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Feng-Qian Li,Rui-Rui Ji,Xu Chen,Ben-Ming You,Yong-Hua Pan,Jia-Can Su 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.12
To control the release rate and mask the bitter taste, cetirizine dihydrochloride (CedH) was entrapped within chitosan nanoparticles (CS-NPs) using an ionotropic gelation process, followed by microencapsulation to produce CS matrix microparticles using a spray-drying method. The aqueous colloidal CS-NPs dispersions with a drug encapsulation efficiency (EE) of <15%, were then spray dried to produce a powdered nanoparticles-in-microparticles system with an EE of >70%. The resultant spherical CS microparticles had a smooth surface, were free of organic solvent residue and showed a diameter range of 0.5~5 μm. The in vitro drug release properties of CedH encapsulated microparticles showed an initial burst effect during the first 2 h. Drug release from the matrix CS microparticles could be retarded by the crosslinking agent pentasodium tripolyphosphate or the wall material. The technique of ‘ionotropic gelation’ combined with ‘spray-drying’ could be applicable for preparation of CS nanoparticlesin-microparticles drug delivery systems. CS-NPs based microparticles might provide a potential micro-carrier for oral administration of the freely water-soluble drug - CedH.
Qian, Ying-Ying,Liu, Xin-You,Wu, Qian,Song, Xian,Chen, Xiao-Feng,Liu, Yi-Qian,Pei, Dong,Shen, Li-Zong,Shu, Yong-Qian Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.19
Background: Although the predictive value of the excision repair cross-complementing group 1 (ERCC1) C118T polymorphism in clinical outcomes of patients with colorectal cancer (CRC) receiving oxaliplatin-based chemotherapy has been evaluated in numerous published studies, the conclusions are conflicting. Therefore, we performed the present meta-analysis to determine the precise role of the ERCC1 C118T polymorphism in this clinical situation and help optimize individual chemotherapy. Materials and Methods: A multiple search strategy was used to identify eligible studies. Pooled odds ratios (ORs) and their 95% confidence intervals (CIs) were used to estimate objective response and oxaliplatin-induced toxicity, with hazard ratios (HRs) with 95%CIs for progression-free survival (PFS) and overall survival (OS). Results: A total of 22 studies including 2,846 CRC patients were eligible in the analysis. Overall, no significant correlation was found between the ERCC1 C118T polymorphism and objective response to oxaliplatin-based chemotherapy, in all patients or in the Asian and Caucasian subgroups. However, the pooled analysis showed that the PFS and OS were significantly shorter in patients who carried T/T or T/C genotypes of ERCC1 C118T as compared to the C/C genotype. On stratified analysis by ethnicity, the ERCC1 118T allele was associated with a favorable prognosis in Caucasians (PFS, HR=0.58, 95%CI: 0.24-1.44; OS, HR=0.38, 95%CI: 0.22-0.64) but an unfavorable prognosis in Asians (PFS, HR=2.49, 95%CI: 1.87-3.33; OS, HR=2.63, 95%CI: 1.87-3.69) based on a dominant model. In addition, we failed to find a statistically significant impact of ERCC1 C118T polymorphism on oxaliplatin-induced toxicity. Conclusions: The ERCC1 C118T polymorphism may have prognostic value in patients with CRC undergoing oxaliplatin-based chemotherapy.
Saroclazines A–C, thio-diketopiperazines from mangrove-derived fungi Sarocladium kiliense HDN11-84
Feng Li,Wenqiang Guo,Li Wu,Tian-jiao Zhu,Qian Qun Gu,De-Hai Li,Qian Che 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.1
Three new diketopiperazine derivatives (DKPs), saroclazines A–C (1–3) along with three known DKPs (4– 6) were isolated from mangrove-derived fungi Sarocladium kiliense HDN11-84. Saroclazines A–B (1 and 2) possessed a free amide structure, which was first found in sulfurcontaining aromatic DKPs. Their structures were elucidated by NMR, HRESIMS and X-ray. The cytotoxic activity of new compounds (1–3) was tested against HeLa cell lines, among which compound 2 showed an IC50 value of 4.2 lM.
