Synthesis and antifungal activity of 2‐azetidinonyl‐5‐(2‐benzoylphenoxy)methyl‐1,3,4‐oxadiazoles against seed‐borne pathogens of Eleusine coracana (L.) Gaertn

BACKGROUND: Finger millet is a major food crop as well as feed and fodder for livestock, especially in regions of southern India. A sturdy crop to fluctuating environmental conditions, it can be cultivated in all seasons of the year. Leaf, neck and finger blast caused by Pyricularia grisea Sacc. and Bipolaris setariae (Saw.) Shoem, as well as leaf spot disease, Bipolaris nodulosa (Berk & M.A.Curtis) Shoem, are major production constraints in southern India. Apart from environmental conditions, the use of harvested seeds by farmers is a major reason for disease prevalence. Benzophenone analogues have been investigated for controlling phytopathogenic fungi. In addition, the most important applications of azetidin‐2‐ones are as antibiotics. Based on this information, the present study was conducted to explore the antifungal activity of integrated 2‐azetidinonyl and 1,3,4‐oxadiazoles moieties into a benzophenone framework. RESULTS: A simple high‐yielding method for the integration of heterocyclic rings, namely 2‐azetidinonyl, at the benzophenone nucleus has been achieved, starting from substituted 2‐hydroxybenzophenones under mild conditions on a wet solid surface using microwave irradiation. In the present study, an array of newly synthesised compounds, 2‐azetidinonyl‐5‐(2‐benzoylphenoxy)methyl‐1,3,4‐oxadiazoles, were screened for their antifungal property against blast and leaf spot causing fungi associated with the seeds of finger millet, cv. Indof‐9. CONCLUSION: Two of the newly synthesised compounds showed promising effects in depleting the incidence of seed‐borne pathogenic fungi of finger millet. The suppression of Pyricularia grisea and Bipolaris setariae resulted in enhanced seed germination and seedling growth. Copyright © 2009 Society of Chemical Industry     

Anticarcinogenic effects of curry leaves in dimethylhydrazine-treated rats

Curry leaves are one of the spices used in Indian dishes for aroma and preservation. There are no reports on the antioxidant properties of curry leaves. In this study, the antioxidant potential of curry leaves in rats treated with a known chemical carcinogen, dimethylhydrazine hydrochloride (DMH) was investigated. Food intake was reduced in the rats fed curry leaf-supplemented diet but the body and the organ weights were not affected.Vitamin A content in the liver was significantly increased whereas glutathione (GSH) content was not altered. A 50% reduction was seen in the micronuclei induced by DMH and a 30% reduction in the activity of ,-glutamyl transpeptidase when the rats were fed a curry leaf-supplemented diet. These results indicate that curry leaves have highpotential as reducer of the toxicity of DMH.     

Relationship Between Ion Accumulation and Growth in Two Spring Wheat Lines Differing in Salt Tolerance at Different Growth Stages

A salt-tolerant line, S24, of spring wheat was compared with a salt-sensitive line, Yecora Rojo, in sand cultures at four different growth stages, i.e. germination, seedling, tillering and booting, under greenhouse conditions. The NaCl treatments used were 0 or 125 mol m⁻³ in full strength Hoagland's nutrient solution. S24 exceeded Yecora Rojo in biomass or grain yield at the tillering and booting stages, but these lines did not differ at the initial growth stages, i.e. germination and seedling. The growth performance of the two lines at different growth stages was positively related to the pattern of accumulation of cations and anions. The superiority of S24 to Yecora Rojo at the two later growth stages was related to its relatively low accumulation of Na⁺ or Cl⁻ and high accumulation of K⁺ in leaves. The former line also maintained higher leaf K/Na ratios, Ca/Na ratios, K versus Na selectivities and Ca versus Na selectivities than the latter particularly at the tillering and booting stages. Salt tolerance in spring wheat, in this study, is found to be age-dependent. The booting stage has been found as one of the most appropriate growth stages where maximum differentiation in salt-tolerant and salt-sensitive lines occurred. As is evident from previous studies with spring wheat, in the present study there is a positive correlation between partial exclusion of Na⁺ or Cl⁻¹ from the tissues and maintenance of high tissue K/Na and Ca/Na ratios, and K versus Na and Ca versus Na selectivities, and salt tolerance of this crop.     

Dietary fiber content of commonly fresh and cooked vegetables consumed in India

Legumes, leafy vegetables,roots and tubers, gourds and other vegetables were analyzed for total (TDF), soluble (SDF) and insoluble (IDF) dietaryfiber contents, both before and after cooking eitherby a conventional open-pan method or by pressurecooker. Data revealed a significant increase inSDF fraction with a concomitant decrease in the IDFfraction upon cooking by both the methods employed. Although the decrease in IDF matched the increase inSDF values in some cases, it was found to be more invegetables categorized as `other'. The dietary fiber values have also been reported on a fresh weight basis which may serve as a guideline for calculating dietary intake of eachcomponent by the consumer.     

