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Structures, activities, and putative biosynthetic pathways of characteristic polyphenolic compounds from Morus plants: A review 桑科植物特征多酚化合物的结构、活性和假定生物合成途径:综述。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-21 DOI: 10.1016/j.fitote.2024.106181
Runjie Shi , Shengzhi Liu , Yu Zhao , Wei Zhu , Ping Wang , Jingkui Tian

Morus plants played a pivotal role in ancient Chinese sericulture and silk production, which served as critical components of economy and culture. Besides, many parts of mulberry trees, including roots, leaves, stems, and fruits, hold various medicinal value, and have been utilized in traditional medicine for thousands of years. The chemical composition of mulberry has been reported in many literatures, while the characteristic compounds have not been systematically summarized. In this review, we focused on the polyphenolic compounds in mulberry, including flavonoids, 2-arylbenzofurans, and Diels–Alder (D–A) adducts, and summarized their structural features, structure-activity relationships, and potential biosynthetic pathways. The results revealed a characteristic class of 2′-hydroxylated flavonoids and stilbenes which played an important role in the biosynthesis of downstream 2-arylbenzofurans and D–A adducts in mulberry but had been overlooked by most studies. The prenylated modifications of different compounds were also discussed and their function as precursors of D–A adducts was emphasized. We also describe the effects of different modifications on biological activities. Besides, the chemical composition of Morus was most similar to that of Artocarpus in the Moraceae family in that they had almost identical characteristic compounds. Finally, a putative total biosynthetic pathway of D–A adducts in mulberry was proposed based on structure derivation and combination of verified reactions. This review contributes to the understanding of the biological activity and biosynthesis of the characteristic components of Morus plants.

桑树在中国古代蚕桑和丝绸生产中发挥着举足轻重的作用,是经济和文化的重要组成部分。此外,桑树的许多部分,包括根、叶、茎和果实,都具有不同的药用价值,数千年来一直被用于传统医药中。桑树的化学成分在许多文献中都有报道,但其特征化合物尚未得到系统总结。在这篇综述中,我们重点研究了桑葚中的多酚类化合物,包括黄酮类、2-芳基苯并呋喃类和 Diels-Alder (D-A) 加合物,并总结了它们的结构特征、结构-活性关系和潜在的生物合成途径。研究结果表明,2'-羟基黄酮类化合物和二苯乙烯类化合物在桑树下游 2-芳基苯并呋喃和 D-A 加合物的生物合成过程中发挥着重要作用,但却被大多数研究忽略。我们还讨论了不同化合物的前酰化修饰,并强调了它们作为 D-A 加合物前体的功能。我们还描述了不同修饰对生物活性的影响。此外,桑属植物的化学成分与桑科植物中的蒿属植物最为相似,它们具有几乎相同的特征化合物。最后,根据结构推导和已验证反应的组合,提出了桑树中 D-A 加合物的推定总生物合成途径。本综述有助于了解桑科植物特征成分的生物活性和生物合成。
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引用次数: 0
Therapeutic effect of iridoid and xanthone glycosides components extracted from Swertia Mussotti on calculous cholecystitis and its clinical complications by targeting COX2 从獐牙菜中提取的鸢尾甙和黄酮甙成分通过靶向 COX2 对结石性胆囊炎及其临床并发症的治疗作用
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-21 DOI: 10.1016/j.fitote.2024.106189
Hong-mei Li , Tao Chen , Li-xia Qian , Shuo Wang , Cheng Shen , Liang-cheng Li , Yu-lin Li

Swertia Mussotti is used as febrifuge, analgesic and to treat calculous cholecystitis, however, the underling mechanism remains unclear. This study investigates the therapeutic effect of the active fraction named iridoid and xanthone glycoside (IXG) extracted from S. mussotii on six animal models related to calculous cholecystitis and its complications, and to explore its potential target proteins. Four main compounds including swertiamarin (STR), sweroside (SRS), gentiopicroside (GPS) and mangiferin (MGR) were identified from the IXG by UHPLC-TOF-MS. The in vivo experiments results confirmed that IXG significantly decreased the level of total bilirubin (TBIL), direct bilirubin (DBIL) and cyclooxygenase-2 (COX2) in calculous cholecystitis. IXG treatment dramatically reduced the number of twists and the time of clicking foot in 2nd phase induced by glacial acetic acid and formalin, however, no effect was showed on central pain established by hot plate test. IXG also significantly decreased the anal temperature induced by yeast and 2,4-dinitrophenol. These results indicated that IXG alleviate calculous cholecystitis and its clinical symptom. In addition, IXG suppressed the expression of Prostaglandin E2 (PGE2) in vitro. Mechanistically, COX2 was identified as the direct target of IXG in RAW264.7 cells, and downregulated the protein levels of COX2. The results confirmed that IXG ameliorates calculous cholecystitis and its clinical symptom (pain and fever) by suppressing the production of PGE2 through targeting COX2.

