Studies On Chemical Constituents And Bioactivities Of The Scutellaria Barbata D.Don

Scuetallria barbata D.Don, belonging to the family Labiatae and widelydistributed in China，has been traditionally used for the treatment of hepatoma, lungcancer, breast cancer, liver cirrhosis etc. However, the active constituents and theirmechanism underlyin g the activity were unclear, which has limited the developmentof Scuetallria barbata. Therefore, we used the bioassayed-guided fractionationmethod to search active components, and prilimilarily explored the synergetic effectbetween subfractions.Isolation and structure determination: Using bioassay-guided isolation, theMeOH extract of the herbs Scuetallria barbata were chromatographed on SephadexLH-20, silicagel and TLC, and semi-preparative HPLC, respectively. As a result,thirty compounds were isolated and purified from the gorgonian Scuetallria barbata.Twenty-four compounds were identified on the basis of spectral methods (1D-NMR,2D-NMR, MS, IR, etc.) and their physicochemical properties. These compounds werestructurally elucidated as six neo-clerodanetype diterpenoids, namely, scutebata P (1),scutebata Q (2), scutebata E (3), scutebata R (4), scutebarbatine B (5), barbatin A (6);and seven flvaonoids, namely,5-hydorxy-7,3′,4′,5′-tetramethoxyflavone (7),5-hydorxy-6,7,3′,4′-tetramethoxyflavone (8), apigenin (9),5,7,4′-trihydorxy-8-methoxyflavone (10),5,7,4-trihydorxy-6-methoxyflavone (11),6-methoxynaringein (12),8-methoxynaringein (13); four sterols: cholesterol (14), stigmasterol(15), β-sitosterol (16), stigmast-4-en-3-one (17); four benzoyl derivatives,namely, E-4-Methyl cinnamic acid (18),4-hydroxybenzaldehyde (19), p-hydroxyaceto phenone (20), benzoic acid (21); two triterpenes: Oleanic acid (22),Ursolic acid (23);and a aurantiamide acetate (24). Respectively, among them, therewere three new compounds (1,2,4) and four known compounds(7,8,18,22)wereobtained from Scutellaria barbata D.Don for the first time. Biological activities: Select three tumor cell lines of P388(murine leukemiacell), K562(chronic myelogenous leukemia cell lines of the original) and Hela(human cervical carcinoma cells) with MTT method and enzyme-linkedimmunosorbent assay (ELISA) method for bioactivity screening of most singlecompounds which came from the active fractions in the preliminary bioactiveevaluation. The results showed that compounds1,2,3,4,5,8showed differentdegrees of antitumor activity to the K562tumor cells at a concentration of10μg/ml.Comprehensive analysis of the activity data, it presented different positive or negativesynergies between fractions.