鲜山豆根干燥加工炮制方法实践及探讨

山豆根在《中国药典》中记载为"有毒"。文献报道其毒性成分主要为苦参碱和氧化苦参碱,苦参碱毒性大于氧化苦参碱。通过对其干燥加工炮制方法及用法与毒性关系进行回顾性研究,提出直接用鲜山豆根切制饮片的思路并进行实践。鲜山豆根采挖后快速清洗,快速晾干表面水分,快速横切成5 mm厚片,快速干燥,其后检测发现苦参碱含量为0.031%,在一定程度上起到了控制和减少苦参碱含量以降低毒性的作用。     

N-9,10-蒽醌-2-甲酰基苯丙氨酸治疗大鼠痛风性关节炎的作用及机制

目的 探究N-9,10-蒽醌-2-甲酰基苯丙氨酸(NAY)对尿酸钠(MSU)所致痛风性关节炎(GA)大鼠的作用及机制。方法 将雄性SD大鼠随机分为7组,每组8只,即正常组、模型组、NAY低(20 mg·kg^-1)、中(40 mg·kg^-1)、高剂量组(80 mg·kg^-1)、秋水仙碱组(0.8 mg·kg^-1)和别嘌呤醇组(10 mg·kg^-1),通过关节腔内注射MSU晶体建立大鼠急性GA模型,各组灌胃给药5 d,给药第3天造模。将原代培养的大鼠腹部巨噬细胞分成空白组、模型组、NAY组、MCC950组和联合给药组。软尺测量大鼠踝关节周长并计算大鼠关节肿胀度;检测大鼠血清尿酸(UA)、肌酐(CRE)和尿素氮(BUN)含量;HE染色观察大鼠踝关节滑膜组织病理切片;检测各组血清、关节滑膜和细胞上清液中肿瘤坏死因子-α(TNF-α)和白介素-1β(IL-1β)的含量;并检测各组关节滑膜和细胞中NOD样受体热蛋白结构域相关蛋白3(NLRP3)、凋亡相关斑点样蛋白(ASC)和半胱氨酸天冬氨...     

共无定形体系提高甲磺酸乐伐替尼的溶出度及消除其凝胶化研究

甲磺酸乐伐替尼(LF)是一种多靶点酪氨酸酶抑制剂,主要用于治疗多种肿瘤.因其溶出过程中发生凝胶化而导致溶出度下降,生物利用度低.本研究通过旋蒸法制得甲磺酸乐伐替尼-黄芩素(LF-BAI)共无定形物(物质的量比为1:1),以提高LF溶出度的同时消除其凝胶化.利用偏光显微观察、粉末X射线衍射法、差示扫描量热法、傅里叶变换红...     

姜黄素改善非酒精性脂肪性肝病的研究进展

非酒精性脂肪性肝病(Non-alcoholic fatty liver disease,NAFLD)是目前全球最常见的慢性肝病之一,发病率呈现不断上升的趋势。姜黄素是从姜科植物姜黄中提取的具有多种生物活性的多酚类化合物。大量研究证实姜黄素具有良好的降脂、抗炎、抗氧化、抗纤维化等药理活性,并且对NAFLD、肥胖、胰岛素抵抗等多种代谢性疾病疗效显著,因而有着重要的临床价值和广阔的应用前景。就姜黄素治疗NAFLD的药理学作用及相关机制研究进行综述,旨在为姜黄素治疗代谢性疾病的研究提供参考,并推广其预防和改善NAFLD以及其它脂质代谢紊乱相关疾病可能的临床应用。      

Amphotericin B releasing nanoparticle topical treatment of Candida spp. in the setting of a burn wound

Candida spp. infection in the context of burn wounds leads to invasive disease with a 14–70% mortality rate. Unfortunately, current administrations of AmB, an important therapeutic demonstrating minimal resistance, are only available via potentially cytotoxic IV infusions. In order to circumvent these sequelae, we investigated the efficacy of nanoparticle encapsulated AmB (AmB-np) as a topical therapeutic against Candida spp. (drug release equilibrated solubilized AmB [AmB-sol] included as control). Clinical strains demonstrated equal or enhanced killing efficacy with 72.4–91.1% growth reduction by 4 hours. AmB-nps resulted in statistically significant reduction of fungal biofilm metabolic activity ranging from 80% to 95% viability reduction (P< 0.001). Using a murine full-thickness burn model, AmB-np exhibited a quicker efficiency in fungal clearance versus AmB-sol by day three, although wound healing rates were similar. These data support the concept that AmB-np can function as a topical antifungal in the setting of a burn wound.From the Clinical EditorThe control of fungal infections with Candida species remains a challenge in the context of burn wounds. A nanoencapsulated topical amphotericin-B compound was studied in a murine model of full thickness burn injury, showing remarkable efficacy in controlling Candida infection. This may become a viable alternative to the potentially toxic intravenous formulations.     

Esterified sterols and their contribution to the total sterols in edible mushrooms

Mushrooms are a valued source of sterols, which can be present in free form and esterified to fatty acids. In addition to the principal ergosterol, several minor sterols occur. Ergosterol and ergosteryl ester were determined directly by gas chromatography coupled to mass spectrometry (GC/MS) in the trimethylsilylated lipid extract of each six samples of button mushrooms, oyster mushrooms, king trumpet mushrooms and shiitake. Free ergosterol was highest in button mushrooms 415–544 mg/100 g dry matter (d.m.) and lowest in oyster and king trumpet mushrooms (<350 mg/100 g d.m.). On the other hand, concentrations of ergosteryl esters were significantly lower (5–26 mg/100 g d.m.) in all mushroom samples. The distribution of minor sterols (most importantly ergosta-7,22-dienol, ergosta-5,7-dienol, ergosta-7-enol) between free and esterified form was determined after group separation with solid phase extraction. Higher proportions of the minor sterols were found esterified to fatty acids and ergosta-7-enol was found predominantly (70%) in this form in oyster mushrooms and shiitake. The minor sterols ergosta-8,24(24¹)-dienol, ergosta-8-enol and 7-dehydro-poriferasterol could be tentatively identified in the samples based on GC/MS data. In addition, four sterols were found only in the steryl ester fraction of the mushroom samples.