獐牙菜被用作清热解毒、镇痛和治疗结石性胆囊炎的药物,但其基本机制仍不清楚。本研究探讨了从獐牙菜中提取的活性成分鸢尾黄酮苷(IXG)对六种结石性胆囊炎及其并发症相关动物模型的治疗效果,并探索其潜在的靶蛋白。通过 UHPLC-TOF-MS 方法从 IXG 中鉴定出了四种主要化合物,包括獐牙菜苷 (STR)、獐牙菜苷 (SRS)、龙胆草苷 (GPS) 和芒果苷 (MGR)。体内实验结果证实,IXG 能显著降低结石性胆囊炎患者的总胆红素(TBIL)、直接胆红素(DBIL)和环氧化酶-2(COX2)水平。IXG 治疗显著减少了冰醋酸和福尔马林诱导的第二阶段扭转次数和点击脚的时间,但对热板试验确定的中枢性疼痛没有影响。IXG 还能明显降低酵母和 2,4-二硝基苯酚引起的肛门温度。这些结果表明,IXG 可减轻结石性胆囊炎及其临床症状。此外,IXG 还能抑制体外前列腺素 E2(PGE2)的表达。从机理上讲,IXG 在 RAW264.7 细胞中的直接靶点是 COX2,并能降低 COX2 的蛋白水平。结果证实,IXG通过靶向COX2抑制PGE2的产生,从而改善结石性胆囊炎及其临床症状(疼痛和发热)。
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引用次数: 0
Catechin and flavonoid glycosides from the Ulmus genus: Exploring their nutritional pharmacology and therapeutic potential in osteoporosis and inflammatory conditions 榆属植物中的儿茶素和黄酮苷:探索它们在骨质疏松症和炎症方面的营养药理学和治疗潜力。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-15 DOI: 10.1016/j.fitote.2024.106188
Chanhyeok Jeong , Chang Hyung Lee , Jiwon Seo , Jung Han Yoon Park , Ki Won Lee

This review investigates the therapeutic effects of Ulmus species extracts, traditionally used as tea ingredients in East Asia, on bone health and inflammatory conditions. Through the analysis of 9757 studies, narrowing down to 56 pertinent ones, we evaluated the safety and efficacy of Ulmus extracts. The focus was on catechin glycosides (CG) and flavonoid glycosides (FG), key compounds identified for their potential benefits. The research highlights the extracts' role in enhancing bone mineral density (BMD) by stimulating osteoblast activity and suppressing osteoclast differentiation, suggesting a protective effect against osteoporosis. Furthermore, the extracts demonstrated significant anti-inflammatory properties by modulating inflammatory markers and pathways. The findings confirm the historical use of Ulmus extracts in East Asia for health benefits and recommend further exploration into functional foods and nutraceuticals. The review calls for more rigorous research, including clinical trials, to establish optimal use and integration into modern health solutions. It underscores the potential of Ulmus extracts in promoting bone health and managing inflammation, advocating for a bridge between traditional practices and contemporary scientific validation. In conclusion, Ulmus extracts, a material long consumed as tea ingredients in East Asia, exhibit significant potential for improving bone health and reducing inflammation. This review calls for additional research to explore their full therapeutic capabilities, emphasizing the need for optimized extraction methods and clinical trials. It reinforces the importance of bridging traditional knowledge with contemporary scientific approaches to health and dietary solutions, promoting overall wellness.

本综述研究了东亚地区传统上用作茶叶成分的榆树提取物对骨骼健康和炎症的治疗效果。通过分析 9757 项研究,我们筛选出 56 项相关研究,评估了榆树提取物的安全性和有效性。研究的重点是儿茶素苷(CG)和黄酮苷(FG),这两种关键化合物被认为具有潜在功效。研究强调了这些提取物通过刺激成骨细胞活性和抑制破骨细胞分化来提高骨矿物质密度(BMD)的作用,这表明它们对骨质疏松症具有保护作用。此外,这些提取物还通过调节炎症标志物和炎症途径,表现出显著的抗炎特性。研究结果证实了东亚地区历来使用榆树提取物来改善健康状况,并建议进一步探索功能食品和营养保健品。综述呼吁开展更严格的研究,包括临床试验,以确定最佳使用方法并将其融入现代健康解决方案。它强调了榆树提取物在促进骨骼健康和控制炎症方面的潜力,主张在传统做法和现代科学验证之间架起一座桥梁。总之,榆树提取物是一种在东亚地区长期作为茶叶成分食用的材料,在改善骨骼健康和减少炎症方面表现出巨大的潜力。本综述呼吁开展更多研究,探索其全部治疗能力,强调优化提取方法和临床试验的必要性。它强调了将传统知识与现代科学方法相结合,促进整体健康和饮食解决方案的重要性。
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引用次数: 0
Neo-5,10-seco-clerodane diterpenoids from Schnabelia terniflora 从 Schnabelia terniflora 中提取的新-5,10-seco-clerodane 二萜。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-15 DOI: 10.1016/j.fitote.2024.106190
Yi Chen , Xu-Lan Bai , Ting-Ting Du , Hong-Tao Xu , Yong-Li Wang , Le-Yi Huang , Xu-Dong Mao , Gui-Xin Chou

