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1.
International Journal of Traditional Chinese Medicine ; (6): 984-986, 2015.
Article in Chinese | WPRIM | ID: wpr-482197

ABSTRACT

Objective To detect the effect of Danhong injection on cerebral vascular hemodynamic parameters, Cys-c and Hcy in patients with transient cerebral ischemia(TIA), and analyze its clinical effect. Methods 80 TIA patients were selected. The patients were divided into a control group and a Danhong injection observation group with 40 cases each group. The control group was given conventional treatment, and the observation group was given conventional treatment and Danhong injection. The treatment course was 14 d. The hemodynamic parameters, Cys-c and Hcy expresssion were observed. Clinical effect was analyzed. Results After treatment, average blood flow speed (20.07 ± 4.28 cm/s vs. 16.17 ± 2.46 cm/s, t=5.230), average blood flow (11.14 ± 2.24 ml/s vs. 9.54 ± 1.65 ml/s, t=3.637), and cerebral vascular resistance (1 602.4 ± 98.3 kPa/s·m-1 vs. 1 738.5 ± 104.3 kPa/s·m-1, t=6.024) was significantly improved in the observation group than those in the control group (P<0.05). Cys-c (0.48 ± 0.11 mg/L vs. 0.71 ± 0.14 mg/L, t=8.170) and Hcy (17.45 ± 3.26 μmol/L vs. 23.62 ± 4.12 μmol/L, t=7.428) were significantly decreased in the observation group than those in the control group (P<0.05). The recurrence rate of TIA and cerebral infarction were 7.5% and 5% in observation group, which were significantly lower than that of 22.5% and 15% in control group (χ2=2.451, P<0.05;χ2=2.630, P<0.05).Conclusion Danhong injection can reduce the expression of Cys-c and Hcy and recurrence rate of TIA and cerebral infarction.

2.
Acta Pharmaceutica Sinica ; (12): 1046-1050, 2005.
Article in Chinese | WPRIM | ID: wpr-253495

ABSTRACT

<p><b>AIM</b>To demonstrate the specific killing of folate receptor (FR)-positive tumor cells can be achieved by folate-targeted penicillin-G amidase (PGA) combined with its prodrug substrate N-(phenylacetyl) doxorubicin (DOXP).</p><p><b>METHODS</b>Folic acid was covalently linked to PGA and folate content value was determined by quantitative UV spectrophotometry. The ability of folate conjugated PGA to hydrolyze DOXP was measured by RP-HPLC. Visual demonstration of uptake by FR (+) HeLa and SKOV3 cells was detected by using FITC labeled folate-PGA and a fluorescence microscopy. The cytotoxicity of DOXP towards the cells in the presence or absence of folate-PGA was assayed by using MTT method.</p><p><b>RESULTS</b>The folate-PGA has a specific activity of 29. 8 U x mg(-1) (protein). FR selectivity was confirmed by fluorescence microscopy. The combination of DOXP prodrug with folate-PGA generated higher cytotoxicity towards the FR (+) cells than free doxorubicin. The IC50 was 0.72 micromol x L(-1) for HeLa cells and 0.75 micromol x L(-1) for SKOV3 cells, respectively. Further, the enhanced cytotoxicity reduced greatly with the addition of free folic acid.</p><p><b>CONCLUSION</b>Folate conjugated PGA did not significantly compromise PGA catalytic activity and enabled binding prodrug-activating enzyme PGA to folate receptor expressing cells, and increased the sensitivity of the cells to doxorubicin followed by administration of its prodrug substrate.</p>


Subject(s)
Female , Humans , Antibiotics, Antineoplastic , Pharmacology , Carrier Proteins , Metabolism , Cell Line, Tumor , Doxorubicin , Pharmacology , Drug Delivery Systems , Folate Receptors, GPI-Anchored , Folic Acid , Chemistry , Pharmacology , HeLa Cells , Inhibitory Concentration 50 , Ovarian Neoplasms , Pathology , Penicillin Amidase , Chemistry , Pharmacology , Prodrugs , Pharmacology , Receptors, Cell Surface , Metabolism
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