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Role of copper chelating agents: between old applications and new perspectives in neuroscience

Neural Regeneration Research 2025年第3期20卷 751-762页

作者： Rosalba Leuci Leonardo Brunetti Vincenzo Tufarelli Marco Cerini Marco Paparella Nikola Puvača Luca Piemontese department of Pharmacy-pharmaceutical Science University of Bari Aldo MoroBariItaly department of Precision and Regenerative Medicine and Jonian Area(DiMePRe-J) Section of Veterinary Science and Animal ProductionUniversity of Bari Aldo MoroBariItaly department of Engineering Management in Biotechnology Faculty of Economics and Engineering Management in Novi SadUniversity Business Academy in Novi SadNovi SadSerbia

The role of copper element has been an increasingly relevant topic in recent years in the fields of human and animal health, for both the study of new drugs and innovative food and feed supplements. This metal plays an important role in the central nervous system, where it is associated with glutamatergic signaling, and it is widely involved in inflammatory processes. Thus, diseases involving copper(Ⅱ) dyshomeostasis often have neurological symptoms, as exemplified by Alzheimer's and other diseases(such as Parkinson's and Wilson's diseases). Moreover, imbalanced copper ion concentrations have also been associated with diabetes and certain types of cancer, including glioma. In this paper, we propose a comprehensive overview of recent results that show the importance of these metal ions in several pathologies, mainly Alzheimer's disease, through the lens of the development and use of copper chelators as research compounds and potential therapeutics if included in multi-target hybrid drugs. Seeing how copper homeostasis is important for the well-being of animals as well as humans, we shortly describe the state of the art regarding the effects of copper and its chelators in agriculture, livestock rearing, and aquaculture, as ingredients for the formulation of feed supplements as well as to prevent the effects of pollution on animal productions.

关键词： agriculture Alzheimer's disease chelators copper feed supplements multi-target

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Recognition and quality mapping of traditional herbal drugs:way forward towards artificial intelligence

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Traditional Medicine Research 2025年第1期10卷 12-26页

作者： Sanyam Sharma Subh Naman Ashish Baldi Faculty of Pharmacy Pacific Academy of Higher Education and Research UniversityUdaipur 313024India Pharma Innovation Lab Department of Pharmaceutical Sciences and TechnologyMaharaja Ranjit Singh Punjab Technical UniversityBathinda 151001India Faculty of pharmaceutical Sciences The ICFAI UniversityBaddi 174103India.

The use of traditional herbal drugs derived from natural sources is on the rise due to their minimal side effects and numerous health ***,a major limitation is the lack of standardized knowledge for identifying and mapping the quality of these herbal *** article aims to provide practical insights into the application of artificial intelligence for quality-based commercialization of raw herbal *** focuses on feature extraction methods,image processing techniques,and the preparation of herbal images for compatibility with machine learning *** article discusses commonly used image processing tools such as normalization,slicing,cropping,and augmentation to prepare images for artificial intelligence-based *** also provides an overview of global herbal image databases and the models employed for herbal plant/drug *** will gain a comprehensive understanding of the potential application of various machine learning models,including artificial neural networks and convolutional neural *** article delves into suitable validation parameters like true positive rates,accuracy,precision,and more for the development of artificial intelligence-based identification and authentication techniques for herbal *** article offers valuable insights and a conclusive platform for the further exploration of artificial intelligence in the field of herbal drugs,paving the way for smarter identification and authentication methods.

关键词： artificial intelligence Ayurveda machine learning models herbal drugs image pre-processing medicinal plants

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Melissa officinalis and rosmarinic acid in management of memory functions and Alzheimer disease

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Asian Pacific Journal of Tropical Biomedicine 2019年第2期9卷 47-52页

作者： Mohaddese Mahboubi Medicinal Plants Research department Research and DevelopmentTabibDaru Pharmaceutical Company

Alzheimer disease(AD) as worldwide progressive neurodegenerative disease is prevalent disease among elderly population. Due to limitation in chemical drugs along with their adverse effects of these treatments, research for finding more effective natural drugs, is one of interesting subjects among the scientists. Melissa officinalis(M. officinalis) has a long history of use in treatment of nervous system diseases. This review article evaluates the potency of M. officinalis in treatment of AD by review of experimental and clinical documents on the efficacy, safety and its mechanisms of action in management of AD. The information is extracted from electronic resources(PubMed, Wiley, Springer and Science Direct), English and Persian scientific books. In spite of different scientific and non-scientific reports on the use of M. officinalis and its main component of rosmarinic acid in neurodegenerative diseases, there is only one clinical trial on the efficacy of M. officinalis ethanol extract in management of AD. Different mechanisms of action for M. officinalis, including inhibitory effects against amyloid beta, reactive oxygen species, and acetylcholine esterase, are involved. Larger clinical trials are recommended to confirm the efficacy and safety of M. officinalis extracts in treatment of AD patients.

