Journal: The Journal of Biological Chemistry

Article Title: Zafirlukast inhibits the growth of lung adenocarcinoma via inhibiting TMEM16A channel activity

doi: 10.1016/j.jbc.2022.101731

Figure Lengend Snippet: ZAF is a novel inhibitor of TMEM16A channel. A , virtual screening flowchart. B , TMEM16A channel inhibitor binding pocket. C , whole-cell currents of HEK293T cells overexpressing (OE) TMEM16A channels were activated by 600 nM Ca 2+ in the pipette solution and inhibited by 10 μM of T16A inh -A01. WT HEK293T as vehicle control. The stimulation protocol: a holding potential of 0 mV for 100 ms, the membrane voltage was clamped in steps of 20 mV from −80 to +80 mV for 750 ms, then back down to −80 mV for 500 ms. D , statistical results of the TMEM16A whole-cell current in ( C ). Data are means ± SD (n = 3; ∗∗∗∗ p < 0.0001, OE TMEM16A + Ca 2+ versus control; ∗∗∗∗ p < 0.0001, OE TMEM16A + Ca 2+ + T16A inh -A01 versus OE TMEM16A + Ca 2+ ). E , the inhibition by Conivaptan, Entrectinib, Pimaricin, and Zafirlukast (100 μM) of TMEM16A current tested at +80 mV. Data are means ± SD (n = 5). F , representative current of TMEM16A inhibited by various concentrations of ZAF (0, 0.01, 0.1, 1, 10, and 100 μM). The stimulation protocol is consistent with ( C ). G , I-V curve of the TMEM16A currents inhibited with different concentrations of ZAF (n = 5). H , concentration response curves of ZAF inhibition of TMEM16A currents in HEK293T cells. The plot was fitted to the Hill equation (n = 5). HEK293T, human embryonic kidney 293T cells; I-V, current–voltage; ZAF, Zafirlukast.

Article Snippet: Entrectinib, Pimaricin, and T16A inh -A01 were purchased from TargetMol.

Techniques: Binding Assay, Transferring, Control, Membrane, Inhibition, Concentration Assay

Journal: Expert opinion on drug delivery

Article Title: Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar solution.

doi: 10.1080/17425247.2020.1719995

Figure Lengend Snippet: Figure 6. The natamycin-loaded micelle was nontoxic to corneal epithelial cells. The cell viability in the Nat group and Nat-Mi group was detected by CCK-8 after 24 h (a) and 72 h (b) of incubation. The data were expressed as mean ± standard deviation (SD), n= 3. Ctrl: control; Nat: natamycin; Nat-Mi: natamycin-loaded micelle.

Article Snippet: Natamycin was purchased from Selleck Chemicals (Houston, USA).

Techniques: CCK-8 Assay, Incubation, Standard Deviation, Control

Journal: Expert opinion on drug delivery

Article Title: Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar solution.

doi: 10.1080/17425247.2020.1719995

Figure Lengend Snippet: Figure 5. (a) TEM images of drug-loaded (or natamycin-loaded, nat-NP) multicore micelle (nat-NP was drop casted from PBS); (b) Solubility of drug-loaded multicore micelle and pure natamycin in PBS (pH 7.4), left for micellar formulations, right for dispersion formulations; (c) In vitro cumulative drug release percentage of natamycin with pH 7.4 at 37°C.

Article Snippet: Natamycin was purchased from Selleck Chemicals (Houston, USA).

Techniques: Solubility, Dispersion, In Vitro

Journal: Expert opinion on drug delivery

Article Title: Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar solution.

doi: 10.1080/17425247.2020.1719995

Figure Lengend Snippet: Figure 7. Natamycin-loaded micelle inhibited Candida growth in vitro. Minimal inhibition concentration (a) and the diameter of zone of inhibition (b) in the Nat-Mi group and Nat group against Candida were measured after 24 h of incubation in/on YPD medium. The data were expressed as mean ± standard deviation (SD), n= 3. Ctrl1 = control 1, Ctrl2 = control 2, Nat: natamycin; Nat-Mi: natamycin-loaded micelle.

