Despite remarkable advances in combination antiretroviral therapy (cART), human immunodeficiency virus type 1 (HIV-1) infection remains incurable due to the incomplete elimination of the replication-competent virus, which persists in latent reservoirs. Strategies for targeting HIV reservoirs for eradication that involves reactivation of latent proviruses while protecting uninfected cells by cART are urgently needed for cure of HIV infection. We screened medicinal plant extracts for compounds that could reactivate the latent HIV-1 provirus and identified a procyanidin trimer C1 derived from Theobroma cacao as a potent activator of the provirus in human T cells latently infected with HIV-1. This reactivation largely depends on the NF-κB and MAPK signaling pathways because either overexpression of a super-repressor form of IκBα or pretreatment with a MEK inhibitor U0126 diminished provirus reactivation by C1. A pan-PKC inhibitor significantly blocked the phorbol ester-induced but not the C1-induced HIV-1 reactivation. Although C1-induced viral gene expression persisted for as long as 48 h post-stimulation, NF-κB-dependent transcription peaked at 12 h post-stimulation and then quickly declined, suggesting Tat-mediated self-sustainment of HIV-1 expression. These results suggest that procyanidin C1 trimer is a potential compound for reactivation of latent HIV-1 reservoirs.
The plant Polygala arillata has been used in the Oriental medicine as a tonic and for the treatment of certain diseases. Our current research on phytochemical profile of the roots of P. arillata led to the isolation of a new oligosaccharide ester (1), a new glucose ester (7), along with five known sucrose esters (2-6). Their structures were elucidated on the basis of extensive chemical and spectroscopic methods (NMR and MS spectra) as well as comparison with the literature data. To the best of our knowledge, the occurence of various oligosaccharide esters in P. arillata including unique compounds play taxonomical impact and suggest potential in medicinal uses of the title plant.
The main goal of this study was to isolate and screen the therapeutic potential of some terpenoids from Dicliptera chinensis (L.) Nees grown in Vietnam. From the leaves of Dicliptera chinensis (L.) Nees (Acanthaceae) collected in Nam Dinh province, one new terpenoid (1) together with five known (2-6) were isolated by chromatographic methods. These compounds were identified as 6-hydroxy-1,12-oleanadien-3-on (1), 1β,4β-dihydroxyeudesm-11-ene (2), 3β-hydroxylup-20(29)-en (3), stigmast-5,22-dien-3-β-ol (4), rutaevine (5), mangiferin (6). All of them were isolated from this plant for the first time. Compound 4 showed signficant potential for COX-2 inhibitory effects with IC50 values of 7.32± 1.82 µg/mL. These pilot results suggest the potential of Dicliptera terpenoids for treating inflamatory conditions.
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