Ecology, genetic diversity, and population structure among commercial varieties and local landraces of Capsicum spp. grown in northeastern states of India.

Northeastern states of India are known for unique landraces of Capsicum spp. with geographical indications. However, little information is available about these valuable landraces of chillies. Surveys and collections were carried out in niche areas to find out their ecology and diversity through morphological traits and molecular analysis using microsatellite markers. Our result characterized the ecology of niche areas as cool (11.0°C-20.7°C) and humid (>60% relative humidity) climates for dalle-chilli (Capsicum annuum L.); mild-warm (12.2°C-28.6°C) and humid for king-chilli (C. chinense Jacq.); and cool to warm (11.3°C-33.1°C) and humid for bird's eye chilli (C. frutescens L.) during the crop period. The canonical correspondence analysis has shown the significant impact of temperature on the agro-morphological traits and distribution of the landraces in their niche areas. A wide variability was observed for different quantitative traits and yield attributing characters (fruit length, diameter, weight, and yield), showing high heritability (97.0%-99.0%), and genetic advance as a percentage of the mean (119.8%-434.0%). A total of 47 SSR markers used for the molecular analysis generated 230 alleles, ranging from 2 (HPMSE-7) to 10 (HPMSE-5), with an average of 4.89 alleles per locus. The average polymorphism information content was also high (0.61) and ranged from 0.20 (HPMSE-7) to 0.85 (CAMS-91). The observed average heterozygosity was lower than the expected value. Analysis of molecular variance has shown significant variation within (69%) and between (31%) of the populations of Capsicum spp. Based on Nei's genetic distance, bird's eye chilli and king-chilli were found to be closer to each other, whereas dalle-chilli, a tretraploid species, was closer to hot pepper (C. annuum). However, the flower size of dalle-chilli was large and found closer to king-chilli in color and differs from C. chinense due to the presence of calyx teeth. For quality traits, landraces king-chilli, dalle-chilli, and bird's eye chilli have shown 2.8, 2.0, and 1.4 times higher average capsaicin and 0.46, 0.25, and 0.22 times higher average oleoresin content over the hot pepper, respectively. The knowledge of ecology and diversity can be used in identifying new areas for production, selection of elite lines, conservation, and crop improvement.

Synthesis of Chirally Enriched Pyrazolylpyrimidinone-Based Glycohybrids via Annulation of Glycals with 2-Hydrazineylpyrimidin-4(3H)-ones.

A new strategy for synthesizing chirally enriched pyrazolylpyrimidinone-based glycohybrids has been achieved, employing an annulation approach in ethanol without any additives or catalysts under microwave conditions. The designed compounds were obtained within a short reaction time (5 min). This method offers several advantages, including mild reaction conditions, a green solvent, and a metal-free approach. Furthermore, the protocol demonstrated a broad substrate scope, successfully incorporating various functional groups with stereochemical diversity and furnishing chirally enriched molecules.

Recent developments on the synthesis of biologically active glycohybrids.

The exploration of hybridization emerges as a potent tool in advancing drug discovery research, with a significant emphasis on carbohydrate-containing hybrid scaffolds. Evidence indicates that linking carbohydrate molecules to privileged bioactive scaffolds enhances the bioactivity of drug molecules. This synergy results in a diverse range of activities, making carbohydrate scaffolds pivotal for synthesizing compound libraries with significant functional and structural diversity. Beyond their synthesis utility, these scaffolds offer applications in screening bioactive molecules, presenting alternative avenues for drug development. This comprehensive review spanning 2015 to 2023 focuses on synthesized glycohybrid molecules, revealing their bioactivity in areas such as anti-microbial, anti-cancer, anti-diabetic, anti-inflammatory activities, enzyme inhibition and pesticides. Numerous novel glycohybrids surpass positive control drugs in biological activity. This focused study not only highlights the diverse bioactivities of glycohybrids but also underscores their promising role in innovative drug development strategies.

Synthesis of triazole bridged N-glycosides of pyrazolo[1,5-a]pyrimidinones as anticancer agents and their in silico docking studies.

