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Timofey V. Malyarenko Alla A. Kicha Natalia V. Ivanchina Anatoly I. Kalinovsky Pavel S. Dmitrenok Svetlana P. Ermakova Valentin A. Stonik 《Steroids》2011,76(12):1280-1287
Six new steroidal biglycosides, cariniferosides A–F (1–6), were isolated along with six previously known glycosides, 7–12, from the alcoholic extract of the starfish Asteropsis carinifera. The structures of 1–6 were determined by extensive NMR and ESIMS techniques. The isolated compounds did not show any apparent cytotoxicity in cancer cell lines HCT-116, RPMI-7951, and T-47D, but sulfated compounds 6, 11, and 12 demonstrated a significant inhibition of RPMI-7951 and T-47D cell colony formation in a soft agar clonogenic assay. 相似文献
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Mayence A Vanden Eynde JJ Kaiser M Brun R Yarlett N Huang TL 《Bioorganic & medicinal chemistry》2011,19(24):7493-7500
A small library of 26 2,2′-[alkane-α,ω-diylbis(oxyphenylene)]bis-1H-benzimidazoles has been prepared and evaluated against Giardia intestinalis, Entamoeba histolytica, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum. Among the tested compounds, eight derivatives (17, 19, 20, 24, 27, 30, 32 and 35) exhibited an anti-Plasmodium falciparum activity characterized by IC50 values in the range of 180–410 nM (0.11–0.21 μg/mL) and selectivity indexes (IC50 rat skeletal myoblasts L6 cells vs IC50P. falciparum K1 strain) varying between 92 and more than 450. Two of the eight novel drug leads, namely compounds 19 and 32, were also active against G. intestinalis and L. donovani with selectivity indexes of 122 and >164 respectively. 相似文献
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Cheng YX Zhou LL Yan YM Chen KX Hou FF 《Bioorganic & medicinal chemistry letters》2011,21(24):7434-7439
Three new cyclic peptides, namely duanbanhuains A–C (1–3), were isolated from the roots of Brachystemma calycinum which is a traditional medicine used to treat rheumatic diseases. Their structures were identified by means of a suite of MS and NMR experiments. These compounds were purposely evaluated for their inhibitory effects on the release of MCP-1, IL-6, collagen IV and reactive oxygen species (ROS) against high-glucose-stimulated mesangial cells. The results showed that compounds 1 and 2 exhibited potent inhibition on the production of IL-6, collagen IV and ROS at the concentration of 10 μM. 相似文献
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Nitirat Chimnoi Chonticha Sarasuk Nisachon Khunnawutmanotham Pakamart Intachote Suchada Seangsai Busakorn Saimanee Somchai Pisutjaroenpong Chulabhorn Mahidol Supanna Techasakul 《Phytochemistry letters》2009,2(4):184-187
A comprehensive reinvestigation of chemical constituents from the rhizomes of Hedychium coronarium resulted in the isolation of one new labdane-type diterpene, together with eight known compounds. Their structures were established by spectroscopic methods. Some of the isolated compounds showed significant cytotoxicity with IC50 values lower than 4 μg ml?1. 相似文献
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Seven triterpenoid saponins, including four new compounds, catunarosides A–D (1–4), and three known compounds, swartziatrioside (5), aralia-saponin V (6), araliasaponin IV (7) were isolated from the stem bark of Catunaregam spinosa, a Chinese mangrove associate. Their structures were elucidated on the basis of their spectral data and hydrolysis experiments. The antifeedant activities of compounds 1–7 against Plutella xylostella were also evaluated. 相似文献
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Jun He Yi Shen Jian-Shuang Jiang Ya-Nan Yang Zi-Ming Feng Pei-Cheng Zhang Shao-Peng Yuan Qi Hou 《Carbohydrate research》2011,(13):1903
Eight new linear polyacetylene glucosides (1–8), containing two C10-, one C13- and five C14-acetylenes, together with three known polyacetylenes (9–11) were isolated from the florets of Carthamus tinctorius L. Their structures were elucidated by means of spectroscopic methods and chemical evidence. The absolute configurations of compounds 3–9 were confirmed by Snatzke and Gerards’s method, observing the induced circular dichroism after addition of dirhodium tetrakis (trifluoroacetate) [Rh2(OCOCF3)4] in CHCl3. All the isolated compounds (1–11) were also tested for inhibitory activities against LPS-induced NO production in murine macrophages and just showed weak activities at concentrations of 1 × 10−5 M. 相似文献
