超声引导股神经-股外侧皮神经阻滞联合喉罩全麻在股骨干骨折手术的应用效果

目的 探讨超声引导下股神经-股外侧皮神经阻滞联合喉罩全麻用于股骨干骨折手术的临床效果。方法 选择2014年9月到2018年5月黄山市人民医院收治的股骨干骨折手术患者30例,采用股神经-股外侧皮神经阻滞联合喉罩全麻,超声定位后注入0.5%罗哌卡因15 mL阻滞股神经和0.375%罗哌卡因5 mL阻滞股外侧皮神经。观察患者神经阻滞前（T₀）、阻滞后5 min（T₁）、10 min（T₂）、15 min（T₃）、30 min（T₄）的血流动力学变化;观察感觉及运动阻滞的起效和持续时间;同时观察有无恶心、呕吐及术后尿潴留等不良反应。结果 30例患者T₀、T₁、T₂、T₃、T₄收缩压分别为（144.67±14.81）、（141.53±14.32）、（141.67±13.88）、（142.00±12.40）、（145.00±11.65）mmHg,不同时间点收缩压的差异无统计学意义（P>0.05）。T₀、T₁、T₂、T₃、T₄舒张压分别为（79.73±4.39）、（77.90±4.29）、（79.87±3.87）、（78.77±4.29）、（79.17±3.48）mmHg,不同时间点舒张压的差异无统计学意义（P>0.05）。T₀、T₁、T₂、T₃、T₄心率分别为（80.00±4.98）、（78.90±3.21）、（78.33±3.92）、（79.33±3.02）、（78.07±3.38）次/分,不同时间点心率的差异无统计学意义（P>0.05）。患者感觉阻滞的起效时间平均为（6.77±0.90）min,持续时间为（339.90±65.67）min;运动阻滞的起效时间平均为（12.23±2.28）min,持续时间为（213.00±39.08）min。30例患者均无恶心、呕吐及术后尿潴留发生。结论 超声引导下行股神经-股外侧皮神经阻滞联合喉罩全麻应用于股骨干骨折手术,血流动力学稳定,镇痛时间长,术后并发症极少,可推广应用。     

右美托咪定联合七氟醚对老年患者腹腔镜下胃肠肿瘤切除术后血流动力学、认知功能及谵妄的影响

目的 探究右美托咪定对老年腹腔镜下胃肠肿瘤切除术患者的作用效果。方法 选择2017年6月—2018年5月我院收治的择期行腹腔镜下胃肠肿瘤切除术患者80例为研究对象,按照随机数字表法分为观察组（n=40）和对照组（n=40）。对照组采用七氟醚麻醉,观察组在对照组的基础上加用右美托咪定麻醉,比较两组患者在五个不同时刻［术前（T₀）、右美托咪定泵注10 min后（T₁）、气管插管后即刻（T₂）、气腹时（T₃）、气管拔管后即刻（T₄）］的平均动脉压（MAP）、心率（HR）、简易智力状态检查量表（MMSE）评分以及术后谵妄的发生率。结果 T₁、T₂、T₃、T₄时刻,观察组患者MAP、HR均明显低于对照组（P<0.05）;术后两组患者MMSE评分均明显低于术前（P<0.05）,但观察组明显高于对照组（P<0.05）;观察组患者术后谵妄的发生率明显低于对照组（P<0.05）。结论 右美托咪定能有效稳定老年腹腔镜胃肠肿瘤切除术患者的血流动力学指标,减少认知功能障碍和谵妄的发生。     

