OBJECTIVETo establish a method for determination of 7 alkaloid in Herba Sophorae Alopecuroidis by HPLC.

METHODX-Brige C18 (4.6 mm x 200 mm, 5 microm) column was used with acetonitriles-0.05 mol x L(-1) KH2PO4 solution (2.0 mL x L(-1) triethylamine) with gradient elution as the mobile phase and 1.0 mL x min(-1) as the flow rate. The detection wavelength was 205 nm.

RESULTAloperin curve was linear in the range from 20.66 to 103.32 microg (r = 0.998 8) and the average recovery was 97.12% (RSD 7. 3%); sophoridine curve was linear in the range from 22.82 to 114.12 microg (r = 0.999 7) and the average recovery was 97.47% (RSD 3.0%); oxymatrine curve was linear in the range from 25.10 to 125.52 microg (r = 0.999 1) and the average recovery was 96.21% (RSD 4.5%); oxysophocarpine curve was linear in the range from 23.88 to 119.40 microg (r = 0.997 5) and the average recovery was 94. 64% (RSD 5.2%); matrine curve was linear in the range from 5.00 to 24.99 microg (r = 0.998 6) and the average recovery was 98.04% (RSD 5.4%); sophocarping curve was linear in the range from 4.69 to 23.46 microg (r = 0.999 6) and the average recovery was 96.24 (RSD 5.8%); lehmannine curve was linear in the range from 4.60 to 23.01 microg (r = 0.997 8) and the average recovery was 101.31% (RSD 4.3%).

CONCLUSIONThe method is accurate, simple and feasible. It can be used as a quality evaluation in Herba S. Alopecuroidis.

Alkaloids ; analysis ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; Piperidines ; analysis ; Quality Control ; Quinolizidines ; analysis ; Quinolizines ; analysis ; Sophora ; chemistry

BACKGROUND: Nadifloxacin is a synthetic fluoroquinolone with a broad spectrum. It has been suggested to not only have antibacterial, but also anti-inflammatory actions. In addition, it is effective against antibiotic-resistant Propionibacterium acne. Upon review of the literature, however, no studies have been performed concerning the efficacy and safety in terms of irritation potential and skin barrier changes after applying nadifloxacin. OBJECTIVE: This study intended to evaluate the skin irritation and changes of the skin barrier function associated with the administration of nadifloxacin 1% cream for the treatment of acne vulgaris. Furthermore, the efficacy and safety of nadifloxacin 1% cream were also assessed. METHODS: The changes in the lesion counts, Korean Acne Grading System (KAGS) and adverse events were recorded. The biophysical profiles of the skin, including transepidermal water loss (TEWL), skin surface hydration and redness were measured by Tewameter(R), Corneometer(R) and Mexameter(R) for 3 weeks. RESULTS: At the end of the therapy, 69% of inflammatory lesions (p<0.0001) and 27% of noninflammatory lesions (p=0.26) resulting from acne were decreased from the baseline. Adverse events were reported in two patients, but they were transient and tolerable. The skin barrier function showed no changes during the treatment periods. CONCLUSION: Nadifloxacin 1% cream is effective for the treatment of acne vulgaris without the changes of skin barrier function.
Acne Vulgaris ; Fluoroquinolones ; Humans ; Propionibacterium ; Quinolizines ; Skin

OBJECTIVETo establish a new method for quality evaluation and validate its feasibilities by simultaneous quantitative assay of five alkaloids in Sophora flavescens.

METHODThe new quality evaluation method, quantitative analysis of multi-components by single marker (QAMS), was established and validated with S. flavescens. Five main alkaloids, oxymatrine, sophocarpine, matrine, oxysophocarpine and sophoridine, were selected as analytes to evaluate the quality of rhizome of S. flavescens, and the relative correction factor has good repeatibility. Their contents in 21 batches of samples, collected from different areas, were determined by both external standard method and QAMS. The method was evaluated by comparison of the quantitative results between external standard method and QAMS.

RESULTNo significant differences were found in the quantitative results of five alkaloids in 21 batches of S. flavescens determined by external standard method and QAMS.

CONCLUSIONIt is feasible and suitable to evaluate the quality of rhizome of S. flavescens by QAMS.

