and Evernia prunastri are processed in the perfume industry, and some lichens are sensitive reagents for the evaluation of air pollution.

The significance of lichens and their metabolites.

Natural products represent a vast repository of materials and compounds with evolved biological activity, including phytotoxicity. Some of these compounds can be used directly or as templates for herbicides. The molecular target sites of these compounds are often unique. Strategies for the discovery of these materials and compounds are outlined. Numerous examples of individual phytotoxins and crude preparations with weed management potential are provided. An example of research to find a natural product solution of a unique pest management problem (blue-green algae in aquaculture) is described. Finally, the problems associated with natural products for pest control are discussed.

https://www.jstor.org/stable/pdfplus/4046356.pdf

Invited Paper: Chemicals from nature for weed management

Poria cocos (Polyporaceae) is a saprophytic fungus that grows in diverse species of Pinus. Its sclerotium, called fu-ling or hoelen, is used in traditional Chinese and Japanese medicine for its diuretic, sedative, and tonic effects. Various studies of this fungus have demonstrated its marked anti-inflammatory activity in different experimental models of acute and chronic inflammation. It is widely used as a constituent of many preparations in Asian medicine, but the number of research papers on its clinical properties is insufficient for establishing its efficacy and safety from a scientific point of view. In this review, we have compiled all the published data concerning the chemistry, pharmacology, and clinical uses of this drug in order to evaluate its clinical interest for future use against various pathologies in which inflammation and immunodepression are implicated. We selected the papers for review on the basis of their ethnopharmacological relevance, using the most relevant databases for the biomedical sciences. Studies on various fungus extracts as well as on the major phytochemical compounds (polysaccharides and triterpenoids) present in Poria cocos comprised the principal objectives of this review. In several of the studies reviewed, the inhibitory effects of triterpenes on phospholipase A (2) (PLA (2)) have been clearly demonstrated. In addition, the inhibitory effects of Poria cocoson the secretion of different cytokines from human peripheral blood monocytes have also been described. Triterpenoids are known to have a pivotal influence on certain diseases such as rheumatoid arthritis, psoriasis, autoimmune uveitis, septic shock, and possibly bronchial asthma, while polysaccharides can potentiate the immune response. Reviewing the literature, we found that polysaccharides from Poria cocos enhanced the secretion of immune stimulators and suppressed the secretion of immune suppressors, thus potentiating the immune response. In addition, they showed antitumor activity against different cancer cell lines. This activity is associated with their capacity to inhibit angiogenesis by downregulating both NF- κB and the induction of NF- κB/Rel translocation.

/pdf/chemical-constituents-and-pharmacological-properties-of-jnlsah833l.pdf

Chemical constituents and pharmacological properties of Poria cocos.

A series of 2-amino-3-substituted-6-[(E)-1-phenyl-2-(N-methylcarbamoyl)vinyl]imidazo[1,2-a]pyridines 1a−i, structurally related to Enviroxime and its analogous benzimidazoles, was designed and prepared for testing as antirhinovirus agents. The imidazo ring in this class of compounds was constructed starting from the aminopyridine after tosylation and subsequent treatment with the appropriate acetamides. The key steps in the synthesis include the development and use of a new Horner−Emmons reagent for the direct incorporation of methyl vinylcarboxamide. The reaction was stereospecific in the substrates 5a−f leading exclusively to the desired E-isomer and avoiding the use of reverse-phase preparative HPLC for the separation of both possible isomers before antiviral activity evaluation. The isopropylsulfonyl group, known as the best substituent at the 1-position in the benzimidazole SAR in terms of activity, was introduced in this new series of imidazo[1,2-a]pyridines via halogen−metal exchange and subsequent...

