共查询到20条相似文献,搜索用时 15 毫秒
1.
Recent investigations have shown that certain flavonoids, especially flavone derivatives, inhibit nitric oxide (NO) production by inducible NO synthase (iNOS) in macrophages, which contribute their anti-inflammatory action. For the purpose of finding the optimized chemical structures of flavonoids that inhibit NO production, various A- and B-ring substituted flavones were synthesized and evaluated for their inhibitory activity using lipopolysaccharide-treated RAW 264.7 cells. It was found that the optimal chemical structures were A-ring 5,7-dihydroxyflavones having the B-ring 2',3'-dihydroxy or 3',4'-dihydroxy or 3',4'-hydroxy/methoxy (methoxy/hydroxy) groups. These structurally optimized compounds were revealed to be down-regulators of iNOS induction, but not direct iNOS inhibitors. Of these derivatives that were evaluated, 2',3',5,7-tetrahydroxyflavone and 3',4',5,7-tetrahydroxyflavone (luteolin) showed the strongest inhibition. The IC50 values for these compounds were 19.7 and 17.1 microM, respectively. Therefore, these compounds may have a potential as new anti-inflammatory agents. 相似文献
2.
Abdel latif Shaker Seddek Motamed Elsayed Mahmoud Takahiko Shiina Haruko Hirayama Momoe Iwami Seiji Miyazawa Hideki Nikami Tadashi Takewaki Yasutake Shimizu 《Journal of natural medicines》2009,63(3):297-303
Calotropis procera latex has long been used in traditional medicines. Extracts from C. procera latex have been reported to have various pharmacological actions, including protection from myocardial infarction, hepatoprotective
action, antitumor activity, antinociceptive, and pro- and anti-inflammatory actions. To evaluate the immunomodulatory functions
of the water-soluble C. procera extract (CPE), we investigated its ability to activate macrophages—effector cells in inflammatory and immune responses. Intraperitoneal
injection of CPE in mice (2 mg/mouse) induced migration of macrophages to the intraperitoneal cavity, confirming the proinflammatory
effects of water-soluble CPE. The direct effects of CPE on macrophages were then assessed by measuring the production of nitric
oxide (NO) as an indicator for macrophage activation. Addition of CPE (1–10 μg/ml) to the culture medium of the murine monocyte/macrophage
cell line RAW264.7 caused an increase in NO production in a time- and dose-dependent manner. CPE-elicited NO production was
blocked by application of an inhibitor of inducible nitric oxide synthase (iNOS). Expression of iNOS mRNA was induced by treatment
of cultured macrophages with CPE. Injection of CPE in mice also resulted in an increase in plasma NO level. The results suggest
that CPE activates macrophages and facilitates NO production via up-regulation of iNOS gene expression.
A. l. S. Seddek and M. Elsayed Mahmoud contributed equally to this work. 相似文献
3.
Kim MJ Han JM Jin YY Baek NI Bang MH Chung HG Choi MS Lee KT Sok DE Jeong TS 《Archives of pharmacal research》2008,31(4):429-437
Oxidized low-density lipoprotein (oxLDL) plays a key role in the inflammatory processes of atherosclerosis. Jaceosidin isolated
from the methanolic extracts of the aerial parts of Artemisia princeps Pampanini cv. Sajabal was tested for antioxidant and anti-inflammatory activities. Jaceosidin inhibited the Cu2+-mediated LDL oxidation with IC50 values of 10.2 μM in the thiobarbituric acid-reactive substances (TBARS) assay as well as the macrophage-mediated LDL oxidation.
The antioxidant activities of jaceosidin were exhibited in the conjugated diene production, relative electrophoretic mobility,
and apoB-100 fragmentation on copper-mediated LDL oxidation. Jaceosidin also inhibited the generation of reactive oxygen species
(ROS) concerning in regulation of NF-κB signaling. And jaceosidin inhibited nuclear factor-kappa B (NF-κB) activity, nitric
oxide (NO) production, and suppressed expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-induced
RAW264.7 macrophages. 相似文献
4.