Alkaloids ; analysis ; Quinolizines ; analysis ; Sophora ; chemistry

Cytisine derivatives are a group of alkaloids containing the structural core of cytisine, which are mainly distributed in Fabaceae plants with a wide range of pharmacological activities, such as resisting inflammation, tumors, and viruses, and affecting the central nervous system. At present, a total of 193 natural cytisine and its derivatives have been reported, all of which are derived from L-lysine. In this study, natural cytisine derivatives were classified into eight types, namely cytisine type, sparteine type, albine type, angustifoline type, camoensidine type, cytisine-like type, tsukushinamine type, and lupanacosmine type. This study reviewed the research progress on the structures, plant sources, biosynthesis, and pharmacological activities of alkaloids of various types.
Alkaloids/chemistry* ; Quinolizines/pharmacology* ; Azocines/chemistry* ; Fabaceae

Alkaloids ; Apoptosis ; HL-60 Cells ; Harringtonines ; Humans ; Quinolizines

OBJECTIVETo investigate the induction of apoptosis on human oral epidermoid carcinoma KB cells and multidrug resistant KBv200 cells by Matrine.

METHODSMTT assay was used to investigate the inhibition ability of Matrine on the cells in vitro. Transmission electron microscope was used to observe the ultrastructure feature of cells. after treated by Matrine. Acridine orange (AO)/Ethidium bromide (EB) fluorescent staining and flow cytometry were used to observe apoptosis induced by Matrine. Flow cytometry was applied to study the effects of the drug on cell cycles of the cells.

RESULTSWhen 0.50, 1.00, 1.50, 2.00 mg/ml of Matrine was used, the vital rates of KB and KBv200 cells were decreased according to Matrine's concentration. The IC50 concentrations of Matrine on KB and KBv200 cells were 1.35 mg/ml and 1.43 mg/ml individually. The results of AO/EB fluorescent staining and flow cytometry showed that Matrine could induce apoptosis of two kinds of cells. While observed by transmission electron microscope, there were more contraction of cells, condensation of nuclei, bubble of cytoplasm in both kinds of cells after treated by Matrine. Matrine could stop the growth of KB and KBv200 cells at S period and restrain mitosis of cells.

CONCLUSIONMatrine can inhibit the growth of KB and KBv200 cells by inducing apoptosis. The apoptosis effect is dose-dependent and it has certain relation to the blocking of S period cells.

Alkaloids ; Apoptosis ; Carcinoma, Squamous Cell ; Humans ; KB Cells ; Quinolizines

BACKGROUND: Antimicrobials have been a mainstay of inflammatory acne treatment for more than 30 years. However, antibiotic-resistant propionibacteria had been isolated with increased frequency, and associated with failure to respond to antibiotic therapy. OBJECTIVE: The aim of this study was to investigate the clinical efficacy and tolerance of 1% nadifloxacin cream. METHODS: In the final analysis, 197 patients with mild to moderate facial acne vulgaris were enrolled. The patients were instructed to apply 1% nadifloxacin cream twice daily to the affected skin after washing the face. Following 2 and 4 weeks of treatment, patients were observed for clinical response: number of the acne lesions, Korea acne grading system (KAGS), global improvement, and occurrence of adverse reactions. RESULTS: During 4 weeks of treatment, nadifloxacin caused significant reduction in the number of inflamed papulo-pustular lesions and open/closed comedones. In addition, significant reduction of KAGS was observed. About 96% of patients showed clinical improvement in the overall evaluation of the therapeutic effect by physicians. All reported adverse events were mild. CONCLUSION: This study shows that 1% nadifloxacin cream can be an effective and safe treatment for mild to moderate acne vulgaris.
Acne Vulgaris ; Fluoroquinolones ; Humans ; Korea ; Quinolizines ; Republic of Korea ; Skin

