青蒿素 artemisinin - PubMed 文献(第 5 页)
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青蒿素 的 PubMed 搜索结果(第 5 页)
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41. Effect of hyperbaric oxygen on the anticancer effect of artemisinin on molt-4 human leukemia cells.
41. 高压氧对青蒿素抗Molt-4人白血病细胞抗癌效果的影响PMID:日期:2010-11[中文摘要] 青蒿素可选择性地杀死细胞内游离铁比正常细胞多的癌细胞。高压氧（HBO₂）可能有益于癌症治疗。本研究的假设是HBO₂可增强青蒿素的抗癌活性。在用12 μM全转铁蛋白预处理后，将Molt-4人白血病细胞在10 μM青蒿素中培养，并暴露于以下三种不同条件之一90分钟：对照、室内空气对照和HBO₂。暴露后48小时测定细胞生长。孵育6小时后观察到生长差异。孵育48小时后，单独用青蒿素或单独用HBO₂处理的细胞生长为无青蒿素对照条件下生长细胞的85%。青蒿素与HBO₂联合处理使生长额外降低22%。HBO₂与青蒿素联合暴露可能是一种有效的抗癌化疗策略。
[英文摘要] Artemisinin selectively kills cancer cells which have more intracellular free iron than do normal cells. Hyperbaric oxygen (HBO(2)) may be beneficial in the treatment of cancer. The hypothesis of this study was that HBO(2) enhances anticancer activity of artemisinin. After pretreatment with 12 μM holotransferrin, Molt-4 human leukemia cells were cultured in 10 μM artemisinin and exposed for 90 min to one of three different conditions: control, room air control, and HBO(2). Cell growth was determined for 48 h after exposure. Differences in growth were noted after 6 h of incubation. After 48 h of incubation, growth of cells treated with artemisinin alone or HBO(2) alone was 85% of that of cells grown under artemisinin-free control conditions. Combined artemisinin and HBO(2) treatment resulted in an additional 22% decrease in growth. Combined HBO(2) and artemisinin exposure may be an effective anticancer chemotherapeutic strategy.
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42. Current status of artemisinin and its derivatives as antimalarial drugs.
42. 青蒿素及其衍生物作为抗疟药物的研究现状PMID:日期:2000[中文摘要] 青蒿素是一种有前景且强效的抗疟药物，能够应对耐药疟原虫和疟疾病情快速进展带来的双重挑战。本文综述了近年来从黄花蒿中生产青蒿素所取得的进展。文中描述了青蒿素的结构、生物合成及分析方法及其作用机制。本综述还重点关注了临床研究、毒性研究、药代动力学以及青蒿素相关化合物的活性。此外，还讨论了包括有机合成、植物提取、体外培养以及提高产量的替代策略在内的生产策略。
[英文摘要] Artemisinin is a promising and a potent antimalarial drug, which meets the dual challenge posed by drug-resistant parasites and rapid progression of malarial illness. This review article focuses on the progress achieved during the last years in the production of artemisinin from Artemisia annua. The structure, biosynthesis and analysis of artemisinin and its mode of action are described. The review also focuses on clinical studies, toxicity studies, pharmacokinetics and activity of artemisinin related compounds. The production strategies including organic synthesis, extraction from plants, in vitro cultures and alternative strategies for enhancing the yields are also discussed.
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43. Continuous synthesis of artemisinin-derived medicines.
43. 青蒿素衍生药物的连续合成PMID:日期:2014-09-11[中文摘要] 描述了一种连续、发散的合成系统，该系统与连续纯化耦合，能够生产四种抗疟疾原料药。该系统由三个相互连接的反应模块组成，分别用于光氧化/环化、还原和衍生化。第四个模块将粗反应流与连续纯化相耦合，以得到纯原料药。
[英文摘要] Described is a continuous, divergent synthesis system which is coupled to continuous purification and is capable of producing four anti-malarial APIs. The system is comprised of three linked reaction modules for photooxidation/cyclization, reduction, and derivatization. A fourth module couples the crude reaction stream with continuous purification to yield pure API.
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44. Absence of Artemisinin Resistance-Associated Mutations in the Plasmodium Falciparum Kelch 13 (K13) Propeller Domain Gene Following Widespread Use of Artemisinin-Based Combination Therapy in Iran.
44. 在伊朗广泛使用基于青蒿素的联合疗法后，恶性疟原虫Kelch 13（K13）螺旋桨结构域基因中没有青蒿素耐药性相关突变PMID:日期:2025-12-16[中文摘要] 对恶性疟原虫Kelch 13（pfk13）基因中与青蒿素耐药相关的突变进行持续监测，对于监控疟疾流行区耐药虫株的出现至关重要。本文评估了在全国范围内引入以青蒿素为基础的联合疗法（ACTs）18年后，伊朗恶性疟原虫分离株中与青蒿素耐药相关的pfk13基因点突变的流行情况。在2022年至2023年期间，共从伊朗有症状、非复杂性恶性疟疾患者中采集了60份指尖采血血样。采用巢式聚合酶链反应（PCR）扩增18S小亚基核糖体RNA（18S ssrRNA）基因以确认感染。利用巢式PCR扩增pfk13基因，随后对扩增产物进行测序，以鉴定已报道的突变和新突变。在成功测序的样本（n=50）中，98%（49/50）携带野生型等位基因。一份样本携带一种新的非同义突变R513C，对应C1537T核苷酸改变。研究人群中未检测到提示青蒿素耐药的经验证的pfk13突变。这些发现表明，青蒿素在该地区治疗恶性疟疾仍然有效。有必要继续进行分子监测，以确保早期发现新出现的耐药性。
[英文摘要] Continuous surveillance of Plasmodium falciparum Kelch 13 (pfk13) mutations associated with artemisinin resistance is essential for monitoring the emergence of drug-resistant parasites in malaria-endemic regions. Herein, we have assessed the prevalence of point mutations in the pfk13 gene linked to artemisinin resistance in Iranian P. falciparum isolates, 18 years following the nationwide introduction of artemisinin-based combination therapies (ACTs). A total of 60 finger-prick blood samples were obtained from Iranian patients with symptomatic, uncomplicated P. falciparum malaria during the period of 2022 to 2023. A nested polymerase chain reaction (PCR) assay was employed to verify infections by amplifying the 18 S small subunit ribosomal RNA (18 S ssrRNA) gene. Nested PCR was utilized to amplify the pfk13 gene, followed by sequencing of the amplicons to identify both previously reported and novel mutations. Of the successfully sequenced samples (n = 50), 98% (49/50) carried the wild-type allele. One sample harbored a novel nonsynonymous mutation, R513C, corresponding to a C1537T nucleotide change. No validated pfk13 mutations indicative of artemisinin resistance were detected in the study population. These findings suggest that artemisinin remains effective for treating P. falciparum malaria in this region. Continued molecular surveillance is warranted to ensure early detection of emerging resistance.
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45. Enhancement of cytotoxicity of artemisinin toward cancer cells by transferrin-mediated carbon nanotubes nanoparticles.
45. 转铁蛋白介导的碳纳米管纳米颗粒增强青蒿素对癌细胞的细胞毒性PMID:日期:2015-03-10[中文摘要] 青蒿素（ART）是一种具有内过氧桥的药物，易于与Fe(2+)反应生成自由基以杀伤癌细胞。然而，将疏水性青蒿素与Fe(2+)离子同时递送至癌细胞内仍是一项重大挑战。本研究构建了一种多功能肿瘤靶向药物递送系统，以透明质酸衍化多壁碳纳米管（HA-MWCNTs）作为药物载体，转铁蛋白（Tf）作为靶向配体，青蒿素作为模型药物用于癌症治疗。该递送系统（HA-MWCNTs/Tf@ART）不仅保留了多壁碳纳米管的光学特性和青蒿素的细胞毒性，还利用青蒿素和转铁蛋白表现出协同抗肿瘤效应。与游离青蒿素相比，由于青蒿素在细胞内的蓄积增加以及转铁蛋白与青蒿素类似物的共同递送，该药物载体在体外培养的MCF-7细胞和体内荷瘤小鼠模型中均实现了显著增强的抗肿瘤疗效。与其他组相比，HA-MWCNTs/Tf@ART联合激光照射表现出最强的抑制效果。该结果可能为利用有前景的天然药物治疗癌症提供新途径。
[英文摘要] Artemisinin (ART) is a kind of drug with an endoperoxide bridge which tends to react with Fe(2+) to generate radicals for killing cancer cells. However, simultaneous delivery of hydrophobic ART and Fe(2+) ions into cancer cells remains a major challenge. In this study, a multi-functional tumor-targeting drug delivery system employing hyaluronic acid-derivatized multi-walled carbon nanotubes (HA-MWCNTs) as drug carriers, transferrin (Tf) as targeting ligand and ART as a model drug for cancer treatment was constructed. This delivery system (HA-MWCNTs/Tf@ART) not only retained optical property of MWCNTs and cytotoxicity of ART but also demonstrated synergistic anti-tumor effect using ART and Tf. Compared with free ART, remarkably enhanced anti-tumor efficacy of this drug vehicle was realized both in cultured MCF-7 cells in vitro and in a tumor-bearing murine model in vivo, due to increased intracellular accumulation of ART and co-delivery of Tf and ART analogs. HA-MWCNTs/Tf@ART with laser irradiation demonstrated the highest inhibition effect compared to the other groups. This result may provide a new way of using promising natural drugs for cancer therapy.
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46. AaMYB15, an R2R3-MYB TF in Artemisia annua, acts as a negative regulator of artemisinin biosynthesis.
46. AaMYB15，黄花蒿中的一个R2R3-MYB转录因子，作为青蒿素生物合成的负调控因子PMID:日期:2021-04-24[中文摘要] 青蒿素是从黄花蒿中提取的一种次生代谢产物。作为世界卫生组织认可的有效抗疟成分，青蒿素具有广泛的经济价值。关于正向调控青蒿素生物合成的转录因子已有大量研究报道，而负向调控因子则鲜有报道。在本研究中，我们鉴定出AaMYB15是黄花蒿中首个负向调控青蒿素生物合成的R2R3-MYB转录因子。实验证据表明，AaMYB15是一个定位于细胞核内的转录因子，主要表达于黄花蒿中青蒿素合成和积累的腺毛分泌毛状体（GSTs）中。AaMYB15的表达受黑暗和茉莉酸（JA）处理的诱导。过表达AaMYB15导致关键酶基因ADS、CYP、DBR2和ALDH1的表达水平显著下降，并使转基因黄花蒿中青蒿素含量显著降低。AaMYB15直接结合AaORA的启动子，抑制其转录活性，从而下调下游关键酶基因的表达水平，负向调控青蒿素的生物合成；AaORA是已报道的茉莉酸信号通路中青蒿素生物合成的正向调控因子。本研究为黄花蒿种质改良提供了候选基因，并为光和茉莉酸介导的青蒿素生物合成调控网络提供了新的认识。
[英文摘要] Artemisinin is a secondary metabolite extracted from Artemisia annua. As an effective antimalarial component certified by WHO, artemisinin has extensive economical values. Numerous studies about transcription factors positively regulating artemisinin biosynthesis have been published while negative regulators are rarely reported. In the present study, we identified AaMYB15 as the first R2R3-MYB that negatively regulates artemisinin biosynthesis in A. annua. Experimental evidences showed that AaMYB15 is a transcription factor within nucleus and predominantly expressed in glandular secretory trichomes (GSTs) in A. annua where artemisinin is synthesized and accumulated. The expression of AaMYB15 was induced by dark and JA treatment. Overexpression of AaMYB15 led to a significant decline in the expression levels of key enzyme genes ADS, CYP, DBR2, and ALDH1 and a significant decrease in the artemisinin contents of transgenic A. annua. AaMYB15 directly bound to the promoter of AaORA, a reported positive regulator of artemisinin biosynthesis in JA signaling pathway, to repress its transcriptional activity, thus downregulating the expression levels of downstream key enzyme genes and negatively regulating the artemisinin biosynthesis. Our study provides candidate gene for improvement of A. annua germplasm and new insights into the artemisinin biosynthesis regulation network mediated by light and JA.
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47. GPX4 inhibition synergistically boosts mitochondria targeting nanoartemisinin-induced apoptosis/ferroptosis combination cancer therapy.
47. GPX4抑制协同增强线粒体靶向纳米青蒿素诱导的凋亡/铁死亡联合癌症治疗PMID:日期:2023-08-22[中文摘要] 青蒿素最初因其抗疟疾活性而被使用，近年来在癌症治疗领域受到了广泛关注。青蒿素的抗癌机制复杂且存在争议。青蒿素在递送方面也持续面临挑战，因为单独使用青蒿素与传统纳米载体联合时，其抗癌效果往往不尽如人意。我们在此报道了具有极高抗癌能力的青蒿素线粒体递送策略。青蒿素在癌细胞线粒体中的作用模式包括：在血红素参与下、不依赖氧的方式将青蒿素转化为碳中心自由基，该自由基在分子氧存在下部分转化为活性氧（ROS）。我们发现，青蒿素单独作用于线粒体即可诱导强烈的癌细胞凋亡。此外，由于青蒿素对GPX4活性的弱抑制作用，还可观察到微弱的铁死亡。我们进一步发现，RSL3可显著抑制MCF-7细胞中的GPX4活性，通过增强铁死亡协同增强青蒿素的抗癌能力。青蒿素与RSL3在线粒体中的协同抗癌活性不仅提高了杀伤癌细胞的能力，还抑制了残留癌细胞的再增殖。本研究为开发高效实用的青蒿素纳米药物用于癌症治疗提供了新的思路。
[英文摘要] Artemisinin, originally used for its antimalarial activity, has received much attention in recent years for cancer therapy. The anticancer mechanisms of artemisinin are complicated and debatable. Challenges in the delivery of artemisinin also persist because the anticancer effect of artemisinin alone is often not satisfactory when used with traditional nanocarriers. We herein report the mitochondrial delivery of artemisinin with extremely high anticancer capacity. The action mode of artemisinin in the mitochondria of cancer cells includes heme-participating and oxygen-independent conversion of artemisinin into a carbon-centered radical, which is partly converted into ROS in the presence of molecular oxygen. We reveal that artemisinin alone in the mitochondria can induce strong cancer cell apoptosis. In addition, due to the weak inhibition of GPX4 activity by artemisinin, weak ferroptosis is also observed. We further discover that GPX4 activity in MCF-7 cells is greatly inhibited by RSL3 to synergistically enhance the anticancer capacity of artemisinin enhancing ferroptosis. The synergistic anticancer activity of artemisinin and RSL3 in the mitochondria not only improves cancer cell-killing ability, but also inhibits the re-proliferation of residual cancer cells. This study provides a new insight into developing highly efficient and practical artemisinin nanomedicines for cancer therapy.
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48. The mode of action of the antimalarial artemisinin and its derivatives.
48. 抗疟药物青蒿素及其衍生物的作用机制PMID:期刊:General pharmacology PubMed日期:1996-06[中文摘要] 青蒿素是一种倍半萜内过氧化物，来源于一种在中国草药中使用了数千年的植物。青蒿素及其衍生物具有强效的抗疟活性，目前已在世界大部分地区用于临床。青蒿素衍生物具有独特的作用机制，涉及铁催化的碳中心自由基生成，随后对疟疾特异性蛋白进行烷基化。
[英文摘要] 1. Atremisinin (qinghaosu) is a sesquiterpene endoperoxide derived from a plant which was used in Chinese herbal medicine for thousands of years. 2. Artemisinin and its derivatives have potent antimalarial activity, and are now being used clinically in much of the world. 3. The artemisinin derivatives have an unusual mode of action involving the iron-catalyzed generation of a carbon-centered free radical followed by the alkylation of malaria-specific proteins.
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49. Artemisinin Bioactivity and Resistance in Malaria Parasites.
