期刊
NATURAL PRODUCT RESEARCH
卷 37, 期 16, 页码 2795-2800出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2022.2132499
关键词
Arnebia euchroma (Royle; ) Johnst; Boraginaceae; xanthine oxidase inhibitor; NMR analysis; mass analysis; uric acid
This study investigates the XO inhibitory potential of biologically active Alkannin/Shikonin (A/S) derivatives and confirms their efficacy through in vitro experiments and pharmacophore hypothesis.
Induction of hypersensitivity reactions (may be fatal too) by specific XO inhibitors has led to development of new molecules that are efficacious and have safer ADME profile. Among natural compounds, biologically active Alkannin/Shikonin (A/S) derivatives have unexplored XO inhibition potential. Therefore, their iso-hexenylnaphthazarin nucleus was studied and found that the nucleus is similar to that of allopurinol, signifying the XO inhibitory potential of these derivatives. For confirmation of their potential, beta,beta-dimethylacrylshikonin and deoxyshikonin were successfully isolated and characterised from Arnebia euchroma (Royle.) Johnst. (Boraginaceae) and were evaluated for in vitro XO inhibitory potential. beta,beta-dimethylacrylshikonin and deoxyshikonin showed a good XO inhibition potential with IC50 values of 7.475 +/- 1.46 mu g/mL and 4.487 +/- 0.88 mu g/mL, respectively. Results also validated the pharmacophore hypothesis, and it was concluded that nucleus iso-hexenylnaphthazarin can be remodelled for optimising the efficacy.
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