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History of Amebiasis
Published in Roberto R. Kretschmer, Amebiasis: Infection and Disease by Entamoeba histolytica, 2020
In 1844 Parkes, as said serving in the Indian army, reported his experience in the treatment of dysentery and stressed that large doses of ipecacuanha were definitely more efficient than small doses of the drug,8 an experience later confirmed by Docker39 in the island of Mauritius. From his recorded experience of 50 cases Parkes concluded that 90 grams of ipecacuanha change the course of the disease or rather its symptoms, and the disease as such is completely cured.”8 Emetine, the alkaloid of ipecacuanha, was isolated by Vedder in 1912, who also demonstrated its anti-amebic activity in vitro. The same year Rogers, then Professor of Pathology at the Calcutta Medical School, reported good results in intestinal and extraintestinal amebiasis using parenteral emetine in three patients unable to take ipecacuanha orally.40 In spite of the reduced number of patients he treated, there is no reason to believe these results to have been fortuitous, since Rogers was in constant contact with patients with amebiasis as revealed by the fact that 2 years earlier he had reported prevention of amebic abscess of the liver using ipecacuanha.41 In 1923 Marchoux introduced the use of arsenicals (acetarsone) for the treatment of syphilis, later extended for the treatment of amebiasis, alas with little success due to its important toxicity. Nonetheless, this event marked the beginning of the use of arsenicals in amebic disease, to be continued well into the present era in the form of phenylarsonic acid and carbarsone, drugs that were introduced in 1932.42 A few years earlier (1921), Muhlens and Menk had discovered iodohydroxyquinolein (Clinofon®) that led to the development of two important halogenated hydroxyquinoleins, namely, Enterovioform® and Diodoquin®.43
Cloning, purification, kinetic and anion inhibition studies of a recombinant β-carbonic anhydrase from the Atlantic salmon parasite platyhelminth Gyrodactylus salaris
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Ashok Aspatwar, Harlan Barker, Heidi Aisala, Ksenia Zueva, Marianne Kuuslahti, Martti Tolvanen, Craig R. Primmer, Jaakko Lumme, Alessandro Bonardi, Amit Tripathi, Seppo Parkkila, Claudiu T. Supuran
Anions and small molecules which were non-inhibitory (up to 50 mM) against GsaCAβ included iodide, azide, nitrate, bicarbonate, carbonate, sulphate, phenylarsonic acid, phenylboronic acid, perchlorate, selenate, pyrophosphate, tetraborate, hexafluorophosphate and triflate. Many of these anions/small molecules poorly interact with metal ions in solution or within the metalloenzymes’ active sites (e.g. perchlorate, hexafluorophosphate and triflate)69, whereas others (e.g. azide, iodide, phenylarsonic acid, phenylboronic acid, etc.) inhibit with various efficacy CAs belonging to other classes13,69–71. Azide, for example, is a rather efficient hCA I inhibitor, with a KI of 1.2 µM, and has thoroughly been characterised by diverse techniques, including X-ray crystallography14–17.
Anion inhibition studies of the α-carbonic anhydrases from Neisseria gonorrhoeae
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Alessio Nocentini, Chad S. Hewitt, Margaret D. Mastrolorenzo, Daniel P. Flaherty, Claudiu T. Supuran
the following anions showed submillimolar (cyanide had a KI of 1 mM) affinity for NgCA: cyanate, thiocyanate, nitrite, nitrate, bisulphite, sulphate, hydrogensulfide, phenylboronic acid, phenylarsonic acid, selenate, tellurate, tetraborate, perrhenate, peroxydisulfate, selenocyanate, iminodisulfonate, and fluorosulfonate, for which KIs in the range of 0.15 – 1.0 mM were measured (Table 1). In the case of phenylboronic acid and phenylarsonic acid, there is also a selective inhibition of the bacterial enzyme versus the human isoforms, which were much less sensitive to inhibition with these two compounds. Based on these data we hypothesise that boronic acid derivatives26 or benzoxaboroles27, which were shown to act as CAIs for other enzymes, might lead to the development of more effective and possibly NgCA-selective inhibitors.
An anion and small molecule inhibition study of the β-carbonic anhydrase from Staphylococcus aureus
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Linda J. Urbanski, Daniela Vullo, Seppo Parkkila, Claudiu T. Supuran
Inorganic anions represent a well-characterised class of CAIs21. Our study included anions known to have a high affinity in solution for complexing metals, such as halides and especially pseudohalides (cyanide, cyanate, thiocyanate, azide, etc.), as well as those which do not easily form complexes with transition metal ions (e.g. sulphate, selenate, tellurate, tetraborate, etc.). Both groups of anions have been shown to possess inhibitory action against all classes of CAs investigated so far, from prokaryotes to eukaryotes21–23. Furthermore, small molecules such as sulfamide, sulphamic acid, phenylboronic, and phenylarsonic acid also possess such properties24. In this study, we investigated a panel of such anions and small molecules for the inhibition of SauBCA (Table 1). The inhibition data of the abundant human (h) isoforms hCA I and II as well as those of another bacterial CA, NgCA from N. gonorrhoeae25 are also shown in Table 1 for comparison.