tyrosinase

Tyrosinase (Polyphenol oxidase) is a key rate-limiting enzyme encoded by the TYR gene that controls melanin production and catalyzes tyrosine oxidation. It is mainly found in melanosomes and plays an important role in melanogenesis, plant secondary metabolism, wound healing and immune response.

Tyrosinase-IN-2 (compound 67) is a potent inhibitor of tyrosinase, a copper-containing metalloenzyme crucial for the rate-limiting step in melanin biosynthesis and enzymatic browning processes. This compound shows promise for research into skin whitening agents and food preservatives [1].

3-O-Ethyl-L-ascorbic acid is a cosmetic tyrosinase inhibitor with whitening ability and is a stabilized vitamin C derivative. It also has antioxidant properties.

Monobenzone (Benoquin) is a Depigmenting Agent. The mechanism of action of monobenzone is as a Melanin Synthesis Inhibitor. The physiologic effect of monobenzone is by means of Depigmenting Activity.

Potassium iodide is used as the treatment of overactive thyroid and as protection of the thyroid gland from the influences of radiation from swallowed or inhaled radioactive iodine. It may be used after accidental exposure to radioactive iodine or before and after administration of medicine containing radioactive iodine.

2-Ketoglutaric acid is a key molecule in the tricarboxylic acid cycle,is also connected to glutamic acid and glutamine metabolisms through the transamination reactions.

Tyrosinase-IN-19 (compound 9), a competitive tyrosinase inhibitor, exhibits potent antioxidant activities by neutralizing ROS, ABTS+, and DPPH radicals and demonstrates dose-dependent suppression of tyrosinase expression [1].

Tyrosinase-IN-15 (Compound 39), with an IC50 of 7.12 μM and a Ki of 11.8 μM, functions as a tyrosinase inhibitor [1].

Viscumneoside III, a dihydroflavone O-glycoside, is a potent tyrosinase inhibitor with an IC50 of 0.5 mM, and has anti-angina pectoris properties.

Isosilybin A is a partial PPARγ agonist, it significantly induced ABCA1 protein expression, it inhibited both monophenolase (IC50=1.7-7.6μM) and diphenolase (IC50=12.1-44.9μM) of tyrosinase. Isosilybin A shows anti-angiogenic efficacy, it has anti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction.

Tyrosinase-IN-14 (compound 7m), a tyrosinase inhibitor, modulates the enzyme's secondary structure to diminish its catalytic function, exhibits low cytotoxicity, and possesses anti-browning properties that effectively prevent banana discoloration during storage [1].

Tyrosinase-IN-40 (Compound 9r) is a competitive inhibitor of tyrosinase, boasting an IC50 value of 17.02 µM and a Ki value of 14.87 µM. This compound also exhibits antioxidant activity and can be utilized in studies related to melanin.

Tyrosinase-IN-37 (Compound 3c) is a potent inhibitor of tyrosinase, with an IC50 value of 1.02 μM, which is 14 times more effective than kojic acid (IC50 of 14.74 μM). This compound effectively prevents the browning of Rosa roxburghii and can also inhibit browning not caused by tyrosinase.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

1. Mulberroside has nephroprotective, hypoglycemic, and antidiabetic effects. 2. Mulberroside A is a glycosylated stilbene of oxyresveratrol; thus, the deglycosylation of Mulberroside A resulted in enhanced inhibition of melanogenesis. 3. Mulberroside A has anti-inflammatory antiapoptotic effects. by decreasing the expressions of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6 and inhibiting the activation of NALP3, caspase-1, and nuclear factor-κB and the phosphorylation of extracellular signal-regulated protein kinases, the c-Jun N-terminal kinase, and p38.

Trans-caffeic acid stearyl ester is posited to inhibit melanogenesis signaling while suppressing cAMP levels and, subsequently, MC1R, MITF, tyrosinase, TRP-2 and TRP-1 down-regulation, resulting in the suppression of tyrosinase activity, DOPA oxidase activity and melanin synthesis.

Tyrosinase-IN-13 (compound 3c), derived from Flurbiprofen, serves as a potent non-competitive inhibitor of tyrosinase with IC50 and Ki values of 68 μM and 36.3 μM, respectively. It exhibits cytotoxicity against several cancer cell lines, including hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) [1].

hTYR AbTYR-IN-1 is a dual hTYR AbTYR inhibitor with inhibitory effects on hTYR and AbTYR, with IC50s of 5.4 μM and 3.52 μM, respectively. hTYR AbTYR-IN-1 can be used for the study of hyperpigmentation and melanoma in humans.

Tyrosinase-IN-12(Non-competitive tyrosinase inhibitor) is a potent non-competitive tyrosinase inhibitor with an IC50 of 49.33 ± 2.64 µM and a Ki of 31.25 ± 0.25 µM. Tyrosinase-IN-12 has significant antioxidant and free radical scavenging activity (IC50:25.39 ± 0.77 µM), reducing reactive oxygen species (ROS) production. Tyrosinase inhibitor (Tyrosinase-IN-12) has significant antioxidant and free radical scavenging activity and reduces the production of reactive oxygen species (ROS) (IC50:25.39 ± 0.77 µM).Tyrosinase-IN-12 can be used for the study of browning of substances in food and fruits.

Tyrosinase-IN-36 is a moderately potent inhibitor of tyrosine, exhibiting an inhibition percentage of 42.75% compared to kojic acid at a concentration of 100 μM and possesses antioxidant activity.

Tyrosinase-IN-39 (compound 5r) is a competitive inhibitor of tyrosinase, with an IC50 of 6.4 μM, and is used in the study of skin diseases.

Tyrosinase-IN-33 (compound 5), a pyridine-based compound, acts as an effective inhibitor of diphenolase activity in mushroom tyrosinase. It significantly reduces enzyme activity with an IC50 of 9.0 μM.

Tyrosinase-IN-38 (compound 6b) is a competitive inhibitor of tyrosinase, demonstrating an IC50 of 25.82 μM and exhibits antioxidant activity.

Tyrosinase-IN-35 (compound 6g), exhibiting a IC 50 value of 2.09 μM, serves as a more effective inhibitor of human tyrosinase compared to Kojic Acid (IC 50: 16.38 μM). At concentrations of 4 μM and 8 μM, this compound effectively lowers melanin levels in melanoma B16F10 cells in vitro.