Displaying publications 4561 - 4580 of 10396 in total

Abstract:
Sort:
  1. Characterization of thymoquinone/hydroxypropyl-β-cyclodextrin inclusion complex: Application to anti-allergy properties
    Al-Qubaisi MS, Rasedee A, Flaifel MH, Eid EEM, Hussein-Al-Ali S, Alhassan FH, et al.
    Eur J Pharm Sci, 2019 May 15;133:167-182.
    PMID: 30902654 DOI: 10.1016/j.ejps.2019.03.015
    Thymoquinone is an effective phytochemical compound in the treatment of various diseases. However, its practical administration has been limited due to poor aqueous solubility and bioavailability. In this work, we developed a novel inclusion complex of thymoquinone and hydroxypropyl-β-cyclodextrin that features improved solubility and bioactivity. The drug solubility was markedly accelerated in the increasing ratio of hydroxypropyl-β-cyclodextrin to thymoquinone amount. The formation of the thymoquinone/hydroxypropyl-β-cyclodextrin inclusion complex was evidenced using X-ray diffraction, differential scanning calorimetry, thermal gravimetric analysis, Fourier transform infrared, scanning electron microscopy and nuclear magnetic resonance. The release behavior of the complex, as well as of their mixtures, was examined in artificial gastric (pH 1.2) and intestinal (pH 6.8) dissolution media. The formulated complex released the drug rapidly at the initial stage, followed by a slow release. Thermodynamic parameters ΔH, ΔS and ΔG were calculated with temperatures ranging from 20 to 45 °C to evaluate the complexation process. The activity of the inclusion complex was evaluated on IgE-mediated allergic response in rat basophilic leukemia (RBL-2H3) cells by monitoring key allergic mediators. The results revealed that compared with free thymoquinone, the inclusion complex more strongly inhibited the release of histamine, tumor necrosis factor-α, and interleukin-4, and was not cytotoxic at the tested thymoquinone concentrations (0.125-4 μg/mL) indicating the inclusion complex possibly had better antiallergic effects. Our finding suggested that the inclusion complex achieved prolonged action and reduced side-effect of thymoquinone.
    Matched MeSH terms: Gastric Juice/chemistry; Intestinal Secretions/chemistry; Benzoquinones/chemistry; Anti-Allergic Agents/chemistry
  2. Fulltext Effect of freeze-dried Carica papaya leaf juice on inflammatory cytokines production during dengue virus infection in AG129 mice
    Norahmad NA, Mohd Abd Razak MR, Mohmad Misnan N, Md Jelas NH, Sastu UR, Muhammad A, et al.
    BMC Complement Altern Med, 2019 Feb 11;19(1):44.
    PMID: 30744623 DOI: 10.1186/s12906-019-2438-3
    BACKGROUND: Carica papaya leaves have been used for traditional treatment of dengue fever and have been reported to exhibit an immunomodulatory activity by affecting the level of cytokine production in vitro and in vivo. Due to the lack of adequate in vivo evidence in dengue disease model, the present study was initiated to screen and identify the cytokines affected by freeze-dried C. papaya leaf juice (FCPLJ) treatment in AG129 mice infected with DEN-2 dengue virus.

    METHODS: The AG129 mice were fed orally with FCPLJ for 3 consecutive days after 24 h of dengue virus inoculation. Plasma cytokines were screened by using ProcartaPlex immunoassay. The gene expression in the liver was analyzed by using RT2 Profiler PCR Array.

    RESULTS: The results showed that FCPLJ treatment has increased the plasma CCL2/MCP-1 level during peak of viremia. Gene expression study has identified 8 inflammatory cytokine genes which were downregulated in the liver of infected AG129 mice treated with FCPLJ. The downregulated inflammatory cytokine genes were CCL6/MRP-1, CCL8/MCP-2, CCL12/MCP-5, CCL17/TARC, IL1R1, IL1RN/IL1Ra, NAMPT/PBEF1 and PF4/CXCL4.

    CONCLUSION: The findings indicated the possible immunomodulatory role of FCPLJ during dengue virus infection in AG129 mice.

