HFIP-mediated C-3-alkylation of indoles and synthesis of indolo[2,3-b]quinolines & related natural products.

An expeditious metal free C-3 alkylation of indoles and its NIS-mediated deviation to indolo[2,3-b]quinolines is reported. This protocol, executed in aqueous HFIP has broad substrate scope and is well inclined towards the ideas of sustainable chemistry. Applications of these strategies in accessing bioactive natural products like vibrindole, norcryptotakeine, neocryptolepine and indenoindolone scaffolds has also been demonstrated.

Micelle-mediated synthesis of quinoxaline, 1,4-benzoxazine and 1,4-benzothiazine scaffolds from styrenes.

A range of heterocycles based on quinoxalines, 1,4-benzoxazines and 1,4-benzothiazines have been accessed from styrenes by reacting them with benzene-1,2-diamine, 2-aminophenol and 2-aminothiophenol respectively in micellar medium. This reaction occurring in a less explored cetylpyridinium bromide (CPB) micellar medium operates in the presence of NBS through a tandem hydrobromination-oxidation cascade, converting styrenes to phenacyl bromides. Its subsequent nucleophilic addition with aromatic 1,2-dinucleophiles and further transformations led to the formation of heterocyclic constructs. The locus of the reaction site was confirmed through NMR studies and the types of interactions between the CPB and solubilizates were established by DFT calculations.

Immunological and molecular diagnostic techniques in fish health: present and future prospectus.

Fish health management is critical to aquaculture and fisheries as it directly affects sustainability and productivity. Fish disease diagnosis has taken a massive stride because of advances in immunological and molecular diagnostic tools which provide a sensitive, quick, and accurate means of identifying diseases. This review presents an overview of the main molecular and immunological diagnostic methods for determining the health of fish. The immunological techniques help to diagnose different fish diseases by detecting specific antigens and antibodies. The application of immunological techniques to vaccine development is also examined in this review. The genetic identification of pathogens is made possible by molecular diagnostic techniques that enable the precise identification of bacterial, viral, and parasitic organisms in addition to evaluating host reactions and genetic variation associated with resistance to disease. The combination of molecular and immunological methods has resulted in the creation of novel techniques for thorough evaluation of fish health. These developments improve treatment measures, pathogen identification and provide new information about the variables affecting fish health, such as genetic predispositions and environmental stresses. In the framework of sustainable fish farming and fisheries management, this paper focuses on the importance of these diagnostic techniques that play a crucial role in protecting fish populations and the aquatic habitats. This review also examines the present and potential future directions in immunological and molecular diagnostic techniques in fish health.

Assessing ecosystem health: A preliminary investigation of the gosikhurd dam ecosystem structure and functioning, an appraisal based on ecological modelling, India.

This study aims to comprehensively understand the Gosikhurd Dam ecosystem (GDE) ecosystem by employing the Ecopath with Ecosim software (version 6.6.5) to construct a trophic mass balancing model. This model consisted of 16 functional groups of organisms, and their interactions and trophic levels were explored. The study focuses on various performance indicators to assess the ecosystem's maturity and complexity. To achieve these objectives, monthly fish samples were collected from June 2022 to May 2023. Performance indicators such as the connectance index (CI), system omnivory index (SOI), Finn's cycling index (FCI), mean path length (FML), ascendency, overhead, and Shannon diversity index were calculated to assess ecosystem maturity and complexity. The Finn's cycling index (FCI) and the mean path length (FML) were calculated as 1.81 and 2.20, respectively, indicating the ecosystem's responsiveness to environmental changes and overall system health and stability. Ascendency and overhead values were also analysed, with ascendency being relatively higher (41.58%), reflecting a system that utilises less than half of its total capacity. The overhead value (58.42%) indicated that the ecosystem is relatively stable and capable of adapting to external perturbations. Furthermore, the Shannon diversity index was 1.67, illustrating less diversity and validating the ecosystem's immaturity. The study identifies critical species and their roles in shaping the ecosystem dynamics, highlighting the importance of zooplankton, zoobenthos, and tilapia as keystone species. These indices propound that GDE is in its developmental stage and lacks complexity compared to mature ecosystems. The findings provide valuable insights into the current state of the ecosystem and can guide future management and conservation efforts.

Indeno-Annulation of o-Formyl-Ynones, o-Bis-Ynones, and p-Bis-o-Formyl-Ynones with Dimethyl Acetone-1,3-Dicarboxylate: One Flask Cascade Synthesis of Functionally Endowed 9-Fluorenols and Indeno[1,2-b]fluorenols.

