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A novel nor-lupane triterpenoid, 3-oxo-29 α -hydroxy-17 β ,20-epoxy-28-norlupane ( 1 ), and two new guaiane sesquiterpenoids, schvenols A–B ( 2 – 3 ), has been isolated from leaves of Schefflera venulosa . Structures of the new compounds were elucidated on the basis of their spectroscopic methods, including 1D and 2D NMR techniques. And the structure of 1 was further confirmed by the X-ray diffraction analysis. None of the compounds showed inhibitory effects on NO release in LPS-stimulated RAW 264.7 macrophage cell line. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: Caesalpinia sappan is a medicinal plant native to China popularly used to treat chronic pelvic inflammation, dysmenorrhea and hysteromyoma. Its main bioactive component is brazilin which had presented antibacterial, anti-inflammatory and anti-platelet aggregation activities. To establish a sensitive, selective, reproducible, and accurate high performance liquid chromatographic (HPLC) method for the quantitative determination of brazilin in plasma, and study the pharmacokinetics of brazilin in rats after intravenous administration of brazilin. Materials and methods: Rats received intravenous injection of 25, 50 and 100mg/kg of brazilin. Concentrations of brazilin in plasma were determined by HPLC method at different time points and all pharmacokinetic parameters were estimated by non-compartmental analysis with WinNonLin 6.2 software. Results: After single intravenous doses of 25, 50 and 100mg/kg brazilin in rats, the main PK parameters were as follows: C max were 18.1±4.1, 46.7±8.7 and 82.2±9.6µg/mL; AUC0–24 were 20.4±4.3, 48.7±6.8 and 90.4±10.3µgh/mL; and t 1/2 were 5.4±1.5, 5.8±0.9 and 6.2±1.2h, respectively. Conclusion: It showed that the brazilin was eliminated moderately in rat by intravenous injection route with t 1/2 of 6h and showed a dose-dependence profile of C max and AUC0–24 at the doses of 25~100mg/kg of brazilin for injection in rats. [ABSTRACT FROM AUTHOR]