    Matched MeSH terms: Antiviral Agents/chemistry; Plant Extracts/chemistry; Plant Leaves/chemistry; Carica/chemistry*
  3. Formulation strategies for achieving high delivery efficiency of thymoquinone-containing Nigella sativa extract to the colon based on oral alginate microcapsules for treatment of inflammatory bowel disease
    Samak YO, Santhanes D, El-Massik MA, Coombes AGA
    J Microencapsul, 2019 Mar;36(2):204-214.
    PMID: 31164027 DOI: 10.1080/02652048.2019.1620356
    Nigella sativa extract (NSE) was incorporated in alginate microcapsules using aerosolisation and homogenisation methods, respectively, with the aim of delivering high concentrations of the active species, thymoquinone (TQ), directly to sites of inflammation in the colon following oral administration. Encapsulation of NSE was accomplished either by direct loading or diffusion into blank microparticles. Microcapsules in the size range 40-60 µm exhibited significantly higher NSE loading up to 42% w/w and encapsulation efficiency (EE) up to 63% when the extract was entrapped by direct encapsulation compared with 4.1 w/w loading, 6.2% EE when NSE was incorporated by diffusion loading. Sequential exposure of samples to simulated intestinal fluids (SIFs) revealed that the microcapsules suppressed NSE release in simulated gastric fluid (SGF) for 2 h and SIF for 4 h and liberated most of the NSE content (80%) in simulated colonic fluid (SCF) over 18 h. NSE released in SCF at 12 h exhibited antioxidant activity, when measured using the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) assay at levels comparable with the activity of unencapsulated extract. These findings demonstrate the potential of oral alginate microcapsules as highly efficient, targeted carriers for colonic delivery of NSE in the treatment of inflammatory bowel disease.
    Matched MeSH terms: Alginates/chemistry*; Capsules/chemistry; Drug Carriers/chemistry*; Nigella sativa/chemistry
  4. ASP2397: a novel antifungal agent produced by Acremonium persicinum MF-347833
    Nakamura I, Yoshimura S, Masaki T, Takase S, Ohsumi K, Hashimoto M, et al.
    J Antibiot (Tokyo), 2017 Jan;70(1):45-51.
    PMID: 27599768 DOI: 10.1038/ja.2016.107
    The novel antifungal agent ASP2397 (Vical's compound ID VL-2397) is produced by the fungal strain MF-347833 that was isolated from Malaysian leaf litter and is identified here as an Acremonium species based on its morphology, physiological properties and 28S ribosomal DNA sequence. Because of its potential importance for producing novel antifungal agents, we determined the taxonomic and biologic properties of MF-347833. We show here that ASP2397 is a cyclic hexapeptide that chelates aluminum ion and is therefore similar to ferrichrome, a hydroxamate siderophore. However, ASP2397 differs structurally from licensed antifungal agents such as amphotericin B, triazoles and echinocandins. To understand the relationship between chemical structure and biological function, we isolated certain ASP2397 derivatives from the culture broth, and we further chemically converted the metal-free form to other derivatives.
    Matched MeSH terms: Aluminum/chemistry; Antifungal Agents/chemistry; Peptides, Cyclic/chemistry; Coordination Complexes/chemistry
  5. Genetic relationship between Coptotermes gestroi and Coptotermes vastator (Isoptera: Rhinotermitidae)
    Yeap BK, Othman AS, Lee VS, Lee CY
    J Econ Entomol, 2007 Apr;100(2):467-74.
    PMID: 17461072
    The phylogenetic relationship of Coptotermes gestroi (Wasmann) and Coptotermes vastator Light (Isoptera: Rhinotermitidae) was determined using DNA sequence comparisons of mitochondrial genes. Partial sequences of the ribosomal RNA small subunit 12S, ribosomal RNA large subunit 16S, and mitochondrial COII were obtained from nine populations of C. gestroi from South East Asia (Malaysia, Singapore, Thailand, and Indonesia) and four populations of C. vastator from the Philippines and Hawaii. In addition, four populations of Coptotermes formosanus Shiraki and Globitermes sulphureus (Haviland) were used as the outgroups. Consensus sequences were obtained and aligned. C. vastator and C. gestroi are synonymous, based on high sequence homology across the 12S, 16S, and COII genes. The interspecific pairwise sequence divergence, based on Kimura 2-parameter model between C. gestroi and C. vastator, varied only up to 0.80%. Morphometric measurements of 16 characteristics revealed numerous overlaps between the examined individuals of both species. Based on the molecular phylogenetics and morphometric data, it is proposed that C. vastator is a junior synonym of C. gestroi.
