[Clinical study on the incidence of femoral head posterior tilt angle in non-displaced femoral neck fractures].

OBJECTIVE: To investigate the occurrence of posterior femoral head tilt after clinical non-displaced femoral neck fracture, and to provide a reference basis for clinical surgery and improvement of disease prognosis. METHODS: Total of 165 patients with non-displaced femoral neck fractures of Garden typeⅠandⅡfrom January 2018 to June 2022 were selected as study subjects including 48 males and 117 females, with an average age of (71.5±8.5) years old ranging from 53 to 89, involving 97 cases of typeⅠand 68 of typeⅡ. On the patient's preoperative sagittal or axial CT film of the hip, the angle formed by the radius line of the femoral head and the midline of the femoral neck was used as the posterior tilt angle of the femoral head (α), and the posterior tilt femoral head angle was measured using the method proposed by Palm. The measured data were divided into 6 groups:α<0°, 0°<α< 5°, 5°≤α<10°, 10°≤α<15°, 15°≤α<20°, α≥20°, and the incidence of different ranges of posterior tilt angle was compared. The sex composition ratio of 165 patients were analyzed and compared, and the age of 65 was used as the cut-off point to compare the incidence of fractures between genders. Patients were divided into the posterior tilt <20° group for 135 cases and the posterior tilt ≥20°group for 30 cases according to the preoperative posterior tilt angle, the differences between two groups in terms of gender and age were analyzed. RESULTS: Among 165 patients with non-displaced femoral neck fractures, 143 cases with poaterior tilt of the femoral head occurred with an incidence of 86.7%. Posterior tilt 0°<α<5° accounted for 36 cases with an incidence of 21.8%;5°≤α<10° accounted for 40 cases with an incidence of 24.2%;10°≤α<15° accounted for 27 cases with an incidence of 16.4%;15°≤α<20° accounted for 10 cases with an incidence of 6.1%;posterior tilt angle α≥20° accounted for 30 cases, the incidence was 18.2%, of which the maximum posterior tilt angle was 42.7°. Statistical analysis showed that the percentage of fractures in the 165 patients selected for this study was significantly higher in female than in male, and that the female group was more likely to have fractures before the age of 65 years compared to the male group. However, gender, age and fracture subtypes (GardenⅠ, Ⅱ) were not influential factors for femoral neck fractures with a preoperative posterior femoral head tilt angle >20°(P>0.05). CONCLUSION: The incidence of femoral head posterior tile in non-displaced femoral neck fractures is relatively high, in which severe posterior tile occurs, and the femoral head posterior tile angle≥20° can reach 18.2%. In patients with closed reduction internal fixation, the fracture end needs to be repositioned as much as possible to reduce the risk of postoperative avascular necrosis of the femoral head. In order to prevent femoral neck fractures, special attention should be paid to anti-osteoporosis treatment for female. Preoperative assessment of posterior tilt is critical for patients of different ages, genders and fracture subtypes (GardenⅠ, Ⅱ).

Preliminary exploration of animal models of congenital choledochal cysts.

BACKGROUND: Various animal models have been used to explore the pathogenesis of choledochal cysts (CCs), but with little convincing results. Current surgical techniques can achieve satisfactory outcomes for treatment of CCs. Consequently, recent studies have focused more on clinical issues rather than basic research. Therefore, we need appropriate animal models to further basic research. AIM: To establish an appropriate animal model that may contribute to the investigation of the pathogenesis of CCs. METHODS: Eighty-four specific pathogen-free female Sprague-Dawley rats were randomly allocated to a surgical group, sham surgical group, or control group. A rat model of CC was established by partial ligation of the bile duct. The reliability of the model was confirmed by measurements of serum biochemical indices, morphology of common bile ducts of the rats as well as molecular biology experiments in rat and human tissues. RESULTS: Dilation classified as mild (diameter, ≥ 1 mm to < 3 mm), moderate (≥ 3 mm to < 10 mm), and severe (≥ 10 mm) was observed in 17, 17, and 2 rats in the surgical group, respectively, while no dilation was observed in the control and sham surgical groups. Serum levels of alanine aminotransferase, aspartate aminotransferase, total bilirubin, direct bilirubin, and total bile acids were significantly elevated in the surgical group as compared to the control group 7 d after surgery, while direct bilirubin, total bilirubin, and gamma-glutamyltransferase were further increased 14 d after surgery. Most of the biochemical indices gradually decreased to normal ranges 28 d after surgery. The protein expression trend of signal transducer and activator of transcription 3 in rat model was consistent with the human CC tissues. CONCLUSION: The model of partial ligation of the bile duct of juvenile rats could morphologically simulate the cystic or fusiform CC, which may contribute to investigating the pathogenesis of CC.

