Osthole: A Traditional Chinese Medicine for Ocular Anti-Angiogenic Therapy

Abstract

Osthole is an agent isolated from Cnidium monnieri (L.) Cusson and has been used to treat several disorders. Corneal neovascularization is a sight-threatening condition associated with several inflammatory or infectious ocular disorders. In this study, we investigated the anti-angiogenic effects of osthole on corneal neovascularization and the underlying mechanism. Methods: MTT assay, HE staining, and calcein-AM/propidium iodide staining was conducted to detect the toxicity of osthole in vitro and in vivo. Corneal neovascularization of ICR mice was induced by alkali burn and observed by a slit lamp microscopy on day 7 after alkali injury. EdU assay, Ki67 immunofluorescence assay, Transwell migration assay, and Matrigel assay were conducted to investigate the role of osthole in endothelial angiogenic effects in vitro. Western blots were conducted to investigate the anti-angiogenic mechanism of osthole in corneal neovascularization. Results: Administration of osthole ranging from 0.05 to 25 µM had no detectable cytotoxicity or tissue toxicity in vivo and in vitro. Topical administration of osthole inhibited corneal neovascularization induced by alkali burn. Osthole decreased the proliferation, migration, and tubeformation of endothelial cells induced by VEGF. Osthole inhibited endothelial angiogenic functions through blocking the phosphorylation of ERK1/2, JNK, and p38. Conclusion: Our study provides evidence that osthole is a promising drug for the treatment of corneal neovascularization.

Clinical Effect of Tongmai Fuming Decoction on Neovascular Ophthalmopathy

“…e treatment is based on tonifying the liver and kidney, accompanied by removing the blood stasis and clearing collaterals, thus reducing the production of pathological VEGF [25][26][27][28][29]. Contemporary pharmacological studies show that part of traditional Chinese medicine for supplementing the liver and kidneys has antioxidation, stabilizes the blood-eye barrier, and has sex hormone-like effects [30][31][32][33][34]. In the clinical treatment of eye disease with the liver and kidney Yin syndrome, the use of Western medicine can be reduced to a certain extent by considering the combination of traditional Chinese and Western medicine.…”

The Effect of Osthole on Transient Receptor Potential Channels: A Possible Alternative Therapy for Atopic Dermatitis

“…Osthole (OST) (7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one) is a natural coumarin and a major chemical constituent of the plant Cnidium monnieri (L) Cusson and is considered a promising natural product that could be used pharmacologically in the future. These include anti-cancer [24][25][26] anti-inflammatory, [27][28][29][30] antioxidant, 31 anti-angiogenic, 32 anti-allergic 27,33,34 immunomodulatory 33,35 and hepatoprotective [36][37][38] activities. In our previous publications, we found that OST is immunosuppressive in peripheral blood mononuclear cells (PBMCs) isolated from children with allergies or asthma 27,30,[39][40][41][42][43] and autism spectrum disorders (ASD), in keratinocytes and fibroblast cell lines 28, and in a 3D skin model.…”

UPLC-Q-TOF/MS-Based Metabolomics Approach Reveals Osthole Intervention in Breast Cancer 4T1 Cells

“…Osthole (OST), also known as methoxyparsleyol, was the first coumarin derivative obtained from medicinal plant Cnidium monnieri (L.) Cusson ( Figure 1 ) [ 12 , 13 ]. OST has anti-cancer effects against many types of cancer such as breast cancer, hepatocellular carcinoma, and kidney cancer [ 14 ].…”