In the pursuit of novel therapeutic agents, we present a comprehensive study on the design, synthesis, and evaluation of a diverse library of triazole bridged N-glycosides of pyrazolo[1,5-a]pyrimidinones, employing a microwave-assisted synthetic approach via 'click chemistry'. This methodology offers efficient and accelerated access to the glycohybrids, showcasing improved reaction conditions that yield high-quality products. In this research endeavor, we have successfully synthesized a series of twenty-seven triazole bridged N-glycosides of pyrazolo[1,5-a]pyrimidinones. Our investigation extends beyond synthetic endeavors to explore the potential therapeutic relevance of these compounds. We subjected them to rigorous in vitro screening against prominent breast cancer cell lines MCF-7, MDA-MB231, and MDA-MB453. Among the library of compounds synthesized, (2S,3S,4R,5S,6S)-2-(acetoxymethyl)-6-(4-((5-(4-methoxyphenyl)-7-oxopyrazolo[1,5-a]pyrimidin-1(7H)-yl)methyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3,4,5-triyl triacetate emerged as a potent compound, exhibiting remarkable anti-cancer activity with an IC50 value of 27.66 µM against the MDA-MB231 cell line. Additionally, (2S,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-((7-oxo-5-(4-(trifluoromethyl)phenyl)pyrazolo[1,5-a]pyrimidin-1(7H)-yl)methyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3,4,5-triyl triacetate displayed notable inhibitory potential against the MCF-7 cell line, with an IC50 value of 4.93 µM. Furthermore, in silico docking analysis was performed to validate our experimental findings. These findings underscore the promise of our triazole bridged N-glycosides of pyrazolo[1,5-a]pyrimidinones as potential anti-cancer agents. This research not only enriches the field of glycohybrid synthesis but also contributes valuable insights into the development of novel anti-cancer therapeutics.

Copper-catalyzed synthesis of pyrazolo[1,5-a]pyrimidine based triazole-linked glycohybrids: mechanistic insights and bio-applications.

Hybrid molecules maintain their stronghold in the drug market, with over 60% of drug candidates in pharmaceutical industries. The substantial expenses for developing and producing biologically privileged drugs are expected to create opportunities for producing hybrid molecule-based drugs. Therefore, we have developed a simple and efficient copper-catalyzed approach for synthesizing a wide range of triazole-linked glycohybrids derived from pyrazolo[1,5-a]pyrimidines. Employing a microwave-assisted copper-catalyzed approach, we developed a concise route using various 7-O-propargylated pyrazolo[1,5-a]pyrimidines and 1-azidoglycosides. This strategy afforded a series of twenty-seven glycohybrids up to 98% yield with diverse stereochemistry. All were achieved within a remarkably shortened time frame. Our investigation extends to evaluating the anticancer potential of these synthesized triazole-linked pyrazolo[1,5-a] pyrimidine-based glycohybrids. In-vitro assays against MCF-7, MDA-MB231, and MDA-MB453 cell lines reveal intriguing findings. (2R,3S,4S,5R,6R)-2-(acetoxymethyl)-6-(4-(((5-(4-chlorophenyl)pyrazolo[1,5-a]pyrimidin-7-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3,4,5-triyl triacetate emerges as a standout with better anticancer activity against MDA-MB231 cells (IC50 = 29.1 µM), while (2R,3R,4S,5R,6R)-2-(acetoxymethyl)-6-(4-(((5-(4-chlorophenyl)pyrazolo[1,5-a]pyrimidin-7-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3,4,5-triyl triacetate demonstrates the best inhibitory effects against MCF-7 cells (IC50 = 15.3 µM) in all derived compounds. These results align with our docking analysis and structure-activity relationship (SAR) investigations, further validating the in-vitro outcomes. This work not only underscores the synthetic utility of our devised protocol but also highlights the promising potential of these glycohybrids as candidates for further anticancer therapeutic exploration.

Recent developments on microwave-assisted organic synthesis of nitrogen- and oxygen-containing preferred heterocyclic scaffolds.