Triterpene esters of cirsium setosum and their anti-inflammatory activity.

Two new triterpene fatty acid esters, 3ß-palmityloxy-12,27-cyclofriedoolean-14-en-11α-ol (1) and 3ß-palmityloxy-19α-hydroxyursane (2), together with 3ß-hydroxy-11-oxo-olean-12-enyl palmitate (3) were isolated from the potent anti-inflammatory active fraction of the petroleum ether-soluble part of Cirsium setosum ethanol extract. Compound 1 was found to be a rare 12,27-cyclopropane triterpenoid. Their structures were determined through spectral data analysis combined with literature reports. Furthermore, in vitro experiment, compounds 1-3 exhibited significant inhibitory effects on nitric oxide production in lipopolysaccharide-activated mouse RAW264.7 macrophages.

Weak Bimetal Coupling-Assisted MN4 Catalyst for Enhanced Carbon Dioxide Reduction Reaction.

The design of multimetal catalysts holds immense significance for efficient CO2 capture and its conversion into economically valuable chemicals. Herein, heterobimetallic catalysts (MiMo)L were exploited for the CO2 reduction reactions (CO2RR) using relativistic density functional theory (DFT). The octadentate Pacman-like polypyrrolic ligand (H4L) accommodates two metal ions (Mo, W, Nd, and U) inside (Mi) and outside (Mo) its month, rendering a weak bimetal coupling-assisted MN4 catalytically active site. Adsorption reactions have access to energetically stable coordination modes of -OCO, -OOC, and -(OCO)2, where the donor atom(s) are marked in bold. Among all of the species, (UiMoo)L releases the most energy. Along CO2RR, it favors to produce CO. The high-efficiency CO2 reduction is attributed to the size matching of U with the ligand mouth and the effective manipulation of the electron density of both ligand and bimetals. The mechanism in which heterobimetals synergetically capture and reduce CO2 has been postulated. This establishes a reference in elaborating on the complicated heterogeneous catalysis.

Seco-nortriterpenoids from Cirsium setosum and their anti-inflammatory activity.

Five unusual seco-nortriterpenoids, 3ß-hydroxy-20,21-seco-30-nortaraxastan-20,21-dioic acid (1), 3ß-hydroxy-20,21-seco-30-nortaraxastan-20-oic-21-oate (2), 3ß-hydroxy-20-oxo-21,22-seco-30-nortaraxastan-22-oic acid (3), 3ß-hydroxy-19-oxo-20,21-seco-29,30-nortaraxastan-21-oic acid (4) and 3ß-hydroxy-19-oxo-20,21-seco-19-norlupan-21-oic acid (5) were isolated and elucidated from the anti-inflammatory activity fraction of the ethanol extract of Cirsium setosum. The structures of these compounds were established through spectroscopic methods. Preliminary biological assays showed that compounds 1-5 had significant inhibitory effect on NO production on lipopolysaccharide-stimulated RAW 264.7 cells, and compound 1 showed the strongest anti-inflammatory activity. This type of ring-opening compound is the first seco-triterpenoid structure discovered from the genus of Cirsium.

Clinical features and prognosis of chronic natural killer cell lymphoproliferative disorders.

OBJECTIVE: To analyze the current treatment status and prognostic regression of the chronic NK cell lymphoproliferative disorder (CLPD-NK). METHODS: We retrospectively analyzed the clinical features, treatment and prognosis of 18 patients with CLPD-NK who were treated at our Hospital between September 2016 and September 2022. RESULTS: Eighteen patients were included: three patients were treated with chemotherapy, five patients underwent immune-related therapy, one patient was treated with glucocorticoids alone, five patients were administered granulocyte colony-stimulating factor, blood transfusion therapy, or anti-infection therapy, followed by observation and follow-up, and four patients were observed without treatment. Fifteen patients survived, including two patients who achieved complete remission (CR) and seven patients who achieved partial remission (PR), of whom one patient progressed to Aggressive NK-cell leukemia (ANKL) and sustained remission after multiple lines of treatment; three patients were not reviewed, of which one patient was still in active disease, three patients developed hemophagocytic syndrome during treatment and eventually died, one of them had positive Epstein-Barr virus (EBV) expression. The 5-years overall survival rate was 83%. CONCLUSION: Most patients with CLPD-NK have inert progression and a good prognosis, whereas some patients have a poor prognosis after progressing to ANKL and combined with hemophagocytic syndrome. Abnormal NK cells invading the center suggest a high possibility of ANKL development, and immunosuppressants and hormones are effective treatments for this disease.

