Repositioning of Thiourea-Containing Drugs as Tyrosinase Inhibitors

Tyrosinase catalyzes two distinct sequential reactions in melanin biosynthesis: The hydroxylation of tyrosine to dihydroxyphenylalanine (DOPA) and the oxidation of DOPA to dopaquinone. Developing functional modulators of tyrosinase is important for therapeutic and cosmetic purposes. Given the abundance of thiourea moiety in known tyrosinase inhibitors, we studied other thiourea-containing drugs as potential tyrosinase inhibitors. The thiourea-containing drugs in clinical use were retrieved and tested for their ability to inhibit tyrosinase. We observed that methimazole, thiouracil, methylthiouracil, propylthiouracil, ambazone, and thioacetazone inhibited mushroom tyrosinase. Except for methimazole, there was limited information regarding the activity of other drugs against tyrosinase. Both thioacetazone and ambazone significantly inhibited tyrosinase, with IC₅₀ of 14 and 15 μM, respectively. Ambazone decreased melanin content without causing cellular toxicity at 20 μM in B16F10 cells. The activity of ambazone was stronger than that of kojic acid both in enzyme and melanin content assays. Kinetics of enzyme inhibition assigned the thiourea-containg drugs as non-competitive inhibitors. The complex models by docking simulation suggested that the intermolecular hydrogen bond via the nitrogen of thiourea and the contacts via thione were equally important for interacting with tyrosinase. These data were consistent with the results of enzyme assays with the analogues of thiourea.     

Acetyl thiourea chitosan as an eco-friendly inhibitor for mild steel in sulphuric acid medium

Acetyl thiourea chitosan polymer (ATUCS) has been synthesized and evaluated as corrosion inhibitor. The electrochemical behavior of mild steel in naturally aerated 0.5 M H₂SO₄ acid containing different concentrations of ATUCS has been studied by potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) measurements and surface examination via scanning electron microscope (SEM) technique. The results of EIS showed that the resistance (R_t) increases slightly with increasing immersion time indicating a slight decrease in corrosion rate of the steel with time. Also, the corrosion rate increases with either increasing temperature or decreasing the polymer concentration as observed by polarization technique. Electrochemical impedance spectroscopy measurements under open-circuit conditions confirmed well polarization results. ATUCS has shown very good inhibition efficiency (IE) in 0.5 M sulphuric acid solution reaches to 94.5% for 0.76 mM concentration. IE of this compound has been found to vary with the concentration of the polymer solution, immersion time and temperature.     

二氧化硫脲水溶液漂白废纸脱墨浆

介绍用直接制备成的二氧化硫脲水溶液漂白废纸脱墨浆的实验情况。探讨二氧化硫脲水溶液用量、NaOH和二氧化硫脲水溶液用量比、浆浓、漂白温度和时间对漂后纸浆白度的影响,并比较二氧化硫脲水溶液、H_2O_2单段漂白、Na_2S_2O_4单段漂白效果。实验结果表明,二氧化硫脲水溶液是一种有效的废纸浆漂白剂和脱色剂。     

DISSOLUTION THEORY OF GOLD IN ALKALINE THIOUREA SOLUTION(Ⅰ) Anodic Behavior on Gold in Alkaline Thiourea Solution Containing Na_2SO_3

ＩＮＴＲＯＤＵＣＴＩＯＮＳｉｎｃｅｔｈｉｏｕｒｅａｗａｓｕｔｉｌｉｚｅｄａｓｔｈｅｌｉｘｉｖｉａｎｔｏｆｇｏｌｄｅａｒｌｙｉｎ１９３２［１］，ｅｘｔｒａｃｔｉｎｇｇｏｌｄｆｒｏｍｏｒｅｏｒｓｃｒａｐｂｙａｃｉｄｉｃｔｈｉｏｕｒｅａｓｏｌｕｔｉｏｎｈａ...     

在酸性溶液中用强酸树脂D001回收硫脲金

Ｄ００１大孔强酸型离子交换树脂回收硫脲金的研究表明，溶液中共存离子对金吸附率与其生成硫脲配离子的稳定性有关，吸附有吸热过程，吸附热ΔＨ＾θ＝１０．１９ｋＪ．ｍｏｌ＾－１，表明树脂骨架的位阻是影响吸附平衡的因素。     

Sesame lignans enhance the thermal stability of edible vegetable oils

The effect of sesame lignans on the thermal and storage stability of edible vegetable oils (soybean-SBO, sunflower-SFO and ricebran-RBO) was studied by (i) determining the total free radical scavenging activity (RSA) using DPPH, (ii) % total tocol retention, (iii) lignan profile and (iv) PUFA composition. The order of RSA and retention of total tocols of oils heated up to 120 min at frying temperature (FT) were RBO = SBO > SFO and RBO > SBO > SFO, respectively. Heating SBO or SFO at FT after addition of 1.2% lignans increased RSA of SBO to a greater extent than that of SFO, and increased retention of total tocols only in SBO. However, addition of lignans did not further increase the RSA of RBO. Heating oils with added lignans, increased sesamol and decreased sesamolin while sesamin was relatively resistant to heat. These findings suggest that sesame lignans may have potential application as natural antioxidants in the edible oil and food industry.     

硫化矿的浸金研究—酸性硫脲溶液体系

本文研究了在用酸性硫脲溶液从硫化矿中浸金时,硫酸铁浓度、硫脲浓度、酸度、温度、搅拌速度、浸取时间、矿石粒度及固液比等实验条件对金、银浸出率的影响。并对所得结果进行了讨论。     

4,6-二甲基-2-甲磺酰基嘧啶的合成

以硫脲为原料,经碳酸二甲酯甲基化,乙酰丙酮环合,再用过氧化氢氧化得到4,6-二甲基-2-甲磺酰基嘧啶,3步反应的总收率为71.0%。目标化合物结构经GC-MS、1H NMR确证。     

一种新型抗高温酸化缓蚀剂的制备与性能评价

硫脲、多乙烯多胺、油酸按照质量比0.2∶1∶2,通过缩合脱水反应合成出了一种油酸硫脲基咪唑啉,并复配表面活性剂、吡啶、醛、炔醇等,得到一种新型抗高温酸化缓蚀剂LX-1,对缓蚀剂的缓蚀性能、相容性、抗温性能进行评价。结果表明,缓蚀剂的缓蚀性能良好,LX-1加量为0.6%时,缓蚀率达到95%,腐蚀速率达0.015 mm/a;与地层离子及各种化学剂相容性好;能抗高温90℃,盐酸浓度20%时,腐蚀速率0.023 mm/a,缓蚀率89.0%。     

4,4’-双(二乙氧基膦酰甲基)联苯合成工艺研究

以联苯二氯苄和亚磷酸三乙酯为原料,合成4,4’-双(二乙氧基膦酰甲基)联苯。研究了配料摩尔比、反应时间、反应温度、析出溶剂用量对收率的影响。结果表明,最佳合成工艺条件为:配料亚磷酸三乙酯和联苯二氯苄的摩尔比3.5∶1,反应温度为160℃,反应时间为5 h,析出溶剂用量140 mL。在此条件下,收率可达97.4%,产品含量达98.2%。