ChemInform Abstract: Antiinflammatory Components of Euphorbia humifusa Willd.

Luyen, Bui Thi Thuy; Tài, Bùi Hữu; Thảo, Nguyễn Phương; Eun, Kim Ji; Yun, Ji; Xin, Ming Jie; Lee, Young Mi

doi:10.1002/chin.201438217

Cited by 2 publications

(3 citation statements)

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“…Similarly, the antiinflammatory activity of EHNB was assessed the best, even Frontiers in Pharmacology frontiersin.org when compared to the NSAID indomethacin. Therefore, our finding enhances prior discoveries demonstrating the antiinflammatory of this species through inhibition of soluble epoxide hydrolase (SEH), lipopolysaccharide (LPS)-induced nitric oxide and the tumor necrosis factors (TNF) productions (Luyen et al, 2014). Interestingly, the antioxidant evaluations via DPPH, ABTS and FRAP assays showed the highest potentialities of the EHNB fraction.…”

Section: Potential Ligands Activities Validationssupporting

confidence: 74%

Exploring potential antidiabetic and anti-inflammatory flavonoids from Euphorbia humifusa with an integrated strategy

Fan

Chen

2022

Front. Pharmacol.

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E. humifusa Willd, a monoecious annual plant, native to Eastern Asia, has been traditionally attributed to the treatment and prevention of miscellaneous diseases, including diabetes mellitus and its associated complications. Earlier studies have supported this species’ pharmacological efficacies including its antibacterial, antidiabetic, and anti-inflammatory properties. Even so, the underlying bioactive components with their mechanisms of action associated with its antidiabetic and anti-inflammatory effects remain elusive. The preamble in vitro assessments of the crude extract and its different fractions revealed that the n-butanol fraction (EHNB) exhibited the best activity, which was subsequently subjected to a rapid screening of candidate ligands through bio-affinity ultrafiltration with the two enzyme targets: α-glucosidase (α-Glu) and cycloxygenase-2 (COX-2) combined with UPLC/QTOF-MS. As a result, 7 compounds were identified from EHNB, among them, vitexin and astragalin were screened out as the most active ligand compounds. Vitexin showed great specific binding (SB) affinity values of 1.26 toward α-Glu and 1.32 toward COX-2, while astragalin showed 1.32 and 1.36, respectively. The docking simulation results exhibited strong interactions of vitexin and astragalin with the key residues of the enzyme targets, suggesting their possible mechanisms of action. The in vitro antidiabetic validation revealed noticeable half-maximal inhibitory effects (IC50) of 36.38 ± 3.06 µM for vitexin and 42.47 ± 4.13 µM for astragalin, much better than that of the positive drug acarbose (109.54 ± 14.23 µM). Similarly, these two compounds showed the inhibitory activity against COX-2 with the half-maximal inhibitory effects (IC50) at 27.91 ± 1.74 µM and 49.05 ± 1.49 µM, respectively. Therefore, these two flavonoid compounds (vitexin and astragalin) were speculated as potential antidiabetic and anti-inflammatory compounds from E. humifusa. Taken together, the integrated strategy applied to E. humifusa led to the fast identification of two potential double-acting flavonoids and enlightened its antidiabetic and anti-inflammatory uses. Besides these findings, the integrated strategy in this study could also be used to facilitate the rapid discovery and development of active candidates from other traditional herbal medicines against multi-drug targets and to aid in revealing their mechanisms of action for their traditional uses.

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Section: Potential Ligands Activities Validationssupporting

confidence: 74%

Exploring potential antidiabetic and anti-inflammatory flavonoids from Euphorbia humifusa with an integrated strategy

Fan

Chen

2022

Front. Pharmacol.

View full text Add to dashboard Cite

show abstract

“…[14,15] This is because previous reports demonstrated that flavonoids can suppress both pathways of arachidonic metabolism, namely lioxygenase and cyclooxygenase pathways. [17,18] In a separate study, Luyen and his colleagues (19) isolated twenty six compounds from Euphorbia humifusa. [19] Most of these compounds demonstrated anti-inflammatory activities as indicated by their inhibitory effects on soluble epoxide hydrolase, lipopolysaccharide-induced NO and TNF-α production.…”

Section: Discussionmentioning

confidence: 99%

“…[17,18] In a separate study, Luyen and his colleagues (19) isolated twenty six compounds from Euphorbia humifusa. [19] Most of these compounds demonstrated anti-inflammatory activities as indicated by their inhibitory effects on soluble epoxide hydrolase, lipopolysaccharide-induced NO and TNF-α production. In a comparable study, thirteen diterpenoids were isolated from the roots of Euphorbia ebracteolata.…”

Section: Discussionmentioning

confidence: 99%