关键词： Lemon balm Melissa officinalis Alzheimer Acetylcholine Rosmarinic acid

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Hepatoprotection by dandelion (Taraxacum officinale) and mechanisms

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Asian Pacific Journal of Tropical Biomedicine 2020年第1期10卷 1-10页

作者： Mohaddese Mahboubi Mona Mahboubi Medicinal Plants Research department Research and DevelopmentTabibDaru Pharmaceutical CompanyKashanIran

The protection of the liver as an essential organ in the body against oxidative stress and deleterious compounds has been the subject of recent *** different compounds,medicinal plants play an important role due to their hepatoprotective *** officinale or"common dandelion"is a popular plant that has been traditionally used for its hepatoprotective ***,there are limited clinical studies on its hepatoprotective *** aim of this review article is to evaluate the hepatoprotective effects of dandelion and its mechanism of *** reviewed literature up to July 2019 on"Taraxacum officinale"or"dandelion"and *** available pharmacological studies indicate that dandelion extracts have hepatoprotective effects against chemical agents due to its antioxidant and antiinflammatory *** anti-inflammatory effects of dandelion,the prebiotic effects of its oligofructans,inhibitory effects against the release of lipopolysaccharides and fasting induced adipose factor,digestive enzymes,and enhancing effects of lipogenesis,reduce lipid accumulation and liver inflammation,which directly or indirectly improve the liver *** emerging evidence on hepatoprotective effects of dandelion,designing large human clinical studies is essential.

关键词： Dandelion Hepatoprotective effects Antioxidant Anti-inflammatory

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Identification of sitosteryl glucoside palmitate in a chloroform-derived fraction of Phyllanthus niruri with antiplasmodial and peripheral antinociceptive properties

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Asian Pacific Journal of Tropical Biomedicine 2014年第9期4卷 707-713页

作者： Ezenyi Ifeoma Chinwude Kulkarni Roshan Joshi Swati Salawu Oluwakanyinsola Adeola Emeje Martins department of Pharmacology and Toxicology National Institute for Pharmaceutical Research and Development Organic Chemistry Division National Chemical Laboratory Centre for Nanomedkine and Biophysical Drug Delivery Department of Pharmaceutical Technology and Raw Material DevelopmentNational Institute for Pharmaceutical Research and Development

Objective:To evaluate the antiplasmodial properties of fractions of chloroform portion of Phyllanthus niruri(***) methanol extract and identify a suitable chemical marker present ***:Chloroform portion of *** methanol extract was separated from silica gel using gradient systems of hexane,ethylacetate and *** fractions were screened for antiplasmodial activity against Plasmodium falciparum HB3 and *** with IC_(50)<10μg/*** parasites were further screened for peripheral analgesic activity,while cytotoxicity was evaluated using THP-1 ***:Fractions 12-14 were very active(IC_(50)<10 μg/mL) against Plasmodium falciparum and showed no significant *** 12 and 13 exhibited significant(P<0.01) reduction in acetic acid-induced writhing in mice,decreasing the number of writhes by 66.67% and 65.22% respectively and comparable with 100 mg/kg aspirin(65.22%).From fraction 12,a compound was isolated and identified as sitosteryl-6-β-D-glucoside-6'-palmitate by ~1H,^(13)C nuclear magnetic resonance and mass ***:Our findings illustrate antiplasmodial column fractions of *** with analgesic activity and identify sitosteryl glucoside pahmitate as a chemical marker of activity.

关键词： Malaria Medicinal plant Plasmodium falciparum

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The compounds fromDerris laxiflora Benth suppresses lipopolysaccharideinduced inflammatory response in murine Raw264.7 cells

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中国药理学与毒理学杂志 2015年第S1期29卷 64-65页

作者： Ai-jen YANG Hsi-lin CHIU Ming-yu CHAO Jui-ching CHEN department of Biotanicals Medical and Pharmaceutical Industry Technology and Development Center

