Mechanism of action of Orthosiphon stamineus against non-alcoholic fatty liver disease: Insights from systems pharmacology and molecular docking approaches

Non-alcoholic fatty liver disease (NAFLD) is one of the most common complications of a metabolic syndrome caused by excessive accumulation of fat in the liver. Orthosiphon stamineus also known as Orthosiphon aristatus is a medicinal plant with possible potential beneficial effects on various metabolic disorders. This study aims to investigate the in vitro inhibitory effects of O. stamineus on hepatic fat accumulation and to further use the computational systems pharmacology approach to identify the pharmacokinetic properties of the bioactive compounds of O. stamineus and to predict their molecular mechanisms against NAFLD. Methods: The effects of an ethanolic extract of O. stamineus leaves on cytotoxicity, fat accumulation and antioxidant activity were assessed using HepG2 cells. The bioactive compounds of O. stamineus were identified using LC/MS and two bioinformatics databases, namely the Traditional Chinese Medicine Integrated Database (TCMID) and the Bioinformatics Analysis Tool for the Molecular Mechanism of Traditional Chinese Medicine (BATMAN-TCM). Pathway enrichment analysis was performed on the predicted targets of the bioactive compounds to provide a systematic overview of the molecular mechanism of action, while molecular docking was used to validate the predicted targets. Results: A total of 27 bioactive compounds corresponding to 50 potential NAFLD-related targets were identified. O. stamineus exerts its anti-NAFLD effects by modulating a variety of cellular processes, including oxidative stress, mitochondrial β-oxidation, inflammatory signalling pathways, insulin signalling, and fatty acid homeostasis pathways. O. stamineus is significantly targeting many oxidative stress regulators, including JNK, mammalian target of rapamycin (mTOR), NFKB1, PPAR, and AKT1. Molecular docking analysis confirmed the expected high affinity for the potential targets, while the in vitro assay indicates the ability of O. stamineus to inhibit hepatic fat accumulation. Conclusion: Using the computational systems pharmacology approach, the potentially beneficial effect of O. stamineus in NAFLD was indicated through the combination of multiple compounds, multiple targets, and multicellular components.     

Hypocholesterolaemic mechanism of bitter melon aqueous extracts via inhibition of pancreatic cholesterol esterase and reduction of cholesterol micellar solubility

This study investigated the hypocholesterolaemic effects of bitter melon aqueous extracts (BMAE) in vitro, the inhibitory effects of BMAE on pancreatic cholesterol esterase (CEase) and incorporation of cholesterol into micelles were investigated. BMAE decreased the in vitro micellar solubility of cholesterol in a dose-dependent manner. The conformation of CEase was investigated by means of circular dichroism (CD) and fluorescence. The result revealed the decrease of α-helix contents, increase of β-sheet and exposure of aromatic amino acid residuals. The incorporation of cholesterol into micelles was inhibited by BMAE. A complex was observed by transmission electron microscopy (TEM), which indicated interaction between cholesterol and BMAE. The result revealed that BMAE can play a role in decreased intestinal cholesterol absorption via inhibition of CEase, and of micelle formation.     

基于多元统计分析的银杏叶提取物中有机酸类成分含量研究

目的建立HPLC法测定银杏叶提取物中9种小分子有机酸类成分莽草酸、儿茶素、表儿茶素、没食子酸、原儿茶酸、6-羟基犬尿喹啉酸、对羟基苯甲酸、对羟基肉桂酸、咖啡酸含量的方法,并结合多元统计分析方法比较不同厂家生产的银杏叶提取物间质量差异。方法采用Inertsil ODS-3 C_(18)(250 mm×4.6 mm,5μm)色谱柱;以乙腈-0.4%磷酸水溶液为流动相,梯度洗脱,波长切换测定(220 nm检测莽草酸、儿茶素、表儿茶素,254 nm检测没食子酸、原儿茶酸、6-羟基犬尿喹啉酸、对羟基苯甲酸,310 nm检测对羟基肉桂酸、咖啡酸),柱温40℃。结果不同厂家生产的银杏叶提取物中有机酸总含量有差异,厂家内部样品中各有机酸含量同样存在差异。经聚类分析、主成分分析、相关与回归分析等多元统计方法分析,筛选出儿茶素、没食子酸、原儿茶酸及6-羟基犬尿喹啉酸为体现样品质量差异的特征成分,同时成分间具有内在相关性。结论建立的方法操作简便、重复性好、结果可靠,可用于银杏叶提取物中有机酸类成分的质量评价。筛选出的儿茶素、没食子酸、原儿茶酸及6-羟基犬尿喹啉酸是体现质量差异的特征成分,又是具有内在关联的共性成分,为提升银杏叶提取物整体质量控制能力提供了依据,同时表明银杏叶提取物的提取工艺并不统一,企业内部工艺的稳定性也有待提高。     

