An article Hydroxyl substituted benzoic acid/cinnamic acid derivatives: Tyrosinase inhibitory kinetics, anti-melanogenic activity and molecular docking studies WOS:000499694600003 published article about VANILLIC ACID; CINNAMIC ACID; L-DOPA; MUSHROOM; MECHANISM; ANTIOXIDANT; PROLIFERATION; PIGMENTATION; ANALOGS in [Nazir, Yasir; Zuegg, Johannes; Cooper, Matthew A.; Blaskovich, Mark A. T.; Ziora, Zyta M.] Univ Queensland, Inst Mol Biosci, St Lucia, Qld 4072, Australia; [Nazir, Yasir; Ashraf, Zaman] Allama Iqbal Open Univ, Dept Chem, Islamabad 44000, Pakistan; [Saeed, Aamer] Quaid i Azam Univ, Dept Chem, Islamabad 45320, Pakistan; [Rafiq, Muhammad] Cholistan Univ Vet & Anim Sci, Dept Physiol & Biochem, Bahawalpur, Pakistan; [Afzal, Samina] Bahauddin Zakria Univ, Fac Pharm, Multan 60800, Pakistan; [Ali, Anser] Mirpur Univ Sci & Technol, Dept Zool, Mirpur 10250, Ajk, Pakistan; [Latif, Muhammad] Taibah Univ, Coll Med, CGID, Al Madinah Al Munawwarah, Saudi Arabia; [Hussein, Waleed M.; Barnard, Ross T.] Univ Queensland, SCMB, St Lucia, Qld 4072, Australia; [Hussein, Waleed M.; Barnard, Ross T.] Univ Queensland, ARC Training Ctr Biopharmaceut Innovat, St Lucia, Qld 4072, Australia; [Hussein, Waleed M.] Helwan Univ, Fac Pharm, Pharmaceut Organ Chem Dept, Einhelwan, Helwan, Egypt; [Fercher, Christian] Univ Queensland, Australian Inst Bioengn & Nanotechnol, St Lucia, Qld 4072, Australia in 2020.0, Cited 47.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6. Recommanded Product: 150-19-6
The inhibition of tyrosinase is an established strategy for treating hyperpigmentation. Our previous findings demonstrated that cinnamic acid and benzoic acid scaffolds can be effective tyrosinase inhibitors with low toxicity. The hydroxyl substituted benzoic and cinnamic acid moieties of these precursors were incorporated into new chemotypes that displayed in vitro inhibitory effect against mushroom tyrosinase. The most active compound, (2-(3-methoxyphenoxy)-2-oxoethyl (E)-3-(4-hydroxyphenyl) acrylate) 6c, inhibited tyrosinase with an IC50 of 5.7 mu M, while (2-(3-methoxyphenoxy)-2-oxoethyl 2, 4-dihydroxybenzoate) 4d had an IC50 of 23.8 mu M. In comparison, the positive control, kojic acid showed tyrosinase inhibition with an IC50 = 16.7 mu M. Analysis of enzyme kinetics revealed that 6c and 4d displayed noncompetitive reversible inhibition of the second tyrosinase enzymatic reaction with K-i values of 11 mu M and 130 mu M respectively. In silico docking studies with mushroom tyrosinase (PDB ID 2Y9X) predicted possible binding modes in the catalytic site for these active compounds. The phenolic para-hydroxy group of the most active compound 6c is predicted to interact with the catalytic site Cu++ ion. The methoxy part of this compound is predicted to form a hydrogen bond with Arg 268. Compound 6c had no observable toxic effects on cell morphology or cell viability at the highest tested concentration of 91.4 mu M. When dosed at 91.4 mu M onto B16F10 melanoma cells in vitro 6c showed anti-melanogenic effects equivalent to kojic acid at 880 mu M. 6c displayed no PAINS (pan-assay interference compounds) alerts. Our results show that compound 6c is a more potent tyrosinase inhibitor than kojic acid and is a candidate for further development. Our exposition of the details of the interactions between 6c and the catalytic pocket of tyrosinase provides a basis for rational design of additional potent inhibitors of tyrosinase, built on the cinnamic acid scaffold.
Recommanded Product: 150-19-6. Welcome to talk about 150-19-6, If you have any questions, you can contact Nazir, Y; Saeed, A; Rafiq, M; Afzal, S; Ali, A; Latif, M; Zuegg, J; Hussein, WM; Fercher, C; Barnard, RT; Cooper, MA; Blaskovich, MAT; Ashraf, Z; Ziora, ZM or send Email.
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles