Displaying publications 181 - 200 of 6929 in total

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  1. Reid JA
    Bull World Health Organ, 1960;22:586-7.
    PMID: 14437086
    Matched MeSH terms: DDT/pharmacology*; Dieldrin/pharmacology*; Insecticides/pharmacology*
  2. Chan EW, Wong SK, Chan HT
    J Integr Med, 2016 Jul;14(4):269-84.
    PMID: 27417173 DOI: 10.1016/S2095-4964(16)60261-3
    Apocynaceae is a large family of tropical trees, shrubs and vines with most species producing white latex. Major metabolites of species are triterpenoids, iridoids, alkaloids and cardenolides, which are known for a wide range of biological and pharmacological activities such as cardioprotective, hepatoprotective, neuroprotective, anti-inflammatory, anticancer and antimalarial properties. Prompted by their anticancer and antimalarial properties, the current knowledge on ten genera (Allamanda, Alstonia, Calotropis, Catharanthus, Cerbera, Dyera, Kopsia, Nerium, Plumeria and Vallaris) is updated. Major classes of metabolites are described using some species as examples. Species with antiproliferative (APF) and/or antiplasmodial (APM) properties have been identified. With the exception of the genus Dyera, nine genera of 22 species possess APF activity. Seven genera (Alstonia, Calotropis, Catharanthus, Dyera, Kopsia, Plumeria and Vallaris) of 13 species have APM properties. Among these species, Alstonia angustiloba, Alstonia macrophylla, Calotropis gigantea, Calotropis procera, Catharanthus roseus, Plumeria alba and Vallaris glabra displayed both APF and APM properties. The chemical constituents of these seven species are compiled for assessment and further research.
    Matched MeSH terms: Antimalarials/pharmacology*; Antineoplastic Agents, Phytogenic/pharmacology*; Plant Extracts/pharmacology*
  3. Tay JW, Lee CY
    J Econ Entomol, 2015 Jun;108(3):1237-42.
    PMID: 26470251 DOI: 10.1093/jee/tov079
    Budding and relocation of nests are important characteristics of the Pharaoh ant, Monomorium pharaonis (L.), an important pest of artificial structures. Pharaoh ant colony movements induced by several types of disturbances were evaluated in the laboratory. The percentages of workers and brood in the source and new nest sites were determined at Days 0, 1, 3, and 5 following physical disturbance (temporal removal of nestmates), chemical disturbance (application of pyrethroid insecticide), invasion by heterospecific ants, food depletion, and moisture depletion in the laboratory. All disturbances were performed in the source nest, which was connected to an empty new nest site. Almost all workers moved and carried the entire brood to the new nest site when subjected to physical disturbance, chemical disturbance, and ant invasion on Day 1, whereas only <5% of workers were present in the new nest site in the undisturbed control. After these disturbances, the brood was never relocated back to the original nest site in this 5-d study. When subjected to food depletion, ∼60% of the brood were found in the new nest site and ∼40% of the brood remained in the original nest on Day 5, resulting in a polydomous population. In contrast, moisture depletion did not show any significant effect on colony movement. These results provide useful information about the causes of Pharaoh ant colony budding and guidance about how to develop effective control and prevention strategies.
    Matched MeSH terms: Insecticides/pharmacology; Nitriles/pharmacology; Pyrethrins/pharmacology
  4. Alhajj M, Aziz MSA, Huyop F, Salim AA, Sharma S, Ghoshal SK
    Biomater Adv, 2022 Nov;142:213136.
    PMID: 36206587 DOI: 10.1016/j.bioadv.2022.213136
    This paper reports the characterization and antibacterial performance evaluation of some spherical and stable crystalline silver (Ag)/copper (Cu) nanocomposites (Ag-CuNCs) prepared in deionized water (DIW) using pulse laser ablation in liquid (PLAL) method. The influence of various laser fluences (LFs) on the structural, morphological, optical and antibacterial properties of these NCs were determined. The UV-Vis absorbance of these NCs at 403 nm and 595 nm was gradually increased accompanied by a blue shift. XRD patterns disclosed the nucleation of highly crystalline Ag-CuNCs with their face centered cubic lattice structure. TEM images showed the existence of spherical NCs with size range of 3-20 nm and lattice fringe spacing of approximately 0.145 nm. EDX profiles of Ag-CuNCs indicated their high purity. The antibacterial effectiveness of the Ag-CuNCs was evaluated by the inhibition zone diameter (IZD) and optical density (OD600) tests against Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacteria. The proposed NCs revealed the IZD values in the range of 22-26 mm and 20-25 mm when tested against E. coli and S. aureus bacteria, respectively. The Ag-CuNCs prepared at LF of 14.15 J/cm2 revealed the best bactericidal activity. It is established that by controlling the laser fluence the bactericidal effectiveness of the Ag-CuNCs can be tuned.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Copper/pharmacology; Silver/pharmacology
  5. Asghar M, Yahya R, Yap AUJ, Azzahari AD, Omar RA
    Caries Res, 2022;56(3):149-160.
    PMID: 35871511 DOI: 10.1159/000525505
