.
Taken together, this first set of data indicated that Sennoside A and B inhibit both RT-associated functions.
2014), we asked whether Sennoside A and B might affect also the IN catalytic function.