    Matched MeSH terms: Electron Transport Complex IV/chemistry; DNA, Mitochondrial/chemistry; RNA, Ribosomal/chemistry; RNA, Ribosomal, 16S/chemistry
  6. Expression and characterization of anticoagulant activity of salivary protein alALP from Asian tiger mosquito Aedes albopictus
    Li XP, Lin D, Zhang Y, Chen SQ, Bai HQ, Zhang SN, et al.
    Trop Biomed, 2020 Mar 01;37(1):116-126.
    PMID: 33612723
    Several bioactive molecules isolated from the saliva of blood-sucking arthropods, such as mosquitoes, have been shown to exhibit potential anticoagulant function. We have previously identified a 30kDa allergen named Aegyptin-like protein (alALP), which is highly homologous to Aegyptin, from the salivary glands of female Aedes albopictus (Asian tiger mosquito). In this study, we identified the conserved functional domain of alALP by using bioinformatic tools, and expressed the His-tagged alALP recombinant protein in sf9 insect cells by generation and transfection of a baculoviral expression plasmid carrying the fulllength cDNA of alALP. We purified this recombinant protein and examined its function on the inhibition of blood coagulation. The results showed that the purified His-alALP prolonged the Activated Partial Thromboplastin Time (APTT), Prothrombin Time (PT) and Thrombin Time (TT) in vitro as well as the Bleeding Time (BT) in vivo, which suggest that alALP could be a novel anticoagulant.
    Matched MeSH terms: Anticoagulants/chemistry*; Recombinant Proteins/chemistry; Salivary Proteins and Peptides/chemistry*; Insect Proteins/chemistry*
  7. Evaluation of the in vitro antileishmanial activities of bioactive guided fractionations of two medicinal plants
    Al Nasr IS
    Trop Biomed, 2020 Mar 01;37(1):15-23.
    PMID: 33612714
    The organisms of the genus Leishmania are flagellated protozoan parasites and are the causative agents of leishmaniasis. This disease is a major health problem, especially in tropical countries. Currently, cutaneous leishmaniasis is treated by chemotherapy using pentavalent antimonials, but these drugs have serious organo-toxicity, drug resistance on several occasions, and low efficiency in controlling the infection. The present work is carried out to evaluate the in vitro antileishmanial activity of methanolic extracts and phytochemical fractions of two plants ethnobotanically used against leishmaniasis and skin infection, Calotropis procera and Rhazya stricta leaves against Leishmania major promastigote and amastigote stages and cytotoxicity against the Vero cell line. The leaves of C. procera and R. stricta were extracted with methanol and fractionated by petroleum ether, chloroform, ethyl acetate, n-butanol, and water. The methanolic extracts of the leaves of C. procera and R. stricta exhibited antileishmanial activity against L. major promastigotes with IC50 values of 66.8 and 42.4 µg mL-1, respectively. While their CC50 2.3 and 298 µg mL-1 and their SI 0.03 and 7.03 respectively. However, the fractionations of the methanolic extract of C. procera leaves revealed antiparasitic activity against both L. major promastigote and amastigote stages in vitro, which significantly increased with polarity with the exception of n-butanol. Hence the best activity was revealed by the water fraction (IC50 of 26.3 and 29.0 µg mL-1) for the two stages. In conclusion, further phytochemical investigation should be performed for the C. procera water extract in terms of antileishmanial active ingredient isolation that may enhance the possibility of avoiding toxic substances and overcome the low SI (1.1 and 1.01).
    Matched MeSH terms: Plants, Medicinal/chemistry; Plant Leaves/chemistry; Apocynaceae/chemistry*; Calotropis/chemistry*
  8. Comparative evaluation of the degree of pegylation of poly(lactic-co-glycolic acid) nanoparticles in enhancing central nervous system delivery of loperamide
    Kirby BP, Pabari R, Chen CN, Al Baharna M, Walsh J, Ramtoola Z
    J Pharm Pharmacol, 2013 Oct;65(10):1473-81.
