Displaying publications 201 - 220 of 6929 in total

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  1. Effects of Piper sarmentosum on Bone Health and Fracture Healing: A Scoping Review
    Ekeuku SO, Chin KY, Mohd Ramli ES
    Endocr Metab Immune Disord Drug Targets, 2023;23(7):908-916.
    PMID: 36453484 DOI: 10.2174/1871530323666221130152737
    BACKGROUND: Piper sarmentosum (PS) is a traditional herb used by Southeast Asian communities to treat various illnesses. Recent pharmacological studies have discovered that PS possesses antioxidant and anti-inflammatory activities. Since oxidative stress and inflammation are two important processes driving the pathogenesis of bone loss, PS may have potential therapeutic effects against osteoporosis.

    OBJECTIVE: This review systematically summarised the therapeutic effects of PS on preventing osteoporosis and promoting fracture healing.

    METHODS: A systematic literature search was performed in November 2021 using 4 electronic databases and the search string "Piper sarmentosum" AND (bone OR osteoporosis OR osteoblasts OR osteoclasts OR osteocytes).

    RESULTS: Nine unique articles were identified from the literature. The efficacy of PS has been studied in animal models of osteoporosis induced by ovariectomy and glucocorticoids, as well as bone fracture models. PS prevented deterioration of bone histomorphometric indices, improved fracture healing and restored the biomechanical properties of healed bone in ovariectomised rats. PS also prevented osteoblast/osteocyte apoptosis, increased bone formation and mineralisation and subsequently improved trabecular bone microstructures and strength of rats with osteoporosis induced by glucocorticoids. Apart from its antioxidant and anti-inflammatory activity, PS also suppressed circulating and skeletal expression of corticosterone and skeletal expression of 11β hydroxysteroid dehydrogenase type 1 but increased the enzyme activity in the glucocorticoid osteoporosis model. This review also identified several research gaps about the skeletal effects of PS and suggested future studies to bridge these gaps.

    CONCLUSION: PS may be of therapeutic benefit to bone health. However, further research is required to validate this claim.

    Matched MeSH terms: Anti-Inflammatory Agents/pharmacology; Antioxidants/pharmacology; Plant Extracts/pharmacology
  2. Fulltext Screening for natural and derived bio-active compounds in preclinical and clinical studies: One of the frontlines of fighting the coronaviruses pandemic
    Khalifa SAM, Yosri N, El-Mallah MF, Ghonaim R, Guo Z, Musharraf SG, et al.
    Phytomedicine, 2021 May;85:153311.
    PMID: 33067112 DOI: 10.1016/j.phymed.2020.153311
    BACKGROUND: Starting December 2019, mankind faced an unprecedented enemy, the COVID-19 virus. The world convened in international efforts, experiences and technologies in order to fight the emerging pandemic. Isolation, hygiene measure, diagnosis, and treatment are the most efficient ways of prevention and intervention nowadays. The health organizations and global care systems screened the available resources and offered recommendations of approved and proposed medications. However, the search for a specific selective therapy or vaccine against COVID-19 remains a challenge.

    METHODS: A literature search was performed for the screening of natural and derived bio-active compounds which showed potent antiviral activity against coronaviruses using published articles, patents, clinical trials website (https://clinicaltrials.gov/) and web databases (PubMed, SCI Finder, Science Direct, and Google Scholar).

    RESULTS: Through the screening for natural products with antiviral activities against different types of the human coronavirus, extracts of Lycoris radiata (L'Hér.), Gentiana scabra Bunge, Dioscorea batatas Decne., Cassia tora L., Taxillus chinensis (DC.), Cibotium barometz L. and Echinacea purpurea L. showed a promising effect against SARS-CoV. Out of the listed compound Lycorine, emetine dihydrochloride hydrate, pristimerin, harmine, conessine, berbamine, 4`-hydroxychalcone, papaverine, mycophenolic acid, mycophenolate mofetil, monensin sodium, cycloheximide, oligomycin and valinomycin show potent activity against human coronaviruses. Additionally, it is worth noting that some compounds have already moved into clinical trials for their activity against COVID-19 including fingolimod, methylprednisolone, chloroquine, tetrandrine and tocilizumab.