改良电休克治疗对重度抑郁症执行功能的影响

目的 探讨改良电休克治疗（MECT）对重度抑郁症执行功能近期及远期影响。方法 选取合肥市第四人民医院2013年9月至2016年9月收治的19例重度抑郁症患者,所有患者均行MECT。于治疗前（T₁）、治疗结束后1周内（T₂）、治疗结束1个月后（T₃）分别使用汉密尔顿抑郁量表（HDRS）评价抑郁程度,言语流畅性测试（VFT）评估执行功能。结果 T₁、T₂、T₃的HDRS评分差异有统计学意义（P<0.05）,T₂的HDRS评分低于T₁评分,差异有统计学意义（P<0.05）,T₃的HDRS评分低于T₁评分,差异有统计学意义（P<0.05）。T₁、T₂、T₃的VFT评分差异有统计学意义（P<0.05）,T₂的VFT评分低于T₁评分,差异有统计学意义（P<0.05）,T₃的VFT评分高于T₂评分,差异有统计学意义（P<0.05）。T₁、T₂间VFT降低值与患者年龄成正相关（r=0.46,P<0.05）,与患者的教育年限成负相关（r=-0.46,P<0.05）。结论 MECT可导致抑郁症近期执行功能损害,但可恢复。MECT所致的执行功能损害程度与年龄、教育程度有关。     

新生儿缺氧缺血性脑病血清NSE和VILIP-1水平变化及意义

目的 探讨新生儿缺氧缺血性脑病（HIE）血清神经元特异性烯醇化酶（NSE）和视椎蛋白样蛋白1（VILIP-1）水平变化及意义。方法 选取2012年3月至2015年4月在郑州市儿童医院住院治疗的136例HIE患儿,根据病情分为轻度（n=58）、中度（n=46）、重度（n=32）,同期,选取正常新生儿45例作为对照组,HIE患儿分别于出生后第24小时（T₀）、48小时（T₁）、72小时（T₂）和7天（T₃）时,对照组于T₀时,检测血清中NSE和VILIP-1水平,HIE患儿和对照组均于T₀时,进行新生儿行为神经测定（NBNA）评分。结果 HIE患儿T₀时血清NSE和VILIP-1水平分别为（28.82±6.34）、（0.91±0.26）μg/L,均高于对照组的（13.94±2.82）、（0.38±0.15）μg/L,NBNA评分为（33.83±2.25）分,低于对照组的（38.24±2.41）分,差异均有统计学意义（P<0.05）;Pearson相关分析显示,HIE患儿T₀时血清NSE水平与VILIP-1水平呈正相关（r=0.612,P<0.05）,血清NSE和VILIP-1水平均与NBNA评分呈负相关（r=-0.481、-0.440,P<0.05）;与轻度相比,中度和重度患儿T_0～3时血清NSE和VILIP-1水平均升高,且重度均高于中度,差异均有统计学意义（P<0.05）。结论 HIE患儿血清NSE和VILIP-1水平升高,动态监测血清NSE和VILIP-1水平对HIE早期诊断、病情判定及治疗效果评估具有重要意义。     

T2*-GETI3D序列对髋关节撞击综合征早期软骨损伤的评价价值

目的 探讨三维多回波合并成像T₂^*WI（以下称T₂^*-GETI3D）对髋关节撞击综合征（FAI）软骨损伤的应用价值。方法 选取42例FAI患者为研究对象,均采用磁共振T₁WI、质子密度加权成像（PDWI）及T₂^*-GETI3D序列进行双髋关节扫描,以关节镜检查结果为金标准,对以上3种成像序列的图像质量及软骨损伤显示阳性率进行对比分析。结果 3种序列图像质量总体评分差异有统计学意义（P<0.001）,多重比较显示T₂^*-GETI3D及PDWI序列图像质量评分[（2.26±0.81）分、（2.01±0.77）分]均高于T₁WI序列[（1.46±0.56）分,P<0.001及P=0.001）],其中T₂^*-GETI3D图像质量评分最高;对软骨损伤的结果显示,T₁WI阳性11例（26.19%）,阴性31例（73.81%）;PDWI阳性24例（57.14%）,阴性18例（42.86%）;T₂^*-GETI3D阳性27例（64.28%）,阴性15例（35.72%）。T₂^*-GETI3D序列对软骨损伤显示的阳性率最高（P<0.01）。结论 3种成像序列中,T₂^*-GETI3D序列图像质量好,对FAI软骨损伤的显示率较高,能为临床术前评估关节软骨损伤程度提供较为可靠的影像信息。     

