海南黎药海巴戟药材质量标准研究

为建立黎药海巴戟药材质量标准,为其质量控制及资源开发利用提供科学依据。依据《中国药典》2015 年版中药质量标准研制的要求,对药材性状、鉴别、检查、浸出物、含量测定等进行研究。明确了海巴戟药材性状和显微结构特征,并建立了其专属性薄层色谱鉴别方法;规定海巴戟药材多糖含量不得少于 6.0%、东莨菪内酯含量不得低于 0.017%、水分不得超过 10.0%、总灰分不得超过 6.0%以及醇溶性浸出物不得少于 20.0%。本研究制定的黎药海巴戟药材质量标准,可为该药材的质量控制提供依据。     

Fucoxanthin,a Marine Carotenoid,Reverses Scopolamine-Induced Cognitive Impairments in Mice and Inhibits Acetylcholinesterase in Vitro

Fucoxanthin, a natural carotenoid abundant in edible brown seaweeds, has been shown to possess anti-cancer, anti-oxidant, anti-obesity and anti-diabetic effects. In this study, we report for the first time that fucoxanthin effectively protects against scopolamine-induced cognitive impairments in mice. In addition, fucoxanthin significantly reversed the scopolamine-induced increase of acetylcholinesterase (AChE) activity and decreased both choline acetyltransferase activity and brain-derived neurotrophic factor (BDNF) expression. Using an in vitro AChE activity assay, we discovered that fucoxanthin directly inhibits AChE with an IC₅₀ value of 81.2 μM. Molecular docking analysis suggests that fucoxanthin likely interacts with the peripheral anionic site within AChE, which is in accordance with enzymatic activity results showing that fucoxanthin inhibits AChE in a non-competitive manner. Based on our current findings, we anticipate that fucoxanthin might exhibit great therapeutic efficacy for the treatment of Alzheimer’s disease by acting on multiple targets, including inhibiting AChE and increasing BDNF expression.     

曼陀罗化学成分与生物活性研究现状及展望

概述了曼陀罗化学成分、生物活性、有效成分、致毒机理、作用方式及应用等方面的研究进展.提出了今后研究的主要方向.     

龙眼果肉提取物改善东莨菪碱诱导小鼠学习记忆功能

【目的】比较不同剂量龙眼果肉醇提物和水提物对东莨菪碱所致记忆获得性障碍小鼠学习记忆功能的影响,初步解释龙眼果肉改善学习记忆的作用机制。【方法】分析龙眼果肉醇提物和水提物中主要活性物质含量。将无特定病原体(SPF级)雄性昆明小鼠随机分为空白组、模型组、龙眼果肉醇提物低剂量组/高剂量组(150 mg·kg~(-1)/300mg·kg~(-1))、龙眼果肉水提物低剂量组/高剂量组(150 mg·kg~(-1)/300 mg·kg~(-1)),共6组,连续灌胃28 d后,空白组腹腔注射等量生理盐水,各试验组腹腔注射东莨菪碱造模,0.5 h后,以潜伏期和穿梭次数为考察指标,采用避暗试验进行行为学测试,作为习得成绩;24 h后再次进行避暗试验,对小鼠进行记忆保持测试,测试结束后摘眼球取血,脱颈致死,取脑组织进行生化指标检测。测定脑组织的胆碱类(乙酰胆碱转移酶choline acetyltransferase,ChAT和乙酰胆碱酯酶acetylcholinesterase,AChE活力)及抗氧化相关指标(超氧化物歧化酶(superoxide dismutase,SOD)、谷胱甘肽过氧物酶(glutathione peroxidase,GSH-Px)活力及丙二醛(malondialdehyde,MDA)含量),血清中抗氧化相关指标(SOD、GSH-Px活力及MDA含量)。通过综合比较各组间行为学试验指标、脑组织、血清生化指标,判断龙眼果肉改善学习记忆功能的作用效果及作用机制。【结果】分析龙眼果肉提取物成分发现,龙眼果肉水提物主要为多糖及蛋白质,醇提物除含有糖类外,还含有较丰富的酚类、黄酮类和磷脂物质,其中,醇提物中总酚、总黄酮、总磷脂含量显著高于水提物的(P0.05)。行为学试验表明,模型组小鼠在避暗试验中5 min内穿梭次数为2.89次,是正常小鼠的6.09倍,高剂量龙眼果肉醇提物和水提物组小鼠穿梭次数分别为0.75次和0.56次,与正常组无显著差异;痴呆小鼠在避暗试验中的潜伏期仅为正常组的0.43倍,与模型组相比,各剂量龙眼果肉醇提物和水提物均能显著增加痴呆小鼠在避暗试验中的潜伏期(P0.05),且存在一定剂量效应关系,其中龙眼果肉醇提物和水提物高剂量组小鼠的避暗潜伏期分别为289.18 s、290.80 s,与正常组相比无显著差异(P0.05)。生化指标方面,与模型组相比,各剂量龙眼果肉醇提物和水提物均能显著增加痴呆小鼠脑组织中ChAT活力,显著降低AChE活力(P0.05),且存在一定的剂量效应关系。相同剂量时,龙眼果肉水提物效果优于醇提物,其中龙眼果肉醇提物高剂量组,龙眼果肉水提物低、高剂量组小鼠脑组织中ChAT活力基本恢复正常水平;在抗氧化水平方面,与模型组相比,龙眼果肉醇提物高剂量组显著增加痴呆小鼠脑组织和血清中SOD、GSH-Px活力,显著降低MDA含量(P0.05),基本达到正常水平,效果优于同等剂量的龙眼果肉水提物。【结论】龙眼果肉水提物和醇提物均可改善东莨菪碱诱导记忆获得性障碍小鼠的学习记忆功能,但二者的作用机制可能存在差异,龙眼果肉水提物主要通过调节胆碱能神经系统改善学习记忆功能,其主要作用的物质基础可能为多糖或糖蛋白;醇提物则主要通过提高机体抗氧化活力改善学习记忆功能,其主要作用物质可能为多酚、黄酮、磷脂等。     

Selection for High Tropane Alkaloid Content in Hyoscyamus muticus Plants

Egyptian henbane, Hyoscyamus muticus L. (Sol-anaceae) is an important source of pharmaceutically valuable compounds, the tropane alkaloids. Even today these alkaloids, scopolamine and hyoscyamine, are extracted on an industrial scale from plants. We have studied the possibilities of increasing the scopolamine content in H. muticus plants by selection during several generations. The quantitative scopolamine and hyoscyamine determinations were performed on the dry leaf material by radio and enzymeimmunoassay. The increased production of these alkaloids by the progenies was an inherited attribute resulting from systematic selection for high-alkaloid-containing plants (inbred). The scopolamine content in the F₁ generation was increased by a factor of 3 and in the F₄ generation by a factor of 20 compared to the P generation, respectively. The year-to-year fluctuation among the mean scopolamine contents of the control groups was small. The maximal scopolamine content in H. muticus strain Cairo exceeded 4%, which is the highest content so far reported in the literature. When crossing the high and low scopolamine-producing plants, the scopolamine content of the progenies was found to be intermediate between that of the two parents, thus indicating that scopolamine synthesis is inherited by the progenies from both parents. The alkaloid production of the plants grown in the greenhouse was significantly higher than those grown in the field.