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, 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