In vitro and in vivo anticancer properties of cucurbitacin isolated from Cayaponia racemosa

Figures & data

Figure 1.  A – Chemical structure of 2β,3β,16α,20(R),25-pentahydroxy-22-oxocucurbita-5-en (1) isolated from Cayaponia racemosa. B – Activity of compound 1 and at 2.5 and 5.0 µg/mL on HL60 cells assessed by Trypan blue exclusion. C – Effect of cucurbitacin on the pattern of HL60 cell death, determined by acridine orange and ethidium bromide staining (AO/BE). Negative controls (C) were treated with solvent (DMSO); positive controls (+) were treated with doxorubicin (0.3 µg/mL). The cells were treated for 24 h. *p < 0.05 compared with controls by ANOVA followed by Student Newman–Keuls test.

Figure 2.  Cucurbitacin 1 induced morphological changes in HL-60 leukemia cells. A – Control cells; B – Cells treated with doxorubicin at 0.3 µg/mL; C and D – Cells treated with compound 1 at 2.5 and 5.0 µg/mL. Black arrows – nuclear fragments showing a periphery of compacted chromatin.

Figure 3.  Tumor mass of mice transplanted with Sarcoma 180 cells after 7 days of treatment by intraperitoneal route with compound 1 (2β,3β,16α,20(R),25-pentahydroxy-22-oxocucurbita-5-en) isolated from Cayaponia racemosa and in association with 5-fluorouracil (5-FU, positive control). Negative control (C) received only DMSO 4%. Data are expressed as mean ± SEM (n = 10 animals/group). Within the square is demonstrated the tumor inhibition capacity expressed as perceptual in comparison with the negative control. *p < 0.01 compared to control by ANOVA followed by Newman–Keuls test.

Figure 4.  Histopathology of tumors excised from Sarcoma 180 transplanted mice after 7 days of intraperitoneal treatment with compound 1 (2β,3β,16α,20(R),25-pentahydroxy-22-oxocucurbita-5-en) isolated from Cayaponia racemosa. A – Negative control (DMSO 4%), B and C – 5-Fluorouracil 10 and 25 mg/kg/day, D and E – Compound 1, 10 and 25 mg/kg/day, F – 5-Fluorouracil + Compound 1 (10 + 10 mg/kg/day), respectively. Magnification, 400×.

Table 1.  Body effects of compound 1 (2β,3β,16α,20(R),25-pentahydroxy-22-oxocucurbita-5-en) isolated from Cayaponia racemosa on mice transplanted with Sarcoma 180 cells.

Treatment	Dose (mg/kg/day)	Animal weight (g)	Liver	Kidneys	Spleen
			g/100 g body weight
Control	-	34.7 ± 0.7	5.29 ± 0.11	1.39 ± 0.04	0.54 ± 0.03
5-FU	10	33.1 ± 0.7	5.29 ± 0.17	1.41 ± 0.05	0.49 ± 0.03
	25	24.6 ± 0.4*	4.86 ± 0.27	1.28 ± 0.03	0.22 ± 0.01*
Compound 1	10	32.3 ± 1.2	5.56 ± 0.16	1.44 ± 0.06	0.70 ± 0.04*
	25	33.0 ± 1.1	5.41 ± 0.10	1.58 ± 0.04	0.84 ± 0.03*
Compound 1 + 5-FU	10 + 10	30.0 ± 0.9*,**	5.64 ± 0.24	1.54 ± 0.04	0.64 ± 0.03*,**

Data are means ± SEM, n = 10 animals/group, treated for 7 days by intraperitoneal route. Negative control received DMSO 4%.

*p < 0.01 compared to control by ANOVA followed by Newman–Keuls test.

**p < 0.01 compared to 5-FU by ANOVA followed by Newman–Keuls test.

Figure 5.  Histopathology of spleens excised from Sarcoma 180 transplanted mice after 7 days of intraperitoneal treatment with compound 1 (2β,3β,16α,20(R),25-pentahydroxy-22-oxocucurbita-5-en) isolated from Cayaponia racemosa. A – Negative control (DMSO 4%), B and C – 5-Fluorouracil 10 and 25 mg/kg/day, D and E – Compound 1, 10 and 25 mg/kg/day, F – 5-Fluorouracil + Compound 1 (10 + 10 mg/kg/day), respectively. Magnification, 400×.