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Isoimperatorin alleviates acetic acid-induced colitis in rats

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Asian Pacific Journal of Tropical Biomedicine 2024年第4期14卷 147-153页

作者： Saied Goodarzi Amir Hossein Abdolghaffari Behnaz Najafi Mostafa Pirali Hamedani Saeed Tavakoli Mahshad Marvi Maryam Baeeri Narguess Yassa Abbas Hadjiakhoondi Mohammad Abdollahi Zahra Tofighi medicinal plants research Center Faculty of PharmacyTehran University of Medical SciencesTehranIran department of Toxicology and Pharmacology Faculty of PharmacyTehran Medical SciencesIslamic Azad UniversityTehranIran department of Pharmacognosy Faculty of PharmacyTehran University of Medical SciencesTehranIran medicinal plants research Center Institute of Medicinal PlantsACECRKarajIran International Campus School of Pharmacy Tehran University of Medical SciencesTehranIran Toxicology and Diseases group The Pharmaceutical Sciences Research CenterTehran University of Medical SciencesTehranIran department of Toxicology and Pharmacology Faculty of PharmacyTehran University of Medical SciencesTehranIran

Objective:To investigate the effect of isoimperatorin on histopathological and biochemical changes in acetic acid-induced colitis ***:Colitis was induced by intracolonic administration of acetic acid solution(4%v/v)in *** were divided into six groups including the sham group,the negative control group,the dexamethasone-treated group,and the groups treated with isoimperatorin(0.1,1,and 10 mg/kg/d by gavage).The treatments were administered for three days and then colonic status was assessed by macroscopic,histopathological,and biochemical ***:Isoimperatorin significantly alleviated colonic damage in a dose-dependent manner and improved histological changes in rats with acetic acid-induced *** also significantly reduced myeloperoxidase,TNF-α,IL-1β,and malodialdehyde ***:Isoimperatorin alleviates acetic acid-induced colitis in rats and may be a potential therapeutic agent for the treatment of colitis.

关键词： Isoimperatorin Inflammatory bowel disease Acetic acid Colitis TNF-α IL-1β

Inhibiting the oligomerization of mycobacterial DNA-directed RNA polymerase(RNAP)using natural compound via in-silico techniques

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Medicine in Novel Technology and Devices 2024年第1期21卷 97-109页

作者： Ehssan H.Moglad department of Pharmaceutics College of PharmacyPrince Sattam Bin Abdulaziz UniversityP.O.Box 173 Alkharj 11942Saudi Arabia department of Microbiology and Parasitology Institute of Medicinal and Aromatic Plants ResearchThe National Center for ResearchP.O.Box 2404KhartoumSudan

Mycobacterium tuberculosis(Mtb)is responsible for the spread of tuberculosis(TB).The current study employed virtual screening of 2569 natural compounds against the DNA-directed RNA polymerase(RNAP)of Mtb to identify the possible binders that can inhibit its *** in-silico methodology included molecular docking to the compounds,further,the stability and flexibility of the best complexes were studied using molecular dynamics simulation,the MM/GBSA binding free energy technique with energy decomposition,PCA,FEL,steered MD simulation,and umbrella *** virtual screenings were conducted for the five RNAP subunits(chains A,B,C,D,and E)to identify a compound capable of inhibiting RNAP oligomerization.A promising compound,isoestradiol 3-benzoate,exhibited a low binding score(−7.28kcal/mol to−8.21kcal/mol)and showed binding ability with all subunits of the ***,the five complexes with isoestradiol 3-benzoate were selected for molecular dynamics simulation ***,RMSD showed that isoestradiol 3-benzoate bound with chain E showed the lowest RMSD of 0.49nm,while with chains A and B it had the most stable and consistent conformations with RMSD of 1.75nm and 1.2nm,*** H-bond between isoestradiol 3-benzoate and chains C and E showed the highest occupancy(58.27%,45.33%,and 50.80%,42.25%,11.75%).Moreover,the MMPBSA technique showed that isoestradiol 3-benzoate had a strong association with chains B and C(ΔGbind=−126.25±2.03 and−129.27±2.25).Additionally,free energy decomposition,PCA,FEL-steered MD simulation,and umbrella sampling were also performed to validate the association of the ligand with the *** 3-benzoate binds strongly to chains B and E;therefore,it should be considered as viable candidate for inhibiting the formation of RNAP protein complex,concluded in this study.

