ABSTRACT
Objective To study the radiosensitization of irisquinone on the Warburg effect of MDA-MB231 cells.Methods MDA-MB231 cells in the exponential growth phase were divided into 6 groups:control group,irisquinone group,radiation group,irisquinone plus radiation group(Irisquinone + RA),negative control group,and experimental group (siRNA).Colony formation assay was used to measure cell survival fraction of MDA-MB231 cells.Single-hit multi-target model was used to fit the survival curve and calculate the sensitive enhancement ratio (SER).Flow cytometry was used to measure cell apoptosis.The relative expression levels of HK Ⅱ mRNA and protein in each group were detected by qRT-PCR and Western blot respectively.Results The values of D0,Dq and SF2 in the irisquinone plus radiation group were obviously lower than those in the radiation group.The SER of irisquinone was 1.52.Compared with the other groups,the cell apoptosis rate was increased (t =13.29,12.09,5.90,3.83,P ＜ 0.05),while the relative expression levels of HK Ⅱ mRNA (t =9.14,10.48,3.40,P＜0.05) and protein (t=13.39,16.08,5.81,P ＜ 0.05) were decreased in the irisquinone plus radiation group significantly.Conclusions Radiosensitization function of irisquinone inhibits the Warburg effect of MDA-MB231 cells by down-regulating the expression of HK Ⅱ.
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Objective To parperare and identify the irisquinone-hydroxypropyl-?-cyclodextrin (irisquinone-HP-?-CD) inclusion compound. The inclusion mechanism and mol ratio of irisquinone and HP-?-CD were studied simultaneously. Methods The irisquinone-HP-?-CD was prepared with lyophilization technique. The mol ratio between host and guest moleculars was also researched by molecular gradient and continuing variational methods in inclusion processing. At the same time, the inclusion compound was identified by X-ray diffraction (XRD) and differential scanning calorimetry (DSC) methods, respectively. Results The above-mentioned systems showed the mol ratio of HP-?-CD-irisquinone (2 : 1) and the inclusion compound enhanced remarkably the most solubilization and more combined constant of irisquinone in 25, 35, and 45℃. The lyophilized powder had been formed inclusion compound by identifying. Conclusion It is advantageous to increase the solubilization and to strengthen the stability of irisquinone by preparing inclusion compound.
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AIM: To investigate the intestinal uptake of risquinone in two dosage forms-capsule and irisquinone-?-hydroxyprol-?-cyclodextrin(HP-?-CD) in rats and its pharmacokinetics. METHODS: Comparing with capsule,the accumulation uptake of irisquinone from HP-?-CD inclusion complex were tested in suit in vivo and the correspondence between pharmacokinetics behavior and uptake of irisquinone in rats were simultaneously analysised. RESULTS: The intestinal absorption rate of irisquinone were 0.047 h~(-1) to capsule and 0.180 h~(-1) to irisquinone-HP-?-CD,respectively.The intestinal uptake of irisquinone in rats was positive correlation with its release from capsule in vitro.The accumulated uptake of irisquinone were 29.58% from capsule and 69.63 % from irisquinone-HP-?-CD.The pharmacokinetics of irisquinone in two formulas were coincidence with one-compartment model in rats.The absorption half life(T_(1/2(ka))) was 0.23 h to irisquinone-HP-?-CD and 0.49 h to capsule.The relative bioavailability of irisquinone-HP-?-CD was 133.9%. CONCLUSION: Inclusion complex may enhance intestinal uptake of drug and improve its bioavailability.
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AIM: To prepare the irisquinone freeze-drying injection and investigate its stability. METHODS: The degradation pattern of irisquinone and its effects were measured. At the same time, the stability of freeze-(drying) injection by classic thermostatical test. RESULTS: Irisquinone solution was unstable to heat and its content decreased remarkably in acid and alkaline solutions. The result showed that oil/water partition coeffecient of irisquinone was very large. The irisquinone-hydropropyl1-?-cyclodextrin inclusion complex freeze-drying injection was very effective to enhance the drug stability. CONCLUSION: Irisquinone inclusion complex injection has character of good stability.
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AIM: To screen and optimize the preparation conditions of irisquinone-hydroxypropyl-?-cyclodextrin inclusion complex (Irisquinone-HP-?-CD) with stiring method. METHODS: The load-drug and recovery of irisquinone were adopted as the index, host-guest molar ratio, alcohol concentration and stiring rate as factors, have been investigated in the techniques of irisquinone-HP-?-CD. RESULTS: The load-drug and recovery of irisquinone-HP-?-CD were respective ( 15.79 ?0.22)% and ( 92.03 ?6.26)% by optimizing conditions which were host-guest molar ratio 2∶1, 90% EtOH and stiring rate 800r?min -1. At the same time, the dissolution test showed that irisquinone was faster released from inclusion complex than that from capsules and mixture dosage form. CONCLUSION: The optimizing techniques fit to prepare irisquinoe-HP-?-CD in industry.