Avermectin

Avermectinernes grundstruktur (her ivermectin, 22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b

Avermectin er fællesnavnet på en række lægemidler med en 16-leddet lakton-ringstruktur, der har en potent virkning mod nematoder (rundorme) og insekter.[1][2]

Avermectinerne er naturligt forkommende som metabolismeprodukter i Streptomyces avermitilis, en jord-actinomycet og anvendes mod nematoder (rundorme) der giver onchocerciasis (flodblindhed) og lymphatisk filariasis (elephantiasis) og andre parasit-sygdomme. Avermectinerne anvendes desuden mod tæger, mider, lus og andre parasitter.

Forskerne William C. Campbell og Satoshi Ōmura blev tildelt den ene halvdel af Nobelprisen i fysiologi eller medicin i 2015.[3]

Kemi

Kemisk er avermectinerne derivater af den samme komplicerede makrocykliske lakton og de lammer invertebraternes nerve- og muskelceller ved at forøge effekterne af glutamat på den invertebrat-specifikke glutamat-gatede chlorid-kanal. De anvendte doser er ikke toxiske for pattedyr eller mennesker, da de ikke har nogen glutamat-gatede chlorid-kanaler.

Se også

Referencer

  1. ^ Ōmura, Satoshi; Shiomi, Kazuro (2007). "Discovery, chemistry, and chemical biology of microbial products". Pure and Applied Chemistry. 79 (4). doi:10.1351/pac200779040581.
  2. ^ Pitterna, Thomas; Cassayre, Jérôme; Hüter, Ottmar Franz; Jung, Pierre M.J.; Maienfisch, Peter; Kessabi, Fiona Murphy; Quaranta, Laura; Tobler, Hans (2009). "New ventures in the chemistry of avermectins". Bioorganic & Medicinal Chemistry. 17 (12): 4085. doi:10.1016/j.bmc.2008.12.069.
  3. ^ Avermectin and Artemisinin - Revolutionary therapies for parasitic diseases. Nobelforsamlingen 2015

Eksterne henvisninger

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