Econazole is an antifungal agent and a new PI3K (phosphatidylinositol-3-kinase) inhibitor and a potential drug that can be used in lung cancer treatment alone or in combination with cisplatin. Econazole significantly suppressed A549 tumor growth in nude mice[3]. Guinea-pigs infected with T. mentagrophytes, M. canis or C. albicans and treated topically or orally with econazole, were cured. In each of these tests the activity of econazole was compared with that of different reference drugs. Vaginal candidiasis in rats was cured after oral administration of econazole. Toxicity and teratogenicity studies in different laboratory animals indicate that econazole is well tolerated[4]. The econazole-bound TRPV5 (transient receptor potential vanilloid 5) structure adopts a closed conformation with a distinct lower gate that occludes Ca2+ permeation through the channel[5]. Moreover, econazole nitrate loaded transethosomes are effective to deliver econazole nitrate transdermally in a controlled fashion for effective elimination of cutaneous candidiasis[6].
Econazole/益康唑 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Nf1/C0//C0 DNSCs
0.1-10 μM
24 hours
To evaluate the effect of econazole on the proliferation and apoptosis of Nf1/C0//C0 DNSCs, results showed that econazole significantly reduced cell proliferation and induced apoptosis.
Cell Rep Med. 2023 Dec 19;4(12):101309.
NF1/C0//C0 hiPSC-SCPs
0.15 μM
72 hours
To evaluate the inhibitory effect of econazole on the proliferation of NF1/C0//C0 hiPSC-SCPs, results showed that econazole effectively inhibited cell proliferation and induced apoptosis.
Cell Rep Med. 2023 Dec 19;4(12):101309.
Candida albicans ATCC 23866
5.6 ± 0.3 μg/ml
To evaluate the in vitro antimycotic activity of econazole and PC-econazole against Candida albicans, showing identical MIC values.
To investigate the effect of Econazole on LPS-induced loss of vascular reactivity, results showed that Econazole partially inhibited the LPS-induced loss of reactivity.
Br J Pharmacol. 1996 Mar;117(6):1053-8.
J774 murine macrophage cells
1x10^-5 M
20 hours
To investigate the effect of Econazole on LPS-induced iNOS activity, results showed that Econazole significantly inhibited LPS-induced [3H]-citrulline production.
Br J Pharmacol. 1996 Mar;117(6):1053-8.
J774 cells
10 μM
4 h
Did not alter LPS-induced inducible NO synthase mRNA levels but almost completely abolished nitrite production
Br J Pharmacol. 1994 Apr;111(4):1257-61.
J774 cells
1-10 μM
24 h
Inhibited LPS-induced nitrite production in a concentration-dependent manner without cytotoxicity
Br J Pharmacol. 1994 Apr;111(4):1257-61.
PVN neurones
10 µM
Blocked Trpm2 channels, significantly increased overall action current frequency (ACf) and inhibited the temperature effect
Front Pharmacol. 2023 Oct 18;14:1256924.
Mouse primary choroidal endothelial cells
50 µM
4 hours
To validate the protective effect of Econazole in primary cells. Results showed that Econazole significantly increased cell survival.
Sci Rep. 2018 Sep 6;8(1):13387.
Fusarium solani
1.0 µg/mL
48 hours
Evaluate the effect of NDDS on the antifungal activity of ECZ, results showed that NDDS significantly enhanced the antifungal activity of ECZ
Drug Deliv. 2018 Nov;25(1):938-949.
NCI-H520 (squamous cell carcinoma)
22.3 μM
24 hours
Econazole significantly decreased the viability of NCI-H520 cells in a dose-dependent manner.
Sci Rep. 2017 Dec 21;7(1):17987.
SK-SEM-1 (squamous cell carcinoma)
22.2 μM
24 hours
Econazole significantly decreased the viability of SK-SEM-1 cells in a dose-dependent manner.
Sci Rep. 2017 Dec 21;7(1):17987.
A549 (adenocarcinoma)
13.5 μM
24 hours
Econazole significantly decreased the viability of A549 cells in a dose-dependent manner.
Sci Rep. 2017 Dec 21;7(1):17987.