    PMID: 24028614 DOI: 10.1111/jphp.12125
    In this study, we examined the relative cellular uptake of nanoparticles (NPs) formulated using poly(lactic-co-glycolic acid) (PLGA) polymers with increasing degree of pegylation (PLGA-PEG) and their potential to deliver loperamide to the brain of a mouse.
    Matched MeSH terms: Drug Carriers/chemistry*; Polyglycolic Acid/chemistry*; Lactic Acid/chemistry*; Nanoparticles/chemistry*
  9. Discovery of α-Glucosidase Inhibitors from Marine Microorganisms: Optimization of Culture Conditions and Medium Composition
    Trang NTH, Tang DYY, Chew KW, Linh NT, Hoang LT, Cuong NT, et al.
    Mol Biotechnol, 2021 Nov;63(11):1004-1015.
    PMID: 34185249 DOI: 10.1007/s12033-021-00362-3
    Various studies showed that the suppression of α-glucosidase activity can impede the glucose absorption in our body, and therefore, it can be used to treat type 2 diabetes. Hence, the compounds with anti-α-glucosidase have gained considerable attention because of their potential application in diabetes treatment. In previous literature studies, these anti-α-glucosidase compounds were extracted from plants and fungus. Less studies are being conducted to identify the anti-α-glucosidase compounds in the microbial community. In this study, 23 marine bacterial strains were screened for their potential to suppress the α-glucosidase activity. The highest inhibitory activity was exhibited by isolated L06 which was identified as Oceanimonas smirnovii EBL6. The cultivation conditions, such as temperature and pH, were optimized to increase the production of α-glucosidase inhibitors by Oceanimonas smirnovii EBL6 strain. The result findings showed that the highest yield of α-glucosidase inhibitors can be obtained at the culture time of 120 h, fermentation temperature of 30 °C, and pH 4.6. Under these conditions, the inhibitory activity of α-glucosidase can reach 81%. The IC50 of n-butanol extract was 13.89 μg/ml, while standard acarbose was 31.16 μg/ml. Overall, these findings suggest that Oceanimonas smirnovii produces α-glucosidase inhibitors and could been applied in the biochemical and medicinal fields in the future.
    Matched MeSH terms: alpha-Glucosidases/chemistry*; Aeromonadaceae/chemistry; Aquatic Organisms/chemistry*; Glycoside Hydrolase Inhibitors/chemistry*
  10. The production and characterisation of trichotoxin peptaibols, by Trichoderma asperellum
    Chutrakul C, Alcocer M, Bailey K, Peberdy JF
    Chem Biodivers, 2008 Sep;5(9):1694-706.
    PMID: 18816522 DOI: 10.1002/cbdv.200890158
    Trichoderma spp. are regularly found as a constituent of the mycoflora of many soils and are noted for their antagonistic activity against bacteria and other fungi. This latter property is the basis for the widespread interest in their use in the biological control of soil-borne fungal plant pathogens. This antagonism is partly based on their ability to produce an impressive inventory of secondary metabolites. An important group of bioactive metabolites produced by Trichoderma spp. are the non-ribosomal peptides (NRPs), especially the peptaibols. A virulent antagonistic strain, T. asperellum, which had been used in biological control strategies in Malaysia and previously examined for mycolytic enzyme production, has been studied for its potential for peptaibol production. The present research demonstrated the ability of T. asperellum to produce at least two metabolites which were identified as acid trichotoxin 1704E (Ac-Aib-Gly-Aib-Leu-Aib-Gln-Aib-Aib-Aib-Ala-Ala-Aib-Pro-Leu-Aib-Iva-Glu-Vol) and neutral trichotoxin 1717A (Ac-Aib-Gly-Aib-Leu-Aib-Gln-Aib-Aib-Aib-Ala-Aib-Aib-Pro-Leu-Aib-Iva-Gln-Vol). Addition of free Aib to the culture medium enhanced the production of trichotoxins. Biological activity of these substances was investigated against Bacillus stearothermophilus. The general characteristics of peptaibols, also found in the trichotoxins, include the presence of high proportions of the uncommon amino acid Aib, the protection of the N- and C-termini by an acetyl group and reduction of the C-terminus to 2-amino alcohols, respectively, amphipathy and microheterogeneity.