Three new neo-5,10-seco-clerodane diterpenoids (13), four previously undescribed ethoxy/methoxy acetal analogues (47), one new etherified labdane diterpenoid (8), and seven known diterpenoids (915) were isolated from the whole plant of Schnabelia terniflora. Their structures were established on the basis of extensive spectroscopic analysis, single-crystal X-ray diffraction data, calculated electronic circular dichroism (ECD), and Mo2(OAc)4-induced circular dichroism. Compounds 2 and 3 represent the first examples of neo-5,10-seco-clerodane diterpenoids containing a 1H-pyrrole-2,5-dione and a pyrrolidine-2,5-dione moiety, respectively. A plausible biosynthetic pathway for 13 is proposed. All diterpenoids were evaluated for their cytotoxic activity against non-small-cell lung cancer lines (A549 and H460) and gastric cancer lines (HGC27 and AGS). Among them, 2 and 14 showed moderate cytotoxicity against four cell lines.

从 Schnabelia terniflora 的全草中分离出了三种新的新-5,10-seco-clerodane 二萜类化合物(1-3)、四种以前未曾描述过的乙氧基/甲氧基乙缩醛类似物(4-7)、一种新的醚化 labdane 二萜类化合物(8)和七种已知的二萜类化合物(9-15)。根据大量的光谱分析、单晶 X 射线衍射数据、电子圆二色性(ECD)计算和 Mo2(OAc)4 诱导的圆二色性,确定了它们的结构。化合物 2 和 3 代表了分别含有 1H-吡咯-2,5-二酮和吡咯烷-2,5-二酮分子的新-5,10-seco-clerodane 二萜化合物的首个实例。提出了 1-3 的合理生物合成途径。评估了所有二萜类化合物对非小细胞肺癌株(A549 和 H460)和胃癌株(HGC27 和 AGS)的细胞毒活性。其中,2 和 14 对四种细胞株具有中等程度的细胞毒性。
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引用次数: 0
Total flavonoids from the aerial parts of Tetrastigma hemsleyanum prevent LPS-induced ALI by modulating the TLR4/NF-κB pathway in mice Tetrastigma hemsleyanum气生部分中的总黄酮类化合物通过调节小鼠的TLR4/NF-κB途径,预防LPS诱发的急性呼吸道感染。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-15 DOI: 10.1016/j.fitote.2024.106175
Jiheng Feng, Chenjun Shen, Shasha Tian, Xingcan Chen, Fangmei Zhou, Mingyuan Zhou, Bingqi Zhu, Xiaoyan Li, Zhishan Ding

Background

The traditional Chinese medicine Tetrastigma Hemsleyanum (TH) is employed in treating respiratory diseases; however, the aerial parts by which its total flavonoids alleviate acute lung injury (ALI) are still unknown. This study investigated the protective effect and mechanism of Tetrastigma Hemsleyanum flavonoids (THF) in lipopolysaccharide (LPS)-induced ALI in mice.

Methods

Firstly, the total flavonoids from the above-ground part of TH were extracted. Subsequently, the composition of THF was analyzed using LC-MS. In vivo, the impact of THF on ALI mice was assessed through lung histopathology and the evaluation of various inflammatory factors' expression in mice. After treating RAW264.7 cells with THF in vitro, changes in inflammatory markers were examined upon LPS stimulation, and mRNA expression levels of inflammatory factors were detected using RT-qPCR. Finally, Western blot analysis was performed to determine TLR4/NF-κB pathway-associated proteins expression.

Results

In summary, a total of 24 flavonoids have been identified in THF. In vivo and vitro results show that THF effectively reduces the damage caused by LPS inflammation by blocking the expression and release of inflammatory factors. THF alleviates inflammatory injury by modulating the TLR4/NF-KB pathway.

Conclusion

The results suggest that flavonoids exhibit a potent anti-inflammatory effect and effectively mitigate LPS-induced injury both in vivo and in vitro. We suggested that these flavonoids exert their therapeutic effects by modulating the TLR4/NF-KB pathway. In conclusion, the development of THF is anticipated to represent a promising new pharmaceutical for treatingALI.

