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Formulation and Assessment of the Efficacy and Stability of an Ointment Containing Ocimum americanum ***

clinical Complementary Medicine and pharmacology 2023年第1期3卷 62-72页

作者： Nakamwi Akombaetwa Lungwani Tyson Muungo James Nyirenda Sergio Muwowo Aubrey Kalungia Chichonyi Moses Mukosha Chiluba Mwila Department of Pharmacy School of Health SciencesUniversity of ZambiaLusaka 10101Zambia Department of chemistry School of Natural SciencesUniversity of ZambiaLusaka 10101Zambia Histopathology Department University Teaching HospitalLusaka 10101Zambia

Background:Ocimum americanum *** an annual herbaceous plant used to manage pain and *** of standard dosage forms,and safety and efficacy data potentially exposes users of this medicinal plant to the risk of toxic or sub-therapeutic effects,as well as drug-herb ***:The study developed a standard dosage form containing *** extract and assessed its anti-inflammatory efficacy and ***:The fusion method was used to formulate an ointment comprising acetone extract,beeswax,and *** optimization involved the application of Box-Behnken Design(BBD)to design an exper-iment whose input variables were%beeswax and%soft-paraffin and its melting *** variables were drug release and viscosity which were quantified using a vertical diffusion cell(VDC)and stanhope-seta viscometer,*** albino rats were used in carrageenan-induced rat hind paw edema(n=6/test,positive and negative control)to assess the anti-inflammatory *** studies comprised assessment of spreadability,thin layer chromatograms(TLC),and microbial growth in ointment batches stored at 25±2℃/60±5%RH and 40±2℃/75±5%***:Temperature and%beeswax significantly influenced drug release(P=0.0024).Optimal drug release and viscosity were obtained at 5.4%beeswax,89.6%soft-paraffin melted at 58℃.The predominant drug release mechanism was Higuchi(R^(2)=0.967±0.023),which implied longer contact between formulation and skin favours drug *** of edema by the ointment was comparable to 1%(w/w)diclofenac gel(t=2.1;CI=(-8.29)-1.15),and both differed significantly with negative control(t=11.3 and 13.4;CI=14.5-23.9 and 18.1-27.5 respectively).Insignificant changes in spreadability(P=0.112),absence of new spots on chromatograms,and deficiency of microbial colonies on agar plates implied physical,chemical,and microbial stability,***:A formulated ointment containing *** extract ex

关键词： O.americanum Formulation optimization Anti-inflammatory Stability

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Pharmacokinetic,Physicochemical and Medicinal Properties of N-glycoside Anti-cancer Agent More Potent than 2-Deoxy-D-Glucose in Lung Cancer Cells

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Journal of Pharmacy and pharmacology 2019年第4期7卷 165-176页

作者： Fidelis Toloyi Ndombera Geoffrey K.K.Maiyoh Vivian C.Tuei Covance Laboratories Inc.BioPharm CMC solutions Greenfield46140IndianaUSA chemistry Department Wayne State UniversityDetroit48201MichiganUSA Department of Medical Biochemistry School of MedicineMoi University30100EldoretKenya Johannesburg Institute for Advanced Study An initiative of the University of Johannesburg and Nanyang Technological UniversitySingapore1 Tolip StreetWestdene 2092P.O Box 524Auckland Park 2006JohannesburgSouth Africa Department of chemistry and Biochemistry School of ScienceUniversity of Eldoret30100EldoretKenya

