characterization of inhibitory effects of the potential therapeutic inhibitors, benzoic acid and pyridine derivatives, on the monophenolase and diphenolase activities of tyrosinase

نویسندگان

nematollah gheibi cellular and molecular research center, qazvin university of medical sciences, qazvin, iran

negar taherkhani department of biology, faculty of basic sciences, islamic azad university of science and research, tehran, iran

abolfazl ahmadi department of biology, faculty of basic sciences, islamic azad university of science and research, tehran, iran

kamahldin haghbeen biochemistry and biophysics department, national institute for genetic engineering and biotechnology, tehran, iran

چکیده

objective(s):involvement of tyrosinase in the synthesis of melanin and cell signaling pathway has made it an attractive target in the search for therapeutic inhibitors for treatment of different skin hyperpigmentation disorders and melanoma cancers. materials and methods: in the present study, we conducted a comprehensive kinetic analysis to understand the mechanisms of inhibition imposed by 2-amino benzoic acid, 4-amino benzoic acid, nicotinic acid, and picolinic acid on the monophenolase and diphenolase activities of the mushroom tyrosinase, and then mtt assay was exploited to evaluate their toxicity on the melanoma cells. results: kinetic analysis revealed that nicotinic acid and picolinic acid competitively restricted the monophenolase activity with inhibition constants (ki) of 1.21 mm and 1.97 mm and the diphenolase activity with kis of 2.4 mm and 2.93 mm, respectively. 2-aminobenzoic acid and 4-aminobenzoic acid inhibited the monophenolase activity in a non-competitive fashion with kis of 5.15 µm and 3.8 µm and the diphenolase activity with kis of 4.72 µm and 20 µm, respectively. conclusion: our cell-based data revealed that only the pyridine derivatives imposed cytotoxicity in melanoma cells. importantly, the concentrations of the inhibitors leading to 50% decrease in the cell density (ic50) werecomparable to those causing 50% drop in the enzyme activity, implying that the observed cytotoxicity is highly likely due to the tyrosinase inhibition. moreover, our cell-based data exhibited that the pyridine derivatives acted as anti-proliferative agents, perhaps inducing cytotoxicity in the melanoma cells through inhibition of the tyrosinase activities.

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منابع مشابه

Characterization of inhibitory effects of the potential therapeutic inhibitors, benzoic acid and pyridine derivatives, on the monophenolase and diphenolase activities of tyrosinase

Objective(s):Involvement of tyrosinase in the synthesis of melanin and cell signaling pathway has made it an attractive target in the search for therapeutic inhibitors for treatment of different skin hyperpigmentation disorders and melanoma cancers. Materials and Methods: In the present study, we conducted a comprehensive kinetic analysis to understand the mechanisms of inhibition imposed by 2-...

متن کامل

Characterization of inhibitory effects of the potential therapeutic inhibitors, benzoic acid and pyridine derivatives, on the monophenolase and diphenolase activities of tyrosinase

OBJECTIVES Involvement of tyrosinase in the synthesis of melanin and cell signaling pathway has made it an attractive target in the search for therapeutic inhibitors for treatment of different skin hyperpigmentation disorders and melanoma cancers. MATERIALS AND METHODS In the present study, we conducted a comprehensive kinetic analysis to understand the mechanisms of inhibition imposed by 2-a...

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عنوان ژورنال:
iranian journal of basic medical sciences

جلد ۱۸، شماره ۲، صفحات ۱۲۲-۱۲۹

کلمات کلیدی
[ 2 , ' a m i n o b e n z o i c a c i d ' , 4 , ' a m i n o b e n z o i c a c i d ' , ' d i p h e n o l a s e a c t i v i t y ' , ' i n h i b i t i o n ' , ' m o n o p h e n o l a s e a c t i v i t y ' , ' m u s h r o o m t y r o s i n a s e ' , ' n i c o t i n i c a c i d ' , ' p i c o l i n i c a c i d ' ]

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