Qian, Ying-Ying,Liu, Xin-You,Pei, Dong,Xu, Jia-Li,Shen, Hua,Chen, Xiao-Feng,Liu, Yi-Qian,Shen, Li-Zong,Shu, Yong-Qian Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.22
Background: The predictive value of the xeroderma pigmentosum group D (XPD) Lys751Gln polymorphism regarding clinical outcomes of patients with colorectal cancer (CRC) receiving oxaliplatin-based chemotherapy has been evaluated in numerous published studies, but the results remain inconclusive. Therefore, we performed a meta-analysis to determine the precise role of the XPD Lys751Gln polymorphism in this clinical situation and optimize individual chemotherapy. Materials and Methods: A multiple search strategy was used to identify eligible studies. Pooled odds ratios (ORs), generalized odds ratio (ORG) and their 95% confidence intervals (CIs) were used to estimate the objective response, while hazard ratios (HRs) with 95%CIs were used for progression-free survival (PFS) and overall survival (OS). Results: A total of 17 studies including 2,286 patients met the inclusion criteria. Overall, the XPD 751Gln allele was associated with a non-significant reduced objective response to oxaliplatin-based chemotherapy in all patients or in the Asian and Caucasian subgroups. However, poor PFS and OS of CRC patients treated with oxaliplatin-based regimens were significantly related to the XPD 751Gln allele in the dominant model (PFS: HR=2.10, 95%CI: 1.65-2.67; OS: HR=3.18, 95%CI: 1.57-6.47). On stratified analysis by ethnicity, these relationships were more pronounced in Asians (PFS: HR=2.49, 95%CI: 1.79-3.47; OS: HR=5.25, 95%CI: 3.46-7.94) than in Caucasians (PFS: HR=1.73, 95%CI: 1.22-2.46; OS: HR=1.78, 95%CI: 1.06-2.99). Conclusions: The XPD Lys751Gln polymorphism may have prognostic value in patients with CRC undergoing oxaliplatin-based chemotherapy.
FSCB phosphorylation in mouse spermatozoa capacitation
( Shun Li Liu ),( Bing Ni ),( Xiang Wei Wang ),( Wen Qian Huo ),( Jun Zhang ),( Zhi Qiang Tian ),( Ze Min Huang ),( Yi Tian ),( Jun Tang ),( Yan Hua Zheng ),( Feng Shuo Jin ),( Yan Feng Li ) 생화학분자생물학회(구 한국생화학분자생물학회) 2011 BMB Reports Vol.44 No.8
It is generally accepted that spermatozoa capacitation is associated with protein kinase A-mediated tyrosine phosphorylation. In our previous study, we identified the fibrous sheath CABYR binding protein (FSCB), which was phosphorylated by PKA. However, the phosphorylation status of FSCB protein during spermatozoa capacitation should be further investigated. To this aim, in this study, we found that phosphorylation of this 270-kDa protein occurred as early as 1 min after mouse spermatozoa capacitation, which increased over time and remained stable after 60 min. Immunoprecipitation assays demonstrated that the tyrosine and Ser/Thr phosphorylation of FSCB occurred during spermatozoa capacitation. The extent of phosphorylation and was closely associated with the PKA activity and spermatozoa motility characteristics. FSCB phosphorylation could be induced by PKA agonist DB-cAMP, but was blocked by PKA antagonist H-89.Therefore, FSCB contributes to spermatozoa capacitation in a tyrosine-phosphorylated format, which may help in further elucidating the molecular mechanism of spermatozoa capacitation. [BMB reports 2011; 44(8): 541-546]
Isoindolin-1-ones from the stems of Nicotiana tabacum and their antiviral activities
Guang-Yu Yang,Jia-Meng Dai,Zhen-Jie Li,Jin Wang,Feng-Xian Yang,Xin Liu,Jing Li,Qian Gao,Xue-Mei Li,Yin-Ke Li,Wei-Guang Wang,Min Zhou,Qiu-Fen Hu 대한약학회 2022 Archives of Pharmacal Research Vol.45 No.8
In previous studies, several isoindolin-1-oneanalogs that exhibited signifi cant anti-tobacco mosaic virus(anti-TMV) activities were isolated from Nicotiana tabacum . Since gene-editing mutants provide a new sample for thediscovery of active metabolites, we focused on the stems ofYN-18–23 (a mutant N. tabacum for gene editing with thealkaloid metabolic pathway cultivated by Yunnan TobaccoCompany), which led to the isolation of four new ( 1–4 )and four known ( 5–8 ) isoindolin-1-ones. To the best of ourknowledge, nicindole C ( 3 ) is the fi rst subclass of isoindolin-1-one bearing a pentacyclic ketone, while nicindole D ( 4 )is the fi rst example of isoindolin-1-one bearing a methylpyridin-2-(1 H )-one moiety. Compounds 1–4 were testedfor their anti-TMV activities, and the results revealed thatcompounds 1 , 3 , and 4 exhibited high anti-TMV activities atconcentrations of 20 μM with inhibition rates of 48.6, 42.8,and 71.5%, respectively. These rates are higher than the inhibitionrate of the positive control (33.2%). The mechanisticstudy of compound 4 , which had the highest anti-TMV activityrevealed that increased potentiation of defense-related enzyme activities and downregulation of expression of theNtHsp70 protein may induce resistance in tobacco againstthe viral pathogen TMV. Molecular docking studies alsorevealed that the isoindolin-1-one substructure is fundamentalfor anti-TMV activity. The methyl-pyridin-2-(1 H )-onemoiety in compound 4 and the 2-oxopropyl groups in compounds1 and 3 at the N -2 position may increase inhibitoryactivities. This study of the structure–activity relationshipis helpful for fi nding new anti-TMV activity inhibitors. Tostudy whether the isoindolin-1-ones have broader antiviralactivities, compounds 1–4 were also tested for their antirotavirusactivities. Compound 4 exhibited high anti-rotavirusactivity with a therapeutic index (TI) value of 20.7. This TI value is close to that of the positive control (20.2).
