微乳液反应法制备磺胺嘧啶银均匀微晶及其质量评价

目的：应用微乳液反应法制备磺胺嘧啶银均匀微晶,并评价其质量。方法：利用磺胺嘧啶钠微乳和硝酸银微乳混合后反应的方法,制备磺胺嘧啶银均匀微晶,用透射电镜观察其形态和大小,以Ｘ－射线衍射分析、红外光谱、核磁共振、差热分析等手段检测磺胺嘧啶银均匀微晶各种理化特性。结果：磺胺嘧啶银均匀微晶的粒径大小约为２～４μｍ,均匀微晶的结晶性好,纯度高。体外抑菌实验表明该品比市售磺胺嘧啶银具有更好的抑菌效果。结论：用微乳液反应法能获得磺胺嘧啶银均匀微晶。     

Effect of low doses of cannabidiolic acid and ondansetron on LiCl-induced conditioned gaping (a model of nausea-induced behaviour) in rats

Background and Purpose

To determine the minimally effective dose of cannabidiolic acid (CBDA) that effectively reduces lithium chloride (LiCl)-induced conditioned gaping reactions (nausea-induced behaviour) in rats and to determine if these low systemic doses of CBDA (5–0.1 μg·kg⁻¹) relative to those of CBD could potentiate the anti-nausea effects of the classic 5-hydroxytryptamine 3 (5-HT₃) receptor antagonist, ondansetron (OND).

Experimental Approach

We investigated the efficacy of low doses of CBDA to suppress acute nausea, assessed by the establishment of conditioned gaping to a LiCl-paired flavour in rats. The potential of threshold and subthreshold doses of CBDA to enhance the reduction of nausea-induced conditioned gaping by OND were then determined.

Key Results

CBDA (at doses as low as 0.5 μg·kg⁻¹) suppressed nausea-induced conditioned gaping to a flavour. A low dose of OND (1.0 μg·kg⁻¹) alone reduced nausea-induced conditioned gaping, but when it was combined with a subthreshold dose of CBDA (0.1 μg·kg⁻¹) there was an enhancement in the suppression of LiCl-induced conditioned gaping.

Conclusions and Implications

CBDA potently reduced conditioned gaping in rats, even at low doses and enhanced the anti-nausea effect of a low dose of OND. These findings suggest that combining low doses of CBDA and OND will more effectively treat acute nausea in chemotherapy patients.     

Asthma caused by potassium aluminium tetrafluoride: a case series

The objective of this study is to describe a case-series of potassium aluminium tetrafluoride (KAlF₄)-induced occupational asthma (OA) and/or occupational rhinitis (OR). The study involves five patients from a heat-exchanger production line who were examined (including specific inhalation challenge tests) for suspected OA and/or OR caused by a flux containing almost 100% KAlF₄ − with fluorides’ workplace air concentrations ranging between 1.7 and 2.8 mg/m³. No subject had a previous history of asthma. All five patients had a positive specific challenge test (three patients were diagnosed with OA alone, one with OR and one with both OR and OA). At the follow-up visit, after three years on average, all patients needed permanent corticosteroid therapy (four topical, one oral). After elimination from the exposure, only one of the observed subjects gave an indication of an improvement, two subjects stabilized and two worsened. Our case series focuses on the correlation between patients’ exposure to fluorides in air-conditioner production and the subsequent occurrence of OR/OA. Currently, it is uncertain whether these OR/OA were caused by hypersensitivity or irritation.     

叶瓜参中的三个脑苷脂(英文)

目的:研究叶瓜参化学成分。方法:对叶瓜参的65%乙醇提取物中小极性部分进行行分离纯化,得到脑苷脂分子种3,对脑苷脂分子种3应用高效液相色谱进一步分离纯化,得到3个脑苷脂单体,CF-3-1(1)、CF-3-2(2)和CF-3-3(3)。结果:根据化合物的波谱数据和化学方法鉴定了其结构。结论:三个化合物为首次从叶瓜参中分离得到,首次得到化合物2和3的单体化合物。     

加味桂枝人参汤对胰岛素抵抗HepG2细胞葡萄糖消耗量的影响

目的:探讨加味桂枝人参汤(MGD)溶液对胰岛素抵抗(IR)HpeG-2细胞模型的保护作用及机理。方法:成功复制HepG2细胞IR模型后,采用MGD溶液进行干预,并与罗格列酮进行对照,观察细胞形态学变化、各孔细胞的葡萄糖消耗量、细胞的数目与活力。结果:MGD对模型细胞的增殖并无明显影响(P0.05),但可以增加其葡萄糖消耗量(P0.01),与西药组比较无显著性差异(P0.05)。结论:中药MGD与罗格列酮具有同等的改善模型细胞IR的作用,可能与其增加HepG2细胞的葡萄糖消耗量,促进葡萄糖的摄取有关。     

滋肾清肝代平方中7种成分血药浓度的测定及其在大鼠体内的药代动力学分析

目的:建立UPLC-MS-MS同时测定大鼠血浆中2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷,1-脱氧野尻霉素和决明子苷、红镰霉素龙胆二糖苷、橙黄决明素、甲基钝叶决明素、白藜芦醇的分析方法,研究大鼠服用滋肾清肝代平方后的药代动力学特征。方法:采用Waters Acquity UPLC BEH C18色谱柱,流动相0.1%甲酸水溶液-乙腈梯度洗脱,采用电喷雾电离源,扫描方式为多反应离子监测。结果:7种成分在大鼠血浆中线性关系良好,提取回收率94.83%~106.58%,日内、日间精密度和准确度良好。7种成分在模型组大鼠中的药时曲线下面积、末端半衰期、达峰时间、清除率、表观分布容积、药峰浓度分别为(326.65±26.66)μg·L-1·h-1,(3.64±1.69)h,0.33 h,(60.56±5.32)L·h-1·kg-1,(325.13±167.18)L·kg-1,(169.25±18.02)μg·L-1。结论:该方法特异、快速、准确、灵敏,可用于滋肾清肝代平方在大鼠体内的药动学研究。     

