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Synthesis, characterization and anticancer, antibacterial activities of pentacyclic triterpenoid glycoside derivatives 五环三萜苷衍生物的合成、表征和抗癌、抗菌活性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-09-24 DOI: 10.1080/10286020.2024.2405224
Pan-Pan Wang , Yan-Dan Liu , Lan-Tian Cui , Gao Li , Long-Xuan Zhao , Mei Jin
As a kind of glycoside, pentacyclic triterpenoid saponins have good biological activities, such as anticancer, antibacterial, antiviral and hypoglycemic effects [1]. In this paper, twenty-four pentacyclic triterpenoid derivatives, including twelve monosaccharide derivatives, were designed and synthesized. The anticancer effect and antibacterial activities of all compounds were evaluated. It is noteworthy that compound UA-2b has the strongest inhibitory effect on the growth of A549, Hela and HepG2 cancer cells (IC50 = 5.37 ± 0.22 µM, 5.82 ± 0.25 µM and 5.47 ± 0.06 µM, respectively). Compounds OA-2b, OA-6a, OA-6b, UA-2b and UA-6a have the best activity against Escherichia coli 1924 (MIC = 16 μg/ml).
五环三萜皂苷作为一种苷类化合物,具有良好的生物活性,如抗癌、抗菌、抗病毒、降血糖等作用 [1]。本文设计并合成了二十四种五环三萜类衍生物,其中包括十二种单糖衍生物。对所有化合物的抗癌效果和抗菌活性进行了评估。值得注意的是,化合物 UA-2b 对 A549、Hela 和 HepG2 癌细胞的生长具有最强的抑制作用(IC50 分别为 5.37 ± 0.22 µM、5.82 ± 0.25 µM 和 5.47 ± 0.06 µM)。化合物 OA-2b、OA-6a、OA-6b、UA-2b 和 UA-6a 对大肠杆菌 1924 的活性最好(MIC = 16 μg/ml)。
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引用次数: 0
Rosmarinic acid suppresses the progression of COPD via Syk by modulating airway inflammation and epithelial apoptosis in vivo and in vitro. 迷迭香酸在体内和体外通过调节气道炎症和上皮细胞凋亡,通过 Syk 抑制慢性阻塞性肺病的发展。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-09-23 DOI: 10.1080/10286020.2024.2403617
Ji-Qiao Yuan, Xu-Yu Li, Yan-Nan Fan, Nan Fang, Ping Li, Xin-Zhu Wen, Qi Hou, Zi-Qian Zhang, Ming-Bao Lin

Rosmarinic acid (RosA), a hydrophilic phenolic compound found in various plants, has several biological effects such as anti-inflammatory and anti-apoptosis activities. However, its potential impact on chronic obstructive pulmonary disease (COPD) and its underlying mechanism has not been investigated. In this study, we explored the potential therapeutic effects and mechanism of RosA on COPD airway inflammation and alveolar epithelial apoptosis in vivo and in vitro. Our data suggested that RosA may be a therapeutic candidate for COPD with low toxicity. The corresponding mechanism lies in its anti-inflammatory effect on macrophage and bronchial epithelial cells, as well as protective effect on lung epithelial apoptosis via the jointly cross-target spleen tyrosine kinase (Syk).

迷迭香酸(RosA)是一种存在于多种植物中的亲水性酚类化合物,具有多种生物效应,如抗炎和抗细胞凋亡活性。然而,它对慢性阻塞性肺病(COPD)的潜在影响及其内在机制尚未得到研究。在这项研究中,我们探讨了 RosA 在体内和体外对慢性阻塞性肺病气道炎症和肺泡上皮细胞凋亡的潜在治疗作用及其机制。我们的数据表明,RosA 可能是慢性阻塞性肺病的一种低毒性候选治疗药物。其相应的机制在于它对巨噬细胞和支气管上皮细胞的抗炎作用,以及通过共同的交叉靶标脾酪氨酸激酶(Syk)对肺上皮细胞凋亡的保护作用。
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引用次数: 0
Study on the anti-HBV activity of matrine alkaloids from Oxytropis ochrocephala by MTT, 3d-QSAR, molecular docking and molecular dynamics simulation 通过MTT、3d-QSAR、分子对接和分子动力学模拟研究牛膝草中的马钱子碱的抗HBV活性
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-09-18 DOI: 10.1080/10286020.2024.2402369
Ya-Kun Zhang , Jian-Bo Tong , Jing Tan , Min Yang , Xiao-Yu Xing , Yan-Rong Zeng , Zhan Xue , Cheng-Jian Tan
To elucidate the structure-activity relationship of 17 matrine alkaloids from Oxytropis ochrocephala Bunge, their effect on hepatitis B surface antigen (HBsAg) secretion was studied using the MTT assay. A 3D-QSAR analysis showed a strong correlation between chemical structures and biological activities (q2 = 0.625, r2 = 0.859). Molecular docking and molecular dynamics simulations revealed that hydrogen bonding and hydrophobic interactions with hepatitis B core protein (PDB:5T2P) are key to inhibiting HBsAg secretion, suggesting potential for developing natural anti-hepatitis B drugs.
