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  1. Fulltext Total synthesis, cytotoxic effects of damnacanthal, nordamnacanthal and related anthraquinone analogues
    Akhtar MN, Zareen S, Yeap SK, Ho WY, Lo KM, Hasan A, et al.
    Molecules, 2013 Aug 20;18(8):10042-55.
    PMID: 23966087 DOI: 10.3390/molecules180810042
    Naturally occurring anthraquinones, damnacanthal (1) and nordamnacanthal (2) were synthesized with modified reaction steps and investigated for their cytotoxicity against the MCF-7 and K-562 cancer cell lines, respectively. Intermediate analogues 2-bromomethyl-1,3-dimethoxyanthraquinone (5, IC50 = 5.70 ± 0.21 and 8.50 ± 1.18 mg/mL), 2-hydroxymethyl-1,3-dimethoxyanthraquinone (6, IC50 = 12.10 ± 0.14 and 14.00 ± 2.13), 2-formyl-1,3-dimethoxyantharquinone (7, IC50 = 13.10 ± 1.02 and 14.80 ± 0.74), 1,3-dimethoxy-2-methylanthraquinone (4, IC50 = 9.40 ± 3.51 and 28.40 ± 2.33), and 1,3-dihydroxy-2-methylanthraquinone (3, IC50 = 25.60 ± 0.42 and 28.40 ± 0.79) also exhibited moderate cytotoxicity against MCF-7 and K-562 cancer cell lines, respectively. Other structurally related compounds like 1,3-dihydroxyanthraquinone (13a, IC50 = 19.70 ± 0.35 and 14.50 ± 1.28), 1,3-dimethoxyanthraquinone (13b, IC50 = 6.50 ± 0.66 and 5.90 ± 0.95) were also showed good cytotoxicity. The target compound damnacanthal (1) was found to be the most cytotoxic against the MCF-7 and K-562 cancer cell lines, with IC50 values of 3.80 ± 0.57 and 5.50 ± 1.26, respectively. The structures of all compounds were elucidated with the help of detailed spectroscopic techniques.
    Matched MeSH terms: Aldehydes/chemistry*; Anthraquinones/chemistry*
  2. Fulltext Antifungal activities of new coumarins
    Al-Amiery AA, Kadhum AA, Mohamad AB
    Molecules, 2012 May 14;17(5):5713-23.
    PMID: 22628043 DOI: 10.3390/molecules17055713
    Newly synthesized coumarins 4-((5-mercapto-4-phenyl-4H-1,2,4-triazol-3-yl)-methoxy)-2H-chromen-2-one and 4-((5-(phenylamino)-1,3,4-thiadiazol-2-yl)-methoxy)-2H-chromen-2-one were tested against selected types of fungi and showed significant activities. DFT calculations of the synthesized coumarins were performed using molecular structures with optimized geometries. Molecular orbital calculations provide a detailed description of the orbitals, including spatial characteristics, nodal patterns, and the contributions of individual atoms.
    Matched MeSH terms: Antifungal Agents/chemistry; Coumarins/chemistry
  3. Current perspectives on fenugreek bioactive compounds and their potential impact on human health: A review of recent insights into functional foods and other high value applications
    Alu'datt MH, Rababah T, Al-Ali S, Tranchant CC, Gammoh S, Alrosan M, et al.
    J Food Sci, 2024 Apr;89(4):1835-1864.
    PMID: 38407443 DOI: 10.1111/1750-3841.16970
    Despite long-standing uses in several food and medicine traditions, the full potential of the leguminous crop fenugreek (Trigonella foenum-graecum L.) remains to be realized in the modern diet. Not only its seeds, which are highly prized for their culinary and medicinal properties, but also its leaves and stems abound in phytochemicals with high nutritional and health promoting attributes. Fenugreek dual food-medicine applications and reported metabolic activities include hypoglycemic, antihyperlipidemic, antioxidative, anti-inflammatory, antiatherogenic, antihypertensive, anticarcinogenic, immunomodulatory, and antinociceptive effects, with potential organ-protective effects at the cardiovascular, digestive, hepatic, endocrine, and central nervous system levels. Effectiveness in alleviating certain inflammatory skin conditions and dysfunctions of the reproductive system was also suggested. As a food ingredient, fenugreek can enhance the sensory, nutritional, and nutraceutical qualities of a wide variety of foods. Its high nutritive density can assist with the design of dietary items that meet the demand for novelty, variety, and healthier foods. Its seeds provide essential protective nutrients and other bioactive compounds, notably galactomannans, flavonoids, coumarins, saponins, alkaloids, and essential oils, whose health benefits, alone or in conjunction with other bioactives, are only beginning to be tapped into in the food industries. This review summarizes the current state of evidence on fenugreek potential for functional food development, focusing on the nutrients and non-nutrient bioactive components of interest from a dietary perspective, and their applications for enhancing the functional and nutraceutical value of foods and beverages. New developments, safety, clinical evidence, presumed mechanisms of action, and future perspectives are discussed. HIGHLIGHTS: Fenugreek seeds and leaves have long-standing uses in the food-medicine continuum. Fenugreek phytochemicals exert broad-spectrum biological and pharmacological activities. They show high preventive and nutraceutical potential against common chronic diseases. Current evidence supports multiple mechanisms of action mediated by distinct bioactives. Opportunities for fenugreek-based functional foods and nutraceuticals are expanding.