背景:传统中药四逆散(Tetrastigma Hemsleyanum,TH)可用于治疗呼吸系统疾病,但其总黄酮类化合物可缓解急性肺损伤(ALI)的气生部位尚不清楚。本研究探讨了Tetrastigma Hemsleyanum黄酮(THF)对脂多糖(LPS)诱导的小鼠ALI的保护作用及其机制:方法:首先,提取TH地上部分的总黄酮。方法:首先提取 TH 地上部分的总黄酮类化合物,然后用 LC-MS 分析 THF 的成分。在体内,通过肺组织病理学和小鼠体内各种炎症因子的表达评估 THF 对 ALI 小鼠的影响。在体外用 THF 处理 RAW264.7 细胞后,检测 LPS 刺激下炎症标志物的变化,并使用 RT-qPCR 检测炎症因子的 mRNA 表达水平。最后,进行 Western 印迹分析以确定 TLR4/NF-κB 通路相关蛋白的表达:总之,在 THF 中总共鉴定出了 24 种黄酮类化合物。体内和体外实验结果表明,THF 通过阻断炎症因子的表达和释放,有效减轻了 LPS 炎症造成的损伤。THF 通过调节 TLR4/NF-KB 通路减轻炎症损伤:结果表明,类黄酮具有强大的抗炎作用,能有效减轻 LPS 在体内和体外诱发的损伤。我们认为这些类黄酮通过调节TLR4/NF-KB途径发挥治疗作用。总之,THF 的开发有望成为一种治疗急性淋巴细胞白血病的新型药物。
{"title":"Total flavonoids from the aerial parts of Tetrastigma hemsleyanum prevent LPS-induced ALI by modulating the TLR4/NF-κB pathway in mice","authors":"Jiheng Feng,&nbsp;Chenjun Shen,&nbsp;Shasha Tian,&nbsp;Xingcan Chen,&nbsp;Fangmei Zhou,&nbsp;Mingyuan Zhou,&nbsp;Bingqi Zhu,&nbsp;Xiaoyan Li,&nbsp;Zhishan Ding","doi":"10.1016/j.fitote.2024.106175","DOIUrl":"10.1016/j.fitote.2024.106175","url":null,"abstract":"<div><h3>Background</h3><p>The traditional Chinese medicine <em>Tetrastigma Hemsleyanum</em> (TH) is employed in treating respiratory diseases; however, the aerial parts by which its total flavonoids alleviate acute lung injury (ALI) are still unknown. This study investigated the protective effect and mechanism of Tetrastigma Hemsleyanum flavonoids (THF) in lipopolysaccharide (LPS)-induced ALI in mice.</p></div><div><h3>Methods</h3><p>Firstly, the total flavonoids from the above-ground part of TH were extracted. Subsequently, the composition of THF was analyzed using LC-MS. In vivo, the impact of THF on ALI mice was assessed through lung histopathology and the evaluation of various inflammatory factors' expression in mice. After treating RAW264.7 cells with THF in vitro, changes in inflammatory markers were examined upon LPS stimulation, and mRNA expression levels of inflammatory factors were detected using RT-qPCR. Finally, Western blot analysis was performed to determine TLR4/NF-κB pathway-associated proteins expression.</p></div><div><h3>Results</h3><p>In summary, a total of 24 flavonoids have been identified in THF. In vivo and vitro results show that THF effectively reduces the damage caused by LPS inflammation by blocking the expression and release of inflammatory factors. THF alleviates inflammatory injury by modulating the TLR4/NF-KB pathway.</p></div><div><h3>Conclusion</h3><p>The results suggest that flavonoids exhibit a potent anti-inflammatory effect and effectively mitigate LPS-induced injury both in vivo and in vitro. We suggested that these flavonoids exert their therapeutic effects by modulating the TLR4/NF-KB pathway. In conclusion, the development of THF is anticipated to represent a promising new pharmaceutical for treatingALI.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"178 ","pages":"Article 106175"},"PeriodicalIF":2.5,"publicationDate":"2024-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141995606","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
Exploring the chemistry, biological effects, and mechanism insights of natural coumaroyltyramine: First report 探索天然香豆酰酪胺的化学、生物效应和机理:首次报告。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-15 DOI: 10.1016/j.fitote.2024.106182
Saad Bakrim , Youssef Elouafy , Jihane Touhtouh , Tarik Aanniz , Kawtar El Kadri , Asaad Khalid , Shereen Fawzy , M. Ahmed Mesaik , Learn-Han Lee , Imane Chamkhi , Abdelhakim Bouyahya
<div><p>Today, pharmaceutical drugs have been shown to have serious side effects, while the bioactive components of botanical plants are proven to be effective in the treatment of several diseases marked by enhanced oxidative stress and mild inflammation, often associated with minimal adverse events. Coumaroyltyramine, designated by various nomenclatures such as paprazine, <em>N-p-</em>trans-coumaroyltyramine, <em>p</em>-coumaroyltyramine and <em>N-p-</em>coumaroyltyramine, could be a promising bioactive ingredient to address health issues thanks to its powerful anti-inflammatory and antioxidant effects. This review represents the first in-depth analysis of coumaroyltyramine, an intriguing phenylpropanoid substance found in many species of plants. In fact, an in-depth examination of coumaroyltyramine's biological characteristics, chemical attributes, and synthesis process has been undertaken. All previous research relating to the discovery, extraction, biosynthesis, and characterization of the biologically and pharmacologically active properties of coumaroyltyramine has been reviewed and taken into consideration in this analysis. All articles published in a peer-reviewed English-language journal were examined between the initial compilations of the appropriate database until February 12, 2024. A variety of phytochemicals revealed that coumaroyltyramine is a neutral amide of hydroxycinnamic acid that tends to concentrate in plants as a reaction against infection caused by pathogens and is extracted from several medicinal herbs such as <em>Cannabis sativa</em>, <em>Solanum melongena</em>, <em>Allium bakeri</em>, <em>Annona cherimola</em>, <em>Polygonatum zanlanscianense, and Lycopersicon esculentum</em>. Thanks to its effectiveness in suppressing the effect of the enzyme α-glucosidase, coumaroltyramine has demonstrated antihyperglycemic activity and could have an impact on diabetes and metabolic disorders. It has considerable anti-inflammatory and antioxidant effects. These results were obtained through biological and pharmacological studies <em>in silico, in vivo</em>, and <em>in vitro</em>. In addition, coumaroyltyramine has demonstrated hypocholesterolemic and neuroprotective benefits, thereby diminishing heart and vascular disease incidence and helping to prevent neurological disorders. Other interesting properties of coumaroltyramine include anticancer, antibacterial, anti-urease, antifungal, antiviral, and antidysmenorrheal activities. Targeted pathways encompass activity at different molecular levels, notably through induction of endoplasmic reticulum stress-dependent apoptosis, arrest of the cell cycle, and inhibition of the growth of cancer cells, survival, and proliferation. Although the findings from <em>in silico</em>, <em>in vivo,</em> and <em>in vitro</em> experiments illustrate coumaroyltyramine's properties and modes of action, further research is needed to fully exploit its therapeutic potential. To improve our understanding of the
如今,药物已被证明具有严重的副作用,而植物中的生物活性成分已被证明可有效治疗多种以氧化应激增强和轻度炎症为特征的疾病,而且通常不良反应极少。香豆酰酪胺有多种命名方法,如木瓜碱、N-对反式香豆酰酪胺、对香豆酰酪胺和 N-对香豆酰酪胺,由于其强大的抗炎和抗氧化作用,它可能是一种很有希望解决健康问题的生物活性成分。本综述是对香豆酰酪胺的首次深入分析,香豆酰酪胺是一种存在于多种植物中的有趣的苯丙氨类物质。事实上,我们对香豆酰酪氨酸的生物特性、化学属性和合成过程进行了深入研究。本分析报告回顾并考虑了以往所有与香豆酰酪氨酸的发现、提取、生物合成以及生物和药理活性特征有关的研究。从相关数据库的最初汇编到 2024 年 2 月 12 日,在同行评审的英文期刊上发表的所有文章都进行了研究。从多种植物化学物质中发现,香豆酰酪胺是羟基肉桂酸的一种中性酰胺,它往往集中在植物中,对病原体引起的感染产生反应,可从多种药材中提取,如大麻、茄属植物、薤白、樱桃葵、蓼属植物和茄属植物。由于香豆素能有效抑制α-葡萄糖苷酶的作用,因此它具有抗高血糖活性,可对糖尿病和代谢紊乱产生影响。它还具有相当大的抗炎和抗氧化作用。这些结果是通过在硅学、体内和体外进行生物学和药理学研究得出的。此外,香豆酰酪胺还具有降低胆固醇和保护神经的功效,从而降低心脏和血管疾病的发病率,并有助于预防神经系统疾病。香豆酰酪胺的其他有趣特性还包括抗癌、抗菌、抗尿毒症、抗真菌、抗病毒和抗痛经活性。靶向途径包括不同分子水平的活性,特别是通过诱导内质网应激依赖性凋亡、细胞周期停滞、抑制癌细胞生长、存活和增殖。尽管来自硅学、体内和体外实验的研究结果说明了香豆酰酪胺的特性和作用模式,但要充分挖掘其治疗潜力还需要进一步的研究。为了更好地了解该化合物的药效学效应和药代动力学途径,首先应开展大规模研究。要确定香豆酰酪胺在临床上是否安全有效,还需要在临床和毒理学领域开展进一步研究。即将开展的这项研究对于实现该物质作为天然药物的整体功效及其与其他药物的潜在协同作用至关重要。
{"title":"Exploring the chemistry, biological effects, and mechanism insights of natural coumaroyltyramine: First report","authors":"Saad Bakrim ,&nbsp;Youssef Elouafy ,&nbsp;Jihane Touhtouh ,&nbsp;Tarik Aanniz ,&nbsp;Kawtar El Kadri ,&nbsp;Asaad Khalid ,&nbsp;Shereen Fawzy ,&nbsp;M. Ahmed Mesaik ,&nbsp;Learn-Han Lee ,&nbsp;Imane Chamkhi ,&nbsp;Abdelhakim Bouyahya","doi":"10.1016/j.fitote.2024.106182","DOIUrl":"10.1016/j.fitote.2024.106182","url":null,"abstract":"&lt;div&gt;&lt;p&gt;Today, pharmaceutical drugs have been shown to have serious side effects, while the bioactive components of botanical plants are proven to be effective in the treatment of several diseases marked by enhanced oxidative stress and mild inflammation, often associated with minimal adverse events. Coumaroyltyramine, designated by various nomenclatures such as paprazine, &lt;em&gt;N-p-&lt;/em&gt;trans-coumaroyltyramine, &lt;em&gt;p&lt;/em&gt;-coumaroyltyramine and &lt;em&gt;N-p-&lt;/em&gt;coumaroyltyramine, could be a promising bioactive ingredient to address health issues thanks to its powerful anti-inflammatory and antioxidant effects. This review represents the first in-depth analysis of coumaroyltyramine, an intriguing phenylpropanoid substance found in many species of plants. In fact, an in-depth examination of coumaroyltyramine's biological characteristics, chemical attributes, and synthesis process has been undertaken. All previous research relating to the discovery, extraction, biosynthesis, and characterization of the biologically and pharmacologically active properties of coumaroyltyramine has been reviewed and taken into consideration in this analysis. All articles published in a peer-reviewed English-language journal were examined between the initial compilations of the appropriate database until February 12, 2024. A variety of phytochemicals revealed that coumaroyltyramine is a neutral amide of hydroxycinnamic acid that tends to concentrate in plants as a reaction against infection caused by pathogens and is extracted from several medicinal herbs such as &lt;em&gt;Cannabis sativa&lt;/em&gt;, &lt;em&gt;Solanum melongena&lt;/em&gt;, &lt;em&gt;Allium bakeri&lt;/em&gt;, &lt;em&gt;Annona cherimola&lt;/em&gt;, &lt;em&gt;Polygonatum zanlanscianense, and Lycopersicon esculentum&lt;/em&gt;. Thanks to its effectiveness in suppressing the effect of the enzyme α-glucosidase, coumaroltyramine has demonstrated antihyperglycemic activity and could have an impact on diabetes and metabolic disorders. It has considerable anti-inflammatory and antioxidant effects. These results were obtained through biological and pharmacological studies &lt;em&gt;in silico, in vivo&lt;/em&gt;, and &lt;em&gt;in vitro&lt;/em&gt;. In addition, coumaroyltyramine has demonstrated hypocholesterolemic and neuroprotective benefits, thereby diminishing heart and vascular disease incidence and helping to prevent neurological disorders. Other interesting properties of coumaroltyramine include anticancer, antibacterial, anti-urease, antifungal, antiviral, and antidysmenorrheal activities. Targeted pathways encompass activity at different molecular levels, notably through induction of endoplasmic reticulum stress-dependent apoptosis, arrest of the cell cycle, and inhibition of the growth of cancer cells, survival, and proliferation. Although the findings from &lt;em&gt;in silico&lt;/em&gt;, &lt;em&gt;in vivo,&lt;/em&gt; and &lt;em&gt;in vitro&lt;/em&gt; experiments illustrate coumaroyltyramine's properties and modes of action, further research is needed to fully exploit its therapeutic potential. To improve our understanding of the","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"178 ","pages":"Article 106182"},"PeriodicalIF":2.5,"publicationDate":"2024-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141995603","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
The multiple mechanisms and therapeutic significance of rutin in metabolic dysfunction-associated fatty liver disease (MAFLD) 芦丁在代谢功能障碍相关性脂肪肝(MAFLD)中的多重机制和治疗意义。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-15 DOI: 10.1016/j.fitote.2024.106178
Qianzhuo Wang , Yingjuan Zhang , Ruiling Lu , Qingwen Zhao , Yue Gao

The global incidence of metabolic dysfunction-associated fatty liver disease (MAFLD) has been steadily increasing, making it a leading chronic liver disease. MAFLD refers to a metabolic syndrome linked with type 2 diabetes mellitus, obesity. However, its pathophysiology is complex, there are currently no effective and approved medicines for therapy. Rutin, a naturally occurring polyphenolic flavonoid, is widely distributed in fruits, vegetables, and other plants. It exhibits a plethora of bioactive properties, such as antioxidant, anticancer, and anti-inflammatory and neuroprotective activities, making it an extremely promising phytochemical. Rutin has shown great potential in the treatment of a wide variety of metabolic diseases and received considerable attention in recent years. Fortuitously, various research studies have validated rutin's extensive biological functions in treating metabolic disorders. Despite the fact that the exact pathophysiological mechanisms through which rutin has a hepatoprotective effect on MAFLD are still not fully elucidated. This review comprehensively outlines rutin's multifaceted preventive and therapeutic effects in MAFLD, including the modulation of lipid metabolism, reduction of insulin resistance, diminution of inflammation and oxidative stress, combatting of obesity, and influence on intestinal flora. This paper details the known molecular targets and pathways of rutin in MAFLD pathogenesis. It endeavored to provide new ideas for treating MAFLD and accelerating its translation from bench to bedside.

