PLGA- corosolic acid implants for potential application in ocular neovascularization diseases

Angiogenesis is the formation of new blood vessels from preexisting vasculature. Uncontrolled angiogenesis is associated with progression of several ocular pathologies, such as diabetic retinopathy and macular degeneration. Thus, the inhibition of this process consists in an interesting therapeutic target. Corosolic acid (CA) is a natural derivative of ursolic acid, found in many medicinal herbs and exhibits numerous biological properties, including the antiangiogenic activity. The present study reports the production of CA-loaded poly d,l-lactidecoglycolide acid (PLGA) devices by melt technique. HPLC-UV method was developed and validated to evaluate the uniformity and the release profile of the developed systems. The devices were also characterized by Fourier transform infrared spectroscopy, thermal analysis, and scanning electron morphology. It was studied the antiangiogenic activity of the CA-polymer system, using an in vivo model, the chorioallantoic membrane assay (CAM). CA was dispersed uniformly in the polymer matrix and no chemical interaction between the components of the formulation was verified. The implants presented a sustained release of the drug, which was confirmed by the morphological study and demonstrated an antiangiogenic activity. Therefore, the developed delivery system is a promising therapeutic tool for the treatment of ocular diseases associated with neovascularization or others related to the angiogenic process.

Study of antiangiogenic activity of “aqueous extract of Nigella sativa seeds” in chick chorioallantoic membrane (CAM) model

Background: Angiogenesis is important for the typical physiological activities such as cure from injury, menstrual cycle and embryo growth. It is also plays a crucial role in several pathological conditions in cancer. Antiangiogenesis, e.g., inhibition of blood vessel growth, is being investigated as a way to prevent the growth of tumors and other angiogenesis-dependent diseases. The chick embryo chorioallantoic membrane (CAM) is commonly used as an experimental in vivo assay to study both angiogenesis and antiangiogenesis in response to tissues, cells or soluble factors. Given the high occurrence of cancer worldwide and the major source of the discovery of new lead molecules are medicinal plants. The objective of the present research was to study the antiangiogenic property of “aqueous extract of Nigella sativa seeds” using chick chorioallantoic membrane (CAM) assayMethods: The chick chorioallantoic membrane (CAM) assay for screening the effect of Nigella sativa on anti-angiogenesis was performed according to the method given by Ribatti and co-workers.Results: The results of present study significantly increased the antiangiogenic effect on CAM by decreasing the proliferation of capillary networks in a dose (50 to 300 µg/egg) dependent manner which is probably related to the inhibition of neovascularization.Conclusions: It is concluded that aqueous extract of N. sativa seeds possesses significant antiangiogenic activity, and this is a possible rationale for its folkloric use as an anticancer agent.

Chemical constituents from roots of Campanumoea javanica and their antiangiogeneic activities / 中草药

Objective: To study the chemical constituents from the roots of Campanumoea javanica and their antiangiogenesis activities. Methods: The compounds were isolated and purified by various chromatographic techniques and their structures were elucidated by spectral analysis, the antiangiogenic activities of the isolated compounds were evaluated using a zebrafish model. Results: Fourteen compounds were isolated and identified from 90% ethanol extract in ethyl acetate fraction in the roots of C. javanica, including campanumoside (1), lobetyol (2), tetradeca-4E,8E,12E-triene-10-yne-1,6,7-triol (3), 9-(tetrahydropyran-2-yl)-non-trans- 8-ene-4,6-diyn-3-ol (4), 9-(tetrahydropyran-2-yl)-nona-trans,trans-2,8-diene-4,6-diyn-1-ol (5), lobetyolinin (6), (Z)-3-hexenyl-O- α-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside (7), 3,4-dihydroxybenzoic acid (8), tangshenoside II (9), zanthocapensol (10), ampelopsin (11), agathisflavone (12), β-ecdysterone (13), and α-tocopherolquinone (14). Conclusion: Compound 1 is a new polyacetylene glucoside named campanumoside. Compounds 2-14 are isolated from the plants of Campanumoea Bl. for the first time. Compounds 3 and 4 exhibit the certain antiangiogenic activity in the pharmacological evaluation with a zebrafish model.