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Xiao Liang Zhao Wen Guang Jing Shu Ying Han Guang Li Sun Yu Mei Liu Qi Wei Zhang Xiao Jun Ma Zhi Min Wang An Liu 《Phytochemistry letters》2011,4(3):267-270
Two new furostanol saponins, 3-O-[α-l-rhamnopyranosyl-(1→4)-β-d-glucopyranosyl]-26-O-β-d-glucopyranosyl-25(R)-furosta-5,22(23)-dien-3β,20α,26-triol (1), 3-O-[β-d-glucopyranosyl-(1→3)-O-α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl]-26-O-β-d-glucopyranosyl-20(R)-methoxyl-25(R)-furosta-5,22(23)-dien-3β,26-diol (2) were isolated from the Dioscorea panthaica along with five known steroidal saponins (3–7). The structures of the new saponins were determined by detailed analysis of spectral data (including 2D NMR spectroscopy). The inhibitory activities of the saponins against α-glucosidase were investigated, gracillin (4) and 3-O-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl]-26-O-β-d-glucopyranosyl-25(R)-furosta-5,20(22)-dien-3β,26-diol (5) were found to exhibit potent activities with IC50 values of 0.11 ± 0.04 mM and 0.09 ± 0.01 mM. 相似文献
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Antonov AS Kalinovsky AI Dmitrenok PS Kalinin VI Stonik VA Mollo E Cimino G 《Carbohydrate research》2011,346(14):2182-2192
Seven new triterpene glycosides, erylosides R1 (1), T1 (3), T2 (4), T3 (5), T4 (6), T5 (7), and T6 (8) along with the known formoside (2) were isolated from the sponge Erylus formosus collected along the Caribbean coast of Mexico. Glycoside 1 was determined as a trisaccharide, glycoside 2 as a tetrasaccharide while glycosides 3–8 were hexasaccharide. Their carbohydrate chains were unprecedented and have never been found in oligosaccharides from other biological sources, except Erylus spp. Three carbohydrate chains in the glycosides 3 and 6, 4 and 7, 5 and 8 correspondingly are new. The glycosides 1–5 have penasterol as aglycone while glycosides 6–8 proved to be glycoconjugates of 24-methylene-14-carboxy-lanost-8(9)-en-3β-ol. 相似文献
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Four brominated aliphatic hydrocarbons (1–4), including a novel brominated ene-tetrahydrofuran named as mutafuran H (1), and five sterols (5–9) were isolated from the South China Sea sponge Xestospongia testudinaria. The structure of 1 was determined on the basis of NMR (1H, 13C NMR, HSQC, HMBC, 1H–1H COSY, and NOESY), MS, and optical rotation analysis. Known compounds were identified by comparison of their NMR data with those reported in the literature. Compounds 1–4, and 6–9 were evaluated for their toxicity against Artemia salina larvae, and anti-acetylcholinesterase activity. 相似文献
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P. Prabhakar Reddy R. Ranga Rao K. Rekha K. Suresh Babu J. Shashidhar G. Shashikiran V. Vijaya Lakshmi J. Madhusudana Rao 《Bioorganic & medicinal chemistry letters》2009,19(1):192-195
Phytochemical investigation of CHCl3 extract of the rhizomes of Hedychium spicatum led to the isolation of two new labdane-type diterpenes, compounds 1 and 2 along with five known compounds (3–7). Their structures were established on the basis of NMR (1D and 2D) and mass spectroscopic analysis. In addition, all the isolates were tested for their cytotoxicity against the Colo-205 (Colo-cancer), A-431 (skin cancer), MCF-7 (breast cancer), A-549 (lung cancer) and Chinese hamster ovary cells (CHO). Two new compounds 1 and 2 were shown good cytotoxic activity. 相似文献