代谢功能障碍相关性脂肪肝(MAFLD)的全球发病率一直在稳步上升,已成为一种主要的慢性肝病。代谢功能障碍相关性脂肪肝是一种与 2 型糖尿病、肥胖症相关的代谢综合征。然而,它的病理生理学十分复杂,目前还没有有效的、获得批准的药物可用于治疗。芦丁是一种天然多酚类黄酮,广泛分布于水果、蔬菜和其他植物中。它具有抗氧化、抗癌、抗炎和神经保护等多种生物活性,是一种极具潜力的植物化学物质。芦丁在治疗各种代谢性疾病方面显示出巨大潜力,近年来受到广泛关注。幸运的是,各种研究已经验证了芦丁在治疗代谢紊乱方面的广泛生物功能。尽管芦丁对 MAFLD 具有保肝作用的确切病理生理机制仍未完全阐明。本综述全面概述了芦丁对 MAFLD 的多方面预防和治疗作用,包括调节脂质代谢、降低胰岛素抵抗、减轻炎症和氧化应激、防治肥胖以及影响肠道菌群。本文详细介绍了芦丁在 MAFLD 发病机制中的已知分子靶点和途径。它致力于为治疗 MAFLD 提供新思路,并加速其从实验室到临床的转化。
{"title":"The multiple mechanisms and therapeutic significance of rutin in metabolic dysfunction-associated fatty liver disease (MAFLD)","authors":"Qianzhuo Wang ,&nbsp;Yingjuan Zhang ,&nbsp;Ruiling Lu ,&nbsp;Qingwen Zhao ,&nbsp;Yue Gao","doi":"10.1016/j.fitote.2024.106178","DOIUrl":"10.1016/j.fitote.2024.106178","url":null,"abstract":"<div><p>The global incidence of metabolic dysfunction-associated fatty liver disease (MAFLD) has been steadily increasing, making it a leading chronic liver disease. MAFLD refers to a metabolic syndrome linked with type 2 diabetes mellitus, obesity. However, its pathophysiology is complex, there are currently no effective and approved medicines for therapy. Rutin, a naturally occurring polyphenolic flavonoid, is widely distributed in fruits, vegetables, and other plants. It exhibits a plethora of bioactive properties, such as antioxidant, anticancer, and anti-inflammatory and neuroprotective activities, making it an extremely promising phytochemical. Rutin has shown great potential in the treatment of a wide variety of metabolic diseases and received considerable attention in recent years. Fortuitously, various research studies have validated rutin's extensive biological functions in treating metabolic disorders. Despite the fact that the exact pathophysiological mechanisms through which rutin has a hepatoprotective effect on MAFLD are still not fully elucidated. This review comprehensively outlines rutin's multifaceted preventive and therapeutic effects in MAFLD, including the modulation of lipid metabolism, reduction of insulin resistance, diminution of inflammation and oxidative stress, combatting of obesity, and influence on intestinal flora. This paper details the known molecular targets and pathways of rutin in MAFLD pathogenesis. It endeavored to provide new ideas for treating MAFLD and accelerating its translation from bench to bedside.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"178 ","pages":"Article 106178"},"PeriodicalIF":2.5,"publicationDate":"2024-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141995605","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
Linderangolides A−D, four new butanolides from the roots of Lindera angustifolia and their cytotoxic activity Linderangolides a - D,Lindera angustifolia根部的四种新丁醇内酯及其细胞毒性活性。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-14 DOI: 10.1016/j.fitote.2024.106180
Jieqin Wei , Jiaqi Guo , Qi Shi , Yiwen Wang , Manjia Zhou , Hangjie Ren , Runchao Ma , Jiani Ying , Xiongyu Meng , Lupin Qin , Huaqiang Li

