According to the super-position principle of the reinforcement of biological activities, a series of novel E-substituted 2, 3-diaryl propenoic acyloxy phosphonate derivatives were designed and synthesized. And the structures of the target compounds were confirmed by IR, 1H NMR, 13C NMR and elemental analysis. Furthermore, the cytotoxicities of all compounds on A-549, SGC-7901 and EC-109 in vitro were evaluated by MTT assay, and some of them showed good antitumor activity. Among the active compounds, especially, the IC50 value of compound 3e was (12.7 ± 1.9) μmol x L(-1) against A-549 cells, similar to cisplatin [IC50 = (8.0 ± 1.5) μmol x L(-1)], compounds 3g and 3k had better inhibition effect on EC-109 cells growth, with the IC50 values of (9.5 ± 1.8) μmol x L(-1) and (11.5 ± 0.9) μmol x L(-1) respectively, and compounds 3i and 3k exhibited good cytotoxic property on A-549, SGC-7901 and EC-109, which were worth further investigation.

Objective To evaluate the changes in expression of NF-κB, IL-6 and TNF-α in spinal cord in a rat model of bone cancer. Methods Seventy-two female SD rats weighing 150-180 g were randomly divided into 3 groups (n = 24 each): control group (group C);sham operation group (group S) and bone cancer pain group (group BP). Bone cancer was induced by intra-tibial inoculation of 1 × 105 Walker 256 breast cancer cells. Paw withdrawal threshold to mechanical stimulation was measured with yon Frey filaments. The expression of NF-κB p65, IL-6 and TNF-α mRNA in the spinal cord was determined by RT-PCR and the expression of NF-κB p65 by immuno-histochemistry and NF-κB p65 positive cell count was determined. Results The paw withdrawal threshold was significantly lower and the expression of NF-κB p65, NF-κB p65 mRNA, IL-6 mRNA, TNF-α mRNA and NF-κB p65 positive cell count in the spinal cord were significantly higher in group BP than in group C and S ( P ＜0.05 or 0.01 ). Conclusion Intra-tibial inoculation of Walker 256 breast cancer cells activates NF-κB in the spinal cord, leading to the increased release of IL-6 and TNF-α and mechanical hyperalgesia.

Aim To pick out the siRNA which could most effectively inhibit the expression of TLR4 in microglial cells and to detect the cytotoxicity of the transfection complex.Methods Five siRNAs were chemicaly synthesized:four of them were used to inhibit TLR4 expression in microglial cells,the rest was fluorescence-labeled mismatch siRNA as a nagative control.They were all transfected into microglial cells,respectively.TLR4 mRNA was detected 24 h after transfection by RT-PCR and its protein expression wasobserved by Western blot 48 h later.The cytotoxicity of complex was detected using MTT.Results ① The transfection rate was high enough in microglial cells with siRNA(40 pmol)and LipofectamineTM 2000(1 μl).② The TLR4 siRNA pool reduced TLR4 mRNA by 85%(siRNA_(439)),73%(siRNA_(312)),67%(siRNA_(1495))and 33%(siRNA_(2062))respectively compared with mismatch siRNA-treated group 24 h after transfection in a microglial cell line.③ The TLR4 siRNA439 was the most effective siRNA(P<0.01).④ The cell survival rates were above 85% in the groups of Lipofectamine~(TM) 2000 1 μl compound less than 40 nmol·L~(-1) siRNA.Conclusions ① The TLR4 siRNA_(439) can inhibit TLR4 expression most effectively in microglial.② 40 nmol·L~(-1) siRNA and 1 μl Lipofectamine~(TM) 2000 have low cytotoxicity,which are suitable for transfection.

Objective:To identify the effective concentrations of Ropivacaine in the modified fascial iliac compartment block(FICB)that would not affect the movement of the affected limb but would offer effective pain relief after total knee arthroplasty(TKA)in elderly patients.In addition, adverse reactions within 24 hours of FICB were examined.Methods:This study was a prospective, single-arm sequential trial.Forty-five elderly patients treated with TKA at the First Affiliated Hospital of Soochow University between September 2021 and March 2022 were selected, with an American Society of Anesthesiologists(ASA)score of Ⅰ or Ⅱ.All patients were given ultrasound-guided FICB on the surgical side under general anesthesia and 10 minutes before the operation, and the injection volume was 30 ml.According to preliminary experiments and relevant literature, the initial concentration of Ropivacaine was 0.1%, and the concentration for the next patient was determined using a modified Dixon sequential method.If the quadriceps femoris muscle strength score of the first patient was ≥4, there was no resting pain[visual analogue scale(VAS)score ≤1], and the VAS score during activity was ≤3, the concentration for the next patient would be reduced.Conversely, the concentration would be increased.The Ropivacaine concentration was increased or decreased by 0.01% each time and the trial would be stopped after 12 reentries.The median effective concentration(ED50), 95% effective concentration(ED95)and corresponding 95% confidence interval(CI)of ropivacaine were calculated using the probit model.Meanwhile, adverse reactions within 24 hours of FICB were monitored.Results:Of 43 elderly patients who completed the trial, the intervention was effective in 23 and ineffective in 20.While ensuring that postoperative limb movement in elderly patients was not affected, a single injection of 30 ml ropivacaine through FICB was able to effectively inhibit postoperative pain, and the ED50 and ED95 of ropivacaine were 0.072%(95% CI: 0.065%-0.078%)and 0.093%(95% CI: 0.084%-0.124%), respectively.Within 24 hours of FICB, 2 patients had lower limb weakness and could not get out of bed and walk, and 5 patients had severe pain and needed additional analgesics.No other adverse reactions were found. Conclusions:The effective ED50 and ED95 of Ropivacaine for postoperative pain relief in elderly patients after TKA are 0.072% and 0.093%, respectively.And the incidence of adverse reactions is low.

