Abstract The discovery of spinosyn insecticide is a remarkable story about how to find useful natural products from fermentation. The key factor that contributed to its discovery is dereplication. Spinosyn is a mixture of metabolites produced by aerobic fermentation of the actinomycete species Saccharopolyspora spinosa. Their chemical structures are mainly a polyketide derived tetracyclic macrolide appended with two amino sugars. Their insecticidal activities were first observed in the mosquito larvicide screen and its first product launched was in the USA in 1997 for pests on cotton plants. Since then, hundreds of products containing spinosad have been launched for crop protection as well as for the protection of food-animals and companion-animals in many countries. Most recently, spinosad was approved to treat head-lice on human in the USA. Extensive structure-activity relationships studies demonstrated that the mixture of modified factor L and factor J of spinosyn, later named spinetoram, has even broader spectrum than spinosad. The outstanding selectivity, low mammalian toxicity, environmentally friendly properties, plus the unique mode of action make spinosyn stands out as one of the most preferable and commercial successful insecticides globally.
摘要 Spinosyn為一種好氧性放射菌 (Saccharopolyspora spinosa) 的天然代謝物質，在殺蟲劑的應用上，因具有高度選擇性、低哺乳動物毒性、低環境毒性與特殊的作用機制，而富有高度商業價值並在全世界被廣泛使用。Spinosyn之化學結構為多烯酮所衍生之四環大環內酯，且具有兩個胺基醣取代基，其開發過程堪稱天然產物開發的典範，透過孑孓實驗，可大量快速篩檢出待測物的毒性效果，而在篩選過程中，最重要的觀念為去除重複 (dereplication)。Spinosyn為一類化學物質之統稱，在商品化後，賜諾殺 (Spinosad) 含Spinosyn A與D最先在1997年推出，應用於棉花之蟲害防治上，自此之後，大量的產品被推出，應用層面除了植物保護外，也可用於食用動物與伴侶動物，甚至是頭蝨的防治，足見其高度選擇性之優點。近來在化學結構上的研究發現，置換取代基之Spinosyn L與J，合稱為Spinetoram (賜諾特)，具有更廣泛之殺蟲效力，同樣深具開發潛力。
| Key words: Spinosyn insecticides and product sales, natural product research, dereplication, Saccharopolyspora spinosa | | 關鍵詞: 賜諾司類殺蟲劑、天然產物研究、去重複、Saccharopolyspora spinosa。 |
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