Fitoterapia最新文献_第8页

Gardenia jasminoides Ellis polysaccharides improve gut microbiota disorder and glucose homeostasis in type 2 diabetic mice 栀子多糖改善2型糖尿病小鼠肠道菌群紊乱和葡萄糖稳态。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2026-01-01 DOI: 10.1016/j.fitote.2025.107080

Wenye Lu , Wanjun Ju , Ningning Niu , Yuanyuan Li , Tianming Wang , Yu Feng , Yueming Ma , Jiasheng Wu

Type 2 diabetes mellitus (T2DM) is the most prevalent metabolic disorder. Gardenia jasminoides Ellis is a traditional herbal medicine used in metabolic disease treatment; however, the effects of Gardenia jasminoides Ellis polysaccharides (GPS) on T2DM remain unknown. This study aimed to investigate the antidiabetic effect of GPS in a T2DM mouse model induced by high-fat diet (HFD) and streptozotocin administration, and to elucidate the potential molecular mechanism. Treatment with low and high doses (200 and 400 mg/kg) of GPS significantly reduced the fasting blood glucose level of T2DM mice by 44.8 % and 33.0 %, respectively. In T2DM mice, oral glucose tolerance test outcomes and insulin tolerance were significantly improved by GPS intervention (p < 0.05), and the pancreatic tissue damage was ameliorated compared with control mice. Moreover, GPS intervention upregulated the liver expression of peroxisome proliferator-activated receptor gamma (PPARγ) by 1.7 fold, improved insulin resistance, and increased glycogen synthesis in T2DM mice compared with in untreated control mice (p < 0.05). More importantly, GPS intervention significantly improved gut microbiota dysbiosis, increased the abundance of short chain fatty acids producing Lactobacillus and Dubosiella by 6.6- and 16.5-fold, respectively, and elevated the serum level of butyric acid in T2DM mice. Furthermore, in vitro experiments confirmed that butyric acid can induce PPARγ expression. In conclusion, these findings suggest that GPS may alleviate T2DM by reshaping the gut microbiota and regulating intestinal metabolites. Therefore, GPS may be a potential prebiotic for modulating T2DM-associated metabolic disorders.

2型糖尿病（T2DM）是最常见的代谢紊乱。栀子是治疗代谢性疾病的传统中草药；然而，栀子多糖（GPS）对T2DM的影响尚不清楚。本研究旨在探讨GPS在高脂饮食（HFD）和链脲佐菌素诱导的T2DM小鼠模型中的降糖作用，并探讨其可能的分子机制。低剂量和高剂量（100和200 mg/kg）的GPS治疗可使T2DM小鼠的空腹血糖水平分别降低44.8% %和33.0% %。在T2DM小鼠中，GPS干预显著改善了口服糖耐量试验结果和胰岛素耐量(p

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引用次数: 0

Antioxidant active ingredients from the seeds of Dimocarpus longan Lour 龙眼种子抗氧化活性成分的研究。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2025-12-23 DOI: 10.1016/j.fitote.2025.107043

Bin Liu , Yang Xu , Lingxiao Ren , Xiaofen Liu , Lixia Chen , Hua Li

The seeds of Dimocarpus longan Lour. are rich in bioactive compounds, notably polyphenols, flavonoids, and sesquiterpenoids, which have demonstrated antioxidant, antitumor, and antifungal activities. Phytochemical investigation of the seeds led to the isolation of thirteen compounds (1−13), comprising six previously undescribed structures (1–6) and seven known analogues (7–13). The structures of the new compounds were elucidated through comprehensive spectroscopic analysis, including 1D/2D NMR, HR-ESI-MS, UV, ECD, and optical rotation. All isolated compounds were evaluated for their protective effects against hydrogen peroxide-induced oxidative stress in BV-2 microglial cells. Among them, compounds 2, 3, 7, 11, and 12 exhibited significant antioxidant activity. These findings underscore the potential of Dimocarpus longan seeds as a valuable source of bioactive agents for medicinal and functional food applications.