In recent decades, the utilization of microwave energy has experienced an extraordinary surge, leading to the introduction of innovative and revolutionary applications across various fields of chemistry such as medicinal chemistry, materials science, organic synthesis and heterocyclic chemistry. Herein, we provide a comprehensive literature review on the microwave-assisted organic synthesis of selected heterocycles. We highlight the use of microwave irradiation as an effective method for constructing a diverse range of molecules with high yield and selectivity. We also emphasize the impact of microwave irradiation on the efficient synthesis of N- and O-containing heterocycles that possess bioactive properties, such as anti-cancer, anti-proliferative, and anti-tumor activities. Specific attention is given to the efficient synthesis of pyrazolopyrimidines-, coumarin-, quinoline-, and isatin-based scaffolds, which have been extensively studied for their potential in drug discovery. The article provides valuable insights into the recent synthetic protocols and trends for the development of new drugs using heterocyclic molecules.

Recent Efforts in Identification of Privileged Scaffolds as Antiviral Agents.

Viral infections are the most important health concern nowadays to mankind, which is unexpectedly increasing the health complications and fatality rate worldwide. The recent viral infection outbreak developed a pressing need for small molecules that can be quickly deployed for the control/treatment of re-emerging or new emerging viral infections. Numerous viruses, including the human immunodeficiency virus (HIV), hepatitis, influenza, SARS-CoV-1, SARS-CoV-2, and others, are still challenging due to emerging resistance to known drugs. Therefore, there is always a need to search for new antiviral small molecules that can combat viral infection with new modes of action. This review highlighted recent progress in developing new antiviral molecules based on natural product-inspired scaffolds. Herein, the structure-activity relationship of the FDA-approved drugs along with the molecular docking studies of selected compounds have been discussed against several target proteins. The findings of new small molecules as neuraminidase inhibitors, other than known drug scaffolds, Anti-HIV and SARS-CoV are incorporated in this review paper.

Rationalizing mineral gypsum use through microbially enriched municipal solid waste compost for amelioration and regaining productivity potential of degraded alkali soils.

Reclamation of alkali soils to harness their productivity potential is more complex due to the presence of excess sodium ions, poor hydraulic conductivity and infiltration rate, resulting in poor plant growth and crop productivity. Sodic soil reclamation using inorganic ameliorants like mineral gypsum or phosphogypsum is beyond the reach of small and marginal farmers having alkali soils because of their higher market prices and shortage of availability. Conjoint use of inorganic and organic amendments can be a pragmatic solution for improving soil physico-chemical and biological properties and sustaining crop productivity. Municipal solid waste compost (MSWC) available in abundant quantity if enriched with the efficient halophilic microbial consortium and used in conjunction with a reduced dose of gypsum can be a cost-effective approach for sustainable reclamation of alkali soils and harnessing their productivity potential. Hence, a field experiment was conducted on a high alkali soil (pH2 9.2 ± 0.10), electrical conductivity (EC) 1.14 ± 0.12 dS m-1, exchangeable sodium percentage 48 ± 2.50 and organic carbon (0.30%) was conducted during 2018-19 to 2020-21 to study the combined effect inorganic and organic (enriched municipal solid waste compost (EMSWC)) amendments on amelioration of alkali soils and sustaining productivity of rice-wheat cropping system. Application of gypsum @ 25% GR + enriched MSW compost @ 10 t ha-1 (T6) showed significant improvement in soil physico-chemical and biological properties over the sole application of organic (T3 and T4), inorganic (T2) and control (T1). A significant improvement in soil fertility status in terms of available nitrogen and micronutrients as well as CO3, HCO3, Cl, Ca and Mg content were recorded with the combined application of organic and inorganic soil amendments (T5 and T6) over the sole application of mineral gypsum. Soil microbial biomass carbon (MBC), nitrogen (MBN) and phosphorus (MBP) improved significantly due to the application of EMSWC with gypsum over the application of gypsum only. Grain yield of rice and wheat increased significantly (P < 0.05) owing to the application of a reduced dose of gypsum (25% GR) and EMSWC @ 10 t ha-1 (T6) with values of 5.55 and 3.83 t ha-1, respectively over rest of the treatments. Three years economic analysis of the study revealed that treatments T6 and T5 gave the highest positive net return whereas it was lowest in treatment T1 and negative in treatment T2. The highest benefit-to-cost ratio (B:C) was obtained in treatments T6 and T5 which were significantly higher compared to the rest of the treatments.