    CONCLUSION: Natural compounds and their derivatives could be used for developing potent therapeutics with significant activity against SARS-COV-2, providing a promising frontline in the fighting against COVID-19.

    Matched MeSH terms: Antiviral Agents/pharmacology*; Biological Products/pharmacology*; Plant Preparations/pharmacology
  3. Fulltext Chemical Composition and Antioxidant, Antimicrobial, and Anti-Inflammatory Properties of Origanum compactum Benth Essential Oils from Two Regions: In Vitro and In Vivo Evidence and In Silico Molecular Investigations
    Al-Mijalli SH, Mrabti NN, Ouassou H, Sheikh RA, Assaggaf H, Bakrim S, et al.
    Molecules, 2022 Oct 28;27(21).
    PMID: 36364152 DOI: 10.3390/molecules27217329
    The purposes of this investigatory study were to determine the chemical composition of the essential oils (EOs) of Origanum compactum from two Moroccan regions (Boulemane and Taounate), as well as the evaluation of their biological effects. Determining EOs' chemical composition was performed by a gas chromatography-mass spectrophotometer (GC-MS). The antioxidant activity of EOs was evaluated using free radical scavenging ability (DPPH method), fluorescence recovery after photobleaching (FRAP), and lipid peroxidation inhibition assays. The anti-inflammatory effect was assessed in vitro using the 5-lipoxygenase (5-LOX) inhibition test and in vivo using the carrageenan-induced paw edema model. Finally, the antibacterial effect was evaluated against several strains using the disk-diffusion assay and the micro-dilution method. The chemical constituent of O. compactum EO (OCEO) from the Boulemane zone is dominated by carvacrol (45.80%), thymol (18.86%), and α-pinene (13.43%). However, OCEO from the Taounate zone is rich in 3-carene (19.56%), thymol (12.98%), and o-cymene (11.16%). OCEO from Taounate showed higher antioxidant activity than EO from Boulemane. Nevertheless, EO from Boulemane considerably inhibited 5-LOX (IC50 = 0.68 ± 0.02 µg/mL) compared to EO from Taounate (IC50 = 1.33 ± 0.01 µg/mL). A similar result was obtained for tyrosinase inhibition with Boulemane EO and Taounate EO, which gave IC50s of 27.51 ± 0.03 μg/mL and 41.83 ± 0.01 μg/mL, respectively. The in vivo anti-inflammatory test showed promising effects; both EOs inhibit and reduce inflammation in mice. For antibacterial activity, both EOs were found to be significantly active against all strains tested in the disk-diffusion test, but O. compactum EO from the Boulemane region showed the highest activity. Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) for O. compactum EO from the Boulemane region ranged from 0.06 to 0.25% (v/v) and from 0.15 to 0.21% (v/v) for O. compactum from the Taounate region. The MBC/MIC index revealed that both EOs exhibited remarkable bactericidal effects.
    Matched MeSH terms: Anti-Inflammatory Agents/pharmacology; Anti-Bacterial Agents/pharmacology; Antioxidants/pharmacology
  4. Fulltext Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer
    Alfaleh MA, Fahmy O, Al-Rabia MW, Abourehab MAS, Ahmed OAA, Fahmy UA, et al.
    Sci Rep, 2022 Nov 14;12(1):19446.
    PMID: 36376469 DOI: 10.1038/s41598-022-24151-3
    As a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, Fluvastatin (FLV) is used for reducing low-density lipoprotein (LDL) cholesterol as well as to prevent cardiovascular problems. FLV showed cell line cytotoxicity and antitumor effect. Melittin (MEL) exhibits antineoplastic activity and is known to be promising as a therapeutic option for cancer patients. The aim of this work was to investigate the combination of FLV with MEL loaded hybrid formula of phospholipid (PL) with alpha lipoic acid (ALA) nanoparticles to maximize anticancer tendencies. This study examines the optimization of the prepared formulation in order to minimize nanoparticles size and maximize zeta potential to potentiate cytotoxic potentialities in colon cancer cells (Caco2), cell viability, cell cycle analysis and annexin V were tested. In addition to biological markers as P53, Bax, bcl2 and Caspase 3 evaluation The combination involving FLV PL ALA MEL showed enhanced cytotoxic potentiality (IC50 = 9.242 ± 0.35 µg/mL), about twofold lower, compared to the raw FLV (IC50 = 21.74 ± 0.82 µg/mL). According to studies analyzing cell cycle, optimized FLV PL ALA MEL was found to inhibit Caco2 colon cancer cells more significantly than other therapeutic treatments, wherein a higher number of cells were found to accumulate over G2/M and pre-G1 phases, whereas G0/G1/S phases witnessed the accumulation of a lower number of cells. The optimized formulation may pave the way for a novel and more efficacious treatment for colon cancer.