Functionalized magnetic metal organic framework nanocomposites for high throughput automation extraction and sensitive detection of antipsychotic drugs in serum samples.

Due to the complexity of biological sample matrix, the automated and high-throughput pretreatment technology is urgently needed for monitoring the antipsychotic drugs for mental patients. In this study, functionalized magnetic zirconium-based organic framework nanocomposites (Fe3O4@SiO2@Zr-MOFs) were successfully designed and synthesized by the layer-by-layer growth. Among them, Fe3O4@SiO2@UiO-67-COOH showed the best adsorption performance, and at the same time it exhibited excellent water dispersibility, high thermal stability, chemical stability and high hydrophobicity. Results of adsorption kinetics, isotherm and FT-IR showed that the adsorption process was dominated by chemical adsorption (hydrogen bond, electrostatic interaction, π-π interaction) and monolayer adsorption. Moreover, the smaller pore size improved the protein exclusion rate which reached 98.9-99.8%. Based on the above result, the synthesized magnetic nanoparticles were introduced to 96-well automatic extractor, antipsychotic drugs in 96 serum samples were automatically extracted within 9 min, which most greatly saved the time and labor costs and avoided artificial errors. By further integrating with ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS), antipsychotic drugs can be detected in the range of 0.2-3.0 ng mL-1 with a quantitative limit of 0.06-0.9 ng mL-1. The recoveries of antipsychotic drugs and their metabolites in serum ranged from 95.7% to 112.3% within 1.4-6.5% of RSD. These features indicate that the proposed method is promising for high throughput and sensitively monitoring of drugs and other hazardous substances.

Enrichment and immobilization of heavy metal ions from wastewater by nanocellulose/carbon dots-derived composite.

Heavy metal ions (HMIs) have been widely applied in various industries because of their excellent physicochemical properties. However, their discharging without appropriate treatment brought about serious pollution problems. So it is desirable but challenging to rapidly and completely clean up these toxic pollutants from water, especially utilizing environmentally friendly and naturally rich biomass materials. In this work, we prepared nanocellulose/carbon dots/magnesium hydroxide (CCMg) ternary composite using cotton via a simple hydrothermal method. The removal mechanism towards Cd2+ and Cu2+ was investigated using a combination of experimental techniques and density functional theory calculations. CCMg shows a good ability to remove HMIs. It is realized that the interaction between each component of CCMg and cadmium nitrate is mainly of hydrogen/dative bonds. Cadmium nitrate is preferentially enriched by the Mg(OH)2 moiety, proved by calculated thermodynamics, interfacial interactions and charges. After transformation, the cadmium carbonate precipitate is fixed on the surface by nanocellulose (NC) via chemical coupling; and of interest is that copper ion precipitates in the form of basic sulfate. Due to its high adsorption effect and simple recovery operation, CCMg is having a wide range of application prospects as a water treatment agent.

Diagnostic accuracy of dual-energy CT for bone marrow edema in patients with acute knee injury: a systematic review and meta-analysis.

BACKGROUND: Knee injuries are prevalent, and early diagnosis is crucial for guiding clinical therapy. MRI is the diagnostic gold standard for bone marrow edema (BME) in patients with acute knee injuries, yet there are still limitations. Dual-energy CT, a possible viable replacement, is being explored (DECT). METHODS: We systematically retrieved studies from EMBASE, Scopus, PUBMED, and the Cochrane Library and collected gray literatures. In accordance with the PRISMA-DTA standards, a systematic review was conducted between the study's initiation and July 31, 2021, utilizing an MRI reference standard and at least 10 adult patients with acute knee injuries to evaluate the diagnostic effectiveness of DECT for diagnosing BME. Two reviewers collected the study's details independently. For the meta-analysis, a bivariate mixed-effects regression model was utilized, and subgroup analysis was employed to determine the sources of variability. RESULTS: The research included nine studies that examined 290 individuals between the ages of 23 and 53 with acute knee injuries who had DECT and MRI. Overall, the sensitivity, specificity, and AUC of the BME were 85% (95% confidence interval [CI]: 77-90%), 96% (95% CI: 93-97%), and 0.97 (95% CI: 0.95-0.98), respectively. To account for the assumed diversity of research, there were no statistically significant differences between the comparison groups in terms of specificity and sensitivity. CONCLUSION: DECT is a viable alternative to MRI for individuals with acute knee injuries when MRI is inappropriate or unavailable.