Electro-organic green synthesis of dicyano-2-(2-oxoindolin-3-ylidene) malononitriles using molecular iodine as catalyst.

The first electrochemical molecular iodine promoted, domino reactions for the green synthesis of biologically relevant dicyano 2-(2-oxoindolin-3-ylidene) malononitriles (11 examples, up to 94% yield) from readily available isatin derivatives, malononitrile, and iodine at room temperature have been presented. This synthesis method showed tolerance towards various EDG and EWG and was completed in a short reaction time at the constant low current density of 5 mA cm-2 in the low redox potential range of -0.14 to 0.07 V. The present study exhibited by-product-free formation, easy operation, and product isolation. In particular the formation of a C[double bond, length as m-dash]C bond was observed at room temperature with a high atom economy. Furthermore, in the present study, the electrochemical behavior of dicyano 2-(2-oxoindolin-3-ylidene) malononitrile derivatives using a cyclic voltammetry (CV) technique in 0.1 M NaClO4 in acetonitrile solution was studied. All the chosen substituted isatin exhibited well-defined diffusion-controlled quasi-reversible redox peaks except 5-substituted derivatives. This synthesis could serve as an alternative strategy to synthesize other biologically important oxoindolin-3-ylidene malononitrile derivatives.

Assessment of ethnobotanical uses, household, and regional genetic diversity of aroid species grown in northeastern India.

Aroids are an important group of indigenous tuber crops, grown widely for their leaves, petioles, stolons, corms, and cormels. A total of 53 genotypes were evaluated for their genetic diversity in northeastern region of India. At household level, a total of 16 landraces of Aroids were recorded having different ethnobotanical uses. Based on the population study under Jhum/Shifting farming, landrace Rengama was dominant in area with 47% of the total population followed by Tamachongkham and Tasakrek. However, Pugarkusu and Chigi occupied 33.0 and 24.0% of the population, respectively under backyard farming, and were considered as major landraces. Tamachongkham, high in acridity and total oxalate content (0.82%), was used for cooking with meat, while Tasakrek was used as a baby food due to high total sugar (>3.0%), low in acridity, and total oxalate content (<0.12%). The Simpson's diversity index of the backyards was higher (0.80) as compared to Jhum field (0.63). The genotypes showed wider variability in growth and yield attributes like; plant height (89.4-206.1 cm), number of side shoots (1.84-5.92), corm weight (38.0-683.3 g), cormel weight (14.0-348.3 g), yield (0.24-1.83 kg plant-1). Similarly, wide variations were also observed for quality traits like total sugar (1.93-4.94%); starch (15.32-32.49%), total oxalate (0.10-0.82%), and dry matter (16.75-27.08%) content. Except for total oxalate, all the growth and yield attributes have shown high heritability and moderate to high genetic advance. Molecular analysis (33 polymorphic SSR markers) detected a total of 136 alleles, ranged 3 to 8 alleles per marker. The observed heterozygosity (0.24) was less than expected heterozygosity (0.69). The group-wise maximum genetic divergence was observed between Colocasia fallax (cv. Chigi) to C. esculenta var. aquatilis (cv. Tharsing); C. fallax (cv. Chigi) to C. gigantea (cv. Ganima) and C. gigantea (cv. Ganima) to Xanthosoma spp., while it was least between eddo and dasheen. The findings indicated, a wider diversity and distinct ethnobotanical uses of Aroid landraces at the house hold levels, which should be conserved and popularized to ensure nutritional security.

Biochemical and antioxidant activity of wild edible fruits of the eastern Himalaya, India.