为了阐明来自 Oxytropis ochrocephala Bunge 的 17 种麻黄碱类生物碱的结构-活性关系,我们使用 MTT 试验研究了它们对乙型肝炎表面抗原(HBsAg)分泌的影响。三维-QSAR 分析表明化学结构与生物活性之间具有很强的相关性(q2 = 0.625,r2 = 0.859)。分子对接和分子动力学模拟显示,与乙型肝炎核心蛋白(PDB:5T2P)的氢键和疏水相互作用是抑制 HBsAg 分泌的关键,这表明该化合物具有开发天然抗乙型肝炎药物的潜力。
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引用次数: 0
Therapeutic potential of Cordyceps sinensis targeting oxidative stress and inflammatory response in the treatment of COPD rats: insights from metabolomics analysis 冬虫夏草针对氧化应激和炎症反应治疗慢性阻塞性肺病大鼠的治疗潜力:代谢组学分析的启示。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-09-17 DOI: 10.1080/10286020.2024.2403611
Ying-Ying Liu , Gai-Jie Dou , Yuan-Can Xiao , Xiao-Yi Chen , Li-Xin Wei , Wen-Bin Zhou
This study aimed to investigate the effects of wild Cordyceps sinensis on chronic obstructive pulmonary disease (COPD) rats through metabolomics approach, combined with biochemical parameters evaluations. Consequently, C. sinensis exhibited regulatory effects on the lung’s metabolic profiles in COPD rats. Treatment with C. sinensis potentially modulated glycerophospholipid metabolism, glutathione metabolism, and tryptophan metabolism, thereby alleviating oxidative stress (by decreasing MDA and GSSG, while increasing SOD and GSH) and inflammatory response (by inhibiting TNF-α, IL-8, and MMP-9) in COPD rats while improving lung tissue damage.
本研究旨在通过代谢组学方法,结合生化参数评估,研究野生冬虫夏草对慢性阻塞性肺病(COPD)大鼠的影响。结果表明,野生冬虫夏草对慢性阻塞性肺病大鼠肺部代谢轮廓有调节作用。使用冬虫夏草可调节甘油磷脂代谢、谷胱甘肽代谢和色氨酸代谢,从而减轻 COPD 大鼠的氧化应激(通过降低 MDA 和 GSSG,同时增加 SOD 和 GSH)和炎症反应(通过抑制 TNF-α、IL-8 和 MMP-9),同时改善肺组织损伤。
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引用次数: 0
Proteomic analysis of two novel peptides from the Odontobuthus doriae scorpion venom 对来自 Odontobuthus doriae 蝎毒的两种新型多肽的蛋白质组分析。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-09-17 DOI: 10.1080/10286020.2024.2403612
Jamil Zargan , Ehsan Jahangirian , Haider A. Khan , Shakir Ali
The venom of the Odontobuthus doriae scorpion, prevalent in East Asia and Iran, has not been fully characterized. This study provides the first proteomic profile of O. doriae venom to explore its potential as a medical. 2D-PAGE analysis revealed 96 protein spots with isoelectric points from 3 to 9 and molecular weights between 6.6 to 205 kDa. Fourteen toxin fractions were isolated via HPLC, and SDS-PAGE showed seven protein bands ranging from 3.8 to 182 kDa. MALDI-TOF MS identified Peptide 1 and Peptide 2, resembling Hemoglobin beta-2 chain and Chaperonin HSP60 and suggest potential therapeutic applications for P1 and P2.
流行于东亚和伊朗的多瑞亚蝎毒尚未完全定性。本研究首次对多利亚蝎毒进行了蛋白质组学分析,以探索其作为药物的潜力。2D-PAGE 分析显示有 96 个蛋白质点,等电点在 3 到 9 之间,分子量在 6.6 到 205 kDa 之间。通过 HPLC 分离出 14 个毒素馏分,SDS-PAGE 显示出 7 条蛋白质带,分子量在 3.8 至 182 kDa 之间。MALDI-TOF MS 鉴定出了肽 1 和肽 2,它们与血红蛋白 beta-2 链和伴侣素 HSP60 相似,并提出了 P1 和 P2 的潜在治疗用途。
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引用次数: 0
Chemical constituents from the endophytic fungus Aspergillus sp. S3 of Hibiscus tiliaceus 木槿内生真菌黑曲霉 S3 的化学成分
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-09-14 DOI: 10.1080/10286020.2024.2399572
Wen-Feng Chen , Meng-Meng Wang , Jing Tian , Bo-Heng Hu , Ya-Nan Lu , Chun-Mei Yang , Han-Qiao Liang , Rui-Zhang Feng
A new sterol, aspersterol E (1), a newly discovered alkaloid, asperginine A (2), and five known compounds (3–7) were obtained from the endophytic fungus Aspergillus sp. S3 of Hibiscus tiliaceus Linn. The compounds were extracted from their fermentation products using silica gel, ODS C18, and semi-preparative HPLC. The structure of each compound was determined through spectroscopic analysis. All the obtained compounds (1–7) were evaluated for their cytotoxic activity against the mouse pre-gastric cancer cell line MFC by using the MTT assay. The IC50 values of compounds 1, 2, 3, and 5 were found to be 153.43 μM, 61.25 μM, 73.19 μM, and 181.69 μM respectively.
从木槿内生真菌 Aspergillus sp. S3 中获得了一种新的甾醇--天冬甾醇 E (1)、一种新发现的生物碱--天冬精氨酸 A (2)和五种已知化合物 (3-7)。
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引用次数: 0
Therapeutic potential of xtr-miR-22-3p from Plastrum testudinis in acute promyelocytic leukemia Plastrum testudinis 中的 xtr-miR-22-3p 对急性早幼粒细胞白血病的治疗潜力
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-08-30 DOI: 10.1080/10286020.2024.2395566
Ming-Yang Chen , Meng Li , Qing-Yi Xu , Shu-Wang Zhang , Guang-Xi Ren , Chun-Sheng Liu
Acute promyelocytic leukemia (APL) is marked by a block at the promyelocyte stage. Treatments like ATRA and ATO face resistance and relapse issues. Plastrum testudinis, a traditional Chinese medicine, may offer therapeutic potential. This study investigated xtr-miR-22-3p from P. testudinis for treating APL. High expression of xtr-miR-22-3p was confirmed, with target prediction indicating interactions with key genes, including PML. xtr-miR-22-3p reduced HL-60 leukemia cell growth, altered the cell cycle, and selectively inhibited HL-60 proliferation while promoting BMSC growth, suggesting its potential as a targeted APL therapy.
急性早幼粒细胞白血病(APL)的特征是早幼粒细胞阶段的阻滞。ATRA和ATO等治疗方法面临耐药性和复发问题。传统中药 "板蓝根 "可用于治疗急性早幼粒细胞白血病(APL)。
{"title":"Therapeutic potential of xtr-miR-22-3p from Plastrum testudinis in acute promyelocytic leukemia","authors":"Ming-Yang Chen ,&nbsp;Meng Li ,&nbsp;Qing-Yi Xu ,&nbsp;Shu-Wang Zhang ,&nbsp;Guang-Xi Ren ,&nbsp;Chun-Sheng Liu","doi":"10.1080/10286020.2024.2395566","DOIUrl":"10.1080/10286020.2024.2395566","url":null,"abstract":"<div><div>Acute promyelocytic leukemia (APL) is marked by a block at the promyelocyte stage. Treatments like ATRA and ATO face resistance and relapse issues. <em>Plastrum testudinis</em>, a traditional Chinese medicine, may offer therapeutic potential. This study investigated xtr-miR-22-3p from <em>P. testudinis</em> for treating APL. High expression of xtr-miR-22-3p was confirmed, with target prediction indicating interactions with key genes, including PML. xtr-miR-22-3p reduced HL-60 leukemia cell growth, altered the cell cycle, and selectively inhibited HL-60 proliferation while promoting BMSC growth, suggesting its potential as a targeted APL therapy.</div></div>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":"27 3","pages":"Pages 387-399"},"PeriodicalIF":1.3,"publicationDate":"2024-08-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142195443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Correlation analysis between potential hepatotoxicity and ingredient content of polygoni multiflori caulis 潜在肝毒性与何首乌成分含量的相关性分析
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-08-17 DOI: 10.1080/10286020.2024.2391472
Ze-Ye Tan , Gui Zhou , Yi-Ming Feng , Nan Xiang , Shan-Ni Li , Rui-Fang Xie , Xin Zhou
Polygoni Multiflori Caulis (PMC) is commonly used in clinical practice. While the adverse reactions of Polygoni Multiflori Radix (RPM) are well-known, the potential adverse reactions of PMC are often neglected. This article aims to clarify the relationship between hepatotoxic components in PMC and its various producing areas. This study provides a qualitative and quantitative analysis of PMC from various regions, which can serve as a basis for safe usage.
