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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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Electrocatalysts with atomic-level site for nitrate reduction to ammonia

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Journal of Energy Chemistry 2024年第9期96卷 642-668页

作者： Shuai Yin Rong Cao Yifan Han Jiachangli Shang Jing Zhang Wei Jiang Guigao Liu National Special Superfine Powder Engineering Research Center School of Chemistry1nd Chemical EngineeringNanjing University of Science1nd TechnologyNanjing 210094JiangsuChina school of pharmacy Jiangsu UniversityZhenjiang 212013JiangsuChina

Ammonia(NH_(3))is an important raw material for modern agriculture and industry,being widely demanded to sustain the sustainable development of modern ***,the industrial production methods of NH_(3),such as the traditional Haber-Bosch process,have drawbacks including high energy consumption and significant carbon dioxide *** recent years,the electrocatalytic nitrate reduction reaction(NO_(3)RR)powered by intermittent renewable energy sources has gradually become a multidisciplinary research hotspot,as it allows for the efficient synthesis of NH_(3)under mild *** this review,we focus on the research of electrocatalysts with atomic-level site,which have attracted attention due to their extremely high atomic utilization efficiency and unique structural characteristics in the field of NO_(3)***,we introduce the mechanism of nitrate reduction for ammonia synthesis and discuss the in-situ characterization techniques related to the mechanism ***,we review the progress of the electrocatalysts with atomic-level site for nitrate reduction and explore the structure-activity relationship to guide the rational design of efficient ***,the conclusions of this review and the challenges and prospective of this promising field are presented.

关键词： Ammonia synthesis Nitrate reduction Electrocatalysts with atomic-level site Reaction mechanism In-situ characterization techniques

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Understanding the Novel Approach of Nanoferroptosis for Cancer Therapy

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Nano-Micro Letters 2024年第9期16卷 501-556页

作者： Afsana Sheikh Prashant Kesharwani Waleed H.Almalki Salem Salman Almujri Linxin Dai Zhe‑Sheng Chen Amirhossein Sahebkar Fei Gao Department of Pharmaceutics School of Pharmaceutical Education and ResearchJamia HamdardNew Delhi 110062India Department of Pharmacology and Toxicology Faculty of PharmacyUmm Al-Qura UniversityMakkahSaudi Arabia Department of Pharmacology College of PharmacyKing Khalid University61421 Asir‑AbhaSaudi Arabia State Key Laboratory of Southwestern Chinese Medicine Resources Pharmacy SchoolChengdu University of Traditional Chinese MedicineChengdu 611130People’s Republic of China Department of Pharmaceutical Sciences College of Pharmacy and Health SciencesSt.John’s UniversityNew York 11439USA Biotechnology Research Center Pharmaceutical Technology InstituteMashhad University of Medical SciencesMashhadIran Applied Biomedical Research Center Mashhad University of Medical SciencesMashhadIran

As a new form of regulated cell death,ferroptosis has unraveled the unsolicited theory of intrinsic apoptosis resistance by cancer *** molecular mechanism of ferroptosis depends on the induction of oxidative stress through excessive reactive oxygen species accumulation and glutathione depletion to damage the structural integrity of *** to their high loading and structural tunability,nanocarriers can escort the delivery of ferro-therapeutics to the desired site through enhanced permeation or retention effect or by active *** review shed light on the necessity of iron in cancer cell growth and the fascinating features of ferroptosis in regulating the cell cycle and ***,we discussed the effect of ferroptosis-mediated therapy using nanoplatforms and their chemical basis in overcoming the barriers to cancer therapy.