    Silver diammine fluoride (SDF) is known as a noninvasive, cost-effective, safe, and simple method of dental caries treatment. However, staining and discoloration seem inseparable with SDF and continue as a cosmetic concern. Research is ongoing to overcome these issues, for example, by using glutathione (G) or potassium iodide among others. Therefore, the study aimed to investigate the effects of incorporating different concentrations of capping agents on SDF chemistry and SDF-mediated tooth staining at different time points. Tannic acid (TA), gallic acid (GA), carboxymethyl chitosan (CM), and G at different concentrations (5, 10, and 15% w/v) were incorporated in 30% SDF. FTIR and UV-Vis spectroscopies of the prepared solutions was performed to evaluate chemical changes. Time-dependent color changes (ΔE) in bovine dentine specimens (6 × 6 × 1 ± 0.25 mm3) were measured spectrophotometrically at application/washup, 1 and 3 h, after 1, 2, 4, 7, and 14 days. Results showed suppression of FTIR peaks at 3,358 cm-1 and 1,215 cm-1 in capping agent-modified SDF indicative of a successful capping effect of the silver ions, which was corroborated by UV-Vis blueshift of ∼∆32 nm. The capping effect on SDF increased proportionally with the concentrations of TA, GA, CM, and G used. A more pronounced tooth staining reduction however was shown more in TA- and G- rather than in GA- and CM-modified SDF. At day 14, SDF showed the highest mean ΔE(50.14 ± 2.14), while 15% TA showed the lowest ΔE(30.14 ± 0.81). In conclusion, capping agent incorporation significantly reduced SDF-mediated tooth staining. This reduction in staining is more dependent on the respective capping agent functional groups than concentrations per se. The potential of capping agents to minimize tooth staining of SDF was TA>G>CM>GA.
    Matched MeSH terms: Quaternary Ammonium Compounds/pharmacology; Cariostatic Agents/pharmacology; Fluorides, Topical/pharmacology
  6. Magalingam KB, Radhakrishnan A, Haleagrahara N
    Int J Immunopathol Pharmacol, 2016 Mar;29(1):30-9.
    PMID: 26542606 DOI: 10.1177/0394632015613039
    There is increasing evidence that free radicals induced oxidative stress is a major causative agent in the pathogenesis of neurodegenerative diseases, particularly Parkinson's disease. Quercetin glycosides, namely rutin and isoquercitrin, are flavonoid polyphenol compounds found ubiquitously in fruits and vegetables and have been known to possess antioxidant effects. This study was designed to compare the neuroprotective effects of quercetin glycosides rutin and isoquercitrin in 6-OHDA-induced rat pheochromocytoma (PC-12) cells. The results showed that both rutin and isoquercitrin significantly increased antioxidant enzymes, catalase, superoxide dismutase, glutathione peroxidase, and glutathione level that were attenuated by 6-OHDA in PC-12 cells. There was no significant difference in the activation of glutathione and glutathione peroxidase enzymes between rutin and isoquercitrin. These two glycosides were equally effective in suppressing lipid peroxidation in 6-OHDA-induced PC-12 cells as both compounds suppressed the malondialdehyde generation and prevented cell damage. In conclusion, quercetin glycosides rutin and isoquercetrin are having a significant neuroprotective effect against 6-OHDA toxicity in PC-12 cells.
    Matched MeSH terms: Quercetin/pharmacology; Rutin/pharmacology*; Neuroprotective Agents/pharmacology*
  7. Ali SG, Jalal M, Ahmad H, Umar K, Ahmad A, Alshammari MB, et al.
    Molecules, 2022 Dec 08;27(24).
    PMID: 36557818 DOI: 10.3390/molecules27248685
    Antimicrobial resistance has posed a serious health concern worldwide, which is mainly due to the excessive use of antibiotics. In this study, gold nanoparticles synthesized from the plant Tinospora cordifolia were used against multidrug-resistant Pseudomonas aeruginosa. The active components involved in the reduction and stabilization of gold nanoparticles were revealed by gas chromatography-mass spectrophotometry(GC-MS) of the stem extract of Tinospora cordifolia. Gold nanoparticles (TG-AuNPs) were effective against P. aeruginosa at different concentrations (50,100, and 150 µg/mL). TG-AuNPs effectively reduced the pyocyanin level by 63.1% in PAO1 and by 68.7% in clinical isolates at 150 µg/mL; similarly, swarming and swimming motilities decreased by 53.1% and 53.8% for PAO1 and 66.6% and 52.8% in clinical isolates, respectively. Biofilm production was also reduced, and at a maximum concentration of 150 µg/mL of TG-AuNPs a 59.09% reduction inPAO1 and 64.7% reduction in clinical isolates were observed. Lower concentrations of TG-AuNPs (100 and 50 µg/mL) also reduced the pyocyanin, biofilm, swarming, and swimming. Phenotypically, the downregulation of exopolysaccharide secretion from P. aeruginosa due to TG-AuNPs was observed on Congo red agar plates.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Gold/pharmacology; Pyocyanine/pharmacology
  8. Muchlisin ZA, Afriani D, Eriani K, Hasri I, Nur FM, Maulida S, et al.
    Cryo Letters, 2022;44(1):13-19.
    PMID: 36625871
    BACKGROUND: The cryopreservation of the sperm of the depik fish, Rasbora tawarensis, has previously been developed. However, the quality of the sperm post cryopreservation was not satisfactory and might be improved through the application of antioxidants.