    Matched MeSH terms: Anti-Bacterial Agents/chemistry; Peptides/chemistry*; Trichoderma/chemistry*; Peptaibols/chemistry*
  11. Fulltext Effect of tiger milk mushroom (Lignosus rhinocerus) supplementation on respiratory health, immunity and antioxidant status: an open-label prospective study
    Tan ESS, Leo TK, Tan CK
    Sci Rep, 2021 06 03;11(1):11781.
    PMID: 34083710 DOI: 10.1038/s41598-021-91256-6
    Tiger milk mushroom (TMM; Lignosus rhinocerus) have been used for a long time by indigenous communities in South East Asia regions as traditional medicine for different ailments, including respiratory disorders. The beneficial effects of TMM have been proven through in vivo and in vitro models, but these effects have yet to be validated in a clinical study. In this study, the beneficial effects of TMM supplementation were investigated in 50 voluntary participants. Participants were required to take 300 mg of TMM twice daily for three months. Level of interleukin 1β (IL-1β), interleukin 8 (IL-8), immunoglobulin A (IgA), total antioxidant capacity, malondialdehyde (MDA), 3-nitrotyrosine (3-NT), 8-hydroxydeoxyguanosine (8-OHdG), pulmonary function and respiratory symptoms were assessed during baseline and monthly follow-up visits. Results demonstrated that supplementation of TMM significantly (p 
    Matched MeSH terms: Agaricales/chemistry*; Antioxidants/chemistry; Immunologic Factors/chemistry; Polyporaceae/chemistry*
  12. A new bis-labdanic diterpene from the rhizomes of Alpinia pahangensis
    Sivasothy Y, Ibrahim H, Paliany AS, Alias SA, Md Nor NR, Awang K
    Planta Med, 2013 Dec;79(18):1775-80.
    PMID: 24356874 DOI: 10.1055/s-0033-1351075
    The rhizomes of Alpinia pahangensis yielded a new bis-labdanic diterpene for which the name pahangensin C (1) was proposed along with twelve known analogues (2-13). The structure of 1 was elucidated via spectroscopic methods including 1D and 2D NMR techniques and LCMS-IT-TOF analysis. Compounds 2 and 12 were isolated for the first time from the genus Alpinia. This is the second occurrence of compounds 2 and 12 in the Zingiberaceae family. Selected analogues exhibited moderate to strong inhibitory activity against Staphylococcus aureus and Bacillus cereus.
    Matched MeSH terms: Diterpenes/chemistry; Plant Extracts/chemistry; Rhizome/chemistry*; Alpinia/chemistry*
  13. Size-dependent effect of cystine/citric acid-capped confeito-like gold nanoparticles on cellular uptake and photothermal cancer therapy
    Saw WS, Ujihara M, Chong WY, Voon SH, Imae T, Kiew LV, et al.
    Colloids Surf B Biointerfaces, 2018 Jan 01;161:365-374.
    PMID: 29101882 DOI: 10.1016/j.colsurfb.2017.10.064
    Physiochemical changes, including size, are known to affect gold nanoparticle cellular internalization and treatment efficacy. Here, we report the effect of four sizes of cystine/citric acid-coated confeito-like gold nanoparticles (confeito-AuNPs) (30, 60, 80 and 100nm) on cellular uptake, intracellular localization and photothermal anticancer treatment efficiency in MDA-MB231 breast cancer cells. Cellular uptake is size dependent with the smallest size of confeito-AuNPs (30nm) having the highest cellular internalization via clathrin- and caveolae-mediated endocytosis. However, the other three sizes (60, 80 and 100nm) utilize clathrin-mediated endocytosis for cellular uptake. The intracellular localization of confeito-AuNPs is related to their endocytosis mechanism, where all sizes of confeito-AuNPs were localized highly in the lysosome and mitochondria, while confeito-AuNPs (30nm) gave the highest localization in the endoplasmic reticulum. Similarly, a size-dependent trend was also observed in in vitro photothermal treatment experiments, with the smallest confeito-AuNPs (30nm) giving the highest cell killing rate, whereas the largest size of confeito-AuNPs (100nm) displayed the lowest photothermal efficacy. Its desirable physicochemical characteristics, biocompatible nature and better photothermal efficacy will form the basis for further development of multifunctional confeito-AuNP-based nanotherapeutic applications.
