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Yuling Qiu,Yali Chen,Haiyang Yu,Qianxiang Zhou,Ran Wang,Meihua Jin,Dexin Kong 한국응용곤충학회 2017 Journal of Asia-Pacific Entomology Vol.20 No.2
Bee venom has been used for treating various diseases for a long time. However, the bioactive constituents of bee venom and its mechanisms remain poorly understood. In the present study, phospholipase A2 (Bt-PLA2) cDNA was cloned, and a mature form of Bt-PLA2 was purified from bumblebee venom (Bombus terrestris). The differentiation induction and apoptosis induction activities of Bt-PLA2 on chronic myelogenous leukemia (CML) K562 cells were also evaluated. Bt-PLA2 cDNA has 540 nucleotides that encode a 180-amino-acid protein. The purified, mature form of Bt-PLA2 was an 18-kDa protein, and it inhibited K562 cell growth, determined by an IC50 value of 29.5 ng/μl. Moreover, Bt-PLA2 induced erythroid differentiation of K562 cells in a dose-dependent manner, and this was supplemented with the upregulation of glycophorin A (GPA) mRNA expression. Bt-PLA2- induced apoptosis, analyzed by DAPI staining, was correlated with the result analyzed by AnnexinV-FITC/PI binding. Furthermore, activation of caspase 3 and poly ADP-ribose polymerase (PARP) and inhibition of p-Akt, determined by western blot, further demonstrated that Bt-PLA2 induced apoptosis mainly through the Akt pathway. The parallel induction of erythroblasts differentiation of K562 cells and apoptosis due to Bt-PLA2 treatment demonstrated the potential use of Bt-PLA2 as an anti-leukemia drug lead.
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Gao Shan,Guo Tingting,Luo Shuyu,Zhang Yan,Ren Zehao,Lang Xiaona,Hu Gaoyong,Zuo Duo,Jia Wenqing,Kong Dexin,Yu Haiyang,Qiu Yuling 한국응용약물학회 2022 Biomolecules & Therapeutics(구 응용약물학회지) Vol.30 No.6
Chronic myeloid leukemia (CML) is a slowly progressing hematopoietic cell disorder. Sphingosine kinase 1 (SPHK1) plays established roles in tumor initiation, progression, and chemotherapy resistance in a wide range of cancers, including leukemia. However, small-molecule inhibitors targeting SPHK1 in CML still need to be developed. This study revealed the role of SPHK1 in CML and investigated the potential anti-leukemic activity of hirsuteine (HST), an indole alkaloid obtained from the oriental plant Uncaria rhynchophylla, in CML cells. These results suggest that SPHK1 is highly expressed in CML cells and that overexpression of SPHK1 represents poor clinical outcomes in CML patients. HST exposure led to G2/M phase arrest, cellular apoptosis, and downregulation of Cyclin B1 and CDC2 and cleavage of Caspase 3 and PARP in CML cells. HST shifted sphingolipid rheostat from sphingosine 1-phosphate (S1P) towards the ceramide coupled with a marked inhibition of SPHK1. Mechanistically, HST significantly blocked SPHK1/S1P/S1PR1 and BCR-ABL/PI3K/Akt pathways. In addition, HST can be docked with residues of SPHK1 and shifts the SPHK1 melting curve, indicating the potential protein-ligand interactions between SPHK1 and HST in both CML cells. SPHK1 overexpression impaired apoptosis and proliferation of CML cells induced by HST alone. These results suggest that HST, which may serve as a novel and specific SPHK1 inhibitor, exerts anti-leukemic activity by inhibiting the SPHK1/S1P/ S1PR1 and BCR-ABL/PI3K/Akt pathways in CML cells, thus conferring HST as a promising anti-leukemic drug for CML therapy in the future.
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