CHARACTERIZATION OF INHIBITORY EFFECTS OF THE POTENTIAL THERAPEUTIC INHIBITORS, BENZOIC ACID AND PYRIDINE DERIVATIVES, ON THE MONOPHENOLASE AND DIPHENOLASE ACTIVITIES OF TYROSINASE

Q: How can I download an article?

To download an article from SID, first log in to the site, search for the article title, and click on the 'Download Article' option.

Q: How can I download an ISI article?

To download an ISI article on SID, enter the keyword or article title in the search bar, view the relevant results, click on the desired article, and select the 'Download Article' option.

Q: How can I access the SID database?

To access the SID database, visit SID.ir, create an account, and log in to access scientific resources.

Q: Is downloading articles from SID free?

Some articles on SID are available for free, while others require payment. Details are specified on the article's page.

GHEIBI NEMATOLLAH; TAHERKHANI NEGAR; AHMADI ABOLFAZL; HAGHBEEN KAMAHLDIN; ILGHARI DARIUSH

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Journal Paper

Paper Information

Journal: Iranian Journal of Basic Medical Sciences Year:2015 | Volume:18 | Issue:2 Page(s): 122-129

Download Full-Text

View:

329

Download:

163

Cites:

Information Journal Paper

Title

CHARACTERIZATION OF INHIBITORY EFFECTS OF THE POTENTIAL THERAPEUTIC INHIBITORS, BENZOIC ACID AND PYRIDINE DERIVATIVES, ON THE MONOPHENOLASE AND DIPHENOLASE ACTIVITIES OF TYROSINASE

Author(s)

Keywords

2-AMINO BENZOIC ACID

4-AMINO BENZOIC ACID

DIPHENOLASE ACTIVITY

INHIBITION

MONOPHENOLASE ACTIVITY

MUSHROOM TYROSINASE

NICOTINIC ACID

PICOLINIC ACID

Abstract

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 mM and 3.8 mM and the DIPHENOLASE ACTIVITY with Kis of 4.72 mM and 20 mM, 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) were comparable 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.

Cites

No record.

References

No record.

Cite

APA: Copy

GHEIBI, NEMATOLLAH, TAHERKHANI, NEGAR, AHMADI, ABOLFAZL, HAGHBEEN, KAMAHLDIN, & ILGHARI, DARIUSH. (2015). CHARACTERIZATION OF INHIBITORY EFFECTS OF THE POTENTIAL THERAPEUTIC INHIBITORS, BENZOIC ACID AND PYRIDINE DERIVATIVES, ON THE MONOPHENOLASE AND DIPHENOLASE ACTIVITIES OF TYROSINASE. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 18(2), 122-129. SID. https://sid.ir/paper/637396/en

Vancouver: Copy

GHEIBI NEMATOLLAH, TAHERKHANI NEGAR, AHMADI ABOLFAZL, HAGHBEEN KAMAHLDIN, ILGHARI DARIUSH. CHARACTERIZATION OF INHIBITORY EFFECTS OF THE POTENTIAL THERAPEUTIC INHIBITORS, BENZOIC ACID AND PYRIDINE DERIVATIVES, ON THE MONOPHENOLASE AND DIPHENOLASE ACTIVITIES OF TYROSINASE. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES[Internet]. 2015;18(2):122-129. Available from: https://sid.ir/paper/637396/en

IEEE: Copy

NEMATOLLAH GHEIBI, NEGAR TAHERKHANI, ABOLFAZL AHMADI, KAMAHLDIN HAGHBEEN, and DARIUSH ILGHARI, “CHARACTERIZATION OF INHIBITORY EFFECTS OF THE POTENTIAL THERAPEUTIC INHIBITORS, BENZOIC ACID AND PYRIDINE DERIVATIVES, ON THE MONOPHENOLASE AND DIPHENOLASE ACTIVITIES OF TYROSINASE,” IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, vol. 18, no. 2, pp. 122–129, 2015, [Online]. Available: https://sid.ir/paper/637396/en

Related Journal Papers

No record.

Related Seminar Papers

No record.

Related Plans

No record.

Recommended Workshops