共查询到20条相似文献,搜索用时 8 毫秒
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Deng S Zhang BJ Wang CY Tian Y Yao JH An L Huang SS Peng JY Liu KX Ma XC 《Bioorganic & medicinal chemistry letters》2012,22(4):1615-1618
A series of analogues of deoxyandrographolide (1) transformed by Cunninghamella blakesleana AS 3.2004 were isolated and identified by spectral methods including 2D NMR. Among them, 3-oxo-17,19-dihydroxy-7,13-ent-labdadien-15,16-olide (9), 3-oxo-19-hydroxy-1,13-ent-labdadien-15,16-olide (16), 3-oxo-1β-hydroxy-14-deoxy-andrographolide (17) and 3-oxo-2β-hydroxy-14-deoxyandrographolide (18) are new compounds. And their structure-activity relationships (SAR) of inhibitory activity on LPS-induced NO production in RAW 264.7 macrophage cells were also discussed. 相似文献
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《Bioorganic & medicinal chemistry letters》2014,24(12):2717-2719
A new dihydropyranocoumarin, (+)-cis-(3′S,4′S)-diisobutyrylkhellactone (1), together with five known compounds, 3′-senecioyl-4′-acetylkhellactone (2), 3′-isovaleryl-4′-acetylkhellactone (3), 3′,4′-disenecioylkhellactone (4), 3′-isovaleryl-4′-senecioylkhellactone (5), and 3′,4′-diisovalerylkhellactone (6), was isolated from Glehnia littoralis. Their chemical structures were elucidated based on the spectroscopic data interpretation, particularly 1D and 2D NMR data including HMQC and HMBC. All the isolated compounds showed the potential to inhibit LPS-induced nitric oxide production in RAW 264.7 cells with IC50 values ranging from 7.4 to 44.3 μM. 相似文献
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Liqin Ding Feng Zhao Lixia Chen Zhihu Jiang Yue Liu Zhuomin Li Feng Qiu Xinsheng Yao 《Bioorganic & medicinal chemistry letters》2012,22(23):7243-7247
Nine new monoterpene glycosides (1–9), together with 18 known compounds were obtained from the n-butanol soluble fraction of ethanol extract from Paeonia suffruticosa Andrews. Their structures were determined on the basis of chemical methods and spectroscopic data. The inhibitory effects of these compounds (except compound 6) on nitric oxide (NO) production in lipopolysaccharide-activated macrophages were evaluated. Compounds 1, 21, 23, 25, and 27 showed strong inhibitory activity on NO production with IC50 values of 31.25, 36.13, 12.41, 6.87, and 41.94 μM, respectively. 相似文献
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Ji Sang Hwang Seon A Lee Seong Su Hong Xiang Hua Han Chul Lee Shin Jung Kang Dongho Lee Youngsoo Kim Jin Tae Hong Mi Kyeong Lee Bang Yeon Hwang 《Bioorganic & medicinal chemistry letters》2010,20(12):3785-3787
Bioactivity-guided isolation of the methanol extract of the stems of Dendrobium nobile yielded a new phenanthrene together with nine known phenanthrenes and three known bibenzyls. Their structures were elucidated by analysis of the spectroscopic data including 2D-NMR. All of the isolates were evaluated for their potential to inhibit the LPS-induced production of nitric oxide in murine macrophage RAW 264.7 cells. Compounds 1–4, 7–13 inhibited nitric oxide production with the IC50 values ranging from 9.6 μM to 35.7 μM. 相似文献
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Haiyan Che Truong Ngoc Tuyen Hyun Pyo Kim Haeil Park 《Bioorganic & medicinal chemistry letters》2010,20(14):4035-4037
A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells. Most of synthesized 1,5-diarylimidazoles exhibited strong inhibitory activities regardless of the position of the 4-methylsulfonylphenyl group. The 1,5-diarylimidazoles with a halogen atom (3c–3h, 3n–3p) gave mostly excellent inhibitory activities regardless of the position and species of the halogen atom. Whereas the 1,5-diarylimidazoles with two fluorine atoms (3k, 3l, 3r, 3s) showed rather reduced inhibitory activities. 相似文献