Acetylated N-xyloside of 1-naphthylamine(K8A)has been shown to be more potent than 2-deoxy-D-glucose in lung cancer cells and has therapeutic potential for further drug *** this paper we evaluate and report cytotoxicity,pharmacokinetic,physicochemical and medicinal properties of this D-Xylose derivative(K8A)as a lead anticancer agent with greater therapeutic potential than 2-deoxy-D-glucose(2-DG).2-DG has been in clinical trials for treatment of solid tumors and other types of *** demonstrate using virtual tools that K8A has better“drug-likeness”than 2-DG and does not violate any Lipinski,Ghose,Veber,Egan or Muegge *** the other hand,2-DG violates Ghose and Muegge rules.A“BOILEDegg evaluation”,predicts that K8A has higher gastrointestinal absorption(HIA)than 2-DG and is not effluxed by P-glycoprotein(P-gp).Additionally,K8A does not penetrate the blood brain barrier(BBB)and is not a substrate of most Cytochrome P450(CYP)***,K8A did not show false positive alert from PAINS screening enabling us to narrow down and rule out false ***,K8A is more potent than 2-DG in H1299 and A549 lung cancer cells.

关键词： Anticancer agent N-glycoside 2-deoxy-D-glucose pharmacokinetics lung cancer

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Exploring the Mechanism of Blumea balsamifera(L.)DC in Preventing and Treating Alzheimer's Disease Based on HPLC-ESI-HRMS and Network pharmacology

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Medicinal Plant 2023年第5期14卷 10-18页

作者： Dong LI Ling LI Yujie HU JiangXiong MA Wenlong ZHANG Chanyuan ZHOU Dongsheng FAN Xiaojian GONG Key Laboratory for Information System of Mountainous Areas and Protection of Ecological Environment Guizhou Normal UniversityGuiyang 550001China Department of Pharmacy the First Affiliated Hospital of Guizhou University of Traditional Chinese MedicineGuiyang 550001China College of chemistry and Materials Engineering Guiyang UniversityGuiyang 550005China

[Objectives]To expose the plausible mechanism of Blumea balsamifera(L.)*** Alzheimer s disease via network pharmacology and HPLC-ESI-HRMS technology.[Methods]To begin with,HPLC-ESI-HRMS was employed to identify the components of ***,the potential targets of the components were identified and predicted based on chemical similarity and online ***,by way of topological analysis of a component-disease target interaction network,the primary candidate targets and potential active components were ***,molecular docking analysis was used to confirm the interaction between active components and therapeutic targets.[Results]According to the final results,HPLC-ESI-HRMS identified 70 *** of these,20 components were potentially biologically active,and most of them were *** to the molecular docking results,the primary active components were appropriately coordinated with the core targets,indicating a high level of pharmacodynamic ***,the sesquiterpenes present in *** are considered potential active ingredients having multi-target and multi-pathway effects for treating Alzheimer s disease.[Conclusions]This research will provide a scientific reference for the future pharmacological activity and clinical application of ***.

关键词： HPLC-ESI-HRMS Alzheimer's disease Blumea balsamifera(L.)DC. Network pharmacology Molecular docking

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QSAR Applied to 4-Chloro-3-formylcoumarin Derivatives Targeting Human Thymidine Phosphorylase

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clinical Complementary Medicine and pharmacology 2022年第2期2卷 19-29页

作者： Thomas Scior Juan Carlos Garcia-Hernandez Hassan H.Abdallah Christian Alexander Departamento de Farmacia Facultad de Ciencias QuímicasBenemérita Universidad Autónoma de PueblaPuebla 72000Pue.Mexico chemistry Department College of EducationSalahaddin University ErbilErbil 44001Iraq Division of Cellular Microbiology Research Center Borstel-Leibniz Lung CenterBorstel 23845Germany

