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Aim: Physcion is a major bioactive ingredient in the traditional Chinese medicine Radix et Rhizoma Rhei, which has an anthraquinone chemical structure and exhibits a variety of pharmacological activities including laxative, hepatoprotective, anti-inflammatory, antimicrobial and anti-proliferative effects. In this study we investigated the effect of physcion on human nasopharyngeal carcinoma in vitro and in vivo, as well as the mechanisms underlying the anti-tumor action. Methods: The nasopharyngeal carcinoma cell line CNE2 was treated with physcion, and cell viability was detected using MTT and colony formation assays. Flow cytometry was used to assess the cell cycle arrest, mitochondrial membrane potential loss, apoptosis, autophagy and intracellular ROS generation. Apoptotic cell death was also confirmed by a TUNEL assay. The expression of target or marker molecules was determined using Western blotting. The activity of caspase-3, 8, and 9 was detected with an ELISA kit. A xenograft murine model was used to evaluate the in vivo anti-tumor action of physcion, the mice were administered physcion (10, 20 mg·kg -1 ·d -1 , ip) for 30 d.Results: Treatment with physcion (5, 10, and 20 μmol/L) dose-dependently suppressed the cell viability and colony formation in CNE2 cells. Physcion (10 and 20 μmol/L) dose-dependently blocked cell cycle progression at G 1 phase and induced both caspase-dependent apoptosis and autophagy in CNE2 cells. Furthermore, physcion treatment induced excessive ROS generation in CNE2 cells, and subsequently disrupted the miR-27a/ZBTB10 axis, resulting in repression of the transcription factor Sp1 that was involved in physcioninduced apoptosis and autophagy. Moreover, physcion-induced autophagy acted as a pro-apoptotic factor, and possibly contributed to physcion-induced apoptosis. In the xenograft murine model, administration of physcion dose-dependently suppressed the tumor growth without affecting the body weight. Furthermore, the anti-tumor effects of physcion were correlated with downregulation of Sp1 and suppression of miR-27a in the tumor tissues. Conclusion: Physcion induces apoptosis and autophagy in human nasopharyngeal carcinoma by targeting Sp1, which was mediated by ROS/miR-27a/ZBTB10 signaling. The results suggest that physcion is a promising candidate for the treatment of human nasopharyngeal carcinoma.

This work was designed to investigate the phenolic composition, antioxidant and pancreatic lipase inhibitory activities of Rhus chinensis Mill. fruits extracted by different solvents, and to illustrate which major phenolic compounds were responsible for lipase inhibition and to evaluate their interactions. Results showed that R. chinensis Mill. fruits were rich in phenolics, which included 13 types identified and quantified by UHPLC-ESI-HRMS/MS. Among the identified phenolics, myricetin-3-O-rhamnoside and quercetin-3-O-rhamnoside were the most dominant detected in all extracts. Extracts with 80% methanol, 80% ethanol and 80% acetone exhibited strong antioxidant and pancreatic lipase inhibitory activities in vitro, and these activities were positively correlated with phenolic contents. Myricetin-3-O-rhamnoside and quercetin-3-O-rhamnoside demonstrated good lipase inhibitory activities in a dose-dependent manner and synergistically inhibited lipase. This work may provide insights into the potential uses of R. chinensis Mill. fruits in food and nutraceutical industries. Keywords Identification and quantification, lipotoxicity, phenolic profile, reduction in fats intake, UHPLC-ESI-HRMS/MS. *Correspondent: E-mails: caikmust2013@163.com (SC) and mjpangkmust@163.com (MP) International