Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma

Twenty four pyrazoline derivatives modified from Celecoxib were designed and synthesized as bi-inhibitor of COX-2 and B-Raf. They were evaluated for their COX-1/COX-2/B-Raf inhibitory and anti-proliferation activities. Compound A3 displayed the most potent activity against COX-2 and HeLa cell line (IC₅₀ = 0.008 μM; GI₅₀ = 19.86 μM) and showed superb COX-1/COX-2 selectivity (>500), being more potent and selective than positive control Celecoxib or 5-fluorouracil. Compounds A5 and B5 were introduced best B-Raf inhibitory activities (IC₅₀ = 0.15 μM and 0.12 μM, respectively). Compound A4 retained superb bioactivity against COX-2 and HeLa cell line (IC₅₀ = 0.015 μM; GI₅₀ = 23.82 μM) and displayed moderate B-Raf inhibitory activity (IC₅₀ = 3.84 μM). Docking simulation was conducted to give binding patterns. QSAR models were built using bioactivity data and optimized conformations to provide a future modification of COX-2/B-Raf inhibitors.     

乌苯美司胶囊联合SOX化疗对晚期胃癌患者的临床疗效研究

目的:探讨乌苯美司胶囊联合SOX化疗对晚期胃癌患者的临床疗效及安全性。方法:选择2013年9月至2015年9月我院接诊的90例晚期胃癌患者,通过随机数表法分为观察组(n=45)和对照组(n=45)。对照组给予SOX化疗方案,观察组在此基础上联合乌苯美司胶囊。比较两组治疗前后CD_4~+、CD_8~+、CD_4~+/CD_8~+、血清基质金属蛋白酶(MMP)-2、MMP-9水平、临床疗效、不良反应发生情况以及6个月、12个月生存率。结果:治疗后,观察组CD_4+、CD_4~+/CD_8~+显著高于对照组(P0.05),血清MMP2、MMP-9水平明显低于对照组(P0.05);临床疗效总有效率高于对照组[68.89%(31/45)vs48.89%(22/45)](P0.05),血小板下降、白细胞下降、恶心呕吐、肝功异常的发生率均显著低于对照组(P0.05)。观察组在6个月、12个月时生存率均高于对照组[93.33%(42/45)vs77.78%(35/45),82.22%(37/45)vs57.78%(26/45)](P0.05)。结论:与单用SOX方案相比,乌苯美司胶囊联合SOX化疗方案治疗晚期胃癌患者的效果显著,可有效改善免疫功能,提高远期生存率,且安全性更高。     

手术前后注射帕瑞昔布钠对脑膜瘤切除术后的镇痛效果评价

目的:比较手术前后注射帕瑞昔布钠对脑膜瘤切除术后的镇痛效果。方法:收集我院收治的120例行脑膜瘤切除术患者,随机分为术前组、术后组以及对照组,每组40例。术前组在麻醉前15 min静注帕瑞昔布钠40 mg所有患者行麻醉诱导(咪达唑仑+异丙酚+罗库溴铵+舒芬太尼)静脉注射,维持麻醉采用异丙酚+瑞芬太尼静脉泵注,行脑膜瘤切除术术毕根据患者具体情况停用异丙酚、瑞芬太尼术后组患者在手术结束前15 min静注帕瑞昔布钠40 mg,对照组患者在手术结束前15 min静注生理盐水2mL。观察并比较三组患者各时间点的疼痛视觉模拟评分(VAS)、简易智能状态量表(MMSE)评分、血清皮质醇(cortisol)水平以及患者不良反应发生率。结果:与对照组相比术前组、术后组患者术后1 h的VAS评分水平较低差异具有统计学意义(P0.05);与术后组相比术前组患者的术后1 h的VAS评分水平较低差异具有统计学意义(P0.05);术后三组患者的MMSE评分与术前相比均下降(P0.05),与对照组相比术前组患者的术后1 h、术后24h MMSE评分较高差异具有统计学意义(P0.05);与对照组相比术前组、术后组患者术后1 h以及术后24 h的皮质醇水平较低差异具有统计学意义(P0.05);与术后组相比术前组患者的皮质醇水平较低差异具有统计学意义(P0.05);三组患者的副作用发生率相比无明显差异(P0.05)。结论:术前注射帕瑞昔布钠的镇痛效果较术后注射更好术后认知功能恢复较快。     

麝香保心丸联合丹参多酚酸盐对冠心病心绞痛患者心功能及血清CRP与Hcy水平的影响

目的:探讨麝香保心丸联合丹参多酚酸盐治疗冠心病心绞痛的临床疗效。方法:选择2014年5月-2016年5月我院收治的冠心病心绞痛患者94例,根据治疗方法不同分为研究组和对照组,每组47例。对照组患者给予丹参多酚酸盐注射液治疗,研究组患者在对照组基础上给予麝香保心丸口服治疗。观察并比较两组患者治疗前后心功能指标及血清同型半胱氨酸(Hcy)及C反应蛋白(CRP)水平。结果:与治疗前比较,两组患者治疗后Pro-BNP,LVEDD及E/A均降低,而LVEF均升高,差异具有统计学意义(P0.05);与对照组比较,研究组治疗后Pro-BNP,LVEDD及E/A较低,而LVEF较高,差异具有统计学意义(P0.05)。与治疗前比较,两组患者治疗后血清Hcy及CRP水平均升高,差异具有统计学意义(P0.05);与对照组比较,研究组患者治疗后血清Hcy及CRP水平较高,差异具有统计学意义(P0.05)。研究组患者临床总有效率显著高于对照组,差异具有统计学意义(P0.05)。结论:麝香保心丸联合丹参多酚酸盐治疗冠心病心绞痛具有显著的临床疗效,可以改善患者心功能,促进冠状动脉血流畅通,值得临床推广应用。     