    Matched MeSH terms: Cystine/chemistry*; Gold/chemistry*; Citric Acid/chemistry*; Metal Nanoparticles/chemistry*
  14. Devosia elaeis sp. nov., isolated from oil palm rhizospheric soil
    Mohd Nor MN, Sabaratnam V, Tan GYA
    Int J Syst Evol Microbiol, 2017 Apr;67(4):851-855.
    PMID: 27902276 DOI: 10.1099/ijsem.0.001683
    A bacterial isolate, designated strain S37T, was isolated from the rhizosphere of oil palm (Elaeis guineensis). Strain S37T was found to be Gram-stain-negative, aerobic, motile and rod shaped. Based on 16S rRNA gene sequence analysis, strain S37T was most closely related to Devosia albogilva IPL15T (97.3 %), Devosia chinhatensis IPL18T (96.8 %) and Devosia subaequoris HST3-14T (96.5 %). The G+C content of the genomic DNA was 63.0 mol%, and dominant cellular fatty acids were summed feature 8 (C18 : 1ω7c and/or C18 : 1ω6c), 11-methyl C18 : 1ω7c and C16 : 0. The predominant isoprenoid quinone was ubiquinone-10 (Q-10), and the major polar lipids were phosphatidylglycerol, diphosphatidylglycerol, glycolipid and phospholipids. Based on the polyphasic taxonomic data, it is clear that strain S37T represents a novel species of the genus Devosia within the family Hyphomicrobiaceae, for which we propose the name Devosia elaeis sp. nov., with strain S37T (=TBRC 5145T=LMG 29420T) as the type strain.
    Matched MeSH terms: Fatty Acids/chemistry; Glycolipids/chemistry; Phospholipids/chemistry; Ubiquinone/chemistry
  15. A Review on the Antinociceptive Effects of Mitragyna speciosa and Its Derivatives on Animal Model
    Chin KY, Mark-Lee WF
    Curr Drug Targets, 2018;19(12):1359-1365.
    PMID: 28950813 DOI: 10.2174/1389450118666170925154025
    Mitragyna speciosa is a tropical plant with narcotic effects. The antinociceptive effects of its crude extracts, bioactive compounds and structurally modified derivatives have been examined in rodent models. This review aims to summarize the evidence on the antinociceptive effects of M. speciosa and its derivatives and explore whether they can offer an alternative to morphine in pain management. Methanolic and alkaloid extracts of M. speciosa were shown to attenuate the nociceptive response in rodents. Mitragynine and 7-hydroxymitragynine offered better antinociceptive effects than crude extracts. Structurally modified derivatives of 7-hydroxymitragynine, such as MGM-9, MGM- 15, MGM-16, demonstrated superior antinociceptive effects compared to morphine. M. speciosa and its derivatives mainly act on the opioid receptor, but receptor subtypes specificity differs between each compound. The tolerance and adverse side effects of M. speciosa and its derivatives are similar with morphine. The affinity of MGM-9 on kappa-opioid receptor could potentially limit the effects of drug dependence. In conclusion, M speciosa derivatives can offer alternatives to morphine in controlling chronic pain. Structural modification of mitragynine and 7-hydroxymitragynine can generate compounds with higher potency and lesser side-effects. Human clinical trials are required to validate the use of these compounds in clinical setting.
    Matched MeSH terms: Analgesics/chemistry; Narcotic Antagonists/chemistry; Plant Extracts/chemistry; Mitragyna/chemistry*
  16. Comparative efficacy of hemorrhage control of a novel mesoporous bioactive glass versus two commercial hemostats
    Pourshahrestani S, Kadri NA, Zeimaran E, Gargiulo N, Samuel S, Naveen SV, et al.
    Biomed Mater, 2018 02 08;13(2):025020.
