Isolamento bioguiado de substâncias antiurolíticas e anti-inflamatórias de Cissus gongylodes (vitaceae)

Abstract

Cissus gongylodes has been traditionally used in the diet of Indigenous peoples in Brazil and in traditional medicine for the treatment of kidney stones and inflammatory diseases. This study aimed to isolate, for the first time, compounds present in the decoction of C. gongylodes leaves responsible for its ethnopharmacological antiinflammatory and anti-urolithiatic properties. The most active fractions of the decoction were fractionated using C18 in an SPE system, and the compounds were purified by HPLC-UV-DAD. The anti-inflammatory activity was evaluated using an ex vivo assay in human blood induced by LPS and calcium ionophore, measuring inflammatory mediators PGE2 and LTB4. The anti-urolithiatic activity was assessed using an in vitro experimental model with human urine to determine the dissolution of calcium oxalate crystals. Furthermore, the decoction was chemically characterized by metabolomic analysis using UHPLC-ESI-HRMS. The isolated compounds, including rutin, eriodictyol 3′-O-glucoside, and isoquercetin, demonstrated significant multitarget actions. These components act as anti-inflammatory agents by inhibiting the synthesis of key inflammatory mediators, PGE2 and LTB4. Additionally, they exhibit anti-urolithiatic properties by promoting the dissolution of calcium oxalate crystals. The characterization of the decoction by UHPLC-HRMS revealed a high content of flavonoids, primarily glycosylated flavonoids. The results support the traditional use of the C. gongylodes decoction, identifying the compounds responsible for its antiinflammatory and anti-urolithiatic effects. The multi-target action exhibited by C. gongylodes is particularly desirable in the treatment of urolithiasis, as inflammation and PGE2 production precede and contribute to the formation of calcium oxalate crystals in the kidneys. Based on these actions, C. gongylodes stands out as a promising source of active compounds for the development of new treatments for urolithiasis.