    Matched MeSH terms: Fatty Acids, Monounsaturated/pharmacology; Indoles/pharmacology; Melitten/pharmacology
  5. Nanoparticle-laden contact lens for controlled release of vancomycin with enhanced antibiotic efficacy
    Tong WY, Tan WN, Kamarul Azizi MA, Leong CR, El Azab IH, Lim JW, et al.
    Chemosphere, 2023 Oct;338:139492.
    PMID: 37451643 DOI: 10.1016/j.chemosphere.2023.139492
    Vancomycin is the last resort antibiotic for the treatment of severe bacterial keratitis. Its clinical application is limited due to its hydrophilicity and high molecular weight. To overcome this, this study aims to develop nanoparticles-laden contact lens for controlled ocular delivery of vancomycin. Polyvinyl alcohol (PVA) was used as encapsulant material. The nanoparticles had a negative surface charge and an average size of 147.6 nm. A satisfactory encapsulation efficiency (61.24%) was obtained. The release profile was observed to be slow and sustained, with a release rate of 1.29 μL mg-1 h-1 for 48 h. Five out of 6 test bacteria were suppressed by vancomycin nanoparticles-laden contact lens. Vancomycin is generally ineffective against Gram-negative bacteria and unable to pass through the outer membrane barrier. In this study, vancomycin inhibited Proteus mirabilis and Pseudomonas aeruginosa. Nano-encapsulation enables vancomycin to penetrate the Gram-negative cell wall and further destroy the bacterial cells. On Hohenstein challenge test, all test bacteria exhibited significant reduction in growth when exposed to vancomycin nanoparticles-laden contact lens. This study created an effective and long-lasting vancomycin delivery system via silicone hydrogel contact lenses, by using PVA as encapsulant. The antibiotic efficacy and vancomycin release should be further studied using ocular in vivo models.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Delayed-Action Preparations/pharmacology; Vancomycin/pharmacology
  6. Mechanistic insight into immunomodulatory effects of food-functioned plant secondary metabolites
    Ali Reza ASM, Nasrin MS, Hossen MA, Rahman MA, Jantan I, Haque MA, et al.
    Crit Rev Food Sci Nutr, 2023;63(22):5546-5576.
    PMID: 34955042 DOI: 10.1080/10408398.2021.2021138
    Medicinally important plant-foods offer a balanced immune function, which is essential for protecting the body against antigenic invasion, mainly by microorganisms. Immunomodulators play pivotal roles in supporting immune function either suppressing or stimulating the immune system's response to invading pathogens. Among different immunomodulators, plant-based secondary metabolites have emerged as high potential not only for immune defense but also for cellular immunoresponsiveness. These natural immunomodulators can be developed into safer alternatives to the clinically used immunosuppressants and immunostimulant cytotoxic drugs which possess serious side effects. Many plants of different species have been reported to possess strong immunomodulating properties. The immunomodulatory effects of plant extracts and their bioactive metabolites have been suggested due to their diverse mechanisms of modulation of the complex immune system and their multifarious molecular targets. Phytochemicals such as alkaloids, flavonoids, terpenoids, carbohydrates and polyphenols have been reported as responsible for the immunomodulatory effects of several medicinal plants. This review illustrates the potent immunomodulatory effects of 65 plant secondary metabolites, including dietary compounds and their underlying mechanisms of action on cellular and humoral immune functions in in vitro and in vivo studies. The clinical potential of some of the compounds to be used for various immune-related disorders is highlighted.
