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Synthesis and therapeutic effect of styrene-maleic acid copolymer-conjugated pirarubicin.

Tsukigawa K, Liao L, Nakamura H, Fang J, Greish K, Otagiri M, Maeda H - Cancer Sci. (2015)

Bottom Line: Consequently, SMA-THP conjugate showed significantly prolonged circulation time compared to free THP and high tumor-targeting efficiency by the enhanced permeability and retention (EPR) effect.As a result, remarkable antitumor effect was achieved against two types of tumors in mice without apparent adverse effects.These findings suggest the potential of SMA-THP conjugate as a highly favorable candidate for anticancer nanomedicine with good stability and tumor-targeting properties in vivo.

View Article: PubMed Central - PubMed

Affiliation: Institute for Drug Delivery Science, Sojo University, Kumamoto, Japan; Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto, Japan.

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In vitro cytotoxicity and intracellular uptake of free pirarubicin (THP) and styrene–maleic acid copolymer (SMA)-conjugated THP (SMA-THP conjugate). Cytotoxicities of free THP and SMA-THP conjugate against HeLa cells (a) and colon 26 cells (b) were measured by MTT assay. Values are means ± SEM. (c) Intracellular uptake of free THP and SMA-THP conjugate in HeLa cells. Values are means ± SEM (n = 3). (d) HPLC analyses of free THP at 6 h (d-i), SMA-THP conjugate at 10 h (d-ii), and 40 h (d-iii) in HeLa cells after each treatment.
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fig03: In vitro cytotoxicity and intracellular uptake of free pirarubicin (THP) and styrene–maleic acid copolymer (SMA)-conjugated THP (SMA-THP conjugate). Cytotoxicities of free THP and SMA-THP conjugate against HeLa cells (a) and colon 26 cells (b) were measured by MTT assay. Values are means ± SEM. (c) Intracellular uptake of free THP and SMA-THP conjugate in HeLa cells. Values are means ± SEM (n = 3). (d) HPLC analyses of free THP at 6 h (d-i), SMA-THP conjugate at 10 h (d-ii), and 40 h (d-iii) in HeLa cells after each treatment.

Mentions: As shown in Figure3(a), SMA-THP conjugate showed dose-dependent cytotoxicity against HeLa cells with an IC50 of 22 μM. In contrast, free THP showed much potent cytotoxicity (IC50, 0.17 μM). Similar results were observed in colon 26 cells: the IC50 of free THP was 0.02 μM, compared to SMA-THP of 12.6 μM (Fig.3b). In both cell lines, cytotoxicity of SMA-THP conjugate was less than 1/100 compared with that of free THP.


Synthesis and therapeutic effect of styrene-maleic acid copolymer-conjugated pirarubicin.

Tsukigawa K, Liao L, Nakamura H, Fang J, Greish K, Otagiri M, Maeda H - Cancer Sci. (2015)

In vitro cytotoxicity and intracellular uptake of free pirarubicin (THP) and styrene–maleic acid copolymer (SMA)-conjugated THP (SMA-THP conjugate). Cytotoxicities of free THP and SMA-THP conjugate against HeLa cells (a) and colon 26 cells (b) were measured by MTT assay. Values are means ± SEM. (c) Intracellular uptake of free THP and SMA-THP conjugate in HeLa cells. Values are means ± SEM (n = 3). (d) HPLC analyses of free THP at 6 h (d-i), SMA-THP conjugate at 10 h (d-ii), and 40 h (d-iii) in HeLa cells after each treatment.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4376435&req=5

fig03: In vitro cytotoxicity and intracellular uptake of free pirarubicin (THP) and styrene–maleic acid copolymer (SMA)-conjugated THP (SMA-THP conjugate). Cytotoxicities of free THP and SMA-THP conjugate against HeLa cells (a) and colon 26 cells (b) were measured by MTT assay. Values are means ± SEM. (c) Intracellular uptake of free THP and SMA-THP conjugate in HeLa cells. Values are means ± SEM (n = 3). (d) HPLC analyses of free THP at 6 h (d-i), SMA-THP conjugate at 10 h (d-ii), and 40 h (d-iii) in HeLa cells after each treatment.
Mentions: As shown in Figure3(a), SMA-THP conjugate showed dose-dependent cytotoxicity against HeLa cells with an IC50 of 22 μM. In contrast, free THP showed much potent cytotoxicity (IC50, 0.17 μM). Similar results were observed in colon 26 cells: the IC50 of free THP was 0.02 μM, compared to SMA-THP of 12.6 μM (Fig.3b). In both cell lines, cytotoxicity of SMA-THP conjugate was less than 1/100 compared with that of free THP.

Bottom Line: Consequently, SMA-THP conjugate showed significantly prolonged circulation time compared to free THP and high tumor-targeting efficiency by the enhanced permeability and retention (EPR) effect.As a result, remarkable antitumor effect was achieved against two types of tumors in mice without apparent adverse effects.These findings suggest the potential of SMA-THP conjugate as a highly favorable candidate for anticancer nanomedicine with good stability and tumor-targeting properties in vivo.

View Article: PubMed Central - PubMed

Affiliation: Institute for Drug Delivery Science, Sojo University, Kumamoto, Japan; Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto, Japan.

Show MeSH
Related in: MedlinePlus