Article Snippet: Natamycin was purchased from Selleck Chemicals (Houston, USA).

Techniques: In Vitro, Inhibition, Concentration Assay, Incubation, Standard Deviation, Control

Journal: Expert opinion on drug delivery

Article Title: Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar solution.

doi: 10.1080/17425247.2020.1719995

Figure Lengend Snippet: Figure 8. Natamycin-loaded micelle recovered the fungal keratitis in clinic. New Zealand white rabbits were infected with Candida albicans and were routinely and visually evaluated for corneal involvement for 15 days under a slit lamp. The control group comprised of untreated fungal keratitis rabbits, while the remaining rabbits were given anti-fungal drugs. A score was assigned for each of the following five criteria: conjunctival hyperemia, corneal clouding, corneal infiltration (measured as the size of epithelial defect in mm), corneal neovascu- larization and hypopyon level. For the 15 consecutive days of observation, the representative images (a) and clinical score measurements (b) are shown. The images indicate the disease progression at 5, 10 and 15 days. *P< 0.05, compared with the Ctrl group at the same time point; #P< 0.05, compared with same group at day five; n= 3. Ctrl: control; Nat: natamycin; Nat-Mi: natamycin-loaded micelle.

Article Snippet: Natamycin was purchased from Selleck Chemicals (Houston, USA).

Techniques: Infection, Control, Biomarker Discovery

Journal: Expert opinion on drug delivery

Article Title: Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar solution.

doi: 10.1080/17425247.2020.1719995

Figure Lengend Snippet: Figure 9. Natamycin-loaded micelle reduced the fungal numbers in vivo. The fungal morphology and numbers were observed with direct smear (left) and confocal microscopy (right) at 5 and 15 days. Scale bars: 10 μm for left, 100 μm for right, n= 3. Ctrl: control; Nat: natamycin; Nat-Mi: natamycin-loaded micelle.

Article Snippet: Natamycin was purchased from Selleck Chemicals (Houston, USA).

Techniques: In Vivo, Confocal Microscopy, Control

Journal: Expert opinion on drug delivery

Article Title: Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar solution.

doi: 10.1080/17425247.2020.1719995

Figure Lengend Snippet: Figure 11. Natamycin-loaded micelle promoted the drug penetration in vivo. The drug levels in eye tissues including the cornea (a) and aqueous humor (b) were detected at the end of 15 days of post-dosing. *P< 0.05, compared with the Ctrl group; #P< 0.05, compared with the Nat group; n= 3. Ctrl: control; Nat: natamycin; Nat-Mi: natamycin-loaded micelle.

Article Snippet: Natamycin was purchased from Selleck Chemicals (Houston, USA).

Techniques: In Vivo, Control

Journal: Expert opinion on drug delivery

Article Title: Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar solution.

doi: 10.1080/17425247.2020.1719995

Figure Lengend Snippet: Figure 10. Natamycin-loaded micelle improved the corneal morphology in vivo. The corneal morphology was observed by anterior segment optical coherence tomography (AS-OCT) (left) and H&E staining (right). Scale bars: 500 μm for left, 100 μm for righ, n= 3. Ctrl: control; Nat: natamycin; Nat-Mi: natamycin-loaded micelle.

Article Snippet: Natamycin was purchased from Selleck Chemicals (Houston, USA).

Techniques: In Vivo, Tomography, Staining, Control

Journal: Translational Vision Science & Technology

Article Title: The Effect of Anti-Amoebic Agents and Ce6-PDT on Acanthamoeba castellanii Trophozoites and Cysts, In Vitro

doi: 10.1167/tvst.9.12.29

Figure Lengend Snippet: Anti-Amoebic Agent Concentrations in Our Experiments

Article Snippet: For the experiments, the anti-amoebic agents PHMB (Pharmacy of Saarland Medical University, Homburg/Saar, Germany), CH (Sigma-Aldrich, USA), DD (European Pharmacopoeia, Strasbourg, France), HD (European Pharmacopoeia, Strasbourg, France), PD (Brolene, Patheon UK Ltd., Swindon, UK), natamycin (5% natamycin ophthalmic suspension preserved with 0.02% benzalkonium chloride; Alcon Laboratories, Fort Worth, TX), PVPI (B. Braun, Melsungen, Germany), MF (Sigma-Aldrich, Switzerland), and chlorin e6 (Ce6, ORPEGEN Pharma, Heidelberg, Germany) were used.

