NO production inhibition

NO 产生抑制
  • 文章类型: Journal Article
    Paeoniaostii,又称“风丹”,在民间医学治疗腰肌劳损有至关重要的作用,膝骨关节炎和颈椎病。在这项研究中,四种新的酚类化合物,特别是PaeoniaostiphA-E(1-4)酚类化合物通过光谱技术进行表征,包括1D和2DNMR,HRESIMS,UV,IR,和电子圆二色性计算来探索它们的结构。还研究了新酚类化合物的细胞毒性和NO产生抑制。细胞毒性实验的结果表明,化合物1对两种人癌细胞系具有细胞毒性,IC50值为13.3至13.5μM。化合物1和2对NO产生显示出一定的抑制活性。这是关于从天然来源中分离成分的第一份报告。
    The Paeonia ostii, also known as \"Feng Dan\" have a crucial role in folk medicine to treat lumbar muscles strain, knee osteoarthritis and cervical spondylosis. In this study, four new phenolic compounds, specifically Paeoniaostiph A-E (1-4) phenolic compounds were characterised through spectroscopic techniques, including 1D and 2D NMR, HRESIMS, UV, IR, and electronic circular dichroism computations to explore their structures. Cytotoxicity and NO production inhibition of the new phenolic compounds were also studied. The results of the cytotoxicity experiment showed that compound 1 is cytotoxic to two human cancer cell lines with IC50 values ranging from 13.3 to 13.5 μM. Compounds 1 and 2 showed certain inhibitory activity on NO production. This is the first report on isolating the components from natural sources.
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  • 文章类型: Journal Article
    十种未描述的二萜化合物(1-10)和三种未描述的菲衍生物(11-13),连同七种已知的化合物,是从茄子的根中分离出来的。它们的结构是通过光谱数据分析的组合确定的,电子圆二色性计算和单晶X射线衍射研究。化合物1-7(类黄精A-G)代表在自然界中首次发现的20-non-podocarpane类的实例。特别是,化合物7具有独特的2,3-seco环系统,其中包含γ-丁醇酰胺部分。评估了所有分离株对HT-29,HCT-116,HCT-15,MCF-7和A549细胞系的细胞毒性活性,以及它们对RAW264.7细胞中脂多糖诱导的NO产生的抑制作用。化合物1,一种具有Δ1,2双键的20-non-ent-po-arcane型二萜,不仅对五种人类癌细胞系表现出相当大的增殖抑制作用,IC50值范围为4.13至23.45μM,但也显示出对NO产生的最有效抑制活性,IC50值在纳摩尔水平(0.63±0.21μM)。
    Ten undescribed diterpenoids (1-10) and three undescribed phenanthrene derivatives (11-13), together with seven known compounds, were isolated from the roots of Baliospermum solanifolium. Their structures were determined by a combination of spectroscopic data analysis, electronic circular dichroism calculations and single-crystal X-ray diffraction studies. Compounds 1-7 (baliosperoids A-G) represent the examples of 20-nor-ent-podocarpane class first discovered in nature. In particular, compound 7 possesses a unique 2,3-seco ring system incorporating γ-butanolide moiety. All isolates were assessed for their cytotoxic activities against HT-29, HCT-116, HCT-15, MCF-7, and A549 cell lines as well as their inhibitory effects on lipopolysaccharide-induced NO production in RAW264.7 cells. Compound 1, a 20-nor-ent-podocarpane-type diterpenoid possessing a Δ1,2 double bond, not only exhibited considerable proliferation inhibition against five human cancer cell lines, with IC50 values ranging from 4.13 to 23.45 μM, but also displayed the most potent inhibitory activity on NO production with IC50 value at the nanomolar level (0.63 ± 0.21 μM).
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  • 文章类型: Journal Article
    三种新的麦角甾醇具有高度共轭的环系统,银杏叶甾醇C-E(1-3),已从真菌Psathyrellarogueiana中分离出来。通过光谱法和单晶X射线衍射阐明了具有绝对构型的结构。化合物1-3表现出对NO产生的抑制活性,IC50值为8.4-21.8μM。化合物1抑制LPS诱导的B淋巴细胞增殖,IC50值为12.3μM。
    Three new ergosterols featuring with a highly conjugated ring system, psathrosterols C-E (1-3), have been isolated from the fungus Psathyrella rogueiana. The structures with the absolute configurations were elucidated by means of spectroscopic methods and single crystal X-ray diffraction. Compounds 1-3 exhibit inhibitory activity against NO production with IC50 values ranging from 8.4 to 21.8 μM. Compound 1 inhibits the LPS-induced proliferation of B lymphocyte cells with an IC50 value of 12.3 μM.