Haemagglutination of Bacteroides fragilis

Abstract The relationship between the ability to cause haemagglutination (HA) and the presence of capsules and/or pili was examined for 50 clinical isolates of Bacteroides fragilis . HA was tested using a slide technique, and bovine, porcine, guinea pig, rat, rabbit, horse, human, chicken and pigeon erythrocytes. Chicken and pigeon erythrocytes were the best indicators for HA with 43 (86%) of the strains tested causing HA and 39 (78%) with strong reactions. Capsule staining showed that the same 43 strains causing HA also produced a demonstrable capsule. No pili were found on either encapsulated or non-encapsulated strains using transmission electron microscopy. These results suggest that adherence of B. fragilis is related to the presence of capsular material, not pili.     

Advances in polymer-based cell encapsulation and its applications in tissue repair

Cell microencapsulation is a more widely accepted area of biological encapsulation. In most cases, it involves fixing cells in polymer scaffolds or semi-permeable hydrogel capsules, providing the environment for protecting cells, allowing the exchange of nutrients and oxygen, and protecting cells against the attack of the host immune system by preventing the entry of antibodies and cytotoxic immune cells. Hydrogel encapsulation provides a three-dimensional (3D) environment similar to that experienced in vivo, so it can maintain normal cellular functions to produce tissues similar to those in vivo. Embedded cells can be genetically modified to release specific therapeutic products directly at the target site, thereby eliminating the side effects of systemic treatments. Cellular microcarriers need to meet many extremely high standards regarding their biocompatibility, cytocompatibility, immunoseparation capacity, transport, mechanical, and chemical properties. In this article, we discuss the biopolymer gels used in tissue engineering applications and the brief introduction of cell encapsulation for therapeutic protein production. Also, we review polymer biomaterials and methods for preparing cell microcarriers for biomedical applications. At the same time, in order to improve the application performance of cell microcarriers in vivo, we also summarize the main limitations and improvement strategies of cell encapsulation. Finally, the main applications of polymer cell microcarriers in regenerative medicine are summarized.     

Embryonic encapsulation and maternal incubation: Requirements for survival of the early stages of the estuarine gastropod Crepipatella dilatata

During their reproductive period, females of Crepipatella dilatata deposit their embryos in capsules that they then brood in the pallial cavity until juveniles emerge several weeks later, after passing through a transient veliger “larval” stage. Artificially excapsulated veligers of this species experimentally exposed to a wide range of salinities (5, 10, 15, 20, 25, and 30 psu) for six hours showed reduced activity at salinities of 15 and 20 psu, whereas encapsulated veligers exposed to those same salinities showed no reduction of activity. Artificially excapsulated veligers showed high mortality at salinities of 5 and 10 psu; encapsulated embryonic stages also showed high mortalities at 5 psu and serious sublethal effects at 10 psu in tests excluding maternal protection, showing that encapsulation alone does not provide complete protection from low salinity stress. Natural tidal cycles in the Quempillén River estuary also reduced embryonic survival at salinities of ≤ 10 psu when the capsules were exposed without maternal protection. In contrast, encapsulated embryos protected by their mothers survived well regardless of the salinity to which they were exposed, under both natural and laboratory-simulated estuarine tidal cycles. C. dilatata are able to develop in the estuary only because of maternal protection, since salinity levels in this environment sometimes decline to as low as 7 psu. Successful embryonic development in this estuary reflects the capacity of C. dilatata adults to detect dangerously low salinity levels and then seal themselves off from the environment for up to 50 hrs (O. Chaparro pers. obs.) when the salinity drops below 22.5 psu, allowing salinity to remain above this level within the pallial cavity despite continued salinity declines in the surrounding seawater.     

风湿祛痛胶囊联合塞来昔布胶囊治疗强直性脊柱炎的疗效及对血液流变学和血清炎性因子的影响

摘要 目的：探讨强直性脊柱炎（AS）患者经风湿祛痛胶囊联合塞来昔布胶囊治疗后的疗效及对血液流变学和血清炎性因子的影响。方法：选取2014年8月-2021年12月在联勤保障部队第九八三医院治疗的80例AS患者。按照随机数字表法分为对照组（常规治疗及塞来昔布胶囊治疗，40例）和研究组（常规治疗及风湿祛痛胶囊联合塞来昔布胶囊治疗，40例），两组患者均治疗8周。对比两组血液流变学指标、血清炎性因子指标、视觉模拟评分法（VAS）评分、C反应蛋白（CRP）、巴氏强直性脊柱炎疾病活动指数（BASDAI）评分、红细胞沉降率（ESR），同时记录两组治疗期间不良反应发生情况。结果：研究组治疗8周后BASDAI、VAS评分低于对照组（P<0.05）。研究组治疗8周后CRP、ESR低于对照组（P<0.05）。研究组治疗8周后全血高切黏度、血浆黏度、全血低切黏度、红细胞压积低于对照组（P<0.05）。研究组治疗8周后白介素-23（IL-23）、肿瘤坏死因子-α（TNF-α）、白介素-1β（IL-1β）均低于对照组（P<0.05）。两组不良反应发生率对比无差异（P>0.05）。结论：风湿祛痛胶囊联合塞来昔布胶囊治疗AS，可有效缓解患者的临床症状，抑制疾病进展，可能与调节血液流变学、降低炎性因子水平有关。     

A review of zoanthid nematocyst types and their population structure

Hydrobiologia - Seven different types of nematocyst are detailed and illustrated from the Zoanthidea. We studied the size population structure of nematocyst capsules: how they are affected by...