UFLC-MS-IT-TOF and Bioassay Guided Isolation of Flavonoids as Xanthine Oxidase Inhibitors from Diospyros dumetorum

• Published in: Natural product communications 2017-11, Vol.12 (11)
• Main Authors: Deng, Zhen-Tao, Yang, Tong-Hua, Huang, Xiao-Yan, Chen, Xing-Long, Zhang, Jian-Gang, Zhang, Xue-Mei, Chen, Ji-Jun, Geng, Chang-An
• Format: Article
• Language: English
• ISSN: 1934-578X; 1555-9475
• DOI: 10.1177/1934578X1701201113

Diospyros dumetorum is an important folk medicine for treating pulmonary abscess and inflammation. The leaves of D. dumetorum revealed xanthine oxidase (XOD) inhibitory activity. With the guidance of UFLC-MS-IT-TOF analyses combined with bioassay in vitro, 15 flavonoids were isolated from the active parts of D. dumetorum. Except for 11 (IC50 > 200μM), all compounds showed obvious XOD inhibitory activity with IC50 values of 32.5 ± 0.7 ~ 145.0 ± 3.3 μM. The preliminary structure-activity relationships study suggested that glycosylation on C-3 was unfavorable for XOD inhibitory activity; hydroxyl groups on ring B were essential for maintaining activity; the activity was closely related with the position of galloylation. This is the first recognition of the XOD inhibitory activity and active constituents of D. dumetorum, and will provide valuable information for this plant as a new resource for treating hyperuricemia and gout.