Depigmenting activity and low cytotoxicity of alkoxy benzoates or alkoxy cinnamte in cultured melanocytes

To obtain effective and safe topical depigmenting agents, we synthesized hydroxybenzoates, alkoxybenzoates, and 3,4,5-trimethoxycinnamate containing a thymol moiety and screened then for high-level inhibitory activity against melanin synthesis in cultured melanocytes. Eight compounds were tested for their depigmenting effect and cytotoxicity using a murine melanocyte cell line. We found that 3,4,5-trialkoxybenzoates and 3,4,5-trimethoxycinnamate, synthesized by conjugating 3,4,5-trialkoxybenzoic acids and 3,4,5-trimethoxycinnmic acid with thymol, showed a potent depigmenting effect and low cytotoxicity. Compound 4h, 5-methyl-2-(methylethyl)phenyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate, showed the most potent depigmenting effect (IC50=10 microM) with low cytotoxicity (IC50=200 microM).     

The Greatest Lower Bound of a Boros–Moll Sequence

Mathematical Notes - The Boros–Moll polynomials $$P_m(a)$$ arise in the evaluation of a quartic integral. In the past few years, there has been some remarkable research on the properties of...     

An efficient preparation of novel 5-fluoropyrazolin-3-one derivatives from α-trifluoromethylated α-arylacetates

The reactions of α-trifluoromethylated α-arylacetates 1 with 3 equiv of hydrazine, methylhydrazine or benzylhydrazine in 1,4-dioxane at reflux for 24 h afforded the corresponding 5-fluoropyrazolin-3-one derivatives 3a-m in high yields. Similarly, treatment of 1 with 3 equiv of PhNLiNH₂ in THF at −78 °C, followed by warming to room temperature, resulted in the formation of 3n-s in high yields.     

Antibacterial activities of polystyrene-block-poly(4-vinyl pyridine) and poly(styrene-random-4-vinyl pyridine)

Styrene was polymerized in the presence of benzoyl peroxide (BPO) and 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO) to yield polystyrene-TEMPO (PS-TEMPO) macroinitiator. The PS-TEMPO macroinitiator with different molecular weight was reacted with 4-vinyl pyridine (4-VP) to synthesize polystyrene-block-poly(4-vinyl pyridine) (PS-b-PVP), which was then quaternized with n-octyl iodide. Antibacterial activity of the quaternized copolymers was assessed against a gram negative bacterium (Pseudomonas aeruginosa) and a gram positive one (Staphylococcus aureus) by using the shake flask test method, and the results were compared with those of poly(styrene-random-4-vinyl pyridine) (P(ST-r--VP)). The quaternized copolymers inhibited greatly the growth of the bacteria, and PS-b-PVP was more active than P(ST-r-VP), which was ascribed to the fact that the content of quaternized 4-VP units on the surface of the particles of the former copolymer was higher than that corresponding to the latter one.     

负载型贵金属催化剂的硫中毒机理——载体的酸碱性与催化剂抗硫性能的关系

以H_2S为毒物,H_2-O_2反应为催化模型反应,制备并考察了一系列不同酸碱性的负载型钯催化剂。以NH_3和吡啶为探针分子,用程序升温脱附(TPD)或红外光谱法测定了催化剂的酸碱性。用交替脉冲微反色谱技术评价了催化剂的活性和耐硫中毒性,并对催化剂的耐硫性能和载体酸碱性进行关联和解释。在以上研究基础上,指出了提高催化剂抗硫性能的途径。     

The structure of new lignans from the seeds of phytolacca americana

From the seeds of Phytolacca americana two new lignans, Americanin B and D, have been isolated and their structures elucidated mainly by spectroscopic methods     

SPECTROSCOPIC STUDIES OF CUTANEOUS PHOTOSENSITIZING AGENTS–XV. ANTHRALIN and ITS OXIDATION PRODUCT 1,8-DIHYDROXYANTHRAQUINONE

The photochemistry (Type I and II) of anthralin and its photo-oxidation product 1,8-dihydroxyanthraquinone (1,8-DHAQ) has been studied in ethanol, acetonitrile and dimethylsulfoxide using spin-trapping and direct detection of singlet oxygen (1O2) luminescence techniques. In ethanol, where it exists in its neutral form (AN), anthralin does not undergo either Type I or II reactions upon UV-irradiation. In contrast, irradiation of anthralin in acetonitrile, a solvent in which anthralin is partially converted to its corresponding mono-anion (AN-), generates both superoxide and singlet oxygen. Irradiation of anthralin in dimethylsulfoxide, where the AN- form is present in substantial quantity, generates superoxide and solvent derived radicals but no detectable singlet oxygen. UV-irradiation of 1,8-DHAQ in ethanol and acetonitrile produces both superoxide and singlet oxygen in significant yields. In dimethylsulfoxide, on the other hand, only superoxide and solvent derived radicals are observed. The 1O2 quantum yield for AN- and 1,8-DHAQ in acetonitrile were determined to be 0.14 and 0.88 relative to rose bengal in the same solvent. These findings suggest that the AN photosensitization occurs via Type I and II pathways, is solvent dependent and involves AN- as well as its oxidation product 1,8-DHAQ, which is a more potent generator of both singlet oxygen and superoxide.