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Fenofibrate, an anti-hyperlipidemic drug and its phase-I biotransformed metabolite fenofibric acid, was studied for COX-1 (PDB ID: 3N8Y) and COX-2 (PDB ID: 1PXX) inhibition potentials in silico and in vitro for their effects on human recombinant COX-2 enzyme isolated from a Baculovirus expression system in sf21 cells (EC 1.14.99.1) using a conventional spectrophotometric assay. Furthermore, the compounds were also screened for their anti-inflammatory potentials in vivo using carrageenan-induced paw oedema method in Wistar rats. The test compounds fenofibric acid, fenofibrate, and the standard drug diclofenac exhibited binding energies of − 9.0, − 7.2, and − 8.0 kcal mol−1, respectively, against COX-2 and − 7.2, − 7.0, and − 6.5 kcal mol−1, respectively, against COX-1. In in vitro studies, both the test compounds inhibited COX-2 enzyme activity. Fenofibric acid showed an IC50 value of 48 nM followed by fenofibrate (82 nM), while diclofenac showed an IC50 value of 58 nM. Furthermore, under in vivo conditions in carrageenan-induced paw oedema rodent model, fenofibric acid exhibited relatively potent anti-inflammatory activity compared with fenofibrate. Hence, we conclude that fenofibric acid and fenofibrate are not only anti-hyperlipidemic but also shows potent anti-inflammatory activity, which may have an additional impact in the treatment of diabetic complications, viz., hyperlipidemia and inflammation leading to atherosclerosis.

Sorghum (Sorghum bicolor) is an important cereal crop which is widely cultivated for food, fiber, forage, ethanol, and sugar production in semi-arid tropics with minimum inputs. At least 150 insects have been reported as pests of sorghum worldwide of which the major ones are shoot fly (Atherigona soccata), stem borer (Chilo partellus), shoot bug (Peregrinus maidis), aphids (Melanaphis sacchari), sorghum midge (Stenodiplosis sorghicola), head bug (Calocoris angustatus), head caterpillars (Helicoverpa, Eublemma, Pyroderces) and spider mites (Oligonychus spp.). The grain yields are generally low (500–800 kg/ha) mainly attributed to damages caused by these insect pests. This chapter provides compiled information on pest bionomics, damage symptoms, and economic losses in sorghum due to pests. Various management strategies adopted, viz., cultural, biological, host plant resistance, use of botanicals, and chemical management, are detailed. Recent advances in pest management, viz., marker-assisted selection, transgenics are also discussed along with some of the integrated pest management strategies adopted.

Sweet sorghum is a climate smart crop with multiple uses. The crop is susceptible to attack by the spotted stemborer, Chilo partellus (Swinhoe). This causes deadheart formation, leading to lodging of plants and consequent high economic losses. Lack of stable sources of resistance make any genetic enhancement through breeding difficult. We report a study to build up host plant resistance using transgenic technology by introducing two different classes of Bt genes (cry1Aa and cry1B) into two elite sweet sorghum genotypes of India (SSV84 and RSSV9). We devised tissue culture methods to suit the genotypes of our interest, SSV84 and RSSV9, and employed two methods of genetic transformation: the particle bombardment and in planta method of Agrobacterium. Modification of in vitro culture methods involved subculture every 3 days in the initial stages of culture and the use of precultured embryos as target tissues. For the in planta method, a floral dip for 1 h in Agrobacterium suspension supplemented with l-cysteine and Tween-20 was used. Sixteen transgenic events were generated; inheritance, integration and stable expression of the transgenes till the T4 generation were confirmed. The amount of Bt Cry1Aa protein at 25–30 days of growth ranged from 24.8 to 72.8 ng/g of fresh leaf tissue. We recorded 78.4 % larval mortality, reduced leaf damage (3.0 out of 9.0) and reduced feeding (41.0 %) over the controls in insect feed assays. Stable inheritance and expression in the in planta-derived transgenics are presented.