    Matched MeSH terms: Plant Extracts/chemistry; Seeds/chemistry
  4. In vitro and in vivo evaluation of the antimicrobial, antioxidant, cytotoxic, hemolytic activities and in silico POM/DFT/DNA-binding and pharmacokinetic analyses of new sulfonamide bearing thiazolidin-4-ones
    Hassan SA, Aziz DM, Abdullah MN, Bhat AR, Dongre RS, Hadda TB, et al.
    J Biomol Struct Dyn, 2024 Apr;42(7):3747-3763.
    PMID: 37402503 DOI: 10.1080/07391102.2023.2226713
    In this work, Schiff bases and Thiazolidin-4-ones, were synthesized using Sonication and Microwave techniques, respectively. The Schiff base derivatives (3a-b) were synthesized via the reaction of Sulfathiazole (1) with benzaldehyde derivatives (2a-b), followed by the synthesis of 4-thiazoledinone (4a-b) derivatives by cyclizing the synthesized Schiff bases through thioglycholic acid. All the synthesized compounds were characterized by spectroscopic techniques such as FT IR, NMR and HRMS. The synthesized compounds were tested for their in vitro antimicrobial and antioxidant and in vivo cytotoxicity and hemolysis ability. The synthesized compounds displayed better antimicrobial and antioxidant activity and low toxicity in comparison to reference drugs and negative controls, respectively. The hemolysis test revealed the compounds exhibit lower hemolytic effects and hemolytic values are comparatively low and the safety of compounds is in comparison with standard drugs. Theoretical calculations were carried out by using the molecular operating environment (MOE) and Gaussian computing software and observations were in good agreement with the in vitro and in vivo biological activities. Petra/Osiris/Molinspiration (POM) results indicate the presence of three combined antibacterial, antiviral and antitumor pharmacophore sites. The molecular docking revealed the significant binding affinities and non-bonding interactions between the compounds and Erwinia Chrysanthemi (PDB ID: 1SHK). The molecular dynamics simulation under in silico physiological conditions revealed a stable conformation and binding pattern in a stimulating environment. HighlightsNew series of Thaiazolidin-4-one derivatives have been synthesized.Sonication and microwave techniques are used.Antimicrobial, Antioxidant, cytotoxicity, and hemolysis activities were observed for all synthesized compounds.Molecular Docking and DFT/POM analyses have been predicted.Communicated by Ramaswamy H. Sarma.
    Matched MeSH terms: DNA/chemistry; Schiff Bases/chemistry
  5. Quality by Design Perspective for Designing Foam-based Formulation: Current State of Art
    Kumar M, Kumar D, Singh S, Chopra S, Mahmood S, Bhatia A
    Curr Pharm Des, 2024;30(6):410-419.
    PMID: 38747045 DOI: 10.2174/0113816128289965240123074111
    Foam-based delivery systems contain one or more active ingredients and dispersed solid or liquid components that transform into gaseous form when the valve is actuated. Foams are an attractive and effective delivery approach for medical, cosmetic, and pharmaceutical uses. The foams-based delivery systems are gaining attention due to ease of application as they allow direct application onto the affected area of skin without using any applicator or finger, hence increasing the compliance and satisfaction of the patients. In order to develop foam-based delivery systems with desired qualities, it is vital to understand which type of material and process parameters impact the quality features of foams and which methodologies may be utilized to investigate foams. For this purpose, Quality-by-Design (QbD) approach is used. It aids in achieving quality-based development during the development process by employing the QbD concept. The critical material attributes (CMAs) and critical process parameters (CPPs) were discovered through the first risk assessment to ensure the requisite critical quality attributes (CQAs). During the initial risk assessment, the high-risk CQAs were identified, which affect the foam characteristics. In this review, the authors discussed the various CMAs, CPPs, CQAs, and risk factors associated in order to develop an ideal foam-based formulation with desired characteristics.
