When the rice blast pathogen Magnaporthe oryzae recognizes J. Pestic. Sci., 30(2), 67-74 (2005) * To whom correspondence should be addressed. E-mail: yamaism@riken.jp © Pesticide Science Society of Japan
Recent Topics on Action Mechanisms of FungicidesIsamu YAMAGUCHI* and Makoto FUJIMURA † Plant Science Center, Tsurumi, Yokohama,, Japan † Faculty of Life Science, University of Toyo, Itakura, Oura-gun, Gunma 374-0193, Japan (Received December 27, 2004) Plant diseases are damaging to crop production in a temperate and humid climate like that of Japan, which has resulted in the development of many excellent fungicides, but wide-spread use of site-specific fungicides can cause pathogens to develop resistance in the field. While all modern fungicides have been developed through extensive safety evaluation, there is deep public concern about their side effects on non-target organisms. Thus there is a growing interest in non-fungicidal disease-controlling agents since they are supposedly specific to target organisms and less likely to cause resistance. Review the surface characteristics of the host plants such as lipophilicity and hardness, its germinating hypha starts differentiating a special cell termed an appressorium to infect the plant. The formation of appressoria involves signal transduction and the expression of many genes. Then, appressorial cells mature by forming a layer of melanin on the innermost part of the cell wall, which affords high osmotic pressure generated inside the cell to penetrate the cuticle layer of the host plant. Thus if melanin biosynthesis is inhibited, the pathogen cannot exert its pathogenicity. In fact, melanin biosynthesis inhibitors (MBIs) are primarily not toxic to the vegetative growth of M. oryzae, but achieve outstanding control of the blast disease in vivo. Actually there are two types of melanin biosynthesis inhibitors; hydroxynaphthalene reductase inhibitors (MBI-R: fthalide, tricyclazole and pyroquilon) and scytalone dehydratase inhibitors (MBI-D: carpropamid, diclocymet and fenoxanil). The buff mutants of M. oryzae were shown to phenotypically resemble the MBI-R-treated wildtype strains and were essentially nonpathogenic to rice plant, which suggested that a melanin biosynthetic pathway is indispensable for the appressoria to obtain infectiosity.
RIKEN
1)Carpropamid was developed as a novel potent controlling agent against the rice blast, 2) and enzyme kinetic data showed that carpropamid is a tight-binding competitive inhibitor of scytalone dehydratase (STD), a key enzyme in the biosynthesis of melanin. Its calculated Ki value was 140 pM, which is more than 10 5 times smaller than the Km for scytalone. 3,4) An X-ray analysis of the crystal structure of the STD complex with carpropamid identified interactions that determine the tight-binding 5) as shown in Fig. 1. Three types of interactions were considered important for the binding: (1) a strong hydrogen bond between N131 (Asn 131) and chlorine, (2) two hydrogen bonds mediated by water molecules (WTA) and (3) the i...