Scutellarein attenuates atopic dermatitis by selectively inhibiting transient receptor potential vanilloid 3 channels was written by Wang, Yujing;Tan, Liaoxi;Jiao, Kejun;Xue, Chu;Tang, Qinglian;Jiang, Shan;Ren, Younan;Chen, Hao;El-Aziz, Tarek Mohamed Abd;Abdelazeem, Khalid N. M.;Yu, Ye;Zhao, Fang;Zhu, Michael X.;Cao, Zhengyu. And the article was included in British Journal of Pharmacology in 2022.HPLC of Formula: 499-75-2 This article mentions the following:
Background and Purpose : Atopic dermatitis (AD) is one of the most common chronic inflammatory cutaneous diseases with unmet clin. needs. As a common ingredient found in several medicinal herbs with efficacy on cutaneous inflammatory diseases, Scutellarein (Scu) has been shown to possess anti-inflammatory and anti-proliferative activities. We aimed to evaluate the therapeutic efficacy of Scu against AD and its underlying mol. mechanism. Exptl. Approach : Efficacy of Scu on AD was evaluated in 2,4-dinitrofluorobenzene (DNFB) and carvacrol-induced dermatitis mouse models. Cytokine mRNA and serum IgE levels were examined using qPCR and ELISA, resp. Voltage clamp recordings were used to measure currents mediated by transient receptor potential (TRP) channels. In silico docking, site-direct mutagenesis, and covalent modification were used to explore the binding pocket of Scu on TRPV3. Key Results : S.c. administration of Scu efficaciously suppresses DNFB and carvacrol-induced pruritus, epidermal hyperplasia and skin inflammation in wild type mice but has no addnl. benefit in Trpv3 knockout mice in the carvacrol model. Scu is a potent and selective TRPV3 channel allosteric neg. modulator with an apparent affinity of 1.18 μM. Mol. docking coupled with site-direct mutagenesis and covalent modification of incorporated cysteine residues demonstrate that Scu targets the cavity formed between the pore helix and transmembrane helix S6. Moreover, Scu attenuates endogenous TRPV3 activity in human keratinocytes and inhibits carvacrol-induced proliferative and proinflammatory responses. Conclusion and Implications : Collectively, these data demonstrate that Scu ameliorates carvacrol-induced skin inflammation by directly inhibiting TRPV3, and TRPV3 represents a viable therapeutic target for AD treatment. In the experiment, the researchers used many compounds, for example, 5-Isopropyl-2-methylphenol (cas: 499-75-2HPLC of Formula: 499-75-2).
5-Isopropyl-2-methylphenol (cas: 499-75-2) belongs to alcohols. Alkyl halides are often synthesized from alcohols, in effect substituting a halogen atom for the hydroxyl group. Alcohols may be oxidized to give ketones, aldehydes, and carboxylic acids. These functional groups are useful for further reactions. Oxidation of organic compounds generally increases the number of bonds from carbon to oxygen (or another electronegative element, such as a halogen), and it may decrease the number of bonds to hydrogen.HPLC of Formula: 499-75-2
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