    OBJECTIVE: To determine the most suitable antioxidant for the cryopreservation of the depik fish spermatozoa.

    MATERIALS AND METHODS: A completely randomized design with a non-factorial experiment was used and the tested antioxidants were glutathione, beta-carotene, ascorbic acid, and butylated hydroxytoluene (BHT) at 6 % concentrations. All treatments had three replications. The sperms were collected from 10 male fishes and diluted with Ringer solution in a ratio of 1: 20 (v/v, sperm: Ringer solution). Then 5% DMSO and 5 % egg yolk were added to the diluted sperms. Furthermore, 6 % of the tested antioxidants were added to the diluents, and then, cryopreservation was carried out in liquid nitrogen for 14 days.

    RESULTS: The ANOVA test showed that the application of antioxidants significantly affected the sperm motility, fertility, and hatching rates of the eggs (P < 0.05). Furthermore, the antioxidants also protected the sperm cells during cryopreservation, with glutathione being the best antioxidant.

    CONCLUSION: The application of antioxidants during the cryopreservation of depik fish sperm had a significant effect on motility, fertility and hatchability of eggs post-cryo. Furthermore, glutathione was the most suitable antioxidant. doi.org/10.54680/fr23110110312.

    Matched MeSH terms: Antioxidants/pharmacology; Cryoprotective Agents/pharmacology; Glutathione/pharmacology
  9. Muchlisin ZA, Afriani D, Eriani K, Hasri I, Nur FM, Maulida S, et al.
    Cryo Letters, 2023;44(1):13-19.
    PMID: 36629837
    BACKGROUND: The cryopreservation of the sperm of the depik fish, Rasbora tawarensis, has previously been developed. However, the quality of the sperm post cryopreservation was not satisfactory and might be improved through the application of antioxidants.

    OBJECTIVE: To determine the most suitable antioxidant for the cryopreservation of the depik fish spermatozoa.

    MATERIALS AND METHODS: A completely randomized design with a non-factorial experiment was used and the tested antioxidants were glutathione, beta-carotene, ascorbic acid, and butylated hydroxytoluene (BHT) at 6 % concentrations. All treatments had three replications. The sperms were collected from 10 male fishes and diluted with Ringer solution in a ratio of 1: 20 (v/v, sperm: Ringer solution). Then 5% DMSO and 5 % egg yolk were added to the diluted sperms. Furthermore, 6 % of the tested antioxidants were added to the diluents, and then, cryopreservation was carried out in liquid nitrogen for 14 days.

