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Persicaria lanigera (Polygonaceae) leaf extract exhibits antiulcerogenic and antiproliferative activities against acetic acid-induced ulcerative colitis and cotton pellet-induced granuloma tissue in rats

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Asian Pacific Journal of Tropical Biomedicine 2024年第7期14卷 269-278页

作者： Meshack Antwi-Adjei ernest Obese Emmanuel Awintiig Adakudugu Benjamin Aboagye Daniel Anokwah Akua Afriyie Karikari Roberta Antwi-Adjei Elvis Ofori Ameyaw Department of Pharmacology School of Medical SciencesUniversity of Cape CoastCape CoastGhana Department of Pharmacotherapeutics and pharmacy Practice School of Pharmacy and Pharmaceutical SciencesUniversity of Cape CoastCape CoastGhana Department of Forensic Sciences School of Biological SciencesUniversity of Cape CoastCape CoastGhana Department of Pharmacognosy and Herbal Medicine School of Pharmacy and Pharmaceutical SciencesUniversity of Cape CoastCape CoastGhana Department of Biomedical Sciences School of Allied Health SciencesCollege of Agriculture and Natural SciencesUniversity of Cape CoastCape CoastGhana

Objective:To assess the effect of leaf extract of Persicaria lanigera on cotton pellet-induced granuloma tissue formation and acetic acid-induced ulcerative ***:Rats were randomly divided into six groups:normal control,negative control,positive control(dexamethasone or sulfasalazine)as well as Persicaria lanigera(100-600 mg/kg)-treated *** effects of the extracts on body weight,antioxidant,and hematological parameters,as well as mast cell proliferation,were *** addition,a histological evaluation was ***:Persicaria lanigera extract significantly decreased the mean exudate amount and suppressed granuloma tissue formation in a concentration-dependent manner in rats(P<0.05).Additionally,the extract significantly increased body weight,improved hematological profile,reduced the disease activity index score and malondialdehyde level,as well as enhanced catalase and superoxide dismutase activities(P<0.05).Histological evaluation showed Persicaria lanigera extract alleviated acetic acid-induced colonic damages,as evidenced by decreased cell necrosis,edema,and inflammatory cell ***:Persicaria lanigera extract possesses antiproliferative,antioxidative,and anti-colitis ***,its underlying mechanisms of action need further investigation.

关键词： Colitis Persicaria lanigera Antioxidant Cotton pellets Mast cells Granuloma tissue formation

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Network Pharmacology and Experimental Study of MomordicineⅠand MomordicineⅡfrom Bitter Melon Saponins in Inhibiting Fat Accumulation

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Biomedical and Environmental Sciences 2024年第5期37卷 526-530页

作者： HUANG Shi Ting LI Shang Yuan LI Xin Yu ZHU Ying ZHU Lin ZHANG Jia Yan ZHAO Yan Sheng DAGLIA maria XIAO Xiang BAI Juan school of Food and Biological Engineering Jiangsu UniversityZhenjiang 212013JiangsuChina Department of pharmacy University of Napoli FedericoⅡVia D.Montesano 4980131 NaplesItaly International Research Center for Food Nutrition and Safety Jiangsu UniversityZhenjiang 212013JiangsuChina

Bitter melon(Momordica Charania L.),a member of the Cucurbitaceae family,is widely distributed across tropical and subtropical ***,an important functional component of bitter melon,has been proven to exert hypoglycemic effects similarly to insulin,and also possesses lipid-lowering properties inhibiting preadipocyte differentiation and fat synthesis^([1]).

关键词： melon Momordica subtropical

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The challenge of molecular selection in liver-limited metastatic colorectal cancer for surgical resection: a systematic review and meta-analysis in the context of current and future approaches

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Oncology Research 2024年第9期32卷 1407-1422页

作者： ROSSANA RONCATO JERRY POLESEL FEDERICA TOSI ELENA PERUZZI ERIKA BRUGUGNOLI CLAUDIA LAURIA PANTANO maria FURFARO FILIPPO DI GIROLAMO ALESSANDRO NANI ARIANNA PANI NOEMI MILAN ELENA DE MATTIA ANDREA SARTORE-BIANCHI ERIKA CECCHIN Experimental and Clinical Pharmacology Unit Centro di Riferimento Oncologico di Aviano(CRO)IRCCSAviano33081Italy Department of Medicine(DMED) University of UdineUdine33100Italy Unit of Cancer Epidemiology Centro di Riferimento Oncologico di Aviano(CRO)IRCCSAviano33081Italy Department of Oncology and Hemato-Oncology Universitàdegli Studi di MilanoMilan20122Italy Department of Hematology Oncologyand Molecular MedicineGrande Ospedale Metropolitano NiguardaMilan20122Italy Oncology pharmacy Unit IRCCS Istituto Romagnolo per lo Studio dei Tumori Dino AmadoriMeldola47014Italy pharmacy Unit Fondazione IRCCS Istituto Tumori di MilanoMilan20122Italy Department of pharmacy Ca’Foncello Treviso Regional HospitalPiazzale Ospedale 1Treviso31100Italy Department of Medical Surgical and Health Sciences University of TriesteTrieste34127Italy Hospital pharmacy Cattinara HospitalAzienda Sanitaria Universitaria Giuliano IsontinaTrieste34148Italy Department of Oncology and Onco-Hematology Postgraduate School of Clinical Pharmacology and ToxicologyUniversity of MilanMilan20122Italy