A mild, scalable, one-pot access to multifunctional 9-fluorenols from o-formyl-ynones and o-bis-ynones on reaction with dimethylacetone-1,3-dicarboxyate through tandem Michael addition-Aldol condensation cascade has been conceptualized and executed. The scope and utility of this synthetic approach have been further amplified for one-pot entry into functionally enhanced, higher order fluorenols like pentacyclic indeno[1,2-b]fluorene-6,12-diols and further to indeno[1,2-b]fluorene-6,12-diones through the implementation of "double indeno-annulation" tactic on p-bis-o-formyl ynones and dimethylacetone-1,3-dicarboxylate. Besides several green attributes, the current approach is also compatible with the emerging time and energy economy features and is a swift gateway to build complexity.

A micelle-mediated approach enables facile access to bridged oxabicyclo[n.3.1]alkene scaffolds.

Oxabicyclo[n.3.1]alkene scaffolds present in a diverse range of complex natural products have been accessed by reacting 2-cycloalkenones with 1,3-cycloalkadiones in a micellar medium. This reaction occurring in a micellar confinement environment operates through a Michael addition/enolization/oxygen addition cascade to furnish highly functionalized constructs using a sustainable organic synthesis protocol. NMR analysis confirms that the locus of the solubilizates is within the palisade and stern regions of the micellar cavity.

Micelle-guided Morita-Baylis-Hillman reaction of ketones in water.

A novel Morita-Baylis-Hillman reaction employing electron-deficient alkenes like acrylonitrile with a wide range of aryl and aliphatic ketones using cooperative catalysis in micellar media has been delineated. This transformation executed in water under mild reaction conditions in a confined environment of micelles is aligned to the ideas of sustainable and green chemistry. The site of the reaction was established by incisive proton NMR studies in the palisade region of the micellar assembly. This study is expected to encourage the use of micellar catalysis for energetically less favorable chemical reactions.

Polyphenolics, antioxidant characterization and DNA barcoding of Kala zeera [Bunium persicum (Boiss.) Fedtsch] through multiple barcode analysis to unravel best barcode combination.

BACKGROUND: Kala zeera [Bunium persicum (Boiss.) Fedtsch] is one of the important spice crops of North Western Himalayas with lot of medicinal and culinary values. In spite of having great importance, this crop is under the threat of extinction due to loss of habitat and lack of awareness. The limited availability of the seeds has ultimately increased the economic value of this spice. The upmarket of Kala zeera leads to its adulteration with other black seeds and cumin seeds. The present investigation was undertaken to evaluate polyphenolics and antioxidant properties of Kala zeera genotypes collected from North Western Himalayas and to develop DNA barcodes that can ensure their purity and can also guide in conservation of selected Kala zeera germplasm lines. METHODS AND RESULTS: Various locations of North Western Himalayas were explored for collecting 31 diverse germplasm lines of Kala zeera. The collected germplasm was maintained at our experimental stations during 2019-2020 and 2020-2021. These genotypes were evaluated for different seed traits and the methanolic extract from Kala zeera seeds was examined for total phenolic content, total flavonoid content, antioxidant activities by DPPH and FRAP. The results revealed significant variation in seed traits, polyphenolic content and antioxidant properties. 100 seed weight ranged from 0.05 to 0.35 g, TPC ranged from 7.5 to 22.56 mg/g, TFC ranged from 0.58 to 4.15 mg/g, antioxidant properties DPPH ranged from 168 to 624.4 µg/ml and FRAP ranged from 0.72 to 6.91 mg/g. Further, three different barcodes (ITS, rbcL and psbA-trnH) were used to reveal the authenticity of selected Kala zeera. MEGA 5 software was used for clustering and the barcodes did clustering based on geographical distribution of Kala zeera germplasm. CONCLUSION: Based on molecular barcoding, best barcode combination was identified that may discriminate the Kala zeera germplasm vis-a-vis can authenticate their purity. Moreover, the identified DNA barcodes will have significant role in studying the evolutionary biology of Bunium species and will be important for designing a strategy to conserve the selected Kala zeera germplasm lines. The identified genotypes with high phenolic content and antioxidant activity can further be utilized in Kala zeera breeding programmes.

