[Effects of HPMCAS MF on absorption of silybin from supersaturable self-nanoemulsifying drug delivery system].

To evaluate the effects of Hydroxypropyl methylcellulose acetate succinate(HPMCAS MF) on absorption of silybin(SLB) from supersaturable self-nanoemulsifying drug delivery system which was pre-prepared at the early stage experiment. The cell toxicity of self-emulsifying preparation was evaluated by the MTT method, and the in vitro membrane permeability and absorption promoting effect of the self-emulsifying preparation were evaluated by establishing a Caco-2 cell monolayer model. The in vivo and in vitro supersaturation correlation was evaluated via the blood concentration of SLB. The results of MTT showed that the concentration of the preparation below 2 mg·mL~(-1)(C_(SLB) 100 µg·mL~(-1)) was not toxic to Caco-2 cells, and the addition of polymer had no significant effect on Caco-2 cells viability. As compared with the solution group, the transport results showed that the P_(app)(AP→BL) of the self-emulsifying preparation had a very significant increase; the transport rate of silybin can be reduced by polymer in 0-30 min; however, there was no difference in supersaturated transport between supersaturated SLB self-nanoemulsion drug delivery system(SLB-SSNEDDS) and SLB self-nanoemulsion drug delivery system(SLB-SNEDDS) within 2 hours. As compared with SLB suspension, pharmacokinetic parameters showed that the blood concentration of both SLB-SNEDDS and SLB-SSNEDDS groups were significantly increased, and C_(max) was 5.25 times and 9.69 times respectively of that in SLB suspension group, with a relative bioavailability of 578.45% and 1 139.44% respectively. C_(max) and relative bioavailability of SLB-SSNEDDS were 1.85 times and 197% of those of SLB-SNEDDS, respectively. Therefore, on the one hand, SSNEDDS can increase the solubility of SLB in gastrointestinal tract by maintaining stability of SLB supersaturation state; on the other hand, the osmotic transport process of SLB was regulated through the composition of its preparations, and both of them could jointly promote the transport and absorption of SLB to improve the oral bioavailability of SLB.

[Study on preparation extraction process of Linggui Zhugan Decoction].

To verify the appropriate preparation process of extracts for the solid substance benchmark of Linggui Zhugan Decoction. The extracts were prepared by different preparation processes, namely the traditional process(process 1), the extract combined with volatile oil separated from traditional process extract liquid(process 2), the modern secondary reflux extraction process(process 3) and the process that volatile oil was extracted first, then prepared according to the traditional process, and combined with extract(process 4); based on the characteristic spectrum, index components of cinnamaldehyde, glycyrrhizin, ammonium glycyrrhizinate, cinnamic acid, and the dry extract rate of process 1, the differences and similarities of four extracts were compared. The results showed that the similarity of the characteristic spectrum of process 2, process 4 and process 1 were all greater than 0.97, while there was no significant difference for the content of 4 quality control components and dry extract rate; the similarity of the characteristic spectrum of process 3 and process 1 was 0.91, the absolute peak area of 13 out of 21 peaks and the relative peak area of 7 peaks increased significantly, and the content of 3 out of 4 quality control components and dry extract rate also significantly increased. In conclusion, the material standards of extracts by the process 2 and 4 are consistent with that of the traditional process, so the two processes are suitable.

[Preparation and in vitro quality evaluation of curcumin supersaturated self-nanoemulsion].

In order to improve the supersaturation and maintenance time of drug dispersion in curcumin self-nanoemulsion(CUR-SNEDDS), precipitation inhibitors(PPIs) were introduced to prepare curcumin supersaturated self-emulsion(CUR-SSNEDDS). The composition of CUR-SNEDDS prescriptions was selected through the solubility test, the compatibility of oil phase and surfactant, the investigation of the emulsifying ability of the surfactant and the drawing of the pseudo-ternary phase diagram. Analytic hierarchy process was used in combination with central composite design-response surface method to optimize the prescription. The type and dosage of precipitation inhibitors(PPIs) were selected to maintain the supersaturated concentration and duration of CUR in artificial gastrointestinal fluids. At the same time, polarizing microscope was used to evaluate the crystallization inhibition effect and the quality and in vitro release behavior of CUR-SSNEDDS. The prepared CUR-SSNEDDS prescription was capryol 90-kolliphor RH40-transcutol HP-Soluplus(7.93∶66.71∶25.36∶5), with the drug loading of(65.12±1.25) mg·g~(-1). CUR-SSNEDDS was transparent yellow, and the nanoemulsion droplets were spherical with uniform distribution. The emulsification time was(21.02±0.13) s, the average particle size was(57.03±0.35) nm, the polydispersity index(PDI) was(0.23 ± 0.01), and the Zeta potential was(-18.10±1.30) mV. CUR-SSNEDDS significantly inhibited the generation and growth of crystals after in vitro dilution. The supersaturation could be maintained above 10 within 2 h, and the dissolution rate and degree of CUR in artificial gastrointestinal fluid were significantly increased. Soluplus could effectively maintain the supersaturated state of CUR and enhance CUR dissolution in vitro.