Objective To explore the antiviral effect and mechanism of interferon-α (IFN-α) in chronic HBV infection mouse model by hydrodynamic tail vein injection. Methods Chronic HBV infection mouse model was constructed with C57BL/6j mice by hydrodynamic tail vein injection of pAAV-HBV1.2 plasmid. Serum IFN-α was determined by ELISA after injection of IFNα- expressing plasmid (i.e., plasmid pKCMvint.IFN-α-2a) or control plasmid pKCMvint. HBsAg and HBeAg levels were assayed on Abbot ARCHITECT i2000SR. Total lymphocytes in liver or spleen were counted and the frequency and function of CD8+T cells and HBV-specific CD8+T cells were analyzed by flow cytometry. Results Serum IFN-α expression level was significantly higher in the animals injected with pKCMvint.IFN-α-2a plasmid than in control group (P＜0.01). Serum HBsAg decreased quickly 12 days after injection and significantly lower than control group. Serum HBeAg was undetectable after IFN-α expression. Interestingly, the frequency of CD8+T cells in the liver of animals injected with pKCMvint.IFN-α-2a plasmid was significant higher than control group (P＜0.05), while total liver lymphocytes and HBV-specific CD8+T cells had a similar trend. Consistently, the HBV-specific CD8+T cells in IFN-α-expressing animals showed higher level of producing IFN-γ, TNF-α and IL-2 than control group. IFN-γ production was significantly different between IFN-α- expressing group and control group (P＜0.05). Conclusions IFN-α can increase the frequency and function of liver CD8+T cells to inhibit HBV gene expression in chronic HBV infection mouse model.

Objective:To construct a Soochow University model of comfortable medical procedures during peri-anesthesia period for patients undergoing radical resection of lung cancer through thoracoscope.Methods:In this prospective study, eight hundreds and sixty patients undergoing radical resection of lung cancer through thoracoscope were enrolled in our hospital in 2018.During peri-anesthesia period, the 860 patients were randomly(by the random number table method)divided into the control group(the group C receiving routine medical procedures, n=430)and the comfort group(the group S receiving the comfortable medical procedures of Soochow University model, n=430). The scores of Visual Analogue Scale(VAS), Richmond Agitation-Sedation Scale(RASS), and Thirsty Analogue Scale(TAS)were recorded at 5 min after extubation(T1), at out of the post-anesthesia care unit(T2), at 1 h(T3), 6 h(T4), 12 h(T5), 24 h(T6), 2 d(T7)and 3 d after surgery(T8)in two groups.The incidences of postoperative sore throat(POST), nausea and vomiting(PONV), catheter-related bladder discomfort(CRBD), thirst and hypothermia were recorded at T2, T6 and T8, respectively.Meanwhile, the peri-anesthesia comfort questionnaire(PCQ)and peri-anesthesia satisfaction questionnaire(PSO)were completed at T6 and T8.Results:The incidences of POST(48.6% vs.16.2%), PONV(24.9% vs.13.0%), CRBD(78.8% vs.20.9%)and thirst(74.9% vs.20.0%)were higher in the group C than in the group S at T2( P<0.05). The comfort score and satisfaction score were lower in the group C than in the group S at T6(3.14±1.04 vs.4.92±1.42, 2.67±0.89 vs.3.30±1.01)and at T8(3.84±1.83 vs.5.05±1.77, 2.74±0.84 vs.3.26±1.06)( P<0.05). Conclusions:The Soochow University model of comfortable medical procedures during peri-anesthesia period for patients undergoing radical resection of lung cancer through thoracoscope has been successfully constructed, and this model can reduce the incidence of complications, and improve the comfort and satisfaction during peri-anesthesia period.

Objective To characterize the distribution and assess the exposure to phthalic acid esters （PAEs） in the indoor dust of Shanghai City. Methods Samples were collected from 33 sampling sites， including homes， hotels， offices and public places， in Shanghai in 2018， 2019， and 2020. The samples were pretreated by 100 sieves， extracted and concentrated， and then analyzed by gas chromatography-mass spectrometry in selected ion mode （SIM）. Results Results on the characteristics of PAEs in indoor dust in different places showed that concentrations of PAEs were in a range of <0.01-2 464 mg·kg^-1.The average concentration of 16 PAEs was 613 mg·kg^-1. Bis（2-ethylhexyl） phthalate （DEHP）， di-iso-butyl phthalate （DiBP）， di-n-butyl phthalate （DBP） and di-n-octyl phthalate （DnOP） were the main components of PAEs in indoor dust， accounting for approximately 99.5% of 16 PAEs. The intake of DEHP， DBP， DEP and BBP was lower than the tolerable daily intake （TDI） and reference doses （RfD） set by EU CSTEE and U.S. EPA. Conclusion Average daily dose （ADD） via indoor dust is estimated， and the order of intake through different pathways is hand-oral intake>skin contact>respiratory inhalation. Exposure risk of PAEs in children is greater than that in adults.