Objectives:Treatment of metastatic colorectal cancer(mCRC)includes resection of liver metastases(LM),however,no validated biomarker identifies patients most likely to benefit from this *** meta-analysis aimed to assess the impact of the most relevant molecular alterations in cancer-related genes of CRC(i.e.,RAS,BRAF,SMAD4,PIK3CA)as prognostic markers of survival and disease recurrence in patients with mCRC surgically treated by LM ***:A systematic literature review was performed to identify studies reporting data regarding survival and/or recurrence in patients that underwent complete liver resection for CRC LM,stratified according to RAS,BRAF,PIK3CA,and SMAD4 mutational *** ratios(HRs)from multivariate analyses were pooled in the meta-analysis and various adjustment strategies for confounding factors were *** search was conducted in numerous databases,including MEDLINE(PubMed),Embase,Cumulative Index to Nursing and Allied Health Literature(CINAHL)(EBSCO host),and WHO Global Index Medicus,through March 18th,***-analyses,editorials,letters to the editor,case reports,studies on other primary cancers,studies with primary metastatic sites other than the liver,studies lacking specific oncological outcome variables or genetic data,non-English language studies,and studies omitting residual disease data from liver metastasectomy were *** remaining 47 studies were summarized in a descriptive table which outlines the key characteristics of each study and final results were graphically ***:RAS mutation status was negatively associated with overall survival(OS)(HR,1.68;95%CI,1.54–1.84)and recurrence free survival(RFS)(HR,1.46;95%CI,1.33–1.61).A negative association was also found for BRAF regarding OS(HR,2.64;95%CI,2.15–3.24)and RFS(HR,1.89;95%CI,1.32–2.73)and SMAD4 regarding OS(HR,1.93;95%CI,1.56–2.38)and RFS(HR,1.95;95%CI,1.31–2.91).For PIK3CA only three studies were eligible and no significant associati

关键词： Metastasectomy Liver metastases RAS BRAF SMAD4 PIK3CA Colorectal

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Development and validation of a rapid UPLC/MS method for the simultaneous determination of I3C, DIM, and related metabolites and its application to pharmacokinetics studies

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Journal of Chinese Pharmaceutical Sciences 2016年第7期25卷 477-488页

作者： Yury Gomez Hu Wang Ah-Ng Tony Kong Graduate Program in Pharmaceutical Science Ernest Mario School of Pharmacy Rutgers The State University of New Jersey Department of Pharmaceutics Ernest Mario School of Pharmacy Rutgers The State University of New Jersey

Indole-3-carbinol(I3C) and diindolylmethane(DIM) are naturally derived dietary phytochemicals with promising anti-cancer properties that have been demonstrated both in vitro and in vivo. Using reversed-phase ultra-performance liquid chromatography(UPLC) coupled with mass spectrometry(MS), a rapid, specific, and high throughput method was developed and validated for the quantification and identification of I3 C, DIM, and other I3 C metabolites in plasma. Samples containing I3 C or DIM and the internal standard 4-methoxy indole(IS) were extracted using a liquid-liquid extraction technique. The mean recovery was 96.21% for I3 C and 108.5% for DIM. Separation was achieved using a Waters Acquity UPLC HSS T3, 1.8 μm, 2.1 mm×150 mm column and acetonitrile–water gradient elution. The flow rate was 0.3 m L/min and the run time was 9 min. The limits of detection and quantification for I3 C and DIM were 15 ng/m L and 25 ng/m L, respectively. Calibration curves for I3 C and DIM were linear(r2>0.99) over a concentration range of 0.025–20 μg/m L. Precision, accuracy, and stability analysis fulfilled the CDER guidelines criteria. The method was successfully applied to the determination of the pharmacokinetic parameters of I3 C or DIM after oral, intravenous, or intraperitoneal administration to Sprague Dawley rats. The method described here is superior over existing analytical methods for I3 C and its metabolites in terms of sensitivity, speed, and separation.