Background:Coumarins are secondary metabolites from the phenylpropanoid-type biosynthesis in higher plants.A plethora of potential phytopharmacological activities have been described for derivatives of the coumarin scaffold:hepatoprotective,antineoplastic,antimicrobial,antituberculosis,antiviral,anti-inflammatory anticoagulant,or antithrombotic ***:A computer-based quantitative structure–activity relationships(QSAR)study for a series of 4‑chloro-3-formylcoumarins was carried ***:To this end we generated the 3D models of 17 published coumarin structures,calculated their physicochemical properties(descriptors)to correlate them to their experimentally known biological activities measured as inhibition concentrations to block the target enzyme *** proposed approach used free molecular modeling software and applies our scripts written in the programming language ***:The final multiple regression models achieved satisfactory results with a small number of descriptors–all of which were statistically significant and meaningful in the field of pharmacodynamics to develop new 3-formylcoumarins with enhanced activities targeting the human thymidine phosphorylase ***:On theoretical grounds,our in silico research contributes in a crucial step in the field of complementary *** step is located between in vivo pharmacological observations of plant extracts on ethnopharmacological,preclinical or controlled clinical levels and the need to identify–at an atomic scale–all those plant ingredients responsible for the biological actions under *** simulations shed light on the modification of phyto-medicine’s physicochemical properties to enhance the interaction with their biomolecular target in the patient’s body.

关键词： Coumarin Phytopharmacy R script Linear model Multiple linear regression QSAR

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Brahmi研究与开发:一种能改善记忆的药用植物(英文)

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中国药理学与毒理学杂志 2015年第S1期29卷 13-13页

作者： KornkanokINGKANINAN NanteetipLIMPEANCHOB SakchaiWITTAYA-AREEKUL KrongkarnCHOOTIP PornnarinTAEPAWARAPRUK NuwatTAEPAWARAPRUK JintanapornWATTANATHORN SeewaboonSIREERATAWONG WarapornPUTALUN WatooPHROMPITTAYARAT HiroyukiTANAKA Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in chemistry Naresuan University Phitsanulok 65000 Thailand Faculty of Medical Sciences Naresuan University Phitsanulok 65000 Thailand Faculty of Medicine Khon Kaen University Khon Kaen 40002 Thailand Faculty of Medicine Chiang Mai University Chiang Mai 50200 Thailand Faculty of Pharmaceutical Sciences Khon Kaen University Khon Kaen 40002 Thailand Faculty of Public Health Naresuan University Phitsanulok 65000 Thailand Graduate School of Pharmaceutical Sciences Kyushu University Fukuoka 812-8582 Japan

OBJECTIVE Brahmi(Bacopa monnieri Wettst.,Schrophulariaceae)has been used in Ayuravedic medicine as a memory *** aimed at research and development of Brahmi for clinical use as the food supplement for memory *** The standardized extract of Brahmi has been *** neuroprotective effect of the extract was tested using in vitro and in vivo assay.A double-blinded randomized control trial of brahmi tablet was conducted in 60 middle-aged elderly *** The in vivo studies indicated that the standardized extract had neuroprotective effect at the doses of 40 and 80mg·*** escape latency time of rats in Morris water maze test was ***,the reduction of neurons and cholinergic neuron densities were *** also tested its protection effect against the beta-amyloid protein and glutamate-induced neurotoxicity in primary cortical cultured *** result demonstrated that Brahmi extract protected neurons from beta-amyloid-induced cell death,but not glutamate-induced *** standardized extract of Brahmi is formulated as a film-coated *** effect of Brahmi extract on learning and memory was studied in the middle aged and elderly *** results showed that Brahmi extract(300and 600mg·d-1)could improve quality of life in the elderly by improving the physical fitness via the increase in efficiency of postural *** also improved the psychological fitness by increasing alertness and attention resulted in the improvement of learning and *** addition,Brahmi extract could decrease depression-like *** dosage used in this study did not produce toxic and side *** The in vitro and in vivo studies suggested that brahmi is a potential medicinal plant for memory *** clinical study showed that brahmi tablet could improve physical fitness and enhance memory in healthy volunteers.