OBJECTIVE The emerging role of chronic inflammation is the major degenerative diseases of modern society such as periodontitis,atherosclerosis,rheumatoid arthritis,Parkinson′s disease and even *** components were isolated from Derris laxiflora Benth.,In this study,we found these compounds from Derris laxiflora Benth suppress lipopolysaccharide-induced inflammatory response in murine macrophage(RAW 264.7)*** RAW 264.7cells were cultured in DMEM media supplemented with 10%(V/V)heated-inactivated FBS,penicillin 100U·mL-1 and streptomycin 100μg·*** cells were incubated at 37℃in a humidified atmosphere of 5%CO2in ***264.7cells were seeded in a 24-well plate at a density of 2×105 mL-1 and then incubated with or without LPS(100ng·mL-1)in the absence or presence of compounds for 24 *** of these isolates on NO production were measured indirectly by analysis of nitrite levels using the Griess *** was used as a positive *** ight components were isolated from Derris laxiflora Benth.,including three new pterocarpans 7,6′-dihydroxy-3′-methoxypterocarpan(1),derrispisatin(2),derriscoumaronochromone(3)and three new flavonoids cis-3,4′-dihydroxy-5,7-dimethoxyflavan(4),derriflavanone B(5),iso-lupinenol(6)as well as two known ones,lonchocarpol A(7)and lonchocarpol D(8).The structures of these new compounds were determined by analysis of their spectroscopic ***264.7 cells were treated with the compounds from Derris laxiflora Benth for 24 *** them,compounds 5,7 and 8 significantly suppressed the NO production in LPS-treated RAW264.7 cells with IC50 values<10μg·*** In this study,we found that compounds from Derris laxiflora Benth suppresses lipopolysaccharide-induced inflammatory response in murine Raw264.7 cells.

关键词： lipopolysaccharide RAW264.7cells Derris laxiflora

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Repositioning of dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 agonists as potential neuroprotective agents

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Neural Regeneration Research 2019年第5期14卷 745-748页

作者： Shaker A.Mousa Bassam M.Ayoub pharmaceutical Research Institute Albany College of Pharmacy and Health Sciences The Center for Drug Research and development (CDRD) Pharmaceutical Chemistry Department Faculty of Pharmacy The British University in Egypt

Repositioning of dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists is a breakthrough in the field of neural regeneration research increasing glucagon like peptide-1 bioavailability, hence its neuroprotective activities. In this article, the authors suggest not only crossing blood-brain barrier and neurodegenerative disease as off target for dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists, but also for ophthalmic preparations for diabetic retinopathy, which may be the latest breakthrough in the field if prepared and used in an appropriate nano-formulation to target the retinal nerves. The relation of neurodegenerative diseases' different mechanisms to the dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists should be further examined in preclinical and clinical settings. The repositioning of already marketed antidiabetic drugs for neurodegenerative diseases should save the high cost of the time-consuming normal drug development process. Drug repositioning is a hot topic as an alternative to molecular target based drug discovery or therapeutic switching. It is a relatively inexpensive pathway due to availability of previous pharmacological and safety data. The glucagon like peptide-1 produced in brain has been linked to enhanced learning and memory functions as a physiologic regulator in central nervous system by restoring insulin signaling. Intranasal administration of all marketed gliptins(or glucagon like peptide-1 receptor agonists) may show enhanced blood-brain barrier crossing and increased glucagon like peptide-1 levels in the brain after direct crossing of the drug for the olfactory region, targeting the cerebrospinal fluid. Further blood-brain barrier crossing tests may extend dipeptidyl peptidase-4 inhibitors' effects beyond the anti-hyperglycemic control to intranasal spray, intranasal powder, or drops targeting the blood-brain barrier and neurodegenerative diseases wit

关键词： repositioning DPP-4 inhibitors GLP-1RA neural regeneration blood-brain barrier Parkinson’s disease Alzheimer’s disease diabetic retinopathy

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Influence of solvent mixtures on HPMCAS-celecoxib microparticles prepared by electrospraying

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Asian Journal of pharmaceutical Sciences 2018年第6期13卷 584-591页

作者： Adam Bohr Yingya Wang Moritz Beck-Broichsitter Mingshi Yang department of Pharmacy Faculty of Health and Medical SciencesUniversity of Copenhagen department of Pharmaceutics and Biopharmacy Philipps-Universitat Chemical and pharmaceutical development Bayer AG Wuya College of Innovation Shenyang Pharmaceutical University