Thirty-two sweet sorghum genotypes were evaluated for resistance to shoot fly and stem borer during rainy seasons 2009–2012. The parameters viz., seedling vigour, glossiness, dead-hearts caused by shoot fly, stem borer, stem borer leaf damage score, stem borer stalk tunneling, stem borer exit holes and stem borer larvae/stalk were assessed for their contribution in imparting resistance to A. soccata and C. partellus. None of the traits considered could discriminate entries as resistant/ susceptible individually. In view of the complexity of interactions between A. soccata, C. partellus with sorghum, principal component analysis was applied considering seven parameters viz., seedling vigour, seedling glossiness, dead-hearts caused by shoot fly, stem borer, stem borer stalk tunneling, stem borer exit holes/stalk and larvae recovered/stalk. Two principal components were extracted explaining a cumulative variation of 84.6 %. PC1 and PC2 explained 69.5 and 15.1 % of the variations, respectively indicating that seedling vigour, glossiness, dead-hearts caused by both pests, stem borer exit holes/stalk were the most reliable parameters for characterization of multiple resistances to A. soccata and C. partellus. The sweet sorghum lines IS 5353, IS 18164, ICSV 93046, ICSV 700, GGUB 50 were classified as resistant to both the pests. The multiple resistant lines with durable resistance can be employed in future sweet sorghum breeding programs for enhancing levels of resistance to shoot fly and stem borer.

Sweet sorghum (Sorghum bicolor (L.) Moench) is an important bioenergy crop that has ability to produce both food (grain) and biofuel (from stalk juice). The objectives of the present investigation were (1) to assess the comparative performance of sweet sorghum experimental hybrids with open pollinated varieties (OPVs) for stalk yield, juice sugar quality traits, grain and bioethanol yields, and (2) to identify the best performing genotypes across the locations for both bioethanol and grain yields. Sixteen experimental sweet sorghum genotypes were evaluated during kharif season, 2007 at thirteen tropical Indian locations under dryland condition. Significant (P ≤ 0.05) differences were observed for stalk and sugar related traits. Fresh biomass varied from 39.0 to 67.0 t ha−1 and hybrids as a group produced 11.0 % more than OPVs. Millable stalk yield ranged from 29.4 to 46.5 t ha−1 among hybrids and OPVs with a mean of 40.2 t ha−1. Grain yield ranged from 1.14 to 2.25 t ha−1, and hybrids produced 38.0 % more grain yield than OPVs. Among all test genotypes, SPSSV30 alone recorded significantly superior juice °Brix, and total soluble sugars (TSS) than checks. Juice °Brix content has shown very strong positive correlations (R 2 = 0.7956, P ≤ 0.01) with TSS. In total sugar and bioethanol yields (range 1.66–2.53 t ha−1 and 925–1,440 L ha−1, res.), genotypes SPSSH 27, PAC52093 and SPSSH 24 in hybrid group, and SPSSV 20, SPSSV 15 and SPSSV 27 in OPV group were superior. Hybrids have recorded 10.0 and 18.0 % higher sugar and bioethanol yields, respectively than OPVs. The promising OPVs identified from this study could be the potential donors for further improvement of sweet sorghum for biofuel production. The results emphasized the importance of sweet sorghum hybrids over OPVs for stalk and bioethanol yields especially in the future climate change scenario.

Sorghum and millets are crucial to food, fodder, and nutritional security in arid and semiarid tracts of the world. Sorghum is vulnerable to several insect pests. Among them, shoot fly, spotted stem borer, greenbug, midge, and head bugs are the most important worldwide. The pearl millet and small millets are relatively less subjected to pest attack and are more susceptible to diseases though sporadic instances of insect attack are reported. However, stem borers and grain midge are of regular occurrence in pearl millet. White grubs in India and spike worms in West Africa are assuming importance. The chapter covers the resistance sources, resistance mechanisms, resistant traits, gene action governing the major traits, and biotechnological advances for the economically important pests in sorghum and millets. Several genotypes resistant to shoot fly and to a lesser extent to stem borer, midge, aphids, and shoot bug have been identified. Development of multiple pest- and disease-resistant cultivars is emphasized.

In the present investigation, thermophilic fungus Rhizomucor pusillus was used to study biotransformation of antihelmintic drug albendazole to produce its active metabolite, albendazole sulfoxide and novel metabolites of commercial interest. A two-stage fermentation procedure was followed for biotransformation of albendazole. The transformation was identified and structures were confirmed by high-performance liquid chromatography and liquid chromatography-tandem mass spectrometry analysis. Four metabolites albendazole sulfoxide, the active metabolite, albendazole sulfone, N-methyl metabolite of albendazole sulfoxide, and a novel metabolite were produced. The study demonstrates the biotransformation ability of thermophilic fungus R. pusillus NRRL28626 in the production of, the active metabolite of albendazole which has industrial and economic importance, other metabolites and a novel metabolite in an ecofriendly way.

