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.

To explore the potential immunomodulatory effects of total extract and different polar parts from Blaps rynchopetera Fairmaire. Phagocytic activity was evaluated by neutral red assay, and the effect of the immune function was investigated by normal and immunocompromised mice models. In vitro, total extract, as well as chloroform, ethyl acetate, n-butanol and water fractions could individually enhance the phagocytic ability of mouse peritoneal macrophages; in addition, chloroform and ethyl acetate fractions had an increasing tendency when combined stimulation with lipopolysaccharide (LPS). In vivo, ethyl acetate fraction (EAF) could enhance the immune organ index, increase the serum hemolysin level and peripheral blood immune cells of immunocompromised mice, while for normal mice, the effect was inconspicuous. Blaps rynchopetera extracts had noteworthy immunomodulatory effect, especially for individuals with immune disorders.

One undescribed fatty glyceride (1), two unreported N-acetyldopamine dimers (2 and 3), and four known structurally diverse N-acetyldopamine dimers were isolated from adult Vespa velutina auraria Smith. Their structures were elucidated based on a comprehensive analysis of spectroscopic data, HRESIMS, and NMR calculations with ML_J_DP4, and the absolute configurations of 2 and 3 were determined via ECD calculations. Regarding their bioactivities, compounds 5 and 6 can inhibit the production of NO. Moreover, compounds 3, 5 and 7 showed stronger antioxidant activity than the positive control (VC) at 14 μg/mL. A network pharmacology study was used to explore the potential bioactive mechanisms. In addition, a docking study of anti-inflammatory and antioxidative compounds was also performed.