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Cytotoxic, antioxidant, and enzyme inhibitory activities of Centaurea stapfiana extracts and their HPLC-ESI-QTOF-MS profiles: Insights into an unexplored Centaurea species 半枝莲提取物的细胞毒性、抗氧化性和酶抑制活性及其 HPLC-ESI-QTOF-MS 图谱:洞察一种尚未开发的半枝莲物种
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-09-08 DOI: 10.1016/j.fitote.2024.106207
Gokhan Zengin , Álvaro Fernández-Ochoa , María de la Luz Cádiz-Gurrea , Francisco-Javier Leyva Jiménez , Abdullahi Ibrahim Uba , Gunes Ak , Sanam Iram Soomro , Maruf Balos , Ugur Cakilcioglu , Maria João Rodrigues , Catarina G. Pereira , Luísa Custódio

The members of the genus Centaurea have a great interest in pharmaceutical and nutraceutical fields due to their biological potential. Based on this information, we aimed to evaluate the biological properties (antioxidant, enzyme inhibition and cytotoxicity) and chemical profile of the extract of Centaurea stapfiana, an unstudied species. The highest total phenolic content was found in the ethanol/water extract with 32.17 mg GAE/g. A total of 102 of them were identified by HPLC-ESI-QTOF-MS analysis. These compounds were mainly hydroxybenzoic acid and hydroxycinnamic acid as well as flavonoids. In the antioxidant tests, the ethanol/water extract had the best free radical scavenging and reducing ability. However, in the enzyme inhibition test, the ethanol extract was the most active. The extracts were also tested on two tumour cell lines (RAW 264.7 and HepG2) and one non-tumour cell line (S17). The ethanol extract showed the promising effect on HepG2 (cell viability: 28.6 % at 50 g/ml). Furthermore, we examined the interactions between the compounds and enzymatic and cellular targets. A good interaction was found between quercetin-3-xylosyl-(1- > 6)-glucoside and iNOS. In summary, our results suggest that C. stapfiana can be considered as a versatile raw material for the development of health-promoting applications in the pharmaceutical and cosmeceutical fields.

矢车菊属植物因其生物潜力而在制药和保健品领域备受关注。基于这些信息,我们旨在评估一种未研究物种--矢车菊(Centaurea stapfiana)提取物的生物特性(抗氧化、酶抑制和细胞毒性)和化学特征。乙醇/水提取物中的总酚含量最高,为 32.17 毫克 GAE/克。通过 HPLC-ESI-QTOF-MS 分析,共鉴定出 102 种酚类化合物。这些化合物主要是羟基苯甲酸、羟基肉桂酸和黄酮类化合物。在抗氧化试验中,乙醇/水提取物的自由基清除和还原能力最强。不过,在酶抑制试验中,乙醇提取物的活性最高。提取物还在两种肿瘤细胞系(RAW 264.7 和 HepG2)和一种非肿瘤细胞系(S17)上进行了测试。乙醇提取物显示出对 HepG2 的良好效果(细胞存活率:50 克/毫升时为 28.6%)。此外,我们还研究了化合物与酶和细胞靶标之间的相互作用。结果发现,槲皮素-3-木糖基-(1- > 6)-葡萄糖苷与 iNOS 之间存在良好的相互作用。总之,我们的研究结果表明,C. stapfiana 可被视为一种多功能原料,用于开发医药和化妆品领域中促进健康的应用。
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引用次数: 0
Sleep-improving effect and the potential mechanism of Morus alba L. on mice 桑叶对小鼠的睡眠改善作用及其潜在机制
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-09-08 DOI: 10.1016/j.fitote.2024.106205
Xiaoran Kong , Xiaolu Zhou , Rui Li , Qiaozhen Kang , Limin Hao , Jiaqing Zhu , Jike Lu

