Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a Representative images of colony formation in multiple human colorectal cancer cell lines HCT15, LST174T, RKO, SW620, NCI-H508, Caco2, and mouse colon cell line CT26 treated with the indicated concentrations of TMPyP4. b The line graph represents the relative colony formation of colorectal cancer cells treated with the indicated concentrations of TMPyP4. c Cell viability of colorectal cancer cells and normal cells was measured with the CCK8 assay. Cells were treated with TMPyP4 for 72 h. d , e Cells were treated with 4 μM or 8 μM TMPyP4 for 48 h. Then, the proportion of apoptotic cells was detected using annexin V-propidium iodide-based flow cytometry. Values are represented as mean ± SD, **** p ≤ 0.0001, by multiple t-tests. f , g Cell cycle analysis of colorectal cancer cells treated with or without TMPyP4 for 24 h. Cellular DNA content was determined by propidium iodide staining and flow cytometry. h, i The tumor size ( h ) and tumor weight ( i ) of nude mice bearing SW620 colorectal tumors treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. Values are represented as mean ± SD, **** p ≤ 0.0001, by unpaired t-test. j , k The tumor size ( j ) and tumor weight ( k ) of nude mice treated with vehicle or 30 mg/kg TMPyP4 in the PDX model. n = 6 mice for both groups. Values are represented as mean ± SD, **** p ≤ 0.0001, by two-way ANOVA ( h , j ) or unpaired t-test ( i , k ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: CCK-8 Assay, Flow Cytometry, Cell Cycle Assay, Staining

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a Experimental treatment strategy for tumor growth inhibition in a syngeneic mouse tumor model. When tumors were palpable, mice were treated with vehicle or 30 mg/kg TMPyP4 three times a week (days 0, 3, 6). b , c The tumor size and tumor weight of BALB/C mice bearing CT26 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. d , e The tumor size and tumor weight of C57BL/6 mice bearing MC38 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. ( f , g ) The tumor size and tumor weight of nude mice bearing MC38 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. h, i Tumor growth inhibition comparison between C57BL/6 and nude mice after TMPyP4 treatment. j – p Graphs show the frequencies of CD45 + cells ( j ), CD3 + T cells ( k ), CD8 + T cells ( l ), DCs ( m ), CD4 + T cells ( n ), NK cells ( o ), and B cells ( p ) in CT26 tumors after TMPyP4 treatment or vehicle control treatment. q – w Graphs show the frequencies of CD45 + cells ( q ), CD3 + T cells ( r ), CD8 + T cells ( s ), DCs ( t ), CD4 + T cells ( u ), NK cells ( v ), and B cells ( w ) in MC38 tumors after TMPyP4 treatment or vehicle control treatment. ns : not significant, * p ≤ 0.05, *** p ≤ 0.001, **** p ≤ 0.0001, by two-way ANOVA ( b , d , f ), or by untailed t-tests ( c , e , g – w ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Inhibition, Comparison, Control

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a – h Representative FACS plots and quantification of IFNγ expression ( a , b ), TNFα expression ( c , d ), perforin expression ( e , f ), and PD-1 expression ( g , h ) among CD8 + T cells in MC38 tumors with TMPyP4 treatment or vehicle control treatment. i – l Surface expression of CD80, CD86, and MHC-I on DCs was determined by FACS. Values are represented as mean ± SD, * p ≤ 0.05, ** p ≤ 0.01, **** p ≤ 0.0001, by untailed t-tests ( b , d , f , h , l ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Expressing, Control

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a , b GSEA of the signaling pathway, including regulation of double-strand break repair and DNA double-strand break response in MC38 tumors with TMPyP4 treatment or vehicle control treatment. c Mean tail moment of the HCT116 and MC38 cells treated with or without TMPyP4 in a comet assay. d Quantification of foci/nucleus of γ-H2AX immunofluorescence staining of HCT116 and MC38 cells treated with or without TMPyP4. e Statistical analysis of γ-H2AX in MC38 tumors with TMPyP4 treatment or vehicle control treatment. f Representative images of G4 and γ-H2AX immunofluorescence staining of HCT116 treated with plasmids pCDNA3.1 or PIF1-pCDNA3.1 in the presence of TMPyP4. g , h Quantification of foci/nucleus of G4 and γ-H2AX in ( f ). i , j Western blots of p-TBK1, TBK1, p-STING, STING, and GAPDH in colorectal cancer cells with the indicated concentrations of TMPyP4. k – m RNA levels of Ccl5, Cxcl10, and Ifn-β were detected in CT26 and MC38 treated with or without TMPyP4 for 48 h. n Representative immunostainings of CD8, CD11c, and P-STING in paraffin sections of MC38 tumors with TMPyP4 treatment or vehicle control treatment (CD8 [green], CD11c [orange], P-STING [red], DAPI [blue]) (magnification ×200). o , p The tumor size and tumor weight of C57BL/6 mice bearing indicated MC38 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 5 mice for both groups. Values are represented as mean ± SD, ns : not significant, ** p ≤ 0.01, *** p ≤ 0.001, **** p ≤ 0.0001, by untailed t-tests ( c , d , e , g , h , k , l , m ), or by two-way ANOVA ( g ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Control, Single Cell Gel Electrophoresis, Immunofluorescence, Staining, Western Blot