地佐辛与舒芬太尼经静脉患者自控镇痛对食管癌患者术后镇痛的效果比较

目的 比较地佐辛与舒芬太尼经静脉患者自控镇痛（PCIA）给药对食管癌患者术后的镇痛效果。方法 116例择期行食管癌根治术的患者随机分为地佐辛组（n=58）和舒芬太尼组（n=58）,两组患者麻醉方法及麻醉药物使用均相同,术毕给予PCIA,地佐辛组药物为0.8 mg/kg地佐辛和6 mg托烷司琼用生理盐水配制成100 mL,舒芬太尼组药物为舒芬太尼2.5 μg/kg和托烷司琼6 mg用生理盐水配制成100 mL。记录两组患者术后48 h内PCIA按压次数和镇痛药物累积消耗量,计算有效按压率;分别于术后6h （T₂）、12 h （T₃）、24 h （T₄）和48 h （T₅）评估疼痛视觉模拟量表（VAS）评分,分别于术前（T₀）、T₁、T₃、T₄和T₅时检测T细胞亚群CD3⁺、CD4⁺、CD8⁺和NK细胞,记录两组患者术后不良反应发生情况。结果 地佐辛组患者术后48 h内按压次数和镇痛药物累积消耗量分别为（5.1±2.2）次和（60.6±11.2） mL,低于舒芬太尼组（7.2±2.6）次和（88.8±9.1） mL （P<0.05）;地佐辛组患者T_2~5时安静时VAS评分[（2.1±0.9）、（1.9±0.6）、（2.0±0.5）、（1.7±0.4）分]和活动时VAS评分[（2.6±1.1）、（2.2±0.8）、（2.3±0.7）、（1.9±0.8）分]均低于舒芬太尼组（P<0.05）;与舒芬太尼组相比,地佐辛组患者T_3~5时CD3⁺细胞[（57.8±9.2）%、（62.3±7.8）%、（66.3±9.5）%]均升高,T₃时CD4⁺[（27.8 ±6.8）%]升高,T_3~4时CD4⁺/CD8⁺比值[（1.15±0.62）、（1.24±0.52）]和NK细胞[（20.2±6.9）%、（21.3±4.9）%]升高,差异均有统计学意义（P<0.05）;地佐辛组患者术后总不良反应发生率22.4%,显著低于舒芬太尼组的39.7%（P<0.05）。结论 与舒芬太尼相比,地佐辛应用于食管癌患者术后镇痛,可提高镇痛效果、改善患者机体细胞免疫功能、减少术后不良反应的发生。     

地佐辛减轻瑞芬太尼麻醉苏醒期痛觉敏化的临床观察

目的 观察在瑞芬太尼全身麻醉中,地佐辛预防患者苏醒期痛觉敏化的临床效果与安全性。方法 选择2015年1月至2016年9月在淮南新华医院进行腹腔镜子宫切除的全身麻醉患者60例,采用随机数字表法分为观察组和对照组,每组30例。两组患者均在BIS监测下,使用瑞芬太尼快通道全身麻醉。气腹开始时,观察组患者给予地佐辛5 mg静脉推注,对照组患者给予安慰剂生理盐水2 mL。观察记录患者手术时间、出血量、气腹时间、拔管前（T₀）、拔管即刻（T₁）、拔管后1 min（T₂）、拔管后3 min（T₃）、拔管后5 min（T₄）平均动脉压（MAP）和心率（HR）。同时,观察记录患者苏醒时间、拔管时间、苏醒期痛觉敏化的发生率和术后咽痛、恶心呕吐、瘙痒等不良反应的发生率。结果 观察组T₁、T₂的MAP[（72.58±10.33、76.65±10.57）mmHg]和HR[（66.64±8.28、67.48±9.36）次/分]较对照组明显下降,差异有统计学意义（P<0.05）。对照组T₁、T₂的MAP[（88.15±9.35、85.89±7.99）mmHg]和HR[（79.28±11.46、77.43±10.65）次/分]较T₀升高,差异有统计学意义（P<0.05）。观察组患者苏醒期痛觉敏化发生率为3.33%,低于对照组,差异有统计学意义（P<0.05）;而两组患者术后咽痛、恶心呕吐和瘙痒的发生率差异无统计学意义（P>0.05）。结论 瑞芬太尼快通道全身麻醉下行腹腔镜手术,于气腹开始时使用地佐辛5 mg静脉推注,可降低苏醒期痛觉敏化的发生率,减轻拔管反应,血流动力学更稳定,同时并不增加苏醒时间和拔管时间。     