Screening-scale studies were performed with 26 fungal cultures for their ability to transform the anti-inflammatory drug meloxicam. Among the different fungi screened, a filamentous fungus, Cunninghamella blakesleeana NCIM 687, transformed meloxicam to three metabolites in significant quantities. The transformation of meloxicam was confirmed by high-performance liquid chromatography (HPLC). Based on the liquid chromatography-tandem mass spectrometry (LC-MS/MS) data, two metabolites were predicted to be 5-hydroxymethyl meloxicam and 5-carboxy meloxicam, the major mammalian metabolites reported previously. A new metabolite was produced, which is not detected in mammalian systems. Glucose medium, pH of 6.0, temperature of 27 degrees , 5-day incubation period, dimethylformamide as solvent, and glucose concentration of 2.0%were found to be suitable for maximum transformation of meloxicam when studied separately. It is concluded that C. blakesleeana can be employed for biotransformation of drugs for production of novel metabolites.

Coconut rhinoceros beetle ( Oryctes rhinoceros L.) is the major constraint in the production of coconut across the Andaman & Nicobar Islands. To suppress the pest population, baculovirus was released for the first time in 1987 at four locations in South Andaman, which brought down palm damage to insignificant levels within 48 months of release. However, during 1999–2000 large-scale felling of old coconut palms to be replaced with fresh ones by the Andaman Plantation Development Corporation (APDC) resulted in a fresh outbreak of coconut rhinoceros beetle. This warranted release of virus through infected beetles to suppress the pest population. A dose of 130 μg crude virus preparation (CVP)/beetle ensured optimum longevity coupled with low fecundity for efficient dispersal of virus. Release of such pre-infected beetles (795) at five locations in South Andaman resulted in over 90% reduction in palm damage within 23 months of release. Examination of experimental and adjoining palm groves confirmed the prevalence of virus among the sampled beetle population, which registered three-fold increases since the release of virus. There was a drastic reduction to the extent of 91% in the occupancy. However, the recent tsunami in December 2004 in addition to destroying 5000 ha of coconut area has generated huge amounts of organic matter, which has resulted in the rhinoceros beetle outbreak. Augmentation of virus is suggested for effective management of the pest.

Specific inhibitors of Cytochrome P4502C9 enzyme (CYP2C9) viz. clopidogrel, fenofibrate fluvoxamine and sertraline at concentration of 50, 100, 150 and 200 µM were employed to investigate the nature of enzyme involved in bioconversion of meloxicam to its main metabolite 5-OH methyl meloxicam by Cunninghamella blakesleeana. Virtual screening for interaction of specific CYP2C9 inhibitors with human CYP2C9 enzyme was performed by molecular docking using Auto dock vina 4.2 version. The in silico studies were further substantiated by in vitro studies, which indicated fenofibrate to be a potent inhibitor of CYP2C9 enzyme followed by sertraline, clopidogrel and fluvoxamine, respectively. Two-stage fermentation protocol was followed to study metabolism of meloxicam and its inhibition by different CYP2C9 inhibitors. Meloxicam metabolites were identified using HPLC, LC–MS analysis and based on previous reports, as 5-OH methyl meloxicam (M1), 5-carboxy meloxicam (M2) and an unidentified metabolite (M3). All the inhibitors tested in the study showed a clear concentration dependent inhibition of meloxicam metabolism. The results suggest that the enzymes involved in metabolism of meloxicam in C. blakesleeana are akin to mammalian metabolism. Hence, C. blakesleeana can be used as a model organism in studying drug interactions and also in predicting mammalian drug metabolism.

