Evaluation of apoptotic effects of mPEG-b-PLGA coated iron oxide nanoparticles as a eupatorin carrier on DU-145 and LNCaP human prostate cancer cell lines / 药物分析学报

Many studies have so far confirmed the efficiency of phytochemicals in the treatment of prostate cancer.Eupatorin,a flavonoid with a wide range of phytomedical activities,suppresses proliferation of and in-duces apoptosis of multiple cancer cell lines.However,low solubility,poor bioavailability,and rapid degradation limit its efficacy.The aim of our study was to evaluate whether the use of mPEG-b-poly(lactic-co-glycolic)acid(PLGA)coated iron oxide nanoparticles as a carrier could enhance the therapeutic efficacy of eupatorin in DU-145 and LNcaP human prostate cancer cell lines.Nanoparticles were prepared by the co-precipitation method and were fully characterized for morphology,surface charge,particle size,drug loading,encapsulation efficiency and in vitro drug-release profile.The inhibitory effect of nanoparticles on cell viability was evaluated by MTT test.Apoptosis was then determined by Hoechest staining,cell cycle analysis,NO production,annexin/propidium iodide(PI)assay,and Western blotting.The results indicated that eupatorin was successfully entrapped in Fe3O4@mPEG-b-PLGA nanoparticles with an efficacy of(90.99 ± 2.1)％.The nanoparticle's size was around(58.5 ± 4)nm with a negative surface charge[(-34.16 ± 1.3)mV].In vitro release investigation showed a 30％initial burst release of eupatorin in 24 h,followed by sustained release over 200 h.The MTT assay indicated that eupatorin-loaded Fe3O4@mPEG-b-PLGA nanoparticles exhibited a significant decrease in the growth rate of DU-145 and LNcaP cells and their IC50 concentrations were 100 μM and 75 μM,respectively.Next,apoptosis was confirmed by nuclear condensation,enhancement of cell population in the sub-G1 phase and increased NO level.Annexin/PI analysis demonstrated that eupatorin-loaded Fe3O4@mPEG-b-PLGA nanoparticles could increase apoptosis and decrease necrosis frequency.Finally,Western blotting analysis confirmed these results and showed that Bax/Bcl-2 ratio and the cleaved caspase-3 level were up-regulated by the designing nanoparticles.Encapsulation of eupatorin in Fe3O4@mPEG-b-PLGA nanoparticles increased its anticancer effects in prostate cancer cell lines as compared to free eupatorin.Based on these results,this formulation can provide a sustained eupatorin-delivery system for cancer treatment with the drug remaining active at a significantly lower dose,making it a suitable candidate for pharmacological uses.

Study on chemical constituents of Artemisia integrifolia / 中草药

Objective: To study the chemical constituents from the aerial parts of Artemisia integrifolia. Methods: The chemical constituents were separated and purified by column chromatographies and HPLC. Their structures were determined on the basis of spectroscopic analyses (1H-NMR, 13C-NMR, 2D-NMR, and MS). Results: Fifteen compounds were isolated from the methanol extract in the aerial parts of A. integrifolia with the structures identified as α-curcumene (1), β-sitosterol-3-O-β-D-glucoside (2), zingiberone (3), 3-(2-hydroxyphenyl) propanoic acid methyl ester (4), (E)-o-hydroxycinnamic acid (5), eupatorin (6), cirsimaritin (7), artemetine (8), loliolide (9), luteolin-7-O-β-D-glucopyranoside (10), (+)-pinoresinol (11), α-spinasterol (12), reynosin (13), 3α-hydroxy-1(10),4,11(13)-diager-12,6α-olide (14), and scopoletin (15). Conclusion: Compounds 1 and 3 are isolated from the plants of Artemisia Linn for the first time and compounds 4-9, 11, 13, and 14 are isolated from this plant for the first time.

Determination of Three Active Flavones in Orthosiphon stamineus by HPLC / 医药导报

Objective To develop a method for content determination of sinensetin,eupatorin,and 3′-hydroxy-5,6,7, 4′-tetramethoxyflavone in Orthosiphon stamineus. Methods The determination was carried out on a Symmetry C18 column (4.6 mm×250 mm,5 μm) by HPLC.The mobile consisted of acetonitrile and water containing 0.05% H3 PO4 in gradient elution. The flow rate was 1 mL?min-1 ,the column temperature was 30 ℃ ,the detected wavelength was set at 365 nm, and the injection volume was 10 μL. Results The peak areas and the sample quantity of the three components presented good linear relationship in the range of 0. 50 - 5. 00 μg for sinensetin,0. 50 - 5. 00 μg for eupatorin, and 0. 05 - 0. 50 μg for 3′-hydroxy-5,6,7,4′-tetramethoxyflavone.The average recoveries were 101.26%,100.28% and 99.66%,respectively. RSD were 1.73%, 0.82% and 1.67%, respectively. Conclusion The method is proved to be simple,accurate and can be used for the quality evaluation of Orthosiphon stamineus.