To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

To study the anticancer activity of FA-P7-PTX in vivo, we performed tumor-bearing mice model with H22cells by administering once every two days peritumoral injection of FA-P7-PTX (12 μmol/kg), PTX (12 μmol/kg, as the positive control), or 0.9% saline as the negative control for 2 weeks. Compared with control group, the tumor volumes of the FA-P7-PTX group were dramatically reduced by 69% with no significant variation in mouse body weight. Meanwhile FA-P7-PTX exhibited stronger inhibitory effects on tumor volume compared with PTX (69% versus 49%). The result confirmed that FA-P7-PTX possessed higher potency in slowing the growth of solid tumors.

The anticancer activities of the conjugates were evaluated using various cancer cells (MCF-7, MCF-7/PTX, K562, A2780 and SKOV3). The IC50 values are listed in Table 3, and PTX was used for comparison. All the conjugates exhibited improved cytotoxic effects on various cancer cells. According to the results, all the conjugates showed significantly stronger antiproliferative activity than former lytic peptides (P3 and P7), and FA-P3-PTX and FA-P7-PTX showed more excellent antiproliferative activity than P3-PTX and P7-PTX in FA-overexpressing cancer cells MCF-7 (1.79 μM versus 2.15 μM; 1.39 μM versus 1.98 μM), MCF-7/PTX (4.54 μM versus 6.11 μM; 2.92 μM versus 5.53 μM), A2780 (1.95 μM versus 2.69 μM; 1.42 μM versus 2.79 μM), respectively. Thus, the conjugate FA-P3-PTX and FA-P7-PTX exhibited great antiproliferative activity on folate receptors overexpressing cancer cells, and almost equal potency to both drug resistant and -sensitive cells. Meanwhile, the conjugates showed weak toxicity to the normal cell lines HUVEC. To assess the safety profile of the designed conjugates, we examined their hemolytic activity using RBCs. As depicted in Fig. 1, all the tested peptides exhibited modest hemolytic activity.

The anticancer activities of the conjugates were evaluated using various cancer cells (MCF-7, MCF-7/PTX, K562, A2780 and SKOV3). The IC50 values are listed in Table 3, and PTX was used for comparison. All the conjugates exhibited improved cytotoxic effects on various cancer cells. According to the results, all the conjugates showed significantly stronger antiproliferative activity than former lytic peptides (P3 and P7), and FA-P3-PTX and FA-P7-PTX showed more excellent antiproliferative activity than P3-PTX and P7-PTX in FA-overexpressing cancer cells MCF-7 (1.79 μM versus 2.15 μM; 1.39 μM versus 1.98 μM), MCF-7/PTX (4.54 μM versus 6.11 μM; 2.92 μM versus 5.53 μM), A2780 (1.95 μM versus 2.69 μM; 1.42 μM versus 2.79 μM), respectively. Thus, the conjugate FA-P3-PTX and FA-P7-PTX exhibited great antiproliferative activity on folate receptors overexpressing cancer cells, and almost equal potency to both drug resistant and -sensitive cells. Meanwhile, the conjugates showed weak toxicity to the normal cell lines HUVEC. To assess the safety profile of the designed conjugates, we examined their hemolytic activity using RBCs. As depicted in Fig. 1, all the tested peptides exhibited modest hemolytic activity.

The anticancer activities of the conjugates were evaluated using various cancer cells (MCF-7, MCF-7/PTX, K562, A2780 and SKOV3). The IC50 values are listed in Table 3, and PTX was used for comparison. All the conjugates exhibited improved cytotoxic effects on various cancer cells. According to the results, all the conjugates showed significantly stronger antiproliferative activity than former lytic peptides (P3 and P7), and FA-P3-PTX and FA-P7-PTX showed more excellent antiproliferative activity than P3-PTX and P7-PTX in FA-overexpressing cancer cells MCF-7 (1.79 μM versus 2.15 μM; 1.39 μM versus 1.98 μM), MCF-7/PTX (4.54 μM versus 6.11 μM; 2.92 μM versus 5.53 μM), A2780 (1.95 μM versus 2.69 μM; 1.42 μM versus 2.79 μM), respectively. Thus, the conjugate FA-P3-PTX and FA-P7-PTX exhibited great antiproliferative activity on folate receptors overexpressing cancer cells, and almost equal potency to both drug resistant and -sensitive cells. Meanwhile, the conjugates showed weak toxicity to the normal cell lines HUVEC. To assess the safety profile of the designed conjugates, we examined their hemolytic activity using RBCs. As depicted in Fig. 1, all the tested peptides exhibited modest hemolytic activity.

