p-Hydroxybenzaldehyde thiosemicarbazone (HBT) and p-methoxybenzaldehyde thiosemicarbazone (MBT) were synthesized and established by (1)H NMR and mass spectra. Both compounds were evaluated for their inhibition activities on mushroom tyrosinase and free-cell tyrosinase and melanoma production from B(16) mouse melanoma cells. Results showed that both compounds exhibited significant inhibitory effects on the enzyme activities. HBT and MBT decreased the steady state of the monophenolase activity sharply, and the IC(50) values were estimated as 0.76 and 7.0 μM, respectively. MBT lengthened the lag time, but HBT could not. HBT and MBT inhibited diphenolase activity dose-dependently, and their IC(50) values were estimated as 3.80 and 2.62 μM, respectively. Kinetic analyses showed that inhibition type by both compounds was reversible and their mechanisms were mixed-type. Their inhibition constants were also determined and compared. The research may supply the basis for the development of new food preservatives and cosmetic additives.
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http://dx.doi.org/10.1021/jf204420x | DOI Listing |
Curr Mol Pharmacol
March 2023
Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, Jiangsu Province 221004, China.
Background: The mechanisms underlying synaptic injury and anxiety-like behavioral changes caused by diabetes and the strategies to reverse these changes are not well understood.
Objectives: This study examined the neuroprotective effects of hesperidin on anxiety-like behaviors in diabetic rats and investigated the underlying mechanisms from the perspective of the PKA/CREB pathway.
Methods: Rats with streptozotocin-induced diabetes were treated orally with hesperidin (50 and 150 mg/kg) for 10 weeks.
Sci Rep
November 2020
Department of Pediatrics, Rostock University Medical Center, Ernst-Heydemann-Str. 8, 18057, Rostock, Germany.
Carbohydrate malabsorption and subsequent gastrointestinal symptoms are a common clinical problem in pediatrics. Hydrogen (H) and methane (CH) breath tests are a cheap and non-invasive procedure for diagnosing fructose and lactose malabsorption (FM/LM) but test accuracy and reliability as well as the impact of non-hydrogen producers (NHP) is unclear. CH breath tests (MBT), blood sugar tests (BST) and clinical symptoms were compared with H breath tests (HBT) for FM/LM.
View Article and Find Full Text PDFCurr Pharm Des
January 2021
Experimental Biology Centre (NUBEX), University of Fortaleza (UNIFOR), Fortaleza, Ceara, Brazil.
Background: Plant lectins have shown promising biological activities in the central nervous system (CNS).
Objective: This study evaluated the effect of DAL, a lectin isolated from the seeds of the Dioclea altissima species, having binding affinity to D-glucose or D-mannose residues, on mice behavior.
Methods: Mice (n=6/group) were treated (i.
Toxicol Sci
August 2015
US Environmental Protection Agency, ORD, NHEERL, Mid-Continent Ecology Division, Duluth, Minnesota.
As in vitro assays are increasingly used to screen chemicals for their potential to produce endocrine disrupting adverse effects, it is important to understand their predictive capacity. The potential for a set of 6 benzothiazoles to affect endpoints related to thyroid hormone synthesis inhibition were assessed using in vitro, ex vivo, and in vivo assays. Inhibition of thyroid peroxidase (TPO) derived from pig thyroid glands was determined for benzothiazole (BTZ), 2-mercaptobenzothiazole (MBT), 5-chloro-2-mercaptobenzothiazole (CMBT), 2-aminobenzothiazole (ABT), 2-hydroxybenzothiazole (HBT), and 2-methylthiobenzothiazole (MTBT).
View Article and Find Full Text PDFTumour Biol
July 2015
Center for Stem Cell and Gene Therapies Research and Practice, Department of Stem Cell, Kocaeli University, Kocaeli, Turkey.
Tumor microenvironment is an important factor, which sustains and promotes the tumors by inflammatory signals. Interleukin-6 (IL-6) is known as a multifunctional cytokine, which is a major activator of the signaling pathway of Janus kinases (JAKs)/signal transducer and activator of transcription 3 (STAT3). In this study, we aimed to investigate the effect of IL-6 in the tumor microenvironment on carcinogenesis.
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