    Matched MeSH terms: Chemistry, Pharmaceutical; Pharmaceutical Preparations/chemistry
  6. Development of a nanozyme-based electrochemical catalyst for real-time biomarker sensing of superoxide and nitric oxide anions released from living cells and exogenous donors
    Arul P, Huang ST, Nandhini C, Huang CH, Gowthaman NSK, Huang CH
    Biosens Bioelectron, 2024 Oct 01;261:116485.
    PMID: 38852323 DOI: 10.1016/j.bios.2024.116485
    Developing quantitative biosensors of superoxide (O2•-) and nitric oxide (NO) anion is crucial for pathological research. As of today, the main challenge for electrochemical detection is to develop high-selectivity nano-mimetic materials to replace natural enzymes. In this study, the dendritic-like morphological structure of silver organic framework (Ag-MOF) was successfully synthesized via a solvothermal strategy. Owing to the introduction of polymeric composites results in improved electrical conductivity and catalytic activity, which promotes mass transfer and leads to faster electron efficiency. For monitoring the electrochemical signals of O2•- and NO, the Ag-MOF electrode substrate was produced by drop-coating, and composites were designed by cyclic voltammetric potential cycles. The designed electrode substrates demonstrate high sensitivity, wide linear concentrations of 1 nM-1000 μM and 1 nM-850 μM, and low detection limits of 0.27 nM and 0.34 nM (S/N = 3) against O2•- and NO. Aside from that, the sensor successfully monitored the cellular release of O2•-, and NO from HepG2 and RAW 264.7 living cells and has the potential to monitor exogenous NO release from donors of Diethylamine (DEA)-NONOate and sodium nitroprusside (SNP). Additionally, the developed system was applied to the analysis of O2•- and NO in real biological fluid samples, and the results were good satisfactory (94.10-99.57 ± 1.23%). The designed system provides a novel approach to obtaining a good electrochemical biosensor platform that is highly selective, stable, and flexible. Finally, the proposed method provides a quantitative way to follow the dynamic changes in O2•- and NO in biological systems.
    Matched MeSH terms: Silver/chemistry; Nitric Oxide Donors/chemistry
  7. Preparation and Preliminary Structure-Activity Relationship Studies of Schwarzinicine A Analogs as Vasorelaxant Agents
    Lee FK, Chan NJ, Krishnan P, Datu Abdul Salam DS, Chee XW, Muhamad A, et al.
    J Nat Prod, 2024 Apr 26;87(4):675-691.
    PMID: 38442031 DOI: 10.1021/acs.jnatprod.3c00707
    Schwarzinicines A-D, a series of alkaloids recently discovered from Ficus schwarzii, exhibit pronounced vasorelaxant activity in rat isolated aorta. Building on this finding, a concise synthesis of schwarzinicines A and B has been reported, allowing further investigations into their biological properties. Herein, a preliminary exploration of the chemical space surrounding the structure of schwarzinicine A (1) was carried out aiming to identify structural features that are essential for vasorelaxant activity. A total of 57 analogs were synthesized and tested for vasorelaxant activity in rat isolated aorta. Both efficacy (Emax) and potency (EC50) of these analogs were compared. In addition to identifying structural features that are required for activity or associated with potency enhancement effect, four analogs showed significant potency improvements of up to 40.2-fold when compared to 1. Molecular dynamics simulation of a tetrameric 44-bound transient receptor potential canonical-6 (TRPC6) protein indicated that 44 could potentially form important interactions with the residues Glu509, Asp530, Lys748, Arg758, and Tyr521. These results may serve as a foundation for guiding further structural optimization of the schwarzinicine A scaffold, aiming to discover even more potent analogs.
    Matched MeSH terms: Alkaloids/chemistry; Ficus/chemistry
  8. Purification of exopolysaccharide produced from Lactobacillus spp. using ionic-liquid as adjuvant in alcohol/salt-based aqueous two-phase system for its antidiabetic properties
    Raj ST, Puspanadan S, Gan CY, Tan JS
    Int J Biol Macromol, 2024 May;267(Pt 2):131376.
