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Antiangiogenic properties of Koetjapic acid, a natural triterpene isolated from Sandoricum koetjaoe Merr.

Nassar ZD, Aisha AF, Ahamed MB, Ismail Z, Abu-Salah KM, Alrokayan SA, Abdul Majid AM - Cancer Cell Int. (2011)

Bottom Line: Treatment with 10-50 μg/ml KA resulted in dose dependent inhibition of new blood vessels growth in ex vivo rat aortic ring assay.KA was found to be non-cytotoxic against HUVECs with IC50 40.97 ± 0.37 μg/ml.KA inhibited major angiogenesis process steps, endothelial cell migration and differentiation as well as VEGF expression.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Pulau Penang, Malaysia. aminmalikshah@gmail.com.

ABSTRACT

Background: Angiogenesis, the formation of new blood vessels, has become an important target in cancer therapy. Angiogenesis plays an important role in tumor growth and metastasis. Koetjapic acid (KA) is a seco-A-ring oleanene triterpene isolated from S. koetjape. The solvent extract of this plant species was shown previously to have strong antiangiogenic activity; however the active ingredient(s) that conferred the biological activity and the mode of action was not established. Given the high concentration of KA in S. koetjape, an attempt has been made in this study to investigate the antiangiogenic properties of KA.

Results: Treatment with 10-50 μg/ml KA resulted in dose dependent inhibition of new blood vessels growth in ex vivo rat aortic ring assay. KA was found to be non-cytotoxic against HUVECs with IC50 40.97 ± 0.37 μg/ml. KA inhibited major angiogenesis process steps, endothelial cell migration and differentiation as well as VEGF expression.

Conclusions: The non-cytotoxic compound, KA, may be a potent antiangiogenic agent; its activity may be attributed to inhibition of endothelial cells migration and differentiation as well VEGF suppression.

No MeSH data available.


Related in: MedlinePlus

Effects of KA on angiogenesis in rat aortic ring assay. Effect of KA on microvessels formation in rat aortic rings. Explants treated with (A) 1% ethanol (B) 10 μg/ml (C) 40 μg/ml and (D) 100 μg/ml suramin as a positive control (4X). (E) The Dose response relationship of KA on rat aorta assay. Data was represented as mean ± SD (n = 3). *P <0.05 and ***P <0.001.
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Figure 2: Effects of KA on angiogenesis in rat aortic ring assay. Effect of KA on microvessels formation in rat aortic rings. Explants treated with (A) 1% ethanol (B) 10 μg/ml (C) 40 μg/ml and (D) 100 μg/ml suramin as a positive control (4X). (E) The Dose response relationship of KA on rat aorta assay. Data was represented as mean ± SD (n = 3). *P <0.05 and ***P <0.001.

Mentions: The anti-angiogenic potential of KA was investigated firstly in the rat aortic model. Figure (2A) shows the microvessels outgrowth from the untreated aortic rings. On the contrary, aortic rings treated with KA exhibited reduced outgrowth with IC50 16.8 ± 1.7 μg/ml (Figure 2B and 2C). The anti-angiogenic effect on explants of rat aorta showed a significant dose dependent relationship (P < 0.05). At 20 μg/ml, KA inhibited vascularisation by 50% and doubling the dose to 40 μg/ml led to a complete inhibition of angiogenesis by 100%. Suramin, which was used as a positive control showed almost 100% inhibition of microvessels outgrowth at 100 μg/ml (Figure 2D).


Antiangiogenic properties of Koetjapic acid, a natural triterpene isolated from Sandoricum koetjaoe Merr.

Nassar ZD, Aisha AF, Ahamed MB, Ismail Z, Abu-Salah KM, Alrokayan SA, Abdul Majid AM - Cancer Cell Int. (2011)

Effects of KA on angiogenesis in rat aortic ring assay. Effect of KA on microvessels formation in rat aortic rings. Explants treated with (A) 1% ethanol (B) 10 μg/ml (C) 40 μg/ml and (D) 100 μg/ml suramin as a positive control (4X). (E) The Dose response relationship of KA on rat aorta assay. Data was represented as mean ± SD (n = 3). *P <0.05 and ***P <0.001.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3111336&req=5

Figure 2: Effects of KA on angiogenesis in rat aortic ring assay. Effect of KA on microvessels formation in rat aortic rings. Explants treated with (A) 1% ethanol (B) 10 μg/ml (C) 40 μg/ml and (D) 100 μg/ml suramin as a positive control (4X). (E) The Dose response relationship of KA on rat aorta assay. Data was represented as mean ± SD (n = 3). *P <0.05 and ***P <0.001.
Mentions: The anti-angiogenic potential of KA was investigated firstly in the rat aortic model. Figure (2A) shows the microvessels outgrowth from the untreated aortic rings. On the contrary, aortic rings treated with KA exhibited reduced outgrowth with IC50 16.8 ± 1.7 μg/ml (Figure 2B and 2C). The anti-angiogenic effect on explants of rat aorta showed a significant dose dependent relationship (P < 0.05). At 20 μg/ml, KA inhibited vascularisation by 50% and doubling the dose to 40 μg/ml led to a complete inhibition of angiogenesis by 100%. Suramin, which was used as a positive control showed almost 100% inhibition of microvessels outgrowth at 100 μg/ml (Figure 2D).

Bottom Line: Treatment with 10-50 μg/ml KA resulted in dose dependent inhibition of new blood vessels growth in ex vivo rat aortic ring assay.KA was found to be non-cytotoxic against HUVECs with IC50 40.97 ± 0.37 μg/ml.KA inhibited major angiogenesis process steps, endothelial cell migration and differentiation as well as VEGF expression.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Pulau Penang, Malaysia. aminmalikshah@gmail.com.

ABSTRACT

Background: Angiogenesis, the formation of new blood vessels, has become an important target in cancer therapy. Angiogenesis plays an important role in tumor growth and metastasis. Koetjapic acid (KA) is a seco-A-ring oleanene triterpene isolated from S. koetjape. The solvent extract of this plant species was shown previously to have strong antiangiogenic activity; however the active ingredient(s) that conferred the biological activity and the mode of action was not established. Given the high concentration of KA in S. koetjape, an attempt has been made in this study to investigate the antiangiogenic properties of KA.

Results: Treatment with 10-50 μg/ml KA resulted in dose dependent inhibition of new blood vessels growth in ex vivo rat aortic ring assay. KA was found to be non-cytotoxic against HUVECs with IC50 40.97 ± 0.37 μg/ml. KA inhibited major angiogenesis process steps, endothelial cell migration and differentiation as well as VEGF expression.

Conclusions: The non-cytotoxic compound, KA, may be a potent antiangiogenic agent; its activity may be attributed to inhibition of endothelial cells migration and differentiation as well VEGF suppression.

No MeSH data available.


Related in: MedlinePlus