桃红四物汤化学成分、药理作用、临床应用的研究进展及质量标志物的预测分析

桃红四物汤,活血祛瘀之经典名方。该文对近年来桃红四物汤的化学成分、药理作用以及临床应用研究进展进行总结与分析。目前,桃红四物汤不同提取部位化学成分的研究较为系统,其药理作用研究主要集中在活血化瘀、调经镇痛、促进骨折愈合等方面,临床可应用于多系统、多脏腑疾病的治疗,例如妇科疾病、内科疾病、骨伤科疾病、皮肤科疾病等。在此基础上,依照质量标志物(Q-marker)有效、特有、传递与溯源、可测和处方配伍的"五原则"对桃红四物汤Q-marker进行预测分析,提示阿魏酸、芍药苷、苦杏仁苷、芍药内酯苷、梓醇、没食子酸、羟基红花黄色素A可作为该复方的Q-marker,后续可选择这些Q-marker为指标,根据药材、饮片、中间体、对应实物的量值传递进行桃红四物汤全程质量控制并创建其质量可溯源体系。     

白术的化学成分与药理作用及复方临床应用进展

白术作为一味传统中药,在历代本草著作中广泛记载,其功效有一定演变。现代研究发现,其主要化学成分有挥发油、多糖、内酯类等,具有抗肿瘤、抗炎、调节消化系统等药理作用。临床以中药复方的形式应用于胃肠道疾病、心血管疾病、免疫系统疾病、肝脏疾病等治疗。对近5年SCI收录的白术相关文章进行分析,简述其化学成分,重点围绕着药理作用以及复方的临床应用展开论述,为其进一步开发利用提供参考。     

经典名方泽泻汤的HPLC指纹图谱及多指标含量测定研究

目的建立经典名方泽泻汤的HPLC指纹图谱,结合化学模式识别技术对其进行分析,并测定泽泻汤中3种成分23-乙酰泽泻醇B、23-乙酰泽泻醇C和白术内酯Ⅲ的含量,为泽泻汤质量控制提供科学依据。方法采用Waters WAT054275C18色谱柱(250 mm×4.6 mm,5μm),以乙腈-水为流动相进行梯度洗脱,建立15批泽泻汤的HPLC指纹图谱,并采用"中药色谱指纹图谱相似度评价系统"、SPSS22.0及SIMCA14.1软件对15批泽泻汤的HPLC指纹图谱进行相似度评价及聚类分析(CA)、偏最小二乘判别分析(PLS-DA)等化学模式识别。同时测定23-乙酰泽泻醇B、23-乙酰泽泻醇C和白术内酯Ⅲ的含量。结果建立了15批泽泻汤的HPLC指纹图谱,相似度均0.94,标定了18个共有峰,指认出3个色谱峰,分别为11号峰白术内酯Ⅲ、15号峰23-乙酰泽泻醇C、16号峰23-乙酰泽泻醇B,CA和PLS-DA将15批泽泻汤样品分为2类,同时15批泽泻汤中23-乙酰泽泻醇B、23-乙酰泽泻醇C和白术内酯Ⅲ的质量分数分别为0.321～0.569、0.075～0.139、0.106～0.142 mg/g。结论 HPLC指纹图谱结合多成分同时测定的方法,快速、简便、重复性好,为泽泻汤及其制剂的质量评价提供参考。     

木鳖子化学成分、毒理与药理作用研究进展

木鳖子是一味传统的有毒中药,始载于北宋《开宝本草》,具有消肿散结,攻毒疗疮的功效,用于治疗疮疡肿毒,乳痈,秃疮等。主要分布在广西、广东等中国南方地区,泰国、越南等东南亚国家也有分布。目前研究表明从木鳖子中提取分离得到的化学成分丰富,主要包括萜类、甾醇类、挥发油类、脂肪酸类等成分。其中已鉴定的萜类化合物30种、挥发油成分102种、植物甾醇6种和脂肪酸类19种。毒理学研究表明,木鳖子水提物及醇提物均含有一定的毒性,毒性随着含油量的增大呈现降低趋势,目前文献报道的主要有毒成分是木鳖子素和木鳖子皂苷类。药理学研究表明,木鳖子除了具有基于传统功效的抗癌、抗炎、抗菌等药理作用外,还具有抗溃疡、抗氧化、调节免疫等多种药理作用。近几年对木鳖子的研究报道不断增多,通过查找中国知网,万方,Pub Med,Web of Science等数据库1964-2019年的国内外相关文献,对木鳖子化学成分,药理作用,毒理研究等方面进行归纳总结,为今后对木鳖子的深入研究应用提供参考。     

Discovery of nitazoxanide-based derivatives as autophagy activators for the treatment of Alzheimer's disease

Drug repurposing is an efficient strategy for new drug discovery. Our latest study found that nitazoxanide (NTZ), an approved anti-parasite drug, was an autophagy activator and could alleviate the symptom of Alzheimer's disease (AD). In order to further improve the efficacy and discover new chemical entities, a series of NTZ-based derivatives were designed, synthesized, and evaluated as autophagy activator against AD. All compounds were screened by the inhibition of phosphorylation of p70S6K, which was the direct substrate of mammalian target of rapamycin (mTOR) and its phosphorylation level could reflect the mTOR-dependent autophagy level. Among these analogs, compound 22 exhibited excellent potency in promoting β-amyloid (Aβ) clearance, inhibiting tau phosphorylation, as well as stimulating autophagy both in vitro and in vivo. What's more, 22 could effectively improve the memory and cognitive impairments in APP/PS1 transgenic AD model mice. These results demonstrated that 22 was a potential candidate for the treatment of AD.     

iPhone charger-induced chemical burn from overnight contact with sweat: Two cases

Smartphones have become essential devices in modern society. The coverage rate of smartphones in 2017 in Japan was 75% according to the Ministry of Internal Affairs and Communications. The iPhone is one of the most well-known smartphone brands. According to the manufacturer of iPhones (Apple), more than 200 million iPhones had been sold worldwide by 2017. These devices are often charged at night-time, especially while being used in bed. There are only three reports of smartphone charger-induced skin damage. We present two new cases of skin ulcers induced by an iPhone charger. The iPhone’s “lightning cable” has electrodes outside, and we found that this can present a higher risk of causing a skin injury compared with other types of phone chargers. We also investigated the mechanism of the skin ulcers caused by the iPhone charger. The results indicated that these ulcers were chemical burns rather than an electrical injury or heat-induced burn.     