龙眼树的种子。富含生物活性化合物，特别是多酚、类黄酮和倍半萜类化合物，具有抗氧化、抗肿瘤和抗真菌活性。对种子的植物化学研究分离出13种化合物（1-13），包括6种以前未描述的结构（1-6）和7种已知的类似物（7-13）。通过1D/2D NMR、HR-ESI-MS、UV、ECD、旋光度等综合光谱分析对新化合物的结构进行了鉴定。所有分离的化合物对BV-2小胶质细胞过氧化氢诱导的氧化应激的保护作用进行了评估。其中化合物2、3、7、11和12表现出显著的抗氧化活性。这些发现强调了龙眼种子作为药用和功能性食品生物活性物质的宝贵来源的潜力。

引用次数: 0

Nagarudine, a new C19-diterpenoid alkaloid from Aconitum nagarum Stapf: Isolation, structure elucidation, synthesis of nagarudine analogue, and apoptotic activity 纳加鲁定：一种新的c19 -二萜类生物碱的分离、结构鉴定、纳加鲁定类似物的合成及细胞凋亡活性研究。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2026-01-03 DOI: 10.1016/j.fitote.2026.107089

Mei-Zhen Ye , Yang Yang , Cheng Yuan , Yu-Qi Yang , Ning Ding , Qin He , Shuai Huang , Lin Chen , Xian-Li Zhou

A previously unreported C₁₉-diterpenoid alkaloid with a tetrahydrofuran skeleton, nagarudine (1), was isolated from the roots of Aconitum nagarum Stapf. The structures and absolute configurations of compound 1 was established via comprehensive spectroscopic analysis, ECD calculation, and X-ray crystallography. To explain the formation of this natural skeleton, the nagarudine analogue was synthesized. 1 displayed proliferation inhibition effect on the Sf9 cell line with an IC₅₀ value of 16.04 μg/mL, and its apoptotic induction effect was illustrated by morphological observation. Combined with flow cytometry, staining, and Western blotting conclusively showed that nagarudine effectively induced apoptosis in Sf9 cells through the mitochondrial pathway.

一种具有四氢呋喃骨架的c19 -二萜生物碱，nagarudine(1)，从Aconitum nagarum Stapf的根中分离得到。化合物1的结构和绝对构型通过综合光谱分析、ECD计算和x射线晶体学得到。为了解释这种天然骨架的形成，合成了nagarudine类似物。1对Sf9细胞株具有增殖抑制作用，IC50值为16.04 μg/mL，并通过形态学观察证实其诱导凋亡作用。结合流式细胞术、染色和Western blotting结果表明，纳加鲁定通过线粒体途径有效诱导Sf9细胞凋亡。

引用次数: 0

Antibacterial diphenyl ether derivatives from mangrove-derived fungus Aspergillus versicolor 21041517 红树林衍生真菌花色曲霉的抗菌二苯醚衍生物21041517。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2026-01-03 DOI: 10.1016/j.fitote.2026.107086

Bin Wang , Jin Cai , Guojun Zhou , Mohan Zhang , Meng Yang , Yanxuan Li , Baoyi Zhang , Youping Luo , Nasihat , Xueming Zhou , Guolei Huang , Caijuan Zheng

Three new diphenyl ethers diorcinols P-Q (1–2), and gibellulin E (3), together with one new sesquiterpene isoversiol H (4), as well as six known diphenyl ethers (5–10) were obtained from the mangrove-derived fungus Aspergillus versicolor 21041517. Comprehensive spectroscopic techniques, ECD calculations, X-ray diffraction analyses, and modified Mosher's method were used to confirm the planner structures and absolute configurations of the new compounds. The diphenyl ethers 1, 5 and 6 exhibited inhibitory activity against three tested pathogenic bacteria. 20 diphenyl ether derivatives (5a1–5j2) were designed and semisynthesized to improve the antibacterial activity of diphenyl ethers. In particular, compound 5a1 showed potent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), with the MIC value of 3.13 μg/mL. Preliminary antimicrobial mechanism investigations of 5a1 were performed. Treatment with 5a1 resulted in the leakage of the AKP, a decrease in intracellular ATP concentration, and a reduction in soluble protein content. Scanning electron microscopy demonstrated that 5a1 can damage the cell membrane of MRSA. Transcriptome assay revealed that 5a1 may target cellular energy metabolism. This study offers valuable insights that contribute to development of novel anti-MRSA agents, and providing potential strategies for addressing antibiotic.