Study on expression of long non-coding RNA in colon cancer tissues and adjacent tissues / 中国病理生理杂志

AIM:To screen the differentially expressed long non-coding RNA(lncRNA)in colon cancer,and to explore its expression in colon cancer tissues and adjacent tissues.METHODS:The "Colon adenocarcinoma:Person neoplasm cancer status" which consisted of 36 cases of colon cancer tissues and 29 cases of normal colonic tissues was downloaded from the lncRNAtor database.The candidate genes were selected from these differentially expressed lncRNAs based on artificial criterion(P<0.01;fold change ≥2 or<0.5)and then validated by real-time PCR in 60 pairs of colon cancer tissues and adjacent tissues.RESULTS:A total of 50 lncRNAs were differentially expressed in colon cancer tis-sues,including 28 up-regulated and 22 down-regulated(P<0.01).The verifying results displayed that HNF1A-AS1 and ZDHHC8P1 were up-regulated(P<0.01),and SUZ12P expression was down-regulated(P<0.05),but the expression of AC069513.3 was not statistically significant between colon cancer tissues and adjacent tissues.The abilities of HNF1A-AS1,ZDHHC8P1,SUZ12P and AC069513.3 to discriminate the colon cancer from normal adjacent tissue by the ROC curve with an AUC of 0.729(sensitivity 78％,specificity 67％),0.617(sensitivity 68％,specificity 55％),0.689(sensitivity 66％,specificity 55％)and 0.518(sensitivity 52％,specificity 48％)were observed.CONCLUSION:Long non-coding RNA HNF1A-AS1 and ZDHHC8P1 are up-regulated and SUZ12P is down-regulated in colon cancer tis-sues,suggesting that they may be involved in the pathogenesis of colon cancer.

Effect of miR-542-3p on carcinogenesis induced by anti-benzo(a) pyrene-7,8-diol-9,10-epoxide / 中华预防医学杂志

<p><b>OBJECTIVE</b>To explore the effect of miR-542-3p in malignant transformation of human bronchial epithelial cells (16HBE) induced by anti-benzo(a)pyrene-7,8-diol-9,10-epoxide (anti-BPDE).</p><p><b>METHODS</b>The relative expression level of mature miR-542-3p in transformed cells (16HBE-T) and untransformed control cells (16HBE-N) was measured by real-time quantitative polymerase chain reaction (qRT-PCR). miRNA mimic was transiently transfected into 16HBE-T to change the expression level of miR-542-3p, and then the influenced changes of cell proliferation, cell cycle, apoptosis, and soft agar colony formation rate and the migration of transfected cells were analyzed.</p><p><b>RESULTS</b>Before transfection, the expression level of mature miR-542-3p in 16HBE-T was lower (39.08 ± 6.95)% than it in 16HBE-N (t = 15.18, P < 0.05). In comparison with the 16HBE-T group, the expression level of miR-542-3p in miR-542-3p mimic-transfected group was (5.23 ± 0.55) fold (t = 17.37, P < 0.05) after transfection. Cell proliferation of mimic-transfected group was decreased to (62.06 ± 5.61)% (t = -17.28, P < 0.05), percentage of cells in G(0)/G(1) phase up to (74.76 ± 4.86)% (t = 4.53, P < 0.05), rate of colony formation degrade to (5.87 ± 0.67)% (t = -6.66, P < 0.05), coverage areas ratio decreased to (0.31 ± 0.08) (t = -6.78, P < 0.05). There was no change with apoptosis.</p><p><b>CONCLUSION</b>Our studies showed that miR-542-3p played the role as a tumor suppressor, which led to a significant decrease in the proliferation capacity and degree of malignancy. These findings suggest aberrantly down-regulated miR-542-3p may be one critical factor that contributes to malignant transformation of 16HBE induced by anti-BPDE.</p>