    RESULTS: The ANOVA test showed that the application of antioxidants significantly affected the sperm motility, fertility, and hatching rates of the eggs (P < 0.05). Furthermore, the antioxidants also protected the sperm cells during cryopreservation, with glutathione being the best antioxidant.

    CONCLUSION: The application of antioxidants during the cryopreservation of depik fish sperm had a significant effect on motility, fertility and hatchability of eggs post-cryo. Furthermore, glutathione was the most suitable antioxidant. doi.org/10.54680/fr23110110312.

    Matched MeSH terms: Antioxidants/pharmacology; Cryoprotective Agents/pharmacology; Glutathione/pharmacology
  10. Kao CY, Lin TL, Lin YH, Lee AK, Ng SY, Huang TH, et al.
    Cells, 2022 Dec 08;11(24).
    PMID: 36552731 DOI: 10.3390/cells11243967
    In scaffold-regulated bone regeneration, most three-dimensional (3D)-printed scaffolds do not provide physical stimulation to stem cells. In this study, a magnetic scaffold was fabricated using fused deposition modeling with calcium silicate (CS), iron oxide nanoparticles (Fe3O4), and poly-ε-caprolactone (PCL) as the matrix for internal magnetic sources. A static magnetic field was used as an external magnetic source. It was observed that 5% Fe3O4 provided a favorable combination of compressive strength (9.6 ± 0.9 MPa) and degradation rate (21.6 ± 1.9% for four weeks). Furthermore, the Fe3O4-containing scaffold increased in vitro bioactivity and Wharton's jelly mesenchymal stem cells' (WJMSCs) adhesion. Moreover, it was shown that the Fe3O4-containing scaffold enhanced WJMSCs' proliferation, alkaline phosphatase activity, and the osteogenic-related proteins of the scaffold. Under the synergistic effect of the static magnetic field, the CS scaffold containing Fe3O4 can not only enhance cell activity but also stimulate the simultaneous secretion of collagen I and osteocalcin. Overall, our results demonstrated that Fe3O4-containing CS/PCL scaffolds could be fabricated three dimensionally and combined with a static magnetic field to affect cell behaviors, potentially increasing the likelihood of clinical applications for bone tissue engineering.
    Matched MeSH terms: Iron/pharmacology; Oxides/pharmacology; Polyesters/pharmacology
  11. Alli YA, Ejeromedoghene O, Oladipo A, Adewuyi S, Amolegbe SA, Anuar H, et al.
    ACS Appl Bio Mater, 2022 Nov 21;5(11):5240-5254.
    PMID: 36270024 DOI: 10.1021/acsabm.2c00670
    Quaternary Trimethyl Chitosan (QTMC) and QTMC-Silver Nanoparticles (QTMC-AgNPs) have been synthesized, characterized, and tested as antibacterial agents against Staphylococcus aureus, Escherichia coli, and two plant fungi (Sclerotium rolfsil and Fusarium oxysporum). The as-prepared water-soluble QTMC was in situ reacted with silver nitrate in the presence of clean compressed hydrogen gas (3 bar) as a reducing agent to produce QTMC-AgNPs. UV-vis, ATR-FTIR, HR-TEM/SEM, XPS, DLS, XRD, and TGA/DTG were employed to assess the optical response, morphology/size, surface chemistry, particle size distribution, crystal nature, and thermal stability of the synthesized QTMC-AgNPs, respectively. The as-prepared QTMC-AgNPs were quasi-spherical in shape with an average particle size of 12.5 nm, as determined by ImageJ software utilizing HR-TEM images and further validated by DLS analysis. The development of crystalline nanoparticles was confirmed by the presence of distinct and consistent lattice fringes with an approximate interplanar d-spacing of 2.04 nm in QTMC-AgNPs. The QTMC-AgNPs exhibited significant antibacterial activity with a clear zone of inhibition of 30 mm and 26 mm around the disks against E. coli and S. aureus, respectively. In addition, QTMC-AgNPs showed highly efficient antifungal activity with 100% and 76.67% growth inhibition against two plant pathogens, S. rolfsii and F. oxysporum, respectively, whereas QTMC revealed no impact. Overall, QTMC-AgNPs showed a promising therapeutic potential and,thus, can be considered for drug design rationale.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Antifungal Agents/pharmacology; Silver/pharmacology
  12. Ahmad MA, Lim YH, Chan YS, Hsu CY, Wu TY, Sit NW
    Acta Pharm, 2022 Jun 01;72(2):317-328.
    PMID: 36651512 DOI: 10.2478/acph-2022-0013