49. 青蒿素在疟疾寄生虫中的生物活性和抗性PMID:日期:2019-11-04[中文摘要] 青蒿素是抗疟疾最广泛使用的化合物，在全球疟疾治疗中发挥着关键作用。大约十年前，东南亚地区出现了青蒿素耐药性，防止其传播或在非洲出现至关重要。青蒿素具有复杂的作用机制，可对疟原虫的多种组分造成广泛损伤。在本综述中，我们概述了受青蒿素影响的不同代谢通路，包括未折叠蛋白反应、蛋白多聚泛素化、蛋白酶体、磷脂酰肌醇-3-激酶以及真核翻译起始因子2α。基于近期发表的数据，我们提出了一个模型，阐述这些不同通路如何相互作用，以及K13（目前发现的主要耐药标志物）的突变如何可能帮助疟原虫在青蒿素压力下存活。
[英文摘要] Artemisinin is the most widely-used compound against malaria and plays a critical role in the treatment of malaria worldwide. Resistance to artemisinin emerged about a decade ago in Southeast Asia and it is paramount to prevent its spread or emergence in Africa. Artemisinin has a complex mode of action and can cause widespread injury to many components of the parasite. In this review, we outline the different metabolic pathways affected by artemisinin, including the unfolded protein response, protein polyubiquitination, proteasome, phosphatidylinositol-3-kinase, and the eukaryotic translation initiation factor 2α. Based on recently published data, we present a model of how these different pathways interplay and how mutations in K13, the main identified resistance marker, may help parasites survive under artemisinin pressure.
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50. Artemisinin and its derivatives in treating helminthic infections beyond schistosomiasis.
50. 青蒿素及其衍生物治疗血吸虫病以外的蠕虫感染PMID:日期:2018-05-01[中文摘要] 世界卫生组织估计，全球有超过15亿人感染土源性蠕虫，而人类食源性吸虫病每年在全球造成约200万生命年因残疾和死亡而损失。迫切需要投入资源用于蠕虫感染的预防、治疗和意识提升，以及发现新的、安全、有效且可负担的抗蠕虫药物。青蒿素（ART）及其衍生物已被广泛用于治疗疟疾和其他原生动物感染；它们也具有抗蠕虫活性。迄今为止，已有许多关于青蒿素及其衍生物抗血吸虫感染的论文被报道和综述。本综述试图总结青蒿素及其衍生物用于治疗除血吸虫属以外的人体和动物蠕虫寄生虫感染的最新进展，包括线虫（犬弓首蛔虫、旋毛虫、捻转血矛线虫、根结线虫属、马铃薯金线虫和标准剑线虫）、绦虫（棘球绦虫属和肥头带绦虫）、吸虫（棘口吸虫属、片形吸虫属、华支睾吸虫、麝猫后睾吸虫、卫氏并殖吸虫、异形异形吸虫和微体同盘吸虫）以及单殖吸虫寄生虫（指环虫和三代虫）。我们得出结论，青蒿素及其衍生物是治疗具有公共卫生意义的多种蠕虫病的潜在有效药物。
[英文摘要] The World Health Organization estimated that more than 1.5 billion people are infected with soil-transmitted helminths globally, and foodborne trematodiases in humans cause ∼2 million life-years lost to disability and death worldwide every year. Investment in prevention, treatment, and awareness of helminth infections and discovery of new, safe, effective, and affordable anti-helminth drugs are urgently needed. Artemisinin (ART) and its derivatives have been widely used to treat malaria and other protozoan infections; they also possess activities against helminths. So far, many papers on ART and its derivatives against schistosomal infections have been reported and reviewed. This review attempts to summarize recent advances in the uses of ART and its derivatives to treat infections of helminth parasites other than Schistosoma spp. in both humans and animals, including nematodes (Toxocara canis, Trichinella spiralis, Haemonchus contortus, Meloidogyne spp., Globodera rostochiensis, and Xiphinema index), cestodes (Echinococcus spp. and Taenia crassiceps), trematodes (Echinostoma spp., Fasciola spp., Clonorchis sinensis, Opisthorchis viverrini, Paragonimus westermani, Heterophyes heterophyes, and Paramphistomum microbothrium), and monogenea parasites (Dactylogyrus and Gyrodactylus). We concluded that ART and its derivatives are potentially effective drugs for treating various helminthic diseases of public health significance.