Four undescribed butanolides, linderangolides A–D (14), along with four known congeners, lincomolide A (5), (−)-epilitsenolide C2 (6), (−)-epilitsenolide C1 (7) and litseakolide H (8), were isolated from the roots of Lindera angustifolia. The planar structures of 14 were elucidated based on extensive spectroscopic analyses, the relative and absolute configurations of 14 were determined by the NOESY spectra and the comparison of calculated and experimental ECD. The cytotoxic activities of all isolated compounds were tested, 4 showed inhibitory activity against SGC-7 cells with IC50 value of 6.62 μM.

从 Lindera angustifolia 的根中分离出了四种未曾描述过的丁内酯,即 linderangolides A-D (1-4),以及四种已知的同系物,即 lincomolide A (5)、(-)-epilitsenolide C2 (6)、(-)-epilitsenolide C1 (7) 和 litseakolide H (8)。通过大量的光谱分析阐明了 1-4 的平面结构,并通过 NOESY 光谱和计算与实验 ECD 的比较确定了 1-4 的相对和绝对构型。测试了所有分离化合物的细胞毒活性,其中 4 号化合物对 SGC-7 细胞具有抑制活性,IC50 值为 6.62 μM。
{"title":"Linderangolides A−D, four new butanolides from the roots of Lindera angustifolia and their cytotoxic activity","authors":"Jieqin Wei ,&nbsp;Jiaqi Guo ,&nbsp;Qi Shi ,&nbsp;Yiwen Wang ,&nbsp;Manjia Zhou ,&nbsp;Hangjie Ren ,&nbsp;Runchao Ma ,&nbsp;Jiani Ying ,&nbsp;Xiongyu Meng ,&nbsp;Lupin Qin ,&nbsp;Huaqiang Li","doi":"10.1016/j.fitote.2024.106180","DOIUrl":"10.1016/j.fitote.2024.106180","url":null,"abstract":"<div><p>Four undescribed butanolides, linderangolides A–D (<strong>1</strong>–<strong>4</strong>), along with four known congeners, lincomolide A (<strong>5</strong>), (−)-epilitsenolide C2 (<strong>6</strong>), (−)-epilitsenolide C1 (<strong>7</strong>) and litseakolide H (<strong>8</strong>), were isolated from the roots of <em>Lindera angustifolia</em>. The planar structures of <strong>1</strong>–<strong>4</strong> were elucidated based on extensive spectroscopic analyses, the relative and absolute configurations of <strong>1</strong>–<strong>4</strong> were determined by the NOESY spectra and the comparison of calculated and experimental ECD. The cytotoxic activities of all isolated compounds were tested, <strong>4</strong> showed inhibitory activity against SGC-7 cells with IC<sub>50</sub> value of 6.62 μM.</p></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"178 ","pages":"Article 106180"},"PeriodicalIF":2.5,"publicationDate":"2024-08-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141916484","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
Annonaceae acetogenins: A potential treatment for gynecological and breast cancer 茴香属植物苷元:治疗妇科和乳腺癌的潜在方法。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-13 DOI: 10.1016/j.fitote.2024.106187
Diego A. Bravo-Alfaro , Efigenia Montalvo-González , J. Martin Zapien-Macias , Jessica M. Sampieri-Moran , Hugo S. García , Gabriel Luna-Bárcenas

