- Synthesis and in vitro evaluation of c‐7 and c‐8 luteolin derivatives as influenza endonuclease inhibitors
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The part of the influenza polymerase PA subunit featuring endonuclease activity is a target for anti‐influenza therapies, including the FDA‐approved drug Xofluza. A general feature of endonuclease inhibitors is their ability to chelate Mg2+ or
- Brynda, Ji?í,Dra?ínsky, Martin,Ko?í?ek, Milan,Konvalinka, Jan,Krá?, Michal,Machara, Ale?,Majer, Pavel,Radilová, Kate?ina,Reiberger, Robert,Zima, Václav
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- Extraction, Isolation and Characterization of Valuable Worked on Acacia Tortilis
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Acacia tortilis is one of the important species of genus Acacia belonging to family Leguminaceae. Though there is no more study performed on this plant but it plays important role in the countries where it found. These countries include North Africa, Arabian Peninsula and Asian countries. The various part of Acacia tortilis plant say leaves, pods, gum exudates and bark were used as antidiabetic, antidiarrhoeal, antiasthmatic and also had several other medicinal benefits. The present discussion deals with the isolation and characterization of the following compounds from the leaves of Acacia tortilis. Lupan-3-ol, 12,20-diene, Lupan-12, 20-dien 3-one, Friedelin, ?-amyrin, ?- sitosterol, Apigenin, Luteolin, Quercetin, 5,7-dihydroxy-4-p-methyl benzylisoflavone, Vitexin, 2',6'-dihydroxy chalcone-4'-O-glucoside.
- Muhaisen, Hasan M. H.
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p. 6731 - 6747
(2021/11/01)
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- Phosphoramidate protides of five flavones and their antiproliferative activity against HepG2 and L-O2 cell lines
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A series of flavone-7-phosphoramidate derivatives were synthesized and tested for their antiproliferative activity in vitro against human hepatoma cell line HepG2 and human normal hepatic cell line L-O2. Compound 8d, 16d and 17d, incorporating the amino acid alanine, exhibited high inhibitory activity on HepG2 cell line with IC50 values of 9.0 μmol/L, 5.5 μmol/L and 6.6 μmol/L. The introduction of acyl groups played a pivotal role in the selective inhibition toward human hepatoma HepG2 cells, except for compound 8a, 9a and 16b. Compound 8d, 16d and 17d could significantly induce G2/M arrest in HepG2 cells. Specially, Compound 16d could lead early apoptosis in HepG2 cells.
- Li, Yue-Qing,Yang, Fei,Wang, Liu,Cao, Zhi,Han, Tian-Jiao,Duan, Zhe-Ang,Li, Zhen,Zhao, Wei-Jie
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p. 196 - 208
(2016/05/02)
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- Synthesis, characterization, anti-inflammatory and anti-proliferative activity against MCF-7 cells of O-alkyl and O-acyl flavonoid derivatives
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A series of O-alkyl and O-acyl flavonoid derivatives was synthesized in high efficiency. Alkylation and acylation of 5-hydroxyflavonoids showed that the low reactivity hydroxyl group, 5-OH, well reacted with strong reagents whereas with weaker reagents, the different products were obtained dependently on structural characteristic of ring C of respective flavonoid. In order to evaluate anti-inflammatory activity, all compounds were tested for in vitro inhibition of bovine serum albumin denaturation and in vivo inhibition of carrageenan-induced mouse paw edema. Among them, the compounds 3, 3b, 4b and 4c demonstrated more effective anti-inflammatory activity than standard drugs (diclofenac sodium and ketoprofen) in both tests. Meanwhile, the flavonoids 2, 2c, 3a and 4b displayed anti-proliferative activity against MCF-7 cell lines. Triacetyl derivative of hesperetin 4b inducing degradation of DNA in MCF-7 cells was observed.
- Hoang, T. Kim-Dung,Huynh, T. Kim-Chi,Nguyen, Thanh-Danh
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- Design and discovery of flavonoid-based HIV-1 integrase inhibitors targeting both the active site and the interaction with LEDGF/p75
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HIV integrase (IN) is an essential enzyme for the viral replication. Currently, three IN inhibitors have been approved for treating HIV-1 infection. All three drugs selectively inhibit the strand transfer reaction by chelating a divalent metal ion in the
- Li, Bo-Wen,Zhang, Feng-Hua,Serrao, Erik,Chen, Huan,Sanchez, Tino W.,Yang, Liu-Meng,Neamati, Nouri,Zheng, Yong-Tang,Wang, Hui,Long, Ya-Qiu
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p. 3146 - 3158
(2014/06/09)
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- Flavonoids of Zizyphus rugosa
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Three flavonolds - kaempferol-4′-methylether, luteolin and luteolin-7-O-glucoside have been isolated from the barks of Zizyphus rugosa and their structures were established by spectral evidences. This is the first report of these flavonoids from Z. rugosa.
- Singh,Pandey,Singh, Sarita,Singh,Singh
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experimental part
p. 177 - 178
(2010/04/05)
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- Flavonoids from Acacia tortilis
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A novel isoflavone, 5,7-dihydroxy-4′- p-methyl benzyl isoflavone 1a, and three known flavonoids apigenin, luteolin and quercetin have been isolated from the leaves of Acacia tortilis. Their structures were elucidated by chemical and physical data (IR, UV,
- Muhaisen, Hasan M.H.,Ilyas,Mushfiq,Parveen, Mehtab,Basudan, Omer A.
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p. 276 - 278
(2007/10/03)
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- Studies on the Constituents of Palmae Plants. I. The Constituents of Trachycarpus fortunei (HOOK.) H. WENDL. (1)
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The constituents of the leaves, stems and underground parts of Trachycarpus fortunei (HOOK.) H.Wendl. (Palmae) have been investigated.Glucoluteolin (3), luteolin 7-O-rutinoside (=scolymoside, 4) and methyl proto-Pb (6) from the leaves, dioscin (1), Pb (2), methyl protodioscin (5) and methyl proto-Pb (6) from the stems, and dioscin (1) and methyl proto-Pb (6) from the underground parts were isolated and identified.This is the first report of the isolation of steroidal saponins from Palmae plants and these results are interesting from the standpoint of chemotaxonomy. keywords - Trachycarpus fortunei; Palmae; steroidal saponin; furostanol oligoside; diosgenin; proto-diosgenin; flavone glycoside; luteolin; glucoluteolin; scolymoside
- Hirai, Yasuaki,Sanada, Shuichi,Ida, Yoshiteru,Shoji, Junzo
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p. 295 - 301
(2007/10/02)
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