2-Amino-3-substituted-6-[(E)-1-phenyl-2-(N-methylcarbamoyl)vinyl]imidazo[1,2-a]pyridines as a Novel Class of Inhibitors of Human Rhinovirus: Stereospecific Synthesis and Antiviral Activity

Inhibitors of MAO-A and MAO-B are in clinical use for the treatment of psychiatric and neurological disorders respectively. Elucidation of the molecular structure of the active sites of the enzymes has enabled a precise determination of the way in which substrates and inhibitor molecules are metabolized, or inhibit metabolism of substrates, respectively. Despite the knowledge of the strong antidepressant efficacy of irreversible MAO inhibitors, their clinical use has been limited by their side effect of potentiation of the cardiovascular effects of dietary amines (“cheese effect”). A number of reversible MAO-A inhibitors which are devoid of cheese effect have been described in the literature, but only one, moclobemide, is currently in clinical use. The irreversible inhibitors of MAO-B, selegiline and rasagiline, are used clinically in treatment of Parkinson’s disease, and a recently introduced reversible MAO-B inhibitor, safinamide, has also been found efficacious. Modification of the pharmacokinetic characteristics of selegiline by transdermal administration has led to the development of a new drug form for treatment of depression. The clinical potential of MAO inhibitors together with detailed knowledge of the enzyme’s binding site structure should lead to future developments with these drugs.

/pdf/inhibitors-of-mao-a-and-mao-b-in-psychiatry-and-neurology-laromc8wsc.pdf

Inhibitors of MAO-A and MAO-B in Psychiatry and Neurology

Hoelen, sclederma of Poria cocos Wolf, has long been used as a sedative and diuretic in traditional medicine. Formerly, we demonstrated that Hoelen in vitro protects red blood cells from AAPH-induced hemolysis. In this study, tests were carried out to identify the main ingredient of Hoelen that has the scavenging effect on free-radicals. Triterpene carboxylic acids isolated from the methanol extract of Hoelen, i.e. pachymic acid, polyporenic acid, 3-epidehydrotumulosic acid, 3β-hydroxylanosta-7,9(11), 24-trien-21-oic acid and 3-o-acetyl-16 α -hydroxytrametenolic acid, were found to have inhibitory activities against AAPH-induced lysis of red blood cells. Copyright © 2003 John Wiley & Sons, Ltd.

Inhibitory effects of triterpenes isolated from Hoelen on free radical-induced lysis of red blood cells.

Favelines, novel tricyclic benzocycloheptenes with cytotoxic activities from brazilian plant, doscolus phyllacanthus

Monoamine oxidase B (MAO-B) inhibitors were isolated from the bark of a Brazilian plant, Himatanthus sucuuba (SPR.). Assignments of the 1H- and 13C-NMR data using two dimensional (2D)-NMR techniques showed the active components to be known lichen depsides, confluentic acid (1) and 2'-O-methylperlatolic acid (2). The depside (1) showed selective inhibition of MAO-B with IC50 value of 0.22 microM.

Confluentic Acid and 2'-O-Methylperlatolic Acid, Monoamine Oxidase B Inhibitors in a Brazilian Plant, Himatanthus sucuuba

PROBLEM TO BE SOLVED: To provide an electric power steering device which is improved in the electrocorrosion resistance, fletching resistance, impact resistance or the like of a motor bearing, excellent in quietness more than before, and also improved in durabilitySOLUTION: A rolling body of a motor bearing is constituted of a first phase containing zirconia and a sintering auxiliary agent, and a second phase composed of aluminum, and formed of a sintered body in which mass ratios of the first phase: second phase=50: 50 to 95: 5 (mass ratio), a content of the sintering auxiliary agent in the first phase is 1 to 55 mol%, a total number of a solid zirconia mass and a solid aluminum mass having grain diameters of 10 to 30 μm is not larger than 15 per cross section 300 mmof the rolling body, and a Young's modulus (E/E) with respect to a Young's modulus of SUJ2 is not higher than 14SELECTED DRAWING: Figure 1

Electric power steering device

Three cytotoxic 6-substituted 5,6-dihydro-2H-pyran-2-ones (1-3) were isolated from a Brazilian medicinal plant, Chorisia crispiflora. (1) was identified as argentilactone, and the structures of two new compounds (2 and 3) were determined on the basis of the physicochemical properties

Yuichi Endo

Papers

Inhibitory effects of triterpenes isolated from Hoelen on free radical-induced lysis of red blood cells.

Favelines, novel tricyclic benzocycloheptenes with cytotoxic activities from brazilian plant, doscolus phyllacanthus

Confluentic Acid and 2'-O-Methylperlatolic Acid, Monoamine Oxidase B Inhibitors in a Brazilian Plant, Himatanthus sucuuba

Electric power steering device

Cytotoxic 6-substituted 5,6-dihydro-2H-pyran-2-ones from a Brazilian medicinal plant, Chorisia crispiflora