关键词： Ferroptosis Nanoparticles Ferrotherapy Cancer Genes Nanotechnology Toxicity Reactive oxygen species

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Multistep continuous flow synthesis of Erlotinib

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Chinese Chemical Letters 2024年第4期35卷 371-375页

作者： Hui Jin Qin Cai Peiwen Liu Yan Chen Derong Wang Weiping Zhu Yufang Xu Xuhong Qian State Key Laboratory of Bioreactor Engineering Shanghai Key Laboratory of Chemical BiologySchool of PharmacyEast China University of Science and TechnologyShanghai 200237China

Erlotinib is an orally administered, highly effective, specific epidermal growth factor receptor tyrosine kinase inhibitor, used to treat non-small cell lung cancer and pancreatic cancer. The traditional synthetic methods for Erlotinib exhibit long reaction time and safety concern. Herein, we describe a novel five-step route for the synthesis of Erlotinib in flow. These five steps comprise etherification, nitration, reduction,addition and cyclization reactions. All steps were optimized and converted to continuous flow process,which drastically reduces the reaction time and considerably improves the process safety as well as the total yield. Enabled by five continuous flow units, Erlotinib is efficiently afforded with an E-factor of 38,an overall yield of 83%, and a total residence time of 25.1 min. Majority steps in this process have been optimized for quantitative conversion, which offers the possibility of telescoping the entire process.

关键词： Erlotinib Continuous flow synthesis Microchannel flow reactor Process optimization Continuous nitration Continuous hydrogenation

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Natural products from untapped sources as a potent reserve against antimicrobial resistance crisis

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Chinese Journal of Natural Medicines 2024年第7期22卷 577-579页

作者： GU Xiaoxia SUN Weiguang HU Zhengxi Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation School of PharmacyTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China

Since the discovery of penicillin in 1928,antibiotics have revolutionized modern medicine by effectively treating infectious diseases and saving countless ***,the widespread development of antimicrobial resistance(AMR)now threatens the efficacy and longevity of these critical drugs.A study published in The Lancet reported that bacterial AMR contributed to approximately 4.95 million deaths globally in 2019,with 1.27 million directly attributable to AMR(Fig.1)[1].Natural products(NPs)continue to play a crucial role in discovering new antibiotics.

关键词： Natural products Untapped sources Antimicrobial resistance

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Microbiota–gut–brain axis and its therapeutic applications in neurodegenerative diseases

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Signal Transduction and Targeted Therapy 2024年第3期9卷 945-997页

作者： Jian Sheng Loh Wen Qi Mak Li Kar Stella Tan Chu Xin Ng Hong Hao Chan Shiau Hueh Yeow Jhi Biau Foo Yong Sze Ong Chee Wun How Kooi Yeong Khaw school of pharmacy Monash University MalaysiaJalan Lagoon Selatan47500 Bandar SunwaySelangorMalaysia school of pharmacy Faculty of Health&Medical SciencesTaylor’s University1Jalan TaylorsSubang Jaya 47500 SelangorMalaysia Digital Health&Medical Advancements Taylor’s University1Jalan TaylorsSubang Jaya 47500 SelangorMalaysia school of Biosciences Faculty of Health&Medical SciencesTaylor’s University1Jalan TaylorsSubang Jaya 47500 SelangorMalaysia UCL school of pharmacy University College London29-39 Brunswick SquareLondon WC1N 1AXUK

The human gastrointestinal tract is populated with a diverse microbial *** vast genetic and metabolic potential of the gut microbiome underpins its ubiquity in nearly every aspect of human biology,including health maintenance,development,aging,and *** advent of new sequencing technologies and culture-independent methods has allowed researchers to move beyond correlative studies toward mechanistic explorations to shed light on microbiome–host *** has unveiled the bidirectional communication between the gut microbiome and the central nervous system,referred to as the“microbiota–gut–brain axis”.The microbiota–gut–brain axis represents an important regulator of glial functions,making it an actionable target to ameliorate the development and progression of neurodegenerative *** this review,we discuss the mechanisms of the microbiota–gut–brain axis in neurodegenerative *** the gut microbiome provides essential cues to microglia,astrocytes,and oligodendrocytes,we examine the communications between gut microbiota and these glial cells during healthy states and neurodegenerative ***,we discuss the mechanisms of the microbiota–gut–brain axis in neurodegenerative diseases using a metabolite-centric approach,while also examining the role of gut microbiota-related neurotransmitters and gut ***,we examine the potential of targeting the intestinal barrier,blood–brain barrier,meninges,and peripheral immune system to counteract glial dysfunction in ***,we conclude by assessing the pre-clinical and clinical evidence of probiotics,prebiotics,and fecal microbiota transplantation in neurodegenerative diseases.A thorough comprehension of the microbiota–gut–brain axis will foster the development of effective therapeutic interventions for the management of neurodegenerative diseases.