    Matched MeSH terms: Immunologic Factors/pharmacology; Plant Extracts/pharmacology; Phytochemicals/pharmacology
  7. Elettaria cardamomum essential oil; immunomodulatory, antioxidant, and anti-inflammatory effects for controlling acute Toxoplasma gondii infection
    Abdullah DA, Aishah EA
    Trop Biomed, 2023 Dec 01;40(4):453-461.
    PMID: 38308833 DOI: 10.47665/tb.40.4.011
    The present study was conducted to investigate the immunomodulatory and anti-inflammatory effects of Elettaria cardamomum essential oil (ECEO) for the control of acute Toxoplasma gondii infection. The effect of ECEO on T. gondii tachyzoites was measured by the tetrazolium bromide method. Mice received ECEO orally at doses of 1-4 mg/kg/day for 14 days. Once acute toxoplasmosis was induced in mice, their mortality rate and parasite load were recorded. The level of liver antioxidant/oxidant enzymes and the level of mRNA expression of interleukin-1 beta and interferongamma were also investigated. ECEO particularly at a concentration of 150 µg/ml has promising in vitro anti-Toxoplasma effects (p<0.001). After treatment with ECEO, the mortality rate (9th day) and parasite load decreased (p<0.001) in the infected mice. ECEO markedly (p < 0.05) restored hepatic oxidant and antioxidant enzyme levels, as well as increased cytokines. These results report a significant inhibitory effect of ECEO mainly at a dose of 4 mg/mL, against the T. gondii Rh strain through strengthening the immune system and reducing inflammation and oxidative stress; however, further research is needed to verify these results.
    Matched MeSH terms: Anti-Inflammatory Agents/pharmacology; Antioxidants/pharmacology; Oxidants/pharmacology
  8. Natural Terpenes Inhibit the Cytopathogenicity of Naegleria fowleri Causing Primary Amoebic Meningoencephalitis in the Human Cell Line Model
    Rajendran K, Ahmed U, Meunier AC, Shaikh MF, Siddiqui R, Anwar A
    ACS Chem Neurosci, 2023 Dec 06;14(23):4105-4114.
    PMID: 37983556 DOI: 10.1021/acschemneuro.3c00258
    Naegleria fowleri is one of the free-living amoebae and is a causative agent of a lethal and rare central nervous system infection called primary amoebic meningoencephalitis. Despite the advancement in antimicrobial chemotherapy, the fatality rate in the reported cases is more than 95%. Most of the treatment drugs used against N. fowleri infection are repurposed drugs. Therefore, a large number of compounds have been tested against N. fowleri in vitro, but most of the compounds showed high toxicity. To overcome this, we evaluated the effectiveness of naturally occurring terpene compounds against N. fowleri. In this study, we evaluated the antiamoebic potential of natural compounds including Thymol, Borneol, Andrographolide, and Forskolin againstN. fowleri. Thymol showed the highest amoebicidal activity with IC50/24 h at 153.601 ± 19.6 μM. Two combinations of compounds Forskolin + Thymol and Forskolin + Borneol showed a higher effect on the viability of trophozoites as compared to compounds alone and hence showed a synergistic effect. The IC50 reported for Forskolin + Thymol was 81.30 ± 6.86 μM. Borneol showed maximum cysticidal activity with IC50/24 h at 192.605 ± 3.01 μM. Importantly, lactate dehydrogenase release testing revealed that all compounds displayed minimal cytotoxicity to human HaCaT, HeLa, and SH-SY5Y cell lines. The cytopathogenicity assay showed that Thymol and Borneol also significantly reduced the host cell cytotoxicity of pretreated amoeba toward the human HaCaT cell line. So, these terpene compounds hold potential as therapeutic agents against infections caused by N. fowleri and are potentially a step forward in drug development against this deadly pathogen as these compounds have also been reported to cross the blood-brain barrier. Therefore, an in vivo study using animal models is necessary to assess the efficacy of these compounds and the need for further research into the intranasal route of delivery for the treatment of these life-threatening infections.
