OBJECTIVETo establish a method of the quantitative determination of acetylharpagide in Ajuga decumbens.

METHODThe chromatographic conditions were as follows: a Phenomenex Luna C18 column was used, the mobile phase was composed of acetontrile-water (15:85), the flow rate was 1.0 mL x min(-1) and the UV absorbance detection was set at 197 nm.

RESULTLinearity of acetylharpagide was in the range of 0.6-3.6 microg (r = 0.9993), and the average recovery and RSD were 99.13% and 2.48%, respectively.

CONCLUSIONThe contents of acetylharpagide ranged 0.40%-6.39% in A. decumbens. The method was simple, accurate and sensitive.

Ajuga ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Plants, Medicinal ; chemistry ; Pyrans ; analysis ; Reproducibility of Results ; Sensitivity and Specificity

8-O-acetylharpagide and harpagide are two kinds of effective component of Ajuga decumbens extract. A sensitive LC-MS/MS method has been established for pharmacokinetics of 8-O-acetylharpagide and harpagide in beagle dog after oral administration of from A. decumbens extract. Female beagle dogs received orally 12.9, 25.7 mg x kg(-1) p. o. Concentrations of 8-O-acetylharpagide and harpagide in plasma were determined by LC-MS/MS method at different time points and all pharmacokinetic parameters were estimated by non-compartment analysis. The mobile phase consisted of 0.1% formic acid in water (A) and acetonitrile (B), which was run at a flow rate of 0.3 mL x min(-1). Chromatographic separation was achieved on an Agilent ZORBAX XDB-C18 column (2.1 mm x 50 mm, 3.5 microm) using a gradient elution of 5% B at 0-2 min, 95% B at 2. 1-5 min and 5% B at 5. 1-10 min. All analytes, including the IS, were monitored under positive ionization conditions and quantified in MRM mode with transitions of m/z 429.2-369.2 for 8-O-acetylharpagide, m/z 387.2-207.2 for harpagide, and m/z 149.2-103.1 for IS. High purity nitrogen was employed as both the nebulizing and drying gas. Other parameters of the mass spectrometer were optimized as follows: drying gas flow 10.0 L x min(-1); drying gas temperature 300 degrees C; capillary voltage 4 000 V. Results showed that 8-O-acetylharpagide and harpagide showed a dose-dependence profile. T(max) of 8-O-acetylharpagide is 1.7 h, and T(max) of harpagide is 1.57 h, which was higher than T(max) of 8-O-acetylharpagide and harpagide after oral administration of from A. decumbens extract in rats. The different pharmacokinetic parameters may be due to the species differences of rat and beagle dog.
Administration, Oral ; Ajuga ; Animals ; Dogs ; Female ; Iridoid Glycosides ; pharmacokinetics ; Plant Extracts ; metabolism ; Pyrans ; pharmacokinetics ; Rats ; Species Specificity

OBJECTIVETo investigate the anticancer and anti-metastatic effect of Ajuga decumbens extraction (HBG) on breast cancer and to clarify the effect of HBG on MMPs and TIMPs.

METHODThe antitumor and antimetastic effect of HBG was determined using orthotopic 4T1 breast cancer mouse model. Western blot analysis was employed to detect the expression of associated proteins in breast cancer metastasis.

RESULTAdministration with 50-200 mg x kg(-1) doses of HBG significantly reduced the tumor weight, tumor volume and numbers of lung tumor nodules in a dose-dependent manner. Tumor metastasis correlated proteins were altered following HBG treatment, MMP-2 and MMP-9 were down-regulated while TIMP-1 and TIMP-2 were up-regulated.

CONCLUSIONHBG showed anticancer and antimetastatic effect towards breast cancer through regulating the expression of MMPs and TIMPs. These data sustain our contention that HBG might be used as a potential therapeutic agent.

Ajuga ; Animals ; Female ; Mammary Neoplasms, Experimental ; chemistry ; drug therapy ; pathology ; Matrix Metalloproteinase 2 ; analysis ; Matrix Metalloproteinase 9 ; analysis ; Metalloproteases ; analysis ; Mice ; Mice, Inbred BALB C ; Neoplasm Invasiveness ; Neoplasm Metastasis ; prevention & control ; Phytotherapy ; Plant Extracts ; therapeutic use ; Tissue Inhibitor of Metalloproteinase-1 ; analysis ; Tissue Inhibitor of Metalloproteinase-2 ; analysis ; Tissue Inhibitor of Metalloproteinases ; analysis

OBJECTIVETo investigate the improvement effects of Jincao tablet on immune function of the model of hysteromyoma in rat and the relationship between the model and pathogenesis.

METHODRats were randomly divided into 6 groups: normal group, model group, treatment groups including low,middle and high dosage groups of Jincao tablet and Guizhi Fuling pill. Rats were injected respectively with diethyl stilbestrol and progesterone. The immune apparatus of rats were measured. The levels of CD3, CD4 and CD4/ CD8 in serum were determined by flow cytometer. The estrogen and receptor were measured by radioligand binding assay and pathologic changes of womb tissue were observed microscopically.

RESULTCompared with normal group, the weight of thymus, the levels of CD3, CD4 and CD4/CD8 of model group were significantly decreased, and the levels of estrogen, estrogen receptor and CD8 were obviously increased. Jincao tablet groups were significant difference compared with model group and could alleviate the pathological changes of womb tissue.

CONCLUSIONJincao tablet could improve the levels of immune function of the model of hysteromyoma in rat, and it might play a role in the pathogenesis of leiomyoma.

Ajuga ; chemistry ; Animals ; CD3 Complex ; blood ; CD4 Antigens ; blood ; CD4-CD8 Ratio ; CD8 Antigens ; blood ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacology ; Estradiol ; blood ; Female ; Flow Cytometry ; Leiomyoma ; blood ; immunology ; pathology ; Phytotherapy ; Plants, Medicinal ; chemistry ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Receptors, Estrogen ; blood ; Tablets ; Uterine Neoplasms ; blood ; immunology ; pathology