    PMID: 38608981 DOI: 10.1016/j.ijbiomac.2024.131376
    Diabetes is a chronic, metabolic disease characterized by hyperglycemia resulting from either insufficient insulin production or impaired cellular response to insulin. Exopolysaccharides (EPS) produced by Lactobacillus spp. demonstrated promising therapeutic potential in terms of their anti-diabetic properties. Extraction and purification of EPS produced by Lactobacillus acidophilus and Limosilactobacillus reuteri were performed using ethanol precipitation, followed by alcohol/salt based aqueous two-phase system (ATPS). The purification process involved ethanol precipitation followed by an alcohol/salt-based ATPS. The study systematically investigated various purification parameters in ATPS, including ethanol concentration, type and concentration of ionic liquid, type and concentration of salt and pH of salt. Purified EPS contents from L. acidophilus (63.30 μg/mL) and L. reuteri (146.48 μg/mL) were obtained under optimum conditions of ATPS which consisted of 30 % (w/w) ethanol, 25 % (w/w) dipotassium hydrogen phosphate at pH 10 and 2 % (w/w) 1-butyl-3-methylimidazolium octyl sulfate. The extracted EPS content was determined using phenol sulphuric acid method. In α-amylase inhibition tests, the inhibitory rate was found to be 92.52 % (L. reuteri) and 90.64 % (L. acidophilus), while in α-glucosidase inhibition tests, the inhibitory rate was 73.58 % (L. reuteri) and 68.77 % (L. acidophilus), based on the optimized parameters selected in ATPS. These results suggest that the purified EPS derived from the postbiotics of Lactobacillus spp. hold promise as potential antidiabetic agents.
    Matched MeSH terms: Ethanol/chemistry; Salts/chemistry
  9. Fulltext Design of three-component essential oil extract mixture from Cymbopogon flexuosus, Carum carvi, and Acorus calamus with enhanced antioxidant activity
    Assaggaf H, Jeddi M, Mrabti HN, Ez-Zoubi A, Qasem A, Attar A, et al.
    Sci Rep, 2024 Apr 22;14(1):9195.
    PMID: 38649707 DOI: 10.1038/s41598-024-59708-x
    The development of novel antioxidant compounds with high efficacy and low toxicity is of utmost importance in the medicine and food industries. Moreover, with increasing concerns about the safety of synthetic components, scientists are beginning to search for natural sources of antioxidants, especially essential oils (EOs). The combination of EOs may produce a higher scavenging profile than a single oil due to better chemical diversity in the mixture. Therefore, this exploratory study aims to assess the antioxidant activity of three EOs extracted from Cymbopogon flexuosus, Carum carvi, and Acorus calamus in individual and combined forms using the augmented-simplex design methodology. The in vitro antioxidant assays were performed using DPPH and ABTS radical scavenging approaches. The results of the Chromatography Gas-Mass spectrometry (CG-MS) characterization showed that citral (29.62%) and niral (27.32%) are the main components for C. flexuosus, while D-carvone (62.09%) and D-limonene (29.58%) are the most dominant substances in C. carvi. By contrast, β-asarone (69.11%) was identified as the principal component of A. calamus (30.2%). The individual EO exhibits variable scavenging activities against ABTS and DPPH radicals. These effects were enhanced through the mixture of the three EOs. The optimal antioxidant formulation consisted of 20% C. flexuosus, 53% C. carvi, and 27% A. calamus for DPPHIC50. Whereas 17% C. flexuosus, 43% C. carvi, and 40% A. calamus is the best combination leading to the highest scavenging activity against ABTS radical. These findings suggest a new research avenue for EOs combinations to be developed as novel natural formulations useful in food and biopharmaceutical products.
    Matched MeSH terms: Biphenyl Compounds/chemistry; Free Radical Scavengers/chemistry
  10. Review of Malaysian medicinal plants with potential wound healing activity
    Wiart C, Tan PL, Rajagopal M, Chew YL, Leong MY, Tan LF, et al.
    BMC Complement Med Ther, 2024 Jul 12;24(1):268.
    PMID: 38997637 DOI: 10.1186/s12906-024-04548-5
    Wound is defined as the damage to biological tissues including skin, mucous membranes and organ tissues. The acute wound heals in less than 4 weeks without complications, while a chronic wound takes longer than 6 weeks to heal. Wound healing occurs in 4 phases, namely, coagulation, inflammatory, proliferative and remodeling phases. Triclosan and benzalkonium chloride are commonly used as skin disinfectants in wound healing. However, they cause allergic contact dermatitis and antibiotic resistance. Medicinal plants are widely studied due to the limited availability of wound healing agents. The present review included six commonly available medicinal plants in Malaysia such as Aloe barbadensis Miller, Carica papaya Linn., Centella asiatica Linn., Cymbopogon nardus Linn., Ficus benghalensis Linn. and Hibiscus rosa sinensis Linn. Various search engines and databases were used to obtain the scientific findings, including Google Scholar, ScienceDirect, PubMed Central and Research Gate. The review discussed the possible mechanism of action of medicinal plants and their active constituents in the wound healing process. In addition, their application in nanotechnology and wound dressings was also discussed in detail.
    Matched MeSH terms: Centella/chemistry; Hibiscus/chemistry
  11. Fulltext Bioassay-Guided extraction of andrographis paniculata for intervention of in-vitro prostate cancer progression in metabolic syndrome environment
    Idris MKH, Hasham R, Ismail HF
    Daru, 2022 Dec;30(2):253-272.
