Fluorescence anisotropy studies on the Hoechst 33258-DNA interaction: the solvent effect

Amirbekyan, Karen; Shahinyan, Gohar A.; Ghazoyan, Heghine H.; Sargsyan, Hasmik R.; Markarian, Shiraz A.

doi:10.1080/07391102.2020.1782267

Cited by 7 publications

(5 citation statements)

References 24 publications

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“…Cell apoptosis can be detected by Hoechst 33258 staining, which emits an intense blue fluorescence by binding to the DNA of apoptotic cells . As shown in Figure A, SK-OV-3 cells treated with I16 emitted strong blue fluorescence, which was brighter than that of cells treated with DMSO.…”

Section: Resultsmentioning

confidence: 98%

“…Cell apoptosis can be detected by Hoechst 33258 staining, which emits an intense blue fluorescence by binding to the DNA of apoptotic cells. 38 As shown in Figure 7 A, SK-OV-3 cells treated with I16 emitted strong blue fluorescence, which was brighter than that of cells treated with DMSO. Moreover, the fluorescence intensity gradually increased as the concentration of I16 increased, suggesting chromatin condensation and apoptosis.…”

Section: I16 Inhibits Migration Of Sk-ov-3mentioning

confidence: 86%

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Design of Selective PARP-1 Inhibitors and Antitumor Studies

Zhang,

Li,

Liu

et al. 2024

J. Med. Chem.

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Designing selective PARP-1 inhibitors has become a new strategy for anticancer drug development. By sequence comparison of PARP-1 and PARP-2, we identified a possible selective site (S site) consisting of several different amino acid residues of α-5 helix and D-loop. Targeting this S site, 140 compounds were designed, synthesized, and characterized for their anticancer activities and mechanisms. Compound I16 showed the highest PARP-1 enzyme inhibitory activity (IC50 = 12.38 ± 1.33 nM) and optimal selectivity index over PARP-2 (SI = 155.74). Oral administration of I16 (25 mg/kg) showed high inhibition rates of Hela and SK-OV-3 tumor cell xenograft models, both of which were higher than those of the oral positive drug Olaparib (50 mg/kg). In addition, I16 has an excellent safety profile, without significant toxicity at high oral doses. These findings provide a novel design strategy and chemotype for the development of safe, efficient, and highly selective PARP-1 inhibitors.

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Section: Resultsmentioning

confidence: 98%

Section: I16 Inhibits Migration Of Sk-ov-3mentioning

confidence: 86%

Design of Selective PARP-1 Inhibitors and Antitumor Studies

Zhang,

Li,

Liu

et al. 2024

J. Med. Chem.

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“…Cell apoptosis was detected by hoechst 33258 staining, which emits a strong blue fluorescence by binding to the DNA of apoptotic cells [27] . As shown in Figure 3A, A549 cells treated with LXQ‐217 emitted strong blue fluorescence.…”

Section: Resultsmentioning

confidence: 99%

Small Molecule SHP2 Inhibitor LXQ‐217 Affects Lung Cancer Cell Proliferation in Vitro and in Vivo

Sun,

Bai,

Zhang

et al. 2024

Chemistry & Biodiversity

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Background SHP2 is highly expressed in a variety of cancer and has emerged as a potential target for cancer therapeutic agents. The identification of uncharged pTyr mimics is an important direction for the development of SHP2 inhibitors. Methods SPR and CETSA were employed to verify the direct binding of LXQ‐217 to SHP2. The inhibitory effect of LXQ‐217 was characterized by linear Weaver‐Burke enzyme kinetic analysis and BIOVIA Discovery Studio. The inhibition of tumor cell proliferation by LXQ‐217 was characterized by cell viability assay, colony formation assays and hoechst 33258 staining. The inhibition of lung cancer proliferation in vivo was studied in nude mice after oral administration of LXQ‐217. Results An electroneutral bromophenol derivative, LXQ‐217, was identified as a competitive SHP2 inhibitor. LXQ‐217 induced apoptosis and inhibited growth of human pulmonary epithelial cells by affecting the RAS‐ERK and PI3K‐AKT signaling pathways. Long‐term oral administration of LXQ‐217 significantly inhibited the proliferation ability of lung cancer cells in nude mice. Moreover, mice administered LXQ‐217 orally at high doses exhibited no mortality or significant changes in vital signs. Conclusions Our findings on the uncharged orthosteric inhibitor provide a foundation for further development of a safe and effective anti‐lung cancer drug.

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“…Staining. Morphological changes in cell nuclei were measured using Hoechst 33258 probe, as described previously [11]. Cal-27 and Tca8113 cells at a density of 5 × 10 4 cells/mL were seeded onto 24-well plates and cultured for 24 h. Te cells were incubated with diferent concentrations (0.25, 1, and 4 μM) of AIL for 24 h. After the incubation, the cells were fxed with 4% paraformaldehyde at room temperature for 10 min.…”

Section: Hoechst 33258mentioning

confidence: 99%

Ailanthone Inhibits Cell Proliferation in Tongue Squamous Cell Carcinoma via PI3K/AKT Pathway

Wang

Cui

Chen

et al. 2022

Evidence-Based Complementary and Alternative Medicine

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Tongue squamous cell carcinoma (TSCC) is the most widespread and invasive subtype of oral cancer with high recurrence rates. Ailanthone (AIL) is an active ingredient in the plant extracts of Ailanthus altissima (Mill.) Swingle. Here, we showed that AIL inhibited the proliferation of human TSCC, the cell viability of Cal-27 and Tca8113 was significantly decreased after AIL treatment for 24 h. Hoechst 33258 staining demonstrated apoptotic characteristics (such as chromatin aggregation) after AIL treatment. The ratio of early- and late-apoptotic cells in AIL-treated Cal-27 and TCA8113 cells increased remarkably when compared with the control group. Bcl-2/Bax ratio and the levels of PARP1, caspase-9, and caspase-3 decreased after AIL treatment, accompanied by significant increase of cleaved PARP1, cleaved caspase-9, and caspase-3 in Cal-27 and TCA8113 cells. Meanwhile, AIL led to Cal-27 cell cycle arrest at G2/M phase. Western blot implied decreased levels of CDK1 and cyclin B1 after AIL treatment. The level of phospho-PI3K p55 subunit and p-Akt were significantly downregulated by AIL in both Cal-27 and TCA8113 cells. These findings implied the potential applications of AIL in the treatment of human TSCC.

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Fluorescence anisotropy studies on the Hoechst 33258-DNA interaction: the solvent effect

Cited by 7 publications

References 24 publications

Design of Selective PARP-1 Inhibitors and Antitumor Studies

Design of Selective PARP-1 Inhibitors and Antitumor Studies

Small Molecule SHP2 Inhibitor LXQ‐217 Affects Lung Cancer Cell Proliferation in Vitro and in Vivo

Ailanthone Inhibits Cell Proliferation in Tongue Squamous Cell Carcinoma via PI3K/AKT Pathway

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