(E)-1-(Furan-2-yl)-(substituted phenyl)prop-2-en-1-one Derivatives as Tyrosinase Inhibitors and Melanogenesis Inhibition: An In Vitro and In Silico Study
被引:14
作者:
论文数: 引用数:
h-index:
机构:
Jung, Hee Jin
[1
]
Noh, Sang Gyun
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Noh, Sang Gyun
[1
]
Ryu, Il Young
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Ryu, Il Young
[1
]
Park, Chaeun
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Park, Chaeun
[1
]
论文数: 引用数:
h-index:
机构:
Lee, Ji Young
[1
]
Chun, Pusoon
论文数: 0引用数: 0
h-index: 0
机构:
Inje Univ, Coll Pharm, Gimhae 50834, Gyeongnam, South Korea
Inje Univ, Inje Inst Pharmaceut Sci & Res, Gimhae 50834, Gyeongnam, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Chun, Pusoon
[2
,3
]
论文数: 引用数:
h-index:
机构:
Moon, Hyung Ryong
[1
]
Chung, Hae Young
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Chung, Hae Young
[1
]
机构:
[1] Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
[2] Inje Univ, Coll Pharm, Gimhae 50834, Gyeongnam, South Korea
[3] Inje Univ, Inje Inst Pharmaceut Sci & Res, Gimhae 50834, Gyeongnam, South Korea
A series of (E)-1-(furan-2-yl)prop-2-en-1-one derivatives (compounds 1-8) were synthesized and evaluated for their mushroom tyrosinase inhibitory activity. Among these series, compound 8 (2,4-dihydroxy group bearing benzylidene) showed potent tyrosinase inhibitory activity, with respective IC50 values of 0.0433 mu M and 0.28 mu M for the monophenolase and diphenolase as substrates in comparison to kojic acid as standard compound 19.97 mu M and 33.47 mu M. Moreover, the enzyme kinetics of compound 8 were determined to be of the mixed inhibition type and inhibition constant (K-i) values of 0.012 mu M and 0.165 mu M using the Lineweaver-Burk plot. Molecular docking results indicated that compound 8 can bind to the catalytic and allosteric sites 1 and 2 of tyrosinase to inhibit enzyme activity. The computational molecular dynamics analysis further revealed that compound 8 interacted with two residues in the tyrosinase active site pocket, such as ASN260 and MET280. In addition, compound 8 attenuated melanin synthesis and cellular tyrosinase activity, simulated by alpha-melanocyte-stimulating hormone and 1-methyl-3-isobutylxanthine. Compound 8 also decreased tyrosinase expressions in B16F10 cells. Based on in vitro and computational studies, we propose that compound 8 might be a worthy candidate for the development of an antipigmentation agent.
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Ismail, Nur Izzati
;
Ming-Tatt, Lee
论文数: 0引用数: 0
h-index: 0
机构:
UCSI Univ, Fac Pharmaceut Sci, Cheras 56000, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Ming-Tatt, Lee
;
Lajis, Nordin
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Inst Biosci, Lab Nat Prod, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Lajis, Nordin
;
Akhtar, Muhammad Nadeem
论文数: 0引用数: 0
h-index: 0
机构:
Univ Malaysia Pahang, Fac Ind Sci & Technol, Gambang 26300, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Akhtar, Muhammad Nadeem
;
Akira, Ahmad
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Akira, Ahmad
;
Perimal, Enoch Kumar
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Perimal, Enoch Kumar
;
Israf, Daud Ahmad
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Israf, Daud Ahmad
;
Sulaiman, Mohd Roslan
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Longev Life Sci & Technol Inst, Busan 46241, South Korea
Pusan Natl Univ, Coll Pharm, Aging Tissue Bank, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Noh, Sang Gyun
;
Park, Yujin
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Park, Yujin
;
Kang, Dongwan
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Kang, Dongwan
;
Chun, Pusoon
论文数: 0引用数: 0
h-index: 0
机构:
Inje Univ, Coll Pharm, Gimhae 47392, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Chun, Pusoon
;
Chung, Hae Young
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Longev Life Sci & Technol Inst, Busan 46241, South Korea
Pusan Natl Univ, Coll Pharm, Aging Tissue Bank, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Interdisciplinary Res Program Bioinformat & Longe, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Noh, Sang Gyun
;
Park, Yujin
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Park, Yujin
;
Kang, Dongwan
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Kang, Dongwan
;
Chun, Pusoon
论文数: 0引用数: 0
h-index: 0
机构:
Inje Univ, Coll Pharm, Gimhae 50834, Gyeongnam, South Korea
Inje Univ, Inje Inst Pharmaceut Sci & Res, Gimhae 50834, Gyeongnam, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Chun, Pusoon
;
Chung, Hae Young
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Interdisciplinary Res Program Bioinformat & Longe, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Liew, Choi Yi
;
Lam, Kok Wai
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Lam, Kok Wai
;
Kim, Min Kyu
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Natl Res Fdn Korea, Seoul 137748, South KoreaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Kim, Min Kyu
;
Harith, Hanis H.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Harith, Hanis H.