综合保温对妇科腹腔镜手术患者复苏期并发症的影响

目的 探讨综合保温法对妇科腹腔镜手术患者复苏期并发症的影响。方法 以安徽医科大学第二附属医院妇科2017年4月至2017年6月收治的145例行腹腔镜手术的患者为研究对象,按接受手术先后顺序结合随机数字表法将其分为干预组（72例）和对照组（73例）。干预组给予综合保温措施,对照组给予常规保温措施,比较两组患者麻醉前（T₀）、入复苏室即刻（T₁）、入复苏室15分钟（T₂）、入复苏室30分钟（T₃）的鼻温数值、心率、平均动脉压和复苏期并发症。结果 两组患者在T₀时的鼻温、心率和平均动脉压比较差异均无统计学意义（P>0.05）;干预组患者在T₁、T₂、T₃时点的鼻温值均高于对照组,差异有统计学意义（P<0.05）;干预组患者在T₁、T₂时点的心率、平均动脉压均低于对照组,差异有统计学意义（P<0.05）;除低血压外,干预组患者低体温、低氧血症、通气异常、高血压、苏醒延迟、寒颤、躁动的发生率均低于对照组,差异均有统计学意义（P<0.05）;干预组苏醒时长（17.5±2.2）分,亦低于对照组的（45.3±3.5）分,差异有统计学意义（P<0.05）。结论 妇科腹腔镜手术患者术中采取综合保温措施可有效降低复苏期并发症的发生率,提高复苏效果。     

低潮气量通气联合肺复张对妇科腹腔镜手术患者肺氧合功能及动脉血气的影响

目的 分析妇科腹腔镜手术中低潮气量通气联合肺复张对患者肺氧合功能及动脉血气的影响。方法 选取马鞍山市人民医院2018年3月至2019年9月择期腹腔镜妇科手术患者70例,采用随机数字表法分为低潮气量组(L组,n=35)和对照组(C组,n=35)。气管插管后L组给予低潮气量通气,术中间断行手控肺复张;C组给予常规潮气量通气。检测两组患者在入室时(T₀)、气腹后10分钟(T₁)、30分钟(T₂)、60分钟(T₃)及停止气腹后10分钟(T₄)时动脉血气;观察并比较T₀～T₄时两组患者平均动脉压(MAP)、心率(HR)、呼末二氧化碳分压(PETCO₂)、气道峰压(Ppeak)、气道平台压(Pplat)、肺顺应性(CL)和术后通气相关不良反应,计算氧合指数(OI)和肺内分流率(Qs/Qt)情况。结果 L组T₂、T₃时MAP低于C组,差异有统计学意义(P<0.05);L组T₃时HR低于C组,差异有统计学意义(P<0.05);L组T₂、T₃时Ppeak、Pplat低于C组,T₂、T₃、T₄时CL高于C组,差异有统计学意义(P<0.05);L组T₁、T₂、T₃时二氧化碳分压(PaCO₂)、PETCO₂高于C组, T₂、T₃时Qs/Qt低于C组,差异有统计学意义(P<0.05);术后72 h内两组患者通气相关不良反应比较,差异无统计学意义(P>0.05)。结论 妇科腹腔镜手术中,L通气联合肺复张能够有效改善患者肺氧合功能,降低肺内分流,维持内环境稳定。     