关键词： Mycobacterium tuberculosis DNA-Directed RNA polymerase Docking Steered MD simulation Natural compounds Binding free energy Umbrella sampling

Josephin domain containing 2(JOSD2)promotes lung cancer by inhibiting LKB1(Liver kinase B1)activity

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Signal Transduction and Targeted Therapy 2024年第2期9卷 693-708页

作者： Tao Yuan Chenming Zeng Jiawei Liu Chenxi Zhao Fujing Ge Yuekang Li Meijia Qian Jiamin Du Weihua Wang Yonghao Li Yue Liu Xiaoyang Dai Jianya Zhou Xueqin Chen Shenglin Ma Hong Zhu Qiaojun He Bo Yang Institute of Pharmacology&Toxicology Zhejiang Province Key Laboratory of Anti-Cancer Drug ResearchCollege of Pharmaceutical SciencesZhejiang UniversityHangzhou 310058China Innovation Institute for Artificial Intelligence in Medicine Zhejiang UniversityHangzhou 311199China Ministry of Education Key Laboratory of Chinese medicinal plants Resource from Lingnan Research Center of Medicinal Plants Resource Science and EngineeringGuangzhou University of Chinese MedicineGuangzhou 510006China Center for Drug Safety Evaluation and research of Zhejiang University Hangzhou 310058China department of Respiratory Disease Thoracic Disease CenterThe First Affiliated HospitalCollege of MedicineZhejiang UniversityHangzhou 310006China department of Oncology Hangzhou Cancer HospitalHangzhou 310002China Cancer Center of Zhejiang University HangzhouChina Engineering research Center of Innovative Anticancer Drugs Ministry of EducationHangzhouChina

Non-small cell lung cancer(NSCLC)ranks as one of the leading causes of cancer-related deaths *** the prominence and effectiveness of kinase-target therapies in NSCLC treatment,these drugs are suitable for and beneficial to a mere~30%of NSCLC ***,the need for novel strategies addressing NSCLC remains ***(DUBs),a group of diverse enzymes with well-defined catalytic sites that are frequently overactivated in cancers and associated with tumorigenesis and regarded as promising therapeutic ***,the mechanisms by which DUBs promote NSCLC remain poorly *** a global analysis of the 97 DUBs’contribution to NSCLC survival possibilities using The Cancer Genome Atlas(TCGA)database,we found that high expression of Josephin Domain-containing protein 2(JOSD2)predicted the poor prognosis of *** of JOSD2 significantly impeded NSCLC growth in both cell/patient-derived xenografts in ***,we found that JOSD2 restricts the kinase activity of LKB1,an important tumor suppressor generally inactivated in NSCLC,by removing K6-linked polyubiquitination,an action vital for maintaining the integrity of the LKB1-STRAD-MO25 ***,we identified the first small-molecule inhibitor of JOSD2,and observed that its pharmacological inhibition significantly arrested NSCLC proliferation in vitro/in *** findings highlight the vital role of JOSD2 in hindering LKB1 activity,underscoring the therapeutic potential of targeting JOSD2 in NSCLC,especially in those with inactivated LKB1,and presenting its inhibitors as a promising strategy for NSCLC treatment.

关键词： LKB1 inhibiting removing

Modulation of the in vitro Oxidative Stress and Erythrocyte Cell Membrane Integrity Using Aqueous, Hydroethanolic and Ethanolic Stem-Barks Extracts of Greenwayodendron suaveolens (Engl. & Diels) Verdc

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Pharmacology & Pharmacy 2024年第3期15卷 39-61页

