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Anti-proliferation and anti-angiogenesis of curcumin-K30 solid dispersion
Chun Chen1, Xiuwang Huang, Huajing Cai
1Department of Pharmacology, College of Pharmacy, Fujian Medical University, Fuzhou 350004, China.
Objective:
To evaluate the anti-proliferation and anti-angiogenesis effect of curcumin-K30 solid dispersion (Cur-K30) on tumors in vivo.
Methods:
Growth inhibition rates of the tumor cells was measured with MTT method. Tumor inhibition was detected by tumors transplanted subcutaneously in mice treated with Cur-K30 [50, 100, and 200 mg/(kg · d)]. The expressions of CD34 and vascular endothelial growth factor (VEGF) were assessed by immunohistochemical study, and analyzed by Imageproplus software.
Results:
Cur-K30 had inhibitory effect on different tumor cell lines in a dose dependent manner with IC₅₀ values from 6.6 to 12.12 μg/mL. The in vivo study showed that the inhibitory rates of the 200 mg/(kg · d) Cur-K30 group on H22, B16, and SW480 were 43.2%, 53.1%, and 59.8%, respectively, which were all much higher than the inhibitory rates of curcumin suspension group with the same dose. Compared with the control group, the expression of CD34 and VEGF in SW480 tumors was down-regulated in the 200 mg/(kg · d) Cur-K30 group (P <0.01).
Conclusion:
The proliferation inhibition of Cur-K30 is higher than curcumin in vivo, and the most significant effect is obtained in SW480 tumors transplanted subcutaneously in nude mice. Down-regulation of VEGF and decreased microvascular density may contribute to the anti-tumor effect of Cur-K30.
Insights
Curcumin-K30 solid dispersion significantly inhibits tumor growth and angiogenesis in vivo, outperforming traditional curcumin. This novel formulation shows potent anti-tumor effects, particularly in SW480 tumors, by down-regulating VEGF.
Area of Science:
- Pharmacology
- Oncology
- Biotechnology
Background:
- Curcumin exhibits anti-cancer properties but suffers from poor bioavailability.
- Curcumin-K30 solid dispersion (Cur-K30) is a novel formulation designed to enhance curcumin's therapeutic potential.
- Solid dispersion technology can improve drug solubility and absorption.
Purpose of the Study:
- To evaluate the anti-proliferation and anti-angiogenesis effects of Cur-K30 in preclinical tumor models.
- To compare the efficacy of Cur-K30 with standard curcumin suspension in vivo.
- To investigate the molecular mechanisms underlying Cur-K30's anti-tumor activity.
Main Methods:
- In vitro cytotoxicity assessed using MTT assay.
- In vivo anti-tumor efficacy evaluated in mice bearing subcutaneous tumors (H22, B16, SW480) treated with varying doses of Cur-K30.
- Immunohistochemical analysis of CD34 and vascular endothelial growth factor (VEGF) expression in tumor tissues.
Main Results:
- Cur-K30 demonstrated dose-dependent inhibition of tumor cell lines with IC50 values ranging from 6.6 to 12.12 μg/mL.
- In vivo, Cur-K30 at 200 mg/(kg·d) achieved significant tumor inhibition rates (43.2% for H22, 53.1% for B16, 59.8% for SW480), exceeding those of curcumin suspension.
- Cur-K30 treatment led to significant down-regulation of CD34 and VEGF expression in SW480 tumors (P <0.01).
Conclusions:
- Cur-K30 exhibits superior anti-proliferative activity compared to curcumin in vivo.
- The enhanced anti-tumor effect of Cur-K30, particularly in SW480 tumors, is associated with the down-regulation of VEGF and reduced microvascular density.
- Cur-K30 represents a promising therapeutic strategy for cancer treatment due to its improved efficacy and anti-angiogenic properties.
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