高脂饮食对双嘧达莫在中国健康人体内药动学的影响

目的 观察中国健康受试者空腹和高脂高热量饮食情况下口服双嘧达莫片的药动学特征。方法 75名健康受试者分别在空腹或高脂饮食条件下单剂量口服双嘧达莫片25 mg,分别在不同时间点采集静脉血样。采用LC-MS/MS测定人血浆中双嘧达莫的浓度,用PhoenixWinNonlin 8.0软件按非房室模型计算药动学参数。结果 空腹和高脂饮食后双嘧达莫片的主要药动学参数如下：C_max分别为(594.69±172.14),(333.64±167.18) ng·mL^-1,餐后较空腹C_max降低了43.9%(P<0.01);t_1/2分别为(9.87±4.21),(10.57±3.75) h;AUC_0-t分别为(1 733.22±715.49),(1 268.61±571.07) ng·mL^-1·h,AUC_0-∞分别为(1 801.69±707.61),(1 353.64±602.29) ng·mL^-1·h,餐后较空腹AUC_0-t及AUC_0-∞分别降低26.8%,24.9%(P<0.01);T_max中位数(范围)分别为0.75[0.50,5.00] h和1.50[0.49,4.52] h,餐后服药的T_max明显延迟(P<0.01)。结论 高脂饮食后服药较空腹条件下服药,C_max、AUC_0-t及AUC_0-∞均明显降低,T_max明显延迟,说明食物对双嘧达莫片的吸收速度、吸收程度均有显著影响。     

circ-E2F3促进宫颈癌细胞增殖的机制研究

目的 研究circ-E2F3通过抑制miR-296-5p影响宫颈癌进展的作用机制。方法 采用qRT-PCR检测宫颈癌组织和癌旁组织中circ-E2F3的表达量，筛选宫颈癌细胞系，通过qRT-PCR检测宫颈癌细胞系和正常宫颈黏膜上皮细胞中circ-E2F3的表达量。采用CCK-8检测细胞活力，通过检索数据库筛查circ-E2F3可能的分子机制，并通过双荧光素酶分析、qRT-PCR等方法证实其调控机制。结果 circ-E2F3在宫颈癌组织和宫颈癌细胞系CaSki中表达上调。体外实验证实circ-E2F3能促进宫颈癌细胞增殖；体内实验证实circ-E2F3通过抑制miR-296-5p促进肿瘤细胞生长。结论 circ-E2F3通过抑制miR-296-5p在宫颈癌的进展中发挥重要作用，高表达的circ-E2F3可能是判断宫颈癌进展的重要指标。     

MicroRNA expression profiling of Chinese follicular lymphoma by microarray: A preliminary study

BackgroundMicroRNAs (miRNAs) have been widely regarded as crucial regulators in various biological processes involved in carcinogenesis. However, the comprehensive miRNA profiles of Chinese follicular lymphoma (FL) remains completely unknown.MethodsThe Exiqon miRCURY LNA™ microRNA Array (v.18.0) was used to detect the miRNA expression profiles of three Chinese FL samples, and compared to three reactive lymphatic nodes (RLN). Quantitative real-time polymerase chain reaction (qRT-PCR) was used to confirm the selected miRNAs in different series. Three databases (miRAnda, miRBase and TargetScan) were used to predict the putative target genes. Bioinformatic analysis (gene ontology analysis and pathway analysis) was performed for further evaluation.ResultsThe microarray assay demonstrated that 1643 miRNAs were expressed; in which 103 miRNAs were upregulated and 68 miRNAs were downregulated, according to P-value (< 0.05) and fold change (FC > 2-fold). Furthermore, qRT-PCR was used to confirm that miR-17-5p, miR-20a-5p and miR-19a-3p were upregulated, and miR-3615 was downregulated (P < 0.05). Bioinformatic analysis (gene ontology analysis and pathway analysis) was used for further evaluation. Pathway analysis indicated that 25 pathways corresponded to differentially expressed miRNAs (P-value cut-off is 0.05). Furthermore, miR-17-5p, miR-20a-5p and miR-19a-3p were validated by qRT-PCR in an independent series including five FL3a and five RLN cases. Data analysis revealed that the changing trend of miR-19a-3p and miR-17-5p expression in the independent series was basically identical with that of the microarray data.ConclusionsOur results are the first to reveal the miRNA expression profiling of Chinese FL and three upregulated miRNAs. Furthermore, the expression of miR-19a-3p and miR-17-5p were found to be significantly upregulated in FL3a. Further study needs to be urgently performed to reveal its potential role in the pathogenesis of FL in the near future.     