    PMID: 29148431 DOI: 10.1088/1748-605X/aa9b3e
    Mesoporous bioactive glass containing 1% Ga2O3 (1%Ga-MBG) is attractive for hemorrhage control because of its surface chemistry which can promote blood-clotting. The present study compares this proprietary inorganic coagulation accelerator with two commercial hemostats, CeloxTM (CX) and QuikClot Advanced Clotting Sponge PlusTM (ACS+). The results indicate that the number of adherent platelets were higher on the 1%Ga-MBG and CX surfaces than ACS+ whereas a greater contact activation was seen on 1%Ga-MBG and ACS+ surfaces than CX. 1%Ga-MBG not only resulted in larger platelet aggregates and more extensive platelet pseudopodia compared to CX and ACS+ but also significantly accelerated the intrinsic pathways of the clotting cascade. In vitro thrombin generation assays also showed that CX and ACS+ induced low levels of thrombin formation while 1%Ga-MBG had significantly higher values. 1%Ga-MBG formed a larger red blood cell aggregate than both CX and ACS+. Direct exposure of 1%Ga-MBG to fibroblast cells increased cell viability after 3 days relative to CX and ACS+, inferring excellent cytocompatibility. The results of this study promote 1%Ga-MBG as a promising hemostat compared to the commercially available products as it possesses essential factors required for coagulation activation.
    Matched MeSH terms: Biocompatible Materials/chemistry*; Thrombin/chemistry; Water/chemistry; Tissue Scaffolds/chemistry*
  17. Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae)
    Wan Othman WNN, Liew SY, Khaw KY, Murugaiyah V, Litaudon M, Awang K
    Bioorg Med Chem, 2016 09 15;24(18):4464-4469.
    PMID: 27492195 DOI: 10.1016/j.bmc.2016.07.043
    Alzheimer's disease is the most common form of dementia among older adults. Acetylcholinesterase and butyrylcholinesterase are two enzymes involved in the breaking down of the neurotransmitter acetylcholine. Inhibitors for these enzymes have potential to prolong the availability of acetylcholine. Hence, the search for such inhibitors especially from natural products is needed in developing potential drugs for Alzheimer's disease. The present study investigates the cholinesterase inhibitory activity of compounds isolated from three Cryptocarya species towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Nine alkaloids were isolated; (+)-nornantenine 1, (-)-desmethylsecoantofine 2, (+)-oridine 3, (+)-laurotetanine 4 from the leaves of Cryptocarya densiflora BI., atherosperminine 5, (+)-N-methylisococlaurine 6, (+)-N-methyllaurotetanine 7 from the bark of Cryptocarya infectoria Miq., 2-methoxyatherosperminine 8 and (+)-reticuline 9 from the bark of Cryptocarya griffithiana Wight. In general, most of the alkaloids showed higher inhibition towards BChE as compared to AChE. The phenanthrene type alkaloid; 2-methoxyatherosperminine 8, exhibited the most potent inhibition against BChE with IC50 value of 3.95μM. Analysis of the Lineweaver-Burk (LB) plot of BChE activity over a range of substrate concentration suggested that 2-methoxyatherosperminine 8 exhibited mixed-mode inhibition with an inhibition constant (Ki) of 6.72μM. Molecular docking studies revealed that 2-methoxyatherosperminine 8 docked well at the choline binding site and catalytic triad of hBChE (butyrylcholinesterase from Homo sapiens); hydrogen bonding with Tyr 128 and His 438 residues respectively.
    Matched MeSH terms: Alkaloids/chemistry; Cholinesterase Inhibitors/chemistry; Isoquinolines/chemistry; Cryptocarya/chemistry
  18. Challenges in pediatric drug use: A pharmacist point of view
    Balan S, Hassali MA, Mak VSL
    Res Social Adm Pharm, 2017 May-Jun;13(3):653-655.