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  • 文章类型: Journal Article
    两个异二聚体,包括clovane-苯基丙烷杂种(1)和clovane-menthane杂种(2),包含四氢呋喃环的五种线性倍半萜化合物(3-6和8),和四个类固醇(7和9-11),从著名的芳香和药用植物Eupatories的乙醇提取物中分离出来。通过对光谱数据的详细分析以及与已知类似物的比较来表征它们的结构。其中七(1-7)是第一次描述。杂种1和2代表与其他类型的天然产物杂化的clovane型倍半萜的第一个例子,化合物3-6和8是标题物种报道的第一个线性倍半萜基成分。评价所有分离物对LPS诱导小鼠RAW264.7巨噬细胞产生NO的抑制作用。和1、7、10和11表现出中等活性,IC50值在24.4-43.5µM范围内。
    Two heterodimers including a clovane-phenylpropanoid hybrid (1) and a clovane-menthane hybrid (2), five linear sesquiterpenoids incorporating a tetrahydrofuran ring (3-6 & 8), and four steroids (7 & 9-11), were separated from the ethanolic extract of a well-known aromatic and medicinal herb Eupatorium fortunei. Their structures were characterised by detailed analyses of spectroscopic data and comparison with known analogues, with seven (1-7) of them being described for the first time. The hybrids 1 and 2 represent the first examples of clovane type sesquiterpenoids hybridising with other class of natural products, and compounds 3-6 and 8 are first linear sesquiterpenyl constituents reported from the title species. All the isolates were evaluated for their inhibitory effect on the NO production induced by LPS in murine RAW264.7 macrophage cells, and 1, 7, 10 and 11 exhibited moderate activity with IC50 values in the range of 24.4-43.5 µM.
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  • 文章类型: Journal Article
    对Gnetumlatifolium树干的植物化学研究导致了一种新型的酚类葡萄糖苷的分离,2E-2,4-二-(3,4-二羟基苯基)丁-2-烯-1-基-O-β-D-吡喃葡萄糖苷(1),以及五种已知的二苯乙烯衍生物(2-6)。它们的结构主要使用高分辨率电喷雾电离质谱和核磁共振光谱分析来确定,然后将观察到的光谱数据与报告值进行比较。发现G.latifolium中的新型化合物1可用作化学分类学标记。生物学评价显示化合物6对一氧化氮的产生有显著的抑制作用,半最大抑制浓度(IC50)值为4.85±0.20µM,远高于阳性对照地塞米松(IC50=14.20±0.54µM)。
    Phytochemical investigation of the trunks from Gnetum latifolium led to the isolation of a novel phenolic glucoside, 2E-2,4-di-(3,4-dihydroxyphenyl)but-2-en-1-yl-O-β-D-glucopyranoside (1), along with five known stilbene derivatives (2-6). Their structures were determined mainly using high-resolution electrospray ionisation mass spectrometry and nuclear magnetic resonance spectroscopic analyses, followed by comparisons of observed spectral data with reported values. The novel compound 1 in G. latifolium was found to be useful as a chemotaxonomic marker. Biological evaluation revealed that compound 6 had remarkable inhibitory effects on nitric oxide production, with a half-maximal inhibitory concentration (IC50) value of 4.85 ± 0.20 µM, which was much higher than that of the positive control dexamethasone (IC50 = 14.20 ± 0.54 µM).
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  • 文章类型: Journal Article
    八种含氮化合物,包括五种未描述的,aeswilnitorusolA(1),aeswilnitrousosidesBD(2-4),和6-(2-羟基-3-甲基丁基氨基)-8-氧代腺嘌呤(5)从七叶树的种子中分离。它们的结构和绝对构型是根据光谱测定建立的,计算电子圆二色性(ECD)分析,以及化学反应方法。在已知的三种化合物中,7和8是首次从七叶树属中获得的,最初从该工厂获得6。首次报道了7和8的13CNMR数据。此外,评估了所有分离株对LPS诱导的RAW264.7巨噬细胞产生一氧化氮的抑制作用.因此,化合物2和8在10、25和50μM下以浓度依赖性方式表现出抗炎活性。
    Eight nitrogenous compounds including five undescribed ones, aeswilnitrousol A (1), aeswilnitrousosides BD (2-4), and 6-(2-hydroxy-3-methylbutylamino)-8-oxoadenine (5) were isolated from the seeds of Aesculus wilsonii. Their structures and absolute configurations were established based on spectroscopic determination, calculated electronic circular dichroism (ECD) analysis, as well as chemical reaction methods. Among the three known compounds, 7 and 8 were obtained from the Aesculus genus for the first time, and 6 was gained from this plant initially. The 13C NMR data of 7 and 8 were reported for the first time. Moreover, the inhibitory effect of all the isolates against LPS-induced nitric oxide production in RAW264.7 macrophages was evaluated. As a result, compounds 2 and 8 exhibited anti-inflammatory activity in a concentration-dependent manner at 10, 25, and 50 μM.
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  • 文章类型: Journal Article
    两个先前未描述的麦角甾醇含有高度共轭的环系统,银杏叶甾醇A和B(1和2),已从真菌Psathyrellarogueiana中分离出来。它们具有绝对构型的结构是通过广泛的光谱方法建立的,以及单晶X射线衍射。化合物1和2显示出对NO产生的抑制活性,IC50值为22.3和16.4μM,分别。
    Two previously undescribed ergosterols containing a highly conjugated ring system, psathrosterols A and B (1 and 2), have been isolated from the fungus Psathyrella rogueiana. Their structures with absolute configurations were established by extensive spectroscopic methods, as well as single crystal X-ray diffraction. Compounds 1 and 2 showed inhibitory activity against NO production with IC50 values of 22.3 and 16.4 μM, respectively.
