小檗红碱的化学与药理

小檗红碱在黄连等中药材中的自然含量很低,但相关药材中的小檗碱在加热条件下可以转化成小檗红碱而使其含量增加.随着对传统中药材微量成分药理活性和药用安全性的日益关注,小檗红碱在相关中药中的治疗作用及安全性已经引起天然药物学领域专家的重视,本文在参考最新文献的基础上,对小檗红碱的化学合成方法、含量分析方法和药理作用等方面进行综述,拟为相关中药质量研究与药理研究提供参考     

小檗碱抗氧化和抗炎作用用于糖尿病治疗的机制研究进展

研究表明氧化应激反应和慢性炎症反应是2型糖尿病糖、脂代谢紊乱和胰岛素抵抗发生的重要病理机制。小檗碱是中药黄连的主要有效成分之一。体内、外研究证实小檗碱可通过抗氧化和抗炎作用发挥对2型糖尿病的治疗作用。本文就小檗碱抗氧化和抗炎作用用于2型糖尿病治疗的分子机制研究进展作一综述。小檗碱抗氧化和抗炎作用机制复杂,目前的研究显示小檗碱可通过AMPK通路、MAPK通路、Nrf2通路和NF-κB通路发挥抗氧化和抗炎作用。然而,小檗碱的抗氧化和抗炎作用仍需进一步的深入研究证实。明确小檗碱的抗氧化和抗炎作用的分子机制,有助于进一步了解小檗碱治疗糖尿病作用的机理,为探寻治疗糖尿病的天然药物提供理论依据。     

小檗碱的抗菌作用研究进展

小檗碱在临床上广泛运用于抗痢治疗,其抗菌作用被认为是其发挥抗痢作用的主要药理学机制.小檗碱的体内外抗茵活性明显,其抗茵机制可能涉及对多种酶蛋白活性抑制,肠毒素拮抗作用和抗粘附作用等机制.小檗碱的直接抗茵作用可能与其非特异性蛋白抑制作用有关.     

小檗碱调节糖脂代谢及其抗糖尿病活性的研究

小檗碱(berberine,BBR)是中药黄连的主要活性成分,属于异喹啉类生物碱,具有广谱抗菌作用。近年来发现它还有降血糖、降血脂、免疫调节及改善充血性心力衰竭等药理作用。研究表明,BBR能够改善糖尿病相关疾病的症状,且作用广泛,不仅可影响编码基因的表达,还与miRNA和lncRNA等非编码基因关系密切,涉及糖脂代谢、肠道菌群等多个方面。该文拟就BBR调节糖脂代谢及其抗糖尿病活性的研究进展做一综述。     

三颗针活性成分的研究

以~3H-硫氮草酮受体结合分析法为指标,从三颗针中分离得到四个生物碱活性单体,经光谱鉴定为小檗碱、小檗胺、巴马汀及药根碱。其中小檗胺为钙拮抗主要活性成分,并在红细胞过氧化氢实验中表现有较强的抗脂质过氧化活性,这些作用为其防治心肌缺血、抗心律不齐的机制提供有益的信息。     

穿心莲内酯等中药有效成分对表皮葡萄球菌生物膜渗透性的比较

目的比较穿心莲内酯、大黄素、盐酸小檗碱等对表皮葡萄球菌生物膜的渗透性,为中药治疗表皮葡萄球菌引起的相关感染提供相关研究的依据。方法在体外建立SE—BF（表皮葡萄球菌生物膜模型）和PB（生物膜渗透模型）,观察穿心莲内酯、大黄素、盐酸小檗碱等中药有效成分对PB的渗透率。结果大黄素、穿心莲内酯36h渗透率分别达到88．00％、82．89％,而盐酸小檗碱渗透率在几种药物中相对较差。结论中药有效成分对表皮葡萄球菌生物膜有较强的渗透性。     