作者： Patrick Hervé Diboue Betote Moustapha Gambo Abdoulaye Francis Ngolsou Esther Del Florence Ndedi Moni Adeline Sabine Fanta Yadang Fidel Castro Lah Weyepe Gabriel A. Agbor Nga Nnanga Maximilienne Ascension Nyegue Laboratory of Pharmacology and Drugs Discovery Centre for Research on Medicinal Plants and Traditional Medicine Institute of Medical Research and Medicinal Plants Studies Yaoundé Cameroon Laboratory of Microbiology Department of Microbiology Faculty of Science University of Yaoundé I Yaoundé Cameroon Multidisciplinary Laboratory Department of Galenical Pharmacy and Pharmaceutical Law Faculty of Medicine and Biomedical Sciences University of Yaoundé I Yaoundé Cameroon department of Physicochemical and Pharmaceutical Sciences Faculty of Health Sciences Abdou Moumouni University Niamey Niger department of Pharmaceutical and Biological Sciences Faculty of Medicine and Pharmaceutical Sciences University of Douala Douala Cameroon Laboratory of Pharmaceutical Technology Centre for Research on Medicinal Plants and Traditional Medicine Institute of Medical Research and Medicinal Plants Studies Yaoundé Cameroon

Pneumonia, a respiratory infection induces acute or chronic inflammation, characterized by increased activity of lymphocytes and neutrophils, thus generating oxygen-free radicals that decrease the endogenous antioxidants defence system. The aim of this experimental study focused on the capacity of nontoxic aqueous, hydroethanolic and ethanolic extracts of Greenwayodendron suaveolens (Engl. & Diels) Verdc. subsp. suaveolens to regulate free reactive species and protein inflammation generated by infectious disease. The phytochemical screenings of G. suaveolens extracts were carried out according to precipitation and colorimetric methods. The total antioxidant and flavonoid contents were determined by the Folin-Ciocalteu and Aluminium Chloride ethanolic methods. The efficiency of G. suaveolens extracts on free radicals was evaluated using DPPH•, ABTS+•, and FRAP methods. The anti-inflammatory properties of extracts were evaluated according to in vitro protein (BSA) denaturation, Proteinase Inhibitory Action, and Red Blood Cell Membrane stabilization assays. The G. suaveolens aqueous, hydroethanolic and ethanolic extracts were used for the acute toxicity assessment according to the OECD protocol. The obtained results showed the presence of flavonoids, phenols, polyphenols, tannins, anthocyanins, alkaloids, terpenoids, and sterols as secondary metabolites families in G. suaveolens extracts. The highest contents of total antioxidants and flavonoids were highlighted in the hydroethanolic extract. However, it’s the G. suaveolens aqueous extract that showed the best free radical DPPH• and ABTS+• scavenging activities (SC50) of 11.06 μg/mL and 15.16 μg/mL respectively. The highest ferric-reducing activity was found in G. suaveolens ethanolic extract with 866.23 μg EGA/mg of dry weight. The hydroethanolic extract has shown a high anti-inflammatory activity through BSA denaturation and erythrocyte membrane haemolysis with i

关键词： Greenwayodendron suaveolens Secondary Metabolites Oxidative Stress Antioxidant Activity Anti-Inflammatory Properties and Oral Acute Toxicity

A review:the mechanism of plant-derived polysaccharides on osteoblasts and osteoclasts

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未来食品学报(英文) 2024年第3期4卷 183-192页

作者： Mengjie Ren Adel F.Ahmed Meng Li Menghan Li Zhiruo Yan Jinmei Wang National R&D Center for Edible Fungus Processing Technology Henan UniversityKaifeng 475004China Joint International research Laboratory of Food&Medicine Resource Function Henan ProvinceKaifeng 475004China medicinal and Aromatic plants researches department Horticulture Research InstituteAgricultural Research CenterGiza 12511Egypt