    Matched MeSH terms: Colforsin/pharmacology; Terpenes/pharmacology; Thymol/pharmacology
  9. Biochemical, Toxicological, and in Silico Aspects of Trillium govanianum Wall. ex D.Don (Trilliaceae): A Rich Source of Natural Bioactive Compounds
    Khan KM, Nadeem MF, Mannan A, Chohan TA, Islam M, Ansari SA, et al.
    Chem Biodivers, 2024 Jan;21(1):e202301375.
    PMID: 38031244 DOI: 10.1002/cbdv.202301375
    Trillium govanianum is a high-value medicinal herb, having multifunctional traditional and culinary uses. The present investigation was carried out to evaluate the phytochemical, biological and toxicological parameters of the T. govanianum Wall. ex D. Don (Family: Trilliaceae) roots collected from Azad Kashmir, Pakistan. Phytochemical profiling was achieved by determining total bioactive contents (total phenolic and flavonoid contents) and UHPLC-MS analysis. For biological evaluation, antioxidant activities (DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelation assays) and enzyme inhibition activities (against AChE, BChE, glucosidase, amylase, and tyrosinase) were performed. Moreover, cytotoxicity was assessed against three human carcinoma cell lines (MDA-MB-231, CaSki, and DU-145). The tested extract was found to contain higher total phenolics (7.56 mg GAE/g dry extract) as compared to flavonoid contents (0.45 mg RE/g dry extract). Likewise, for the antioxidant activity, higher CUPRAC activity was noted with 39.84 mg TE/g dry extract values. In the case of enzyme assays, higher activity was pointed out against the cholinesterase, glucosidase and tyrosinase enzymes. The plant extract displayed significant cytotoxicity against the cell lines examined. Moreover, the in-silico studies highlighted the interaction between the important phytochemicals and tested enzymes. To conclude, the assessed biological activity and the existence of bioactive phytochemicals in the studied plant extract may pave the way for the development of novel pharmaceuticals.
    Matched MeSH terms: Antioxidants/pharmacology; Flavonoids/pharmacology; Plant Extracts/pharmacology
  10. Surface contact toxicity and synergism of several insecticides against different stages of the tropical bed bug, Cimex hemipterus (Hemiptera: Cimicidae)
    How YF, Lee CY
    Pest Manag Sci, 2011 Jun;67(6):734-40.
    PMID: 21370390 DOI: 10.1002/ps.2123
    Five formulated insecticides (lambda-cyhalothrin at 10 mg m⁻², bifenthrin at 50 mg m⁻², fipronil at 10 mg m⁻², fenitrothion at 50 mg m⁻², imidacloprid at 5 mg m⁻²) and one active ingredient (DDT at 500 mg m⁻²) were evaluated using a surface contact method against early and late instars and adults of two strains of the tropical bed bug, Cimex hemipterus (F.). Synergism of lambda-cyhalothrin and fipronil using piperonyl butoxide (PBO) was also assessed.
    Matched MeSH terms: DDT/pharmacology; Fenitrothion/pharmacology; Imidazoles/pharmacology; Insecticides/pharmacology*; Nitriles/pharmacology; Nitro Compounds/pharmacology; Pesticide Synergists/pharmacology*; Piperonyl Butoxide/pharmacology; Pyrazoles/pharmacology; Pyrethrins/pharmacology
  11. Fulltext Cytotoxic and antioxidant compounds from the stem bark of Goniothalamus tapisoides Mat Salleh
    Kim RP, Bihud V, Bin Mohamad K, Leong KH, Bin Mohamad J, Bin Ahmad F, et al.
    Molecules, 2012 Dec 21;18(1):128-39.
    PMID: 23344192 DOI: 10.3390/molecules18010128
    Eleven compounds:goniomicin A (1), goniomicin B (2), goniomicin C (3), goniomicin D (4), tapisoidin (5), goniothalamin (6), 9-deoxygoniopypyrone (7), pterodondiol (8), liriodenine (9), benzamide (10) and cinnamic acid (11), were isolated from the stem bark of Goniothalamus tapisoides. All compounds were identified by spectroscopic analysis and, for known compounds, by comparison with published data. Goniothalamin (6) exhibited mild cytotoxic activity towards a colon cancer cell line (HT-29), with an IC(50)value of 64.17 ± 5.60 µM. Goniomicin B (2) give the highest antioxidant activity in the DPPH assay among all compounds tested, with an IC(50) of 0.207 µM.