OBJECTIVE: To study the effect of matrine on tumor growth, inflammatory factors and immune function in Wistar rat with breast cancer. METHODS: Sixty female Wistar rats were randomly divided into control group (=10) and the modeling group of breast cancer cell tumor-bearing rat (=50), then the rats in modeling group were randomly divided into five groups (=10):vehicle group, matrine low dose group (50 mg/kg), medium dose group (100 mg/kg), high dose group (200 mg/kg), and lentinan group (200 mg/kg). Except the control group, each rat in the other groups was subcutaneously inoculated 0.4 ml Walker 256 breast cancer cell suspension (5×10 cells/ml) in the right axillary. Each group was treated with corresponding drug by ig administration (10 ml/kg body weight) twice a day for 14 days. After 14 days, the blood sample was collected from ventral aorta, the tumor was removed and weighed to calculate tumor inhibitory rate. The levels of interleukin-2 (IL-2), interferon-γ (IFN-γ), interleukin-6 (IL-6), interleukin-10 (IL-10), transforming growth factor-β (TGF-β), CD3, CD4, CD8, IgG, IgM, IgA in peripheral blood were determined. RESULTS: The mean tumor weight of matrine low-dose, medium-dose, high-dose groups and lentinan group were (4.99±0.93) g, (4.52±0.92) g, (4.22±1.18) g and (4.52±0.92) g respectively, which were significantly lower than that in model group. There was no statistical difference on the mean tumor weight among matrine groups and lentinan group (>0.05). After the drug intervention, the tumor inhibitory rates of matrine low-dose, medium dose, high-dose groups and lentinan group were 24.6%, 31.7%, 36.3%, and 27.9% respectively, there was no statistical difference among the four groups. The levels of IL-2, IFN-γ, CD8+ in vehicle group were lower than those of control group obviously (<0.01), however, the levels of IL-6, IL-10, TGF-β, CD3, CD4, IgG, IgM, IgA were higher significantly than those of control group (<0.01). The levels of IL-2, IFN-γ, CD8 in matrine low-dose, medium dose, high-dose groups and lentinan group were higher than those of vehicle group obviously (<0.01, <0.05); while the levels of IL-6, IL-10, TGF-β, CD3, CD4, IgG, IgM, IgA were lower than those of model group markedly (<0.01, <0.05). The levels of IgM and IgA in matrine low-dose and medium-dose groups were higher than those of lentinan group obviously (<0.01, <0.05); the levels of IL-2, IFN-γ and IgA in matrine high-dose group were higher than those of lentinan group obviously (<0.01, <0.05); while the levels of IFN-γ in matrine low-dose group were lower than those of lentinan group markedly (<0.05); the levels of IL-10 and CD4 in matrine high-dose group were lower than those of lentinan group markedly (<0.01, <0.05). CONCLUSIONS Matrine has an obvious antitumor action which is related to its ability to enhance cellular and humoral immunity, reduce inflammatory reaction.
Alkaloids ; Animals ; Breast Neoplasms ; Female ; Quinolizines ; Rats ; Rats, Wistar

OBJECTIVETo study the effects of matrine on gamma-globin synthesis in K562 cells in vitro.

METHODSBenzidine staining was used to study the dose- and time-dependent effects of matrine on hemoglobin synthesis in K562 cells, and Western blotting was performed to determine the level of hemoglobin F(alpha(2)gamma(2)).

RESULTSBenzidine staining showed that K562 cells treated with matrine of 0.1 mg/ml had a positivity rate for benzidine (BZ%) of 15.67% at 96 h after the treatment, and Western blotting indicated increased synthesis of hemoglobin F.

CONCLUSIONMatrine can induce gamma-globin synthesis and increase hemoglobin F level in K562 cells, the effect of which resembles that of sodium butyrate.

Alkaloids ; pharmacology ; Blotting, Western ; Fetal Hemoglobin ; biosynthesis ; Globins ; biosynthesis ; Humans ; K562 Cells ; Quinolizines ; pharmacology

OBJECTIVETo observe the effects of oxymatrine on the expression of interleukin-6 (IL-6), interleukin-1beta (IL-1beta) mRNA of human periodontal ligament cell (PDLC) stimulated by lipopolysaccharides (LPS), and to discuss oxymatrine's inhibition mechanism on periodontal inflammation stimulated by LPS.

METHODSFirstly, isolate PDLC externally and culture them; for oxymatrine experimental group we used different combination of LPS and oxymatrine in different concentration, and for the matched group we use DEME nutrient solutions of 1% FBS. Then reverse transcription-polymerase chain reaction (RT-PCR) for checking the level of IL-6 and IL-1beta mRNA.

RESULTS25 microg x mL(-1) LPS can significantly enhance the expression of both IL-6 and IL-1beta mRNA's level, and oxymatrine could restrain above phenomena.

CONCLUSIONOxymatrine can restrain the expression of IL-6 and IL-1beta mRNA of human PDLC stimulated by LPS.

Alkaloids ; Humans ; Interleukin-1beta ; Interleukin-6 ; Lipopolysaccharides ; Periodontal Ligament ; Quinolizines ; RNA, Messenger