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a – f Tumor growth of vehicle, TMPyP4 alone (30 mg/kg), anti-PD1 alone (200 μg/body), and TMPyP4 plus anti-PD1 groups in BALB/C mice injected with CT26 cells ( a – c ) or C57BL/C mice injected with MC38 cells ( d – f ). n = 4 mice for each group. g , h The frequencies of CD8 + T cells in CT26 ( g ) and MC38 ( h ) tumors after vehicle, TMPyP4 alone (30 mg/kg), anti-PD1 alone (200 μg/body), and TMPyP4 plus anti-PD1 groups treatment. Values are represented as mean ± SD, * p ≤ 0.05, ** p ≤ 0.01, *** p ≤ 0.001, by two-way ANOVA ( b , e ), or by untailed t-tests ( c , f , g , h ). i Relationship between G4 expression and immunotherapy efficacy in colorectal patients. j The overview of the study.

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Injection, Expressing

Journal: Nucleic Acids Research

Article Title: Guanine quadruplexes in the RNA genome of the tick-borne encephalitis virus: their role as a new antiviral target and in virus biology

doi: 10.1093/nar/gkac225

Figure Lengend Snippet: Antiviral activity and cytotoxicity of G4 ligands in cell-based assays. ( A ) Cytotoxicity of the indicated G4-ligands for porcine kidney stable (PS) cells determined in a concentration range of 0–50 μM and expressed as a percentage of cell viability. PS cells were seeded in 96-well plates for 24 h, then treated with G4 ligands and incubated for 48 h. ( B ) Inhibition of TBEV replication by the indicated G4-ligands. PS cell monolayers were treated with the indicated G4 ligands (50 μM) and simultaneously infected with TBEV strains Neudoerfl and Hypr at MOI of 0.1. The infected cells were then incubated with the compounds for 48 h. Following incubation, media supernatants were collected and viral titers were determined using a plaque assay and expressed as PFU/ml. Compounds PDS, cPDS, NMM, TMPyP4, berberine and PhenDC3 (marked in red) were selected for further evaluation of their antiviral potencies. ( C , D ) The dose-dependent anti-TBEV activities of the indicated G4-ligands were determined for TBEV Neudoerfl (C) and Hypr (D) strains. PS cell monolayers were treated with the compounds at concentrations of 0–50 μM and infected with the respective TBEV strain at MOI of 0.1. The infected cells were then incubated with the compounds for 48 h p.i. or 72 h p.i. and viral titers were determined using the plaque assay. The mean titers from three biological replicates of two independent experiments are shown and error bars indicate standard errors of the mean ( n = 3). The horizontal dashed line indicates the minimum detectable threshold of 1.44 log 10 PFU/ml.

Article Snippet: N-Methylmesoporphyrin IX (NMM) ( , ) and 5,10,15,20-tetrakis-( N -methyl-4-pyridyl)porphine (TMPyP4) ( , ) were obtained from Santa Cruz Biotechnology (Heidelberg, Germany).

Techniques: Activity Assay, Concentration Assay, Incubation, Inhibition, Infection, Plaque Assay

Journal: Nucleic Acids Research

Article Title: Guanine quadruplexes in the RNA genome of the tick-borne encephalitis virus: their role as a new antiviral target and in virus biology

doi: 10.1093/nar/gkac225

Figure Lengend Snippet: Antiviral and cytotoxicity properties of G4-ligands incubated with virus-infected PS cells for 48 h.p.i.

Article Snippet: N-Methylmesoporphyrin IX (NMM) ( , ) and 5,10,15,20-tetrakis-( N -methyl-4-pyridyl)porphine (TMPyP4) ( , ) were obtained from Santa Cruz Biotechnology (Heidelberg, Germany).

Techniques: Incubation, Virus

Journal: Journal of Biomedical Science

Article Title: Targeting the G-quadruplex as a novel strategy for developing antibiotics against hypervirulent drug-resistant Staphylococcus aureus

doi: 10.1186/s12929-024-01109-3

Figure Lengend Snippet: Confirmation of antibacterial activity. A The antibacterial activities of NMM, TMPyP2, BRACO19, TMPyP4, and Thioflavin T against SAUSA300 were examined by measuring cell growth in terms of OD at 600 nm. B, C SAUSA300 cell growth assessed as CFU/mL ( B ); representative sheep-blood agar plates showing the appearance of colonies during CFU enumeration ( C ). D , E Comparative killing kinetics of vancomycin (Van), Tetracycline (Tet), and NMM against SAUSA300 based on CFU/mL at 1.0 × ( D ); and 10 × ( E ) MIC of Van, Tet, NMM, and 0.05% Triton X-100 at different time points (0 to 12 h). F Comparative live/dead assay of SAUSA300 with 1 × MIC of NMM (5 µM) and Van (0.6 µM) using confocal microscopy, showing the proportion of live/dead SAUSA300 cells. SYTO9 and PI were used to stain the number of total and dead cells as green-fluorescent and red-fluorescent cells, respectively. All experiments were performed in triplicate and the average data was plotted with standard deviation. Significance of the data was analyzed using Student’s t -test. p -values less than 0.05 were considered significant (ns = non-significant p > 0.05, * p < 0.05, ** p < 0.01, *** p < 0.005, and **** p < 0.0001)