The anticancer activities of the conjugates were evaluated using various cancer cells (MCF-7, MCF-7/PTX, K562, A2780 and SKOV3). The IC50 values are listed in Table 3, and PTX was used for comparison. All the conjugates exhibited improved cytotoxic effects on various cancer cells. According to the results, all the conjugates showed significantly stronger antiproliferative activity than former lytic peptides (P3 and P7), and FA-P3-PTX and FA-P7-PTX showed more excellent antiproliferative activity than P3-PTX and P7-PTX in FA-overexpressing cancer cells MCF-7 (1.79 μM versus 2.15 μM; 1.39 μM versus 1.98 μM), MCF-7/PTX (4.54 μM versus 6.11 μM; 2.92 μM versus 5.53 μM), A2780 (1.95 μM versus 2.69 μM; 1.42 μM versus 2.79 μM), respectively. Thus, the conjugate FA-P3-PTX and FA-P7-PTX exhibited great antiproliferative activity on folate receptors overexpressing cancer cells, and almost equal potency to both drug resistant and -sensitive cells. Meanwhile, the conjugates showed weak toxicity to the normal cell lines HUVEC. To assess the safety profile of the designed conjugates, we examined their hemolytic activity using RBCs. As depicted in Fig. 1, all the tested peptides exhibited modest hemolytic activity.

The anticancer activities of the conjugates were evaluated using various cancer cells (MCF-7, MCF-7/PTX, K562, A2780 and SKOV3). The IC50 values are listed in Table 3, and PTX was used for comparison. All the conjugates exhibited improved cytotoxic effects on various cancer cells. According to the results, all the conjugates showed significantly stronger antiproliferative activity than former lytic peptides (P3 and P7), and FA-P3-PTX and FA-P7-PTX showed more excellent antiproliferative activity than P3-PTX and P7-PTX in FA-overexpressing cancer cells MCF-7 (1.79 μM versus 2.15 μM; 1.39 μM versus 1.98 μM), MCF-7/PTX (4.54 μM versus 6.11 μM; 2.92 μM versus 5.53 μM), A2780 (1.95 μM versus 2.69 μM; 1.42 μM versus 2.79 μM), respectively. Thus, the conjugate FA-P3-PTX and FA-P7-PTX exhibited great antiproliferative activity on folate receptors overexpressing cancer cells, and almost equal potency to both drug resistant and -sensitive cells. Meanwhile, the conjugates showed weak toxicity to the normal cell lines HUVEC. To assess the safety profile of the designed conjugates, we examined their hemolytic activity using RBCs. As depicted in Fig. 1, all the tested peptides exhibited modest hemolytic activity.

The anticancer activities of the conjugates were evaluated using various cancer cells (MCF-7, MCF-7/PTX, K562, A2780 and SKOV3). The IC50 values are listed in Table 3, and PTX was used for comparison. All the conjugates exhibited improved cytotoxic effects on various cancer cells. According to the results, all the conjugates showed significantly stronger antiproliferative activity than former lytic peptides (P3 and P7), and FA-P3-PTX and FA-P7-PTX showed more excellent antiproliferative activity than P3-PTX and P7-PTX in FA-overexpressing cancer cells MCF-7 (1.79 μM versus 2.15 μM; 1.39 μM versus 1.98 μM), MCF-7/PTX (4.54 μM versus 6.11 μM; 2.92 μM versus 5.53 μM), A2780 (1.95 μM versus 2.69 μM; 1.42 μM versus 2.79 μM), respectively. Thus, the conjugate FA-P3-PTX and FA-P7-PTX exhibited great antiproliferative activity on folate receptors overexpressing cancer cells, and almost equal potency to both drug resistant and -sensitive cells. Meanwhile, the conjugates showed weak toxicity to the normal cell lines HUVEC. To assess the safety profile of the designed conjugates, we examined their hemolytic activity using RBCs. As depicted in Fig. 1, all the tested peptides exhibited modest hemolytic activity.