Designing of promising Tromethamine-Diflunisal-Pyrrole combinations based on COX binding, drug-properties and safety

Gastric issues that accompany the use of NSAIDs (Non-steroid anti-inflammatory drugs) are always a serious global concern. The inhibition of the Cycloxygenase enzyme (COX) limits the prostaglandin synthesis and thereby facilitates the control of pains, inflammation etc. But this creates gastric issues due to the reduction of mucin formation in the stomach. The present work was performed to create a modification in the structure of NSAID drug Diflunisal, to reduce the gastric effect of acidic moiety in the structure and elevate the overall biological properties. The drug Tromethamine, a base used in acidosis treatment was substituted to reduce the acidic issues. The heterocyclic compound pyrrole was substituted to elevate the properties. Neutral, salt, amide and ester combinations of Tromethamine-Diflunisal were designed, optimized and docked to the crystal structures of COX-1 (PDB ID: 6Y3C) and COX-2 (PDB ID: 5IKR) enzymes, using PyRx software. The combinations with lower COX-1 and COX-2 binding energies relative to Diflunisal were noted. It was analysed if the combinations of Diflunisal, Tromethamine and pyrrole lowers drug-properties or induce toxicities. Pyrrole substitution at position R4 was not found favourable for COX binding. Among the favourable combinations, DF19 is the Diflunisal-Pyrrole-Tromethamine combination, equally favourable for binding to COX targets

Occurrence of teleomorphic phase of Colletotrichum gloeosporioides sensu lato, the incitant of black pepper anthracnose

Anthracnose caused by Colletotrichum gloeosporioides sensu lato, the ascomycetous pathogen is a major constraint in black pepper cultivation. In the present study, surveys carried out in black pepper cultivating regions of Karnataka, India revealed the prevalence of anthracnose disease manifested as diverse array of foliar symptoms. An atypical foliar symptom was also noticed in the black pepper nurseries, characterized by grayish necrotic lesions with brown-blackish margins and randomly distributed blackish structures of pin-head size in the lesion area manifested particularly on the older leaves. The pin-head structures produced orangish exudation embedded with asci, ascospores and perithecia, when incubated under high humid conditions. Typical anthracnose symptoms were developed on susceptible host in pathogenicity studies and subsequent isolation yielded two distinct colonies designated as black and orange. The perithecia were induced artificially under in vitro conditions, which retained fertility and infectivity more than three months. Alternation of generation was observed when the perithecia were cultured on potato dextrose medium which resulted in the formation of acervuli with abundant conidiation. The results of present investigation shed light into the occurrence and potential role of perithecial (teleomorphic) phase in the survival of C. gloeosporioides s. l. infecting black pepper

Harnessing ornamental fisheries resources for sustainable growth and development: A trade perspective from Kerala, India

Ornamental fish trade has gained paramount importance with more than 125 countries involved in the freshwater and marine fishes. The global trade is estimated to be around US $ 450 million registering a growth rate of ten percent since 2001. Asia caters up to 60 per cent of the global trade while India stands with a dismal 0.9 per cent with a portfolio of 30-35 fresh water species. The ornamental fish resources of Kerala has huge potential with untapped and unexploited resources. However the performance of the sector is not worthy and production is much below the demand. The SWOL analysis - Strengths, Weaknesses, Opportunities and Limitations analysis - is done to analyse the status of ornamental fish industry in Kerala. The results indicated that good export market, high demand, availability of under-utilized marine resources, potential for rural development, low cost effort, efficiency of ornamental fish marketers, institutional support for development and promotions were the major strengths. Dependence on wild caught species, inadequate data on resources, wastage of resources, unwillingness towards marine fishes, lack of trained/ skilled manpower and organized trade, lack of adept technologies, poor marketing facilities, backwardness in international market, weak market image and lack of fishing regulations were the major inherent weaknesses. The major opportunities were enhancement of species portfolio, increasing market value, less capital intensive, high popularity and demand, breeding and culture of indigenous fishes, faster market growth, entry to new market destinations, increased awareness of international buyers and support of government. Technological backwardness, technology transfer, insufficient awareness programmes, adverse government policies, competitions from neighboring countries, sustainability of resources and drastic drop in fish prices were the major limitations. The study suggests concerted efforts by the different stakeholders to enhance the production of the sector

Screening small cardamom (Elettaria cardamomum Maton) field gene bank accessions for phenotypic characters, yield potential and disease resistance

Evaluation of 117 field gene bank accessions of small cardamom for phenotypic characters along with yield potential and disease resistance (rhizome rot and leaf blight) at ICAR-Indian Institute of Spices Research Regional Station, Appangala revealed significant variation with respect to phenotypic characters. The highest plant height (350 cm) and number of bearing tillers (36.4) were recorded in the accessions, field gene bank (FGB) 65 and FGB 16, respectively. The highest fresh weight of capsules (399.61 g) and maximum number of capsules (244.20) plant-1 were recorded in the accession, FGB 13. Further, based on screening for disease resistance, 35 and 15 accessions of cardamom were identified as resistant to leaf blight and highly resistant to rhizome rot, respectively. Based on the multivariate cluster analysis, 117 FGB accessions were classified into 5 clusters viz., clusters 1 and 2 encompassing equal number of accessions (44), cluster 3 with one accession (FGB 10), clusters 4 and 5 with 8 and 20 accessions, respectively

Ectropothecium sodale (Hypnaceae, Bryophyta) — New to India from the peninsula

The moss Ectropothecium sodale is added here to the flora of India from the peninsular part of the country. A brief description with illustrations and a photographic plate are provided