Platanic Acid-Aryl Enones as Potential Anticancer Compounds: Synthesis and Biological Profiling against Breast, Prostate and Lung Cancer Cell Lines.

A series of rationally designed platanic acid-based compounds derived from naturally occurring betulinic acid were synthesized through a sequence of Lemieux-Johnson oxidation and Aldol condensation reaction. All the compounds were screened for cytotoxicity against a panel of human cancer and normal cell lines using MTT assay. From the biological data, it was observed that some of these semi-synthetic congeners exhibited potent biological profiles compared to platanic acid. One of the compounds with the p-tolyl substitution was found to be most active in this study, and its cytotoxicity against two of the cell lines, MDA-MB 231 and A-549 were in tune with the standard compound, 5-fluorouracil.

Conceptualization and Synthesis of the First Inosito-Inositol (Decahydroxydecalin, DHD): In†silico Binding to ß-Amyloid Protein.

Previously unknown entities in the form of 1,2,3,4,5,6,7,8,9,10-decahydroxydecalins (DHDs) have been conceptualized and the first member of this class, an inosito-inositol, has been synthesized from aromatic hydrocarbon naphthalene following a flexible strategy that is amenable to diversity creation. The DHD accessed here has been subjected to preliminary in silico evaluation with Aß and may hold some promise in Alzheimer's disease therapeutics.

Thyroid hormone levels and Thyroid Hormone Levels and Ultrasonographic Changes in the Thyroid Gland of Patients on Long-Term Lithium Treatment for Affective Disorders: A Controlled Study.

BACKGROUND: Although lithium is known to cause thyroid dysfunction and increased thyroid gland volume, clinical examination and biochemical assessment are fundamental to thyroid workup of patients on lithium treatment. We aimed to determine thyroid gland volume and the Thyroid hormone levels of patients who have been receiving lithium treatment for affective disorders in comparison to voluntary healthy controls. METHODS: This was a cross-sectional, hospital-based observational study which was performed in 43 patients on long-term lithium treatment for bipolar disorder, major depressive and schizoaffective disorders. Patients with documented continuous and adequate serum lithium levels for more than or equal to 6 months recruited consecutively underwent the ultrasonographic examination of the thyroid gland. Ultrasonographic examinations were also done in all gender- and age-matched healthy controls. All cases and controls underwent biochemical thyroid function tests. RESULTS: There were no statistically significant differences in gender (P = 0.198; Chi-square = 1.654) of cases and controls. Most of the cases were married, maximum number of them unemployed and belonged to the lower socioeconomic status. Total thyroid volume was significantly greater in the lithium-treated group than the controls (9.40 ± 1.41 vs. 4.79 ± 0.45). Clinical inspection and palpation only detected goiter in six (n = 6, 13.95%) of patients on lithium and none among controls. The mean triiodothyronine, mean thyroxine, and mean scores for thyroid-stimulating hormone were significantly increased in patients receiving lithium therapy as compared to controls. CONCLUSION: It would seem wise from a clinical point of view to include ultrasonographic examination of the thyroid gland as part of the standard thyroid workup before initiating lithium treatment.

Dimethoate Induced Behavioural Changes in Juveniles of Cyprinus carpio var. communis under Temperate Conditions of Kashmir, India.

The present study was designed to investigate acute toxicity of dimethoate on juvenile Cyprinus carpio var. communis. Fishes weighing 10 ± 2 gms were selected and mortality data was statistically evaluated by Finney's Probit Method. The 96-hour LC50 value for Cyprinus carpio was found as 1.1 ppm in static bioassay system. Mean values of physicochemical parameters of aquarium waters determined during bioassay depicted slight variation indicating that the mortality in aquarium fishes occurred due to pesticide exposure and not suffocation. Lab. temperature ranged from 12 to 13°C; water temperature ranged from 11 to 12°C; dissolved oxygen ranged from 3.90 to 4.56 mg/L; pH ranged from 6.90 to 7.05; total dissolved solids ranged from 2.66 to 3.0 × 10(3) mg/L, while CO2 remained at a constant value of 2.0 mg/L. The fishes elicited various behavioural responses such as uncoordinated movements, convulsions, excessive mucus secretion, and imbalanced swimming which ended in a collapse to the bottom of the aquarium. Prior to death, the clinical signs like scale erosion, pale body colour, and hemorrhagic patches over the body were noticed which became more vivid up to the termination of experiments. Results of the study indicate potential toxicity of dimethoate in fingerlings of common carp for which the natural waterbodies must be continuously monitored to reduce its impact across food chains.