何首乌是临床常用药物。虽然何首乌的不良反应众所周知,但其潜在的不良反应却往往被忽视。本文旨在阐明何首乌中的肝毒性成分与其各产区之间的关系。这项研究对不同产区的何首乌进行了定性和定量分析,可作为安全使用何首乌的依据。
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引用次数: 0
Quantitative predictive model for screening optimal processing methods of Polygonati rhizoma 筛选何首乌最佳加工方法的定量预测模型。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-08-16 DOI: 10.1080/10286020.2024.2390496
Shi-Jie Bi , An-Lei Yuan , Zi-Jun Chen , Yue Ren , Kai-Yang Liu , Chao-Qun Liu , Zhen-Zhen Xu , Ze-Wen Wang , Yan-Ling Zhang
Polygonati rhizoma (Huangjing in Chinese) is a common clinical tonic with the traditional effects of tonifying Qi, nourishing Yin. However, the lack of precise control of processing parameters has led to the uneven quality of processed Huangjing. A prediction model using the CRITIC method optimizes processing by correlating method, component contents, and biological activity, ensuring consistent quality and efficacy.
黄精是临床常用的滋补品,具有补气养阴的传统功效。然而,由于缺乏对加工参数的精确控制,导致加工后的黄精质量参差不齐。利用 CRITIC 方法建立的预测模型可通过关联方法、成分含量和生物活性来优化加工过程,从而确保质量和功效的一致性。
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引用次数: 0
Bioactive prenylated c6–c3 derivatives from the roots of Illicium brevistylum 从Illicium brevistylum的根中提取的具有生物活性的前炔基c6-c3衍生物。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-08-14 DOI: 10.1080/10286020.2024.2365437
Three new prenylated C6–C3 compounds (1–3), together with two known prenylated C6–C3 compounds (4–5) and one known C6–C3 derivative (6), were isolated from the roots of Illicium brevistylum A. C. Smith. The structures of 1–3 were elucidated by spectroscopic methods including 1D and 2D NMR, HRESIMS, CD experiments and ECD calculations. The structure of illibrefunone A (1) was confirmed by single-crystal X-ray diffraction analysis. All compounds were evaluated in terms of their anti-inflammatory potential on nitric oxide (NO) generation in lipopolysaccharide-stimulated murine RAW264.7 macrophages and murine BV2 microglial cells, antiviral activity against Coxsackievirus B3 (CVB3) and influenza virus A/Hanfang/359/95 (H3N2). Compounds 3 and 4 exhibited potent inhibitory effects on the production of NO in RAW 264.7 cells with IC50 values of 20.57 and 12.87 μM respectively, which were greater than those of dexamethasone (positive control). Compounds 1 and 4–6 exhibited weak activity against Coxsackievirus B3, with IC50 values ranging from 25.87 to 33.33 μM.
从 Illicium brevistylum A. C. Smith 的根中分离出了三种新的前烯化 C6-C3 化合物(1-3),以及两种已知的前烯化 C6-C3 化合物(4-5)和一种已知的 C6-C3 衍生物(6)。通过光谱方法,包括一维和二维核磁共振、HRESIMS、CD 实验和 ECD 计算,阐明了 1-3 的结构。通过单晶 X 射线衍射分析证实了伊利布酮 A (1) 的结构。评估了所有化合物在脂多糖刺激的小鼠 RAW264.7 巨噬细胞和小鼠 BV2 微神经胶质细胞中产生一氧化氮(NO)的抗炎潜力,以及对柯萨奇病毒 B3(CVB3)和流感病毒 A/HANfang/359/95 (H3N2)的抗病毒活性。化合物 3 和 4 对 RAW 264.7 细胞中 NO 的产生具有强效抑制作用,IC50 值分别为 20.57 和 12.87 μM,高于地塞米松(阳性对照)。化合物 1 和 4-6 对柯萨奇病毒 B3 的活性较弱,IC50 值在 25.87 至 33.33 μM 之间。
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引用次数: 0
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Journal of Asian Natural Products Research
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