N3-(4-Methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP) and 2-amino-2- deoxy-D-glucitol-6-phosphate (ADGP) are strong inhibitors of the essential fungal enzyme, glucosamine-6-phosphate synthase, but their antifungal activity is poor, due to slow penetration of these agents through the cytoplasmic membrane. In the present studies we have exploited the possibility of enhancement of ADGP and FMDP antifungal activity by improving their transport properties. It has been found that membrane-permeabilising polyene macrolides amphotericin B (AMB) and its .N-methyl-^-fructosyl methyl ester derivative (MF-AME), at subinhibitory concentrations, facilitate diffusion of ADGP through the fungal cell membrane, thus allowing a decrease of its minimal inhibitory concentration (MIC). Synergistic effects have been observed for combinations of ADGP with AMB or MF-AME. Fractional inhibitory concentration (FIC) indexes, determined against a number of Candida spp., have been in the 0.18-0.81 range. Weak antifungal synergistic effects have been found for combinations of FMDP with AMB or MF-AME.ADGP can be easily encapsulated into unilamellar lipid vesicles. Liposomal preparations of ADGP demonstrated stronger antifungal activity against some fungal strains than free ADGP.
The paper presents the results of research on magnesium effect on beneficial enthomopathogenic fungi and nematodes as well as some predatory arthropods. Magnesium fertilization of soil contaminated with heavy metals does not significantly affect numbers of the majority of epigeal invertebrates, but it may influence numbers of single species, favouring the occurrence of some (Bembidion sp.) while restricting the presence of others (Harpalus rufipes De Geer). Magnesium synergism with heavy metal ions has been found to increase infectiveness and pathogenicity of enthomopathogenic fungi. Magnesium, in a dose of 160 mg⋅dm-3 present in the medium, significantly enhances pathogenicity of fungi, such as Beauveria bassiana, Paecilomyces farinosus, Paecilomyces fumoso-roseus or Metarhizium ansopliae. Increased pathogenicity of Steinernema carpocapsae and Heterorhabditis bacteriophora towards test insects has also been observed when magnesium ions were added to a solution in which these nematodes were kept. An effective magnesium dose differed depending whether the nematodes were used separately for test insects (450 mg⋅dm-3) or jointly with enthomopathogenic fungi (320 mg⋅dm-3). This protective effect of magnesium ions on beneficial microorganisms has also been observed in soil contaminated with heavy metals. An addition of magnesium to a solution in which enthomopathogenic nematodes were kept (160 mg⋅dm-3) and to a medium on which fungi were cultured (320 mg⋅dm-3) increased pathogenic abilities of these organisms in contaminated soil to a very high degree (10- to 300- fold higher than the natural heavy metal content in soil).
The cowpea aphid (Aphis craccivora Koch) is considered a serious insect pest attacking several crops. We carried out biochemical studies to elucidate the role of the metabolising enzymes in conferring resistance to thiamethoxam, in two strains (resistant and susceptible) of the cowpea aphid. Bioassay experiments showed that the thiamethoxam selected strain developed a 48 fold resistance after consecutive selection with thiamethoxam for 12 generations. This resistant strain also exhibited cross-resistance to the tested carbamates; pirimicarb and carbosulfan, organophosphorus (malathion, fenitrothion, and chlorpyrifos-methyl), and the neonicotinoid (acetamiprid). Synergism studies have indicated that S,S,S-tributyl phosphorotrithioate (DEF), a known inhibitor for esterases, increased thiamethoxam toxicity 5.58 times in the resistant strain compared with the susceptible strain. Moreover, the biochemical determination revealed that carboxylestersae activity was 30 times greater in the resistant strain than in the susceptible strain. In addition, the enzyme activity of glutathione S-transferase (GST) and mixed function oxidases (mfo) increased only in the resistant strain 3.7 and 2.7 times, respectively, in relation to the susceptible (the control). Generally, our results suggest that the higher activity of the detoxifying enzymes, particularly carboxylesterase, in the resistant strain of the cowpea aphid, apparently have a significant role in endowing resistance to thiamethoxam, although additional mechanisms may contribute.