Hypromellose acetate succinate(HPMCAS) microparticles containing the poorly-water soluble drug celecoxib(CEL) were prepared by electrospraying intended for oral drug delivery. Various solvent mixtures with different solubility for CEL and HPMCAS were used to induce changes in the polymer structural conformation of the microparticles. The performance of the prepared microparticles was evaluated by studying the solid state from, particle size and morphology, radial drug distribution and drug release. CEL was amorphous in all electrosprayed HPMCAS microparticles. The particle size and morphology was dependent on the solubility of HPMCAS in the solvent mixture used with poorer solvents resulting in smaller microparticles with rougher appearance. The CEL distribution on the particles surface was relatively homogeneous and similar for all microparticles. Drug release from the microparticles was observed at a higher rate depending on the solubility of HPMCAS in the solvent used for electrospraying, and in all cases an at least 4-fold higher rate was observed compared with the crystalline drug. Drug precipitation from the supersaturated solution was inhibited by HPMCAS for all microparticles based on its parachute effect while crystalline CEL did not reach supersaturation. This study demonstrated that electrospraying can be used to produce microparticles with tailored properties for pharmaceutical application by adjusting solvent selection.

关键词： Celecoxib Electrospraying Hypromellose acetate succinate Oral drug delivery Polymeric microparticles Solvent mixture

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Pharmacokinetics of propafenone hydrochloride sustained-release capsules in male beagle dogs

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Acta Pharmaceutica Sinica B 2015年第1期5卷 74-78页

作者： Liping Pan Yafang Qian Minlu Cheng Pan Gu Yanna He Xiaowen Xu Li Ding department of pharmaceutical Analysis China Pharmaceutical University

Ins paper describes the development and validation of a liquid chromatography mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hydrochloride sustained-release capsule (SR-test), as an instant-release tablet (IR-reference) and as the market leader sustained-release capsule (Rythmod SR-reference) in male beagle dogs (n= 8). In Study A comparing SR-test with IR-reference in a crossover design T-max and t(1/2) of propafenone for SR-test were significantly higher than those for IR-reference while C-max and AUC were lower demonstrating the sustained release properties of the new formulation. In Study B comparing SR-test with SR-reference the observed C and A TIC of propafenone for SR test (124.5 +/- 140.0 ng/mL and 612.0 +/- 699.2 ng.h/mL, respectively) were higher than for SR-reference (78.52 +/- 72.92 ng/mL and 423.6 +/- 431.6 ng.h/mL, respectively) although the differences were not significant. Overall, the new formulation has as good if not better sustained release characteristics to the market leader formulation. (C) 2015 Chinese pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier By All rights reserved.

关键词： Propaferione PHarmacokinetics Sustained-release Beagle dog Plasma

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New therapeutic option for irritable bowel syndrome:Serum-derived bovine immunoglobulin

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World Journal of Gastroenterology 2015年第11期21卷 3361-3366页

作者： Larry Good Roxanne Rosario Raymond Panas department of Gastroenterology South Nassau Communities Hospital department of Research Good Pharmaceutical Development Company department of Medical Affairs Entera HealthInc.

Oral prescription medical foods have long been used in hospital settings but are also appropriate therapies for gastrointestinal disorders in outpatient medical *** serum-derived bovine immunoglobulin/protein isolate(SBI) has been shown in clinical studies to reduce loose stools and improve stool consistency as well as other symptoms(i.e.,abdominal pain,bloating,and urgency) in patients with irritable bowel syndrome with diarrhea(IBS-D) and human immunodeficiency virus-associated *** case series reports the outcomes of 14 IBS patients who received SBI as an addition to standard of care at an individual physician's clinical *** patients:2 IBS with constipation(IBS-C),7 IBS-D,2 mixed diarrhea and constipation IBS(IBS-M) and 3 undefined IBS(IBS-U; also described by some physicians as IBS-Bloating),ranged in age from 22-87 ***(5 g or 10 g daily dose) was added to the patient's current standard care and followed for several weeks to determine if symptoms were improved with the addition of ***,12 of the 14 patients indicated some level of improvement through direct questioning of the patients regarding changes from the prior *** IBS-Bloating patient had a resolution of symptoms and two patients(1 IBS-Bloating and 1 IBS-C) discontinued therapy because of insufficient *** 12 patients who continued on therapy reported an overall improvement in symptoms with better stool consistency,decreased frequency as well as reductions in abdominal pain,bloating,distention,and *** most cases,therapeutic effects of SBI were seen within the first four weeks of therapy with continued improvements at subsequent *** has a multifaceted mechanism of action and may help to manage IBS by providing a distinct protein source required to normalize bowel function,gastrointestinal microbiota,and nutritionally enhance tight junction protein expression between intestinal epithelial *** as a medical food provides a safe o

关键词： Irritable bowel syndrome Diarrhea Immu-noglobulin

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