Figure 1
Chemical structure and inhibition data of cardiac glycoside/aglycones on HIV-1 gene expression. Chemical structure and dose-response data of CSs on HIV-1 (Gag) gene expression (IC50s) are summarized from Supplementary Figure S2 from HeLa rtTA-HIV-ΔMls cells (except data was not shown from inactive compounds: RIDK-20, -21, -27, and -28) and Fig. 2 from HIV-infected PBMCs of patients. The steroid core and the position of various chemical substituents of CSs (red) are depicted (top). The different modifications of each CS (A–J) are listed below by chemical substituent. The presence and absence of a glycoside (a) distinguish between cardiac glycoside and aglycones, respectively. Differences in the lactone moiety from butyrolactone and α-pyrone (g) demarcate cardenolide and bufadienolide classes of CSs, respectively. The presence and absence of a hydroxyl group (−OH) at position 12 (b) describes “digoxin-like” and “digitoxin-like” CSs, respectively. Modifications of the steroid in (d–f) except for ouabain are specific to convallatoxin derivatives while changes in (h–j) are specific only to cinobufagin.
