Synergistic effect of tolfenamic acid and glycyrrhizic acid on TPA-induced skin inflammation in mice

Liu, Wenfeng; Huang, Shun; Li, Yonglian; Zheng, Xi; Zhang, Kun

doi:10.1039/c9md00345b

Cited by 12 publications

(6 citation statements)

References 32 publications

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“…Fenamates have also been shown to inhibit calcium influx in isolated mitochondria and polymorphonuclear leukocytes [ 38 ], offering improvement in various disorders characterized by pain and inflammation [ 39 , 40 ]. Furthermore, when co-administered with other anti-inflammatory and cellular protective molecules, it has been proven to offer synergistic anti-inflammatory effects [ 41 ]. This may be the case with both compounds 2 and 3 that have almost a 2.5- and 1.5-fold increased anti-inflammatory activity, respectively, compared with the parent acid.…”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis and Evaluation of Antioxidant and NSAID Derivatives with Antioxidant, Anti-Inflammatory and Plasma Lipid Lowering Effects

Theodosis-Nobelos,

Marc,

Rekka

2024

Molecules

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Amides containing methyl esters of γ-aminobutyric acid (GABA), L-proline and L-tyrosine, and esters containing 3-(pyridin-3-yl)propan-1-ol were synthesized by conjugation with 3,5-di-tert-butyl-4-hydroxybenzoic, an NSAID (tolfenamic acid), or 3-phenylacrylic (cinnamic, (E)-3-(3,4-dimethoxyphenyl)acrylic and caffeic) acids. The rationale for the conjugation of such moieties was based on the design of structures with two or more molecular characteristics. The novel compounds were tested for their antioxidant, anti-inflammatory and hypolipidemic properties. Several compounds were potent antioxidants, comparable to the well-known antioxidant, Trolox. In addition, the radical scavenging activity of compound 6 reached levels that were slightly better than that of Trolox. All the tested compounds demonstrated remarkable activity in the reduction in carrageenan-induced rat paw edema, up to 59% (compound 2, a dual antioxidant and anti-inflammatory molecule, with almost 2.5-times higher activity in this experiment than the parent NSAID). Additionally, the compounds caused a significant decrease in the plasma lipidemic indices in Triton-induced hyperlipidemic rats. Compound 2 decreased total cholesterol by 75.1% and compound 3 decreased triglycerides by 79.3% at 150 μmol/kg (i.p.). The hypocholesterolemic effect of the compounds was comparable to that of simvastatin, a well-known hypocholesterolemic drug. Additionally, all compounds lowered blood triglycerides. The synthesized compounds with multiple activities, as designed, may be useful as potential candidates for conditions involving inflammation, lipidemic deregulation and oxygen toxicity.

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Section: Resultsmentioning

confidence: 99%

Design, Synthesis and Evaluation of Antioxidant and NSAID Derivatives with Antioxidant, Anti-Inflammatory and Plasma Lipid Lowering Effects

Theodosis-Nobelos,

Marc,

Rekka

2024

Molecules

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“…The possible topical anti-inflammatory role of KXRG on skin was examined using an acute ear edema mouse model, in which edema was induced by TPA application in Balb/c mice [ 19 ]. As shown in Figure 3 , the skin thickness started to increase significantly at 3 h after TPA treatment, and reached a maximum at 5 h, which lasted for at least 24 h. Indomethacin pretreatment significantly reduced the TPA-mediated ear edema by 26%.…”

Section: Resultsmentioning

confidence: 99%

Tea Seed Kaempferol Triglycoside Attenuates LPS-Induced Systemic Inflammation and Ameliorates Cognitive Impairments in a Mouse Model

