The Impact of a Quinone Scaffold on Thermo-TRPs Modulation by Dimethylheptyl Phytocannabinoids

International Journal of Molecular Sciences, Journal Year: 2025, Volume and Issue: 26(6), P. 2682 - 2682

Published: March 17, 2025

Phytocannabinoids (pCBs) from Cannabis sativa represent an important class of bioactive molecules, potentially useful for the treatment a wide range diseases. Their efficacy is due to their ability interact with multiple targets endocannabinoid system, including thermosensitive transient receptor potential (Thermo-TRPs), namely TRPV1-4, TRPA1, and TRPM8 channels. Previously, we demonstrated shift in selectivity toward TRPA1 activity profile main pCBs, that is, CBD, ∆8-THC, CBG, CBC, CBN, by swapping pentyl chain α,α-dimethylheptyl (DMH) one. Using these derivatives as starting point, here investigate effects on thermo-TRPs integration quinone group into resorcinol scaffold. We found that, while substantially retained, increase potency/efficacy TRPV3 modulation observed. Docking studies were used elucidate binding modes most active compounds this receptor, providing rationale biological activity. In summary, show DMH-pCBs are endowed TRPA1/TRPV3 desensitizing activity, skin diseases sustained inflammatory conditions.

Language: Английский

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Sıçanlarda Etanol ile İndüklenen Gastrik Ülser Modelinde Idebenon ve Krisinin Koruyucu Etkileri

Deleted Journal, Journal Year: 2025, Volume and Issue: 5(1), P. 30 - 37

Published: Jan. 17, 2025

Bu çalışmada, sıçanlarda etanol ile indüklenen gastrik ülsere karşı idebenon ve krisinin koruyucu etkileri araştırılmıştır. Yirmi sekiz Sprague-Dawley erkek sıçan dört gruba ayrılmıştır: 1 ml serum fizyolojik alan kontrol grubu, ülser indüklemek için (ET) (5 ml/kg) ET grubu iki tedavi grubu; biri ET'yi takiben (200 mg/kg), diğeri krisin (100 mg/kg) gruplar. Tedaviler oral gavaj yoluyla uygulanmıştır. Gastrik mukozal hasarı tedavilerin mekanizmasını değerlendirmek için, somatostatin aquaporin-1 düzeylerine odaklanan histopatolojik incelemeler immünohistokimyasal analizler gerçekleştirilmiştir. Histopatolojik incelemelerde, muamele edilen grupta şiddetli dejeneratif nekrotik değişiklikler gözlenmiştir. Sonuçlar, gruplarında hasarın grubuna kıyasla önemli ölçüde azaldığını lezyonların şiddetinde anlamlı bir azalma olduğunu göstermiştir. Kantitatif analiz, ekspresyonunda artış ortaya koymuştur (P < 0,05), bu da artmış savunmayı göstermektedir. İdebenon krisinin, ülserlerde azalttığı ekspresyonunu artırdığı bulunmuştur. Nekrotik lezyonlardaki savunma mekanizmalarının güçlenmesi, ülserlerin önlenmesi tedavisi terapötik potansiyel sunabileceğini düşündürmektedir.

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Toxicity profiling and HR-LCMS analysis of Indigofera longiracemosa leaf methanolic extract exhibiting anti-inflammatory activity

3 Biotech, Journal Year: 2025, Volume and Issue: 15(6)

Published: May 9, 2025

Language: Английский

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Insight into the Antioxidant Activity of 1,8-Dihydroxynaphthalene Allomelanin Nanoparticles

Antioxidants, Journal Year: 2023, Volume and Issue: 12(8), P. 1511 - 1511

Published: July 28, 2023

Melanins are stable and non-toxic pigments with great potential as chemopreventive agents against oxidative stress for medical cosmetic applications. Allomelanin is a class of nitrogen-free melanin often found in fungi. The artificial allomelanin obtained by the polymerization 1,8-dihydroxynaphthalene (DHN), poly-DHN (PDHN), has been recently indicated better radical quencher than polydopamine (PDA), model dopamine (DA); however, chemical mechanisms underlying this difference unclear. Here we investigate, experimental theoretical methods, ability PDHN nanoparticles (PDHN-NP), comparison to PDA-NP, trap alkylperoxyl (ROO•) hydroperoxyl (HOO•) radicals that involved propagation peroxidation real conditions. Our results demonstrate PDHN-NP present higher antioxidant efficiency respect PDA-NP ROO• water at pH 7.4 mixed HOO• acetonitrile, showing catalytic cross-termination activity. capacity 0.8 mmol/g (ROO• quenched 1 g PDHN-NP), rate constant 3 × 105 M−1 s−1 each reactive moiety. Quantum-mechanical calculations revealed that, thanks formation H-bond network, quinones have high affinity H-atoms, thus justifying reactivity observed experimentally.

Language: Английский

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Pyrroloquinoline Quinone (PQQ): Exploring its Impact on Human Health and Potential Benefits

Current Research in Food Science, Journal Year: 2024, Volume and Issue: 9, P. 100889 - 100889

Published: Jan. 1, 2024

Language: Английский

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