59887-91-1Relevant articles and documents
The Antiangiogenic Activity of Naturally Occurring and Synthetic Homoisoflavonoids from the Hyacinthaceae (sensu APGII)
Schwikkard, Sianne,Whitmore, Hannah,Sishtla, Kamakshi,Sulaiman, Rania S.,Shetty, Trupti,Basavarajappa, Halesha D.,Waller, Catherine,Alqahtani, Alaa,Frankemoelle, Lennart,Chapman, Andy,Crouch, Neil,Wetschnig, Wolfgang,Knirsch, Walter,Andriantiana, Jacky,Mas-Claret, Eduard,Langat, Moses K.,Mulholland, Dulcie,Corson, Timothy W.
, p. 1227 - 1239 (2019)
Excessive blood vessel formation in the eye is implicated in wet age-related macular degeneration, proliferative diabetic retinopathy, neovascular glaucoma, and retinopathy of prematurity, which are major causes of blindness. Small molecule antiangiogenic
The study on structure-activity relationship between chromone derivatives and inhibition of superoxide anion generating from human neutrophils
Chang, Yi-Han,Shu-Yen, Fang,Lai, Hsuan-Yu,Hwang, Tsong-Long,Hung, Hsin-Yi
supporting information, (2021/02/09)
Over activation of neutrophils has been linked to many inflammatory diseases; one of critical pathologic mechanisms is that generation and exocellular release of superoxide anion from neutrophils results in peripheral tissues damage. Besides, in this study, 2-(3,5-dimethoxyphenoxy)-5,7-dimethoxy-chromen-4-one (4), a 2-phexnoychromone from our compound bank, was demonstrated to have the moderate inhibitory effect on superoxide anion generating. Therefore, serial chromones substituted with phenols or 3-flourothiophenol were designed, synthesized, and examined for suppression of superoxide anion generation. In accordance with the results, the methoxy group at 7 position (R3) of the chromone, as well as a hydrogen bond donor at a meta site of the phenyl ring greatly impacted on the activity. 2-(3-fluorophenyl)sulfanyl-7-methoxy-chromen-4-one (16), a successful example of bioisosteres from a phenol to a thiophenol, exhibited prominent anti-inflammatory effects with the IC50 value against superoxide anion generation of 5.0 ± 1.4 μM.
Synthetic method for portulacanone D and anti-inflammatory pharmaceutical compounds containing thereof
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Paragraph 0073; 0074; 0076; 0078, (2019/10/08)
Inventors of the present invention synthesized natural homoisoflavonoid portulacanone D (compound 6) isolated from Portulaca oleracea L (POL). An ability to inhibit NO production in LPS-induced RAW 264.7 macrophages was assessed as an indicator of anti-inflammatory activity. The tested portulacanone D did not show clear cytotoxicity and inhibited NO production in the RAW 264.7 macrophages in a concentration dependent manner. The portulacanone D exhibits 92.5% of NO production inhibition at 10 andmu;M and has an IC50 value of 2.09 andmu;M. The finding has additional correlation with the suppressed expression of iNOS induced by LPS. According to the information obtained from the study of the present invention, the portulacanone D can be used in the development of anti-inflammatory drugs targeting NO production.COPYRIGHT KIPO 2019