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OBJECTIVE:To prepare argininate betulinic acid,and to investigate the effect of the proliferation of triple-negative human breast cancer cell MDA-MB-231. METHODS:By using argininate as the solubilization carrier,argininate betulinic acid was prepared by co-grinding equal molar ratio of betulinic acid and argininate. The argininate betulinic acid was characterized with powder X-ray diffractometry,infrared spectroscopy and differential scanning calorimetry. The solubility of betulinic acid and argininate betulinic acid were compared. MTT method was used to assay the effects of 15,30,60,120 μ g/mL betulinic acid, argininate betulinic acid and 5-FU on the proliferation of MDA-MB-231 cell. RESULTS:Prepared argininate betulinic acid was a new phase which was different from the physical mixing of argininate and betulinic acid,among which carboxyl group of betulinic acid and amino group of argininate formed as a salt,and the salt had no obvious melting peak. Betulinic acid was almost insoluble in water. The solubility of betulinic acid in argininate betulinic acid aqueous solution was 50.72 μg/mL. Compared with betulinic acid,the inhibitory rate of argininate betulinic acid on the growth of MDA-MB-231 cell was increased significantly(P<0.05), there was no statistical significance between its effect and 5-FU(P>0.05). CONCLUSIONS:Argininate betulinic acid with good solubility is prepared successfully,and can inhibit the proliferation of MDA-MB-231 cell.
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Objective To establish a novel method to determine the absolute content of quercetin by proton nuclear magnetic resonance (qNMR).Methods DMSO-d6 was employed as solvent,and maleic acid as an internal standard.Proton signal peaks at δ7.50-7.58 and δ6.26 of maleic acid were served as quantification peaks.The content of quercetin is determined with qNMR in comparison with the results obtained by mass balance method.Results Linear regression of quantitative peak areas ratio (As/Ar) of quercetin-maleic acid vs mass ratio (ms/mr) yielded a correlation coefficient of 0.999 3 and a regression equation ofy =2.963 x + 0.134 1.The contents of three batches quercetin were 85.20％,84.93％,and 85.27％,the average was 85.13％ and its RSD was 0.21％.The results were generally consistent with that of mass balance methods.Conclusion This method was easy and simple to handle,and the analysis results were accurate.It could be the complementary for the mass balance method.
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Objective To prepare,characterize glycyrrhetinic acid lysinate,and study the solubilization and inhibitory action antitumor activity of glycyrrhetinic acid lysinate on cell proliferation of colorectal cancer cell line HCT-8. Methods Glycyrrhetinic acid lysinate was prepared by co-grinding glycyrrhetinic acid with lysine in 1∶1 molar mixture for 10 hours. Characterization of glycyrrhetinic acid lysinate was achieved by X-ray powder diffraction, infrared spectroscopy, and ultraviolet spectrum techniques.HPLC method was used to study the solubilization of glycyrrhetinic acid lysinate.The MTT method was used to assay the inhibitory action of glycyrrhetinic acid lysinate on cell proliferation. Results The solubility of glycyrrhetinic acid lysinate was enhanced 260 folds,compared with glycyrrhetinicacid in water. The inhibitory cell proliferation action on HCT-8 of glycyrrhetinic acid lysinate was 7 times higher than that of glycyrrhetinic acid. Conclusion The satisfactory water solubility and antitumor activity of glycyrrhetinic acid lysinate will be potentially useful for its application as a new pharmaceutical formulation in cancer treatment in the future.
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Purpose To investigate the clinicopathological features, histogenesis, morphological characteristics, immunophenotypes and differential diagnosis of primary extragonadal yolk sac tumor ( eYST) . Methods Clinicopathological data, morphological charac-teristics and immunophenotypes results of 40 cases of eYST were retrospectively studied and the relevant literatures were reviewed. Re-sults All 40 patients, which included 24 male and 16 female, aged from 6 months to 42 years with a 12 years average age and 17 (42.5%) cases were over 12 years old. Mediastinum, sacrococcygeal, retroperitoneal, pineal gland and vagina were involved in 16 (40.0%), 12(30.0%), 5(12.5%), 4(10.0%) and 3(7.5%), respectively. All 40 cases included 32(80.0%) cases pure YSTs, while other 8(20.0%) cases contained other one or two types of germ cell tumor (GCT) components. Conclusions Primary eYST is rare, mediastinum and sacrococcygeal are the most common anatomic sites for eYST, and these mediastinal tumor patients are overwhelmingly confined to adult males, whose average age are significantly older than that in sacrococcygeal, retroperitoneal, pineal gland and vaginal tumor patients (P<0.05), while other sites eYST are restricted to prepubertal children. Adult eYST contain other types of GCT components in some cases, and children's counterparts are always pure YST. Extragonadal eYST manifestate pleomorphic histological features, which combine with immunohistochemical markers is definite value for diagnosis, differential diagnosis.
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Objective To study the therapeutic effect and mechanism of Dicliptera chinensis polysaccharide ( DCP) on liver injury induced by antituberculosis drugs. Methods Sixty mice were randomly divided into six groups, namely normal control group, model group, glucurolactone group (in the dosage of 200 mg·kg-1·d-1), and high-, middle- and low-dose DCP groups ( in the dosage of 600, 400, 200 mg·kg-1·d-1, respectively). Except for the normal control group, the rats in the other groups were given intragastric administration of isoniazid and rifampicin ( 100 mg/kg) to induce liver injury model, and were simultaneously treated with corresponding agents, once a day. On the experiment day 30, the blood and liver tissue were sampled. The serum levels of alanine aminotransferase ( ALT) , aspartate aminotransferase ( AST) , alkaline phosphatase ( AKP) and microsomal nitric oxide ( NO) were detected by biochemical method. The contents of tumor necrosis factor alpha (TNF-α) and interleukin 6 (IL-6) in liver tissue were determined by enzyme-linked immunosorbent assay ( ELISA) , and the hepatic histopathology was observed after HE staining. Results In DCP groups, the hepatic pathological changes of the mice were improved, the number of the inflammatory cells was reduced, and the activities of serum ALT, AST and AKP as well as the contents of hepatic TNF-α, IL-6 and NO were reduced ( P<0.05 or P<0.01 compared with those in the model group). Conclusion Dicliptera chinensis polysaccharide is effective for liver injury induced by antituberculosis drug, and the mechanism may be associated with its anti-inflammatory action.