Development of diagnostic assays for rapid and sensitive detection of Phytophthora infecting major spices and plantation crops

Phytophthora, the ubiquitous stramenopile phytopathogen is a major threat to several economically important horticultural crops including spices and plantation crops. Trans-seasonal survival of Phytophthora in plant debris and soil continuum has considerable epidemiological significance as the quiescent propagules often serve as primary foci of infection with inherent potential to trigger epiphytotics in the succeeding season favoured by conducive environmental conditions. Hence, early and rapid detection of over summering propagules is highly imperative to manage Phytophthora induced diseases efficiently and economically. Twelve isolates representing different species of Phytophthora (P. capsici, P. tropicalis, P. palmivora. P. citrophthora and P. meadii) representing hosts such as black pepper, cardamom, nutmeg, coconut, arecanut and cocoa were used to develop nucleic acid-based diagnostic tools viz., polymerase chain reaction (PCR), real-time PCR, loop-mediated isothermal amplification (LAMP) and real-time LAMP. Phytophthora genus-specific primers were designed from the conserved region of nuclear ribosomal DNA. Each of the assays was specific and detected different species of Phytophthora and not other pathogens (Rhizoctonia solani, Pythium vexans, Fusarium oxysporum and Colletotrichum gloeosporioides) and plant samples. Sensitivity assays indicated that, real-time PCR detected Phytophthora upto 1.3 fg, followed by LAMP (13 fg) and PCR (13 pg)

Epidemiological parameters to delineate weather-disease interactions and host plant resistance against leaf blight in small cardamom (Elettaria cardamomum Maton)

Small cardamom, the versatile spice of Zingiberaceae is cultivated in diverse agro-climatic regions of India especially in South India. Leaf blight incited by Colletotrichum gloeosporioides sensu lato is one among the major challenges encountered across different cardamom growing tracts. In the present investigation, epidemiology of cardamom leaf blight was studied and an attempt was made to decipher the resistant nature of Malabar, Mysore and Vazhukka genotypes based on epidemiological parameters. The average percent disease index recorded in Malabar, Mysore and Vazhukka varied from 23.41 to 27.72, 18.79 to 20.34 and 18.74 to 20.38, respectively. The disease exhibited a positive correlation with respect to Tmax and Tmin in all the genotypes, however, significant correlation was observed only in Malabar and Mysore with respect to Tmax. Whereas, rainfall and rainy days had negative correlation with leaf blight in all genotypes however found to be non-significant. The average infection rate was maximum (0.000429) in Malabar, whereas it was 0.000124 and 0.000186 in Mysore and Vazhukka, respectively. The area under disease progress curve registered the highest for Malabar (8814.15) and lowest in Vazhukka (6531.02) while, Mysore type recorded 6612.96 indicating that, Vazhukka and Mysore types might posses horizontal resistance and Malabar with vertical resistance. In the light of above results, plant protection measures could be scheduled based on the take-off level and genotypes with horizontal resistance could be promising candidates in resistance breeding programmes

Structures of FOX-4 cephamycinase in complex with transition-state analog inhibitors

Boronic acid transition-state analog inhibitors (BATSIs) are partners with β-lactam antibiotics for the treatment of complex bacterial infections. Herein, microbiological, biochemical, and structural findings on four BATSIs with the FOX-4 cephamycinase, a class C β-lactamase that rapidly hydrolyzes cefoxitin, are revealed. FOX-4 is an extended-spectrum class C cephalosporinase that demonstrates conformational flexibility when complexed with certain ligands. Like other β-lactamases of this class, studies on FOX-4 reveal important insights into structure–activity relationships. We show that SM23, a BATSI, shows both remarkable flexibility and affinity, binding similarly to other β-lactamases, yet retaining an IC50 value < 0.1 μM. Our analyses open up new opportunities for the design of novel transition-state analogs of class C enzymes

Identification of bacterial pathogens in dry bovine udder and their antimicrobial susceptibility

Mastitis is a multi-etiological production disease of dairy cows worldwide. The likelihood of developing clinical mastitis in subsequent calving is enhanced by intramammary infections with pathogens during the late dry and post-calving period. There is an increase in the occurrence of intramammary infections during early and late dry period. Thirty apparently healthy, pregnant cross-bred dairy cows were screened for the presence of contagious mastitis pathogens in the secretions taken after 48 h of cessation of milking. A total of 118 bacterial isolates were obtained from the secretions collected from 108 quarters, and identified using morphological and cultural characteristics. Among them, 50.8 per cent were coagulase negative Staphylococci (CNS), 16 per cent were coagulase positive Staphylococci (CPS) and 27.1 per cent were Streptococci isolates. Micrococci and E. coli constituted 2.5 per cent each and Klebsiella spp. formed 0.8 per cent of the total isolates obtained. The CNS isolates identified included 22 S. chromogens, 14 S. xylosus, 12 S. saprophyticus, six S. hominis and S. epidermidis each. Among the CPS isolated 11.8 per cent were S. aureus and 4.2 per cent were non-aureus coagulase positive Staphylococcus which included three S. hyicus and two S. pseudointermedius. Molecular confirmation of S. aureus, CNS isolates, St. agalactiae were done by targeting nuc, cns and 16SrRNA gene respectively. Identification of bacterial pathogens that are present during dry period can help in formulating an effective dry cow therapy. Antibiogram studies of the isolates obtained were done using in vitro antibiotic sensitivity testing method