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@#Phosphoinositide 3-kinase(PI3K), a key regulator in the PI3K/AKT/mTOR signaling pathway, plays a critical role in regulation of cell growth, differentiation, metastasis apoptosis, and angiogenesis processes. Abnormal activation of PI3K is closely related to the development of many types of human cancers. PI3Kδ is an important isoform of PI3K family, mainly expressed in leukocytes, which makes it an attractive target for the treatment of hematological malignancies. Great efforts in both industry and academia have been made to develop PI3Kδ selective inhibitors as anti-cancer agents. This review attempts to provide an overview of recent advances in the research of PI3Kδ selective inhibitors, fueling the progress of the ideal selective PI3Kδ inhibitors in the future.
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OBJECTIVE: To develop RP-HPLC method for the rapid determination of resveratrol in serum and tissue homogenates (in some organs) of mice.METHODS:HPLC determination was performed using Kromasil C18 column,the mobile phase consisted of methanol - water (48∶ 52) with a flow rate of 1ml/min,the column was under room temperature with its pressure at 12kPa,the detection wavelength was 303nm and the sample size was 20?l. RESULTS: The linear range for resveratrol was 0.25～25?g/ml, with minimal detectable drug concentration at 0.1?g/ml (S/N=3). The average absolute rec_overy of the samples was above 88% and the methodological recovery rates of which ranged from 96% to 100%,RSD were below 10%. CONCLUSIONS: The established determination method is economical, reliable, simple and rapid, and suitable for the blood concentration determination of resveratrol and the study of its distribution in animal body.
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OBJECTIVE: To establish RP-HPLC method for the fast determination of floxuridinein in serum and homogenate of some of the organs of mice. METHODS: The determination was performed on C18 chromatographic column with its mobile phase consisted of phosphate buffer(pH= 7.4) - methanol(95∶5) and with its detection wavelength at 268nm. RESULTS: Linear detection concentration ranges of floxuridinein were all at 15～240?g/ml. The minimum detection concentration was 3?g/mL(S/N≥3). The average extraction recovery was above 95%. The average recovery ranged from 91%to 112%. Both the intra-day and inter-day precisions were less than 10%. CONCLUSION: The method is simple, rapid, reliable and economical, and it can be used for the determination of serum floxuridinein concentration and the study of its body distribution in animals.
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OBJECTIVE:To develop a rapid RP-HPLC quantitative determination of lamivudine(LAM) in mouse serum and tissue homogenates METHODS:0 1ml of serum of tissue homogenates and 0 5ml of methanol were vortexed in a plastic tube for 30s and the mixture was then centrifuged at 15 000r/min for 10min 20?l of the resulting supernatant was directly injected and LAM was chromatographed on a reversed-phase Kromasil C column(150mm?4 6mm,5?m) using a mixture of phosphate buffer(pH6 8)and methanol(91∶9,v/v)and monitored at 270nm RESULTS:The standard curves were linear over a range from 0 25?g/ml to 50?g/ml The minimal detectable drug concentration was 60ng/ml(S/N=3) The average extraction recovery of LAM was more than 88% The average methodological recoveries of LAM ranged from 97% to 100% The within-dayand between-day precisions were less than 10% CONCLUSION:The assay is economic,simple,rapid and specific
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OBJECTIVE:To optimize the preparation techniques for floxuridinyl diacetate solid lipid nanoparticles(FUDRA-SLN).METHODS:The FUDRA-SLN was prepared by film-ultrasound dispersion method with soybean phos?pholipids as carrier,and the preparation techniques were optimized by means of an orthogonal test design with entrapment ef?ficiency and appearance as indexes of investigation.RESULTS:The FUDRA-SLN prepared in the optimized techniques was even and regular in appearances,with particle diameter at(215?83)nm,entrapment efficiency at98.27%and drug loading dosage at8.20%.CONCLUSIONS:FUDRA-SLN prepared by the optimized film-ultrasound dispersion method has a high entrapment efficiency and high drug loading dosage,and this method is suitable for the laboratory preparation.
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OBJECTIVE:To evaluate the performances of prescription automatic screening system(PASS).METHODS:40101medication orders of616inpatients in14departments of our hospital were monitored retrospectively by using“Army Health No.1”Hospital Information System Pharmaceutical Workstation that equipped with PASS.RESULTS:There were835irrational drug use medication orders and the incidences of irrational drug use stood at2.08%.Of which,91.02%involved adverse drug interactions,4.55%involved irrational in vitro injection combinations and4.43%were irrational use of drugs for children.CONCLUSION:PASS system is conducive to rational drug use in clinics,yet it is still for from being perfect thus further improvement is needed.