通莲汤对胃癌MGC803细胞周期及NF-κBs信号通路的影响

目的: 研究通莲汤对胃癌MGC803细胞形态、生长周期的调节作用及细胞核转录因子κB(NF-κB)信号通路的影响,以探讨该方抑制胃癌细胞增殖的机制。 方法: 将MGC803细胞以1×10⁴个细胞/孔的密度接种于96孔细胞培养板,以含5%胎牛血清DMEM培养液培养,37 ℃,5%饱和湿度的CO₂培养箱孵育,细胞贴壁24 h,分别加入浓度为25~800 mg·L^-1倍比梯度的通莲汤提取液,以10~160 mg·L^-1倍比浓度的氟脲嘧啶为阳性对照组,孵育48 h后,倒置显微镜下观察细胞形态,MTT比色法检测细胞增殖变化,曲线拟合法计算通莲汤和氟脲嘧啶50%抑制浓度(IC₅₀);以两者48 h IC₅₀浓度处理细胞48 h,流式细胞技术(FCM)测定细胞周期,Western blot法测定细胞IκB激酶β(IKKβ),NF-κB,phosph-NF-κB蛋白水平。 结果: 通莲汤和氟脲嘧啶48 h IC₅₀值分别为192.74 mg·L^-1,23.61 mg·L^-1;与空白对照组相比,通莲汤显著影响MGC803细胞周期中G₂期,氟脲嘧啶显著影响MGC803细胞周期中G₁期(P<0.05);通莲汤和氟脲嘧啶均能显著抑制IKKβ与NF-κB的蛋白表达。 结论: 通莲汤抑制MGC803细胞生长与抑制细胞于G₂期,下调NF-κB通路中IKKβ,NF-κB蛋白的表达有关。     

上海市社区居民中心性肥胖与打鼾对血脂异常的交互作用

目的 探讨上海市社区居民中心性肥胖与打鼾对血脂异常的交互作用。方法 利用2017年上海市慢性病及其危险因素监测数据（SHCR-2017）,通过多阶段分层抽样,合计纳入研究对象20 259人,应用多因素logistic回归评价中心性肥胖与打鼾对血脂异常患病的影响。采用相乘交互、相加交互作用模型评估中心性肥胖和打鼾对血脂异常患病的交互作用。结果 上海市血脂异常检出率为35.5%,高甘油三酯血症（18.2%）和低高密度脂蛋白胆固醇血症（15.8%）为主要特征。经混杂因素调整后,中心性肥胖（OR=1.74,95%CI:1.63～1.85)与打鼾（OR=1.16,95%CI:1.09～1.24）均与血脂异常相关。交互作用分析表明,中心性肥胖与打鼾对血脂异常患病无显著相乘交互作用（OR=0.98,95%CI:0.87～1.11）。两者对血脂异常患病存在相加交互作用（RERI=2.21,95%CI:1.61～2.81;SI=3.40,95%CI:3.07～3.78;AP=0.54,95%CI:0.49～0.58）。血脂异常四种临床类型中,研究对象对高甘油三酯血症、低高密度脂蛋白胆固醇血症患病的相加交...     

The anti-nausea effects of CB1 agonists are mediated by an action at the visceral insular cortex

BACKGROUND AND PURPOSE

Conditioned gaping reactions reflect nausea-induced behaviour in rats. Cannabinoid 1 receptor (CB₁) agonists interfere with the establishment of nausea-induced conditioned gaping; however, it is not known if their effects are mediated by an action at peripheral or central CB₁ receptors.

EXPERIMENTAL APPROACH

We utilized the conditioned gaping model of nausea to evaluate the effect of peripheral and central administration of the peripherally restricted CB₁ agonist, CB13, on the establishment of LiCl-induced gaping in rats. We further evaluated the ability of HU-210 administered to the gustatory insular cortex (GIC) or visceral insular cortex (VIC) to interfere with LiCl-induced conditioned gaping and determined if this effect was mediated by CB₁ receptors.

KEY RESULTS

Central, but not peripheral, CB13 suppressed LiCl-induced conditioned gaping. Central administration of the potent CB₁ agonist, HU-210, delivered to the VIC, but not the GIC, suppressed the establishment of LiCl-induced gaping reactions, but not LiCl-induced suppression of hedonic reactions or conditioned taste avoidance. This pattern of results suggests that HU-210 delivered to the VIC prevented LiCl-induced nausea, but not learning per se. The suppression of LiCl-induced conditioned gaping by HU-210 was mediated by CB₁ receptors because it was prevented by co-administration of CB₁ antagonist/inverse agonist, AM-251, into the VIC. A high dose of AM-251 (20 µg) administered alone into the VIC did not produce conditioned gaping reactions.

CONCLUSIONS AND IMPLICATIONS

The nausea-relieving effects of CB₁ agonists, but not the nausea-inducing effects of CB₁ inverse agonists, are mediated, at least in part, by their action at the VIC in rats.