Inflammation is generally considered a key risk factor in the progress of several chronic diseases, such as arthritis, gastritis, and hepatitis. Natural products with anti-inflammatory ability have played a great role in the process of overcoming these inflammatory diseases. In this study, we evaluated the anti-inflammatory activities of ten natural compounds derived from lotus seedpod and discovered (E)-9-octadecenoic acid ethyl ester (E9OAEE) inhibited the production of nitric oxide (NO) optimally in lipopolysaccharide (LPS)-induced RAW264.7 macrophages. Furthermore, we explored the effects of E9OAEE on inflammatory responses and the underlying mechanisms in LPS-induced RAW264.7 macrophages. The results indicated that E9OAEE significantly suppressed the production of NO, prostaglandin E2 (PGE2), and tumour necrosis factor-α (TNFα) in a dose-dependent manner. The protein expression and mRNA levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX2) were inhibited by pretreatment of E9OAEE. Furthermore, E9OAEE restrained the phosphorylation of mitogen-activated protein kinase (MAPKs) family members, ERK, P38, and JNK stimulated by LPS-treated for 30min and prevented the nuclear translocation of nuclear factor-kappa B (NF-κB) prompted by LPS-treated for 6h in RAW264.7 macrophages. Taken together, we discovered an anti-inflammatory component from lotus seedpod and identified E9OAEE attenuated the inflammatory response in LPS-induced RAW264.7 macrophages probably by regulating the activation of MAPKs and NF-κB signalling pathways, which would provide some base for the development of new anti-inflammatory drugs.

Background: Epidermal growth factor receptor H773_V774 insH (EGFR‐insH) is an EGFR exon 20 insertion mutation in non‐small cell lung cancer (NSCLC), which is naturally resistant to available EGFR tyrosine kinase inhibitors (TKIs) and lacks a patient‐derived cell line.Methods: A Ba/F3 cell line expressing EGFR‐insH mutation (Ba/F3‐insH cell line) was generated using an IL3‐deprivation method. A cell proliferation assay was performed to screen natural compounds that exhibit a synergistic effect with erlotinib. Trypan blue staining was used to assess cell growth and crystal violate staining was recruited to evaluate clonogenic potential. Flow cytometry was used to detect EGFR expression and cell apoptosis. A xenograft model was created to evaluate the effect of ellagic acid (EA) with erlotinib on tumor growth.Results: EA was identified to synergistically inhibit the proliferation of Ba/F3‐insH cells with erlotinib. The growth and clonogenic potential of Ba/F3‐insH cells were definitely constrained by EA with erlotinib, whereas, the apoptosis of Ba/F3‐insH cells was dramatically promoted by the combination. In a xenograft model of the Ba/F3‐insH cell line, the combination treatment also exhibited a synergistic reduction in tumor growth.Conclusions: In this study, we generated a Ba/F3 cell line expressing EGFR H773_V774 insH mutation and identified a synergistic treatment (EA with erlotinib) that markedly inhibited the viability of Ba/F3‐insH cells in vitro and in vivo.Key points: Our results indicated that the combination of ellagic acid with erlotinib has synergistic effects against EGFR H773_V774 insH mutation.

Gynura procumbens is a traditional herb and food extensively cultivated in China and Southeast Asian countries. In this work, the crude extract (CE) of G. procumbens was purified with macroporous resin to obtain the refined fraction, and its anti-inflammatory activity was compared with that of CE. Moreover, the detailed mechanisms of anti-inflammatory activity were also investigated for the first time. The results indicated that CE was more effective in anti-inflammatory activity and it could reduce the secretion of NO, TNF-α, and PGE2 via decreasing the iNOS, TNF-α, and COX-2 genes transcription and related proteins translation, which were associated with the inhibition of AP-1 and NF-κB nuclear translocation and downregulation of PI3K/Akt and MAPK signaling pathways. In conclusion, the extract of G. procumbens has a promising potential in inflammation-related disorders alleviation, and these findings could provide the basis for the comprehensive utilization of G. procumbens and the new functional food development.