Weldon Paul J, Kramer Matthew, Gordon Scott, Spande Thomas F, Daly John W
Conservation and Research Center, Smithsonian Institution, Front Royal, VA 22630, USA.
Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17818-21. doi: 10.1073/pnas.0608646103. Epub 2006 Nov 9.
Neotropical poison frogs (Dendrobatidae) contain a variety of lipophilic alkaloids in their diffusely distributed cutaneous glands, including a major class of compounds known as pumiliotoxins. Pumiliotoxins are highly toxic and are believed to protect frogs against predators. Their potential activity against ectoparasites, however, has not been investigated. We tested female yellow fever mosquitoes (Aedes aegypti) for responses to 8-hydroxy-8-methyl-6-(2'-methylhexylidene)-1-azabicyclo[4.3.0]nonane, designated pumiliotoxin 251D [PTX (+)-251D], a skin alkaloid present in all genera of dendrobatids and in other anurans, and to its unnatural enantiomer, PTX (-)-251D. Both enantiomers of PTX 251D presented on silicone feeding membranes reduced landing and feeding by A. aegypti, but PTX (+)-251D did so at lower concentrations. PTX (+)-251D also induced toxicosis, shown when mosquitoes failed to fly off membranes. Similarly, mosquitoes confined with copper wires coated with PTX (+)-251D exhibited greater latencies to fly off the substrate and a higher incidence of leg autotomy than did those confined with the (-)-enantiomer. Our results on the contact toxicities of PTX 251D enantiomers parallel those reported for mice injected with them. The presentation of serial dilutions of PTX (+)-251D to A. aegypti revealed a minimum toxic concentration of 0.1 microg/cm2. This value is substantially lower than that estimated for the cutaneous abundance of this compound in some frogs, an observation consistent the function of PTX 251D in anuran chemical defense against ectoparasitic arthropods.
新热带区毒蛙(箭毒蛙科)在其分布广泛的皮肤腺中含有多种亲脂性生物碱,其中包括一类主要的化合物,即箭毒蛙毒素。箭毒蛙毒素具有高毒性,被认为能保护毒蛙免受捕食者侵害。然而,其对外寄生虫的潜在活性尚未得到研究。我们测试了雌性埃及伊蚊对8 - 羟基 - 8 - 甲基 - 6 -(2'- 甲基亚己基)- 1 - 氮杂双环[4.3.0]壬烷(命名为箭毒蛙毒素251D [PTX(+)-251D])的反应,该皮肤生物碱存在于所有箭毒蛙属以及其他无尾目动物中,同时也测试了其非天然对映体PTX(-)-251D。涂覆在硅酮喂食膜上的PTX 251D的两种对映体都减少了埃及伊蚊的着陆和取食,但PTX(+)-251D在较低浓度下就能做到。PTX(+)-251D还会引发中毒症状,表现为蚊子无法从膜上飞走。同样,与涂有PTX(+)-251D的铜丝放在一起的蚊子,比起与(-)-对映体放在一起的蚊子,飞起离开底物的延迟时间更长,腿部自切的发生率更高。我们关于PTX 251D对映体接触毒性的研究结果与给小鼠注射这些对映体的报道结果相似。向埃及伊蚊呈现系列稀释的PTX(+)-251D后发现,最低毒性浓度为0.1微克/平方厘米。这个值大大低于在某些毒蛙皮肤中该化合物的估计含量,这一观察结果与PTX 251D在无尾目动物对外寄生节肢动物的化学防御中的作用相符。