ABSTRACT
It is shown that phytochemicals have a protective effect on colon cancer. Curcumin, polysaccharides (apple polysaccharides, mushroom glucans), saponins (paridis saponins, ginsenosides), resveratrol, quercetin and other plant drugs can inhibit colon cancer cell proliferation and promote cell apoptosis through different signaling pathways. In addition, it also has anti-inflammatory, antioxidant, anti-angiogenesis, reduce the toxic side effects of chemotherapy drugs, and reverse the drug resistance of tumor cells. Understan-ding the prevention and cure effect of plant medicine on colon cancer and its possible mechanism can provide more theoretical basis and therapeutic ideas for the clinical prevention and cure of colon cancer.
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OBJECTIVE:To screen the α-glucosidase inhibitory active part from Pothos chinensis. METHODS:The aqueous extractions of P. chinensis were extracted by petroleum,ethyl acetate,n-butyl alcohol in turn to obtain different polarparts. Effect of each part on α-glucosidase inhibitory activity was determined,and enzyme inhibition kinetics was conducted for the screened parts with strong activity and relatively high yield rate;effects of each part on blood glucose level of mice loaded with glucose,su-crose and starch were respectively determined (using Acacoside tablet as positive control). RESULTS:Enzyme inhibition kinetics in vitro showed the ethyl acetate part [yield rate was 0.40%,enzyme activity inhibition rate was(72.90±2.85)%] had strongα-glu-cosidase inhibitory activity and showed a dose-dependent,fast,non-competitive and reversible model. Results of in vivo glucose tol-erance indicated that Acacoside tablet and each part of P. chinensis had no effects on blood glucose level of glucose-loaded mice (P>0.05);while Acacoside tablet and ethyl acetate part in P. chinensis could reduce 30,60 min blood glucose level of su-crose-loaded mice and 30,60,120 min blood glucose level of starch-loaded mice(P<0.05 or P<0.01). CONCLUSIONS:Ethyl acetate part is theα-glucosidase inhibitory active part from Yao medicine P. chinensis.
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OBJECTIVE:To prepare Polygala fallax rapidly disintegrating oral tablets and investigate its in vitro dissolution. METHODS:The rapidly disintegrating tablets was prepared by direct powder compression method. Using disintegration time as in-dex,the ratio of stuffing bulking agent mannitol to disintegrating agent microcrystalline cellulose,the amount of drug extract,the amount of lubricant magnesium stearate and other influential factors were investigated by single factor test and orthogonal test. The drug dissolution effect of prepared tablet(using senegenin as substance control)was evaluated by in vitro dissolution test(using wa-ter as dissolution medium,paddle method). RESULTS:The optimal formulation was that the amount of drug extract was 15%;the ratio of mannitol to microcrystalline cellulose was 1.5:1;the amount of magnesium stearate was 1.0%. The disintegration time of prepared tablet was(31±4)s;tablet hardness was(3.4±0.2)kg;tablet friability was(0.23±0.07)%(RSD<0.11%,n=3). Ac-cumulative dissolution rate of total saponins was more than 90% within 5 min. The dissolution parameters T50 was equal to 0.84 min and Td was equal to 1.77 min. CONCLUSIONS:Polygala fallax rapidly disintegrating oral tablets will dissolve quickly and dis-integrate rapidly in aqueous solution.
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AIM:To explore the promoting action of chloroquine on the anti-proliferation effect of dexametha-sone on acute lymphoblastic leukemia cells .METHODS:CCK-8 assay was used to assess the viability of the dexametha-sone-resistant human acute lymphoblastic leukemia CEM-C1 cell line treated with the combination of chloroquine and dexa-methasone .Western blotting , quantitative real-time PCR and LysoTracker Red staining were utilized to examine the mecha-nism.RESULTS:Combination of chloroquine and dexamethasone significantly inhibited the proliferation of CEM -C1 cells compared with control group (P<0.01).The combination of chloroquine and dexamethasone increased the abundance of glucocorticoid receptor and inhibited lysosomal function , while lysosomal inhibitor bafilomycin A 1 also increased glucocorti-coid signaling .CONCLUSION:Dexamethasone combined with chloroquine triggers an anti-proliferation effect on CEM-C1 cells via a lysosome-mediated pathway .