A sesquiterpene lactone, 1-O-acetyl-4R,6S-britannilactone (1) isolated from the flowers of Inula britannica L. var. chinensis (Rupr.) Reg. (Compositae), was found as an iNOS inhibitory constituent for the first time with an IC50 value of 22.1 microM which is more potent than the positive control, L-N6-(1-iminoethyl)lysine (IC50 = 33.7 microM). Structure of compound 1 was identified by 1D and 2D NMR experiments and by comparison with the reference standard. 相似文献
5.
Nitric oxide (NO) is an important bioactive agent that mediates a wide variety of physiological and pathophysiological events. NO overproduction by inducible nitric oxide synthase (iNOS) results in severe hypotension and inflammation. This investigation is part of a study to discover new iNOS inhibitors from medicinal plants using a macrophage cell culture system. Two sesquiterpenes (1 and 2) were isolated from Artemisia iwayomogi (Compositae) and were found to inhibit NO synthesis (IC50 3.64 microg/mL and 2.81 microg/mL, respectively) in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Their structures were identified as 3-O-methyl-isosecotanapartholide (1) and iso-secotanapartholide (2). Compounds 1 and 2 inhibited the LPS-induced expression of the iNOS enzyme in the RAW 264.7 cells. The inhibition of NO production via the down regulation of iNOS expression may substantially modulate the inflammatory responses. 相似文献
6.
8,14-labdadien-13-ol (1) and dehydroabietic acid (2) were isolated from the fruit body of Phellinus pini. Elucidation of their structures was based on spectroscopic methods including IR, MS, and NMR (1D and 2D). Two compounds
were screened for their ability to inhibit NO production in LPS-activated RAW 264.7 cells. Compounds 1 and 2 at 30 μM and 50 μM, respectively, inhibited NO production in activated macrophages. 相似文献
7.
Tanaka H Hattori H Tanaka T Sakai E Tanaka N Kulkarni A Etoh H 《Journal of natural medicines》2008,62(2):228-231
A new Erythrina alkaloid, 10-hydroxy-11-oxoerysotrine (1), has been isolated from the flowers of Erythrina herbacea together with five known compounds: erytharbine (2), 10,11-dioxoerysotrine (3), erythrartine (4), erysotramidine (5) and erysotrine-N-oxide (6). The structure of the new compound was elucidated on the basis of its spectral data, including 2-D NMR and mass (MS) spectra.
The new compound is a rare C-10 oxygenated Erythrina alkaloid. The antioxidant activities of the isolated compounds 1–6 were evaluated by scavenging with peroxynitrite. 相似文献
8.
Angelica decursiva has long been used in Korean traditional medicine as an antitussive, analgesic, antipyretic, and cough remedy. In this study, the anti-inflammatory activity of 9 coumarin derivatives isolated from a 90 % methanol fraction was evaluated via inhibition of production of nitric oxide (NO) and tumor necrosis factor-α (TNF-α), as well as the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Among the tested compounds, edulisin II (1) exhibited the most potent NO production inhibitory activity, followed by decursidin (2), Pd–C-III (3), 4-hydroxy Pd–C-III (4), Pd–C-I (5), and Pd–C-II (6). In contrast, (+)-trans-decursidinol (7) did not exhibit NO suppressive effects on LPS-stimulated RAW 264.7 cells. Structure-activity relationships revealed that esterification of the hydroxyl at C-3′ or C-4′ of 7 with an angeloyl/senecioyl/acetyl group is essential for its inhibitory activity against NO production, while the number of angeloyl or senecioyl groups, and their positions greatly affect the potency of these coumarins. Coumarins 1-6 also inhibited TNF-α production and iNOS protein expression, while compounds 1-4 inhibited COX-2 protein expression in LPS-stimulated RAW 264.7 cells. These results suggest that coumarins isolated from A. decursiva might be used as potential leads for the development of therapeutic agents for inflammation-associated disorders. 相似文献
9.