Clinico-pathomorphological, serum biochemical and histological studies in broilers fed ochratoxin A and a toxin deactivator (Mycofix Plus)

1. Toxic effects of two concentrations (0.5 and 1 mg/kg) of ochratoxin A (OTA) and attenuating effects of a toxin deactivator (Mycofix Plus(MTV INSIDE)) containing the yeast Trichosporon mycotoxinivorans on the performance (feed conversion ratio; body weight gain), serum enzymes (lactate dehydrogenase, gamma-glutamyltranspeptidase and aspartate aminotransferase) and clinico-pathomorphology of internal organs were studied in 270 one-day-old broiler chicks divided into 9 groups over a 42-d period. 2. Feed conversion ratios (FCR) in groups fed toxin deactivator were improved compared with groups receiving OTA only. An increase in the relative weight of kidney and liver was observed in groups fed 0.5 and 1 mg/kg OTA on day 42 of the experiment as compared with the control group. In contrast, relative weights of bursa of Fabricius and spleen were not significantly affected in experimental groups exposed to OTA as compared to control groups determined on days 28 and 42 of age. 3. Serum enzymes (LDH, GGT and AST) values in OTA treated groups determined on days 28 and 42 were higher than those of the control group. 4. Histopathological examination of kidney on day 42 revealed degenerative changes in the epithelial cells of the proximal convoluted tubules and massive necrosis of the proximal tubular epithelial cells. These changes were less marked in birds receiving 0.5 mg/kg OTA than in those receiving 1 mg/kg. In general, histological changes in kidneys, liver, bursa and spleen were less pronounced in birds receiving OTA and toxin deactivator concomitantly. 5. Dietary OTA at 0.5 and 1 mg/kg adversely affects FCR, increases the serum liver enzymes and induces pronounced pathomorphological and histological changes in internal organs of broiler chicks. Co-administration of OTA with deactivator attenuated the harmful effects.     

Durantol - a phytosterol antifungal contributor from <Emphasis Type="Italic">Duranta repens</Emphasis> Linn. For organic Management of Sorghum Downy Mildew

Downy mildew of sorghum (DMS) has serious implications agronomically worldwide and to-date the search for a potent fungicide is a high priority and necessity. Phytochemicals have proven to be effective against various plant pathogens with minimal or no side effects. Duranta repens aqueous extract exhibited a promising potential as an organic fungicide for management of sorghum downy mildew (Peronosclerospora sorghi) in greenhouse conditions, at low concentration of 5 %. Activity guided bio-prospecting lead to the isolation of active principle which could control the DMS at as low as 0.1 % concentration. Spectral studies identified the bioactive contributor as a phytosterol namely 16-Hydroxy-8,10,13-trimethyl-1,2,8,10,12,13,14,15-octahydro cyclopenta [a] phenanthren-3-one, designated as Durantol. The results of microscopy exhibited the inhibition of conidial germ-tube growth by formation of bulb-like swellings at the tip, suggesting the mechanism of action of Durantol was via hampering the membrane integrity of the pathogen. Further, the same was virtually predicted using molecular docking for structure-activity relationship (SAR) against four best known membrane receptors namely 1-UDP-glycosyltransferases (UGT), cytochromes P450 (P450), oxidosqualene cyclase (OSC) and serine carboxypeptidase-like acyltransferase (SCPL), proposing that glycosylation onto the membrane would be a reason for inhibition and which is evident from atomic contact energy (ACE) values. The results of the study indicate that, organic management of airborne inoculum of downy mildew of sorghum is feasible and preferable, as compared to the use of chemical fungicides, considering human and environmental health concerns.

Open image in new window

Graphical abstract ?

     

Synthesis and anti-mildew activity of 5-(2-aroyl)aryloxymethyl-2-phenyl-1 ,3,4-oxadiazoles against downy mildew of pearl millet

A manipulatively simple, rapid, high-yielding and environmentally benign method for the integration of a heterocyclic ring, 1,3,4-oxadiazole, at the benzophenone nucleus has been achieved through intramolecular cyclization of substituted aroylaryloxyacetohydrazides to substituted 5-(2-aroyl)aryloxymethyl-2-phenyl-1,3,4-oxadiazoles under solventless 'dry' conditions using montmorillonite K10 clay and microwave irradiation. A comparison is made of the microwave-accelerated reaction with conventional heating conditions. Certain of the derivatives tested showed significant anti-mildew activity against Sclerospora graminicola (Sacc) Schroeter, the downy mildew pathogen of pearl millet.