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| As a proof of concept,a non-polar amino acid (valine) was attached to the C20position of SN38 via an ester bond to generate Val-SN38 (Fig. 6B). The exact solubility of the Val-SN38 in lipids was not reported. It was categorised as a lipophilic prodrug given the non-polarity of the attached valine moiety. Val-SN38 improved intracellular accumulation in MCF7 cells by more than 5-fold in comparison to SN38, without inducing significant multiple-drug resistance. Improved accumulation of ValSN38 has been suggested to be due to augmented uptakeviavarious amino acid transporters. The prodrug, however, showed poor stability and readily converted to the inactive carboxylate form in PBS, MCF 7 cell lines and plasma. Further optimisation of the prodrug to better control the conversion rate to the carboxylate form may result in more potent prodrugs. Alternatively, the prodrug may be incorporated into lipid-based formulations to stabilise the lactone form. |
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gundnir: 金币+50, 翻译EPI+1 2014-02-26 01:07:11
gundnir: 金币+50, 翻译EPI+1 2014-02-26 01:07:11
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As a proof of concept, a non-polar amino acid (valine) was attached to the C20position of SN38 via an ester bond to generate Val-SN38 (Fig. 6B). The exact solubility of the Val-SN38 in lipids was not reported. It was categorised as a lipophilic prodrug given the non-polarity of the attached valine moiety. 作为一个概念验证,非极性氨基酸(缬氨酸) 通过酯键附加成至SN38的C20位置生成Val-SN38(图6 b)，Val-SN38在脂质的溶解度未被报道。这种归类为亲脂性的药物前体的具有非极性加成缬氨酸的成分。 Val-SN38 improved intracellular accumulation in MCF7 cells by more than 5-fold in comparison to SN38, without inducing significant multiple-drug resistance. Improved accumulation of Val-SN38 has been suggested to be due to augmented uptake via various amino acid transporters. 与SN38相比，Val-SN38 在MCF7细胞胞内积累提高了5倍以上，没有引起显著的多药耐药性。Val-SN38的改进积累一直被猜想是由于氨基酸转运蛋白的吸收增强。 The prodrug, however, showed poor stability and readily converted to the inactive carboxylate form in PBS, MCF 7 cell lines and plasma. Further optimisation of the prodrug to better control the conversion rate to the carboxylate form may result in more potent prodrugs. 然而,该前体药物表现为稳定性差，在PBS,MCF 7细胞系和细胞质中容易转化为不活跃的羧酸盐形式。前体药物的进一步优化,以更好地控制羧酸盐形式转化率可能导致更高活性化合物。 Alternatively, the prodrug may be incorporated into lipid-based formulations to stabilise the lactone form. 另外,前体药物可能以稳定的内酯形式被纳入基于脂质的制剂。 作为一个概念验证，非极性氨基酸(缬氨酸) 通过酯键附加成至SN38的C20位置生成Val-SN38(图6 b)，Val-SN38的脂溶度未被报道。这种归类为亲脂性的药物前体的具有非极性加成缬氨酸的成分。与SN38相比，Val-SN38 在MCF7细胞胞内积累提高了5倍以上，没有引起显著的多药耐药性。Val-SN38的改进积累一直被猜想是由于氨基酸转运蛋白的吸收增强。然而，该前体药物表现为稳定性差，在PBS、MCF 7细胞系和细胞质中容易转化为不活跃的羧酸盐形式。随着前体药物的进一步优化，以更好地控制羧酸盐的转化率可能导致更高活性化合物。另外，前体药物可能以稳定的内酯形式被纳入基于脂质的制剂。 |
2楼2014-02-25 22:31:40