    Matched MeSH terms: Antioxidants/pharmacology*; Aporphines/pharmacology; Benzamides/pharmacology; Cinnamates/pharmacology; Heterocyclic Compounds/pharmacology; Lactones/pharmacology; Plant Extracts/pharmacology*; Pyrans/pharmacology; Pyrones/pharmacology; Sesquiterpenes/pharmacology
  12. Fulltext Chemical Constituents of Malaysian U. cordata var. ferruginea and Their in Vitro α-Glucosidase Inhibitory Activities
    Abdullah NH, Salim F, Ahmad R
    Molecules, 2016 Apr 27;21(5).
    PMID: 27128898 DOI: 10.3390/molecules21050525
    Continuing our interest in the Uncaria genus, the phytochemistry and the in-vitro α-glucosidase inhibitory activities of Malaysian Uncaria cordata var. ferruginea were investigated. The phytochemical study of this plant, which employed various chromatographic techniques including recycling preparative HPLC, led to the isolation of ten compounds with diverse structures comprising three phenolic acids, two coumarins, three flavonoids, a terpene and an iridoid glycoside. These constituents were identified as 2-hydroxybenzoic acid or salicylic acid (1), 2,4-dihydroxybenzoic acid (2), 3,4-dihydroxybenzoic acid (3), scopoletin or 7-hydroxy-6-methoxy-coumarin (4), 3,4-dihydroxy-7-methoxycoumarin (5), quercetin (6), kaempferol (7), taxifolin (8), loganin (9) and β-sitosterol (10). Structure elucidation of the compounds was accomplished with the aid of 1D and 2D Nuclear Magnetic Resonance (NMR) spectral data and Ultraviolet-Visible (UV-Vis), Fourier Transform Infrared (FTIR) spectroscopy and mass spectrometry (MS). In the α-glucosidase inhibitory assay, the crude methanolic extract of the stems of the plant and its acetone fraction exhibited strong α-glucosidase inhibition activity of 87.7% and 89.2%, respectively, while its DCM fraction exhibited only moderate inhibition (75.3%) at a concentration of 1 mg/mL. The IC50 values of both fractions were found to be significantly lower than the standard acarbose suggesting the presence of potential α-glucosidase inhibitors. Selected compounds isolated from the active fractions were then subjected to α-glucosidase assay in which 2,4-dihydroxybenzoic acid and quercetin showed strong inhibitory effects against the enzyme with IC50 values of 549 and 556 μg/mL compared to acarbose (IC50 580 μg/mL) while loganin and scopoletin only showed weak α-glucosidase inhibition of 44.9% and 34.5%, respectively. This is the first report of the isolation of 2-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid and loganin from the genus and the first report of the α-glucosidase inhibitory potential of 2,4-dihydroxybenzoic acid.
    Matched MeSH terms: Coumarins/pharmacology; Flavonoids/pharmacology; Plant Extracts/pharmacology; Terpenes/pharmacology; Iridoid Glycosides/pharmacology; Hydroxybenzoates/pharmacology; Glycoside Hydrolase Inhibitors/pharmacology*
  13. Information overload in the teaching of pharmacology
    Achike FI, Ogle CW
    J Clin Pharmacol, 2000 Feb;40(2):177-83.
    PMID: 10664924
    Medical students are usually drawn from the best of students, but it is not unusual to see these brilliant students fail their exams or even dismissed from medical school because of poor academic performance. Information overload has been recognized as one of the major contributing factors to this problem. The situation is expected to get worse, with the ever-present technology-induced exponential growth in information. In discussing this issue, the authors echo the concerns of several experts regarding the content overload of medical school curricula, particularly in pharmacology. It is the increasing awareness of this problem that led the Association of American Medical Colleges and the General Medical Council of Britain to promote the concept of a core curriculum for each of the principal disciplines in medicine. Several medical schools have adopted the concept and also the problem-based learning approach, which focuses on ameliorating the complex problems associated with information growth in medical education. Based on the authors' experience as medical students, medical practitioners, and pharmacology teachers, they discuss the factors that contribute to information overload, from psychological and nonpsychological perspectives. Issues such as the design and structure of the curriculum, the quality of training and effectiveness of the teachers (clinically qualified vs. nonclinically qualified teachers), and the psychological preparedness of the students are discussed. The authors make suggestions for improvement.
