Study on the substituents' effects of a series of synthetic chalcones against the yeast Candida albicans

Batovska, Daniela; Parushev, St.; Slavova, Angela; Bankova, Vassya; Tsvetkova, Iva; Ninova, Mariana; Najdenski, Hristo

doi:10.1016/j.ejmech.2006.08.012

Cited by 93 publications

(64 citation statements)

References 11 publications

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“…Total twelve compounds (4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) were synthesized as shown Inhibitory Effects on LPS-induced ROS and NO Production in RAW 264.7 Macrophages. Inhibitory activity of LPS-induced ROS and NO production in RAW 264.7 macrophages of prepared compounds is shown in Table 1.…”

Section: Resultsmentioning

confidence: 99%

Thieny/Furanyl-hydroxyphenylpropenones as Inhibitors of LPS-induced ROS and NO Production in RAW 264.7 Macrophages, and Their Structure-Activity Relationship Study

Kadayat¹,

Kim²,

Nam³

et al. 2014

Bulletin of the Korean Chemical Society

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Twelve thienyl/furanyl-hydroxyphenylpropenones were systematically designed and synthesized, and evaluated for their inhibitory effect on LPS-induced ROS and NO production in RAW 264.7 macrophages. Compound 11 displayed the most significant inhibitory activity of LPS-induced ROS and NO production in RAW 264.7 macrophages. Structure-activity relationship study indicated that para-hydroxyphenyl moiety plays an important role for inhibitory activities on both LPS-induced ROS and NO production as well as 3-thienyl moiety on molecule.

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Section: Resultsmentioning

confidence: 99%

Thieny/Furanyl-hydroxyphenylpropenones as Inhibitors of LPS-induced ROS and NO Production in RAW 264.7 Macrophages, and Their Structure-Activity Relationship Study

Kadayat¹,

Kim²,

Nam³

et al. 2014

Bulletin of the Korean Chemical Society

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“…In addition, slow reactions can be easily followed by a continuous recording of the signal for a long time without any disturbance of the system. Microcalorimetry can also reveal temporal details (such as thermal effect) that are not observable by other techniques (Batovska et al, 2007;Leng et al, 2007;Kwon et al, 2008). It has already been demonstrated that calorimetric methods can be used for fundamental studies of organisms' growth (von Ah et al, 2008;Yan et al, 2009b).…”

Section: Original Articlementioning

confidence: 99%

Applications of microcalorimetry in the antibacterial activity evaluation of variousRhizoma coptidis

Feng¹,

Yan²,

Zhao³

et al. 2011

Pharmaceutical Biology

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“…A number of previous studies have demonstrated that chalcones and its various derivatives regulate diverse biological functions and become the attractive molecule for the development of pharmacological agents in many diseases. In addition to the original observation showing the potent inhibitory effect on topoisomerase and subsequent on anti-cancer effects (Kim et al, 2013), chalcone and its derivatives also possess anti-bacterial (Avila et al, 2008), anti-fungal (Batovska et al, 2007), anti-oxidant (Dinkova-Kostova et al, 2001 properties. In particular, recent studies have shown the potent anti-inflammatory activities of the chalcones in various experimental conditions (Kontogiorgis et al, 2008).…”

Section: Wwwbiomoltherorgmentioning

confidence: 99%

TI-I-174, a Synthetic Chalcone Derivative, Suppresses Nitric Oxide Production in Murine Macrophages via Heme Oxygen-ase-1 Induction and Inhibition of AP-1

Kim¹,

Kadayat²,

Kim³

et al. 2014

Biomol Ther

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This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. www.biomolther.orgChalcones (1,3-diaryl-2-propen-1-ones), a flavonoid subfamily, are widely known for their anti-inflammatory properties. Propenone moiety in chalcones is known to play an important role in generating biological responses by chalcones. In the present study, we synthesized chalcone derivatives structurally modified in propenone moiety and examined inhibitory effect on nitric oxide (NO) production and its potential mechanisms. Among the chalcone derivatives used for this study, TI-I-174 (3-(2-Hydroxyphenyl)-1-(thiophen-3-yl)prop-2-en-1-one) most potently inhibited lipopolysaccharide (LPS)-stimulated nitrite production in RAW 264.7 macrophages. TI-I-174 treatment also markedly inhibited inducible nitric oxide synthase (iNOS) expression. However, TI-I-174 did not significantly affect production of IL-6, cyclooxygenase-2 (COX-2) and tumor necrosis factor-α (TNF-α), implying that TI-I-174 inhibits production of inflammatory mediators in a selective manner. Treatment of macrophages with TI-I-174 significantly inhibited transcriptional activity of activator protein-1 (AP-1) as determined by luciferase reporter gene assay, whereas nuclear factor-kB (NF-kB) activity was not affected by TI-I-1744. In addition, TI-I-174 significantly inhibited activation of c-Jun-N-Terminal kinase (JNK) without affecting ERK1/2 and p38MAPK, indicating that down-regulation of iNOS gene expression by TI-I-174 is mainly attributed by blockade of JNK/AP-1 activation. We also demonstrated that TI-I-174 treatment led to an increase in heme oxygenase-1 (HO-1) expression both at mRNA and protein level. Transfection of siRNA targeting HO-1 reversed TI-I-174-mediated inhibition of nitrite production. Taken together, these results indicate that TI-I-174 suppresses NO production in LPS-stimulated RAW 264.7 macrophages via induction of HO-1 and blockade of AP-1 activation. , 1997). In addition, recent studies have also revealed that HO-1 induction modulates inflammatory process via suppressing the production of pro-inflammatory mediators, such as COX-2, TNF-α and iNOS (Wang et al., 2001). Furthermore, deficiency of HO-1 in mice exhibited a severe inflammation (True et al., 2007), while HO-1 over-expression prevented inflammatory responses in various experimental conditions (Otterbein et al., 2003;Onyiah et al., 2013). Therefore, based on previous reports, modulation of HO-1 activity may be a promising strategy for the treatment of the diseases associated with inflammatory conditions. Chalcones (1,3-diaryl-2-propen-1-ones), a group of polyphenolic and flavonoid family, are widely biosynthesized in plants. A number of previous studies have demonstrated that chalcones and its various derivatives regulate diverse biological functions and be...

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Study on the substituents' effects of a series of synthetic chalcones against the yeast Candida albicans

Cited by 93 publications

References 11 publications

Thieny/Furanyl-hydroxyphenylpropenones as Inhibitors of LPS-induced ROS and NO Production in RAW 264.7 Macrophages, and Their Structure-Activity Relationship Study

Thieny/Furanyl-hydroxyphenylpropenones as Inhibitors of LPS-induced ROS and NO Production in RAW 264.7 Macrophages, and Their Structure-Activity Relationship Study

Applications of microcalorimetry in the antibacterial activity evaluation of variousRhizoma coptidis

TI-I-174, a Synthetic Chalcone Derivative, Suppresses Nitric Oxide Production in Murine Macrophages via Heme Oxygen-ase-1 Induction and Inhibition of AP-1

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