Mitochondrial DNA variability to explore the relationship complexity of Schizothoracine (Teleostei: Cyprinidae).

Despite numerous studies on the taxonomy of a highly complex group of schizothoracine (snow trouts), with over five recognized species from Kashmir, India (Schizothorax niger, Schizothorax esocinus, Schizothorax plagiostomus, Schizothorax curvifrons and Schizothorax labiatus) based on traditional morphological data, the relationships between these species is poorly understood and the taxonomic validity is still under debate. To resolve the evolutionary relationships among these species, we sequenced mitochondrial fragments, including 16Sr RNA, Cytb and the D-loop. Separate analyses of 16S and Cytb showed intermixing of the species and 16S was found more conserved than Cytb. The D-loop was found highly variable and showed length variation between and within species. Length variation was observed in di-nucleotide (TA)n microsatellite repeats with a variable number of repeat units (n = 7-14) that did not show heteroplasmy. Central conserved sequence blocks (CSBs) in D-loop sequences were found comparable to other vertebrate species. All phylogenetic reconstructions recovered the focal taxa as a monophyletic clade within the schizothoracines. Analyses with combined mitochondrial data sets showed close genetic relationships of all the five species. In addition to a close relationship between S. niger and S. curvifrons, two distinct groupings of S. ecoscinus and S. plagiostomus were supported by all the analyses. This study gives an insight into molecular phylogeny of the species and improves our understanding of historical and taxonomic relationships derived from morphological and ecological studies.

Annulation reactions of allenyl esters: an approach to bicyclic diones and medium-sized rings.

A flexible approach to construct sterically congested bicyclo-alkenedione frameworks is reported. Under the action of potassium carbonate, α-sulphonyl cycloalkanones are added to functionalized allenyl esters, leading to a lactone intermediate that is subsequently reduced to initiate an intramolecular aldol cyclization to [3.2.1], [3.3.1], and [4.3.1] bicycles. Oxidation then affords bicyclic diones in good three-step yields. Under exceptionally mild conditions, these bicycles are converted to highly functionalized medium-sized rings through a Grob-type fragmentation.

Metal free stereoselective synthesis of functionalized enamides.

An efficient and expeditious DABCO-mediated synthesis of functionalized enamides from alkenes is delineated. The reaction proceeds through an unprecedented cascade involving an Aza-Michael addition/α-bromination/elimination and a Morita-Baylis-Hillman type reaction to generate functionalized enamides in a regio- & stereoselective fashion.

Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation.

A diverse range of 9-substituted 1,8-dioxohexahydroxanthenes was conceptualized and synthesized through a TFA-mediated approach in near quantitative yields without the use of column chromatography. From a series of 25 compounds, we found that compounds 14c and 14r exhibited promising anti-tuberculosis potential against avirulent and virulent strains of Mycobacterium tuberculosis with a Minimal Inhibitory Concentration (MIC) of 8 µg ml-1, achieving 99% bactericidal activity at the same concentration. This series of compounds was found to be inactive against common Gram-positive and Gram-negative pathogens, indicating that the activity is mycobacteria-specific. Since the strategies for treating tuberculosis employ a combinatorial therapy, we tested and observed that the two lead compounds displayed synergistic behavior with known anti-TB drugs (ATDs) and a significant (16-32 fold) decrease in MIC values of both leads was observed in combination with either RIF or INH. Interestingly the lead molecule 14c displayed only time-dependent kill kinetics and sterilized the whole culture of Mycobacterium tuberculosis H37Rv in just 48 hours.

Gastrointestinal parasites of the wild ungulates (Mammalia: Cetartiodactyla) in the Hemis National Park, Ladakh, India.

We evaluated the gastrointestinal parasitic prevalence and intensity of wild ungulates in the Hemis National Park of Ladakh by examining their fresh faecal samples. A total of 327 fresh faecal samples from three wild ungulates, blue sheep Pseudois nayaur (n = 127), Ladakh urial Ovis vignei vignei (n = 110), and Himalayan ibex Ibex siberica (n = 90) were collected between June 2021 and May 2022. The techniques of flotation and sedimentation were used to find parasite eggs and oocysts from the faecal samples. Out of 327 samples examined, 165 samples were infected with gastrointestinal parasites making an overall prevalence of 50.45%. Seven parasitic taxa, including one protozoan (Eimeria spp.), five nematodes (Nematodirus spp., Strongyloides spp., Haemonchus sp., Trichuris sp., and Trichostrongylus spp.), and one cestode (Monezia spp.), were found during the current investigation. Mixed infection was reported in 36 (11%) of the total examined samples. The prevalence of gastrointestinal parasites was found to be highest in blue sheep (55.11%), followed by Ladakh urial (49.09%) and Himalayan ibex (45.55%). The highest prevalence was recorded in the summer (64.42%), and the lowest in the winter (33.82%). A significant difference in parasitic prevalence was observed across seasons in each of the three wild ungulate hosts. However, there was no significant difference in the prevalence of parasites between these hosts.