    Matched MeSH terms: Pharmacology*
  14. The patterns and transmissibility of antibiotic resistance among clinical strains of Pseudomonas aeruginosa
    Palillo ES, Salleh MA
    Microbiol. Immunol., 1992;36(11):1195-200.
    PMID: 1491621
    Four hundred and ninety-eight predominantly pyocin-type 10 clinical strains of Pseudomonas aeruginosa were analyzed for resistance to carbenicillin, cefoperazone, cefotaxime, ceftazidime, gentamicin, amikacin and netilmicin. Based on NCCLS-recommended MIC breakpoints, 245 strains were found to be resistant, of which 41.6% were resistant to carbenicillin, 38% to gentamicin, 37.8% to netilmicin, 26.3% to cefoperazone, 17.9% to cefotaxime, 0.6% to amikacin and none to ceftazidime. Quadruple resistance to carbenicillin, cefoperazone, gentamicin and netilmicin was the most frequent pattern observed. Resistance to older antibiotics (kanamycin, streptomycin and tetracycline) and to mercuric chloride were also common. Conjugation experiments suggested that self-transmissible and non-transmissible plasmids occurred in at least 66 strains.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology; Carbenicillin/pharmacology; Cefoperazone/pharmacology; Cefotaxime/pharmacology; Ceftazidime/pharmacology; Cephalosporins/pharmacology; Tetracycline/pharmacology
  15. Pharmacodynamic optimization of warfarin therapy
    Doi SA
    Clin. Pharmacol. Ther., 1994 May;55(5):597-601.
    PMID: 8181204
    Pharmacokinetic-pharmacodynamic information regarding warfarin is used to produce a predictive model based on the idea that pharmacodynamic variability is more important than pharmacokinetic variability in the overall dose-response variability to warfarin. A modification of the maximum effect model is tested on a group of patients initiating oral anticoagulation with warfarin. Results indicate that the model can account for at least half of the total variation in maintenance doses observed (sample coefficient of determination, 0.53) and offer the physician a framework for dose requirements at the onset of therapy. The basic prediction equation is as follows: Maintenance dose = (11/international normalized ratio)-1, with a coefficient of correlation of 0.73 (95% confidence limits, 0.46-0.88). Application of this model may improve on the traditional empiric approach to warfarin dose adjustment.
    Matched MeSH terms: Warfarin/pharmacology*
  16. Selection, purification, and evaluation of acarbose-an α-glucosidase inhibitor from Actinoplanes sp
    Tuyen DT, Yew GY, Cuong NT, Hoang LT, Yen HT, Hong Thao PT, et al.
    Chemosphere, 2021 Feb;265:129167.
    PMID: 33307502 DOI: 10.1016/j.chemosphere.2020.129167
    Actinoplanes sp. A1094 strain had been selected for its high production of acarbose from 20 different strains of Actinoplanes sp. can be found in wild. The content for glucosidase inhibitor of acarbose concentration was recorded at 1.12 g/L. The conducted analysis of 16S rRNA sequence of Actinoplanes sp. A1094 showed 99% similar identity to the corresponding sequence of Actinoplanes hulinensis. Acarbose was purified from Actinoplanes hulinensis 1094 with a yield of 8.48%, purity of 98% and further identified by LC/MS and NMR methods (C25H43NO18; m/z: 645.6 g/mol). The purified acarbose was used to evaluate the hypoglycemia in streptozotocin (STZ)-induced diabetic mice model. The purified acarbose reduced postprandial blood glucose level in comparison with Glucobay® as medication for control type 2 diabetes in a combination therapy. Notably, the outcomes of native acarbose on fasting blood glucose levels in mice resemble akin to the commercial product and the acarbose accumulating fermentation and metabolic engineering from the cell gene in which would reduce in production cost. Therefore, acarbose from Actinoplanes hulinensis 1094 could be potentially used to make products for the treatment of type II diabetes.