小檗碱对大鼠肠道菌群结构的体外影响

目的研究小檗碱在体外对高脂饮食诱导的肥胖、胰岛素抵抗大鼠(HFD)肠道菌群和正常饮食对照大鼠(NCD)肠道菌群结构的体外影响。方法采用体外厌氧培养、PCR-DGGE和454焦磷酸测序技术研究小檗碱对肠道菌群结构和多样性的影响。结果 DGGE指纹图谱和454焦磷酸测序结果都表明,小檗碱可以改变肠道菌群的结构,高剂量的小檗碱可以减少肠道微生物的多样性。应用偏最小二乘法判别模型分析(PLS-DA)挑选与小檗碱相关的细菌类群(OTU),在HFD组中挑选了55个关键OTUs,其中53个被明显抑制或消除,剩余2个分别属于Proteus和Escherichia/Shigella属的OTUs则被小檗碱富集。在NCD组中挑选的51个关键OTUs中,32个被小檗碱抑制,17个被小檗碱富集。被富集的除了属于Klebsielal属的OTU外,还包括可以产生短链脂肪酸的Lactobacillus、Blautia属的OTUs。结论小檗碱可以直接调节肠道菌群的结构,对不同结构的肠道菌群其作用也不相同,不同浓度的小檗碱对肠道菌群的影响有较大差异。高浓度的小檗碱可以抑制大部分细菌的生长(其中有很多为肠道条件致病菌),减少肠道微生物的多样性,富集Enterobacteriaceae科的细菌(Proteus、Escherichia/Shigella、Klebsielal)。相较于HFD组,小檗碱可以显著富集NCD组大鼠肠道菌群中的短链脂肪酸产生菌。     

蓖麻植物化学成分及生物活性研究进展CSCD

蓖麻(Ricinus communis L.)为大戟科蓖麻属植物,其整株可作为传统中药和民族药使用,具有治疗跌打损伤、泻下通滞和消肿拔毒等功效。化学研究表明,蓖麻具有多种化学成分,类型涉及萜类、甾醇类、黄酮类、脂肪酸类、生育酚类、生物碱类、酚酸类和香豆素类,而且提取物及单体成分具有广泛的药理活性,包括抗肿瘤、抗糖尿病、抗氧化、消炎镇痛、抗生育、神经抑制、抑菌和杀虫等。本文旨在综述蓖麻的化学成分和生物药理活性,以期为蓖麻的后续研究和综合开发利用提供科学依据。     

一测多评法测定不同产地黄柏炭中4种生物碱含量

为建立同时测定不同产地黄柏炭中4种生物碱成分(黄柏碱、木兰花碱、小檗红碱、小檗碱)的一测多评法。实验以小檗碱为内参物,基于HPLC法建立小檗碱与其它成分的相对校正因子,并用校正因子计算4种成分的含量;用外标法和一测多评法同时测定30批黄柏炭样品的含量。结果表明30批黄柏炭样品的外标法与一测多评法结果之间无明显差异,说明了一测多评法的准确性和可行性。因此在缺乏对照品的情况下,以小檗碱为内参物同时测定黄柏碱、木兰花碱、小檗红碱的含量是可行的。该方法准确性和重复性良好,可用于黄柏炭的质量控制。     

银杏叶提取物抗肿瘤机制研究进展

银杏叶提取物已被广泛应用于治疗心血管和外周血管灌注不足、过敏性疾病和神经性疾病等,最近研究证明银杏叶提取物对多种肿瘤具有抑制作用,其机制主要包括诱导凋亡、抗氧化和免疫调节等,银杏叶提取物抗肿瘤作用的具体研究对指导临床预防和治疗肿瘤有重要意义,对目前银杏叶提取物的抗肿瘤机制做一综述。     

Berberine Attenuates Axonal Transport Impairment and Axonopathy Induced by Calyculin A in N2a Cells

Berberine is a primary component of the most functional extracts of Coptidis rhizome used in traditional Chinese medicine for centuries. Recent reports indicate that Berberine has the potential to prevent and treat Alzheimer''s disease (AD). The previous studies reported that Calyculin A (CA) impaired the axonal transport in neuroblastoma-2a (N2a) cells. Berberine attenuated tau hyperphosphorylation and cytotoxicity induced by CA. Our study aimed at investigating the effects of Berberine on the axonal transport impairment induced by CA in N2a cells. The results showed that Berberine could protect the cell from CA -induced toxicity in metabolism and viability, as well as hyperphosphorylation of tau and neurofilaments (NFs). Furthermore, Berberine could reverse CA-induced axonal transport impairment significantly. Berberine also partially reversed the phosphorylation of the catalytic subunit of PP-2A at Tyrosine 307, a crucial site negatively regulating the activity of PP-2A, and reduced the levels of malondialdehyde and the activity of superoxide dismutase, markers of oxidative stress, induced by CA. The present work for the first time demonstrates that Berberine may play a role in protecting against CA-induced axonal transport impairment by modulating the activity of PP-2A and oxidative stress. Our findings also suggest that Berberine may be a potential therapeutic drug for AD.     