关键词： Bacopa monnieri clinical study memory neuroprotect

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Immunostimulatory and Immunorestorative Effects of Leaf Extract and Fractions of Musanga cecropioides on Immunocompetent and Experimentally Immunocompromised Mice

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clinical Complementary Medicine and pharmacology 2023年第1期3卷 53-61页

作者： Cyril O.Ogbue Felix A.Onyegbule Christopher O.Ezugwu Ifebi H.M.Nchekwube Amara A.Ajaghaku Department of Pharmacognosy and Traditional Medicine Faculty of Pharmaceutical SciencesNnamdi Azikiwe UniversityAgulu 422102Anambra StateNigeria Department of Pharmaceutical and Medicinal chemistry Faculty of Pharmaceutical SciencesNnamdi Azikiwe UniversityAgulu 422102Anambra StateNigeria Department of Pharmacognosy and Environmental Medicine University of NigeriaNsukka400221Enugu StateNigeria Department of Pharmacognosy and Traditional Medicine Faculty of Pharmaceutical SciencesChukwuemeka Odumegwu Ojukwu UniversityIgbariam432106Anambra StateNigeria

Background:Stimulation of the immune system against disease and restoration of immune functions in immun-odeficiency disease state are essential for maintaining good ***:This study investigated the immunomodulatory effects of the leaf extract and fractions of Musanga cecropioides in immunocompetent and immunocompromised animal ***:Humoral immune stimulatory effect of the extract and its fractions at 200 mg·kg^(−1) and 400 mg·kg^(−1) against sheep red blood cells(SRBCs)antigen was determined in both immunocompetent and cyclophosphamide(80 mg·kg^(−1))induced immunosuppressed *** effect of the most active fraction on leucopoiesis was also determined following high dose cyclophosphamide(300 mg·kg^(−1))suppression of the immune *** at 2.5 mg·kg^(−1) was used as the reference drug throughout the ***:The extract dose dependently stimulated the humoral immune response to SRBC antigen in immuno-competent animals;however,its stimulatory effect was not significant(P>0.05).In the immunosuppressed model,the extract at 400 mg·kg^(−1) evoked significant(P<0.05)increase in antibody titer value with a corre-sponding 67%immune-restorative *** ethyl acetate fraction(EAF)maintained the most active fraction with significant(P<0.05)antibody stimulatory effect in immunocompetent and immunosuppressed ***,higher recovery rate was demonstrated by the EAF as shown by steep time recovery curve in high dose immunosuppressed *** EAF at 200 mg·kg^(−1) and 400 mg·kg^(−1) showed above 50%leucopoiesis just like the reference drug(2.5 mg·kg^(−1) levamisole),against 33.83%of leucopoiesis shown by the immune-suppressed control ***:*** boosted immune stimulation in immunocompetent animals and brought about fast rate of restoration of immune status in immunocompromised animals.

关键词： Musanga cecropioides Immunostimulation Immunorestoration Leucopoiesis Antibody

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Chemical Composition of Gossypium herbaceum linn and its Antioxidant, Antibacterial, Cytotoxic and Antimalarial Activities

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clinical Complementary Medicine and pharmacology 2021年第1期1卷 68-76页

作者： Rotimi Abisoye Larayetan Gideon Ayeni Abdulrazaq Yahaya Abayomi Ajayi Sunday Omale Umar Ishaq Dauda Joseph Abiodun Chijioke Olisah Julius Aigbogun Swesme Enyioma-Alozie Department of chemistry Kogi State UniversityPMB 1008AnyigbaKogi StateNigeria Department of Pure and Applied chemistry University of Fort Hare Alice 5700South Africa Department of Biochemistry Kogi State UniversityPMB 1008AnyigbaKogi StateNigeria Department of Biochemistry School of Life SciencesUniversity of KwaZulu-NatalWestville CampusDurban 4000South Africa Department of Anatomy Faculty of Basic Medical SciencesCollege of Health SciencesKogi State University AnyigbaPMB 1008AnyigbaKogi StateNigeria Botany Department Institute for Costal and Marine ResearchNelson Mandela UniversityPort Elizabeth 6031South Africa Jacio Environmental Limited 3 Airoboyi EstatesKM 2RefineryRefinery RoadEffurunDelta StateNigeria Department of Anatomy Faculty of Basic Medical SciencesBaze UniversityPlot 686Cadastral Zone C 00Jabi Airport Road Bypass(Ring Road)Behind National Judicial InstituteAbujaNigeria