Associations between the functional polymorphisms in the ABCB1 transporter gene and colorectal cancer risk: a case-control study in Turkish population

Abstract

Colorectal cancer is among the most common cancer types in the world and its etiology involves the interaction of genetic and environmental factors. ABCB1 is highly expressed in the apical surface of colonic epithelial cells and acts as an efflux pump by transporting toxic endogenous substances, drugs and xenobiotics out of cells. ABCB1 polymorphisms may either change its protein expression or alter its function. Several studies have reported a possible association between ABCB1 variants and colorectal cancer, but no consistent conclusion has been arrived at. Therefore, we aimed to investigate the relationship between colorectal cancer and the functional common variants of ABCB1 (1236C?>?T; 2677G?>?T/A; 3435C?>?T). The distributions of the variants were determined in 103 patients with colorectal cancer and 150 healthy volunteers using polymerase chain reaction–restriction fragment length polymorphism methods. ABCB1 1236C?>?T was statistically significantly associated with colorectal cancer risk (OR, odd ratio?=?1.91; 95% CI, confidence interval?=?1.09–3.35; p?=?0.034). In haplotype-based analysis, the proportion of individuals with the ABCB1 haplotype C₁₂₃₆-G₂₆₇₇-T₃₄₃₅ was significantly more common in patients than in controls (OR?=?11.96; 95% CI?=?2.59–55.32; p?=?0.0004). We believe that the findings may be beneficial to the development of efficacious preventive strategies and therapies for colorectal cancer.     

Alteration of the ERK5 pathway by hydroxysafflor yellow A blocks expression of MEF2C in activated hepatic stellate cells in vitro: Potential treatment for hepatic fibrogenesis

Context: Hepatic fibrosis ultimately leads to cirrhosis if not treated effectively. Hepatic stellate cells (HSC) are a main mediator of hepatic fibrosis through the accumulation of extracellular matrix proteins. Suppression activation of passaged HSC has been proposed as therapeutic strategies for the treatment and prevention of hepatic fibrosis.

Objective: To evaluate the effect of hydroxysafflor yellow A (HSYA), an active chemical compound derived from the flowers of Carthamus tinctorius L. (Compositae), on HSC inhibition, and to begin elucidating underlying mechanisms.

Materials and methods: Primary HSCs were isolated from rats by in situ pronase/collagenase perfusion. Culture-activated HSCs were treated with or without HSYA at 30?μM in the presence or absence of PD98059 for 48?h, and then cell proliferation was measured by MTS assays. Messenger RNA (mRNA) expression was quantified by polymerase chain reaction, and protein was quantified by Western blots or enzyme-linked immunosorbent assays.

Results: HSYA significantly inhibits culture-activated HSC proliferation in a dose-dependent and time-dependent manner with an IC₅₀ value of 112.79?μM. HSYA (30?μM) induce the suppression of HSC activation, as indicated by decreases in contents of type I alpha collagen in HSC-cultured media and expression of α-smooth muscle actin protein in culture-activated HSC by 55 and 71%, respectively. HSYA (30?μM) also caused significant decreases in mRNA expression of type III alpha collagen in HSC by 28%. HSYA (30?μM) suppresses myocyte enhancer factor 2?C (MEF2C) expression both at its mRNA and protein levels by 60 and 61%, respectively. Further study demonstrated that HSYA (30?μM) caused significant decreases in p-ERK5 by 49%. Blocking extracellular signal-regulated protein kinase 5 (ERK5) activity by XMD 8--92, an ERK5 inhibitor, markedly abrogated the inhibitive effects of HSYA on HSC activation, and blocked the HSYA-mediated MEF2C down-regulation.

Conclusions: HSYA suppress HSC activation by ERK5-mediated MEF2C down-regulation and makes it a potential candidate for prevention and treatment of hepatic fibrogenesis.     

Antibacteriophage Properties of Some Greek Plant Extracts

Abstract

The ethanol extracts (70%) of 45 plants grown in Greece were screened for antibacteriophage properties against 6 bacteriophages: coliphages T₁, T₂, T₄, T₇, φX174, and MS₂- Eight samples were found to induce a significant antiphage activity and can be used as material for further antiviral studies in vitro and in vivo.     

Hydroxysafflor yellow A attenuates left ventricular remodeling after pressure overload-induced cardiac hypertrophy in rats

Context: Hydroxysafflor yellow A (HSYA), the main chemical component of the safflower yellow pigments, is used extensively in traditional Chinese medicine for the treatment of cerebrovascular and cardiovascular diseases.