[Research progress of caput femoris posterior tilt and its impact on prognosis in nondisplaced femoral neck fractures].

There are still many unresolved problems in the treatment and prognosis of nondisplaced femoral neck fractures, such as nonunion and avascular necrosis of the caput femoris .In order to reduce the risk of various complications after non-displaced femoral neck fractures, the caput femoris posterior tilt of femoral neck fractures and its impact on prognosis have attracted more and more attention. A large number of scholars' studies have found that when the posterior tilt exceeds 20°, the risk of internal fixation failure increases significantly. Based on this concept, we can choose to use primary artificial joint replacement instead of three-screw internal fixation according to the different posterior tilt angles of patients to reduce the incidence of postoperative complications. At the same time, our analysis found that comminution of the posterior segment of the femoral neck would lead to an increase in the posterior inclination angles. The purpose of this review was to investigate the relationship between caput femoris posterior tilt of femoral neck fractures and surgical outcome, and to introduce a new method for measuring caput femoris posterior tilt of the femoral neck.

Tuning the Alkyl Chain of Nitrilotriacetamide for Selectively Extracting Trivalent Am over Eu Ions.

The successful management and safe disposal of high-level nuclear waste necessitate the efficient separation of actinides (An) from lanthanides (Ln), which has emerged as a crucial prerequisite. Mixed donor ligands incorporating both soft and hard donor atoms have garnered interest in the field of An/Ln separation and purification. One such example is nitrilotriacetamide (NTAamide) derivatives, which have demonstrated selectivity in extracting minor actinide Am(III) ions over Eu(III) ions. Nevertheless, the Am/Eu complexation behavior and selectivity remain underexplored. In the work, a comprehensive and systematic investigation has been conducted for [M(RL)(NO3)3] complexes (M = Am and Eu) utilizing relativistic density functional theory. The NTAamide ligand (RL) is substituted with various alkyl groups, namely, methyl, ethyl, propyl, n-butyl, n-pentyl, n-hexyl, n-heptyl, and n-octyl. Thermodynamic calculations show that the alkyl chain length in NTAamide is capable of tuning the separation selectivity of Am and Eu. Moreover, the differences in calculated free energies between Am and Eu complexes are more negative for R = Bu-Oct than Me-Pr. This indicates that elongation of the alkyl chain can increase the efficiency of selective separation of Am(III) from Eu(III). Based on the quantum theory of atoms in molecules and charge decomposition analyses, it has been observed that the strength of Am-RL bonds is higher than that of Eu-RL bonds. This disparity is attributed to a greater degree of covalency in Am-RL bonds and a higher level of charge transfer from ligands to Am within complexes containing these bonds. Energies of occupied orbitals with the central N character are recognized overall lower for [Am(OctL)(NO3)3] than for [Eu(OctL)(NO3)3], indicative of stronger complexation stability of the former. These results offer valuable insights into the separation mechanism of NTAamide ligands, which can help guide the development of more powerful agents for An/Ln separation in future applications.

Design and Synthesis of Bouchardatine Derivatives as a Novel AMP-Activated Protein Kinase Activator for the Treatment of Colorectal Cancer.

Metabolic reprogramming is a crucial hallmark of tumorigenesis. Modulating the reprogrammed energy metabolism is an attractive anticancer therapeutic strategy. We previously found a natural product, bouchardatine, modulated aerobic metabolism and inhibited proliferation in the colorectal cancer cell (CRC). Herein, we designed and synthesized a new series of bouchardatine derivatives to discover more potential modulators. We applied the dual-parametric high-content screening (HCS) to evaluate their AMP-activated protein kinase (AMPK) modulation and CRC proliferation inhibition effect simultaneously. And we found their antiproliferation activities were highly correlated to AMPK activation. Among them, 18a was identified with nanomole-level antiproliferation activities against several CRCs. Interestingly, the evaluation found that 18a selectively upregulated oxidative phosphorylation (OXPHOS) and inhibited proliferation by modulating energy metabolism. Additionally, this compound effectively inhibited the RKO xenograft growth along with AMPK activation. In conclusion, our study identified 18a as a promising candidate for CRC treatment and suggested a novel anti-CRC strategy by AMPK activating and OXPHOS upregulating.

