Tissue distribution of 2-methoxyestradiol nanosuspension in rats and its antitumor activity in C57BL/6 mice bearing lewis lung carcinoma

Figures & data

Figure 1.  Chemical structure of 2-methoxyestradiol.

Table 1.  Overall targeting efficiency of 2-ME in tissues after i.v. administration of 2-ME nanosuspension and 2-ME solution to rats (mean ± SD, n = 5).

Tissue	TE^Q (%)		TE^QN/TE^QS
	2-ME-N	2-ME-S
Heart	1.54 ± 0.11	4.51 ± 1.10	0.34
Liver	43.27 ± 3.21	51.86 ± 3.82	0.83
Spleen	0.61 ± 0.04	2.02 ± 0.27	0.30
Lung	51.95 ± 4.11	28.71 ± 2.13	1.81
Kidney	0.71 ± 0.10	3.06 ± 0.54	0.23
Brain	1.91 ± 0.23	9.83 ± 1.58	0.19

2-ME, 2-methoxyestradiol; TE^Q: overall targeting efficiency.

Figure 2.  The distribution of 2-ME in rats tissues at different time points after iv. administration of 2-ME solution (A) and 2-ME nanosuspension (B) (mean ± SD, n = 5).

Figure 3.  MTT assay showing that 2-ME nanosuspension and 2-ME solution treatment inhibit growth of LLC cells in a time- and dose-dependent manner. Results are expressed as mean ± SD (n = 6). ^#p < 0.05 vs. control group. *p < 0.05 vs. 2-ME solution group. **p < 0.01 vs. 2-ME solution group.

Table 2.  Inhibition effect of 2-ME nanosuspension on tumors weight (mean ± SD, n = 6).

Groups	Inhibition rate of weight
	Dose/mg·kg^−1	Weight/g	Inhibition (%)
Control group	–	1.76 ± 0.21
Cyclophosphamide group	30.0	0.92 ± 0.23*	47.72
2-ME solution	30.0	1.00 ± 0.21*	43.18
2-ME nanosuspension	15.0	0.91 ± 0.13*	48.29
	30.0	0.78 ± 0.21*^,#,**	55.68
	60.0	0.70 ± 0.11*^,##	60.23

*p < 0.01 vs. negative control group.

^#p < 0.05 vs. cyclophosphamide group.

**p < 0.05 vs. 2-ME solution group.

^##p < 0.01 vs. 2-ME solution group.

2-ME, 2-methoxyestradiol.

Figure 4.  The growth curve of solid tumors.

Table 3.  Effects of 2-ME nanosuspensions on organ index of lewis tumour bearing mice (mean ± SD, n = 6).

Groups	Dose (mg·kg^−1)	Heart index(mg·g^−1)	Liver index (mg·g^−1)	Spleen index (mg·g^−1)	Lung index (mg·g^−1)	Kidney index (mg·g^−1)
Control	–	5.53 ± 0.94	64.75 ± 3.07	5.64 ± 0.96	6.64 ± 0.95	13.53 ± 2.23
Cyclophos-phamide	30	6.48 ± 0.24	60.52 ± 5.11	3.33 ± 0.77*	7.29 ± 0.47	12.70 ± 1.26
2-ME-S	30	6.18 ± 0.50	67.63 ± 7.56	5.38 ± 1.30^#	7.16 ± 0.88	13.45 ± 2.40
2-ME-N	30	6.21 ± 0.55	72.25 ± 4.82*^,#	5.75 ± 0.71^##	7.26 ± 1.15	13.57 ± 0.82

*p < 0.05 vs. negative control group.

^#p < 0.05 vs. cyclophosphamide group.

^##p < 0.01 vs. cyclophosphamide group.

2-ME, 2-methoxyestradiol.