    PMID: 27493130 DOI: 10.1016/j.sapharm.2016.06.014
    The pediatric population is an enormously diverse segment of population varying both in size and age. The diversity caused pharmacists face various challenges primarily related to procuring, provision as well as use of drugs in this group of patients. Pediatric dose calculation is particularly a concern for pharmacists. Another challenge faced by pharmacists is unavailability of suitable formulations for pediatric use. This has also led many pharmacists to prepare extemporaneous liquid preparations, even though stability data on such preparations are scarce. Some extemporaneous preparations contain excipients which are potentially harmful in children. Besides that, inadequate labeling and drug information for pediatric drug use had not only challenged pharmacists in recommending and optimizing drug use in children, but also inadvertently caused many drugs used outside the approved terms of the product license (off-label use). Pharmacists are striving to stay connected to overcome the common and comparable challenges faced in their day to day duties and strive to maximize the safe and effective use of medicines for children.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods; Pharmaceutical Preparations/chemistry; Excipients/chemistry
  19. Fulltext Combinatorial Cytotoxic Effects of Damnacanthal and Doxorubicin against Human Breast Cancer MCF-7 Cells in Vitro
    Aziz MY, Abu N, Yeap SK, Ho WY, Omar AR, Ismail NH, et al.
    Molecules, 2016 Sep 14;21(9).
    PMID: 27649120 DOI: 10.3390/molecules21091228
    Despite progressive research being done on drug therapy to treat breast cancer, the number of patients succumbing to the disease is still a major issue. Combinatorial treatment using different drugs and herbs to treat cancer patients is of major interest in scientists nowadays. Doxorubicin is one of the most used drugs to treat breast cancer patients. The combination of doxorubicin to other drugs such as tamoxifen has been reported. Nevertheless, the combination of doxorubicin with a natural product-derived agent has not been studied yet. Morinda citrifolia has always been sought out for its remarkable remedies. Damnacanthal, an anthraquinone that can be extracted from the roots of Morinda citrifolia is a promising compound that possesses a variety of biological properties. This study aimed to study the therapeutic effects of damnacanthal in combination with doxorubicin in breast cancer cells. Collectively, the combination of both these molecules enhanced the efficacy of induced cell death in MCF-7 as evidenced by the MTT assay, cell cycle, annexin V and expression of apoptosis-related genes and proteins. The effectiveness of doxorubicin as an anti-cancer drug was increased upon addition of damnacanthal. These results could provide a promising approach to treat breast cancer patients.
    Matched MeSH terms: Anthraquinones/chemistry; Antineoplastic Combined Chemotherapy Protocols/chemistry; Doxorubicin/chemistry; Morinda/chemistry
  20. Direct recovery of Bacillus subtilis xylanase from fermentation broth with an alcohol/salt aqueous biphasic system
    Ng HS, Chai CXY, Chow YH, Loh WLC, Yim HS, Tan JS, et al.
    J Biosci Bioeng, 2018 May;125(5):585-589.
    PMID: 29339003 DOI: 10.1016/j.jbiosc.2017.12.010
    Xylanase enzyme degrades linear polysaccharide β-1,4 xylan and the hemicellulose of the plant cell wall. There is a growing demand in finding a cost-effective alternative for industrial scale production of xylanase with high purity for pharmaceutical applications. In this study, an alcohol/salt aqueous biphasic system (ABS) was adopted to recover xylanase from the Bacillus subtilis fermentation broth. The effects of several ABS parameters such as types and concentrations of alcohols and salts (i.e., sulphate, phosphate, and citrate), amount of crude loading and pH of the system on the recovery of xylanase were investigated. Partition coefficient of xylanase (KE), selectivity (S) and yield (YT) of xylanase in top phase of the ABS were measured. Highest KE (6.58 ± 0.05) and selectivity (4.84 ± 0.33) were recorded in an ABS of pH 8 composed of 26% (w/w) 1-propanol, 18% (w/w) ammonium sulphate. High YT of 71.88% ± 0.15 and a purification fold (PFT) of 5.74 ± 0.33 were recorded with this optimum recovery of xylanase using alcohol/salt ABS. The purity of xylanase recovered was then qualitatively verified with sodium dodecyl sulphate (SDS) gel electrophoresis. The SDS profile revealed the purified xylanase was successfully obtained in the top phase of the one-step 1-propanol/sulphate ABS with a distinct single band.
    Matched MeSH terms: Ethanol/chemistry; Culture Media/chemistry*; Sodium Chloride/chemistry; Water/chemistry
Related Terms
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links