2017
DOI: 10.1055/s-0043-104775
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Correlating In Vitro Target-Oriented Screening and Docking: Inhibition of Matrix Metalloproteinases Activities by Flavonoids

Abstract: Metalloproteases are a family of zinc-containing endopeptidases involved in a variety of pathological disorders. The use of flavonoid derivatives as potential metalloprotease inhibitors has recently increased.Particular plants growing in Sicily are an excellent yielder of the flavonoids luteolin, apigenin, and their respective glycoside derivatives (7-O-rutinoside, 7-O-glucoside, and 7-O-glucuronide).The inhibitory activity of luteolin, apigenin, and their respective glycoside derivatives on the metalloproteas… Show more

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Cited by 26 publications
(22 citation statements)
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“…It is also reported to interact and inhibit enzymes like sentrin-specific protease 1 (SENP1) (a SUMO protease that is involved in the development of prostate cancer), aldose reductase (an enzyme that is responsible for conversion of glucose to sorbitol and has a pathophysiological role in Diabetic retinopathy), and Matrix metalloproteases (MMPs) (an enzyme that is overexpressed in cancer, arthritis, atherosclerosis, etc.) (AID 651697, 2012; Crascì et al., 2017 ; Jung et al., 2011 ). This molecule exhibited one common amino-acid residue interaction with GLU-166 ( Figure 16 ).…”
Section: Resultsmentioning
confidence: 99%
“…It is also reported to interact and inhibit enzymes like sentrin-specific protease 1 (SENP1) (a SUMO protease that is involved in the development of prostate cancer), aldose reductase (an enzyme that is responsible for conversion of glucose to sorbitol and has a pathophysiological role in Diabetic retinopathy), and Matrix metalloproteases (MMPs) (an enzyme that is overexpressed in cancer, arthritis, atherosclerosis, etc.) (AID 651697, 2012; Crascì et al., 2017 ; Jung et al., 2011 ). This molecule exhibited one common amino-acid residue interaction with GLU-166 ( Figure 16 ).…”
Section: Resultsmentioning
confidence: 99%
“…These compounds display antioxidant, anti-inflammatory, anti-mutagenic and anti-carcinogenic activities [ 24 ]. They are also potent inhibitors of several enzymes—for instance, xanthine oxidase [ 25 ], cyclo-oxygenase [ 26 ], protein kinases [ 27 ] and matrix metalloproteinases (MMPs) [ 21 , 28 , 29 ].…”
Section: Discussionmentioning
confidence: 99%
“…For instance, gallocatechin, isoquercitrin, pinostrobin, and quercetin-3-O-rhamnoside isolated from different plant species have been shown to inhibit hemorrhagic activity of different viperid and elapid venoms and some isolated SVMPs [ 17 , 18 , 19 , 20 ]. Similarly, the ability of flavonoids to inhibit human matrix metalloproteinases (MMPs) has been demonstrated [ 21 , 22 ]. The phenolic nucleus of flavonoids is able to form multiple interactions with proteins: hydrogen bonds, hydrophobic interactions, metal chelation and stacking interactions [ 23 ].…”
Section: Introductionmentioning
confidence: 99%
“…On the contrary, the presence of a hydroxyl group at the 3 position was less important in determining the inhibitory effect on MMP-2 and MMP-9 [29]. In addition, drug absorption and interaction with MMPs may be affected by compound lipophilicity, expressed as the octanol-water partition coefficient (log P), and topological polar surface area (TPSA), resulting from the sum of the surfaces of polar atoms in a molecule [30].…”
Section: Introductionmentioning
confidence: 99%