As insufficient sleep has become a widespread concern in modern society, potential sleep-improving effect of mulberry (Morus alba L.) leaf ethanol extract (MLE) and the related mechanism were investigated in the present study. According to the results, MLE could significantly shorten sleep latency by 33 %, extend sleep duration by 56 % and increase sleep ratio of mice through increasing 5-HT and GABA release in serum, hypothalamus and hippocampus. Metabonomic analysis showed that phenylalanine metabolism, arginine and proline metabolism might be the potential pathways of MLE to improve sleep. Network pharmacological and LC-MS analysis suggested that the key sleep-improving active ingredients in MLE might be luteolin, kaempferol, naringenin, morin, stigmasterol and β-sitosterol. Further molecular docking and qRT-PCR results demonstrated that the key targets for MLE to improve sleep might be MAOA, GABRA1 and GABRA2. In conclusion, MLE showed outstanding sleep-improving effect and great potential for the application as novel sleep-improving functional food.

由于睡眠不足已成为现代社会普遍关注的问题,本研究探讨了桑叶乙醇提取物(MLE)潜在的改善睡眠作用及其相关机制。结果表明,桑叶乙醇提取物能通过增加小鼠血清、下丘脑和海马中5-羟色胺和GABA的释放,使小鼠的睡眠潜伏期明显缩短33%,睡眠持续时间延长56%,睡眠比率增加。代谢分析表明,苯丙氨酸代谢、精氨酸和脯氨酸代谢可能是 MLE 改善睡眠的潜在途径。网络药理学和LC-MS分析表明,MLE中改善睡眠的主要活性成分可能是木犀草素、山奈酚、柚皮苷、吗啉、豆甾醇和β-谷甾醇。进一步的分子对接和 qRT-PCR 结果表明,MLE 改善睡眠的关键靶点可能是 MAOA、GABRA1 和 GABRA2。总之,MLE 表现出了突出的改善睡眠效果,在作为新型改善睡眠功能食品方面具有巨大的应用潜力。
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引用次数: 0
Comprehensive review of Hesperetin: Advancements in pharmacokinetics, pharmacological effects, and novel formulations 全面回顾橙皮甙:药代动力学、药理作用和新型制剂方面的进展
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-09-08 DOI: 10.1016/j.fitote.2024.106206
Bocui Song , Meihan Hao , Shuang Zhang , Wenqi Niu , Yuqi Li , Qian Chen , Shuang Li , Chunyu Tong

Hesperetin is a flavonoid compound naturally occurring in the peel of Citrus fruits from the Rutaceae family. Previous studies have demonstrated that hesperetin exhibits various pharmacological effects, such as anti-inflammatory, anti-tumor, antioxidative, anti-aging, and neuroprotective properties. In recent years, with the increasing prevalence of diseases and the rising awareness of traditional Chinese medicine, hesperetin has garnered growing attention for its wide-ranging pharmacological effects. To substantiate its health benefits and elucidate potential mechanisms, knowledge of pharmacokinetics is crucial. However, the limited solubility of hesperetin restricts its bioavailability, thereby diminishing its efficacy as a beneficial health agent. To enhance the bioavailability of hesperetin, various novel formulations have been developed, including nanoparticles, liposomes, and cyclodextrin inclusion complexes. This article reviews recent advances in the pharmacokinetics of hesperetin and methods to improve its bioavailability, as well as its pharmacological effects and mechanisms, aiming to provide a theoretical basis for clinical applications.