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A series of new N′-[N-(2,3,4-tri-O-acetyl-β-d-xylopyranosyl)thiocarbamoyl]-2-[(1-aryl-1H-tetrazol-5-yl)sulfanyl]acetohydrazides 5a–5e were synthesized rapidly in high yields from 2-(1-aryl-1H-tetrazol-5-ylsulfanyl)acetohydrazides 3a–3e and 2,3,4-tri-O-acetyl-β-d-xylopyranosyl isothiocyanate 4, then 5a–5e were converted to a series of new 5-(1-aryl-1H-tetrazol-5-ylsulfanylmethyl)-N-(2,3,4-tri-O-acetyl-β-d-xylopyranosyl)-1,3,4-oxadiazole-2-amines 6a–6e and 5-(1-aryl-1H-tetrazol-5-ylsulfanylmethyl)-N-(2,3,4-tri-O-acetyl-β-d-xylopyranosyl)-1,3,4-thiadiazole-2-amines 7a–7e, respectively under mercuric acetate/alcohol system or acetic anhydride/phosphoric acid system, then deacetylated in the solution of CH3ONa/CH3OH. All of the novel compounds were characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis. The structures of compounds 2e, 3e, 5a and 5c have been determined by X-ray diffraction analysis. Some of the synthesized compounds displayed PTP1B inhibition and microorganism inhibition. 相似文献
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dos Santos MS Oliveira ML Bernardino AM de Léo RM Amaral VF de Carvalho FT Leon LL Canto-Cavalheiro MM 《Bioorganic & medicinal chemistry letters》2011,21(24):7451-7454
A series of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (4a–g) and 5-amino-1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (5a–g) were synthesized and evaluated in vitro against three Leishmania species: L. amazonensis, L. braziliensis and L. infantum (L. chagasi syn.). The cytotoxicity was assessed. Among the derivatives examined, six compounds emerged as the most active on promastigotes forms of L. amazonensis with IC50 values ranging from 15 to 60 μM. The reference drug pentamidine presented IC50 = 10 μM. However, these new compounds were less cytotoxic than pentamidine. Based on these results, the more promising derivative 5d was tested further in vivo. This compound showed inhibition of the progression of cutaneous lesions in CBA mice infected with L. amazonensis relative to an untreated control. 相似文献
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The house dust mite (Dermatophagoides pteronissinus) plays an important role in the pathogenesis of allergic diseases, including atopic dermatitis, and asthma. Monocyte chemotactic protein 1 (MCP-1/CCL2)/IL-6/IL-8 (CXCL8) plays a pivotal role in mediating the infiltration of various cells into the skin of atopic dermatitis and psoriasis. The aim of this study was to investigate the effect of D. pteronissinus extract (DpE) on expression of MCP-1/IL-6/IL-8 mRNA and protein and the signal transduction in the human monocytic cell line, THP-1. The mRNA and protein expression of MCP-1/CCL2, IL-6, and IL-8 were elevated by DpE in a time and dose-dependent manner in THP-1 cells. The increased expression of MCP-1, IL-6, and IL-8 was not affected by aprotinin (serine protease inhibitor) or E64 (cysteine protease inhibitor). We found that MCP-1 and IL-6 expression due to DpE was related to Src, protein kinase C δ (PKC δ), extracellular-signal-regulated kinase (ERK) and p38 mitogen-activated protein kinase (MAPK) and IL-8 expression was involved in Src family tyrosine kinase, PKC δ, ERK. DpE increased the phosphorylation of ERK and p38 MAPK after 5 min and peaked at 30 min. The activation was significantly blocked by PP2, an inhibitor of Src family tyrosine kinase and rottlerin, an inhibitor of PKC δ (p < 0.01). DpE increases MCP-1, IL-6, and IL-8 expression and transduces its signal via Src family tyrosine kinase, PKC, and ERK in a protease-independent manner. This finding may contribute to the elucidation of the pathogenic mechanism triggered by DpE . 相似文献
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Two new labdane-type diterpenes, blakielloside (1) and bartsiifolicoside (2), have been isolated from the dichloromethane extract of the foliar exudates of Blakiella bartsiifolia (S.F. Blake), an endemic and rare high altitude plant of the northern Andes, Venezuela. The structures of the new compounds were elucidated through extensive spectroscopic methods (IR, HR-FIA-MS, 1D and 2D NMR). Both natural products showed phytotoxic activity against Allium cepa, Cucumis sativus and Solanum lycopersicum. 相似文献
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Deng Y Chin YW Chai HB de Blanco EC Kardono LB Riswan S Soejarto DD Farnsworth NR Kinghorn AD 《Phytochemistry letters》2011,4(3):213-217