关键词： UPLC/MS Indole-3-Carbinol Diindolylmethane Pharmacokinetics Single-dose administration Sprague-Dawley Rats

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The role of Eph receptors in lens function and disease

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Science China(Life Sciences) 2012年第5期55卷 434-443页

作者： SON Alexander I. PARK Jeong Eun Department of Chemical Biology Ernest Mario School of PharmacyRutgersThe State University of New Jersey

Cataract is the single largest contributor to blindness in the world,with the disease having a strong genetic *** recent years the Eph family of receptor tyrosine kinases has been identified as a key regulator in lens... 详细信息

关键词： cataract lens EphA2 ephrin-A5

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Discovery of direct inhibitors of Keap1–Nrf2 protein–protein interaction as potential therapeutic and preventive agents

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Acta Pharmaceutica Sinica B 2015年第4期5卷 285-299页

作者： Dhulfiqar Ali Abed Melanie Goldstein Haifa Albanyan Huijuan Jin Longqin Hu Department of Medicinal Chemistry Ernest Mario School of Pharmacy Rutgers The State University of New Jersey school of Pharmaceutical Sciences Shanxi Medical University

The Keap1–Nrf2–ARE pathway is an important antioxidant defense mechanism that protects cells from oxidative stress and the Keap1–Nrf2 protein–protein interaction(PPI) has become an important drug target to upregulate the expression of ARE-controlled cytoprotective oxidative stress response enzymes in the development of therapeutic and preventive agents for a number of diseases and conditions. However, most known Nrf2 activators/ARE inducers are indirect inhibitors of Keap1–Nrf2PPI and they are electrophilic species that act by modifying the sulfhydryl groups of Keap1's cysteine residues. The electrophilicity of these indirect inhibitors may cause "off-target" side effects by reacting with cysteine residues of other important cellular proteins. Efforts have recently been focused on the development of direct inhibitors of Keap1–Nrf2 PPI. This article reviews these recent research efforts including the development of high throughput screening assays, the discovery of peptide and small molecule direct inhibitors, and the biophysical characterization of the binding of these inhibitors to the target Keap1 Kelch domain protein. These non-covalent direct inhibitors of Keap1–Nrf2 PPI could potentially be developed into effective therapeutic or preventive agents for a variety of diseases and conditions.

关键词： Oxidative stress Keap1 Nrf2 Direct inhibitors of protein–protein interaction High throughput screening assays Structure–activity relationships X-ray crystallography

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Insects: an underrepresented resource for the discovery of biologically active natural products

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Acta Pharmaceutica Sinica B 2017年第4期7卷 409-426页

作者： Lauren Seabrooks Longqin Hu Department of Medicinal Chemistry Ernest Mario School of Pharmacy Rutgers The State University of New Jersey Cancer Institute of New Jersey

Nature has been the source of life-changing and-saving medications for centuries. Aspirin,penicillin and morphine are prime examples of Nature's gifts to medicine. These discoveries catalyzed the field of natural product drug discovery which has mostly focused on plants. However, insects have more than twice the number of species and entomotherapy has been in practice for as long as and often in conjunction with medicinal plants and is an important alternative to modern medicine in many parts of the world. Herein, an overview of current traditional medicinal applications of insects and characterization of isolated biologically active molecules starting from approximately 2010 is presented. Insect natural products reviewed were isolated from ants, bees, wasps, beetles, cockroaches, termites, flies, true bugs,moths and more. Biological activities of these natural products from insects include antimicrobial,antifungal, antiviral, anticancer, antioxidant, anti-inflammatory and immunomodulatory effects.

关键词： Natural products Insects Entomotherapy Traditional medicine Drug discovery

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Comparison of phenolic profiles and antioxidant activities in skins and pulps of eleven grape cultivars(Vitis vinifera L.)

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Journal of Integrative Agriculture 2019年第5期18卷 1148-1158页

作者： LI Fu-xiang LI Fu-hua YANG Ya-xuan YIN Ran MING Jian College of Food Science Southwest University Research Center of Food Storage & Logistics Southwest University ernest Mario school of pharmacy Rutgers University

Eleven grape cultivars were analysed to explore the variety differences of fresh grape phenolic profiles. The results showed that free phenolics were predominant in grape skins and pulps, and showed the higher antioxidant activities than bound. In 11 cultivars, Muscat Kyoho extracts had the highest total phenolic content in skins(10.525 mg GAE g^(–1) FW) and pulps(1.134 mg GAE g^(–1) FW), and exhibited the highest DPPH radical scavening capacity(EC_(50)=11.7 μg mL^(–1)) and oxygen radical absorbance capacity(ORAC) value(190.57 μmol TE g^(–1) FW) of free phenolic in skin. In addition, the most abundant phenolics in grape skins were found to be flavonoids such as kaempferol in Kyoho skin(541.2 μg g^(–1) FW), rutin, catechin and epicatechin in Muscat Kyoho skin(262.3, 86.3 and 70.0 μg g^(–1) FW, respectively). Furthermore, the principal component analysis showed a strong difference of phenolic profiles with the cultivars, existing forms and distributions. Pearson correlation coefficient analysis showed a significant linear correlation between total phenolic content and antioxidant activity(P<0.05). Therefore, both skins and pulps were rich sources of bioactive phenolic compounds, and Muscat Kyoho was the ideal source among all samples.

