Aim: This study examined nanoparticle entry into tumor-associated vascular endothelial cells during transport to hepatocellular carcinoma cells and tumors. Materials & methods: siVEGF was loaded into CS-SS-9R/BSA-cRGD nanoparticles (CBc NPs). The intracellular uptake, gene silencing efficiency, antiproliferation and antiangiogenic effect of the NPs were performed on EA.hy926 cells. In vivo antitumor and antiangiogenic effects were investigated in Bel-7402 tumor-bearing nude mice. Results: siVEGF-loaded CBc NPs entered EA.hy926 cells and suppressed their proliferation and capillary formation. The NPs also inhibited tumor proliferation and angiogenesis in tumor-bearing mice, which attributed to the downregulation of VEGF mRNA expression in tumor tissue. Conclusion: The uptake of siVEGF-loaded CBc NPs by tumor-associated vascular endothelial cells made important contributions in controlling the progression of hepatocellular carcinoma.
Biotransformation of betulonic acid
(1) by Rhizopus arrhizus CGMCC 3.868
resulted in the production
of 16 new (3, 5, 6, and 9–21) and five known compounds. Structures
of the new compounds were established by analysis of spectroscopic
data. Hydroxylation, acetylation, oxygenation, glycosylation, and
addition reactions involved the C-20–C-29 double bond. Antineuroinflammatory
activities of the obtained compounds in NO production were tested
in lipopolysaccharides-induced BV-2 cells. Compared with the substrate
betulonic acid, biotransformation products 3, 8, 9, 14, and 21 exhibited
an improved inhibitory effect, with IC50 values of 10.26,
11.09, 5.38, 1.55, and 4.69 μM, lower than that of the positive
control, N
G-monomethyl-l-arginine.
In this study, the biotransformation of asiatic acid by Cunninghamella echinulata CGMCC 3.970 and Circinella muscae CGMCC 3.2695 was investigated. Scaled-up biotransformation reactions yielded eight metabolites. Their structures were established based on extensive NMR and HR-ESI-MS data analyses and four of them are new compounds. C. echinulata could catalyze the regioselecitve hydroxylation, carbonylation, and lactonization to yield five metabolites. C. muscae could selectively catalyze hydroxylation, acetylation and glycosylation to yield four products.Furthermore, all the identified metabolites were evaluated for their anti-neuroinflammatory activities in LPS-induced BV-2 cells. Most metabolites displayed pronounced inhibitory effect on nitric oxide (NO) production. The results suggested that biotransformed derivatives of asiatic acid might be served as potential neuroinflammatory inhibitors.
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