3-Hydroxycoumarin
3-Hydroxycoumarin as a new matrix for matrix-assisted laser desorption/Ionization time-of-flight mass spectrometry of DNA. It shows strong inhibiting ability against recombinant human tyrosinase. 3-Hydroxyscopoletin and 3-hydroxyumbelliferone have a high inhibitory potency for 5-lipoxygenase and for α-D-glucosidase respectively, they serve as lead compounds for new drugs.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Biochemical & Biophysical Research Communications, 1990, 168(1):169-175.
3-Hydroxycoumarins: First direct preparation from coumarins using a Cu2+-ascorbic acid-O2 system, and their potent bioactivities.[Reference:
WebLink]
METHODS AND RESULTS:
First direct 3-hydroxylation of a coumarin ring via a purely chemical system, previously only possible using cytochrome P-450, was successfully conducted by a Cu 2+-ascorbic acid-O 2 system; the two 3-Hydroxycoumarins obtained were novel compounds, 3-hydroxyscopoletin and 3-hydroxyisoscopoletin. 5-Lipoxygenase and α-D-glucosidase inhibitory activities of coumarins greatly increased through 3-hydroxylation.
CONCLUSIONS:
3-Hydroxyscopoletin and 3-hydroxyumbelliferone had a high inhibitory potency for 5-lipoxygenase and for α-D-glucosidase respectively; they serve as lead compounds for new drugs.
Colloids & Surfaces B Biointerfaces, 2018, 171:675-681.
3-Hydroxycoumarin Loaded Vesicles for Recombinant Human Tyrosinase Inhibition in Topical Applications.[Reference:
WebLink]
Tyrosinase is one of the key enzymes in mammalian melanin biosynthesis. Decreasing tyrosinase activity has been targeted for the prevention of conditions related to the hyperpigmentation of the skin, such as melasma and age spots. This paper is devoted to the engineering of vesicle formulations loaded with 3-Hydroxycoumarin for topical pharmaceutical applications.
METHODS AND RESULTS:
At first, it was demonstrated the strong inhibiting ability of
3-Hydroxycoumarin against recombinant human tyrosinase. Then, such a drug was effectively encapsulated within liquid or gel-like vesicle formulations, both based on monoolein and lauroylcholine chloride. In vitro skin penetration and permeation studies proved these formulations efficiently overcome the barrier represented by the stratum corneum, delivering 3-Hydroxycoumarin to the deeper skin layers. The effect of applying for different times the liquid and the gel formulation was also evaluated. Results revealed that application of the gel formulation for 2 h favored the drug accumulation into the skin with low transdermal delivery, thus indicating this combination of administration time and formulation as ideal to locally inhibit tyrosinase activity with minimal systemic absorption. Moreover, when incubated with B16F10 melanoma cells, the liquid vesicle formulations did not show cytotoxic activity.
Journal of the American Society for Mass Spectrometry, 2007, 17(12):1665-1668.
3-Hydroxycoumarin as a New Matrix for Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Mass Spectrometry of DNA[Reference:
WebLink]
METHODS AND RESULTS:
3-Hydroxycoumarin (3-HC) was designed, synthesized, and tested as a matrix for matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) analyses of a variety of synthetic oligodeoxynucleotides ranging long from three to 70 bases. Using the matrix solution of 3-HC dissolved in a mixed solvent of acetone and diammonium hydrogen citrate, DNA segments over the mass range 800 Da to 6900 Da were isotopically resolved with high signal-to-noise (S/N) ratio. The individual isotopic molecular ion peaks of a group of 23-mer mixed-base oligomers differing by one or two bases with mass differences of 9 or 7 Da were recorded. Larger oligodeoxynucleotide segments of 34-mer, 50-mer, and 70-mer have also been analyzed effectively. Less than 250 attomol of a 10-mer DNA segment was clearly detected without any fragmentation.
The new matrix can be used for the analysis of DNA segments in both positive- and negative-ion modes, and the quality of all negative-ion mode spectra are as good as that obtained in positive-ion mode shown in this paper.
CONCLUSIONS:
Compared with conventional matrices of 3-hydroxypicolinic acid (3-HPA) and 6-aza-2-thiothymine (ATT), 3-HC had noticeable improvement in resolution, S/N ratio, spot-to-spot-, and sample-to-sample reproducibility for analyzed DNA segments.