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Four new triterpenoid saponins, clematochinenoside H–K (1–4), and five known structures (5–9), were isolated from the roots and rhizomes of Clematis chinensis. Their structures were elucidated on the basis of spectroscopic evidence and hydrolysis products. All isolates were evaluated for inhibitory effects against nitric oxide (NO) production in LPS-induced RAW 246.7 macrophages. Monodesmosidic saponins (1–3, 5, and 6) with a free carboxylic acid function at C-28 exhibited potent inhibitory activities with IC50 values in the range of 12.9–32.3 μM, where as bisdesmosidic saponin (4, and 7–9) showed modest inhibitory effects with the inhibition ratios (%) from 39.9 to 59.0 at 50 μM. In addition, the hydroxyl group at C-21 showed negative effect on the NO production inhibitory activity. 相似文献
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Shin SY Shin MC Shin JS Lee KT Lee YS 《Bioorganic & medicinal chemistry letters》2011,21(15):4520-4523
Sulfuretin is one of major constituents of Rhus verniciflua that exerts anti-inflammatory activities. Some of aurones were synthesized as sulfuretin derivatives and evaluated for their abilities to inhibit NO and PGE2 production in LPS-induced RAW 264.7 cells in order to reveal the relationship. Of the aurones synthesized in the present study, 2h and 2i, which possess C-6 hydroxyl group in A-ring and methoxy substituents in B-ring, more potently inhibited NO and PGE2 production and were less cytotoxic than sulfuretin. 相似文献
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Two new oleanane-type triterpene saponins, identified as 16α-hydroxy-22-O-angeloyl-23-formyl-28,31-dihydroxymethylene-olean-12-ene-3β-O-{β-d-galactopyranosyl-(1 → 2)[β-d-xylopyranosyl-(1 → 2)-α-l-arabinopyranosyl(1 → 3)]-β-d-glucopyranosiduronic acid} (oleiferasaponin B1, 1) and 22-O-hydrocinnamoyl-23-formyl-28-dihydroxymethylene-olean-12-ene-3β-O-{β-d-glucopyranosyl-(1 → 2)[β-d-xylopyranosyl-(1 → 2)-α-l-arabinopyranosyl(1 → 3)]-β-d-glucopyranosiduronic acid} (oleiferasaponin B2, 2), were isolated from the seed cake of Camellia oleifera Abel. Their structures were established by extensive 1D- and 2D-NMR experiments along with TOF-MS analysis and acid hydrolysis. The cytotoxicity of the isolated compounds was evaluated in four human carcinoma cell lines: A 549, SK-OV-3, SK-MEL-2 and HCT15. Both compounds 1 and 2 exhibited significantly cytotoxic activity with IC50 values of 18.5 μM (A549), 11.3 μM (SK-OV-3), 13.9 μM (SK-MEL-2) and 1.6 μM (HCT15) for 1 and IC50 values of 8.4 μM (A549), 6.3 μM (SK-OV-3), 9.2 μM (SK-MEL-2) and 0.8 μM (HCT15) for 2. In addition, compound 2 showed more effective cytotoxic activity than compound 1. 相似文献
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Ping Guo Yushan Li Da-qing Jin Jing Xu Yisha He Lei Zhang Yuanqiang Guo 《Phytochemistry letters》2012,5(3):563-566
Two new neo-clerodane diterpenes, (12S)-6α-acetoxy-4α,18-epoxy-12-hydroxy-19-tigloyloxy-neo-clerod-13-en-15,16-olide (1) and 6α,18-diacetoxy-4α-hydroxy-19-tigloyloxy-neo-clerod-13-en-15,16-olide (2), along with three known analogs (3–5) have been isolated from the whole plants of Ajuga ciliata Bunge. Their structures were elucidated on the basis of spectroscopic data analyses (IR, ESI-MS, HR-ESI-MS, HMQC, HMBC, COSY, and NOESY). The inhibitory activities on LPS-induced NO production of these diterpenes were evaluated and compounds 1 and 5 showed inhibitory effects. 相似文献