    This study was conducted to evaluate the chemical composition and biological activities of the leaf extracts of Syzygium myrtifolium Walp. (Myrtaceae). The results indicate that the leaf extracts of S. myrtifolium contain various classes of phytochemicals (alkaloids, anthraquinones, flavonoids, phenolics, saponins, tannins and triterpenoids) and possess antioxidant, antibacterial, antifungal and antiviral activities. Ethyl acetate, ethanol, methanol, and water extracts exhibited significantly higher (p < 0.05) oxygen radical absorbance capacity and ferric-reducing antioxidant power than the hexane and chloroform extracts. However, all extracts exhibited stronger inhibitory activity against four tested species of yeasts (minimal inhibitory concentration: 0.02-0.31 mg mL-1) than against six tested species of bacteria (minimal inhibitory concentration: 0.16-1.25 mg mL-1). The ethanolic extract offered the highest protection of Vero cells (viability > 70 %) from the cytopathic effect caused by the Chikungunya virus while the ethyl acetate extract showed significant replication inhibitory activity against the virus (p < 0.001) using the replicon-enhanced green fluorescent protein reporter system.
    Matched MeSH terms: Antioxidants/pharmacology; Antiviral Agents/pharmacology; Plant Extracts/pharmacology
  13. Abdul Rahim R, Jayusman PA, Muhammad N, Mohamed N, Lim V, Ahmad NH, et al.
    PMID: 33805420 DOI: 10.3390/ijerph18073532
    Oxidative stress and inflammation are two common risk factors of various life-threatening disease pathogenesis. In recent years, medicinal plants that possess antioxidant and anti-inflammatory activities were extensively studied for their potential role in treating and preventing diseases. Spilanthes acmella (S. acmella), which has been traditionally used to treat toothache in Malaysia, contains various active metabolites responsible for its anti-inflammatory, antiseptic, and anesthetic bioactivities. These bioactivities were attributed to bioactive compounds, such as phenolic, flavonoids, and alkamides. The review focused on the summarization of in vitro and in vivo experimental reports on the antioxidant and anti-inflammatory actions of S. acmella, as well as how they contributed to potential health benefits in lowering the risk of diseases that were related to oxidative stress. The molecular mechanism of S. acmella in reducing oxidative stress and inflammatory targets, such as inducible nitric oxide synthase (iNOS), transcription factors of the nuclear factor-κB family (NF-κB), cyclooxygenase-2 (COX-2), and mitogen-activated protein kinase (MAPK) signaling pathways were discussed. Besides, the antioxidant potential of S. acmella was measured by total phenolic content (TPC), total flavonid content (TFC), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and superoxide anion radical scavenging (SOD) and thiobarbituric acid reactive substance (TBARS) assays. This review revealed that S. acmella might have a potential role as a reservoir of bioactive agents contributing to the observed antioxidant, anti-inflammatory, and health beneficial effects.
    Matched MeSH terms: Anti-Inflammatory Agents/pharmacology; Antioxidants/pharmacology; Plant Extracts/pharmacology
  14. Idris N, Leong KH, Wong EH, Abdul Rahim N
    J Antibiot (Tokyo), 2023 Dec;76(12):711-719.
    PMID: 37821539 DOI: 10.1038/s41429-023-00659-2
    Polymyxins are last-line antibiotics against multidrug-resistant Klebsiella pneumoniae but using polymyxins alone may not be effective due to emerging resistance. A previous study found that combining polymyxin B with chloramphenicol effectively kills MDR K. pneumoniae, although the bone marrow toxicity of chloramphenicol is concerning. The aim of this study is to assess the antibacterial efficacy and cytotoxicity of polymyxin B when combined with chloramphenicol and its derivatives, namely thiamphenicol and florfenicol (reported to have lesser toxicity compared to chloramphenicol). The antibacterial activity was evaluated with antimicrobial susceptibility testing using broth microdilution and time-kill assays, while the cytotoxic effect on normal bone marrow cell line, HS-5 was evaluated using the MTT assay. All bacterial isolates tested were found to be susceptible to polymyxin B, but resistant to chloramphenicol, thiamphenicol, and florfenicol when used alone. The use of polymyxin B alone showed bacterial regrowth for all isolates at 24 h. The combination of polymyxin B and florfenicol demonstrated additive and synergistic effects against all isolates (≥ 2 log10 cfu ml-1 reduction) at 4 and 24 h, respectively, while the combination of polymyxin B and thiamphenicol resulted in synergistic killing at 24 h against ATCC BAA-2146. Furthermore, the combination of polymyxin B with florfenicol had the lowest cytotoxic effect on the HS-5 cells compared to polymyxin B combination with chloramphenicol and thiamphenicol. Overall, the combination of polymyxin B with florfenicol enhanced bacterial killing against MDR K. pneumoniae and exerted minimal cytotoxic effect on HS-5 cell line.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Chloramphenicol/pharmacology; Polymyxins/pharmacology