    PMID: 35922691 DOI: 10.1007/s40199-021-00414-8
    BACKGROUND: Metabolic syndrome (MetS) is a risk factor for prostate cancer (PCa) progression. Thus, this life-threatening disease demands a proactive treatment strategy. Andrographis paniculata (AP) is a promising candidate with various medicinal properties. However, the bioactivity of AP is influenced by its processing conditions especially the extraction solvent.

    OBJECTIVE: In the present study, bioassay-guided screening technique was employed to identify the best AP extract in the management of MetS, PCa, and MetS-PCa co-disease in vitro.

    METHODS: Five AP extracts by different solvent systems; APE1 (aqueous), APE2 (absolute methanol), APE3 (absolute ethanol), APE4 (40% methanol), and APE5 (60% ethanol) were screened through their phytochemical profile, in-vitro anti-cancer, anti-obese, and anti-hyperglycemic properties. The best extract was further tested for its potential in MetS-induced PCa progression.

    RESULTS: APE2 contained the highest andrographolide (1.34 ± 0.05 mg/mL) and total phenolic content (8.85 ± 0.63 GAE/gDW). However, APE3 has the highest flavonoid content (11.52 ± 0.80 RE/gDW). APE2 was also a good scavenger of DPPH radicals (EC50 = 397.0 µg/mL). In cell-based assays, among all extracts, APE2 exhibited the highest antiproliferative activity (IC50 = 57.5 ± 11.8 µg/mL) on DU145 cancer cell line as well as on its migration activity. In in-vitro anti-obese study, all extracts significantly reduced lipid formation in 3T3-L1 cells. The highest insulin-sensitizing and -mimicking actions were exerted by both APE2 and APE3. Taken together, APE2 showed collectively good activity in the inhibition of PCa progression and MetS manifestation in vitro, compared to other extracts. Therefore, APE2 was further investigated for its potential to intervene DU145 progression induced with leptin (10-100 ng/mL) and adipocyte conditioned media (CM) (10% v/v). Interestingly, APE2 significantly diminished the progression of the cancer cell that has been pre-treated with leptin and CM through cell cycle arrest at S phase and induction of cell death.

    CONCLUSION: In conclusion, AP extracts rich with andrographolide has the potential to be used as an alternative to ameliorate PCa progression induced by factors highly expressed in MetS.

    Matched MeSH terms: Plant Extracts/chemistry; Solvents/chemistry
  12. A novel photocatalytic degradation of mixed dye through chemically synthesized ZnO/Fe2O3 nanocomposite
    Manojkumar U, Kaliannan D, Balasubramanian B, Kamyab H, Vasseghian Y, Chelliapan S, et al.
    Environ Geochem Health, 2024 Jun 07;46(7):221.
    PMID: 38849635 DOI: 10.1007/s10653-024-02000-8
    This study reported the synthesis and assessment of zinc oxide/iron oxide (ZnO/Fe2O3) nanocomposite as photocatalysts for the degradation of a mixture of methylene red and methylene blue dyes. X-ray diffraction analysis confirms that the crystallite of zinc oxide (ZnO) has a hexagonal wurtzite phase and iron oxide (Fe2O3) has a rhombohedral phase. Fourier Transform Infra-Red spectrum confirms the presence of Zn-O vibration stretching at 428, 480 and 543 cm-1 stretching confirming Fe-O bond formation. Scanning Electron Microscope images exhibited a diverse size and shape of the nanocomposites. The ZnO-90%/Fe2O3-10% and ZnO-10%/Fe2O3-90% nanocomposites reveal good photocatalytic activity with reaction rate constants of 1.5 × 10-2 and 0.66 × 10-2; and 1.3 × 10-2 and 0.60 × 10-2 for methylene blue and methyl red dye respectively. The results revealed that the synthesized ZnO/Fe2O3 nanocomposite is the best catalyst for dye degradation and can be used for industrial applications in future.
    Matched MeSH terms: Azo Compounds/chemistry; Water Pollutants, Chemical/chemistry
  13. Exploring the Biochemical and Nutra-Pharmaceutical Prospects of Some Thymus Species - A Review
    Anwar F, Mahrye, Khan R, Qadir R, Saadi S, Gruczynska-Sekowska E, et al.
    Chem Biodivers, 2024 Jul;21(7):e202400500.