The eastern Himalayas, one of the important hotspots of global biodiversity, have a rich diversity of wild edible fruit trees. The fruits of these tree species have been consumed by the tribal people since time immemorial. However, there is limited information available on the biochemical and antioxidant properties of the fruits. Therefore, the present investigation was undertaken to study the physico-chemical and antioxidant properties of the nine most important wild fruit trees. Among the species, Pyrus pashia had the maximum fruit weight (37.83 g), while the highest juice (43.72%) and pulp content (84.67%) were noted in Haematocarpus validus and Myrica esculenta, respectively. Maximum total soluble solids (18.27%), total sugar (11.27%), moisture content (88.39%), ascorbic acid content (63.82 mg/100 g), total carotenoids (18.47 mg/100 g), and total monomeric anthocyanin (354.04 mg/100 g) were recorded in H. validus. Docynia indica had the highest total phenolic content (19.37 mg GAE/g), while H. validus recorded the highest total flavonoids and flavanol content. The antioxidant activities of the different fruits ranged from 0.17 to 0.67 IC50 for DPPH activity and 3.59-13.82 mg AAE/g for FRAP. These fruits had attractive pigmentation of both pulp and juice and were a good potential source for the extraction of natural edible color in the food industry. The fruits also possess high market prices; Prunus nepalensis fetched $ 34.10-$ 141.5 per tree. Therefore, these fruits are rich sources of antioxidants, pigments and have a high market value for livelihood and nutritional security.

Conservation Tillage and Waste Crop Residue Based Zinc Fortification in Rice and Wheat under Reclaimed Sodic Soils: Progress toward Nutrient Circularity and Sustainability.

Nearly 50% of the population across the globe is at risk of malnutrition with respect to zinc (Zn) in areas where a cereal based dietary system dominates. The present study estimated daily Zn intake in humans through field experiments in reclaimed sodic soil, utilizing waste crop residue (CR) in conservation tillage where CR played a vital role in enhancing Zn uptake in rice and wheat grains. Zn dynamics, its bioavailability, interaction with soil properties, and plausible contribution in dietary intake were studied extensively to supplement the research. A higher mobility factor (2.70%) and plant available Zn resulted in its higher uptake in rice (58.2 mg kg-1) and wheat (67.2 mg kg-1) under zero tillage in rice followed by zero tillage in wheat where CR was retained on the surface (ZTR-ZTW+CR). Daily Zn intake was found to be maximum (0.651 mg kg-1 day-1) under ZTR-ZTW+CR, demonstrating zinc sufficiency. Thus, this study may help in formulating actionable policies for combating both nutritional security and environmental hazards due to CR burning.

Linseed oil in boar's diet improved in vivo fertility and antioxidant status.

The reactive oxygen species (ROS) which are produced during storage of boar semen are causing oxidative stress and leads to poor fertility. Also, tropical and sub-tropical weather condition adversely impacts the physicomorphological quality and fertility of boar sperm. The aim of this study was to examine the effects of feeding linseed oil to boar on its seminal attributes, sperm kinetics, biomarkers of antioxidant, fatty acid profile of seminal plasma (SP) and sperm and in vivo fertility. Six Hampshire crossbreed boars were fed with 90 ml linseed oil (LIN) whereas six Hampshire crossbreed boars were fed 90 ml canola oil (CON) for 16 weeks. Sperm quality was evaluated (60 ejaculates for each group; a total of 120 ejaculates) for motility, livability, abnormal morphology, acrosomal membrane integrity, hypo-osmotic swelling test (HOST) and sperm kinetic parameters by computer assisted semen analysis (CASA) at 0 h and at 72 h of storage at 17°C. Biomarkers of antioxidant (glutathione peroxidase; GPx, catalase; CAT, total antioxidant capacity; TAC) and malondialdehyde (MDA) were measured in SP and serum. Gas chromatography-mass spectrometry (GC-MS) was used for the estimation of fatty acid composition of SP and sperm. Boars fed with linseed oil had higher semen volume (p < .01) and more total sperm numbers (p < .01). Feeding linseed oil to boar enhanced seminal attributes (p < .05) at 0 h as well as at 72 h of storage. Linseed oil feeding (p < .01) improved biomarkers of antioxidants and significantly (p < .01) lowered the lipid peroxidation in serum and SP. Linseed oil feeding (p < .05) increased the proportion of alpha linolenic (ALA), arachidonic and docosahexaenoic (DHA) fatty acids in SP. The ratio of n-6 to n-3 fatty acids in sperm increased significantly (p < .01) in treatment group. Farrowing rate was significantly (p < .05) higher in treatment group. In conclusion, feeding linseed oil to boar improved the in vivo fertility, enhanced antioxidant capacity and increased the DHA content of SP and sperm.