橙皮素是一种黄酮类化合物,天然存在于芸香科柑橘类水果的果皮中。以往的研究表明,橙皮素具有多种药理作用,如抗炎、抗肿瘤、抗氧化、抗衰老和神经保护等。近年来,随着疾病发病率的增加和人们对传统中药认识的提高,橙皮素因其广泛的药理作用而受到越来越多的关注。要证实其对健康的益处并阐明其潜在机制,了解药代动力学至关重要。然而,橙皮素的溶解度有限,限制了其生物利用度,从而降低了其作为有益健康药物的功效。为了提高橙皮素的生物利用度,人们开发了各种新型制剂,包括纳米颗粒、脂质体和环糊精包合物。本文综述了七叶皂苷药代动力学的最新进展和提高其生物利用度的方法,以及其药理作用和机制,旨在为临床应用提供理论依据。
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引用次数: 0
Retraction notice to “Helenalin attenuates alcohol-induced hepatic fibrosis by enhancing ethanol metabolism, inhibiting oxidative stress and suppressing HSC activation” [Fitoterapia 95 (2014) 203–213] 海伦纳林通过增强乙醇代谢、抑制氧化应激和抑制造血干细胞活化减轻酒精诱导的肝纤维化》的撤稿通知 [Fitoterapia 95 (2014) 203-213]。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-31 DOI: 10.1016/j.fitote.2024.106195
Xing Lin , Shijun Zhang , Renbin Huang , Ling Wei , Shimei Tan , Shuang Liang , Yuanchun Tian , Xiaoyan Wu , Zhongpeng Lu , Quanfang Huang
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引用次数: 0
Untargeted metabolic analysis of Epaltes mexicana by LC-QTOF-MS: Terpenes with activity against human cancer cell lines 利用 LC-QTOF-MS 对 Epaltes mexicana 进行非靶向代谢分析:对人类癌细胞株具有活性的萜烯类化合物。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-30 DOI: 10.1016/j.fitote.2024.106194
Tamara Juárez-Velázquez , José Arnold González-Garrido , Irma Sánchez-Lombardo , Nelly del Carmen Jiménez-Pérez , Ivonne María Olivares-Corichi , José Rubén García-Sánchez , Oswaldo Hernández-Abreu

Epaltes mexicana is a plant widely used in traditional medicine and as a food in Mexico; however, its phytochemical and pharmacological studies are limited. This study aimed to identify the active secondary metabolites of Epaltes mexicana and determine its cytotoxic activity on cancer cell lines. Three organic extracts were obtained by maceration using n-hexane, dichloromethane, and methanol. The n-hexane extract was fractioned by simple column chromatography. Eight terpenes were annotated in collection 6 (C6) by LC-QTOF-MS using a gradient elution and Electrospray Ionization (ESI) in positive ion mode: 1) Gibberellin A15, 2) farfugin A, 3) dehydromyodesmone, 4) eremopetasitenin A1, 5) hydroxyisonobilin, 6) anhydrocinnzeylanine, 7) nigakilactone H and 8) taxodione. On the other hand, C6 showed a concentration-dependent cytotoxic effect on cancer cell lines MCF-7 (Emax = 74.69 ± 6.19 % and IC50 = 6.31 μg/mL), MDA-MB-231 (Emax = 79.28 ± 12.12 % and IC50 = 124.21 μg/mL), and SiHa (Emax = 82.96 ± 6.02 % and IC50 = 124.31 μg/mL). The C6 did not show a cytotoxic effect against DU-145 and non-cancerous cells from the mammary glands MCF-10A. These results indicate cytotoxic specificity on cancer cell lines and support the hypothesis that terpenes identified in E. mexicana must be investigated and developed for non-clinical and clinical trials as potential anti-cancer drugs.