Background:Gossypium herbaceum(***),a plant commonly found in the wild in Nigeria,is said to possess some therapeutic ***,there is a dearth of information on its chemical ***,there is a need to investigate its therapeutic ***:To investigate the qualitative and quantitative phytochemical components of the leaf extracts of ***,as well as its antioxidant,antimalarial and cytotoxic ***:Gas chromatography-mass spectrometry(GC-MS)analysis was used to determine the components of ethanol and hexane extracts of *** leaf while 2,2-diphenyl-1-picrylhydrazyl(DPPH)and nitric oxide assays were used to determine the antioxidant *** parasites viability was examined using parasite lactate dehydrogenase(pLDH)technique and HeLa cell was used for the cytotoxicity ***:Bioactive compounds identified in ethanol and hexane extracts of *** were 37 and 30 kinds,respectively,with major components as linoleic acid(36.10%and 33.82%),vitamin E(7.15%and 5.98%)and caryophyllene(4.21%and 5.08%).It also has tannins,saponins,alkaloids,flavonoids steroids,phenols and *** antibacterial test,significant inhibitory potentials against multidrug-resistant bacteria strains were *** vitro antioxidant potentials(IC 50)of ethanol and hexane extracts were 3.33 and 4.12μg/mL for DPPH assays,and 3.87 and 5.00μg/mL for nitric oxide assays,*** activities(IC 50)were 9.99 and 9.76μg/mL for ethanol and hexane extracts,***:*** leaf may provide novel plant-derived therapeutic agents,effective in treating infectious diseases arising from multiple drug-resistant bacteria and a target in the management of oxidative stress.

关键词： Antimalarial Antimicrobial Antioxidant Bioactive components MBC MBF GC-MS Gossypium herbaceum

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Effects of Citrullus colocynthis Seed Aqueous Extracts upon Sodium Transport across A6 Kidney Cell Monolayers

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clinical Complementary Medicine and pharmacology 2023年第1期3卷 47-52页

作者： N.Benariba K.Louchami R.Djaziri A.Sener Willy J.Malaisse Laboratory of Antibiotic and Antifungal Physico-chemistry Synthesis and Biological ActivityDepartment of BiologyFaculty SNV-STUUniversity Abou Bekr BelkaïdTlemcen BP119-13000Algeria Laboratoire d’Histologie générale Neuroanatomie et Neuropathologie(LHNN)UniversitéLibre de BruxellesBrussels CP620-1070Belgium Department of Biochemistry UniversitéLibre de BruxellesBrussels CP611-1070Belgium Laboratory of Experimental Hormonology UniversitéLibre de BruxellesCP611-1070Belgium

Background:Various extracts from Citrullus colocynthis seeds were recently examined for their possible favorable effects on glucose homeostasis,other metabolic variables,and pancreatic islet size in streptozotocin-induced diabetic ***:Considering the effectiveness of insulin upon target cells as another process susceptible to be influenced by plant extracts,the present study is used to compare the effects of either crude or defatted aqueous extracts from *** seeds upon Na+transport in A6 kidney ***:The intensity of electrical currents,taken as the potential difference divided by the epithelial resistance was measured in monolayers of A6 kidney cells exposed at the basolateral side to either crude untreated aqueous(EI)or defatted aqueous(EII)extracts,as well as their fractions EI1 and EII1 containing components with high molecular weight(>5 kDa),and EI2 and EII2 containing components with low molecular weight(<5 kDa).The effect of insulin was to assess the functional integrity of the A6 ***:All extracts caused a rapid and sustained increase in current *** defatted aqueous extract(EII)was more efficient than the non-defatted aqueous extract(EI)in terms of increasing the intensity of current in the A6 *** components of the defatted aqueous extract responsible for such a greater efficiency were located in the fraction containing components with low molecular weight and acted in a time-related progressive fashion upon Na+***:These data suggest that colocynth seed extracts mainly containing components with low molecular weight increased the current intensity in A6 cells,thus suggesting that colocynth may affect Na+transport in kidney cells.