Objective: The present study determined the effects of HSYA on left ventricular hypertrophy after pressure overload and investigated the underlying mechanisms.

Materials and methods: Cardiac hypertrophy was induced by the ligation of abdominal aorta in male Wistar rats. The rats were then divided into five groups and treated with captopril (100?mg/kg) or HSYA at different doses (0, 10, 20 and 40?mg/kg). Six weeks after treatment, the weight of left ventricle, LVMI (left ventricular mass index) and pathological changes were measured. MMP-2 (metalloproteinase 2) and MMP-9 (metalloproteinase 9) levels were determined by ELISA. Protein expressions of Bcl-2 and Bax were evaluated by immunohistochemistry.

Results: HSYA (20, 40?mg/kg) significantly attenuated the increase of LVMI (ventricular weight/body weight) by 13.04 and 30.43% respectively, when compared with the model group. This was associated with the amelioration of pathological lesion, such as cardiac muscle fibers were smaller and the nuclei of cardiomyocytes were lightly stained in animals treated with HSYA (20, 40?mg/kg). In addition, the administration of HSYA at doses of 20 and 40?mg/kg increased the Bcl-2/Bax ratio (1.17?±?0.08 and 1.39?±?0.07 versus 0.71?±?0.06). In addition, the serum MMP-2 and MMP-9 levels were blocked by the treatment at doses of 20 and 40?mg/kg HSYA (MMP-2, 76.1?±?9.2 and 65.6?±?6.8 versus 82.9?±?6.2, ng/ml; MMP-9, 66.6?±?4.8 and 57.5?±?5.0 versus 83.5?±?6.0, ng/ml).

Conclusion: These findings indicated that HSYA has beneficial effects on hypertensive ventricular remodeling, which may involve mechanisms of inhibiting cell apoptosis and suppressing metalloproteinases expression.     

New C-19-modified geldanamycin derivatives: synthesis,antitumor activities,and physical properties study

Thiazinogeldanamycin (2) was identified from Streptomyces hygroscopicus 17997 at the late stage of the fermentation. The pH was firstly proposed as an important factor in the biosynthesis of it. It was verified that 2 was produced by direct chemical reactions between geldanamycin (1, GDM) and cysteine or aminoethanethiol hydrochloride at pH > 7 in vitro. The proposed synthesis pathway for compound 2 was also discussed. Eleven new C-19-modified GDM derivatives, including five stable hydroquinone form derivatives, were synthesized, most of which exhibited desirable properties such as lower cytotoxicity, increased water solubility, and potent antitumor activity. Especially, compounds 5 and 8 showed antitumor activities against HepG2 cell with IC₅₀ values of 2.97–6.61 μM, lower cytotoxicity and at least 15-fold higher water solubility compared with 1 in pH 7.0 phosphate buffer.     

二甲双胍在结肠癌中通过抑制lncRNA-MALAT1的表达发挥抗肿瘤效应

目的 探讨二甲双胍（MET）对结肠癌细胞的抑制作用及其机制。方法 采用CCK-8、流式细胞术及Transwell检测MET对结肠癌细胞SW480和SW620增殖、凋亡及侵袭的影响,qRT-PCR检测5种lncRNA在结肠癌细胞中的表达,Western blotting检测MET和/或MALAT1基因敲减在体外对PI3K/AKT和ERK通路活性的影响。结果 MET在体外对SW480和SW620细胞具有抑制作用,且呈剂量和时间依赖性（P<0.05）。MET可促进SW480和SW620细胞凋亡（P<0.05）。在5种lncRNA中,lncRNA-MALAT1在SW480和SW620细胞中的表达水平最高（P<0.01）。siRNA可抑制lncRNA-MALAT1表达,并进一步增强MET介导的抗结肠癌作用（P<0.05）。MET可下调结肠癌细胞中lncRNA-MALAT1的表达（P<0.05）,并通过PI3K/AKT和ERK信号通路与lncRNA-MALAT1敲减协同抑制结肠癌细胞的增殖和侵袭,并促进其凋亡（P<0.01）。结论 MET在结肠癌细胞中通过抑制lncRNA-MALAT1的表达发挥抗肿瘤效应。