Abstract
Crocetin and crocin are two important carotenoids isolated from saffron (Crocus sativus L.), which have been used as natural biomedicines with beneficial effects for improving the suboptimal health status associated with abnormal angiogenesis. However, the anti-angiogenic effects and underlying mechanisms of the effects of crocetin and crocin have not been investigated and compared. The anti-angiogenic effects of crocetin and crocin were tested on human umbilical vein endothelial cells (HUVECs) in vitro, and in zebrafish in vivo. In vivo, crocetin (20 μM) and crocin (50 and 100 μM) significantly inhibited subintestinal vein vessels formation, and a conversion process between them existed in zebrafish, resulting in a difference in their effective concentrations. In the HUVEC model, crocetin (10, 20 and 40 μM) and crocin (100, 200 and 400 μM) inhibited cell migration and tube formation, and inhibited the phosphorylation of VEGFR2 and its downstream pathway molecules. In silico analysis further showed that crocetin had a higher ability to bind with VEGFR2 than crocin. These results suggested that crocetin was more effective than crocin in inhibiting angiogenesis through regulation of the VEGF/VEGFR2 signaling pathway. These compounds, especially crocetin, are potential candidate natural biomedicines for the management of diseases associated with abnormal blood vessel growth, such as age-related macular degeneration.
Highlights
IntroductionCrocetin and crocin ( known as crocin-I or α-crocin) are two important carotenoids isolated from the dried stigma of the flowers of Crocus sativus L. (saffron)
Crocetin and crocin are two important carotenoids isolated from the dried stigma of the flowers of Crocus sativus L
Quantification of the total area of subintestinal vessels (SIVs) showed that both crocetin and crocin significantly reduced the formation of SIVs in a concentrationdependent manner, and the maximal effects were comparable to VEGFR tyrosine kinase inhibitor II (VRI), a strong VEGF receptor (VEGFR) inhibitor that greatly inhibits SIVs angiogenesis (Li et al, 2014)
Summary
Crocetin and crocin ( known as crocin-I or α-crocin) are two important carotenoids isolated from the dried stigma of the flowers of Crocus sativus L. (saffron). Crocetin is a lipophilic carotenoid and crocin is the hydrophilic diester of crocetin with gentiobiose (Figure 1) Both compounds have been shown to exhibit a number of biological properties, such as anti-oxidative, antiinflammatory, anti-lipidemic and anti-tumor activities, and have potential health benefits by modifying different disease processes, including in cardiovascular diseases, metabolic syndromes, ocular disorders and cancer (Alavizadeh and Hosseinzadeh, 2014; Bukhari et al, 2018; Hashemi and Hosseinzadeh, 2019). In comparison to their anti-hypoxic and anti-tumor effects, only a few previous studies have investigated the effects of crocetin and crocin on angiogenesis. It is not clear whether crocetin and crocin can inhibit endothelial cell motility or sprouting angiogenesis, nor the difference between them in these respects
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