The pederin family of antitumor agents: structures, synthesis and biological activity.

Abstract

In 1775 the Danish entomologist Johann Christian Fabricius (1745-1808) first described the genus Paederus, which at that time included only two species. In the ensuing two centuries, over 600 species have been identified, including Paederus fuscipes, whose natural history deserves some mention (Frank and Kanamitsu 1987). Paederus fuscipes is about 8 mm long with a black head and abdominal apex, an orange thorax and abdominal base and iridescent blue elytra (wing case). It inhabits riverbanks, marshes, and irrigated fields, where it feeds mainly on insects, mites, soil nematodes, and decaying vegetable matter. Like most members of the genus, Paederus fuscipes is a predator of the fly population, but it is also a pest to man. The insect does not sting or bite, but a toxin in its hemolymph causes severe dermatitis when it is crushed on the skin, and the eyes are particularly sensitive though the palms of the hands and the soles of the feet are resistant. In addition to the lesions, severe symptoms such as fever, edema, neuralgia, arthralgia, and vomiting are observed with erythema persisting for several months. It has been suggested (Frank and Kanamitsu 1987) that both the affliction and its causative agent were known to Chinese medicine over 1200 years earlier. An insect called ch’ing yao ch’ung was described by Ch’en in 739 A.D.: “It contains a strong poison and when it touches the skin it causes the skin to swell up. It will take the skin off one’s face and remove tattoo marks completely. It is used as a caustic for toxic boils, nasal polypi, and ringworm.”