Novedosos lignanos antiinflamatorios identificados en hojas de Piper nigrum L. mediante aislamiento guiado por...

Piper nigrum L. is widely cultivated in Hainan, China, and its abundant leaves represent an underutilized resource. This study aims to investigate its phytochemical constituents and anti-inflammatory potential. Through anti-inflammatory activity-guided phytochemical isolation, thirty-one compounds were isolated from P. nigrum leaves, including three novel lignans (1-3) and twenty-eight known compounds (4-31). Notably, 24 components are identified in P. nigrum for the first time. All isolated compounds were assessed for anti-inflammatory activity in LPS-induced BV-2 cells, of which 4 showed potent inhibitory activity of NO production (IC₅₀ = 2.7 μM) and dose-dependently reduced the levels of TNF-α, IL-6, and IL-1β. In addition, a validated UPLC-TQ-ESI-MS/MS method was developed to quantify eight representative compounds (4, 6, 9, 14, 16, 17, 29, and 30). These findings enrich the phytochemical profile of P. nigrum and identify promising anti-inflammatory candidates, exploring the potential for developing natural anti-inflammatory agents and herbal supplements from agricultural waste.