    PMID: 38719739 DOI: 10.1002/cbdv.202400500
    The Thymus genus includes various medicinal and aromatic species, cultivated worldwide for their unique medicinal and economic value. Besides, their conventional use as a culinary flavoring agent, Thymus species are well-known for their diverse biological effects, such as antioxidant, anti-fungal, anti-bacterial, anti-viral, anti-tumor, anti-inflammatory, anti-cancer, and anti-hypertensive properties. Hence, they are used in the treatment of fever, colds, and digestive and cardiovascular diseases. The pharmaceutical significance of Thymus plants is due to their high levels of bioactive components such as natural terpenoid phenol derivatives (p-cymene, carvacrol, thymol, geraniol), flavonoids, alkaloids, and phenolic acids. This review examines the phytochemicals, biological properties, functional food, and nutraceutical attributes of some important Thymus species, with a specific focus on their potential uses in the nutra-pharmaceutical industries. Furthermore, the review provides an insight into the mechanisms of biological activities of key phytochemicals of Thymus species exploring their potential for the development of novel natural drugs.
    Matched MeSH terms: Antioxidants/chemistry; Phytochemicals/chemistry
  14. Fulltext Discovery of Amide-Functionalized Benzimidazolium Salts as Potent α-Glucosidase Inhibitors
    Khan IA, Ahmad M, Ashfaq UA, Sultan S, Zaki MEA
    Molecules, 2021 Aug 06;26(16).
    PMID: 34443347 DOI: 10.3390/molecules26164760
    α-Glucosidase inhibitors (AGIs) are used as medicines for the treatment of diabetes mellitus. The α-Glucosidase enzyme is present in the small intestine and is responsible for the breakdown of carbohydrates into sugars. The process results in an increase in blood sugar levels. AGIs slow down the digestion of carbohydrates that is helpful in controlling the sugar levels in the blood after meals. Among heterocyclic compounds, benzimidazole moiety is recognized as a potent bioactive scaffold for its wide range of biologically active derivatives. The aim of this study is to explore the α-glucosidase inhibition ability of benzimidazolium salts. In this study, two novel series of benzimidazolium salts, i.e., 1-benzyl-3-{2-(substituted) amino-2-oxoethyl}-1H-benzo[d]imidazol-3-ium bromide 9a-m and 1-benzyl-3-{2-substituted) amino-2-oxoethyl}-2-methyl-1H-benzo[d] imidazol-3-ium bromide 10a-m were screened for their in vitro α-glucosidase inhibitory potential. These compounds were synthesized through a multistep procedure and were characterized by 1H-NMR, 13C-NMR, and EI-MS techniques. Compound 10d was identified as the potent α-glucosidase inhibitor among the series with an IC50 value of 14 ± 0.013 μM, which is 4-fold higher than the standard drug, acarbose. In addition, compounds 10a, 10e, 10h, 10g, 10k, 10l, and 10m also exhibited pronounced potential for α-glucosidase inhibition with IC50 value ranging from 15 ± 0.037 to 32.27 ± 0.050 µM when compared with the reference drug acarbose (IC50 = 58.8 ± 0.12 μM). A molecular docking study was performed to rationalize the binding interactions of potent inhibitors with the active site of the α-glucosidase enzyme.
    Matched MeSH terms: Amides/chemistry; Salts/chemistry
  15. Performance analysis of snail shell biomaterials in solar still for clean water production: nature-inspired innovation for sustainability
    Dhivagar R, Suraparaju SK, Atamurotov F, Kannan KG, Opakhai S, Omara AAM
    Water Sci Technol, 2024 Jun;89(12):3325-3343.
    PMID: 39150427 DOI: 10.2166/wst.2024.189
    In this current investigation, the experimental performance of a solar still basin was significantly enhanced by incorporating snail shell biomaterials. The outcomes of the snail shell-augmented solar still basin (SSSS) are compared with those of a conventional solar still (CSS). The utilization of snail shells proved to facilitate the reduction of saline water and enhance its temperature, thereby improving the productivity of the SSSS. Cumulatively, the SSSS productivity was improved by 4.3% over CSS. Furthermore, the SSSS outperformed in energy and exergy efficiency of CSS by 4.5 and 3.5%, respectively. Economically, the cost per liter of distillate (CPL) for the CSS was 3.4% higher than SSSS. Moreover, the SSSS showed a shorter estimated payback period (PBP) of 141 days which was 6 days less than CSS. Considering the environmental impact, the observed CO2 emissions from the SSSS were approximately 14.6% higher than CSS over its 10-year lifespan. Notably, the SSSS exhibited a substantial increase in the estimated carbon credit earned (CCE) compared to the CSS. Ultimately, the research underscores the efficacy of incorporating snail shells into solar still basins as a commendable approach to organic waste management, offering economic benefits without compromising environmental considerations.
