Synthesis and anti-tumor activity evaluation of Matijin-Su derivatives.

A series of Matijin-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-l-phenylalanol) derivatives was synthesized and evaluated for their anti-tumor activities in hepatocellular carcinoma cells. The IC50 of compounds 1, 3, 4, 11, 13 were less than 20µM, and compound 1 and 3 showed an IC50 value of less than 9µM. Expansion inhibition could be found significantly in compound 1 and 3-treated human hepatoma cell HepG2 and PLC/PRF/5, while both compounds exhibit lower toxicity to human hepatocyte cell line L-02. Compound 1 and 3 could induce cell cycle arrest at G1/S phase. This may be attributed to increase level of intracellular reactive oxygen species (ROS). Up-regulation of p38 MAPK activity in responding the ROS stabilize p53 and activate p21 transcription, the critical regulatory in G1/S checkpoint. Observations in this study shed light on the potential of MTS derivatives compound 1 and 3 as novel suppressors to human liver cancer.

Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents.

A series of Matijing-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-L-phenylalanol) derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity in 2.2.15 cells. The IC(50) of compounds 14a (0.71 µM), 13c (2.85 µM), 13b (4.37 µM), etc. and the selective index of 13g (161.01), 13c (90.45), 13a (85.09) etc. of the inhibition on the replication of HBV DNA were better than those of the positive control lamivudine (IC(50): 82.42 µM, SI: 41.59). Compounds 13o, 13p, and 16a also exhibited significant anti-HBV activity.

Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives.

A series of derivatives of Matijing-Su (MTS, N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol) was synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC(50) of compounds 9c (1.40 microM), 9g (2.33 microM) and 9n (2.36 microM), etc. and the selective index of 9n (45.93) of the inhibition on the replication of HBV DNA were higher than those of the positive control lamivudine [41.59, (IC(50): 82.42 microM)]. Compounds 11d, 12a and 12e also exhibited significant anti-HBV activities.

A novel iridoid from Torricellia angulata var intermedia.

A new iridoid, named torricellate, was isolated from root bark of Torricellia angulata var intermedia, a Chinese folk medicinal plant used to treat bone fracture, tonsillitis and asthma. Its structure was elucidated by NMR, MS, IR and UV, and confirmed by X-ray diffraction studies.

[Determination of glycyrrhizic acid in different decoctions of sanaotang by HPLC and comparison with antifugal effects in vitro].

OBJECTIVE: To investigate the contents of glycyrrhizic acid in hejian decoction (mixed the traditional Chinese herbs together, then boiling them with water) and the fenjian decoction (boiling the single traditional Chinese herb with water separately, then mixed the abstracts) of Sanaotang (composed of Ephedra sinica, Prunus armeniaca and Glycyrrhiza uralensis) and to compare with their anti-bacterial activities in vitro. METHOD: A HPLC method was established with a Agilent Zorbax SB-C18 column (4. 6 mm x 250 mm, 5 microm), a mobile phase of acetonitrile-0.2% acetic acid solution (35:65), a flow rate of 1 mL x min(-1) and a detection wavelength of 254 nmn in order to determine the contents of glycyrrhizic acid minimal bacterial inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) antagonized the common bacteria in different decoctions were rieasured in vitro by employing dilution method. RESULT: The average content of glycyrrhizic acid of the hejian decoction was higher than that of the fenjian decoction. The hejian decoction could display the inhibitory bactericidal activity to Aeruginosus bacillus, but the fenjian decoction could not. And to Staphylococcus aureus, the inhibitory bactericidal activity the hejian decoction was slightly stronger than that of the fenjian decoction. CONCLUSION: Comparing with that of the fenjian decoction, the content of glycyrrhizic acid of the hejian decoction was higher and the anti-bacterial activities was stronger.

Two new naturally occurring optical polyacetylene compounds from Torricellia angulata var intermedia and the determination of their absolute configurations.

Four compounds were isolated from Torricellia angulata var intermedia (Harms.) Hu (Torricelliaceae), followed by formation of derivatives, which gave two new polyacetylene compounds 3 and 4 with respectively a chiral carbon center whose absolute configurations were determined unambiguously by the recently developed extended Mosher's method. This is the first time to obtain natural polyacetylenes possessing a chiral hydroxyl group.

Effects of different compounding of formulae on content of gardenoside in Yin Chen Hao decoction.

In order to observe the effects of the ground and intact Zhi Zi (Fructus Gardeniae) and different combinations of the ingredients and refined single Chinese drug granules in Yin Chen Hao Decoction compound prescription on the contents of gardenoside (an effective component of the prescription), the contents of gardenoside were determined with reversed phase high performance liquid chromatography (HPLC), with acetonitrile-water (15:85) as mobile phase, at wave length 238 nm. The results indicated that the gardenoside-decocted-out rates in the decoctions prepared by different combinations of the ingredients with the ground Zhi Zi (Fructus Gardeniae) all were higher significantly than those in the decoction with intact Zhi Zi (Fructus Gardeniae), and generally, different combinations of the ingredients in the decoction had only little effect on the gardenoside-decocted-out rate.

[Measurement of baicalin contents by HPLC].

OBJECTIVE: To compare the contents of baicalin in the raw medical material and the different prepared medical materials of Scutellaria baicalensis. METHOD: The contents of baicalin were determined by HPLC. Chromatographic conditions included Hypersil C18 column and the mobile phase consisting of a mixture of methanol-0.04% phosphoric acid (46:54). Baicalin was detected at 280 nm. The standard curve was linear in the range of 0.0280-4.6700 micrograms with correlation coefficient 1.0000. The average recovery of baicalin was 101.22% with RSD = 2.54% (n = 5). RESULT: The contents of baicalin were 6.80% in raw material, 6.00% and 6.73% in the different prepared medical materials of S. baicalensis respectively. CONCLUSION: The two different kinds of preparing methods can be used to the raw material of S. baicalensis.