关键词： grape phenolics varietal diversity antioxidant activity principal component analysis

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Natural dietary anti-cancer chemopreventive compounds:redox-mediated differential signaling mechanisms in cytoprotection of normal cells versus cytotoxicity in tumor cells

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Acta Pharmacologica Sinica 2007年第4期28卷 459-472页

作者： Sujit NAIR Ah-Ng Tony KONG Graduate Program in Pharmaceutical Sciences Department of Pharmaceutics Ernest Mario School of PharmacyRutgersThe StateUniversity of New JerseyPiscatawayNew Jersey 08854USA

Many dietary phytochemicals exhibit health-beneficial effects including preven-tion of diseases such as cancer,as well as neurological,cardiovascular,inflam-matory,and metabolic ***,herbivorous and omnivorousanimals have been ingesting *** interaction between"animal-plant"ecosystems has resulted in an elaborate system of detoxification and defensemechanisms evolved by animals including *** cells,includinghuman cells,respond to these dietary phytochemicals by"non-classical receptorsensing"mechanisms of electrophilic chemical-stress typified by"thiol-modu-lated"cellular signaling events primarily leading to the gene expression of phar-macologically beneficial effects,but sometimes unwanted cytotoxicity *** has been studying two groups of dietary phytochemical cancer-chemopreventive compounds (isothiocyanates and polyphenols),which areeffective in chemical-induced,as well as genetically-induced,animal carcinogen-esis *** compounds typically generate"cellular stress"and modulategene expression of phase Ⅱ detoxifying/antioxidant ***,reac-tive oxygen species,and reactive nitrogen species are known to act as secondmessengers in the modulation of many cellular signaling pathways leading togene expression changes and pharmacological ***-sensitive tran-scription factors such as nuclear factor-E2-related factor 2 (Nrf2),AP-1,NF-κB,tocite a few examples,sense and transduce changes in the cellular redox status andmodulate gene expression responses to oxidative and electrophilic stresses,pre-sumably via sulfhydryl modification of critical cysteine residues found on theseproteins and/or other upstream redox-sensitive molecular *** the currentreview,we will explore dietary cancer chemopreventive phytochemicals,discussthe link between oxidative/electrophilic stresses and the redox circuitry,and con-sider different redox-sensitive transcription *** will also discuss thekelch-l

关键词： redox Nrf2 Keapl NES NLS gene expression profiles

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Prostate cancer and chemoprevention by natural dietary phytochemicals

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Journal of Chinese Pharmaceutical Sciences 2016年第9期25卷 633-650页

作者： Asia Abed Al-Mahmood Limin Shu Hyuck Kim Christina Ramirez Douglas Pung Yue Guo Wenji Li Ah-Ng Tony Kong Graduate Program in Pharmaceutical Sciences Ernest Mario School of PharmacyRutgersThe State University of New JerseyPiseatawayNJ08854USA Department of Pharmaceuties Ernest Mario School of PharmacyRutgersThe State University of New JerseyPiseatawayNJ08854USA Center for Cancer Prevention Research Ernest Mario School of PharmacyRutgersThe State University of New JerseyPiscatawayNJ08854USA Graduate Program in Cellular and Molecular Pharmacology RutgersThe State University of New JerseyPiscatawayNJ 08854USA

Prostate cancer is the second leading cancer among men in the United States. Several studies have correlated the development of prostate cancer with diet and life-style. Therefore, a balanced diet and improved life style might inhibit prostate cancer progression. Cancer chemoprevention has emerged as an important factor in controlling cancer development through natural or synthetic compounds. Oxidative stress is among the factors contributing to prostate cancer development. The transcription factor nuclear factor(erythroid-derived 2)-like 2(Nrf2) controls detoxifying antioxidant enzymes expression by binding to the antioxidant response element(ARE) in the promoter of these genes to activate their expression. Many natural products can fight oxidative stress and protects cells from DNA damage by activating the Nrf2/ARE pathway. High consumption of fruits and vegetables can reduce disease incidence and invasive tumors. In this review, the roles of important fruit and vegetable phytochemicals in regulating prostate cancer progression and tumor growth are discussed.

关键词： Prostate cancer Phytochemicals Chemoprevention Nuclear factor(erythroid-derived 2)-like 2 Oxidative stress Antioxidant response element

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