Breast and gynecological cancers are major health concerns due to their increasing incidence rates, and in some cases, their low survival probability. In recent years, multiple compounds of natural origin have been analyzed as alternative treatments for this disease. For instance, Acetogenins are plant secondary metabolites from the Annonaceae family, and its potential anticancer activity has been reported against a wide range of cancer cells both in vitro and in vivo. Several studies have demonstrated promising results of Acetogenins' antitumor capacity, given their selective activity of cellular inhibition at low concentrations. This review outlines the origin, structure, and antineoplastic activities in vitro and in vivo of Acetogenins from Annonaceae against breast cancer and gynecological cancers reported to date. Here, we also provide a systematic summary of the activity and possible mechanisms of action of Acetogenins against these types of cancer and provide references for developing future therapies based on Acetogenins and nanotechnologies.

由于乳腺癌和妇科癌症的发病率越来越高,而且在某些情况下,其存活率很低,因此成为人们关注的主要健康问题。近年来,人们对多种天然化合物进行了分析,将其作为治疗这种疾病的替代方法。例如,乙酰苷元是来自芒柄花科的植物次生代谢物,据报道,它在体外和体内对多种癌细胞都具有潜在的抗癌活性。鉴于乙酰皂苷能在低浓度下对细胞产生选择性抑制作用,多项研究表明乙酰皂苷具有良好的抗肿瘤能力。本综述概述了迄今为止所报道的来自芒萁科植物的乙酰皂苷元的来源、结构以及在体外和体内对乳腺癌和妇科癌症的抗肿瘤活性。在此,我们还系统地总结了乙酰皂苷元对这些类型癌症的活性和可能的作用机制,并为开发基于乙酰皂苷元和纳米技术的未来疗法提供了参考。
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引用次数: 0
Hepatoprotective dibenzocyclooctadiene lignans from the fruits of Kadsura coccinea 从 Kadsura coccinea 果实中提取的具有肝脏保护作用的二苯并环辛二烯木酚素。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-12 DOI: 10.1016/j.fitote.2024.106184
Wenming Wu , Jian Liu , Hanli Ruan , An Jin

The phytochemical investigations on the fruits of Kadsura coccinea led to the isolation of six undescribed dibenzocyclooctadiene lignans named kadcolignans B-G, together with eleven previously described analogues. The structures of these compounds were established by spectroscopic methods including NMR, HRESIMS, and CD experiments. All isolated compounds were evaluated for their hepatoprotective activity by measuring the levels of triglyceride (TG), total cholesterol (TC), and reactive oxygen species (ROS) in FFA-induced HepG2 cells. As a result, compounds 4, 5, 9, 13, and 15 showed potent inhibitory effects on hepatocyte lipid accumulation at a concentration of 100 μM. Our research not only broadens the understanding on the chemical composition of K. coccinea but also provides experimental and theoretical evidences supporting the fruit's active ingredients in alleviating nonalcoholic fatty liver disease (NAFLD).

通过对 Kadsura coccinea 果实进行植物化学研究,分离出了六种未曾描述过的二苯并环辛二烯木酚素,命名为 Kadcolignans B-G,以及十一种之前描述过的类似物。通过 NMR、HRESIMS 和 CD 实验等光谱方法确定了这些化合物的结构。通过测量脂肪酸诱导的 HepG2 细胞中甘油三酯(TG)、总胆固醇(TC)和活性氧(ROS)的水平,评估了所有分离化合物的保肝活性。结果表明,在 100 μM 浓度下,化合物 4、5、9、13 和 15 对肝细胞脂质积累有很强的抑制作用。我们的研究不仅拓宽了人们对 K. coccinea 化学成分的认识,还提供了实验和理论证据,支持该果实的活性成分在缓解非酒精性脂肪肝(NAFLD)方面的作用。
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引用次数: 0
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Fitoterapia
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