Facile Synthesis of a Crystalline Zinc Sulfide/Chitosan Biopolymer Nanocomposite: Characterization and Application for Photocatalytic Degradation of Textile Dyes and Anticancer Activity.

In the present study, we have synthesized a zinc sulfide/chitosan (ZS/CS) nanocomposite by utilizing simple, economical, and environmentally friendly methods. The synthesized nanomaterials were characterized by different analytical techniques such as XRD, FE-SEM, EDS, and FTIR to determine the phase structure, morphology, and elemental composition. FTIR spectroscopy was used to confirm the functional groups of the synthesized zinc sulfide (ZS) nanoparticles and ZS/CS composite. Besides, the optical properties of the as-synthesized nanocomposite was analyzed by a UV-visible spectrophotometer, and the estimated band gap energy is ∼3.03 eV. The photocatalytic efficiency of the synthesized ZS/CS nanocomposite was investigated against two textile dyes, Crystal Violet (CV) and Acid Red-I (AR-I), under UV-visible light irradiation. The nanocomposite showed excellent photocatalytic activity against the dyes, and photodegradation was estimated to be about 93.44 and 90.67% for CV and AR-I, respectively. The nanocomposite was reused for three consecutive cycles. The results revealed that the photocatalyst displayed good reusability during the photocatalytic decomposition and thus is considered a cost-effective and promising photocatalyst in degrading dye pollutants. The kinetic study proved that the pseudo-first-order reaction kinetics was followed by the degradation process. We also examined the anticancer activity of ZS and ZS/CS against human breast and myelogenous leukemia cancer cell lines, namely, MCF-7 and K-562, and the half minimal inhibitory concentrations were found to be less than 50 µg/mL.

Chemoselective oxidation of aromatic aldehydes to carboxylic acids: potassium tert-butoxide as an anomalous source of oxygen.

Chemoselective oxidation of aromatic and heteroaromatic aldehydes (>45 examples) to their corresponding carboxylic acids has been developed. Potassium tert-butoxide acts as an oxygen source during this transformation that delivers the corresponding acids without chromatographic purifications. The use of bench-top reagents, operational simplicity, and high level of chemo-selectivity with respect to oxidation of the least preferred aldehyde functionality, in the presence of more susceptible functional groups, are some of the highlights of this strategy.

In-vivo anti-hyperglycemic effect of herbal extracts Tribulus terrestris (L) and Curcuma amada (R) on streptozotocin-induced diabetic rats and its associated histopathological studies.

Dia/betes is a serious health concern in many countries with high blood glucose, obesity, and multiple organ failures in late stages. Treating diabetes with effective drugs is still a challenging issue since most of the available diabetic drugs are not effective in combating diabetes, especially in secondary disease complications like obesity, retinopathy, and nephropathy associated with diabetes. Hence search for effective antidiabetic medication, especially from natural sources is mandatory with no adverse side effects. In the present study, a combined herbal aqueous extract of Tribulus terrestris and Curcuma amada was administered to diabetic-induced rats for 37 days. During experimentation, the mean blood glucose level was estimated and at the end of the experiment on the 37th day, the animal was sacrificed and observed for weight gain, plasma insulin, glycogen, glycated hemoglobin, urea, and creatinine level. The results revealed that TT and CA extract-treated diabetic groups significantly lowered the mean blood glucose level followed by increased glycogen and insulin level. Urea, creatinine, and HbA1c levels were considerably reduced in TT and CA-treated diabetic animals as compared to that of antidiabetic drug Glibenclamide-treated groups. TT and CA-treated diabetic animals showed considerable net body weight gain at the end of the experimental day. A concluding remark of the study shows that TT and CA herbal extract is effective against diabetes and it can be considered as an antidiabetic agent in ayurvedic medicine practice.