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In our survey on the chemical composition of Chinese folk medicines to further elucidate their chemical substances for the treatment of diseases, we investigated the chemical constituents of the plants Eupatorium fortunei. The investigation led to the isolation and identification of two new (1 and 2) and five known (3–7) thymol derivatives. Their structures were elucidated on the basis of extensive 1D and 2D NMR (COSY, HMQC, HMBC, and NOESY) and mass (ESIMS and HR-ESIMS) spectroscopic data analyses. The inhibitory activities on LPS-induced NO production of these compounds were also evaluated. 相似文献
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Chitosan oligosaccharide (COS) inhibits LPS-induced inflammatory effects in RAW 264.7 macrophage cells 总被引:2,自引:0,他引:2
Yoon HJ Moon ME Park HS Im SY Kim YH 《Biochemical and biophysical research communications》2007,358(3):954-959
The focus of this study was to clarify the relation between the nitric oxide (NO) production and cytokine expression including tumor necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6), and also investigated the effect of COS on LPS stimuli from RAW 264.7 cell. The lipopolysaccharide (LPS) of Gram-negative bacteria induces the expression of cytokines and potent inducers of inflammatory cytokines such as TNF-alpha and IL-6. In this experiment, upon stimulation with increasing concentrations of chitosan, the LPS-stimulated TNF-alpha and IL-6 secretion was significantly recovered within the incubation media of RAW 264.7 cells. Consistently, RT-PCR with mRNA and Western blot with anti-cytokine antiserum including TNF-alpha and IL-6 showed that the amount of TNF-alpha and IL-6 secretion in the incubation media recovered with the concentration of chitosan. The LPS-stimulated NO secretion was significantly recovered within the 6h and 12h incubation media of RAW 264.7 cells, too. The recovery effect of chitosan on IL-6 and NO secretion may be induced via the stimulus of TNF-alpha in RAW 264.7 cell. These results once again suggest that chitosan oligosaccharide may have the anti-inflammatory effect via the stimulus of TNF-alpha in the LPS-stimulated inflammation in RAW 264.7 cells. 相似文献
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Xu J Jin DQ Guo Y Xie C Ma Y Yamakuni T Ohizumi Y 《Bioorganic & medicinal chemistry letters》2012,22(11):3612-3618
A phytochemical investigation of the roots of Euphorbia prolifera led to the isolation of ten new myrsinol diterpenes, named euphorbialoids A-J (1-10), and two known analogues (11 and 12). Their structures were elucidated on the basis of extensive 1D and 2D NMR (COSY, HMQC, HMBC and NOESY) spectroscopic data analyzes, and the structures of 1 and 9 were confirmed by X-ray crystallography. The inhibitory activities on LPS-induced NO production of these diterpenes were evaluated and all the compounds showed inhibitory effects. 相似文献
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Zunhua Yang Tuyen N. Truong Tuan-Anh N. Pham Jae-Won Lee Sung-Soo Kim Haeil Park 《Bioorganic & medicinal chemistry》2012,20(21):6256-6259
A number of 1,5-diarylimidazole analogs were synthesized and evaluated their inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin E2 production. Reactions of 1,5-diarylimidazoles with halogenating reagents (NCS, NBS, NIS) afforded halogenated analogs. Among the analogs tested, compounds Ib, IIa, IIb and IIe exhibited significantly improved inhibitory activities against COX-2-mediated PGE2 production from LPS-induced RAW 264.7 cells compared to those of the parent 1,5-diarylimidazoles. Especially, the analogs Ib (IC50 = 0.55 μM) and IIa (IC50 = 0.58 μM) showed best results. Halogenation on the 1,5-diarylimidazole ring enhanced inhibitory activities against COX-2 catalyzed PGE2 production, however, inhibitory activities were significantly varied by position(s) and species of the substituted halogen(s). 相似文献
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Sumioka H Harinantenaina L Matsunami K Otsuka H Kawahata M Yamaguchi K 《Phytochemistry》2011,72(17):2165-2171
