Chao Han
China Pharmaceutical University
ProdrugCytotoxicityCancerMass spectrometryHigh-performance liquid chromatographyEnzymeChemistryApoptosisGlycolysisIn vitroIn vivoAcetophenoneMelicopeNatural productDrug deliveryDoxorubicinDemethylaseMitochondrionLYSINE-SPECIFIC DEMETHYLASE 1ChromatographyReactive oxygen speciesEnantiomerCancer researchBiochemistryCell growthCountercurrent chromatographyStereochemistryElutionCell cultureBiologyResolution (mass spectrometry)Cell biologyCancer cellPharmacology
27Publications
11H-index
288Citations
Publications 27
Newest
#1Chen Chen (CPU: China Pharmaceutical University)H-Index: 6
#2Tianyu Zhu (CPU: China Pharmaceutical University)H-Index: 5
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 10 authors...
Abstract null null The first rate-limiting enzyme of the serine synthesis pathway (SSP), phosphoglycerate dehydrogenase (PHGDH), is hyperactive in multiple tumors, which leads to the activation of SSP and promotes tumorigenesis. However, only a few inhibitors of PHGDH have been discovered to date, especially the covalent inhibitors of PHGDH. Here, we identified withangulatin A (WA), a natural small molecule, as a novel covalent inhibitor of PHGDH. Affinity-based protein profiling identified that...
Source
#1Xiao Xu (CPU: China Pharmaceutical University)H-Index: 5
#2Chao Han (CPU: China Pharmaceutical University)H-Index: 11
Last. Ling-Yi KongH-Index: 58
view all 6 authors...
Rationale: Integration of several monotherapies into a single nanosystem can produce remarkable synergistic antitumor effects compared with separate delivery of combination therapies. We developed near-infrared (NIR) light-triggered nanoparticles that induce a domino effect for multimodal tumor therapy. Methods: The designed intelligent phototriggered nanoparticles (IPNs) were composed of a copper sulfide-loaded upconversion nanoparticle core, a thermosensitive and photosensitive enaminitrile mo...
1 CitationsSource
#1Chunling Ren (CPU: China Pharmaceutical University)
#2Yaolan Lin (CPU: China Pharmaceutical University)H-Index: 5
Last. Chao Han (CPU: China Pharmaceutical University)H-Index: 11
view all 8 authors...
Abstract Lysine-specific histone demethylase 1 (LSD1) was the first histone demethylase identified in epigenetics and has recently emerged as an attractive therapeutic target for treating tumors. To date, almost all reported LSD1 inhibitors have been chemosynthesized; however, natural products possess pharmacological and biological activity and can be sources for drug development. Here, we established a target separation countercurrent chromatography technique to isolate LSD1 inhibitors from zed...
Source
#1Dan Yan (CPU: China Pharmaceutical University)H-Index: 1
#2Xiao Xu (CPU: China Pharmaceutical University)H-Index: 5
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 7 authors...
Abstract On-demand therapy following effective tumor detection would considerably reduce the side effects of traditional chemotherapy. DT-diaphorase (DTD), whose level is strongly elevated in various tumors, is a cytosolic flavoenzyme that promotes intracellular reactive oxygen species (ROS) generation via the redox cycling of hydroquinones. Incorporation of the DTD-responsive substrate to the structures of the probe and prodrug may facilitate the tumor detection and therapy. Herein, we establis...
Source
#1Chao Han (CPU: China Pharmaceutical University)H-Index: 11
#2Xiao Xu (CPU: China Pharmaceutical University)H-Index: 3
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 7 authors...
Abstract Targeting mitochondria-mediated apoptosis has emerged as a promising strategy for tumor therapy. However, technologies used to treat tumors that enable the direct visualization of mitochondria-mediated apoptosis in living cells have not been developed to date. Cytochrome c (Cyt c) translocation from mitochondria is a central mediating event in cell apoptosis. In this study, we developed a multifunctional nanosensor that can monitor the real-time translocation of Cyt c from mitochondria ...
2 CitationsSource
#1Yaolan Lin (CPU: China Pharmaceutical University)H-Index: 5
#2Jian-Guang Luo (CPU: China Pharmaceutical University)H-Index: 28
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 8 authors...
Abstract It is significant to precisely isolate potential active compounds from medicinal herbs containing multiple compounds. Herein, a new strategy for precise separation of lysine-specific demethylase 1 (LSD1) inhibitors from the rhizome of Corydalis yanhusuo (RCY) using counter-current chromatography (CCC) guided by molecular docking and liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) analysis was established. First, representative alkaloids from RCY were docked with LSD...
3 CitationsSource
#1Wen-Li Wang (CPU: China Pharmaceutical University)H-Index: 6
#2Xiao-Qin Liu (CPU: China Pharmaceutical University)H-Index: 2
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 10 authors...
Taxodisones A and B, C30¬-terpenes with an unprecedented tetracyclo[12.4.0.0.2,709,14]octodecane core, were isolated from the seeds of Taxodium distichum. Their structures including configurations were unambiguously determined. Their biomimetic synthesis was described to suggest they stemmed from diterpenes and monoterpenes not from squalene or oxidosqualene. In addition, their bioactivities were also evaluated.
2 CitationsSource
#1Yaolan Lin (CPU: China Pharmaceutical University)H-Index: 5
#2Chao Han (CPU: China Pharmaceutical University)H-Index: 11
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 8 authors...
Abstract The ability to separate bioactive compounds from herbal medicines, which contain abundant components, is crucial for drug discovery. Conventional Countercurrent chromatography (CCC) methods for separating bioactive compounds are labor intensive and show low efficiency. Here, we present a novel integrative CCC method for separating lysine-specific demethylase 1 (LSD1) inhibitors from the roots of Salvia miltiorrhiza (RSM). The methanol extracts of RSM were separated into hydrosoluble and...
5 CitationsSource
#1Jin-Fang Xu (Shanxi Medical University)H-Index: 6
#2Chao Han (CPU: China Pharmaceutical University)H-Index: 11
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 8 authors...
Abstract Melicolones C–K (1–9), nine acetophenone derivatives with three unprecedented architectures, were characterized from the leaves of Melicope ptelefolia. Among them, melicolone C (1) was a novel acetophenone analogue possessing a highly rearranged spiro skeleton. Melicolones D-F (2–4) were three novel acetophenone congeners bearing unusual octalactone ring. Melicolones G-K (5–9) were five new prenylated acetophenone derivatives featuring a 9-oxatricyclo [3.2.1.13, 8]nonane core. Their str...
3 CitationsSource
#1Shanting Liao (CPU: China Pharmaceutical University)H-Index: 8
#2Chao Han (CPU: China Pharmaceutical University)H-Index: 11
Last. Ling-Yi Kong (CPU: China Pharmaceutical University)H-Index: 58
view all 6 authors...
Activated macrophages switch from oxidative phosphorylation to aerobic glycolysis, similar to the Warburg effect, presenting a potential therapeutic target in inflammatory disease. The endogenous metabolite itaconate has been reported to regulate macrophage function, but its precise mechanism is not clear. Here, we show that 4-octyl itaconate (4-OI, a cell-permeable itaconate derivative) directly alkylates cysteine residue 22 on the glycolytic enzyme GAPDH and decreases its enzyme activity. Glyc...
54 CitationsSource