    Matched MeSH terms: Glycoside Hydrolase Inhibitors/pharmacology
  17. Synthetic and Semi-synthetic Drugs as a Promising Therapeutic Option for the Treatment of COVID-19
    Shirbhate E, Patel P, Patel VK, Veerasamy R, Sharma PC, Sinha BN, et al.
    Mini Rev Med Chem, 2021;21(8):1004-1016.
    PMID: 33280595 DOI: 10.2174/1389557520666201204162103
    The novel coronavirus disease-19 (COVID-19) is a global pandemic that emerged from Wuhan, China, and has spread all around the world, affecting 216 countries or territories with 21,732,472 people infected and 770,866 deaths globally (as per WHO COVID-19 updates of August 18, 2020). Continuous efforts are being made to repurpose the existing drugs and develop vaccines for combating this infection. Despite, to date, no certified antiviral treatment or vaccine exists. Although, few candidates have displayed their efficacy in in vitro studies and are being repurposed for COVID- 19 treatment. This article summarizes synthetic and semi-synthetic compounds displaying potent activity in clinical uses or studies on COVID-19 and also focuses on the mode of action of drugs being repositioned against COVID-19.
    Matched MeSH terms: Antiviral Agents/pharmacology
  18. Therapeutic uses of Amaranthus caudatus L
    Jimoh MO, Afolayan AJ, Lewu FB
    Trop Biomed, 2019 Dec 01;36(4):1038-1053.
    PMID: 33597473
    The use of plants as therapy is not alien to man. Among plants that could offer novel choice to the limited therapeutic alternatives is Amaranthus caudatus. It is typically rich in bioactive compounds such as phenolic acids, lycopene, polyphenols, unsaturated fatty acids, glucosinolates, proteins, soluble peptides, flavonoids, squalene and betacarotene to say the least. As widely reported in the literature, its various capacities to fight diseases when ingested as food or medicine may not be unconnected to these bioactive compounds available in high concentrations. This current review, therefore, harmonized reports from scientific investigations that validated the use of A. caudatus for the treatment of various ailments such as Diabetes mellitus, cancer, malaria, hypercholesterolemia, atherosclerosis, helminthic and bacterial infections, inflammation, hepatic diseases and cardiovascular complications. With this, we hope to put in perspective, the key therapeutic options available in the plant.
    Matched MeSH terms: Phytochemicals/pharmacology*
  19. Fulltext Resistance patterns in DDT-resistant Aedes aegypti
    Busvine JR, Coker WZ
    Bull World Health Organ, 1958;18(4):651-6.
    PMID: 13536807
    Colonies of three strains of Aëdes aegypti resistant to DDT were obtained from Trinidad, Haiti and Malaya and reared beside a normal colony. From their relative resistance to a series of compounds analogous to DDT, characteristic resistance "spectra" were obtained. The two colonies from the West Indies showed a similar type of resistance, rather different from the (smaller) resistance of the Malay strain. No resistance to methoxychlor or dieldrin was found.
    Matched MeSH terms: DDT/pharmacology*
  20. Fulltext Resistance to insecticides in the larvae of Culex fatigans in Malaya
    Reid JA
    Bull World Health Organ, 1955;12(5):705-10.
    PMID: 14379006
    After two years' use of hexachlorocyclohexane (BHC) as a larvicide in Georgetown, on Penang Island, control of Culex fatigans breeding became unsatisfactory. Two laboratory colonies of fatigans were established, one from Georgetown, and one from Kuala Lumpur where no insecticides had been used; tests were then made to determine the median lethal concentrations (MLC) of BHC, dieldrin, and DDT for the larvae of the two strains. The Georgetown strain was found to have acquired a tenfold resistance to BHC, and also to dieldrin to which it had not been exposed, but it showed no significant increase of resistance to DDT, to which it had also not been exposed. A year later, when both strains had passed through some ten generations in the laboratory without exposure to insecticides, the Georgetown strain was found to have lost much of its resistance to BHC, although the MLC was still twice that of the non-resistant Kuala Lumpur strain.
    Matched MeSH terms: Insecticides/pharmacology*
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