From the roots of Lindera strychnifolia, seven sesquiterpenes, named linderolides A-F and linderoline, were isolated together with six known compounds. The structures of linderolides A-F were elucidated to be eudesmane-type sesquiterpenes and linderoline was found to be a derivative of a germacrane-type sesquiterpene. Their structures were elucidated by means of spectroscopic evidence and that of linderolide A was confirmed by X-ray analysis. The inhibitory activity toward NO production was assayed using RAW264.7 cells with evaluating the cell growth by MTT method, linderolides C, D and F being found to be moderately active. 相似文献
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Tae Hoon Kwon Ik Hwan Yoon Ji-Sun Shin Young Hun Lee Bong Jin Kwon Kyung-Tae Lee Yong Sup Lee 《Bioorganic & medicinal chemistry letters》2013,23(9):2571-2574
Arvelexin is one of major constituents of Brassica rapa that exerts anti-inflammatory activities. Several indolyl-3-acetonitrile derivatives were synthesized as arvelexin analogs and evaluated for their abilities to inhibit NO and PGE2 productions in LPS-induced RAW 264.7 cells. Of the indolyl-3-acetonitriles synthesized, compound 2k, which possesses a hydroxyl group at C-7 position of the indole ring and an N-methyl substituent, more potently inhibited NO and PGE2 productions and was less cytotoxic than arvelexin on macrophage cells. 相似文献
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为研究连翘脂素的抗炎效应及其抗炎机制,以地塞米松作为阳性对照,建立脂多糖(LPS)诱导小鼠巨噬细胞RAW264.7炎症模型,检测炎症因子的释放及相关蛋白和mRNA的表达,以期提高对连翘脂素抗炎作用的全面认识并为连翘脂素临床开发提供有力的科学依据。实验采用Griess法检测细胞上清液中NO含量,ELISA法检测TNF-α和IL-6的含量,Westernblot法检测iNOS、COX-2蛋白的表达,RT-qPCR法检测iNOS、COX-2mRNA的表达。与LPS组比较,连翘脂素组和地塞米松组可以明显降低LPS诱导的RAW264.7细胞释放NO、TNF-α和IL-6的量,并呈现浓度依赖关系。Westrenblot和RT-qPCR结果显示连翘脂素能抑制LPS诱导的iNOS、COX-2的蛋白表达以及mRNA的表达,并呈浓度依赖关系。实验研究表明连翘脂素能够明显抑制LPS诱导的RAW264.7细胞炎症因子的释放,iNOS、COX-2蛋白及mRNA的表达从而抑制炎症反应。 相似文献
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Thamizhiniyan Venkatesan Young-Woong Choi Jennifer Lee Young-Kyoon Kim 《Molecular and cellular biochemistry》2018,442(1-2):169-175
The purpose of the study was to investigate the mechanism of total flavone of Desmodium styracifolium (TFDS) in regulating the formation of urinary calculi. Protein levels of KIM-1, LC3-II, p-p38 were measured by Western blot. The effect of different COM concentrations, different TFDS concentrations, SB203580 (specific inhibitor of p38/MAPK), and overexpression of KIM-1 on cell viability were detected by WST-1 assay. The apoptotic cells and FITC positive cells were detected by flow cytometry. HK-2 cell viability decreased with the increase of COM concentration, and the protein levels of KIM-1, LC3-II, and p-p38 increased with the time. Blocking the p38/MAPK pathway or co-cultured with TFDS inhibited the effects of COM on apoptosis and autophagy of HK-2 cells. In addition, blocking the p38/MAPK pathway inhibited the expression of KIM-1. In COM-induced cells, after treated with SB203580, overexpression of KIM-1 could reverse the protection effect of SB203580 on COM-induced cell damage and the inhibition of SB203580 on COM-induced excessive autophagy, suggesting p38/MAPK regulated KIM-1 to regulate COM-induced cell apoptosis and autophagy. Finally, we proved that TFDS inhibited p38/MAPK pathway. And the protection effect of COM-induced cell injury increased with the increase of TFDS concentration, and the adhesion between COM and cells decreased with the increase of TFDS concentration. With the increase of the concentration of TFDS, p38/MAPK pathway was gradually inhibited, and KIM-1 and autophagy related proteins were decreased. TFDS inhibited HK-2 cell apoptosis and autophagy by regulating KIM-1 via p38/MAPK pathway. 相似文献