The coupling of graphene, graphitic carbon nitride and cellulose to fabricate zinc oxide-based sensors and their enhanced activity towards air pollutant nitrogen dioxide.

It is desirable but challenging to sense toxic nitrogen dioxide (NO2) for it has become one of the most prominent air pollutants. Zinc oxide-based gas sensors are known to detect NO2 gas efficiently, however, the sensing mechanism and involved intermediates structures remain underexplored. In the work, a series of sensitive materials, including zinc oxide (ZnO) and its composites ZnO/X [X = Cel (cellulose), CN (g-C3N4) and Gr (graphene)] have been comprehensively examined by density functional theory. It is found that ZnO favors adsorbing NO2 over ambient O2, and produces nitrate intermediates; and H2O is chemically held by zinc oxide, in line with the non-negligible impact of humidity on the sensitivity. Of the formed composites, ZnO/Gr exhibits the best NO2 gas-sensing performance, which is proved by the calculated thermodynamics and geometrical/electronic structures of reactants, intermediates and products. The interfacial interaction has been elaborated on for composites (ZnO/X) as well as their complexes (ZnO- and ZnO/X-adsorbates). The current study well explains experimental findings and opens up a way to design and unearth novel NO2 sensing materials.

Confinement effect of network-structured carbon dots/cellulose nanofiber/magnesium hydroxide for enhanced heavy metal ions capture and immobilization.

To solve pollution problem of heavy metal ions (HMIs) and recover them for sustainable development, a high-efficient-sewage treatment agent, carbon dots/cellulose nanofiber/Mg(OH)2 (CCMg), has been fabricated via a simple hydrothermal method. A variety of characterizations show that cellulose nanofiber (CNF) formed a layered-net structure. Hexagonal Mg(OH)2 flakes of about 100 nm has been attached on CNF. Carbon dots (CDs) around 10-20 nm in size were produced from CNF and distributed along CNF. The extraordinary structural feature endows CCMg with high removal performance towards HMIs. The up-taken capacities reach 992.8 and 667.3 mg g-1 for Cd2+ and Cu2+, respectively. The composite bears excellent durability in treating wastewater. Notably, the qualification of the drinking water can be satisfied while applying CCMg to handle Cu2+ wastewater. The mechanism of removal process has been proposed. Practically, Cd2+/Cu2+ ions were immobilized by CNF due to the space confinement effect. It achieves the facile separation and recovery of HMIs from the sewage, and more importantly, eliminates the risk of secondary contamination.

[Finite element analysis of optimal selection of cannulated threaded screw for the prevention of femoral neck shortening after internal fixation for femoral neck fracture].

OBJECTIVE: To propose the an optimal screw placement scheme to prevent femoral neck shortening, finite element analysis was used to evaluate the biomechanical outcome of different numbers formed by full threaded screws at different positions in the treatment of femoral neck fractures of Pauwels type Ⅱ. METHODS: Recruited for this study was a 55-year-old female volunteer with a weight of 70 kg and a height of 165 cm. CT scan data of her right femur was collected. The models of femoral of Pauwels typeⅡ and fully threaded screw(FTS) and partially threaded screw(PTS) were constructed in three-dimensional modeling software. All these screw placement schemes were divided into eight groups simulated the inverted triangular configuration:three PTSs, an anterosuperior FTS and two PTSs, a posterosuperior FTS and two PTSs, an inferior FTS and two PTSs, an anterosuperior PTS and two FTSs, a posterosuperior PTS and two FTSs, an inferior PTS and two FTSs and three FTSs. All fracture internal fixation models were processed in finite element analysis software. Parameters of postoperative femoral neck length, displacement distribution and peak displacement of screws and VonMises stress distribution and peak stress of screws, the proximal femur and fracture section were collected. RESULTS: The maximum VonMises stress of screws was 239.71, 213.44, 199.37, 230.82, 201.63, 215.72, 185.65 and 192.64 MPa, respectively, which was concentrated in the inferior screw near the fracture line. The maximum Von Mises stress of the proximal femur was 269.48, 241.62, 249.43, 269.69, 271.60, 346.64, 236.97 and 439.62 MPa, respectively, which was concentrated in the inferior medial area of subtrochanteric femur. The maximum Von Mises stress of fracture section was 149.12, 143.04, 140.47, 139.63, 139.81, 130.07, 117.77 and 57.89 MPa, respectively, which was concentrated around the partially threaded screw channel instead of the fully threaded screw channel. The maximum displacement of screws was 5.52, 5.43, 5.32, 5.17, 5.05, 5.13, 5.28 and 5.04 mm, respectively, which was along the axis of the femoral neck, and the displacement distribution was concentrated on the tip of the screw. The length of postoperative femoral neck length was 74.69, 74.72, 74.70, 74.70, 74.72, 74.70, 74.72 and 74.74 mm, respectively. CONCLUSION: The placement of one anterosuperior partially threaded screw and two fully threaded screws with an inverted triangular distribution can not only meet the sliding compression effect to promote femoral neck healing and ensure the stability of the proximal femur, but also reduce the degree of postoperative femoral neck shortening and reduce the incidence of hip joint dysfunction. This study provides a new optimal screw placement solution for the treatment of femoral neck fractures.

Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.

The development of triple-negative breast cancer (TNBC) is highly associated with G-quadruplex (G4); thus, targeting G4 is a potential strategy for TNBC therapy. Because concomitant histone deacetylases (HDAC) inhibition could amplify the impact of G4-targeting compounds, we designed and synthesized two novel series of G4/HDAC dual-targeting compounds by connecting the zinc-binding pharmacophore of HDAC inhibitors to the G4-targeting isaindigotone scaffold (1). Among the new compounds, a6 with the potent HDAC inhibitory and G4 stabilizing activity could induce more DNA G4 formation than SAHA and 1 in TNBC cells. Remarkably, a6 caused more G4-related DNA damage and G4-related differentially expressed genes, consistent with its effect on disrupting the cell cycle, invasion, and glycolysis. Furthermore, a6 significantly suppresses the proliferation of various TNBC cells and the MDA-MB-231 xenograft model without evident toxicity. Our study suggests a novel strategy for TNBC therapeutics through dual-targeting HDAC and G4.

Uranium-Doped Zinc, Copper, and Nickel Oxides for Enhanced Catalytic Conversion of Furfural to Furfuryl Alcohol: A Relativistic DFT Study.

Transition metal oxides (TMOs) and actinide ones (AnOs) have been widely applied in catalytic reactions due to their excellent physicochemical properties. However, the reaction pathway and mechanism, especially involving TM-An heterometallic centers, remain underexplored. In this respect, relativistic density functional theory (DFT) was used to examine uranium-doped zinc, copper, and nickel oxides for their catalytic activity toward the conversion of furfural to furfuryl alcohol. A comparison was made with their undoped TMOs. It was found that the three TMOs were capable of catalyzing the reaction, where the free energies of adsorption, hydrogenation, and desorption fell between -33.93 and 45.00 kJ/mol. The uranium doping extremely strengthened the adsorption of CuO-U and NiO-U toward furfural, making hydrogenation or desorption much harder. Intriguingly, ZnO-U showed the best catalytic performance among all six catalyst candidates, as its three reaction energies were very small (-10.54-8.12 kJ/mol). The reaction process and mechanism were further addressed in terms of the geometrical, bonding, charge, and electronic properties.

Design, Synthesis, and Evaluation of New Sugar-Substituted Imidazole Derivatives as Selective c-MYC Transcription Repressors Targeting the Promoter G-Quadruplex.

c-MYC is a key driver of tumorigenesis. Repressing the transcription of c-MYC by stabilizing the G-quadruplex (G4) structure with small molecules is a potential strategy for cancer therapy. Herein, we designed and synthesized 49 new derivatives by introducing carbohydrates to our previously developed c-MYC G4 ligand 1. Among these compounds, 19a coupled with a d-glucose 1,2-orthoester displayed better c-MYC G4 binding, stabilization, and protein binding disruption abilities than 1. Our further evaluation indicated that 19a blocked c-MYC transcription by targeting the promoter G4, leading to c-MYC-dependent cancer cell death in triple-negative breast cancer cell MDA-MB-231. Also, 19a significantly inhibited tumor growth in the MDA-MB-231 mouse xenograft model accompanied by c-MYC downregulation. Notably, the safety of 19a was dramatically improved compared to 1. Our findings indicated that 19a could become a promising anticancer candidate, which suggested that introducing carbohydrates to improve the G4-targeting and antitumor activity is a feasible option.