The edible Blaps rynchopetera Fairmaire is widely used for its various medicinal effects. From its ethyl acetate fraction, three new hydroxytyrosol dimers, rynchopeterine H (1), rynchopeterine I (2) and trans-2-(3,4-dihydroxy-phenyl)-3-hydroxy-7-(2-hydroxyethyl)-1,4-benzdioxane (3), together with four known similar dimers were obtained by chromatography of silica gel and Sephadex LH-20. Their structures were identified by HRESIMS, 1D and 2D NMR spectra analysis. Compounds 1-4 were obtained as a mixture, and cytotoxicity screening for HepG2, Caco-2, U251, AGS, B16 and Bel-7402 cell lines showed that the mixture of compounds 1-4 exhibited significantly selective cytotoxicity and good inhibitory activity on the proliferation of mouse melanoma cells (B16) with an IC50 value of 27.37 μg·mL−1.
CII-3 is the effective part of Periplaneta americana for application in oncotherapy. This study investigated its main chemical components for macrophage polarization regulation activity. Compounds were separated and purified, and their structures were elucidated based on NMR and HR-ESI-MS analyses. After inducing the M1 and M2 phenotype macrophages, CII-3 and testing components were added and co-incubated to evaluate their effects on the relevant markers of macrophages. Then, gradient concentrations of CII-3 and active monomers were further investigated for their effects on M2 macrophages. The effects were detected by RT-PCR, ELISA, flow cytometry, and immunofluorescence. Twelve compounds were identified from CII-3. CII-3 and pericanaside (5) had no obvious effect on M1 macrophages, while they significantly reduced the expression levels of M2 macrophage markers. Specifically, they significantly reduced the levels of TGF-β and IL-10 and the mRNA expression levels of ARG-1 and CD206 in the M2 phenotypes of RAW264.7 and Ana-1 macrophages. The conditioned medium of CII-3 and pericanaside (5) could inhibit the migration capacity of CT26.WT tumor cells. Macrophage M1/M2 polarization is a dynamic equilibrium, and the M2 phenotype, which can promote the growth of tumor cells, is relatively highly expressed in the tumor microenvironment. CII-3 and pericanaside could significantly reduce the phenotype of M2-type macrophages, indicating that the anti-tumor activity of CII-3 could be related to the inhibitory effect on M2 polarization, and pericanaside was one of the active components.
Vespa velutina auraria Smith is an edible and medicinal insect in China. This study demonstrated the in vitro antioxidant and anti-inflammatory bioactivities and the volatile composition identification determined by Gas chromatography mass spectrometry (GC-MS). The antioxidant activity screening results showed that the ethanol extracts of both the fresh and dried samples exhibited an efficient antioxidant activity for three models, 2,2′-azino-bis (3-ethylbenzo-thiazoline-6-sulfonic acid diammonium salt) free radicals scavenging capacity, 1,1-diphenyl-2-picrylhydrazyl scavenging capacity, and ferric reducing antioxidant power. The anti-inflammatory activity screening in vitro indicated that ethanol extracts had considerable inhibitory effect on Tumor Necrosis Factor-α and Interleukin-1β (IL-1β) in macrophages, but had no influence on IL-6 expression. GC-MS analyses of volatile composition of V. auraria identified 46 components, representing 75.76% of the total peak areas from fresh sample, and 34 components, 84.70% of the total peak areas from dried ones. The volatile constituents were very different in the petroleum ether part of fresh and dried ones. The three major components are hentriacontane (7.76%), n-hexadecanoic acid (6.54%), and palmitoleic acid (4.50%) in the fresh sample, while they are benzeneacetaldehyde (13.11%), dodecanoic acid (7.08%), and oleic Acid (6.72%) in the dried sample.
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