et al. 2022

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(1) Background: The current research intended to obtain functional compounds from agricultural by-products. A functional tea seed flavonoid, kaempferol-3-O-[2-O-β-d-xylopyranosyl-6-O-α-L-rhanmopyranosyl]-β-d-glucopyranoside (KXRG), was isolated from tea seed dregs. We further determined its chemical structure and evaluated the protective effects of KXRG against local and systemic inflammation in vivo; (2) Methods: First, cytotoxicity and proinflammatory cytokine release were examined in a cell-culture system. The biological activities of KXRG were investigated in a mouse model of ear edema, and from inflammatory damage to organs as demonstrated by histologic examination, in addition to brain function evaluation using the Y-maze test. Serum biochemical analysis and western blotting were utilized to explore the related cellular factors; (3) Results: KXRG inhibited IL-6 in RAW264.7 cells at a non-toxic concentration. Further experiments confirmed that KXRG exerted a stronger effect than indomethacin in terms of the prevention of 12-O-tetradecanoylphorbol acetate (TPA)-induced ear inflammation in a mouse model. KXRG feeding significantly prevented LPS-induced small intestine, liver, and kidney inflammatory damage, as demonstrated by histologic examination. KXRG also significantly improved LPS-induced cognitive impairments. Serum biochemical analysis showed that KXRG elevated antioxidant capacity and reduced levels of proinflammatory cytokines. Western blotting revealed that KXRG reduced the COX-2 expression induced by LPS in mouse tissues; (4) Conclusions: KXRG can be purified from agricultural waste, and hence it is inexpensive, with large amounts of raw materials available. Thus, KXRG has strong potential for further development as a wide-use anti-systemic inflammation drug to prevent human disease.

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“…Inflammation was accompanied by production of inflammatory cytokines, such as TNF-α, IL-6, and COX-2, which can all be activated by TPA ( 49 , 50 ). Expression of inflammatory cytokines is a biomarker indicating severity of inflammation.…”

Section: Resultsmentioning

confidence: 99%

Essential oils of Zingiber officinale: Chemical composition, in vivo alleviation effects on TPA induced ear swelling in mice and in vitro bioactivities

Zhang

Zhang²,

Yu³

et al. 2022

Front. Nutr.

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Zingiber officinale (ZO) is a traditional food condiment. The essential oils of Z. officinale (ZOEOs) are known to have multiple bioactivities. In this study, gas chromatography mass spectrometer (GC-MS) analytical method was used to identify active ingredient present in ZOEOs. A total of 41 compounds were identified in ZOEOs. Major components in ZOEOs were zingiberene (19.71%), (+)-β-cedrene (12.85%), farnesene (12.17%), α-curcumene (10.18%) and β-elemene (3.54%). Experimental results of 12-O-tetradecanoylphorbol-13 acetate (TPA) induced ear swelling validation mice model showed that ZOEOs treatment has better anti-inflammatory effect compared with ibuprofen (positive control) at high concentrations. Histological and immunohistochemical analysis showed that ZOEOs significantly decreased COX-2, IL-6 and NF-κB expression in a dose dependent manner. The mRNA levels of COX-2 and NF-κB were also down regulated by the application of ZOEOs. This indicated that ZOEOs exhibited positive effects in ear skin protection. Antibacterial experimental results showed that EOZOs had anti-bacterial effects on Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. DPPH radical scavenging, A549 cell line and LNCaP cell line inhibition results indicated that ZOEOs exhibited potential antioxidant and anti-tumor properties. The findings of these study provide scientific basis on therapeutic use of ZO in food, cosmetic and pharmaceutical industries.

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Synergistic effect of tolfenamic acid and glycyrrhizic acid on TPA-induced skin inflammation in mice

Abstract: Combinational use of tolfenamic acid and glycyrrhizic acid has importantly enhanced influences on treating inflammatory skin diseases.

Cited by 12 publications

References 32 publications

Design, Synthesis and Evaluation of Antioxidant and NSAID Derivatives with Antioxidant, Anti-Inflammatory and Plasma Lipid Lowering Effects

Design, Synthesis and Evaluation of Antioxidant and NSAID Derivatives with Antioxidant, Anti-Inflammatory and Plasma Lipid Lowering Effects

Tea Seed Kaempferol Triglycoside Attenuates LPS-Induced Systemic Inflammation and Ameliorates Cognitive Impairments in a Mouse Model

Essential oils of Zingiber officinale: Chemical composition, in vivo alleviation effects on TPA induced ear swelling in mice and in vitro bioactivities

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