Cardenolide and pregnatriene compounds from the roots of Nerium oleander.

Cardenolide and pregnatriene compounds were isolated from the chloroform fraction of the 95% aqueous ethanolic extract of dried roots of Nerium oleander. The stereochemical structure of the cardenolide and pregnatriene compounds was determined to be 3ß-O-(D-diginosyl)-14ß-hydroxy card-20(22)-enolide and 12ß-hydroxy pregna-4,6,16-triene-3,20-dione using spectroscopic methods including IR, HRMS and NMR spectroscopy.

Evaluation of cultivated and wild genotypes of Lens species under alkalinity stress and their molecular collocation using microsatellite markers.

In this study, 285 lentil genotypes were phenotyped under hydroponic and alkaline field conditions. Significant genotypic variation for alkalinity stress was observed among the six Lens species screened hydroponically and in the field having pH up to 9.1. The crucial parameters, like whole Na+ and K+ contents and the Na+/K+ ratio at 40 mM NaHCO3 were found significantly correlated with seedling survivability under hydroponics (r = -0.95, r = 0.93 and -0.97). Genotypes, ranked on the bases of seed yield, restricted uptake of Na+ with thick pith area, increased vascular bundles, less H2O2 production and low Na+/K+ ratio, were found important physio-anatomical traits for alkalinity stress tolerance. The proper regulation of Na+ uptake was found for maintaining higher K+. This relationship is probably the main factor responsible for a better mechanism for tolerance to high pH up to 9.1 in tolerant breeding lines PDL-1 and PSL-9 (cultivars) and ILWL-15, ILWL-192 and ILWL-20 (wild accessions). Based on UPGMA dendrogram, all the genotypes were clustered into four diverse groups. DMRT was implied within the group to differentiate genotypes based on phenotypic response under alkalinity stress. These results can be utilized for selecting diverse parents for developing alkalinity tolerant genotypes.

Fluoride in the environment and its metabolism in humans.

The presence of environmental fluoride and its impact on human health is well documented. When consumed in adequate quantity, fluoride prevents dental caries, assists in the formation of dental enamels, and prevents deficiencies in bone mineralization. At excessive exposure levels, ingestion of fluoride causes dental fluorosis skeletal fluorosis, and manifestations such as gastrointestinal, neurological, and urinary problems. The distribution of fluoride in the environment is uneven and largely is believed to derive from geogenic causes. The natural sources of fluoride are fluorite, fluorapatite, and cryolite, whereas anthropogenic sources include coal burning, oil refining, steel production, brick-making industries, and phosphatic fertilizer plants, among others. Among the various sources of fluoride in the environment, those of anthropogenic origin have occasionally been considered to be major ones. The gourndwater is more susceptible to fluoride accumulation and contamination than are other environmental media, primarily because of its contact with geological substrates underneath. The high fluoride concentration in water usually reflects the solubility of fluoride (CaF2). High concentrations are also often associated with soft, alkaline, and calcium-deficient waters. The fluoride compounds that occur naturally in drinking water are almost totally bioavailable (90%) and are completely absorbed from the gastrointestinal tract. As a result, drinking water is considered to be the potential source of fluoride that causes fluorosis. Because the bioavailability of fluoride is generally reduced in humans when consumed with milk or a calcium-rich diet, it is highly recommended that the inhabitants of fluoride-contaminated areas should incorporate calcium-rich foods in their routine diet. Guidelines for limiting the fluoride intake from drinking water have been postulated by various authorities. Such limits are designed to protect public health and should reflect all fluoride intake sources, including dietary fluoride. The toxicological risks posed by fluoride could be better understood if epidemiological surveillance for dental and skeletal fluorosis would be systematically conducted in fluoride-affected areas. Such input would greatly improve understanding of the human dose-response relationship. Such surveillance of potentially high fluoride areas is also important because it would help to delineate, much earlier, the remedial measures that are appropriate for those areas.