    Matched MeSH terms: Biocompatible Materials/chemistry; Animal Shells/chemistry
  16. Fulltext Purification and Characterization of Gum-Derived Polysaccharides of Moringa oleifera and Azadirachta indica and Their Applications as Plant Stimulants and Bio-Pesticidal Agents
    Shobana N, Prakash P, Samrot AV, Jane Cypriyana PJ, Kajal P, Sathiyasree M, et al.
    Molecules, 2022 Jun 09;27(12).
    PMID: 35744846 DOI: 10.3390/molecules27123720
    Plant gums are bio-organic substances that are derived from the barks of trees. They are biodegradable and non-adverse complex polysaccharides that have been gaining usage in recent years due to a number of advantages they contribute to various applications. In this study, gum was collected from Moringa oleifera and Azadirachta indica trees, then dried and powdered. Characterizations of gum polysaccharides were performed using TLC, GC-MS, NMR, etc., and sugar molecules such as glucose and xylose were found to be present. Effects of the gums on Abelmoschus esculentus growth were observed through root growth, shoot growth, and biomass content. The exposure of the seeds to the plant gums led to bio stimulation in the growth of the plants. Poor quality soil was exposed to the gum polysaccharide, where the polysaccharide was found to improve soil quality, which was observed through soil analysis and SEM analysis of soil porosity and structure. Furthermore, the plant gums were also found to have bio-pesticidal activity against mealybugs, which showed certain interstitial damage evident through histopathological analysis.
    Matched MeSH terms: Polysaccharides/chemistry; Plant Gums/chemistry
  17. Advancement of lignin into bioactive compounds through selective organic synthesis methods
    Jadhav P, Bhuyar P, Misnon II, Rahim MHA, Roslan R
    Int J Biol Macromol, 2024 Sep;276(Pt 2):134061.
    PMID: 39043289 DOI: 10.1016/j.ijbiomac.2024.134061
    The conversion of lignin into bioactive compounds through selective organic synthesis methods represents a promising frontier in the pursuit of sustainable raw materials and green chemistry. This review explores the versatility of lignin-derived bioactive compounds, ranging from their application in drug discovery to their role in the development of biodegradable materials. Despite notable advancements, the synthesis routes and yields of highly bioactive molecules from lignin still require further exploration and improvement. This review provides an in-depth examination of the progress made in understanding the complex structure of lignin and developing innovative approaches to exploit its potential. Specifically, the types of lignins covered include softwood Kraft lignin, hardwood organosolv lignin, and soda lignin. This work is divided into three parts: first, the transformation of lignin into bioactive molecules with chemically active centres and functionalised hydroxyl groups through depolymerisation; second, kinetic modelling techniques essential for understanding the chemical kinetics of lignin and enabling significant scaling up in the conversion of organic molecules; third, efficient catalytic pathways for synthesising molecules with anticancer and antibacterial properties. In conclusion, this comprehensive review spurs further investigations into lignin-derived bioactive compounds, their applications, and the advancement of sustainable processes.
    Matched MeSH terms: Antineoplastic Agents/chemistry; Chemistry Techniques, Synthetic
  18. The role of chitosan in promoting the catalytic activity of bismuth ferrite as peroxymonosulfate activator for antibiotics removal
    Tong ZX, Oh WD
    Int J Biol Macromol, 2024 Oct;277(Pt 3):134453.
    PMID: 39098691 DOI: 10.1016/j.ijbiomac.2024.134453
    Chitosan possesses electron-rich amino (-NH2) and hydroxyl (-OH) moieties which can anchor with transition metal ions during synthesis. Herein, chitosan was employed as an additive to prepare bismuth ferrite (BFO) via hydrothermal approach. The characterization studies revealed that adding chitosan during BFO synthesis leads to the creation of more oxygen vacancies. The performance of chitosan modified BFO (CMB) was evaluated as peroxymonosulfate (PMS) activator for ciprofloxacin (CIP) removal. Apparently, the addition of 10 wt% chitosan during BFO synthesis (CMB-10) resulted in 1.7 times increase of performance compared to the pristine BFO. Increasing the catalyst loading and PMS dosage resulted in positive effect with 5.7 and 1.9 times rate enhancement, respectively. The CMB-10 exhibited tolerance against pH variation, water matrix, and interfering species. The scavenging experiments indicated that singlet oxygen (1O2), superoxide radicals (O2•-) and sulfate radicals (SO4•-) played a major role in CIP degradation. These reactive oxygen species were generated from PMS activation via Fe3+/Fe2+ and Bi5+/Bi3+ coupling, and oxygen vacancies on the catalyst surface. The CIP degradation pathways were also elucidated based on the detected CIP intermediates. Overall, this study provides insights into the use of chitosan to prepare sustainable materials for pollutants removal via PMS activation.