Techniques:

Journal: Translational Vision Science & Technology

Article Title: The Effect of Anti-Amoebic Agents and Ce6-PDT on Acanthamoeba castellanii Trophozoites and Cysts, In Vitro

doi: 10.1167/tvst.9.12.29

Figure Lengend Snippet: Cytotoxic effect (mean ± standard error) of polyhexamethylene biguanide (PHMB), chlorhexidine (CH), hexamidine-diisethionate (HD), propamidine-isethionate (PD), dibromopropamidine-diisethionate (DD), natamycin (NM), miltefosine (MF), and chlorin e6 photodynamic therapy (PDT) on 1BU trophozoites (LDH assay; n = 5). PHMB, CH, HD, PD, DD, NM, MF, and chlorin e6-PDT increased LDH activity significantly in trophozoite cultures ( P < 0.01) compared with controls. The use of Ce6 without illumination did not change LDH activity ( P = 0.96) compared with Ce6 with illumination. * P ≤ 0.05; ** P ≤ 0.011; *** P ≤ 0.005.

Article Snippet: For the experiments, the anti-amoebic agents PHMB (Pharmacy of Saarland Medical University, Homburg/Saar, Germany), CH (Sigma-Aldrich, USA), DD (European Pharmacopoeia, Strasbourg, France), HD (European Pharmacopoeia, Strasbourg, France), PD (Brolene, Patheon UK Ltd., Swindon, UK), natamycin (5% natamycin ophthalmic suspension preserved with 0.02% benzalkonium chloride; Alcon Laboratories, Fort Worth, TX), PVPI (B. Braun, Melsungen, Germany), MF (Sigma-Aldrich, Switzerland), and chlorin e6 (Ce6, ORPEGEN Pharma, Heidelberg, Germany) were used.

Techniques: Lactate Dehydrogenase Assay, Activity Assay

Journal: Translational Vision Science & Technology

Article Title: The Effect of Anti-Amoebic Agents and Ce6-PDT on Acanthamoeba castellanii Trophozoites and Cysts, In Vitro

doi: 10.1167/tvst.9.12.29

Figure Lengend Snippet: Cytotoxic effect (mean ± standard error) of polyhexamethylene biguanide (PHMB), chlorhexidine (CH), hexamidine-diisethionate (HD), propamidine-isethionate (PD), dibromopropamidine-diisethionate (DD), miltefosine (MF), povidone iodine (PVPI), and chlorin e6 photodynamic therapy (PDT) on 1BU trophozoites (trypan blue assay; n = 3). All tested drugs increased the percentage of trypan blue-stained 1BU trophozoites significantly ( P < 0.01) compared with controls. Concerning different drug concentrations, all displayed significantly ( P ≤ 0.02) increased cytotoxicity on 1BU trophozoites compared with controls, except 0.005% PHMB ( P = 0.59), 0.005% CH ( P = 0.10), and Ce6 without illumination ( P = 0.99). * P ≤ 0.05; ** P ≤ 0.011; *** P ≤ 0.005.

Article Snippet: For the experiments, the anti-amoebic agents PHMB (Pharmacy of Saarland Medical University, Homburg/Saar, Germany), CH (Sigma-Aldrich, USA), DD (European Pharmacopoeia, Strasbourg, France), HD (European Pharmacopoeia, Strasbourg, France), PD (Brolene, Patheon UK Ltd., Swindon, UK), natamycin (5% natamycin ophthalmic suspension preserved with 0.02% benzalkonium chloride; Alcon Laboratories, Fort Worth, TX), PVPI (B. Braun, Melsungen, Germany), MF (Sigma-Aldrich, Switzerland), and chlorin e6 (Ce6, ORPEGEN Pharma, Heidelberg, Germany) were used.