关键词： degenerative therapeutic diseases

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Exosomes derived from pulmonary metastatic sites enhance osteosarcoma lung metastasis by transferring the miR-194/215 cluster targeting MARCKS

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Acta Pharmaceutica Sinica B 2024年第5期14卷 2039-2056页

作者： Pei Yu Yubao Han Lulu Meng Yanyuan Tian Zhiwei Jin Jun Luo Chao Han Wenjun Xu Lingyi Kong Chao Zhang State Key Laboratory of Natural Medicines Jiangsu Key Laboratory of Bioactive Natural Product ResearchSchool of Traditional Chinese PharmacyChina Pharmaceutical UniversityNanjing 211198China

Osteosarcoma,a prevalent primary malignant bone tumor,often presents with lung metastases,severely impacting patient survival *** vesicles,particularly exosomes,play a pivotal role in the formation and progression of osteosarcoma-related pulmonary ***,the communication between primary osteosarcoma and exosome-mediated pulmonary lesions remains obscure,with the potential impact of pulmonary metastatic foci on osteosarcoma progression largely *** study unveils an innovative mechanism by which exosomes originating from osteosarcoma pulmonary metastatic sites transport the miR-194/215 cluster to the primary tumor *** transportation enhances lung metastatic capability by downregulating myristoylated alanine-rich C-kinase substrate(MARCKS)*** this phenomenon,in this study we employ cationic bovine serum albumin(CBSA)to form nanoparticles(CBSA-anta-194/215)via electrostatic interaction with antagomir-miR-194/*** nanoparticles are loaded into nucleic acid-depleted exosomal membrane vesicles(anta-194/215@Exo)targeting osteosarcoma lung metastatic *** with bioengineered exosome mimetics(anta-194/215@Exo)not only impedes osteosarcoma progression but also significantly prolongs the lifespan of tumor-bearing *** findings suggest that pulmonary metastatic foci-derived exosomes initiate primary osteosarcoma lung metastasis by transferring the miR-194/215 cluster targeting MARCKS,making the miR-194/215 cluster a promising therapeutic target for inhibiting the progression of patients with osteosarcoma lung metastases.

关键词： Lung–bone transmission miR-194/215 cluster Exosome Lung metastasis Epithelial–mesenchymal transition Vasculogenic mimicry Bioengineered exosome mimetics Osteosarcoma

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Progress in approved drugs from natural product resources

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Chinese Journal of Natural Medicines 2024年第3期22卷 195-211页

作者： LUO Zhongwen YIN Fucheng WANG Xiaobing KONG Lingyi State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Bioactive Natural Product Research School of Traditional Chinese PharmacyChina Pharmaceutical UniversityNanjing 211198China

Natural products (NPs) have consistently played a pivotal role in pharmaceutical research, exerting profound impactson the treatment of human diseases. A significant proportion of approved molecular entity drugs are either directly derived from NPs orindirectly through modifications of NPs. This review presents an overview of NP drugs recently approved in China, the United States,and other countries, spanning various disease categories, including cancers, cardiovascular and cerebrovascular diseases, centralnervous system disorders, and infectious diseases. The article provides a succinct introduction to the origin, activity, development process, approval details, and mechanism of action of these NP drugs.