在墨西哥,Epaltes mexicana 是一种广泛用于传统医药和食品的植物;然而,对它的植物化学和药理学研究却很有限。本研究旨在鉴定墨西哥桉树的活性次生代谢物,并确定其对癌细胞株的细胞毒性活性。研究人员使用正己烷、二氯甲烷和甲醇浸泡,获得了三种有机提取物。正己烷提取物通过简单的柱层析法进行分馏。采用梯度洗脱和正离子模式下的电喷雾离子化(ESI),通过 LC-QTOF-MS 对第 6 组(C6)中的 8 种萜烯类化合物进行了注释:1) 赤霉素 A15,2) 远志霉素 A,3) 脱水毛地黄酮,4) 赤霉素 A1,5) 羟基异异黄酮素,6) 羟基嗪基苯胺,7) 黑内酯 H 和 8) 紫杉二酮。另一方面,C6 对癌细胞株 MCF-7(Emax = 74.69 ± 6.19 %,IC50 = 6.31 μg/mL)、MDA-MB-231(Emax = 79.28 ± 12.12 %,IC50 = 124.21 μg/mL)和 SiHa(Emax = 82.96 ± 6.02 %,IC50 = 124.31 μg/mL)具有浓度依赖性细胞毒性作用。C6 对 DU-145 和来自乳腺 MCF-10 A 的非癌细胞没有细胞毒性作用。这些结果表明了对癌细胞株的细胞毒性特异性,并支持这样的假设,即必须研究和开发在 E. mexicana 中发现的萜类化合物,将其作为潜在的抗癌药物进行非临床和临床试验。
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引用次数: 0
Nano-cubosomes of the phyto-active principle in Withania somnifera: LC-MS-NMR, anti-microbial, and insights of the anti-neuropathic and anti-inflammatory mechanism 薇甘菊植物活性成分的纳米立方体:LC-MS-NMR、抗微生物以及对抗神经病学和抗炎机制的见解。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-30 DOI: 10.1016/j.fitote.2024.106196
Karim M. Raafat , Ibrahim A. Abdelwahab , Sally A. El-Zahaby

Withania somnifera (W. somnifera) has a long history of safety in the amelioration of neuro-active ailments. The current study aims to explore Withania somnifera phyto-active principle anti-microbial, ant-neuropathic, and anti-inflammatory activities, and to modify these activities utilizing nano-cubosomes exploiting their mechanisms of action. Bio-guided fractionation technique was utilized, to identify the most phyto-active compound, using LC-MS-NMR online technique and biological models of diabetes, neuropathy, and inflammation. In-vitro antibacterial activity was also monitored. The HbA1c, in-vivo antioxidant (serum-catalase, TBARS, and GSH), serum insulin, and pro-inflammatory serum cytokines (TNF alpha, IL-six, and IL-ten) levels have been assessed to establish the anti-neuropathic and anti-inflammatory mechanisms. The nano-cubosomal formulations (CUB 1–3) were utilized to improve the W. somnifera most active compound efficacy. W. somnifera has shown ten major peaks; coagulin Q (10.2 %), dihydrowithanolide A (2.4 %), dihydrowithaferin D (1.8 %), physagulin D (7.6 %), withanoside V (2.3 %), withanolide A (WDA, 10.3 %), withafrin A (4.9 %), withaferin D (7.7 %), withanone 9 (9.9 %), withanolide D (4.8 %). The bio-guided fractionation technique utilizing LC-MS-NMR technique has proved that withanolide A (WDA) is the most phyto-active compound in W. somnifera. The latter has shown better results than WDA, which might be due to other effective compounds in Ws. However, CUB 3 (WDA nano-cubosomes dispersion) has shown more prominent anti-diabetic, anti-neuropathic, anti-inflammatory, and anti-bacterial potentials than Ws and WDA. Thus, CUB 3 modified WDA activity, and improved its efficacy. The normalization of HbA1c levels, increased insulin secretagogue potential, and the amelioration of the oxidative-stress may be the underlying Ws, WDA, and CUB 3 antidiabetic neuropathy mechanism. Moreover, the Ws, WDA, and CUB 1–3 anti-inflammatory mechanism might be due to the amelioration of the pro-inflammatory serum cytokines (decreasing TNF alpha and IL-six levels and increasing IL-ten). Thus, CUB 3 might be a powerful tool in augmenting Withania somnifera activity as an oral drug-delivery system and improving its efficacy against neuropathy and inflammation.