  15. Lee JY, Wong CY, Koh RY, Lim CL, Kok YY, Chye SM
    Yale J Biol Med, 2024 Jun;97(2):205-224.
    PMID: 38947104 DOI: 10.59249/JNKB9714
    Neuroinflammation, toxic protein aggregation, oxidative stress, and mitochondrial dysfunction are key pathways in neurodegenerative diseases like Alzheimer's disease (AD). Targeting these mechanisms with antioxidants, anti-inflammatory compounds, and inhibitors of Aβ formation and aggregation is crucial for treatment. Marine algae are rich sources of bioactive compounds, including carbohydrates, phenolics, fatty acids, phycobiliproteins, carotenoids, fatty acids, and vitamins. In recent years, they have attracted interest from the pharmaceutical and nutraceutical industries due to their exceptional biological activities, which include anti-inflammation, antioxidant, anticancer, and anti-apoptosis properties. Multiple lines of evidence have unveiled the potential neuroprotective effects of these multifunctional algal compounds for application in treating and managing AD. This article will provide insight into the molecular mechanisms underlying the neuroprotective effects of bioactive compounds derived from algae based on in vitro and in vivo models of neuroinflammation and AD. We will also discuss their potential as disease-modifying and symptomatic treatment strategies for AD.
    Matched MeSH terms: Antioxidants/pharmacology; Biological Products/pharmacology; Neuroprotective Agents/pharmacology
  16. Ayipo YO, Ahmad I, Alananzeh W, Lawal A, Patel H, Mordi MN
    J Biomol Struct Dyn, 2023 Nov;41(19):10096-10116.
    PMID: 36476097 DOI: 10.1080/07391102.2022.2153168
    Antibiotic resistance (AR) remains one of the leading global health challenges, mostly implicated in disease-related deaths. The Enterobacteriaceae-producing metallo-β-lactamases (MBLs) are critically involved in AR pathogenesis through Zn-dependent catalytic destruction of β-lactam antibiotics, yet with limited successful clinical inhibitors. The efficacy of relevant broad-spectrum β-lactams including imipenem and meropenem are seriously challenged by their susceptibility to the Zn-dependent carbapenemase hydrolysis, as such, searching for alternatives remains imperative. In this study, computational molecular modelling and virtual screening methods were extensively applied to identify new putative Zn-sensitive broad-spectrum inhibitors of MBLs, specifically imipenemase-1 (IMP-1) from the IBScreen database. Three ligands, STOCK3S-30154, STOCK3S-30418 and STOCK3S-30514 selectively displayed stronger binding interactions with the enzymes compared to reference inhibitors, imipenem and meropenem. For instance, the ligands showed molecular docking scores of -9.450, -8.005 and -10.159 kcal/mol, and MM-GBSA values of -40.404, -31.902 and -33.680 kcal/mol respectively against the IMP-1. Whereas, imipenem and meropenem showed docking scores of -9.038 and -10.875 kcal/mol, and MM-GBSA of -31.184 and -32.330 kcal/mol respectively against the enzyme. The ligands demonstrated good thermodynamic stability and compactness in complexes with IMP-1 throughout the 100 ns molecular dynamics (MD) trajectories. Interestingly, their binding affinities and stabilities were significantly affected in contacts with the remodelled Zn-deficient IMP-1, indicating sensitivity to the carbapenemase active Zn site, however, with non-β-lactam scaffolds, tenable to resist catalytic hydrolysis. They displayed ideal drug-like ADMET properties, thus, representing putative Zn-sensitive non-β-lactam inhibitors of IMP-1 amenable for further experimental studies.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Imipenem/pharmacology; beta-Lactamase Inhibitors/pharmacology
  17. Ali JS, Saleem H, Mannan A, Zengin G, Mahomoodally MF, Locatelli M, et al.
    BMC Complement Med Ther, 2020 Oct 16;20(1):313.
    PMID: 33066787 DOI: 10.1186/s12906-020-03093-1
    BACKGROUND: Ethnobotanical and plant-based products allow for the isolation of active constituents against a number of maladies. Monotheca buxifolia is used by local communities due to its digestive and laxative properties, as well as its ability to cure liver, kidney, and urinary diseases. There is a need to explore the biological activities and chemical constituents of this medicinal plant.