中药治疗创伤后应激障碍的研究进展

创伤后应激障碍(PTSD)是指突发性、威胁性或灾难性生活事件导致个体延迟出现和长期持续存在的精神障碍,其临床表现以再度体验创伤为特征,并伴有情绪的易激惹和回避行为。PTSD的发生不仅伴随着行为学指标异常,机制研究表明还表现出神经生物学指标异常。PTSD的发生机制研究多集中在神经内分泌系统、中枢神经系统和免疫系统等方面,主要表现为应激激素、促炎细胞因子、神经递质、神经保护因子的水平异常。中药因其具有多靶点、多成分和多途径的特点,在治疗PTSD方面表现出了许多优势。当前研究表明,多种中药能够改善PTSD模型中动物行为异常、逆转神经生物学指标。其中很多中药复方已经应用于临床并且具有很好的疗效,因此中药治疗PTSD具有广阔的应用前景。但是,尚未有PTSD的专属治疗药物,且尚未完全厘清PTSD的机制。故本文对当前中药治疗PTSD的研究进行综述,并且从治疗的中药种类、作用机制、动物模型等角度,重点阐述PTSD的发生与治疗进展,以期为PTSD的治疗提供参考。     

天麻素生物合成的研究进展

天麻素是我国名贵中药材天麻中的一种主要活性成分，具有降血压、抗癫痫、抑制肿瘤、保护神经等多方面的药理活性。随着市场对天麻素需求的不断增长以及传统获取方法固有的问题，导致急需新的方法来解决天麻素生产实际中面临的各项困难。生物合成法是一种有别于传统获取法的新方法，已在天麻素获取上取得了较大进展和成果，故现阶段有必要从天麻素生物合成途径、植物转化法和微生物转化法3个方面，对天麻素生物合成进行系统地阐述，从而为进一步改进和完善天麻素生产方法，以满足人们对其不断增长的需求提供有价值的参考。     

A Survey of Plants Used as Wild Vegetables in Four Districts of Botswana

A survey of plants used as wild vegetables was conducted in four districts of Botswana in August and September 2005. The objective was to determine which wild plants were used as vegetables in the study area, and to document their cooking and preservation methods. Fourteen species representing seven families were mentioned as wild vegetables. In addition, six species from four families had other uses in traditional medicine. The implications of the documented processing methods on the retention of nutrients in the vegetables are discussed.     

刺五加水提物对人精子体外运动活力的影响

目的研究刺五加水提物对正常男性精子体外运动活力的影响，探讨其可能的作用机制。方法将20例正常男性的精子通过上游优化法处理后，一组精子加入10 mg·mL^-1的刺五加水提物，另一组加入等量的Ham’s F10培养液作对照。应用计算机辅助的精子分析系统，分别测定孵育0.5，1，2，3，4，5 h后人精子各运动参数。结果随着时间的延长，加入Ham’s F10培养液的精子活动能力有不同程度的下降；加入10 mg·mL^-1的刺五加水提物后，不同时段精子的运动能力均较对照组明显提高，精子存活率、前向运动精子百分率、曲线运动速度、直线运动速度和平均路径速度与对照组比较，均明显改善(均P＜0.05)。 结论刺五加水提物能明显提高正常男性精子的体外存活率和运动能力。     

植物抗体及其应用

20世纪80年代末科学家将抗体基因转入烟草表达,标志着植物抗体的诞生.人类既可以以植物为生物反应器异源表达和生产具有药用及商业价值的蛋白质;也可用抗体在植物体中进行免疫调节,以研究植物生理代谢机制,或增加植物抵抗病虫害的能力.本文旨对植物抗体的优越性、表达生产及其在医药学、植物抗病及代谢等领域的进展进行综述和讨论.     

Antioxidant properties and xanthine oxidase inhibitory effects of Tamus communis L. root extracts

This study was conducted to search for xanthine oxidase (XO) inhibitors from the root extracts of Tamus communis L. traditionally used in folk medicine in Algeria. Root extracts with different solvents were screened for purified milk xanthine oxidase inhibition. The root extracts (methanol, chloroform and ethyl acetate) and proteins, obtained in distilled water, inhibited bovine, sheep and human milk XO from three species in a concentration-dependent manner, with an additional superoxide scavenging capacity, which reached its highest level with ethyl acetate extract (IC(50) = 0.15, 0.04 and 0.09 g/L) for bovine XO, sheep XO and human XO, respectively. The antioxidant potential was confirmed with the non-enzymatic method, total radical-trapping antioxidant parameter (TRAP) assay, which showed that the Tamus communis L. extracts have a potential antioxidant activity in the same order obtained by using the reduction of cytochrome c, an enzymatic method, in which the antioxidant activity followed a decreasing order: ethyl acetate extract > chloroform extract > protein.     

粤东地区菊科药用植物资源研究

资源丰富,共有植物64属、115 种.文章介绍了的种类、生境、药用功效和利用现状,提出了保护及开发利用菊科植物资源的一些建议.