Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI)

Qian, Jianchang; Chen, Xianxin; Shu, Shengqiang; Zhang, Wenxin; Fang, Bo; Zhao, Yunjie; Liu, Zhiguo; Liang, Guang

doi:10.1016/j.ejmech.2019.02.042

Cited by 38 publications

(28 citation statements)

References 30 publications

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Section: Recent Development In Anti-inflammatory Agentsmentioning

confidence: 99%

“…It was found that compounds 40a and 40b (Figure 4) showed the most potent anti-inflammatory activities. In addition, the two compounds had higher structural stability, orally bioavailability in vitro and markedly alleviated LPSinduced acute lung injury (ALI) 55 . Two chalcone derivatives as anti-inflammatory agents were developed by Emam et al They reported that compound 41 (Figure 4) exhibited the highest anti-inflammatory activity by inhibition of NO concentration in LPS-induced RAW264.7 macrophages (IC 50 ¼11.2 mM).…”

Section: Chalcone Derivatives As Anti-inflammatory Agentsmentioning

confidence: 99%

See 1 more Smart Citation

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Bian

Wu³

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Inflammation and disease are closely related. Inflammation can induce various diseases, and diseases can promote inflammatory response, and two possibly induces each other in a bidirectional loop. Inflammation is usually treated using synthetic anti-inflammatory drugs which are associated with several adverse effects hence are not safe for long-term use. Therefore, there is need for anti-inflammatory drugs which are not only effective but also safe. Several researchers have devoted to the research and development of effective anti-inflammatory drugs with little or no side effects. In this review, we studied some small molecules with reported anti-inflammatory activities and hence potential sources of anti-inflammatory agents. The information was retrieved from relevant studies published between January 2019 and May, 2021 for review. This review study was aimed to provide relevant information towards the design and development of effective and safe anti-inflammation agents.

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Section: Recent Development In Anti-inflammatory Agentsmentioning

confidence: 99%

Section: Chalcone Derivatives As Anti-inflammatory Agentsmentioning

confidence: 99%

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Bian

Wu³

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Mitogen-activated protein kinases (MAPKs) pathway, composed of ERK, c -Jun amino-terminal kinases (JNK) and p38, was one of the key signaling pathways in the release of inflammatory cytokines stimulated by LPS [ 18 ]. The release of inflammatory mediators can be regulated through activation of MAPK signaling pathways, especially p38 and ERK [ 19 ]. The possible mechanism of the anti-inflammatory activity of the compound 6h in vivo was explored by studying the MAPK signaling pathway.…”

Section: Resultsmentioning

confidence: 99%

Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury

Chen

Wei

Zhu

et al. 2021

European Journal of Medicinal Chemistry

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Acute lung injury/acute respiratory distress syndrome (ALI/ARDS), a clinically high mortality disease, has not been effectively treated till now, and the development of anti-acute lung injury drugs is imminent. Acute lung injury was efficiently treated by inhibiting the cascade of inflammation, and reducing the inflammatory response in the lung. A series of novel compounds with highly efficient inhibiting the expression of inflammatory factors were designed by using 4-indolyl-2-aminopyrimidine as the core skeleton. Totally eleven 4-indolyl-2-arylaminopyrimidine derivatives were designed and synthesized. As well, the related anti -ALI activity of these compounds was evaluated. Compounds 6c and 6h showed a superior activity among these compounds, and the inhibition rate of IL-6 and IL-8 release ranged from 62% to 77%, and from 65% to 72%, respectively. Furthermore, most of compounds had no significant cytotoxicity in vitro . The infiltration of inflammatory cells into lung tissue significantly reduced by using compound 6h (20 mg/kg) in the ALI mice model, which achieved the effect of protecting lung tissue and improving ALI. In addition, the inflammatory response was inhibited by using compound 6h through inhibiting phosphorylation of p-38 and ERK in MAPK signaling pathway, and resulted in protective effect on ALI. These data indicated that compound 6h showed good anti-inflammatory activity in vitro and in vivo , which was expected to become a leading compound for the treatment of ALI.

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“…Further studies are required to determine whether these constituents may be the lead compound for further development to treat inflammatory diseases including sepsis. It is also worth noting that since curcumin is recognized as the most pharmacologically active constituent isolated from C. longa, many studies have also been conducted to improve the anti-inflammatory activity of curcumin through structural modifications [118][119][120][121][122][123].…”

Section: Curcuma Longamentioning

confidence: 99%

A Review of Malaysian Herbal Plants and Their Active Constituents with Potential Therapeutic Applications in Sepsis

Liew

Hafiz

Chong

et al. 2020

Evidence-Based Complementary and Alternative Medicine

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Sepsis refers to organ failure due to uncontrolled body immune responses towards infection. The systemic inflammatory response triggered by pathogen-associated molecular patterns (PAMPs), such as lipopolysaccharide (LPS) from Gram-negative bacteria, is accompanied by the release of various proinflammatory mediators that can lead to organ damage. The progression to septic shock is even more life-threatening due to hypotension. Thus, sepsis is a leading cause of death and morbidity globally. However, current therapies are mainly symptomatic treatment and rely on the use of antibiotics. The lack of a specific treatment demands exploration of new drugs. Malaysian herbal plants have a long history of usage for medicinal purposes. A total of 64 Malaysian plants commonly used in the herbal industry have been published in Malaysian Herbal Monograph 2015 and Globinmed website (http://www.globinmed.com/). An extensive bibliographic search in databases such as PubMed, ScienceDirect, and Scopus revealed that seven of these plants have antisepsis properties, as evidenced by the therapeutic effect of their extracts or isolated compounds against sepsis-associated inflammatory responses or conditions in in vitro or/and in vivo studies. These include Andrographis paniculata, Zingiber officinale, Curcuma longa, Piper nigrum, Syzygium aromaticum, Momordica charantia, and Centella asiatica. Among these, Z. officinale is the most widely studied plant and seems to have the highest potential for future therapeutic applications in sepsis. Although both extracts as well as active constituents from these herbal plants have demonstrated potential antisepsis activity, the activity might be primarily contributed by the active constituent(s) from each of these plants, which are andrographolide (A. paniculata), 6-gingerol and zingerone (Z. officinale), curcumin (C. longa), piperine and pellitorine (P. nigrum), biflorin (S. aromaticum), and asiaticoside, asiatic acid, and madecassoside (C. asiatica). These active constituents have shown great antisepsis effects, and further investigations into their clinical therapeutic potential may be worthwhile.

show abstract

Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI)

Cited by 38 publications

References 30 publications

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury

A Review of Malaysian Herbal Plants and Their Active Constituents with Potential Therapeutic Applications in Sepsis

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