A phytochemical investigation of the leaves of Vitex quinata (Lour.) F.N. Williams (Verbenaceae), guided by a cytotoxicity assay against the MCF-7 human breast cancer cell line, led to the isolation of a new δ-truxinate derivative (1) and a new phytonoic acid derivative (2), together with 12 known compounds. The structures of the new compounds were determined by spectroscopic methods as dimethyl 3,4,3′,4′-tetrahydroxy-δ-truxinate (1) and methyl 10R-methoxy-12-oxo-9(13),16E-phytodienoate (2), respectively. In a cytotoxicity assay, (S)-5-hydroxy-7,4′-dimethoxyflavanone (3) was found to be the sole active principle, with ED50 values of 1.1–6.7 μM, respectively, when tested against a panel of three human cancer cells. Methyl 3,4,5-O-tricaffeoyl quinate (4) showed activity in an enzyme-based ELISA NF-κB p65 assay, with an ED50 value of 10.3 μM. 相似文献
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Summary. The effect of taurine (Tau) and taurine chloramine (Tau-Cl) on the production of TNF-α, IL-1β, and IL-6 by peripheral blood mononuclear cells of healthy volunteers was examined. Cells were stimulated with bacterial
lipopolysaccharide (LPS) in the presence of either Tau or Tau-Cl. After 24 h culture the cytokine concentrations were measured
in both culture supernatants (secreted) and cell lysates (cell-associated) using ELISA. In LPS-stimulated cells Tau-Cl inhibited
both the secreted and cell-associated IL-1β and IL-6, while exerted dual effect on TNF-α production: raising it slightly at low and reducing at higher concentration. By contrast, Tau had no significant effect on
the cytokine production. These results indicate that Tau-Cl modulates synthesis of pro-inflammatory cytokines, and therefore
it may play a role in the initiation and propagation of immune response.
Received November 29, 2001 Accepted January 18, 2002 Published online August 30, 2002
Acknowledgments This research was supported by grants from the State Committee for Scientific Research of Poland (No 4 P05B 01018) and the
Institute of Rheumatology (No I/14). The Institute of Rheumatology is supported by a core grant from the State Committee for
Scientific Research of Poland.
Authors' address: Ewa Kontny, Ph.D., Department of Pathophysiology and Immunology, Institute of Rheumatology, Spartanska 1, 02-637 Warsaw,
Poland, E-mail: zpatiir@warman.com.pl
Abbreviations: Tau, taurine; Tau-Cl, taurine chloramine; LPS, lipopolysaccharide; TNF-α, tumor necrosis factor-α; IL-1β, interleukin 1β; IL-6, interleukin 6; PBMC, peripheral blood mononuclear cells 相似文献
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Nguyen Hoai Nam Phan Van Kiem Ninh Khac Ban Nguyen Phuong Thao Nguyen Xuan Nhiem Nguyen Xuan Cuong Christophe Tistaert Bieke Dejaegher Yvan Vander Heyden Joëlle Quetin-Leclercq Do Thi Thao Chau Van Minh 《Phytochemistry letters》2011,4(3):348-352
Two new cycloartane derivatives, macrostachyosides A (1) and B (2), and seventeen known compounds were isolated from the methanol extract of Mallotus macrostachyus leaves. Their structures were elucidated by NMR and MS data. Macrostachyosides A (1) and B (2) showed significant cytotoxic activities on KB (epidermoid carcinoma) and LU-1 (lung adenocarcinoma) human cancer cell lines with IC50 values ranging from 4.31 ± 0.09 to 7.12 ± 0.07 μg/mL. 相似文献
19.
As part of an effort to generate broad-spectrum inhibitors of rhinovirus replication, novel series of (E)-3-[(E)-3-phenylallylidene]chroman-4-ones 1a–e, (E)-3-(3-phenylprop-2-yn-1-ylidene)chroman-4-ones 2a and 2b, (Z)-3-[(E)-3-phenylallylidene]chromans 3a–e, and (E)-3-(3-phenylprop-1-en-1-yl)-2H-chromenes 4a–d were designed and synthesized. All the compounds were tested in vitro for their efficacy against infection by human rhinovirus (HRV) 1B and 14, two representative serotypes for rhinovirus group B and A, respectively. Most of the analogues were found to be potent and selective inhibitors of both HRVs, although HRV 1B was generally more susceptible than HRV 14. Mechanism of action studies of (E)-6-chloro-3-(3-phenylprop-1-en-1-yl)-2H-chromene 4b, the most potent compound on HRV 1B infection, suggested that 4b behaves as a capsid-binder probably acting at the uncoating level. 相似文献