Bone loss and deterioration of bone microarchitecture would increase the bone fragility and fracture risk,leading to the *** and more evidences proved that plant-derived polysaccharides could have a remarkable influence on osteoblasts and osteoclasts,exerting anti-osteoporosis *** to the previous research,the extract of Cibotium barumoz,Achyranthes bidentata,Curculigo orchioides,Epimedium brevicornum,Angelica sinensis,Polygonatum sibiricum,Dendrobium officinale,Morinda officinalis,Nelumbo mucifera,Diospyros kaki,Hordeum vulgare,Cistanche deserticola,Commiphora Myrrha and other plant-derived polysaccharides could benefit to the osteoblasts and *** essential mechanisms are mainly related to the activation or inhibition of many factors,including runt-related transcription factor 2(Runx2),B-catenin,osterix(Osx),activator protein-1(AP-1),osteocalcin(OCN/BGP),alkaline phosphatase(ALP),osteopontin(OPN),bone morphogenetic protein(BMP),phosphatidylinositol 3-kinase(PI3K)/C-Jun N-terminal kinase(JNK)/extracellular regulated protein kinase(ERK),osteoprotegerin(OPG),receptor activator of nuclear factor-kB(RANK),monocyte/macrophage colony-stimulating factor(M-CSF),tumor necrosis factor receptor-associated factor 6(TRAF-6),receptor activator of nuclear factor(NF)-KB ligand(RANKL),nuclear factor of activated T cells 1(NFATc1),c-Fos,matrix metallopeptidase-9(MMP-9),glycogen synthase kinase 3β(GSK3B)/B-catenin,nuclear factor E2-related factor 2(Nf2),as well as these related pathways,such as Wnt/p-catenin,BMP-2/SMAD1/5/8,PI3K/AKT,OPG/RANKL/RANK,NF-κB,MAPKs,*** plant-derived polysaccharides could improve the dynamic balance of bone formation and resorption through promoting the differentiation and maturation of osteoblast or inhibiting its *** reviewed plant-derived polysaccharides and their regulating mechanisms on the osteoclasts and osteoblasts provide the evidences for the development of osteoporosis therapeutics.

关键词： Osteoporosis Plant-derived polysaccharides Osteogenesis promotion Osteoclasts inhibition

Drosophila X virus-like particles as delivery carriers for improved oral insecticidal efficacy of scorpion Androctonus australis peptide against the invasive fruit fly,Drosophila suzukii

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Insect Science 2024年第3期31卷 847-858页

作者： Qi Xue Luc Swevers Clauvis Nji Tizi Taning Faculty of Bioscience Engineering Department of Plants and CropsGhent UniversityGhentBelgium Insect Molecular Genetics and Biotechnology Institute of Biosciences and ApplicationsNational Centre for Scientific Research"Demokritos"AthensGreece

Insect-specific neurotoxic peptides derived from the venoms of scorpions and spiders can cause acute paralysis and death when injected into insects,offering a promising insecticidal component for insect pest ***,effective delivery systems are required to help neurotoxic peptides pass through the gut barrier into the hemolymph,where they can ***,we investigated the potential of a novel nanocarrier,Drosophila X virus-like particle(DXV-VLP),for delivering a neurotoxin from the scorpion Androctonus australis Hector(AaIT)against the invasive pest fruit fly,Drosophila *** results show that the fusion proteins of DXV polyproteins with AalT peptide at their Ctermini could be sufficiently produced in Lepidoptera Hi5 cells in a soluble form using the recombinant baculovirus expression system,and could self-assemble into VLPs with similar particle morphology and size to authentic DXV *** addition,the AalT peptides displayed on DXV-VLPs retained their toxicity,as demonstrated in injection bioassays that resulted in severe mortality(72%)in adults after 72 *** fed to adults,mild mortality was observed in the group treated with DXV-AalT(38%),while no mortality occurred in the group treated with AaIT peptide,thus indicating the significant role of DXV-VLPs in delivering AalT ***,this proof-of-concept study demonstrates for the first time that VLPs can be exploited to enhance oral delivery of insect-specific neurotoxic peptides in the context of pest ***,it provides insights for further improvements and potentially the development of neurotoxin-based bioinsecticides and/or transgenic crops for insect pest control.

关键词： AalT Drosophila suzuki nanocarrier neurotoxic peptides pest control virus-like particle(VLP)

Molecular regulation of the key specialized metabolism pathways in medicinal plants

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Journal of Integrative Plant Biology 2024年第3期66卷 510-531页

作者： Min Shi Siwei Zhang Zizhen Zheng Itay Maoz Lei Zhang Guoyin Kai Zhejiang Provincial International S&T Cooperation Base for Active Ingredients of medicinal and Edible plants and Health Zhejiang Provincial Key TCM Laboratory for Chinese Resource Innovation and TransformationSchool of Pharmaceutical SciencesJinhua AcademyZhejiang Chinese Medical UniversityHangzhou 310053China department of Postharvest Science Agricultural Research OrganizationVolcani CenterRishonLeZion 7505101Israel department of Pharmaceutical Botany School of PharmacyNaval Medical UniversityShanghai 200433China

The basis of modern pharmacology is the human ability to exploit the production of specialized metabolites from medical plants,for example,terpenoids,alkaloids,and phenolic ***,in most cases,the availability of these valuable compounds is limited by cellular or organelle barriers or spatio-temporal accumulation patterns within different plant *** factors(TFs)regulate biosynthesis of these specialized metabolites by tightly controlling the expression of biosynthetic ***-edge technologies and/or combining multiple strategies and approaches have been applied to elucidate the role of *** this review,we focus on recent progress in the transcription regulation mechanism of representative high-value products and describe the transcriptional regulatory network,and future perspectives are discussed,which will help develop high-yield plant resources.