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  • 文章类型: Journal Article
    24种芳香族化合物,包括5种新型化合物,多利abphenosidesA(1),B1(2)、B2(3)、C1(4),和C2(5)是从DolichoslablabL的种子中获得的。它们的结构是基于光谱分析和化学反应建立的。在已知的化合物中,第一次从豆科获得了9、10、14、17、19和22-24,和6、8、11-13、15、16、18、20以及21个首先从Dolichos属中鉴定。此外,在RAW264.7巨噬细胞中,所有分离物对LPS诱导的一氧化氮(NO)产生的抑制作用评估表明,化合物1-3、6、7、11-15、17、20、21、23、24以浓度依赖性方式表现出抗炎活性。此外,新的化合物,多利abphenosidesA(1),B1(2)、发现B2(3)抑制炎性细胞因子IL-1β的分泌。
    Twenty-four aromatic compounds including five novel ones, dolilabphenosides A (1), B1 (2), B2 (3), C1 (4), and C2 (5) were obtained from the seeds of Dolichos lablab L. Their structures were established based on spectroscopic analyses and chemical reactions. Among the known compounds, 9, 10, 14, 17, 19, and 22-24 were gained from the family Leguminosae for the first time, and 6, 8, 11-13, 15, 16, 18, 20, as well as 21 were firstly identified from Dolichos genus. Moreover, the inhibitory effect evaluation of all the isolates against LPS-induced nitric oxide (NO) production in RAW264.7 macrophages suggested that compounds 1-3, 6, 7, 11-15, 17, 20, 21, 23, 24 exhibited anti-inflammatory activity in a concentration-dependent manner. Moreover, the novel compounds, dolilabphenosides A (1), B1 (2), B2 (3) were found to inhibit the secretion of inflammatory cytokine IL-1β.
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  • 文章类型: Journal Article
    七个以前没有描述过的细胞松弛症,即,波松弛素A-G,和一个类似物一起,从真菌Boeremiaexigua的固体培养物中表征。在广泛的光谱分析以及电子圆二色性计算的基础上,阐明了它们的结构和绝对构型。值得注意的是,boerechalasinF具有一个不寻常的亚砜部分,可能来自甲硫氨酸,而boerechalasinG在N-2位有一个不寻常的5-甲基环己烷-1,2,3-三醇取代基。BoerechalasinsA和E对LPS诱导的RAW264.7巨噬细胞中一氧化氮的产生表现出抑制活性,IC50值为21.9和5.7μM,分别。BoerechlasinF对人MCF-7细胞具有细胞毒性,IC50值为22.8μM。
    Seven previously undescribed cytochalasans, namely, boerechalasins A-G, together with one analogue, were characterized from the solid culture of the fungus Boeremia exigua. Their structures and absolute configurations were elucidated on the basis of extensive spectroscopic analysis as well as electronic circular dichroism calculations. Remarkably, boerechalasin F possessed an unusual sulfoxide moiety that might be derived from methionine, while boerechalasin G had an unusual 5-methylcyclohexane-1,2,3-triol substituent at N-2 position. Boerechalasins A and E exhibited inhibitory activities against nitric oxide production in LPS-induced RAW264.7 macrophages with IC50 values of 21.9 and 5.7 μM, respectively. Boerechalasin F displayed cytotoxicity against human MCF‒7 cells with an IC50 value of 22.8 μM.
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  • 文章类型: Journal Article
    Paeoniasuffruticosa,被称为“冯丹”,在传统中药中已经使用了数千年。在我们对植物根皮的化学研究中,五种新的酚类二聚体,即,苯并呋喃酮A-E(1-5),被表征。它们的结构是使用光谱分析确定的,包括1D和2DNMR,HRESIMS,UV,IR,以及ECD计算。化合物2、4和5显示对三种人类癌细胞系的细胞毒性,IC50值范围为6.7至25.1μM。化合物1和2对NO产生显示出一定的抑制活性。据我们所知,本文首次报道了苯并呋喃酮二聚体及其对苦参的细胞毒性。
    The Paeonia suffruticosa, known as \'Feng Dan\', has been used for thousands of years in traditional Chinese medicine. In our chemical investigation on the root bark of the plant, five new phenolic dimers, namely, paeobenzofuranones A-E (1-5), were characterized. Their structures were determined using spectroscopic analysis including 1D and 2D NMR, HRESIMS, UV, and IR, as well as ECD calculations. Compounds 2, 4, and 5 showed cytotoxicity against three human cancer cell lines, with IC50 values ranging from 6.7 to 25.1 μM. Compounds 1 and 2 showed certain inhibitory activity on NO production. To the best of our knowledge, the benzofuranone dimers and their cytotoxicity of P. suffruticosa are reported for the first time in this paper.
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