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医学理论与实践 2024年第12期37卷 1994-1997页

作者：曲鑫邸旭天津市第四中心医院乳腺甲状腺外科 300140

目的:M2型丙酮酸激酶(PKM2)在多种肿瘤中异常表达并有望成为潜在治疗靶点,本研究旨在阐明PKM2特异性小分子抑制剂alkannin对乳腺癌恶性进展的影响及其分子机制。方法:通过生物信息学分析鉴定PKM2在乳腺癌组织及癌旁正常组织中的表达情... 详细信息

目的:M2型丙酮酸激酶(PKM2)在多种肿瘤中异常表达并有望成为潜在治疗靶点,本研究旨在阐明PKM2特异性小分子抑制剂alkannin对乳腺癌恶性进展的影响及其分子机制。方法:通过生物信息学分析鉴定PKM2在乳腺癌组织及癌旁正常组织中的表达情况及与预后的相关性。测定乳腺癌细胞MDA-MB-231中alkannin的半致死浓度(IC50)。将乳腺癌细胞分为阴性对照组和alkannin处理组,通过CCK-8实验、克隆形成实验及Transwell实验检测alkannin对肿瘤细胞存活、运动侵袭能力的影响。通过免疫印迹、qPCR、双荧光素酶报告基因等实验解析alkannin调控PKM2/β-连环蛋白(β-catenin)信号轴影响乳腺癌恶性进展的分子机制。结果:PKM2在乳腺癌组织中的表达显著高于癌旁正常组织,高表达PKM2提示患者预后不良。alkannin能够显著削弱MDA-MB-231细胞的存活、运动和侵袭能力。alkannin可通过靶向PKM2抑制β-catenin的激活。结论:本文证实了PKM2抑制剂alkannin在乳腺癌中发挥抗肿瘤作用,同时也为乳腺癌临床治疗提供了新思路。

关键词：乳腺癌 alkannin M2型丙酮酸激酶 β-连环蛋白

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Pharmacological and analytical aspects of alkannin/shikonin and their derivatives:An update from 2008 to 2022

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Chinese Herbal Medicines 2022年第4期14卷 511-527页

作者： Kirandeep Kaur Rashi Sharma Atamjit Singh Shivani Attri Saroj Arora Sarabjit Kaur Neena Bedi Department of Pharmaceutical Sciences Guru Nanak Dev UniversityAmritsar 143005India Department of Botanical and Environmental Sciences Guru Nanak Dev UniversityAmritsar 143005India

alkannin/shikonin(A/S)and their derivatives are naturally occurring naphthoquinones majorly found in Boraginaceae family *** are integral constituents of traditional Chinese medicine Zicao(roots of Lithospermum erythrorhizon).In last two decades significant increase in pharmacological investigations on alkannin/shikonin and their derivatives has been reported that resulted in discovery of their novel mechanisms in various diseases and *** review throws light on recently conducted pharmacological investigations on alkannin/shikonin and their derivatives and their *** analytical aspects are also discussed and brief summary of patent applications on inventions containing alkannin/shikonin and its derivatives is also provided.

关键词： alkannin naphthoquinones patents shikonin

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New Asymmetric Synthesis of alkannin and Shikonin

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Chinese Chemical Letters 2005年第4期16卷 465-467页

作者： JianGangZHANC QunLU WenHuDUAN JunCaoCAI ShanghaiInstituteofMateriaMedica ShanghaiInstitutesforBiologicalSciencesGraduateSchooloftheChineseAcademyofScienceChineseAcademyofSciencesShanghai201203

A new approach for asymmetric synthesis of alkannin and shikonin is presented. The chiral centers of the targets were introduced via an asymmetric C-arylation of protected chiral glyceraldehyde in high de. The two e... 详细信息

关键词： Asymmetric synthesis alkannin shikonin arylglycerols.

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Novel electrospun poly-hydroxybutyrate scaffolds as carriers for the wound healing agents alkannins and shikonins

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Regenerative Biomaterials 2021年第3期8卷 94-109页

作者： Athanasios S.Arampatzis Konstantina Giannakoula Konstantinos N.Kontogiannopoulos Konstantinos Theodoridis Eleni Aggelidou Angelique Rat Elli Kampasakali Anne Willems Dimitrios Christofilos Aristeidis Kritis Vassilios P.Papageorgiou Ioannis Tsivintzelis Andreana N.Assimopoulou Laboratory of Organic Chemistry School of Chemical EngineeringAristotle University of Thessaloniki(AUTh)Thessaloniki 54124Greece Natural Products Research Centre of Excellence(NatPro-AUTh) Center of Interdisciplinary Research and Innovation of Aristotle University of Thessaloniki(CIRI-AUTh)Thessaloniki 57001Greece Department of Physiology and Pharmacology School of MedicineFaculty of Health SciencesAristotle University of Thessaloniki(AUTh)ThessalonikiGreece Laboratory of Microbiology Faculty of SciencesGhent UniversityGhent 9000Belgium Faculty of Engineering School of Chemical Engineering and Physics LaboratoryAristotle University of ThessalonikiThessaloniki 54124Greece Physical Chemistry Laboratory School of Chemical EngineeringAristotle University of ThessalonikiThessaloniki 54124Greece

The aim of this study was to investigate the potential of novel electrospun fiber mats loaded with alkannin and shikonin(A/S)derivatives,using as carrier a highly biocompatible,bio-derived,ecofriendly polymer such as poly[(R)-3-hydroxybutyric acid](PHB).PHB fibers containing a mixture of A/S derivatives at different ratios were successfully fabricated via *** evidenced by scanning electron microscopy,the fibers formed a bead-free mesh with average diameters from 1.25 to 1.47 *** measurements suggest that electrospinning marginally increases the amorphous content of the predominantly crystalline PHB in the fibers,while a significant drug amount lies near the fiber surface for samples of high total A/S *** scaffolds displayed satisfactory characteristics,with the lower concentrations of A/S mixture-loaded PHB fiber mats achieving higher porosity,water uptake ratios,and entrapment *** in vitro dissolution studies revealed that all samples released more than 70%of the encapsulated drug after 72 *** PHB scaffolds tested by cell viability assay were proven non-toxic for Hs27 fibroblasts,with the 0.15 wt.%sample favoring cell attachment,spreading onto the scaffold surface,as well as cell ***,the antimicrobial activity of PHB meshes loaded with A/S mixture was documented for Staphylococcus epidermidis and ***.

关键词： electrospinning polyhydroxyalkanoates alkannin shikonin wound healing

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