Effect of Resistant Starch on HCl/ethanol-induced Gastric Injury in Rats
Qian, Yu,Li, Guijie,Zhu, Kai,Sun, Peng,Feng, Xia,Zhao, Xin The Korean Society for Applied Biological Chemistr 2013 Applied Biological Chemistry (Appl Biol Chem) Vol.56 No.6
Three types of resistant starch (RS) products were purchased for the evaluation of gastric injury preventive effect in Sprague-Dawley rats. We used an animal model to check for gastric injury preventive activities of these RS products in vivo. RS3 reduced the levels of serum proinflammatory cytokines of IL-6 and TNF-${\alpha}$ as compared to those of RS2 and RS4. The gastric secretion volumes from high to low order were control rats, RS2-treated rats, RS4-treated rats, RS3-treated rats, and normal rats, whereas pH levels of gastric juice showed the opposite trend. The gastric injury level was significantly decreased by RS, demonstrating its anti-inflammatory properties, with RS3 showing the best anti-inflammatory effect. Gastric tissues of RS3 group rats showed significantly decreased mRNA and protein expression levels of inflammation-related genes of iNOS, COX-2, TNF-${\alpha}$, and IL-$1{\beta}$ compared with the control group, as shown by RT-PCR and Western blot analyses. These results suggest that RS shows a gastric injury preventive effect, with RS3 showing the best inhibitory effect on gastric injury.
Li Dong,Rui-Mei Feng,Li Zhang,Xiao-qian Xu,Xue-Lian Zhao,Margaret Zhuoer Wang,You-Lin Qiao,Fang-Hui Zhao 대한부인종양학회 2017 Journal of Gynecologic Oncology Vol.28 No.5
Objective: To investigate the extent of the cross-reactivity of hybrid capture 2 (HC2) assay andevaluate the potential effect of cross-reactivity on the long-term risk for cervical cancer andprecancers. Methods: Based on the Shanxi Province Cervical Cancer Screening Study-I (SPOCCS-I)cohort from 2005 to 2014 in Shanxi, China, SPF10-line probe assay (LiPA) was performedin all 598 HC2 positive and 300 random-selected HC2 negative cervical specimens. Tenyearcumulative incidence rate (CIR) of cervical intraepithelial neoplasia grade 2 or worse(CIN2+) of these two tests was evaluated using Kaplan-Meier methods. Possible humanpapillomavirus (HPV) types to be cross-reacted by HC2 were also analyzed. Results: The overall agreement between HC2 and SPF10-LiPA for detecting carcinogenic HPVwas 73.27%. The highest 10-year cumulative risk of CIN2+ was observed in both HC2 positiveand LiPA-carcinogenic HPV positive women (25.70%; 95% confidence interval [CI]=23.55%–27.91%), followed by HC2 positive but LiPA-non-carcinogenic HPV positive women (9.97%;95% CI=8.57%–11.50%), HC2 negative but LiPA-carcinogenic HPV positive (2.56%; 95%CI=2.44%–2.70%) and HC2 positive but LiPA-HPV negative (1.85%; 95% CI=1.78%–1.92%)women. The proportion of cross-reactivity of HC2 with untargeted carcinogenic types was8.9%, most of which were attributable to HPV26, 73, 82, 69, 71, 53, 11, 43, and 54. Conclusion: The noticeable high risk of CIN2+ in women infected with cross-reacted noncarcinogenicHPV and low risk in those with miss-to-detective carcinogenic HPV supportedan overall good clinical performance of HC2 for a general cervical cancer screening.