A study dealing with ecological sustainability of plantation based land use initiated in 1991 in a 19 yr old coconut plantation consists of growing certain leguminous crops like Atylosia, Pueraria, Centrosema and Calopogonium as soil cover in separate plots with lemon grass as live bounds. These cover crops are grown during the rainy season and incorporated into the soil towards the end of the monsoon every year. The effect of such cover crops on soil microbial counts (total counts, fungi, actinomycetes and bacteria), biomass C, organic C, total N and on the activity of enzymes like urease, amidase, L-glutaminase, aryl sulphatase and dehydrogenase was determined in soils (Ap horizon) collected from these plots after 5 years. Soils with cover crops registered significantly higher microbial biomass, biomass C, organic C and total N compared to control. Consequently, all the enzymes were activated to different degrees in soils with cover crops. Significant and positive relationships of enzyme activities with organic C, mineral N and total N suggested that growing cover crops, increased C turnover and N availability and therefore, provided a conducive environment for microbial proliferation, enzyme synthesis and accumulation in the soil matrix. Einflus von Leguminosen als Deckfrucht auf mikrobielle und ausgewahlte Enzymaktivitaten in Boden einer Plantage Zur Untersuchung der okologischen Nachhaltigkeit der Bodennutzung im Plantagenanbau wurde 1991 in einer 19 Jahre alten Kokosplantage ein Versuch mit Leguminosen als Deckfrucht auf getrennten Parzellen und mit Lemongrass als Trennstreifen angelegt. Die Deckfruchte wuchsen wahrend der Regenzeit und wurden gegen Ende des Monsuns alljahrlich eingearbeitet. Nach 5 Jahren wurde in Ap-Proben die Wirkung der verschiedenen Deckfruchte auf Mikroorganismen (Gesamtzahlen, Pilze, Actinomyceten und Bakterien), Biomasse-C, org. C und Gesamt-N und auf die Enzymaktivitaten wie Urease, Amidase, L-Glutaminase, Arylsulfatase und Dehydrogenase untersucht. Boden mit Deckfrucht wiesen signifikant hohere Werte bei mikrobieller Biomasse, Biomasse-C, org. C sowie mineralischem und Gesamt-N auf als die Kontrolle. Als Folge waren unter Deckfrucht alle Enzymaktivitaten — in unterschiedlichem Grade erhoht. Signifikante positive Korrelationen von Enzymaktivitaten mit organischem C, mineralischem und Gesamt-N sind Anzeichen dafur, das unter den wachsenden Deckfruchten Kohlenstoffumsatz und N-Verfugbarkeit gunstig beeinflust waren und damit mikrobielles Wachstum und Enzymsynthese und -anreicherung gefordert wurden.

A fertilizer management study involving incorporation of poultry manure, farm yard manure, sesbania and gliricidia into soils of a rice-rice system was initiated in May 1993. In order to determine the effects of organic manure incorporation on soil microbial biomass and enzyme activity, soils were collected from the respective plots at the end of the second rice crop in February 1996. and were incubated with and without the respective organic manure at the rate of 15 Mg ha−1 at 25°C, under submergence. The total viable microbial counts, bacteria, actinomycetes, N flush, biomass C and activities of urease, amidase, acid and alkaline phosphatase, dehydrogenase and L-glutaminase were determined after 60 days of incubation. Soils freshly amended and soils previously amended with organic manures registered significantly greater microbial biomass and enzyme activity than the unamended control. The microbial biomass and enzyme activity, however, varied with the type of organic manure incorporated into the soil. Except for acid phosphatase, which showed slight inhibition, all the other enzymes were activated to different degrees by organic manure incorporation. A significant and positive relationship of enzyme activity with organic C and total N suggested that the addition of organic manure to soils increased C turnover, N availability and microbial activity which in turn led to greater enzyme synthesis and accumulation in the soil matrix.

Different fungi viz. Aspergillus niger NCIM 589, A.ochraceous NCIM 1140, Cunninghamella blakesleeana NCIM 687, C. echinulata NCIM 691, Rhizopus stolonifer NCIM 880, Mucor rouxi MTCC 386, Trichothecium roseum NCIM 1147 were screened for their potential to biotransform anti-hyperlipidemia and anti-hypertriglyceridemia drug, fenofibrate to fenofibric acid, the active metabolite and other mammalian metabolites. Among the fungi screened C. blakesleeana transformed fenofibrate to fenofibric acid and other three metabolites. HPLC, LC-MS/MS analysis and previous reports confirmed the transformation of fenofibrate and metabolites as fenofibric acid (M1), reduced fenofibric acid (M2), reduced fenofibric acid taurine conjugate (M3), reduced fenofibric acid ester glucuronide (M4), the mammalian metabolites reported previously. The results proved the potential of C.blakesleeana NCIM 687 in the production of mammalian phase I (M1 and M2) and phase II (M3 and M4) metabolites in large quantities and also as an in vitro model for drug metabolism studies.

Screening scale studies were performed to biotransform anthelmintic drug albendazole by using twelve bacterial strains representing six genera and five actinomycetes cultures. Among the cultures studied, Bacillus subtilis MTCC 619, Escherichia coli MTCC 118 and Klebsiella pneumoniae MTCC 109 could transform albendazole to one metabolite whereas, Enterobacter aerogenes NCIM 2695, Klebsiella aerogenes NCIM 2258, Pseudomonas aeruginosa NCIM 2074 and Streptomyces griseus NCIM 2622 could transform albendazole into two metabolites in significant quantities. The transformation of albendazole was identified by HPLC. Based on LC-MS-MS data, the two metabolites were predicted to be albendazole sulfoxide (M1) and albendazole sulfone (M2), the major mammalian metabolites reported previously. Since M1 is active metabolite, the results prove the versatility of microorganisms to perform industrially attractive chemical reactions.