    METHODS: In this work, the biochemical potential of M. buxifolia (Falc.) A. DC was explored and linked with its biological activities. Methanol and chloroform extracts from leaves and stems were investigated for total phenolic and flavonoid contents. Ultrahigh-performance liquid chromatography coupled with mass spectrometry (UHPLC-MS) was used to determine secondary-metabolite composition, while high-performance liquid chromatography coupled with photodiode array detection (HPLC-PDA) was used for polyphenolic quantification. In addition, we carried out in vitro assays to determine antioxidant potential and the enzyme-inhibitory response of M. buxifolia extracts.

    RESULTS: Phenolics (91 mg gallic-acid equivalent (GAE)/g) and flavonoids (48.86 mg quercetin equivalent (QE)/g) exhibited their highest concentration in the methanol extract of stems and the chloroform extract of leaves, respectively. UHPLC-MS analysis identified a number of important phytochemicals, belonging to the flavonoid, phenolic, alkaloid, and terpenoid classes of secondary metabolites. The methanol extract of leaves contained a diosgenin derivative and polygalacin D, while kaempferol and robinin were most abundant in the chloroform extract. The methanol extract of stems contained a greater peak area for diosgenin and kaempferol, whereas this was true for lucidumol A and 3-O-cis-coumaroyl maslinic acid in the chloroform extract. Rutin, epicatechin, and catechin were the main phenolics identified by HPLC-PDA analysis. The methanol extract of stems exhibited significant 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical-scavenging activities (145.18 and 279.04 mmol Trolox equivalent (TE)/g, respectively). The maximum cupric reducing antioxidant capacity (CUPRAC) (361.4 mg TE/g), ferric-reducing antioxidant power (FRAP) (247.19 mg TE/g), and total antioxidant potential (2.75 mmol TE/g) were depicted by the methanol extract of stems. The methanol extract of leaves exhibited stronger inhibition against acetylcholinesterase (AChE) and glucosidase, while the chloroform extract of stems was most active against butyrylcholinesterase (BChE) (4.27 mg galantamine equivalent (GALAE)/g). Similarly, the highest tyrosinase (140 mg kojic-acid equivalent (KAE)/g) and amylase (0.67 mmol acarbose equivalent (ACAE)/g) inhibition was observed for the methanol extract of stems.

    CONCLUSIONS: UHPLC-MS analysis and HPLC-PDA quantification identified a number of bioactive secondary metabolites of M. buxifolia, which may be responsible for its antioxidant potential and enzyme-inhibitory response. M. buxifolia can be further explored for the isolation of its active components to be used as a drug.