Techniques: Staining

Journal: Translational Vision Science & Technology

Article Title: The Effect of Anti-Amoebic Agents and Ce6-PDT on Acanthamoeba castellanii Trophozoites and Cysts, In Vitro

doi: 10.1167/tvst.9.12.29

Figure Lengend Snippet: Cytotoxic effect (mean ± standard error) of polyhexamethylene biguanide (PHMB), chlorhexidine (CH), hexamidine-diisethionate (HD), propamidine-isethionate (PD), dibromopropamidine-diisethionate (DD), miltefosine (MF), povidone iodine (PVPI), and chlorin e6 photodynamic therapy (PDT) on 1BU cysts (trypan blue assay; n = 3). All tested drugs increased the percentage of trypan blue-stained 1BU cysts significantly ( P < 0.01) compared with controls. All drug concentrations displayed significantly ( P < 0.01) increased cytotoxicity to 1BU cysts compared with controls, except 0.005% CH ( P = 0.29), Ce6 without illumination ( P = 0.94), and 0.00095% or 0.0038% Ce6 with illumination ( P = 0.14; P = 0.06). * P ≤ 0.05; ** P ≤ 0.011; *** P ≤ 0.005.

Article Snippet: For the experiments, the anti-amoebic agents PHMB (Pharmacy of Saarland Medical University, Homburg/Saar, Germany), CH (Sigma-Aldrich, USA), DD (European Pharmacopoeia, Strasbourg, France), HD (European Pharmacopoeia, Strasbourg, France), PD (Brolene, Patheon UK Ltd., Swindon, UK), natamycin (5% natamycin ophthalmic suspension preserved with 0.02% benzalkonium chloride; Alcon Laboratories, Fort Worth, TX), PVPI (B. Braun, Melsungen, Germany), MF (Sigma-Aldrich, Switzerland), and chlorin e6 (Ce6, ORPEGEN Pharma, Heidelberg, Germany) were used.

Techniques: Staining

Journal: Translational Vision Science & Technology

Article Title: The Effect of Anti-Amoebic Agents and Ce6-PDT on Acanthamoeba castellanii Trophozoites and Cysts, In Vitro

doi: 10.1167/tvst.9.12.29

Figure Lengend Snippet: Impact of the drug treatment on the encystment and growth behavior of A. castellani 1BU cysts on non-nutrient agar E. coli plates. Cysts were incubated in PBS medium either in absence of drugs (control) or with the drugs and concentrations indicated (0.02% PHMB, 0.02% CH, 0.1% HD, 0.1% PD, 0.1% DD, 5% NM, 0.0065% MF, or 1% PVPI), subsequently stained with trypan blue and afterward diluted in medium to a cell density of 2.000 cysts/mL. There were 10 µl of the solution (approximately 20 cysts) were pipetted onto the centers of fresh non-nutrient agar E. coli plates. Cysts containing solutions were allowed to aspirate for 10 minutes before the first set of images were recorded by bright field microscopy. Cyst-inoculated plates were subsequently incubated at 30°C for up to 3 weeks and images of the central and peripheral regions were taken at the time points indicated. Images are representative of four independent biological experiments. The disinfectant lysoform served as killing control.

Article Snippet: For the experiments, the anti-amoebic agents PHMB (Pharmacy of Saarland Medical University, Homburg/Saar, Germany), CH (Sigma-Aldrich, USA), DD (European Pharmacopoeia, Strasbourg, France), HD (European Pharmacopoeia, Strasbourg, France), PD (Brolene, Patheon UK Ltd., Swindon, UK), natamycin (5% natamycin ophthalmic suspension preserved with 0.02% benzalkonium chloride; Alcon Laboratories, Fort Worth, TX), PVPI (B. Braun, Melsungen, Germany), MF (Sigma-Aldrich, Switzerland), and chlorin e6 (Ce6, ORPEGEN Pharma, Heidelberg, Germany) were used.

Techniques: Incubation, Control, Staining, Microscopy