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Gefitinib, an epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI),is the currently recommended first-line therapy for advanced EGFR-mutant lung cancer, and understanding the mechanism of resistance is the key to formulating therapeutic strategies for EGFR-TKIs. In this study, we evaluate the expression patterns and potential biological functions of the pseudogene DUXAP10 in gefitinib resistance. We find that pseudogene DUXAP10 expression is significantly upregulated in NSCLC gefitinib-resistant cells and tissues. Gain and loss of function assays reveal that knockdown of DUXAP10 by siRNA reverses gefitinib resistance both in vitro and in vivo. Furthermore, DUXAP10 interacts with the histone methyltransferase enhancer of zeste homolog 2 (EZH2) to repress the expression of 2′,5′-oligoadenylate synthetase (OAS2). Overall, our study highlights the pivotal role of DUXAP10 in gefitinib resistance, and the DUXAP10/EZH2/OAS2 axis might be a promising therapeutic target to overcome acquired gefitinib resistance in NSCLC.

(1) Background: Discarded young fig fruits (DYFFs) result in a waste of resources, such as sparse fruits and residual fruits, and there has been no research on the relationship between phenolic compounds and biological activity in DYFFs (2) Methods: Different deep eutectic solvents (DESs) and 80% ethanol were used to prepare DYFF extracts, and polyphenol extraction efficiency and bioactivities in the DYFFs extracts were compared. (3) Results: More than 1700 phytochemicals were identified in DYFFs, and thirteen of these typical phenolic compounds were analyzed quantitatively; chlorogenic acid, rutin, luteolin 8-C-glucoside, and epicatechin are the main polyphenols in DYFFs, especially chlorogenic acid with 2720–7980 mg/kg. Ferulic acid, caffeic acid, epicatechin, (+)-catechin, luteolin 8-C-glucoside, rutin, hesperetin, and chlorogenic acid showed different degrees of correlation with in vitro antioxidant activity. Moreover, the highest total phenol content found in the extracts of ChCl-Ethylene glycol (Choline chloride:Ethylene glycol = 1:2) was 8.88 mg GAE/g DW, and all quantitatively analyzed phenolic compounds had high levels in various DESs and 80% ethanol. The 80% ethanol and Choline chloride (ChCl) solvent system showed the greatest antioxidant properties, and the Choline chloride-Urea (Choline chloride: Urea = 1:2) extract of DYFFs exhibited the highest inhibitory activity. (4) Conclusions: DESs have demonstrated potential as promising green solvents, especially the ChCl solvent system, which facilitates the extraction of polyphenols. [ABSTRACT FROM AUTHOR]

Phenolic compounds (PCs), flavonoids, non-flavonoids and hybrid phenolics, with antibacterial and antioxidant properties, which can be applied to improve the fruit quality at the postharvest phase. Exogenous PCs improve postharvest fruits quality by inhibiting disease, maintaining nutraceutical compounds, delaying senescence, and improving respiratory metabolism and energy status. They attach to targets in cell walls and membranes of fungal, can inhibit the defensive enzyme activity and disturb the synthesis of ergosterol that is the main component of fungal cell membrane. Moreover, they can significantly decrease the reactive oxygen species (ROS) content in fruits as effective ROS scavengers. Therefore, this paper reviewed the classification and the potential mechanism and application of exogenous PCs treatment in controlling diseases, improving fruits quality and regulating metabolism in fruits during storage, and encourages research on more precise physical simulation methods to determine the specific action sites in PCs-fungal-fruits. [ABSTRACT FROM AUTHOR]

Soybean functional peptides (SFPs) are obtained via the hydrolysis of soybean protein into polypeptides, oligopeptides, and a small amount of amino acids. They have nutritional value and a variety of functional properties, including regulating blood lipids, lowering blood pressure, anti-diabetes, anti-oxidant, preventing COVID-19, etc. SFPs have potential application prospects in food processing, functional food development, clinical medicine, infant milk powder, special medical formulations, among others. However, bitter peptides containing relatively more hydrophobic amino acids can be formed during the production of SFPs, seriously restricting the application of SFPs. High-quality confirmatory human trials are needed to determine effective doses, potential risks, and mechanisms of action, especially as dietary supplements and special medical formulations. Therefore, the physiological activities and potential risks of soybean polypeptides are summarized, and the existing debitterness technologies and their applicability are reviewed. The technical challenges and research areas to be addressed in optimizing debittering process parameters and improving the applicability of SFPs are discussed, including integrating various technologies to obtain higher quality functional peptides, which will facilitate further exploration of physiological mechanism, metabolic pathway, tolerance, bioavailability, and potential hazards of SFPs. This review can help promote the value of SFPs and the development of the soybean industry. [ABSTRACT FROM AUTHOR]

Gefitinib, an epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI),is the currently recommended first-line therapy for advanced EGFR-mutant lung cancer, and understanding the mechanism of resistance is the key to formulating therapeutic strategies for EGFR-TKIs. In this study, we evaluate the expression patterns and potential biological functions of the pseudogene DUXAP10 in gefitinib resistance. We find that pseudogene DUXAP10 expression is significantly upregulated in NSCLC gefitinib-resistant cells and tissues. Gain and loss of function assays reveal that knockdown of DUXAP10 by siRNA reverses gefitinib resistance both in vitro and in vivo . Furthermore, DUXAP10 interacts with the histone methyltransferase enhancer of zeste homolog 2 (EZH2) to repress the expression of 2',5'-oligoadenylate synthetase (OAS2). Overall, our study highlights the pivotal role of DUXAP10 in gefitinib resistance, and the DUXAP10/EZH2/OAS2 axis might be a promising therapeutic target to overcome acquired gefitinib resistance in NSCLC.

It is well known that long non-coding RNAs (lncRNAs) play an important role in the regulation of tumor genesis and development. They can modulate gene expression of transcriptional regulation, epigenetic regulation of chromatin modification, and post-transcriptional regulation, thus influencing the biological behavior of tumors, such as cell proliferation, apoptosis, cell cycle, invasion, and migration. Tumor angiogenesis not only provides nutrients and helps excrete metabolites, but it also opens a pathway for tumor metastasis. Anti-angiogenic therapy has become one of the effective treatment methods for tumor. But its drug resistance leads to the limitation of clinical application. Recent studies have shown that lncRNAs are closely related to tumor angiogenesis and anti-angiogenic therapy resistance, which provides a new direction for tumor research. lncRNAs are expected to be new targets for tumor therapy. For the first time to our knowledge, this paper reviews advancement of lncRNAs in tumor angiogenesis and anti-angiogenic therapy resistance and further discusses their potential clinical application., Competing Interests: The authors declare no competing interests., (© 2022 The Authors.)