Hari?Jang Jin?Woo?Lee Chul?Lee Qinghao?Jin Jeong?Yeon?Choi Dongho?Lee Sang?Bae?Han Youngsoo?Kim Jin?Tae?Hong Mi?Kyeong?Lee Bang?Yeon?Hwang
A new oplopane-type sesquiterpenoid tussilagofarin (1) and a new chromone tussilagofarol (2), along with 18 known compounds 3–20, were isolated from the flower buds of Tussilago farfara. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR and HRESIMS data. Of the isolated compounds, oplopane- and bisabolane-type sesquterpenoids 1, 8–12, 15, and 16 were found to inhibit nitric oxide production in LPS-induced RAW 264.7 cells with IC50 values of 3.5–28.5 μM. 相似文献
10.
Five new coumarins, (+)-peujaponisin (1) and multivittans A–D (2–5), were isolated from the roots of Ligusticum multivittatum Franch., and their structures were established by spectral means. 相似文献
11.
Tan MA Takayama H Aimi N Kitajima M Franzblau SG Nonato MG 《Journal of natural medicines》2008,62(2):232-235
Bioassay-guided chromatographic purification of the antitubercular chloroform extract of Pandanus tectorius Soland. var. laevis leaves afforded a new tirucallane-type triterpene, 24,24-dimethyl-5β-tirucall-9(11),25-dien-3-one (1), squalene and a mixture of the phytosterols stigmasterol and β-sitosterol. Microplate Alamar Blue Assay (MABA) showed that
1 inhibited the growth of Mycobacterium tuberculosis H37Rv with a MIC of 64 μg/mL, while squalene and the sterol mixture have MICs of 100 and 128 μg/mL, respectively. 相似文献
12.
Twenty-eight samples of mericarps of Perilla frutescens var. frutescens were collected through fieldwork performed in Phongsali and Xieng Khouang provinces in northern Laos. No perilla samples
were collected from Savannakhet province in the south although more than 20 sites were investigated. Perilla plants are mostly
grown mixed with dry-paddy rice by slash-and-burn cultivation in Laos. The most popular local name for perilla mericarps in
the area was “Ma Nga Chan”. Weight of 1,000 grains and hardness of the mericarps were measured, and all mericarps were found
to be large (weight of 1,000 grains around 2 g) and soft (limit load weight under 300 g), which were preferred for culinary
use in Laos. The composition of the essential oils obtained from the herbaceous plants raised from the mericarps was divided
into five types, perillaketone, elemicine plus myristicine, shisofuran, piperitenon, and myristicine, and GC–MS analysis of
these Laotian perilla samples showed that they were similar to those of corresponding types of known Japanese perilla strains.
One of the shisofuran-type perilla contained large amounts of putative α-naginatene, which is likely to be an intermediate
of the biosynthesis of naginataketone. The farmers' indifference to the oil type of the leaf seems to leave Laotian perilla
as a good genetic resource for studies of the biosynthesis of oil compounds. 相似文献
13.
14.
Bioassay-guided fractionation of the MeOH extract of Suaeda glauca yielded four phenolic compounds, methyl 3,5-di-O-caffeoyl quinate (1) and 3,5-di-O-caffeoyl quinic acid (2), isorhamnetin 3-O-beta-D-galactoside (3), and quercetin 3-O-beta-D-galactoside (4). Compounds 1 and 2 were hepatoprotective against tacrine-induced cytotoxicity in human liver-derived Hep G2 cells with the EC(50) values of 72.7+/-6.2 and 117.2+/-10.5 microM, respectively. Silybin as a positive control showed an EC(50) value of 82.4+/-4.1 microM. 相似文献
15.
The dichloromethane extract of the air-dried leaves of Artemisia vulgaris afforded a new sesquiterpene 1, caryophyllene oxide, phytyl fatty acid esters, squalene, stigmasterol and sitosterol. The structure of 1 was elucidated by extensive one- and two-dimensional nuclear magnetic resonance spectroscopy. 相似文献
16.