关键词： Citrullus colocynthis seed extracts Sodium transport A6 kidney cell monolayer

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The Anti-parasitic Effect of Extract of Ceiba pentandra (L.) Gaertn Is Related to Its Anti-inflammatory, Analgesic and Anthelmintic Activities on Haemonchus contortus

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clinical Complementary Medicine and pharmacology 2023年第2期3卷 65-73页

作者： Bogning Zangueu Calvin Alowanou Goue Géorcelin Belle Ebanda Kedi Phillipe Olounlade Abiodoun Pascal Magne Fongang Annie Laure Kojom Wanche Jacquy Joyce Nguemfo Edwige Laure Azebaze Anatole Guy Blaise Dongmo Alain Bertrand Hounzangbe-Adote Mawulé Sylvie Laboratory of Animal Biology Faculty of ScienceUniversity of DoualaDouala 24157Cameroon Laboratory of Ethnopharmacology and Animal Health Faculty of Agronomics SciencesUniversity of Abomey Calavi01 P.O.Box 526CotonouBenin Pluridisciplinairy Laboratory School of Management and Exploitation of livestock SystemsUniversity National of Agricultural of Porto-Novo01 P.O.Box 55Porto-NovoBenin Department of Biological Sciences Faculty of Medicine and Pharmaceuticals SciencesUniversity of DoualaDouala 2701Cameroon Laboratory of chemistry Faculty of ScienceUniversity of DoualaDouala 24157Cameroon

Background:Ceiba pentandra is a medicinal plant used as alternative therapy to control parasitic nematodes in ***:This study aims to investigate anti-parasitic effect of aqueous stem back extract of Ceiba pentandra(L.)Gaertn through the evaluation of its anthelmintic,anti-inflammatory and analgesic ***:In vitro,the efficacy of aqueous extract(75 to 2400μg·mL−1)diluted in phosphate buffered saline(PBS)was tested against three stages of the life cycle of Haemonchus contortus through larval migration inhibition assay(LMIA),egg hatch assay(EHA),and adult worms motility inhibition assay(AMIA).In vivo,anti-inflammatory and antinociceptive properties of the aqueous extract(150 and 300 mg·kg−1)was evaluated on rodent using phlogistic and algic ***:Significant inhibition activity(P<0.05)was obtained on EHA with the greatest inhibition of 46.63%obtained at 2400μg·mL−*** plant treatment dramatically(P<0.05)inhibited L3 larval migration as compared to *** highest inhibition rate was 53.33%at 1200μg·mL−*** of polyvinylpolyrrolidone(PVPP)to the extract significantly(P<0.01)reduced at 38.6%the activity of the plant extract on larval migration compared to extract without *** Ceiba pentandra extract reduced(P<0.05)worm motility after 24 h post exposure as compared to *** vitro,aqueous extract significantly(P<0.05)inhibited the paw inflammation induced by carragenine,with a significant(P<0.05)reduction of the number of abdominal contortions induced by acetic acid to 41.11%at 300 mg·kg−1 and the paw licking time induced by formaline in both phases to 57.22%and 63.59%at 300 mg·kg−1 likened to ***:In vitro results suggest that,this plant possess anti-parasitic *** and anti-inflammatory effects of *** can contribute to its anti-parasitic property.

关键词： Anti-inflammatory Antinociceptive Anthelmintic Ceiba pentandra Haemonchus contortus

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