关键词： New drugs Natural products Structural modification

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Tumor microenvironment of cancer stem cells:Perspectives on cancer stem cell targeting

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Genes & Diseases 2024年第3期11卷 275-302页

作者： Qianqian Guo Yi Zhou Tianyuan Xie Yin Yuan Huilong Li Wanjin Shi Lufeng Zheng Xiaoman Li Wenzhou Zhang Department of pharmacy The Affiliated Cancer Hospital of Zhengzhou University&Henan Cancer HospitalZhengzhouHenan 450003China Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica School of PharmacyNanjing University of Chinese MedicineNanjingJiangsu 210023China school of Life Science and Technology Jiangsu Key Laboratory of Carcinogenesis and InterventionChina Pharmaceutical UniversityNanjingJiangsu 211198China

There are few tumor cell subpopulations with stem cell characteristics in tumor tis-sue,defined as cancer stem cells(CSCs)or cancer stem-like cells(CSLCs),which can recon-struct neoplasms with malignant biological behaviors such as invasiveness via self-renewal and unlimited *** microenvironment that CsCs depend on consists of various cellular components and corresponding medium *** these factors existing at a variety of levels and forms,cytokine networks and numerous signal pathways play an important role in signaling *** factors promote or maintain cancer cell stem-ness,and participate in cancer recurrence,metastasis,and *** review aims to summarize the recent molecular data concerning the multilayered relationship between CsCs and CsC-favorable *** also discuss the therapeutic implications of target-ing this synergistic interplay,hoping to give an insight into targeting cancer cell stemness for tumortherapyandprognosis.

关键词： Cancer stem cells Cancerstem-like cells Cellular factors Non-cellularfactors Tumor microenvironment

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Tanshinone IIA ameliorates energy metabolism dysfunction of pulmonary fibrosis using 13C metabolic flux analysis

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Journal of Pharmaceutical Analysis 2024年第2期14卷 244-258页

作者： Baixi Shan Haoyan Zhou Congying Guo Xiaolu Liu Mingyu Wu Rao Zhai Jun Chen State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing210009China Department of Pharmacognosy School of Traditional Chinese PharmacyChina Pharmaceutical UniversityNanjing210009China

Evidence indicates that metabolic reprogramming characterized by the changes in cellular metabolic patterns contributes to the pathogenesis of pulmonary fibrosis (PF). It is considered as a promising therapeutic target anti-PF. The well-documented against PF properties of Tanshinone IIA (Tan IIA) have been primarily attributed to its antioxidant and anti-inflammatory potency. Emerging evidence suggests that Tan IIA may target energy metabolism pathways, including glycolysis and tricarboxylic acid (TCA) cycle. However, the detailed and advanced mechanisms underlying the anti-PF activities remain obscure. In this study, we applied [U-13C]-glucose metabolic flux analysis (MFA) to examine metabolism flux disruption and modulation nodes of Tan IIA in PF. We identified that Tan IIA inhibited the glycolysis and TCA flux, thereby suppressing the production of transforming growth factor-β1 (TGF-β1)-dependent extracellular matrix and the differentiation and proliferation of myofibroblasts in vitro. We further revealed that Tan IIA inhibited the expression of key metabolic enzyme hexokinase 2 (HK2) by inhibiting phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR)/hypoxia-inducible factor 1α (HIF-1α) pathway activities, which decreased the accumulation of abnormal metabolites. Notably, we demonstrated that Tan IIA inhibited ATP citrate lyase (ACLY) activity, which reduced the collagen synthesis pathway caused by cytosol citrate consumption. Further, these results were validated in a mouse model of bleomycin-induced PF. This study was novel in exploring the mechanism of the occurrence and development of Tan IIA in treating PF using 13C-MFA technology. It provided a novel understanding of the mechanism of Tan IIA against PF from the perspective of metabolic reprogramming.

关键词： Pulmonary fibrosis Tanshinone IIA 13C-metabolic flux analysis Metabolic reprogramming

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