睡茄(Withania somnifera)在改善神经活性疾病方面的安全性由来已久。目前的研究旨在探索睡茄的植物活性原理,即抗微生物、抗神经病和抗炎活性,并利用纳米立方体利用其作用机制来改变这些活性。利用生物导向分馏技术,采用 LC-MS-NMR 在线技术和糖尿病、神经病变和炎症生物模型,确定了最具植物活性的化合物。此外,还对体外抗菌活性进行了监测。评估了 HbA1c、体内抗氧化剂(血清催化酶、TBARS 和 GSH)、血清胰岛素和促炎血清细胞因子(TNF alpha、IL-6 和 IL-10)的水平,以确定抗神经病变和抗炎机制。纳米立方体制剂(CUB 1-3)被用来提高索姆尼佛最有效化合物的功效。索米非拉有十个主要峰值:凝结素 Q(10.2%)、二氢岩白菜素内酯 A(2.4%)、二氢岩白菜素 D(1.8%)、physagulin D(7.6 %)、黄葵苷 V(2.3 %)、黄葵内酯 A(WDA,10.3 %)、黄葵素 A(4.9 %)、黄葵素 D(7.7 %)、黄葵酮 9(9.9 %)、黄葵内酯 D(4.8 %)。利用 LC-MS-NMR 技术进行的生物导向分馏技术证明,睡茄中最具植物活性的化合物是睡茄内酯 A(WDA)。与 WDA 相比,后者显示出更好的效果,这可能是由于 Ws 中含有其他有效化合物。不过,CUB 3(WDA 纳米立方体分散体)比 Ws 和 WDA 显示出更突出的抗糖尿病、抗神经病、抗炎和抗菌潜力。因此,CUB 3 改变了 WDA 的活性,提高了其疗效。HbA1c 水平的正常化、胰岛素分泌潜能的增加以及氧化应激的改善可能是 Ws、WDA 和 CUB 3 抗糖尿病神经病变的基本机制。此外,Ws、WDA 和 CUB 1-3 的抗炎机制可能是由于改善了促炎血清细胞因子(TNF alpha 和 IL-six 水平下降,IL-ten 水平上升)。因此,CUB 3 可能是一种强有力的工具,可增强睡茄作为口服给药系统的活性,并提高其抗击神经病变和炎症的功效。
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引用次数: 0
Chemistry and bioactivity of marine algal toxins and their geographic distribution in China 海洋藻毒素的化学性质和生物活性及其在中国的地理分布。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-24 DOI: 10.1016/j.fitote.2024.106193
Changrong Lai , Xiaojun Dai , Danmei Tian , Songhui Lv , Jinshan Tang

Marine algal toxins are usually produced by some toxic algae during toxic algal blooms which can be accumulated in marine organisms through food chains, leading to contamination of aquatic products. Consumption of the contaminated seafood often results in poisoning in human being. Although algal toxins are harmful for human health, their unique structures and broad spectrum of biological activities have attracted widespread attention of chemists and pharmacologists. Marine algal toxins are not only a reservoir of biological active compound discovery, but also powerful tools for exploring life science. This review first provides a comprehensive overview of the chemistry and biological activities of marine algal toxins, with the aim of providing references for biological active compound discovery. Additionally, typical shellfish poisoning incidents occurred in China in the past 15 years and the geographical distribution of the marine algal toxins in China Sea are discussed, for the purpose of enhancing public awareness of the possible dangers of algal toxins.

海洋藻类毒素通常由一些有毒藻类在有毒藻类大量繁殖时产生,可通过食物链在海洋生物体内积累,导致水产品污染。食用受污染的海产品往往会导致人类中毒。虽然藻毒素对人类健康有害,但其独特的结构和广泛的生物活性引起了化学家和药理学家的广泛关注。海洋藻类毒素不仅是发现生物活性化合物的宝库,也是探索生命科学的有力工具。本综述首先全面概述了海洋藻类毒素的化学和生物活性,旨在为生物活性化合物的发现提供参考。此外,还讨论了中国近 15 年来发生的典型贝类中毒事件以及中国海域海洋藻类毒素的地理分布,以提高公众对藻类毒素可能造成危害的认识。
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引用次数: 0
Phytochemical investigation of Chrysanthellum americanum Vatke and its constituents- a targeted approach for the treatment of leishmaniasis Chrysanthellum americanum Vatke 及其成分的植物化学研究--一种治疗利什曼病的靶向方法。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-24 DOI: 10.1016/j.fitote.2024.106192
Aneela Fayaz , Muhammad Yousuf , Abdoulaye Segda , Atia-tul-Wahab , Humaira Zafar , Muhammad Kamran , Roland Nâg-Tiéro Meda , Yan Wang , M. Iqbal Choudhary