    Matched MeSH terms: Ciprofloxacin/chemistry; Water Pollutants, Chemical/chemistry
  19. Fulltext A comprehensive Review into Emission Sources, Formation Mechanisms, Ecological Effects, and Biotransformation Routes of Halogenated Polycyclic Aromatic Hydrocarbons (HPAHs)
    Ali L, Alam A, Ali AM, Teoh WY, Altarawneh M
    Ecotoxicol Environ Saf, 2024 Nov 01;286:117196.
    PMID: 39426109 DOI: 10.1016/j.ecoenv.2024.117196
    Halogenated polycyclic aromatic hydrocarbons (HPAHs, H = F, Cl, Br) are a new class of PAHs derivatives that mainly originate from the incomplete combustion of halogen-laden materials and via metallurgical operations. These compounds circulate extensively in various environmental matrices. This survey provides a comprehensive review on governing synthesis routes of HPAHs, their environmental occurrence, and their health and ecological effects. The review comprehensively enlists and presents emission sources of these emerging organic pollutants into the air that serves as their main reservoir. The formation of HPAHs ensues through successive addition reactions of related precursors accompanied by ring cyclization steps; in addition to direct unimolecular fragmentation of parents halogenated. Halogenation of parent PAHs rapidly occurs in saline ecosystems, thus multiplying the availability of these notorious compounds in the environment. Certain HPAHs appear to be more carcinogenic than dioxins. Transmission routes of HPAHs from their emission sources to water bodies, soil, aquatic life, plants, terrestrial animals, and humans are well-documented. Later, the direct and indirect diffusion of HPAHs from air to the biotic (plants, animals, humans) and abiotic components (soil, water, sediments) are described in detail. The study concludes that HPAHs are permeable to the carbon matrices resulting in the alleviation of the source-to-sink interface. As a potential future perspective, understanding the transmission interfaces lays a foundation to intervene in the introduction of these toxicants into the food chain.
    Matched MeSH terms: Environmental Pollutants/chemistry; Hydrocarbons, Halogenated/chemistry
  20. Microwave-assisted extraction of polysaccharides from Micromelum minutum leaves using citric acid monohydrate-glycerol based deep eutectic solvents and evaluation of biological activities
    Md Yusoff MH, Shafie MH
    Anal Chim Acta, 2024 Dec 01;1331:343351.
    PMID: 39532430 DOI: 10.1016/j.aca.2024.343351
    BACKGROUND: The extraction of polysaccharides using an acidic extraction media has been extensively reported, highlighting its effectiveness in yielding high-quality polysaccharides. A higher concentration of acidic solution could hydrolyze the structure of polysaccharide, while a low concentration reduces the extraction efficiency. Despite this challenges, deep eutectic solvents (DES) were introduced as an alternative extraction medium due to additional interactions such as inter and intra-molecular interactions, Van de Waals, hydrogen bond, and electrostatic interactions, which could improve the polysaccharide extraction efficiency and biological activities. Furthermore, the extraction conditions such as extraction medium and extraction parameters could affect the properties of polysaccharides as well as influence their structure-activity relationship for biological activities.

    RESULTS: The result showed that the microwave-assisted extraction of Micromelum minutum leaf polysaccharide (MMLP) using DES as an extraction media (MMLP-DES) gave a higher yield (improvement of 101.20 %) than citric acid monohydrate (CAM) (MMLP-CAM) and required a lower percentage of microwave power (19.83 % less) and time (0.78 min less). The properties of MMLPs significantly differ based on their pH, molecular weight, viscosity, degree of esterification and monosaccharide molar ratio which influenced the biological activities. Compared to MMLP-CAM, MMLP-DES had a more branched and less linear structure. The bioactivities study revealed that MMLP-DES exhibited higher antioxidant and anti-α-amylase activities (i.e.

    , DPPH: 74.52 %, FRAP: 2.87 mM FeSO4 and α-amylase inhibition: 86.23 %) compared to MMLP-CAM (i.e.

    , DPPH: 49.33 %, FRAP: 1.49 mM FeSO4, and α-amylase inhibition: 81.76 %). The mechanism and structure-activity relationship of MMLPs on bioactivities were also hypothesized.

    SIGNIFICANCE: Based on our previous study, the citric acid monohydrate-glycerol based DES as an extraction medium has enhanced the extraction yield of polysaccharides from M. minutum. This study highlights the DES combined with microwave-assisted extraction to improve the yield of MMLP and evaluate the biological activities compared to CAM as a classical solvent. In conclusion, the DES showed the advantages for extraction of polysaccharides with desired biological activities.

    Matched MeSH terms: Biphenyl Compounds/chemistry; Meliaceae/chemistry
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