in vitro and in silico studies of the inhibitory effects of some novel kojic acid derivatives on tyrosinase enzyme
نویسندگان
چکیده
objective(s): tyrosinase is a key enzyme in pigment synthesis. overproduction of melanin in parts of the skin results in hyperpigmentation diseases. this enzyme is also responsible for the enzymatic browning in fruits and vegetables. thus, its inhibitors are of great importance in the medical, cosmetic and agricultural fields. materials and methods: a series of twelve kojic acid derivatives were designed to be evaluated as tyrosinase activity inhibitors. the potential inhibitory activity of these compounds was investigated in silico using molecular docking simulation method. four compounds with a range of predicted tyrosinase inhibitory activities were prepared and their inhibitory effect on tyrosinase activity was evaluated. the antioxidant properties of these compounds were also investigated by in vitro dpph (2,2-diphenyl-1-picrylhydrazyl) and hydrogen peroxide scavenging assays. results: compound iiid exhibited the highest tyrosinase inhibitory activity with an ic50 value of 0.216 ± 0.009 mm which was in accordance with the in silico δgbind results (-13.24 kcal/mol). conclusion: based on the docking studies, from the twelve compounds studied, one (iiid) appeared to have the highest inhibition on tyrosinase activity. this was confirmed by enzyme activity measurements. compound iiid has an no2 group which binds to both of cu2+ ions located inside the active site of the enzyme. this compound appeared to be even stronger than kojic acid in inhibiting tyrosinase activity. the dpph free radical scavenging ability of all the studied compounds was more than that of bht. however, they were not as strong as bht or gallic acid in scavenging hydrogen peroxide.
منابع مشابه
In vitro and in silico studies of the inhibitory effects of some novel kojic acid derivatives on tyrosinase enzyme
Objective(s): Tyrosinase is a key enzyme in pigment synthesis. Overproduction of melanin in parts of the skin results in hyperpigmentation diseases. This enzyme is also responsible for the enzymatic browning in fruits and vegetables. Thus, its inhibitors are of great importance in the medical, cosmetic and agricultural fields. Materials and Methods: A series of twelve kojic acid derivatives wer...
متن کاملIn vitro and in silico studies of the inhibitory effects of some novel kojic acid derivatives on tyrosinase enzyme
OBJECTIVES Tyrosinase is a key enzyme in pigment synthesis. Overproduction of melanin in parts of the skin results in hyperpigmentation diseases. This enzyme is also responsible for the enzymatic browning in fruits and vegetables. Thus, its inhibitors are of great importance in the medical, cosmetic and agricultural fields. MATERIALS AND METHODS A series of twelve kojic acid derivatives were ...
متن کاملsynthesis and tyrosinase inhibitory properties of some novel derivatives of kojic acid
tyrosinase is a multifunctional oxidase that is widely distributed in nature. it is a key enzyme in melanin biosynthesis and is involved in determining the color of mammalian skin and hair. in addition it is responsible for the undesirable enzymatic browning that occurs in plant-derived foods, limiting the shelf -life of fresh-cut products with the resultant economic loss. in recent years ther...
متن کامل: the effect of sericin levels (silk glue protein) on rate of in vitro maturation, fertilization and culture of sheep oocytes
هدف از آزمایش اول بررسی اثر سطوح مختلف سریسین [0 (control), 0.1, 0.5, 1.0, 2.5 %] افزوده شده به محیط , ivm بر cumulus cell expansion، بلوغ هسته و توسعه متوالی جنین، در گوسفندان نژاد سنجابی در فصل تولید مثلی می باشد. از سرگیری میوز به وسیله خارج شدن اولین پولار بادی اندازه گیری و هم چنین درصد رسیدن جنین های دو سلولی به مرحله کلیواژ و بلاستوسیت نیز به عنوان نشانه ای از میزان شایستگی توسعه اولیه ج...
the effect of e-64 on the developmental competence of sheep cocs during in vitro maturation
in the present study, the effect of e-64 at different concentrations (0.5, 1, 5 and 10 µm) added to (1) the ivm medium on oocyte nuclear maturation and developmental competence of ovine oocytes, and (2) to the ivc medium on embryonic development of ovine embryos were investigated.
on translation of politeness strategies in dialogues involving female characters in translations and retranslations of novels translated before and after the islamic revolution of iran and their effects on the image of women: a polysystem theory approach
abstract reception environment has considerable effects on accepting a translation. as the expectations of a target culture and its values and needs change throughout history, its criteria for accepting a translation or rejecting it will change accordingly (gentzler, 2001). the expectations of iran, as the reception environment in the present study, have changed after the islamic revolution. i...
منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
iranian journal of basic medical sciencesجلد ۱۹، شماره ۲، صفحات ۱۳۲-۱۴۴
کلمات کلیدی
میزبانی شده توسط پلتفرم ابری doprax.com
copyright © 2015-2023