伊犁河流域红果小檗资源分布与形态调查

红果小檗(Berberis nummularia Bge.)系小檗科(Berberidaceae)小檗属(Berberis L.)植物,是新疆及中亚地区特有的植物物种之一.对伊犁河流域的药食兼用植物红果小檗(Berberis nummularia Bge.)的资源分布、形态特征、生态条件、繁殖特征及人工栽培等进行了综合调查、对植物各部位标本采集及采样分析研究,并对其药用价值、经济价值、生态价值、观赏价值、资源开发及保护管理等方面进行了系统地探讨,为民族药的发掘和整理、丰富中华民族中药宝库以及野生植物资源的保护和合理开发可持续性利用提供了科学依据.     

Pharmacotherapeutic values of berberine: A Chinese herbal medicine for the human cancer management

Berberine (BBR), a traditional Chinese phytomedicine extracted from various parts of Berberis plants, is an isoquinoline alkaloid used for centuries to treat diabetes, hypercholesterolemia, hypertension, and so forth. It has recently received immense attention worldwide to treat cancer due to its potent pro-apoptotic, antiproliferative, and anti-inflammatory properties. BBR efficiently induces tumor apoptosis, replicative quiescence and abrogates cell proliferation, epithelial–mesenchymal transition, tumor neovascularization, and metastasis by modulating diverse molecular and cell signaling pathways. Furthermore, BBR could also reverse drug resistance, make tumor cells sensitive to current cancer treatment and significantly minimize the harmful side effects of cytotoxic therapies. This review comprehensively analyzed the pharmacological effects of BBR against the development, growth, progression, metastasis, and therapy resistance in wide varieties of cancer. Also, it critically discusses the significant limitations behind the development of BBR into pharmaceuticals to treat cancer and the future research directions to overcome these limitations.     

Berberine inhibits human colon cancer cell migration via AMP-activated protein kinase-mediated downregulation of integrin β1 signaling

Colon cancer is associated with a poor prognosis, motivating strategies to prevent its development. An encouraging preventative strategy is the use of nutraceuticals; however, scientific verification of therapeutic functions and mechanisms of biological activity are necessary for the acceptance of dietary supplements in cancer treatment. Berberine is a benzylisoquinoline alkaloid extracted from many kinds of medicinal plants that has been extensively used as a Chinese traditional medicine. Recently, berberine has been reported to possess antitumoral activities. Among the various cellular targets of berberine is AMP-activated protein kinase (AMPK), which regulates tumor progression and metastasis. However, the specific role of berberine-induced AMPK activation and its effects on the metastatic potential of colon cancer remain largely unknown. The present study investigated berberine-induced activation of AMPK and its effects on colon cancer cell migration. Berberine decreased the migration of SW480 and HCT116 cells. We found that berberine activated AMPK in human colon cancer cell lines. Notably, berberine-induced activation of AMPK reduced the integrin β1 protein levels and decreased the phosphorylation of integrin β1 signaling targets. Knockdown of AMPKα1 subunits using small interfering RNA significantly attenuated berberine-induced downregulation of integrin β1 and inhibition of tumor cell migration. Collectively, our results suggest that berberine-induced AMPK activation inhibits the metastatic potential of colon cancer cells by decreasing integrin β1 protein levels and downstream signaling.     

