Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL[1]. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM[2].
4-Chlorocinnamic acid has inhibitory effects on tyrosinase. 4-Chlorocinnamic acid has antibacterial activity. 4-Chlorocinnamic acid also inhibits Colletotrichum gloeosporioides growth[1][2][3].
4-Butylresorcinol is a phenol derivative which can inhibit tyrosinase with IC50 of 11.27 μM.
Mulberroside A, the major active anti-tyrosinase compound in the root bark extract of Morus alba L. (Moraceae), is widely employed as an active ingredient in whitening cosmetics. IC50 value: 1.29 μmol/L (inhibition of the monophenolase activity); KI value: 0.385 μmol/L (the inhibition constant of the effectors on tyrosinase); KIS value: 0.177 μmol/L (the inhibition constant of the enzyme-substrate complex) [3] Target:In vitro: Mulberroside A decreased the expressions of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6 and inhibited 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 exhibiting anti-inflammatory antiapoptotic effects [1]. Mulberroside A treatment significantly decreased the mRNA and protein expression of P-gp in Caco-2 cells after treatment with Mulberroside A (5–20 μM). PKC and NF-κB might play crucial roles in Mulberroside A-induced suppression of P-gp [2]. In vivo:
Tyrosinase-IN-16 (compound 19a) is a tyrosine kinase (Tyrosinase) inhibitor with Ki=470 nM. Tyrosinase-IN-16 is cytotoxic to B16F10 cells, with >90% inhibition at 20 μM[1].
Viscumneoside III, a dihydroflavone O-glycoside, is a potent tyrosinase inhibitor with an IC50 of 0.5 mM. Viscumneoside III has anti-angina pectoris[1].
Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 is a melanotropin, a melanocyte-stimulating hormone. Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 stimulates tyrosinase and exhibits thermoregulatory effect in rats model[1][2].
Mulberroside F is one of the main bioactive constituents in mulberry (Morus alba L.)[1]. Mulberroside F shows inhibitory effects on tyrosinase activity and on the melanin formation. Mulberroside F also exhibits superoxide scavenging activity that is involved in the protection against auto-oxidation[2].
2,3-Dihydroisoginkgetin, a biflavonoid, is a inhibitor of Tyrosinase, with 36.84% inhibition at 0.1 mM. 2,3-Dihydroisoginkgetin shows less toxicity in HEMn (human epidermal melanocytes) cells, with an IC50 of 86.16 μM[1].
5-Feruloylquinic acid (5-FQA) possesses antioxidative effects and tyrosinase inhibitory activities[1].
Glycolic Acid is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity[1].
2-Ketoglutaric acid calcium (Alpha-Ketoglutaric acid calcium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid calcium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid calcium is a reversible inhibitor of tyrosinase (IC50=15 mM)[1][2].
Tyrosinase (Polyphenol oxidase) is a rate-limiting enzyme that controls the production of melanin and is encoded by TYR gene. Tyrosinase is mainly found in melanosomes synthesized by skin melanocytes[1].
(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM[1].
Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM.
Tyrosinase-IN-17 (Compound 5b) is a lipophilic, skin-permeable, and non-cytotoxic Tyrosinase inhibitor (pIC50=4.99). Tyrosinase-IN-17 can be used for research on melanin-related diseases, such as melanoma, melanogenesis, etc[1].
Tyrosinase-IN-10 (Compound 23) is a partially competitive tyrosinase inhibitor with an IC50 of 1.6 μM against tyrosinase activity from human melanoma cell lysates[1].
Flanvotumab (IMC-20D7S) is a human monoclonal antibody targeting to tyrosinase-related protein (TYRP1), specifically expressed in melanocytes and melanoma cells. Flanvotumab acts function via natural killing-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Flanvotumab has potent anti-tumor activity and good tolerance[1].
Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities[1][2][3].
Tyrosinase-IN-11 is a potent tyrosinase inhibitor with IC50s of 50 nM and 64 nM for L-tyrosinase and L-dopa, respectively. Tyrosinase-IN-11 has significant antioxidant activity and low cytotoxicity. Tyrosinase-IN-11 has the potential for skin hyperpigmentation research[1].
2-Ketoglutaric acid-13C5 is the 13C labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
Kojic acid dipalmitate (Kojic dipalmitate) is a derivative of Kojic acid (HY-W050154), a fungal metabolite that can be produced by species of Aspergillus, Acetobacter and Penicillium. Kojic acid dipalmitate is a slow and reversible competitive inhibitor of tyrosinase. Kojic acid dipalmitate can be used for skin‐lightening agent research[1].
Chetoseminudin B possesses mushroom tyrosinase inhibitory activity with IC50 of 31.7 μM[1].
Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinase inhibitory activity with an IC50 of 506 μM[1]. Trifolirhizin exhibits potential anti-inflammatory and anticancer activities[2].
Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research[1][21][3].
Dihydroaltenuene B is a potent mushroom tyrosinase inhibitor with an IC50 of 38.33 µM. Dihydroaltenuene B shows the hydrogen bonding interactions between the 3-OH and 4’-OH and the His244, Met280 and Gly281 residues of tyrosinase[1].
Obtusifolin-2-O-glucoside (compound 7) is a Tyrosinase inhibitor (IC50=9.2 μM). Obtusifolin-2-O-glucoside can be isolated from cassia seed[1].
Broussonin C is a competitive inhibitor of Tyrosinase that can be isolated from Broussonetia kazinoki. Broussonin C inhibits monophenolase and diphenolase with IC50s of 0.43 and 0.57 μM, respectively[1].
Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) is a potent, non-competitive tyrosinase inhibitor with an IC50 value of 49.33 ± 2.64 µM and Ki value of 31.25 ± 0.25 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) have the highest radical scavenging activity to reduce the production of reactive oxygen species (ROS) with an IC50 value of 25.39 ± 0.77 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) can be used for anti-browning substances in the food and agricultural sectors[1].