ABSTRACT
Objective: To investigate in vivo metabolic profiles of two lignans, 6-hydroxy-4-(4-hydroxy-3-methoxyphenyl)-3- hydroxymethyl-7-methoxy-3,4-dihydro-2-naphthaldehyde (VB-1) and vitedoin A (VB-2) in the rats. Methods: A UFLC-IT- TOF-MS method was applied to characterize the prototypes and metabolites of VB-1 and VB-2 in rat feces, urine, bile, and plasma after oral administration. Results: Eleven metabolites of the two parent compounds were detected and two prototypes were identified unambiguously by comparing with references. Analysis of metabolites revealed that glucuronidation, sulfation, and hydroxylation were major biotransformation pathways of two lignans. Conclusion: In this study, under the analysis of metabolites of two lignans, its in vivo metabolic process is basically clarified. The results could be helpful for the further pharmacokinetics and pharmacological evaluations of VB-1 and VB-2.
ABSTRACT
Chemical constituents from the fruits of Vitex negundo var. cannabifolia and their nitric oxide (NO) inhibitory and cytotoxic activities were investigated. The compounds were isolated and purified by various column chromatography, and their structures were identified by physiochemical properties and spectroscopic data. Thirteen lignans and six phenolic compounds were isolated from the CH2Cl2 extract of the fruits of V. negundo var. cannabifolia, respectively. Their structures were elucidated as 6-hydroxy-4-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-3,4-dihydro-2-naphthaldehyde (1), vitedoin A (2), vitexdoin F (3), detetrahydroconidendrin (4), vitexdoin E (5), 4-oxosesamin (6), L-sesamin (7), (+)-beechenol (8), ligballinol (9), 2-(4-hydroxyphenyl)-6-(3-methoxy-4-hydroxyphenyl)-3,7-dioxabicyclo[3.3.0]octane (10), (-)-pinoresinol (11), balanophonin (12), thero-guaiacylglycerol-β-coniferyl aldehyde ether (13), trans-p-coumaryl aldehyde (14), coniferyl aldehyde (15), 5,7-dihydroxychromone (16), trans-3,5-dimethoxy-4-hydroxy-cinnamic aldehyde (17), frambinone (18), and alternariol 4-methyl ether (19). Compounds 8-10,14,18,19 were firstly isolated from Verbenaceae family, compound 13 was obtained from Vitex species, and 6,7,12,15-17 from V. negundo var. cannabifolia for the first time, respectively. The isolated compounds were evaluated for their anti-inflammatory and cytotoxic effects in vitro. Eight compounds (3,5,7,10,11,14,15,17) showed inhibition against NO production in LPS-stimulated RAW 267.4 cells (IC₅₀ in the range of 7.8-81.1 μmol•L⁻¹) and four compounds (1-4) showed cytotoxicity on HepG-2 cells (IC₅₀ in the range of 5.2-24.2 μmol•L⁻¹).
ABSTRACT
OBJECTIVE: To study the accumulation dynamics and distribution law of vitexin during the whole year period in different parts of Vitex negundo var.cannabifolia (Sieb. et Zucc.). METHODS: Vitexin was obtained by ultrasonic extraction, and its content was determined by HPLC. Filodoor column (4.6 mm×150 mm, 5 μm) was used. Methanol-water (volume ratio of 4;6) was used as the mobile phase at a flow rate of 1 mL·min-1. The UV detective wavelength was set at 340 nm, injection volume was 5 μL, and the column temperature was set at 35°C. RESULTS: The content of vitexin was low in vitex negundo branches and flowers, and had obvious regularity in different growth periods of Vitex negundo leaves. The content of vitexin was the highest (1.380%-1.465%) in June and July. Along with the blooming and formation of negundo chastetree to their maturation, the content of vitexin in Vitex negundo leaves decreased. Its content was the lowest (0.720%-0.751%) in September and October. The content of vitexin in Vitex negundo seeds increased(0.435%-1.231%)with seed maturation. CONCLUSION: The content of vitexin in different parts of Vitex negundo presents a regular change in different periods. The detection of vitexin in different growth periods provides experimental basis for the selection of best collection phase and medical parts.