Abstract:Thimerosal (Merthiolate) is an ethylmercury-containing pharmaceutical compound that is 49.55% mercury and that was developed in 1927. Thimerosal has been marketed as an antimicrobial agent in a range of products, including topical antiseptic solutions and antiseptic ointments for treating cuts, nasal sprays, eye solutions, vaginal spermicides, diaper rash treatments, and perhaps most importantly as a preservative in vaccines and other injectable biological products, including Rho(D)-immune globulin preparation… Show more
“…Thimerosal is an organomercury compound that is used as a common antiseptic. Mercury compounds induce cell death by rapid oxidation of sulfhydryl groups in proteins rendering vital enzymes inactive (31). Hexachlorophene is used as an antiseptic and leads to cell death by inhibiting fatty acid biosynthesis in bacteria (32).…”
Candida albicans is the most common etiologic agent of systemic fungal infections with unacceptably high mortality rates. The existing arsenal of antifungal drugs is very limited and is particularly ineffective against C. albicans biofilms. To address the unmet need for novel antifungals, particularly those active against biofilms, we have screened a small molecule library consisting of 1,200 off-patent drugs already approved by the Food and Drug Administration (FDA), the Prestwick Chemical Library, to identify inhibitors of C. albicans biofilm formation. According to their pharmacological applications that are currently known, we classified these bioactive compounds as antifungal drugs, as antimicrobials/antiseptics, or as miscellaneous drugs, which we considered to be drugs with no previously characterized antifungal activity. Using a 96-well microtiter plate-based high-content screening assay, we identified 38 pharmacologically active agents that inhibit C. albicans biofilm formation. These drugs were subsequently tested for their potency and efficacy against preformed biofilms, and we identified three drugs with novel antifungal activity. Thus, repurposing FDA-approved drugs opens up a valuable new avenue for identification and potentially rapid development of antifungal agents, which are urgently needed.
“…Thimerosal is an organomercury compound that is used as a common antiseptic. Mercury compounds induce cell death by rapid oxidation of sulfhydryl groups in proteins rendering vital enzymes inactive (31). Hexachlorophene is used as an antiseptic and leads to cell death by inhibiting fatty acid biosynthesis in bacteria (32).…”
Candida albicans is the most common etiologic agent of systemic fungal infections with unacceptably high mortality rates. The existing arsenal of antifungal drugs is very limited and is particularly ineffective against C. albicans biofilms. To address the unmet need for novel antifungals, particularly those active against biofilms, we have screened a small molecule library consisting of 1,200 off-patent drugs already approved by the Food and Drug Administration (FDA), the Prestwick Chemical Library, to identify inhibitors of C. albicans biofilm formation. According to their pharmacological applications that are currently known, we classified these bioactive compounds as antifungal drugs, as antimicrobials/antiseptics, or as miscellaneous drugs, which we considered to be drugs with no previously characterized antifungal activity. Using a 96-well microtiter plate-based high-content screening assay, we identified 38 pharmacologically active agents that inhibit C. albicans biofilm formation. These drugs were subsequently tested for their potency and efficacy against preformed biofilms, and we identified three drugs with novel antifungal activity. Thus, repurposing FDA-approved drugs opens up a valuable new avenue for identification and potentially rapid development of antifungal agents, which are urgently needed.
“…In our case, Al-DT complex with absorption maximum λ max = 557 ± 3 nm is forming in postcolumn derivatization where Al remains in fully soluble form. For comparison, λ max for DT alone is 478 nm [43], and in this paper, 480 ± 3 nm; for Hg(DT) 2 , complex is 490 nm [51]; for TM-DT, complex is 538 nm [43]. According to Shrivastaw and Singh [43], detection limit for DT-TM complex is 0.2 μg TM.…”
Section: The Problem Of Tm and Al Simultaneous Determinationmentioning
confidence: 99%
“…It was introduced to the market in 1920 [2] as antibacterial and antifungal agent and is still being used as an antiseptic and preservative in various formulations [3][4][5]. The degradation of thimerosal (TM) involves creation of ethylmercury cation (CH 3 CH 2 Hg + ) [6][7][8][9][10].…”
Summary.A simple and convenient chromatographic method of simultaneous separation, identification, and quantitative determination of thimerosal (TM) (preservative) and aluminum (adjuvant) in vaccines and pharmaceuticals by reversed phase highperformance liquid chromatography (RP-HPLC) with visible (VIS) detection was developed and validated. Due to postcolumn derivatization with dithizone, any interference from matrix was excluded. Similarly, a possibility of on-column decomposition of dithizonates was eliminated. Evaluated detection limits were 0.3 μg TM and 3.0 μg Al, which correspond to the smallest, but possible to recognize, visible peak.
“…Since the 1930s, Thimerosal has been extensively used as an antibacterial agent in vaccines (Geier et al, 2007). Thimerosal has been implicated as a cause of autism.…”
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