Achieving CLARITY on bisphenol A,brain and behaviour

There is perhaps no endocrine disrupting chemical more controversial than bisphenol A (BPA). Comprising a high‐volume production chemical used in a variety of applications, BPA has been linked to a litany of adverse health‐related outcomes, including effects on brain sexual differentiation and behaviour. Risk assessors preferentially rely on classical guideline‐compliant toxicity studies over studies published by academic scientists, and have generally downplayed concerns about the potential risks that BPA poses to human health. It has been argued, however, that, because traditional toxicity studies rarely contain neural endpoints, and only a paucity of endocrine‐sensitive endpoints, they are incapable of fully evaluating harm. To address current controversies on the safety of BPA, the United States National Institute of Environmental Health Sciences, the National Toxicology Program (NTP), and the US Food and Drug Administration established the Consortium Linking Academic and Regulatory Insights on BPA Toxicity (CLARITY‐BPA). CLARITY‐BPA performed a classical regulatory‐style toxicology study (Core study) in conjunction with multiple behavioural, molecular and cellular studies conducted by academic laboratories (grantee studies) using a collaboratively devised experimental framework and the same animals and tissues. This review summarises the results from the grantee studies that focused on brain and behaviour. Evidence of altered neuroendocrine development, including age‐ and sex‐specific expression of oestrogen receptor (ER)α and ERβ, and the abrogation of brain and behavioural sexual dimorphisms, supports the conclusion that developmental BPA exposure, even at doses below what regulatory agencies regard as “safe” for humans, contribute to brain and behavioural change. The consistency and the reproducibility of the effects across CLARITY‐BPA and prior studies using the same animal strain and almost identical experimental conditions are compelling. Combined analysis of all of the data from the CLARITY‐BPA project is underway at the NTP and a final report expected in late 2019.     

Intestinal polycyclic aromatic hydrocarbon-DNA adducts in a population of beluga whales with high levels of gastrointestinal cancers

Carcinogenic polycyclic aromatic hydrocarbons (PAHs) were disposed directly into the Saguenay River of the St. Lawrence Estuary (SLE) by local aluminum smelters (Quebec, Canada) for 50 years (1926–1976). PAHs in the river sediments are likely etiologically related to gastrointestinal epithelial cancers observed in 7% of 156 mature (>19-year old) adult beluga found dead along the shorelines. Because DNA adduct formation provides a critical link between exposure and cancer induction, and because PAH–DNA adducts are chemically stable, we hypothesized that SLE beluga intestine would contain PAH–DNA adducts. Using an antiserum specific for DNA modified with several carcinogenic PAHs, we stained sections of paraffin-embedded intestine from 51 SLE beluga (0–63 years), 4 Cook Inlet (CI) Alaska beluga (0–26 years), and 20 beluga (0–46 years) living in Arctic areas (Eastern Beaufort Sea, Eastern Chukchi Sea, Point Lay Alaska) and aquaria, all with low PAH contamination. Stained sections showed nuclear light-to-dark pink color indicating the presence of PAH–DNA adducts concentrated in intestinal crypt epithelial lining cells. Scoring of whole tissue sections revealed higher values for the 51 SLE beluga, compared with the 20 Arctic and aquarium beluga (P = 0.003). The H-scoring system, applied to coded individual photomicrographs, confirmed that SLE beluga and CI beluga had levels of intestinal PAH–DNA adducts significantly higher than Arctic and aquarium beluga (P = 0.003 and 0.02, respectively). Furthermore, high levels of intestinal PAH–DNA adducts in four SLE beluga with gastrointestinal cancers, considered as a group, support a link of causality between PAH exposure and intestinal cancer in SLE beluga. Environ. Mol. Mutagen. 60:29–41, 2019. Published 2018. This article is a U.S. Government work and is in the public domain in the USA.     

血芙蓉化学成分的研究

目的研究血芙蓉Teucrium viscidum Bl.的化学成分。方法血芙蓉70%乙醇提取物采用硅胶、ODS、Sephadex LH-20凝胶柱进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果从中分离得到20个化合物,分别鉴定为20β-羟基熊果酸(1)、β-谷甾醇(2)、羽扇豆醇(3)、齐墩果酸(4)、木犀草素(5)、槲皮素(6)、芹菜素(7)、β-胡萝卜苷(8)、芹菜素-7-O-β-D-葡萄糖苷(9)、teuvisone (10)、lipidiol (11)、teucvisin B (12)、1,5,9-epideoxyloganin (13)、1,5,9-epideoxyloganic acid (14)、5-epideoxyloganin (15)、argylioside (16)、8-epideoxyloganic acid (17)、radiatoside E (18)、radiatoside F (19)、enmenol-glucoside (20)。结论化合物1、3、7、9、13~20为首次从该植物中分离得到,化合物1、13~20为首次从石蚕属植物中分离得到。