Pérez Gutiérrez RM Martínez Flores A Vargas Solís R Carmona Jimenez J 《Journal of natural medicines》2008,62(3):328-331
Two abietane diterpenes were isolated from cyanobacteria Microcoleous lacustris, 20-nor-3α-acetoxyabieta-5,7,9,11,13-pentaene and 20-nor-3α-acetoxy-12-hydroxy-abieta-5,7,9,11,13-pentaene. These compounds were assayed against Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhi, Vibrio cholerae, Bacillus subtilis, Bacillus cereus, Escherichia coli, and Klebsiella pneumoniae. Both compounds showed activity against S. aureus, S. epidermidis, S. typhi, and V. cholerae, but not against the other bacteria. 相似文献
17.
Jang SI Kim BH Lee WY An SJ Choi HG Jeon BH Chung HT Rho JR Kim YJ Chai KY 《Archives of pharmacal research》2004,27(9):923-929
Stylopine is a major component of the leaf of Chelidonium majus L. (Papaveraceae), which has been used for the removal of warts, papillomas and condylomas, as well as the treatment of liver disease, in oriental countries. Stylopine per se had no cytotoxic effect in unstimulated RAW 264.7 cells, but concentration-dependently reduced nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. The levels of inducible nitric oxide synthase (iNOS) and COX-2 protein expressions were markedly suppressed by stylopine in a concentration dependent manner. These results suggest that stylopine suppress the NO and PGE2 production in macrophages by inhibiting the iNOS and COX-2 expressions. These biological activities of stylopine may contribute to the anti-inflammatory activity of Chelidonium majus. 相似文献
18.
Qu Y Xu F Nakamura S Matsuda H Pongpiriyadacha Y Wu L Yoshikawa M 《Journal of natural medicines》2009,63(1):102-104
From the dried rhizomes of Curcuma
comosa cultivating in Thailand, 26 known sesquiterpenes were isolated: zederone, zederone epoxide, furanodienone, isofuranodienone,
1(10)Z,4Z-furanodiene-6-one, glechomanolide, dehydrocurdione, neocurdione, curdione, 7α-hydroxyneocurdione, 7β-hydroxycurdione, germacrone-1(10),4-diepoxide, germacrone, 13-hydroxygermacrone, curzerenone, curcolonol, alismol, alismoxide,
zedoarondiol, isozedoarondiol, procurcumenol, isoprocurcumenol, aerugidiol, zedoalactone B, curcumenone, and curcumadione.
Their structures were elucidated on the basis of physicochemical evidence. Among them, glechomanolide, curzerenone, curcolonol,
alismol, alismoxide, and zedoarondiol showed no significant optical activities, so they may be artifact products during the
isolation or drying process. 相似文献
19.
Frequencies of spontaneous mutation from inducible resistance to constitutive resistance were determined for the four clinical
isolates of erythromycin-resistant enterococci, including one isolate with ermB gene and three clinical isolates with ermA gene. The rate of ermB mutation was higher than that of ermA mutation by more than 10 fold. Sequence analysis of the regulatory regions of erm genes revealed that mutation type of ermB was just point mutation, by contraries the mutation type of ermA was either deletion or tandem duplication. These results showed distinct characteristics in mutation patterns of ermB and ermA. 相似文献
20.
Hyung Sik Kim Jin Woo Lee Hari Jang Thi Phuong Linh Le Jun Gu Kim Moon Soon Lee Jin Tae Hong Mi Kyeong Lee Bang Yeon Hwang 《Archives of pharmacal research》2018,41(2):192-195
A new phenolic amide, named cis-terrestriamide (7), together with ten known compounds (1–6, 8–11), were isolated from the methanolic extract of the fruits of Tribulus terrestris. The structure of 7 was elucidated on the basis of extensive analyses of 1D and 2D nuclear magnetic resonance spectroscopic and high resolution mass spectrometry data. Compounds 1, 2, 5, 6, 8, 9, and 11 exhibited inhibitory effects on the lipopolysaccharide-stimulated nitric oxide production in RAW 264.7 cells, with IC50 values of 18.7–49.4 μM. 相似文献