Biological evaluation and molecular docking studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity

Tumer, Tugba Boyunegmez; Önder, Ferah Cömert; Ipek, Hande; Güngör, Tuğba; Savranoglu, Seda; Tok, Tuğba Taşkın; Çelik, Ayhan; Ay, Mehmet Oğuzhan

doi:10.1016/j.intimp.2016.12.009

Cited by 26 publications

(18 citation statements)

References 36 publications

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“…Normally, this highly regulated and self-limiting phenomenon promotes the healing process. However, uncontrolled and pro-longed process, called as chronic inflammation, may cause sustained activation of immune cells resulted in high amount of cytokine release [344,345]. This persistent response potentially leads to pathological disorders such as autoimmune diseases, diabetes, heart diseases, cancer and various neurodegenerative disorders.…”

Section: Biological Activities Piper Plantsmentioning

confidence: 99%

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

et al. 2019

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Piper species are aromatic plants used as spices in the kitchen, but their secondary metabolites have also shown biological effects on human health. These plants are rich in essential oils, which can be found in their fruits, seeds, leaves, branches, roots and stems. Some Piper species have simple chemical profiles, while others, such as Piper nigrum, Piper betle, and Piper auritum, contain very diverse suites of secondary metabolites. In traditional medicine, Piper species have been used worldwide to treat several diseases such as urological problems, skin, liver and stomach ailments, for wound healing, and as antipyretic and anti-inflammatory agents. In addition, Piper species could be used as natural antioxidants and antimicrobial agents in food preservation. The phytochemicals and essential oils of Piper species have shown strong antioxidant activity, in comparison with synthetic antioxidants, and demonstrated antibacterial and antifungal activities against human pathogens. Moreover, Piper species possess therapeutic and preventive potential against several chronic disorders. Among the functional properties of Piper plants/extracts/active components the antiproliferative, anti-inflammatory, and neuropharmacological activities of the extracts and extract-derived bioactive constituents are thought to be key effects for the protection against chronic conditions, based on preclinical in vitro and in vivo studies, besides clinical studies. Habitats and cultivation of Piper species are also covered in this review. In this current work, available literature of chemical constituents of the essential oils Piper plants, their use in traditional medicine, their applications as a food preservative, their antiparasitic activities and other important biological activities are reviewed.

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Section: Biological Activities Piper Plantsmentioning

confidence: 99%

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

et al. 2019

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“…1). 25,26 Once the 4-(nitrophenyl)hydrazone derivatives of N-acylhydrazone were designed, an efficient synthetic route was implemented on the grounds of the problem's retrosynthetic analysis (Scheme 1), leading to a series of novel compounds, which was studied by screening substituents attached to the aryl ring located near to the acyl group (Scheme 2). A set of para-substituents was selected by physical-chemical criteria: r p -Hammett constant, ranging from À0.83 for N,N-dimethylamino to +0.78 for nitro, lipophilicity and hydrogen bond acceptor/donor, allowing us to study the substituent effect on the activity.…”

Section: Introductionmentioning

confidence: 99%

Structural design, synthesis and substituent effect of hydrazone-N-acylhydrazones reveal potent immunomodulatory agents

Meira

Filho²,

Sousa

et al. 2018

Bioorganic & Medicinal Chemistry

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4-(Nitrophenyl)hydrazone derivatives of N-acylhydrazone were synthesized and screened for suppress lymphocyte proliferation and nitrite inhibition in macrophages. Compared to an unsubstituted N-acylhydrazone, active compounds were identified within initial series when hydroxyl, chloride and nitro substituents were employed. Structure-activity relationship was further developed by varying the position of these substituents as well as attaching structurally-related substituents. Changing substituent position revealed a more promising compound series of anti-inflammatory agents. In contrast, an N-methyl group appended to the 4-(nitrophenyl)hydrazone moiety reduced activity. Anti-inflammatory activity of compounds is achieved by modulating IL-1b secretion and prostaglandin E2 synthesis in macrophages and by inhibiting calcineurin phosphatase activity in lymphocytes. Compound SintMed65 was advanced into an acute model of peritonitis in mice, where it inhibited the neutrophil infiltration after being orally administered. In summary, we demonstrated in great details the structural requirements and the underlying mechanism for anti-inflammatory activity of a new family of hydrazone-N-acylhydrazone, which may represent a valuable medicinal chemistry direction for the anti-inflammatory drug development in general.

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“…The effects of GR24 (5, 10, 20, 50, 100 μM) on cell viability were determined using the MTT assay as described previously …”

Section: Methodsmentioning

confidence: 99%

Multitarget Profiling of a Strigolactone Analogue for Early Events of Alzheimer’s Disease: In Vitro Therapeutic Activities against Neuroinflammation

Kurt

Ozleyen

Antika

et al. 2020

ACS Chem. Neurosci.

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Neuropathological changes in Alzheimer's disease (AD) are directly linked to the early inflammatory microenvironment in the brain. Therefore, disease-modifying agents targeting neuroinflammation may open up new avenues in the treatment of AD. Strigolactones (SLs), subclasses of structurally diverse and biologically active apocarotenoids, have been recently identified as novel phytohormones. In spite of the remarkable anticancer capacity shown by SLs, their effects on the brain remained unexplored. Herein, the SIM-A9 microglial cell line was used as a phenotypic screening tool to search for the representative SL, GR24, demonstrating marked potency in the suppression of lipopolysaccharide (LPS)-induced neuroinflammatory/neurotoxic mediators by regulating NF-κB, Nrf2, and PPARγ signaling. GR24 also in the brain endothelial cell line bEnd.3 mitigated the LPS-increased permeability as evidenced by reduced Evans' blue extravasation through enhancing the expression of tight junction protein, occludin. Collectively, the present work shows the anti-neuroinflammatory and glia/neuroprotective properties of GR24, making SLs promising scaffolds for the development of novel anti-AD candidates.

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Biological evaluation and molecular docking studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity

Cited by 26 publications

References 36 publications

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

Structural design, synthesis and substituent effect of hydrazone-N-acylhydrazones reveal potent immunomodulatory agents

Multitarget Profiling of a Strigolactone Analogue for Early Events of Alzheimer’s Disease: In Vitro Therapeutic Activities against Neuroinflammation

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