Novel derivatives of eugenol as potent anti-inflammatory agents <i>via</i> PPARγ agonism: rational design, synthesis, analysis, PPARγ protein binding assay and computational studies

Anjum, Noor Fathima; Shanmugarajan, Dhivya; Shivaraju, Vasanth Kumar; Faizan, Syed; Naishima, Namburu Lalitha; Kumar, B. R. Prashantha; Javid, Saleem; Purohit, Madhusudan

doi:10.1039/d2ra02116a

Cited by 7 publications

(3 citation statements)

References 41 publications

(56 reference statements)

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“…Numerous anti-inflammatory, antioxidant, antiallergic, antimutagenic, anticancer, and analgesic properties can be found in eugenol ( Figure 1 B) [ 21 , 31 , 59 , 60 , 61 ]. Eugenol treatment in combination with conventional medications has significant potential and ability to eradicate drug-resistant strains, forming a part of natural essential oil offers far less downsides than other types of synthetically produced substances.…”

Section: Phytochemical Compositionmentioning

confidence: 99%

An Update on the Therapeutic Anticancer Potential of Ocimum sanctum L.: “Elixir of Life”

et al. 2023

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In most cases, cancer develops due to abnormal cell growth and subsequent tumour formation. Due to significant constraints with current treatments, natural compounds are being explored as potential alternatives. There are now around 30 natural compounds under clinical trials for the treatment of cancer. Tulsi, or Holy Basil, of the genus Ocimum, is one of the most widely available and cost-effective medicinal plants. In India, the tulsi plant has deep religious and medicinal significance. Tulsi essential oil contains a valuable source of bioactive compounds, such as camphor, eucalyptol, eugenol, alpha-bisabolene, beta-bisabolene, and beta-caryophyllene. These compounds are proposed to be responsible for the antimicrobial properties of the leaf extracts. The anticancer effects of tulsi (Ocimum sanctum L.) have earned it the title of “queen of herbs” and “Elixir of Life” in Ayurvedic treatment. Tulsi leaves, which have high concentrations of eugenol, have been shown to have anticancer properties. In a various cancers, eugenol exerts its antitumour effects through a number of different mechanisms. In light of this, the current review focuses on the anticancer benefits of tulsi and its primary phytoconstituent, eugenol, as apotential therapeutic agent against a wide range of cancer types. In recent years, tulsi has gained popularity due to its anticancer properties. In ongoing clinical trials, a number of tulsi plant compounds are being evaluated for their potential anticancer effects. This article discusses anticancer, chemopreventive, and antioxidant effects of tulsi.

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Section: Phytochemical Compositionmentioning

confidence: 99%

An Update on the Therapeutic Anticancer Potential of Ocimum sanctum L.: “Elixir of Life”

et al. 2023

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“…Eugenol possesses diverse biological properties such as analgesic, antioxidant, antiviral, and antibacterial properties [4][5][6]. It has also been studied by its anti-inflammatory, antidepressant, antiepileptic, neuroprotective, and anticancer activity [7][8][9]. Eugenol has been observed to affect both peripheral and central neurons, potentially affecting TRPV1, TRPV3 and TRPA1 channels [10][11][12].…”

Section: Introductionmentioning

confidence: 99%

Diclofenac-eugenol modulation of Kv7 and TRPV1 ion channels

Rivera-Ruedas,

Medina-Vilchis,

Romero-Tovar

et al. 2024

Preprint

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Pharmacological targeting of ion channels represents a crucial avenue for pain management. Among these, the Kv7 family of ion channels plays a significant role controlling neuronal excitability and the generation and propagation of pain-related nerve impulses, thus mitigating excessive electrical signaling and curtailing the exaggerated transmission of pain signals. Pain management strategies often involve a multimodal approach, combining various medications with distinct mechanisms of action to achieve optimal outcomes. Eugenol possesses a spectrum of biological activities, including analgesic and anti-inflammatory properties. When used in conjunction with the anti-inflammatory drug diclofenac, eugenol demonstrates enhanced analgesic efficacy in animal models. We investigated the effects of diclofenac and eugenol on Kv7 and TRPV1 ion channels, both agents act as Kv7 activators, whereas diclofenac inhibits the TRPV1 current, and eugenol reduce the capsaicin-activated current presumably competing for the same binding site. Eugenol shows a time dependent biphasic effect on acid-activated TRPV1 current, first activating and then a slow decay of the current. When eugenol and diclofenac are used together, they limit the extent of depolarization of cells expressing Kv7 and TRPV1. Our results shed light on the combined effectiveness of eugenol and diclofenac in the treatment of acute pain.

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“…Eugenol is the main constituent of clove ( Syzygium aromaticum ) essential oil, and exhibits important antimicrobial [ 14 ], antitumor [ 15 , 16 ], anti-oxidant [ 17 , 18 ], and anti-inflammatory effects [ 19 , 20 ]. The antimicrobial activity of eugenol is mainly attributed to its phenolic structure and hydrophobic character.…”

Section: Introductionmentioning

confidence: 99%

MAPLE Processed Nanostructures for Antimicrobial Coatings

Hudiţă

Grumezescu

Gherasim

et al. 2022

IJMS

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Despite their great benefits for debilitated patients, indwelling devices are prone to become easily colonized by resident and opportunistic microorganisms, which have the ability to attach to their surfaces and form highly specialized communities called biofilms. These are extremely resistant to host defense mechanisms and antibiotics, leading to treatment failure and device replacement, but also to life-threatening complications. In this study, we aimed to optimize a silica (SiO2)-coated magnetite (Fe3O4)-based nanosystem containing the natural antimicrobial agent, eugenol (E), suitable for MAPLE (matrix-assisted pulsed laser evaporation) deposition as a bioactive coating for biomedical applications. X-ray diffraction, thermogravimetric analysis, Fourier-transform infrared spectroscopy, and transmission electron microscopy investigations were employed to characterize the obtained nanosystems. The in vitro tests evidenced the superior biocompatibility of such nanostructured coatings, as revealed by their non-cytotoxic activity and ability to promote cellular proliferation and sustain normal cellular development of dermal fibroblasts. Moreover, the obtained nanocoatings did not induce proinflammatory events in human blood samples. Our studies demonstrated that Fe3O4 NPs can improve the antimicrobial activity of E, while the use of a SiO2 matrix may increase its efficiency over prolonged periods of time. The Fe3O4@SiO2 nanosystems showed excellent biocompatibility, sustaining human dermal fibroblasts’ viability, proliferation, and typical architecture. More, the novel coatings lack proinflammatory potential as revealed by the absence of proinflammatory cytokine expression in response to human blood sample interactions.

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Novel derivatives of eugenol as potent anti-inflammatory agents via PPARγ agonism: rational design, synthesis, analysis, PPARγ protein binding assay and computational studies

Abstract: Rational design, synthesis, analysis, PPARγ protein binding assay and computational studies of novel eugenol derivatives.

Cited by 7 publications

References 41 publications

An Update on the Therapeutic Anticancer Potential of Ocimum sanctum L.: “Elixir of Life”

An Update on the Therapeutic Anticancer Potential of Ocimum sanctum L.: “Elixir of Life”

Diclofenac-eugenol modulation of Kv7 and TRPV1 ion channels

MAPLE Processed Nanostructures for Antimicrobial Coatings

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