关键词： biosynthesis medicinal plants omics secondary metabolism transcription factors

Three rare anti-inflammatory sesquiterpene lactones from Magnolia grandiflora

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Chinese Journal of Natural Medicines 2024年第3期22卷 265-272页

作者： XU Shuangyu ZHANG Feng TAO Linlan JIANG Yangming HUANG Tao LI Yanan HU Zhanxing YANG Jue HAO Xiaojiang YUAN Chunmao State Key Laboratory of Functions and Applications of medicinal plants Guizhou Medical UniversityGuiyang 550014China School of Pharmaceutical Sciences Guizhou Medical UniversityGuiyang 550025China Natural Products research Center of Guizhou Province Guiyang 550014China State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650201China

Four new sesquiterpene lactones(SLs)(1–4),along with a biosynthetically related SL(5),have been isolated from the leaves of Magnolia *** A(1)is notable as the first C18 homogemarane type SL,featuring a unique 1,7-dioxaspiro[4.4]nonan-6-one *** 2 and 3,representing the first instances of chlorine-substituted gemarane-type SL analogs in natural products,were also *** structures of these isolates were elucidated through a combination of spectroscopic data analysis,electronic circular dichroism calculations,and X-ray single-crystal diffraction *** isolates demonstrated anti-inflammatory activity in lipopolysaccharide-stimulated RAW264.7 ***,3–5 showed a significant inhibitory effect on nitric oxide production,with IC50 values ranging from 0.79 to 4.73μmol·L^(−1).Additionally,4 and 5 exhibited moderate cytotoxic activities against three cancer cell lines,with IC50 values between 3.09 and 11.23μmol·L^(−1).

关键词： Magnolia grandiflora Sesquiterpene lactones Isolation and identification Anti-inflammatory activity

Developing fertility control for rodents: a framework for researchers and practitioners

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Integrative Zoology 2024年第1期19卷 87-107页

作者： Giovanna MASSEI Jens JACOB Lyn A.HINDS Botstiber Institute for Wildlife Fertility Control Department of Environment and GeographyUniversity of YorkHeslingtonYorkUK Rodent research Institute for Epidemiology and Pathogen DiagnosticsJulius Kühn–Institute(JKI)Federal Research Institute for Cultivated PlantsMünsterGermany CSIRO Health and Biosecurity CanberraACTAustralia

Fertility control is often heralded as a humane and effective technique for management of overabundant wildlife,including *** intention is to reduce the use of lethal and inhumane methods,increase farm productivity and food security as well as reduce disease transmission,particularly of *** developed a framework to guide researchers and stakeholders planning to assess the effectiveness of a potential contraceptive agent for a particular *** guidelines describe the overarching research questions which must be sequentially addressed to ensure adequate data are collected so that a contraceptive can be registered for use in broad-scale rodent *** framework indicates that studies should be undertaken iteratively and,at times,in parallel,with initial research being conducted on(1)laboratory-based captive assessments of contraceptive effects in individuals;(2)simulation of contraceptive delivery using bait markers and/or surgical sterilization of different proportions of afield-based or enclosure population to determine how population dynamics are affected;(3)development of mathematical models which predict the outcomes of different fertility control scenarios;and(4)implementation of large-scale,replicated trials to validate contraceptive efficacy under various management-scalefield *** some circumstances,fertility control may be most effective when integrated with other methods(*** culling).Assessment of non-target effects,direct and indirect,and the environmental fate of the contraceptive must also be *** fertility control for a species is a resource-intensive commitment but will likely be less costly than the ongoing environmental and economic impacts by rodents and rodenticides in many contexts.

关键词： captive studies field applications modeling oral contraceptive delivery population management rodents