H661 (large cell lung cancer)
6.0 μM
24 hours
Econazole significantly decreased the viability of H661 cells in a dose-dependent manner.
Sci Rep. 2017 Dec 21;7(1):17987.
RF/6A endothelial cells
1 to 100 µM
4 hours
To evaluate the protective effect of Econazole against complement-mediated cell lysis. Results showed that Econazole significantly reduced cell lysis and increased cell survival at concentrations of 10, 20, and 50 µM.
Sci Rep. 2018 Sep 6;8(1):13387.
Econazole/益康唑 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
CBA/J (H-2k) mice
Experimental vaginal candidiasis model
Topical vaginal administration
1%
Once daily for five consecutive days
To evaluate the therapeutic efficacy of econazole and PC-econazole in treating vaginal candidiasis in mice. Results showed that PC-econazole significantly reduced the C. albicans burden post-treatment, with some mice achieving complete clearance.
Econazole significantly suppressed A549 tumor growth without affecting mouse body weight.
Sci Rep. 2017 Dec 21;7(1):17987.
Nude mice
Human cNF xenograft model
Topical application
1% econazole nitrate cream
Twice daily for 24, 48, or 72 hours
To evaluate the effect of econazole on apoptosis in tumor tissue in a human cNF xenograft model, results showed that econazole effectively induced apoptosis in tumor tissue.
Cell Rep Med. 2023 Dec 19;4(12):101309.
Japanese white rabbits
Fungal keratitis model
Topical ocular administration
50 µL of 0.3% w/v
Single dose, sustained for 4 hours
Evaluate the effect of NDDS on corneal penetration and bioavailability of ECZ, results showed that NDDS significantly increased the concentration of ECZ in the cornea and aqueous humor
United States, Arizona
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Tucson, Arizona, United States, 85741
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New York, New York, United States, 10032
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Portland, Oregon, United States, 97210 收起 <<
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Tucson, Arizona, United States, 85741
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New York, New York, United States, 10032
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Portland, Oregon, United States, 97210 收起 <<
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Francisco Flores, MD
Miramar, Florida, United States, 33027
United States, Michigan
Daniel M. Stewart, DO
Clinton Township, Michigan, United States, 48038
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Cyaandi Dove, DPM
Las Vegas, Nevada, United States, 89119
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Robert S. Haber, MD
South Euclid, Ohio, United States, 44118
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Cynthia Strout, MD
Mt. Pleasant, South Carolina, United States, 29464
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Michael H. Gold, MD
Nashville, Tennessee, United States, 37215
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Jeffrey Adelglass, MD
Plano, Texas, United States, 75234 收起 <<
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Sunil S. Dhawan, MD
Fremont, California, United States, 94538
United States, Delaware
Guy F. Webster, MD, PhD
Hockessin, Delaware, United States, 19707
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Marta I. Rendon, MD
Boca Raton, Florida, United States, 33486
Jonathan Kantor, MD
Jacksonville, Florida, United States, 32204
United States, Minnesota
Steven E. Kempers, MD
Fridley, Minnesota, United States, 55432
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Joel Schlessinger, MD
Omaha, Nebraska, United States, 68144
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Phoebe Rich, MD
Portland, Oregon, United States, 97210
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Edward J. Primka III, MD
Knoxville, Tennessee, United States, 37917
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Michael T. Jarratt, MD
Austin, Texas, United States, 78759
William Abramovits, MD
Dallas, Texas, United States, 75230
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David M. Pariser, MD, FAAD, FACP
Norfolk, Virginia, United States, 23507
United States, Wisconsin
Harry H. Sharata, MD, PhD
Madison, Wisconsin, United States, 53719 收起 <<
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Stacy Smith, MD
San Diego, California, United States, 92123
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Daniel Stewart, DO
Clinton Township, Michigan, United States, 48038
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Steven Kempers, MD
Fridley, Minnesota, United States, 55432
United States, Tennessee
Michael Gold, MD
Nashville, Tennessee, United States, 37215
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Michael Jarratt, MD
Austin, Texas, United States, 78759
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Leonard Swinyer, MD
Salt Lake City, Utah, United States, 84124 收起 <<
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