    Matched MeSH terms: Antioxidants/pharmacology*; Enzyme Inhibitors/pharmacology*; Plant Extracts/pharmacology*
  18. Jamalis J, Yusof FSM, Chander S, Wahab RA, P Bhagwat D, Sankaranarayanan M, et al.
    PMID: 31241020 DOI: 10.2174/1871523018666190625170802
    Psoralen or furocoumarin is a linear three ring heterocyclic compound. Psoralens are planar, tricyclic compounds, consisting of a furan ring fused to a coumarin moiety. Psoralen has been known for a wide spectrum of biological activities, spanning from cytotoxic, photosensitizing, insecticidal, antibacterial to antifungal effect. Thus, several structural changes were introduced to explore the role of specific positions with respect to the biological activity. Convenient approaches utilized for the synthesis of psoralen skeleton can be categorized into two parts: (i) the preparation of the tricyclic ring system from resorcinol, (ii) the exocyclic modification of the intact ring system. Furthermore, although psoralens have been used in diverse ways, we mainly focus in this work on their clinical utility for the treatment of psioraisis, vitiligo and skin-related disorder.
    Matched MeSH terms: Dermatologic Agents/pharmacology; Furocoumarins/pharmacology*; Photosensitizing Agents/pharmacology
  19. Aldurrah Z, Mohd Kauli FS, Abdul Rahim N, Zainal Z, Afzan A, Al Zarzour RH, et al.
    PMID: 37301417 DOI: 10.1016/j.cbpc.2023.109678
    Andrographis paniculata (A. paniculata) showed an anti-depressive effect in rodent models. Zebrafish has recently emerged as a worthy complementary translational model for antidepressant drug discovery study. This study investigates the anti-depressive effect of A. paniculata extract and andrographolide in the chronic unpredictable stress (CUS)- zebrafish model. Four groups of zebrafish (n = 10/group), i.e. control, CUS (stressed, untreated), CUS + A. paniculata (100 mg/L) and CUS + fluoxetine (0.01 mg/L) were assessed in open-field and social interaction tests, 24 h after treatment. After extract screening, behavioural and cortisol analysis of andrographolide (5, 25 and 50 mg/kg, i.p.) and fluoxetine (10 mg/kg, i.p.) were evaluated. Before the behavioural study, acute toxicity and characterization of A. paniculata extract using UHPLC-ESI-MS/MS were performed. A significant reduction in freezing duration was found in A. paniculata- (t-test, p = 0.0234) and fluoxetine-treated groups (t-test, p 
    Matched MeSH terms: Antidepressive Agents/pharmacology; Fluoxetine/pharmacology; Plant Extracts/pharmacology
  20. Delgado-Núñez EJ, López-Arellano ME, Olmedo-Juárez A, Díaz-Nájera JF, Ocampo-Gutiérrez AY, Mendoza-de Gives P
    Trop Biomed, 2023 Mar 01;40(1):108-114.
    PMID: 37356010 DOI: 10.47665/tb.40.1.017
    Haemonchus contortus (Hc) is a hematophagous parasite affecting the health and productivity of flocks. The administration of chemical anthelmintic drugs (AH) is the common method of deworming; however, generates resistance in the parasites to AH and it is a public health risk due to drug residues in milk, meat and sub-products. Natural compounds from plants are explored to diminish this parasitosis, improving their health and productivity, without the negative effects of AH. Ipomoea genus is a group of climbing plants belonging to the Convulvulaceae family possessing perennial leaves and tuberous roots. Medicinal properties has been attributed to this plant including nutritional agents, emetics, diuretics, diaphoretics, purgatives and pesticides. The objective of this study was assessing the in vitro nematocidal activity of a hydroalcoholic extract (HA-E) obtained from Ipomoea pauciflora (Cazahuate) flowers against Hc infective larvae (L3) and to identify its phytochemical profile (PhC-P). The assay was carried out using microtiter plates (MTP). Four HA-E concentrations were assessed and Ivermectin and distilled water were used as positive and negative control groups, respectively. Approximately 100 Hc L3 were deposited in each well (n=12) and incubated at 25-35°C for 7 days. Data were analyzed using ANOVA and a General Linear Model (GLM) followed by Tukey test (P<0.05). The treatments showing a concentration-dependent effect (CDE) were analyzed to identify their 50% and 90% lethal concentrations (CL50, 90) via a Probit Analysis. The highest mortality was observed at 50 mg/mL (82.64 ± 0.71%) and the lowest at 6.25 mg/mL (56.46 ± 2.49%), showing a CDE with increasing mortality from 6.25 to 50 mg/mL. The PhC-P revealed the presence of alkaloids, coumarins, flavonoids, tannins and triterpenes/ sterols. A HA-E from flowers of I. pauciflora will be considered to assess its potential use in the control of haemonchosis in small ruminants.
    Matched MeSH terms: Antinematodal Agents/pharmacology; Plant Extracts/pharmacology; Phytochemicals/pharmacology
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