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Fig 1.

Chemical structure of test compounds.

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Fig 2.

Cytotoxicity tests of compounds by MTT assay.

Cells were treated with various compounds for 4h, and grown for another 20h. (A)IC50 of HeLa and HepG2 cells (B)HEK-293T cells Data represent the mean± standard deviation (n = 6).

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Fig 3.

FE-SEM images of Tf-LP-Compound 2.

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Table 1.

Size, ζ-potential and Encapsulation efficiency of LPs before and after coupling of Tf at pH 7.4.

Data are shown as means and standard deviation (n = 3).

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Table 1 Expand

Fig 4.

In vitro release of LP-Compound 2, Tf-LP-Compound 2 and free Compound 2.

Drug release during 24 h incubation in PBS (0.5%v/v Tween 80) at 37 degree C, mean SD values (n = 3) are presented.

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Fig 5.

Cytotoxicity tests of various formulations in various cells.

(A) HeLa cells (B) HepG2 cells (C) HEK-293T cells. Data represent the mean± standard deviation (n = 6) (*p<0.05, ** p<0.01: Tf-LP-Compound 2 versus LP-Compound 2).

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Fig 6.

Fluorescence image of HeLa and HepG2 cells stained with JC-1.

(A)Photograph showing JC-1 red, JC-1 green and merge image. (B)Numerical data were expressed in terms of the ratio of JC-1 aggregates to JC-1 monomers. Data are representative of three independent experiments and expressed as means ±SD, *p, 0.05, **p, 0.01 and ***p, 0.001 as compared with the control.

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Fig 7.

Cellular uptake of LP-Compound 2 and Tf-LP-Compound 2.

Flow cytometry after incubation of LP-Compound 2, Tf-LP-Compound 2 and Tf-LP-Compound 2 with holo Tf. Data represent the mean± standard deviation (n = 3)(**p<0.01 vs LP-Compound 2).

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Fig 8.

Intracellular localization of LP-Compound 2 and Tf-LP-Compound 2.

Confocal microscopy analysis after 4 h of incubation of LP-Compound 2 and Tf-LP-Compound 2 at 37°C with HeLa cells (A) and HepG2 cells (B). NBD-DOPE fluorescence is shown in green, sulforhodamine B is shown in red, and DAPI nuclear stain is shown in blue.

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Fig 8 Expand