;
Tham, Chau Ling
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Tham, Chau Ling
;
Cheah, Yoke Kqueen
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Cheah, Yoke Kqueen
;
Sulaiman, Mohd Roslan
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Sulaiman, Mohd Roslan
;
Lajis, Nordin H.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Univ Putra Malaysia, Fac Sci, Dept Chem, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Lajis, Nordin H.
;
Israf, Daud A.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Ismail, Nur Izzati
;
Ming-Tatt, Lee
论文数: 0引用数: 0
h-index: 0
机构:
UCSI Univ, Fac Pharmaceut Sci, Cheras 56000, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Ming-Tatt, Lee
;
Lajis, Nordin
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Inst Biosci, Lab Nat Prod, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Lajis, Nordin
;
Akhtar, Muhammad Nadeem
论文数: 0引用数: 0
h-index: 0
机构:
Univ Malaysia Pahang, Fac Ind Sci & Technol, Gambang 26300, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Akhtar, Muhammad Nadeem
;
Akira, Ahmad
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Akira, Ahmad
;
Perimal, Enoch Kumar
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Perimal, Enoch Kumar
;
Israf, Daud Ahmad
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
Israf, Daud Ahmad
;
Sulaiman, Mohd Roslan
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, MalaysiaUniv Putra Malaysia, Dept Biomed Sci, Fac Med & Hlth Sci, Serdang 43400, Malaysia
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Longev Life Sci & Technol Inst, Busan 46241, South Korea
Pusan Natl Univ, Coll Pharm, Aging Tissue Bank, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Noh, Sang Gyun
;
Park, Yujin
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Park, Yujin
;
Kang, Dongwan
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Kang, Dongwan
;
Chun, Pusoon
论文数: 0引用数: 0
h-index: 0
机构:
Inje Univ, Coll Pharm, Gimhae 47392, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Chun, Pusoon
;
Chung, Hae Young
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Longev Life Sci & Technol Inst, Busan 46241, South Korea
Pusan Natl Univ, Coll Pharm, Aging Tissue Bank, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Interdisciplinary Res Program Bioinformat & Longe, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Noh, Sang Gyun
;
Park, Yujin
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Park, Yujin
;
Kang, Dongwan
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Kang, Dongwan
;
Chun, Pusoon
论文数: 0引用数: 0
h-index: 0
机构:
Inje Univ, Coll Pharm, Gimhae 50834, Gyeongnam, South Korea
Inje Univ, Inje Inst Pharmaceut Sci & Res, Gimhae 50834, Gyeongnam, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Chun, Pusoon
;
Chung, Hae Young
论文数: 0引用数: 0
h-index: 0
机构:
Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea
Pusan Natl Univ, Interdisciplinary Res Program Bioinformat & Longe, Coll Pharm, Busan 46241, South KoreaPusan Natl Univ, Coll Pharm, Busan 46241, South Korea
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Liew, Choi Yi
;
Lam, Kok Wai
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Lam, Kok Wai
;
Kim, Min Kyu
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Natl Res Fdn Korea, Seoul 137748, South KoreaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Kim, Min Kyu
;
Harith, Hanis H.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Harith, Hanis H.
;
Tham, Chau Ling
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Tham, Chau Ling
;
Cheah, Yoke Kqueen
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Cheah, Yoke Kqueen
;
Sulaiman, Mohd Roslan
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Sulaiman, Mohd Roslan
;
Lajis, Nordin H.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Univ Putra Malaysia, Fac Sci, Dept Chem, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Lajis, Nordin H.
;
Israf, Daud A.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia
Univ Putra Malaysia, Fac Med & Hlth Sci, Dept Biomed Sci, Serdang 43400, Selangor, MalaysiaUniv Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43400, Selangor, Malaysia