The present study is focused on the isolation and identification of new therapeutic candidates from Chrysanthellum americanum Vatke., and their efficacy against pteridine reductase-1 (PTR1), a valid chemotherapeutic target in the Leishmania parasite. Henceforth, a new compound, chrysanamerine (1), along with 7 known compounds, polyacetylene 2, and flavonoids 38, were isolated from C. americanum. Their structures were determined by chemical and spectroscopic analyses and compared with the reported spectroscopic data. All compounds were evaluated for their anti-leishmanial activity against PTR1 via biochemical mechanism-based assay. The in vitro results showed five potential hits including a new compound, chrysanamerine (1), and four known compounds against the PTR1 enzyme. Among them, compound 1 showed a potent enzyme inhibition with an IC50 of 31.02 ± 2.36 μM, whereas a moderate inhibition was observed in cases of compounds 5 and 6 (IC50 = 59.86 ± 3.32, and 45.32 ± 3.5 μM, respectively). Whereas, compounds 3 and 8 showed mild inhibition (IC50 = 72.12 ± 1.12, and 97.18 ± 1.23 μM, respectively) against PTR1, compared with trimethoprim (positive control) (IC50 = 21.07 ± 1.6 μM). Moreover, the results were further validated via molecular docking and molecular dynamics (MD) simulations. Compound 1 showed a strong affinity to the binding site with a docking score of −11.83, along with the formation of a stable protein-ligand complex over the trajectory of 100 ns. Besides, compounds 18 were found to be non-cytotoxic on BJ (human fibroblast) cells.

本研究的重点是从 Chrysanthellum americanum Vatke.中分离和鉴定新的候选疗法,以及它们对蝶啶还原酶-1(PTR1)的疗效,PTR1 是利什曼寄生虫的有效化疗靶标。因此,从美洲金合欢中分离出了一种新化合物--金合欢碱(1),以及 7 种已知化合物、聚乙炔 2 和黄酮类化合物 3-8。通过化学和光谱分析确定了这些化合物的结构,并与报告的光谱数据进行了比较。所有化合物都通过基于生化机理的方法评估了它们对 PTR1 的抗利什曼活性。体外实验结果显示,有五种化合物具有潜在的抗 PTR1 酶活性,包括一种新化合物 Chrysanamerine(1)和四种已知化合物。其中,化合物 1 显示出强效的酶抑制作用,IC50 为 31.02 ± 2.36 μM,而化合物 5 和 6 则显示出中度抑制作用(IC50 分别为 59.86 ± 3.32 和 45.32 ± 3.5 μM)。而与三甲氧苄啶(阳性对照)(IC50 = 21.07 ± 1.6 μM)相比,化合物 3 和 8 对 PTR1 的抑制作用较弱(IC50 = 72.12 ± 1.12 和 97.18 ± 1.23 μM)。此外,还通过分子对接和分子动力学(MD)模拟进一步验证了研究结果。化合物 1 与结合位点的亲和力很强,对接得分为 -11.83,并在 100 ns 的轨迹上形成了稳定的蛋白质配体复合物。此外,还发现化合物 1-8 对 BJ(人成纤维细胞)细胞无毒性。
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引用次数: 0
Retraction notice to “Beneficial effects of asiaticoside on cognitive deficits in senescence-accelerated mice” [Fitoterapia 87 (2013) 69–77]. 茜草苷对衰老加速小鼠认知障碍的有益影响》[Fitoterapia 87 (2013) 69-77]的撤稿通知。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-08-22 DOI: 10.1016/j.fitote.2024.106191
Xing Lin , Renbin Huang , Shijun Zhang , Ling Wei , Lang Zhuo , Xiaoyan Wu , Aicun Tang , Quanfang Huang
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引用次数: 0
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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Fitoterapia
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