Article Snippet: The G4 compounds were procured as BRACO19 trihydrochloride (GC50140, GLPBIO); Quarfloxin or CX-3543 (A12380, AdooQ), TMPyP2 or meso-Tetra (3-pyridyl) porphine (T40846, Frontier Scientific), TMPyP4 tosylate (GC12092, GLPBIO), PDS or Pyridostatin trifluoroacetate salt (18013, Cayman Chemical), PhenDC3 trifluoromethanesulfonate (CS-7711, Chemscene), Thioflavin T (2390-54-7, MedChemExpress), Quinacrine dihydrochloride (69-05-6, MedChemExpress), N-methyl mesoporphyrin IX or NMM (GC44416, GLPBIO), and Quercetin (117-39-5, MedChemExpress) (Fig. S1).

Techniques: Activity Assay, Live Dead Assay, Confocal Microscopy, Staining, Standard Deviation

Journal: Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry

Article Title: Utilisation of Targeted Nanoparticle Photosensitiser Drug Delivery Systems for the Enhancement of Photodynamic Therapy

doi: 10.3390/molecules23102628

Figure Lengend Snippet: Targeting moiety approaches used to enhance NP PSs active drug delivery systems in tumours.

Article Snippet: DNA G-quadruplex Aptamer , Direct , Sgc8 leukemia aptamer, which can specifically bind to protein tyrosine kinase 7 (PTK7) receptor , CEM cells CEM (CCL-119, T-cell line, human & Ramos (CRL-1596, B-cell line, human Burkitt’s lymphoma) & Cervical cancer (HeLa) mouse models , In vitro & in vivo , 5, 10, 15, 20-tetrakis (1-methylpyridinium-4-yl) porphyrin (TMPyP4) , Zr-based nanoscale metal-organic frameworks (Zr-NMOFs) , Nanosystem induced 90% cell death of targeted cells & maintained more than 76% tumour inhibition within the entire experimental period. , [ ] .

Techniques: Over Expression, In Vitro, In Vivo, Inhibition, Irradiation

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: The structure of the free-base ligand (H 2 TMPyP 4+ = 5,10,15,20-tetrakis(1-methyl-4-pyridinium-)porphyrin).

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques:

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Soret bands of Ni(II)TMPyP 4+ in various media.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques:

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: ( a ) Molar absorptivity of Q-bands and S1 fluorescence of the high-spin Ni(II)TMPyP 4+ complex. ( b ) Molar absorptivity of Q-bands and S 1 fluorescence of the low-spin Ni(II)TMPyP 4+ complex.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques: Fluorescence

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Excitation and absorption spectra of Ni(II)TMPyP 4+ in water, an equilibrium system involving both high-spin and low-spin species.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques:

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Change in absorption spectra of Ni(II)TMPyP 4+ with increasing temperature in aqueous solution. The red spectrum belongs to 20 °C, the blue one to 75 °C.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques:

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Thermodynamic data calculated for the coordination and spin-state equilibrium of Ni(II)TMPyP 4+ .

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques:

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Spectral change in the Ni(II)TMPyP 4+ solution upon 455 nm irradiation. The blue spectrum was recorded at the end of irradiation.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques: Irradiation

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Concentration changes in the low- and high-spin forms during the 455 nm irradiation of the Ni(II)TMPyP 4+ solution.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques: Concentration Assay, Irradiation

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Spectral changes in the Soret band region for the Ni(II)TMPyP 4+ solution with increasing TEOA concentration in the range of 0–0.5 M. The blue spectrum belongs to 0 M, the red one to 0.5 M.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques: Concentration Assay

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: Partial mole fractions of different Ni(II)TMPyP 4+ species as functions of the TEOA concentration.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques: Concentration Assay

Journal: Molecules

Article Title: Effects of Temperature, Axial Ligand, and Photoexcitation on the Structure and Spin-State of Nickel(II) Complexes with Water-Soluble 5,10,15,20-Tetrakis(1-methylpyridinium-4-yl)porphyrin

doi: 10.3390/molecules29020310

Figure Lengend Snippet: The slope of the line obtained as a function of the TEOA concentration per Equation (5) yields the equilibrium constant regarding the association of Ni(II)TMPyP 4+ with TEOA.

Article Snippet: Tetrachloride salt of Ni(II)TMPyP 4+ was purchased from Frontier Scientific (Newark, DE, USA).

Techniques: Concentration Assay