广西龙胜红瑶传统药用植物的民族植物学知识

瑶族是一个拥有悠久历史和灿烂文化的民族,红瑶是其中一个分支,因妇女服饰上的花纹图案以大红色为主而得名,其生活习俗饱含民族特色,对植物尤其是药用植物的利用方式,与其他民族不同。该研究采用经典的民族植物学理论和方法,访问调查了广西龙胜红瑶传统药用植物种类,根据植物拉丁名、中文名、当地名、用途、用法及药用部位,对其进行民族植物学编目,并与《中国药典》作了比较。结果表明:共记录到药用植物95种,隶属于57科83属,其中蔷薇科、百合科种类最多,分别含有7种,显示龙胜红瑶传统药用植物资源的多样性;全株入药的植物种类41种,占总数的43.16%;根入药的种类为23种,占总数的24.21%;叶入药的种类为13种,占总数的13.68%。药用植物的药用部位以全株、根及叶为主;治疗风湿类疾病的药物比重最大,为23.47%,推测与其生活的环境有关;与《中国药典》比较,发现71种植物未被其收录,另有17种虽被收录但主治功效不同,有7种被收录且主治功效大致相同,为新型中药的研发提供了借鉴。同时,还探讨了龙胜红瑶传统药用植物的药用价值、资源现状及文化传承的问题。     

氮素形态对黄檗幼苗三种生物碱含量的影响

通过改变水培溶液中NH 4-N和NO3--N的比例,探讨了氮素形态对黄檗幼苗主要药用成分小檗碱、药根碱及掌叶防己碱含量的影响。结果表明,小檗碱的含量与氮素形态有明显关系,在根和茎中都表现为NO3--N比例高更有利于小檗碱的积累。单纯的NO3--N供给最有利于药根碱在黄檗幼苗根中的积累,而处理46d后,NH4 -N/NO3--N为75/25和25/75时黄檗幼苗茎中的药根碱含量最高。黄檗幼苗根和茎中的掌叶防己碱含量对营养液中NH4 -N和NO3--N的比例反应类似,在处理46d后,掌叶防己碱含量由高到低所对应的NH4 -N/NO-3-N为25/75、50/50、75/25、0/100、100/0。处理33d后,黄檗幼苗根中的小檗碱、药根碱、掌叶防己碱含量随处理天数的增加呈下降趋势,而在茎中呈上升趋势。如果同时考虑氮素形态对黄檗幼苗生物量的影响,那么NH4 -N/NO3--N为0/100时其小檗碱产量(含量与生物量乘积)最高,而NH4 -N/NO-3-N为25/75时药根碱和掌叶防已碱的产量最高。     

THE PLANTS OF JOHN BRADBY BLAKE

Analysis of the John Bradby Blake plant illustrations in the library of the Oak Spring Garden Foundation identifies a total of 138 species belonging to over 100 genera and 62 families. Especially well‐represented are useful plants of all kinds, including a high proportion of plants that are used in Chinese traditional medicine.     

The mother – child nexus. Knowledge and valuation of wild food plants in Wayanad, Western Ghats, India

Traditional plant use in Nepal has been documented for millennia. The importance of plants as medicine has not diminished in any way in recent times, and traditional medicines are still the most important health care source for the vast majority of the population. This paper examines the ethnobotany and traditional use of plants extracted from the vulnerable alpine zone in the Dolpa, Humla, Jumla and Mustang districts of Nepal. The results of this ethnobotanical study indicate that a very large number of plant species is used as traditional medicines. There were 107, 59, 44 and 166 species of ethnomedicinal importance in surveyed areas of Dolpa, Humla, Jumla and Mustang district respectively. Of these, 84 common species, used at least in two districts, were selected to enumerate their ethnomedicinal properties. The 84 species belonged to 75 genera and 39 families. The commonest species in this pharmacopoeia were: Allium wallichii, Cordyceps sinensis, Dactylorhiza hatagirea, and Rheum australe. A total of 21 species were most common in three districts and 59 in two districts. The genera Aconitum, Allium, Arisaema, Berberis, Corydalis, Gentiana, Hippophae, Juniperus and Rhododendron each possessed two species with ethnomedicinal use. Labiatae was the most medicinally important family with five species used, followed by Araceae, Compositae, Liliaceae, Polygonaceae, Ranunculaceae, Scrophulariaceae and Umbelliferae, each contributing four species.     

Novel antimalarial drugs from plants?

In all countries where malaria is endemic, plants are used in traditional medicine for treatment of the disease. Examples are numerous - the plant product data base napralert (Box I) lists 152 genera which are allegedly used for the treatment of malaria. But with the urgent need to develop new, safe and effective drugs against malaria, it is vital that such claims be fully investigated. In this article, David Phillipson and Melanie O'Neill discuss the potential of plant products for new antimoloriols, drawing attention particularly to the quassinoids - a diverse group of terpenoids from the family Simoroubaceoe.