ABSTRACT
Multidrug resistance (multidrug,resistance,MDR) is the result of joint action of a multi mechanism results,including the abnormal expression of multidrug resistance gene,drug targets down etc.MDR is one of the main reasons for the failure of cancer chemotherapy,so the study of MDR reversal agents has become a research hotspot at home and abroad.Due to chemical medicine reversal agent toxicity,target is single,limited application,Traditional Chinese medicine is safe and effective,multi targets and low cost advantage,This paper summarizes the research progress of Chinese medicine to reverse MDR in breast cancer.
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Objective Establishing a fingerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality.Methods RP-HPLC was developed for fingerprint analysis and determination of four ingredients in G macrophylla roots from different sources.LC-ESI-TOF-MS was employed to identify the chromatographic peaks of the fingerprint.Results Five common peaks were identified by comparing their retention time with reference secoiridoid glucosides.Eight major peaks in chromatographic fingerprint were analyzed by on-line LC-ESI-TOF-MS.Four secoiridoid glucosides were identified based on their MS data.Conclusion The method is specific and could be served for the quality identification and comprehensive evaluation of G macrophylla.
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Objective To establish a method for measuring serum content of gentiopicroside in Beagle dogs and to explore its internal pharmacokinetic features. Methods The rapid and sensitive HPLC method was adopted as external standard. After intravenous injection of gentiopicroside, serum samples of the Beagle were collected and measured on C18 reverse-phase chromatographic column after liquid -liquid extraction. Results The linear range of gentiopicroside was 0.1343～687.375 ?g?mL-1(r2=0.99993). The recovery was within 81.15 %～97.99 %. The limit of detection (LOD) was 0.1343 ?g?mL-1. Conclusion The pharmacokinetic process of gentiopicroside can be described as one-compartment model with intravenous injection , t1/2 = 1.1324 h, Ke = 0.5811 h-1, V= 0.5316 L?kg-1, CL = 0.3274 L?kg-1?h-1. This indicates that gentiopicroside can be quickly distributed and eliminated and is not liable to be accumulated in the body.
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Objective To systematically study the chemical constituents in the roots of Gentiana macrophylla from Shaanxi Province. Methods Various column chromatographic techniques were used for isolation and purification of the principles. The structures were elucidated on the basis of spectral data (UV, IR, MS, (~1H-NMR), (~(13)C-NMR), (~1H-~1H COSY) and (~1H-~(13)C COSY), HMBC, and HMQC) and identified by comparing with the authentic substance. Results Five compounds were got from fat-soluble fraction. They are identified as: N-pentacosyl-2-carboxy-benzoyl amide (Ⅰ), 5-carboxyl-3, 4-dihydrogen-1H-2-benzopyran-1-one (Ⅱ), erythrocentaurin (Ⅲ), roburic acid (Ⅳ), oleanolic acid (Ⅴ). Conclusion Compounds Ⅰ and Ⅱ are two novel ones. They are named as qinjiaoamide and erythrocentauric acid, respectively. Compound Ⅲ is isolated from the plants of Gentiana L. for the first time.
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Objective: To determine the anti rejection effects of CTLA 4 Ig fusion protein on cardiac allografts in mice and to discuss its mechanism in vivo . Methods: BALB/c recipients were performed cervical heterotopic heart transplantation to receive C57BL/6 donor hearts with a cuff technique. BALB/c recipients were intraperitoneally injected with CTLA 4 Ig [100 ?g/d?15 times], control immunoglobins and PBS to observe the survival time of allografts with ECG. The hyporesponsiveness of splenic T cell, the polarization of the T subsets were analyzed after the recipients treated with CTLA 4 Ig. Results: After treated with CTLA 4 Ig, the survival of cardiac grafts was significantly prolonged compared with the control groups, and more than 40% cardiac grafts survived over 2 months. The splenic T cells isolated from recipients did not respond to restimulation of donor splenocytes in MLR, but did exhibit the capacity to proliferate in response to C3H splenocytes(third party).The levels of IL 2 and IFN ? decreased and the level of IL 10 increased in CTLA 4 Ig treated mice. Conclusion: Administration of CTLA 4 Ig can induce donor specific tolerance, which induce T subsets to polarize toward Th2 subset and hyporesponsiveness to alloantigen, and prolong the survival time of the cardiac grafts effectively. [