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Objective:To investigate the clinical efficacy of 125I seed implantation combined with anlotinib hydrochloride in the treatment of non-small cell lung cancer (NSCLC). Methods:61 cases of NSCLC patients were enrolled, of which 30 cases (observation group) received 125I seed implantation combined with anlotinib treatment, and 31 cases (control group) received 125I seed implantation only. To evaluate the curative effect and adverse reactions of all patients, the carcinoembryonic antigen (CEA), cytokeratin 19 fragment (CYFRA21-1), neuroendocrine enolase (NSE), squamous cell carcinoma antigen (SCC) in the peripheral blood of the two groups was measured before the treatment and at 1 and 3 months after the treatment. Results:The effective rates in the observation group were 90.00% and 93.33%, the effective rates in the control group were 67.74% and 74.19% at 1 and 3 months after the treatment, respectively, and the difference in efficacy between the two groups was statistically significant ( χ2=4.504, P=0.034 vs. χ2=4.075, P=0.044). There was no significant difference in the incidence of adverse reactions between the two groups of patients after treatment ( P=0.785). At 1 and 3 months after the treatment, the levels of CEA, CYFRA21-1, NSE and SCC in the peripheral blood of the two groups of patients were lower than those before the treatment (all P<0.05). Conclusions:125I seed implantation combined with anlotinib hydrochloride is safe for the treatment of advanced non-small cell lung cancer, and has promotion value.
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Fritillaria thunbergii Miq. has been widely used in traditional Chinese medicine for its expectorant, antitussive, antiinflammatory and analgesic properties. Moreover, modern pharmacological studies have demonstrated that F. thunbergii Miq. has efficacy in the treatment of leukemia and cancers of the liver and cervix. Although the alkaloid, peimine, is largely responsible for these pharmacological effects, it has very low oral bioavailability. The aim of this study was to investigate the intestinal absorption of peimine in Caco-2 cell monolayers. Having demonstrated that peimine is non-toxic to Caco-2 cells at concentrations <200 μmol/L, the effect of peimine concentration, pH, temperature, efflux transport protein inhibitors and EDTA-Na2 on peimine transport were studied. The results show that peimine transport is concentration-dependent; that at pH 6.0 and 7.4, the P app(AP-BL) of peimine is not significantly different but the P app(BL-AP)) is; that both P app(AP-BL) and P app(BL-AP) at 4 °C are significantly higher than their corresponding values at 37 °C; that the P-glycoprotein (P-gp) inhibitors, verapamil and cyclosporin A, increase absorption of peimine; and that EDTA-Na2 has no discernible effect. In summary, the results demonstrate that the intestinal absorption of peimine across Caco-2 cell monolayers involves active transport and that peimine is a substrate of P-gp.
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ABSTRACT:The aim of the present study was to investigate the inhibitory effects of TLR7 on Mycobacterium tuberculosis . TLR7 on infected RAW264 .7 cells was activated by chemical synthesis of TLR7 activation motif ssRNA .Activated RAW264 .7 cells were inoculated with Mycobacterium tuberculosis ,quantitative PCR method was applied to detect the phagocytosis rate of cell to bacteria at different time after infection .Cytokine production was measured by ELISA from cell supernatant .Cells were cultured on Roche medium and counted after sterile cracked with TritonX‐100 and diluted with PBS .Scanning electronic micro‐scope ( SEM ) was applied to detect the morphological changes of cells treated with TLR7 activation motif ssRNA .The highest phagocytosis rate of bacteria of RAW264 .7 cells was at 3 hours post infection (P>0 .05) .Compared with that of the control group ,treatment after 36 hours intracellular bacterial quantity in ssRNA treated group was lower (P<0 .05) ,levels of IL‐12 (P<0 .05) and IL‐4 (P<0 .05) were increased .For treatment after 48 hours ,level of IL‐4 (P<0 .05) was decreased ,and TNF‐α (P<0 .05) was increased .For treatment after 3 hours ,cell morphology of the ssRNA group was obviously better than the control group and appeared lots of phagosomes .Results suggested that TLR7 could enhance macrophages in killing Myco‐bacterium tuberculosis by forming phagosomes and regulating cytokines production ,and TLR7 activation motif ssRNA could be used in the treatment of tuberculosis .
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To study the in situ intestinal absorption kinetics and compatibility influence of peimine and peiminine in rats, the absorption of peimine and peiminine in small intestine (duodenum, jejunum and ileum) and colon of rats was investigated using in situ single-pass perfusion method and the drug content was measured by HPLC-ELSD. Perfusion rate, pH, concentration of drug, gender and bile duct ligation can significantly affect the absorption of peimine and peiminine, the Ka, and Papp values in the condition of pH 6.8 and pH 7.4 had significant difference (P 0.05). Bitter almonds and licorice can significantly reduce the absorption of peimine and peiminine with the usual dose (P 0.05). Experimental results show that the absorption features of peimine and peiminine are basically the same, both of them could be absorbed at all segments of the intestine in rats and had no special absorption window, and with significant differences between male and female individuals. The absorption of peimine and peiminine complies with the active transport and facilitated diffusion in the general intestinal segments. Bitter almond and licorice can reduce the intestinal absorption rate ofpeimine and peiminine.
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The purpose of the study was to investigate the impact of rat cytomegalovirus(RCMV) infection on the development of the nervous system in rat embryos,and to evaluate the involvement of Wnt signaling pathway key molecules and the downstream gene neurogenin 1(Ngn1) In RCMV infected neural stem cells(NSCs).Infection and control groups were established,each containing 20 pregnant Wistar rats.Rats in the infection group were inoculated with RCMV by intraperitoneal injection on the first day of pregnancy.Rat E20 embryos were taken to evaluate the teratogenic rate.NSCs were isolated from E13 embryos,and maintained in vitro.We found:1) Poor fetal development was found in the infection group with low survival and high malformation rates.2) The proliferation and differentiation of NSCs were affected.In the infection group,NSCs proliferated more slowly and had a lower neurosphere formation rate than the control.The differentiation ratio from NSCs to neurons and glial cells was significantly different from that of the control,showed by immunofluorescence staining.3) Ngn1 mRNA expression and the nuclear β-catenin protein level were significantly lower than the control on day 2 when NSCs differentiated.4) The Morris water maze test was performed on 4-week pups,and the infected rats were found worse in learning and memory ability.In a summary,RCMV infection caused abnormalities in the rat embryonic nervous system,significantly inhibited NSC proliferation and differentiation,and inhibited the expression of key molecules in the Wnt/β-catenin signaling pathway so as to affect NSCs differentiation.This may be an important mechanism by which RCMV causes embryonic nervous system abnormalities.
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Objective To study the optimum parameters of the supercritical CO2 fluid extraction of Polyrhachis vicina Roger and chemical constituents of ant oil. Methods The experiments were designed with the uniform design. Three factors are extraction pressure, temperature and time. GC-MS was applied for analyzising. Results The optimum condition was obtained:the extraction pressure is 36 MPa, the temperature of extraction is 40 ℃ and extraction time is 50min. 45 components were identified from 60 chromatographic peaks. The main chemical constituents were (Z)-9-octadecenoicacid (48.278%), hexadecanoicacid (17.574%), (Z)-9-hexadecenoi (4.912%), cholesterol (2.957%). There are some linear paraffin in ant oil. Conclusion This method can extract the ant oil from Polyrhachis vicina Roger quickly and efficiently. This experiment provide foundation for exploitation and utilization of ant resource.