Grape seeds, by-products of brewing wines, are rich in polyphenol and other ingredients. The optimized extraction, composition of constituents and hypoglycemic activity were investigated in this study. The results showed that grape seeds were rich in anthocyanins and polyphenols and other active substances, inhibited α-glucosidase and α-amylase activity, which provide background and practical knowledge for the deep-processed products of grape seeds with high added value.
The purpose of this study was to produce and characterize an inclusion complex between β‐cyclodextrin (β‐CD) and Exocarpium Citri Grandis essential oil (EEO), and to evaluate its antioxidant properties. The volatile compounds of EEO were characterized by gas chromatography‐mass spectrometer. A comparison of the β‐CD, EEO, and the physical mixture with the inclusion complex revealed differences in their thermal stabilities and morphologies, which confirmed the formation of the β‐CD‐EEO inclusion complex. Complexed with β‐CD, the β‐CD‐EEO inclusion complex showed a higher stability and antioxidant activity when compared with physical mixture and EEO. Therefore, β‐CD can be used to form inclusion complexes with EEO to expand its potential applications in the food and drug industries.
Practical Application
Exocarpium Citri Grandis is rich in essential oil and other ingredients. The optimized extraction, constituent composition, and encapsulation of EEO in β‐CD were investigated in this study. The results showed that the encapsulation process increased the antioxidant activity and stability of EEO, which provides both fundamental and practical knowledge for the application of EEO in the food and drug industries.
Philadelphia chromosome-positive (Ph+) leukemia is a fatal hematological malignancy. Although standard treatments with tyrosine kinase inhibitors (TKI) have achieved remarkable success in prolonging patient survival, intolerance, relapse and TKI resistance remain serious issues for patients with Ph+ leukemia. Here, we report a new leukemogenic process in which RAPSYN and BCR-ABL co-occur in Ph+ leukemia, and RAPSYN mediates the neddylation of BCR-ABL. Consequently, neddylated BCR-ABL enhances the stability by competing its c-CBL-mediated degradation. Furthermore, SRC phosphorylates RAPSYN to activate its NEDD8 E3 ligase activity, promoting BCR-ABL stabilization and disease progression. Moreover, in contrast to in vivo ineffectiveness of PROTAC-based degraders, depletion of RAPSYN expression or its ligase activity decreased BCR-ABL stability and, in turn, inhibited tumor formation and growth. Collectively, these findings represent an alternative to tyrosine kinase activity for the oncoprotein and leukemogenic cells and generate a rationale of targeting RAPSYN-mediated BCR-ABL neddylation for the treatment of Ph+ leukemia.
Philadelphia chromosome-positive (Ph+) leukemia is a fatal hematological malignancy. Although standard treatments with tyrosine kinase inhibitors (TKI) have achieved remarkable success in prolonging patient survival, intolerance, relapse and TKI resistance remain serious issues for patients with Ph+ leukemia. Here, we report a new leukemogenic process in which RAPSYN and BCR-ABL co-occur in Ph+ leukemia, and RAPSYN mediates the neddylation of BCR-ABL. Consequently, neddylated BCR-ABL enhances the stability by competing its c-CBL-mediated degradation. Furthermore, SRC phosphorylates RAPSYN to activate its NEDD8 E3 ligase activity, promoting BCR-ABL stabilization and disease progression. Moreover, in contrast to in vivo ineffectiveness of PROTAC-based degraders, depletion of RAPSYN expression or its ligase activity decreased BCR-ABL stability and, in turn, inhibited tumor formation and growth. Collectively, these findings represent an alternative to tyrosine kinase activity for the oncoprotein and leukemogenic cells and generate a rationale of targeting RAPSYN-mediated BCR-ABL neddylation for the treatment of Ph+ leukemia.
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