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Nanoparticles containing mixed lipid monolayer shell, biodegradable polymer core and rabies virus glycoprotein (RVG) peptide as brain targeting ligand, were developed for brain targeted delivery of paclitaxel (PTX) to treat malignant glioma. RVG conjugated PTX loaded NPs (RVG-PTX-NPs) had the desirable size (~140 nm), narrow size distribution and spherical shape. RVG-PTX-NPs showed poor uptake by neurons and selective targeting to the brain tumor associated macrophages (TAMs) with controlled release and tumor specific toxicity. In vivo studies revealed that RVG-PTX-NPs were significant to cross the blood-brain barrier (BBB) and had specific targeting to the brain. Most importantly, RVG-PTX-NPs showed effectiveness for anti-glioma therapy on human glioma of mice model. We concluded that RVG-PTX-NPs provided an effective approach for brain-TAMs targeted delivery for the treatment of glioma.

We investigated the phytochemicals from an ethanol extract of Acacia pennata (L.) Willd stems, a Vietnam medicinal plant, which led to the isolation of a new saponin termed 21β- O-[(2 E)-6-hydroxyl-2,6-dimethyl-2,7-octadienoyl] pitheduloside G (1), as well as pitheduloside G (2), a known saponin. The structures of compounds 1 and 2 were elucidated via spectroscopy and compared with those reported in the literature. The isolates (1 and 2) were tested for their inhibitory effects on human immunodeficiency virus type 1 (HIV-1) protease (PR). We found that the new compound, 21β- O-[(2 E)-6-hydroxyl-2,6-dimethyl-2,7-octadienoyl] pitheduloside G (1), possessed potent anti-HIV-1 PR activity, with a half-maximum inhibitory concentration (IC50) value of 2.0 ± 0.2 μM. In contrast, pitheduloside G (2) exhibited much less inhibition, with an IC50 value of 18 ± 0.5 μM. Both compounds were nontoxic in human embryonic kidney 293T cells at concentrations effective against HIV-1 PR. This is the first report regarding the isolation of an anti-HIV-1 PR compound (1) from an Acacia plant species.