从红木曲霉（Aspergillus versicolor 21,041,517）中分离得到3个新的二苯基醚diorcinols P-Q（1-2）和gibellulin E(3)， 1个新的倍半萜异醇H(4)和6个已知的二苯基醚（5-10）。综合光谱技术、ECD计算、x射线衍射分析和改进的Mosher方法确定了新化合物的规划结构和绝对构型。二苯醚1、5、6对3种病原菌均有抑制作用。为提高二苯醚的抗菌活性，设计并合成了20种二苯醚衍生物（5a1-5j2）。其中，化合物5a1对耐甲氧西林金黄色葡萄球菌（MRSA）表现出较强的抗菌活性，MIC值为3.13 μg/mL。初步探讨了5a1的抗菌机制。5a1处理导致AKP渗漏，细胞内ATP浓度降低，可溶性蛋白含量降低。扫描电镜显示5a1能破坏MRSA的细胞膜。转录组分析显示5a1可能靶向细胞能量代谢。该研究为开发新型抗mrsa药物提供了有价值的见解，并为解决抗生素问题提供了潜在的策略。

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引用次数: 0

Auslactones A−E, austalide meroterpenoids from Aspergillus ustus NRRL 275 牛曲霉nrrl275中的牛内酯A-E，牛曲霉烯萜类化合物。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2026-01-21 DOI: 10.1016/j.fitote.2026.107105

Lin Liu , Yinhui Zhou , Shu-Ming Li , Hanli Ruan

Five new austalide meroterpenoids, named auslactones A − E (1–5), one new natural product (6), together with ten known analogues (7–16), were isolated from the fungus Aspergillus ustus NRRL 275. Auslactones A − B (1–2) represent a class of austalides containing 5/6/6/6/6/5 hexacyclic ring with a hydroxymethyl group at C-15. Auslactones C − D (3–4) enrich the type of 5/6/6/6/5/6/5 heptacyclic austalides. Auslactone E (5) contains 5/6/6/6 tetracyclic ring system. Meanwhile, the NMR data of auslactone F (6) were reported for the first time. Their structures were elucidated by extensive spectroscopic analysis. The absolute configuration of compound 1 was established by single-crystal X-ray diffraction, whereas those for the others were established by circular dichroism (CD) data analysis. No cytotoxic or immunosuppressive activity was found for compounds 1–6.

从真菌Aspergillus usstus NRRL 275中分离得到5个新的austalide meroterpenoids，命名为auslactones A - E(1-5)， 1个新的天然产物(6)和10个已知的类似物（7-16）。ausallactones A - B（1-2）代表了一类含有5/6/6/6/ 5六环并在C-15上有一个羟基甲基的austalides。Auslactones C - D（3-4）丰富了5/6/6/6/5/6/5七环austalides的类型。奥内酯E(5)含有5/6/6/6四环环体系。同时，首次报道了auslactone F(6)的NMR数据。它们的结构通过广泛的光谱分析得以阐明。化合物1的绝对构型由单晶x射线衍射确定，其余化合物的绝对构型由圆二色性（CD）数据分析确定。化合物1 ~ 6无细胞毒性或免疫抑制活性。

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引用次数: 0

Vasorelaxation and antihypertensive activity of standardized extract of Gymnema sylvestre in rodent model 匙羹藤标准提取物对啮齿动物的血管舒张及降压作用。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2026-01-22 DOI: 10.1016/j.fitote.2026.107111

Poonam Rani , Deepak Kumar , Kumari Savita , Divya Mishra , Shweta Parashar , Palak Singh , Manisha Yadav , Feroz Khan , Madhav Nilakath Mugale , Prasant Kumar Rout , Debabrata Chanda

Gymnema sylvestre (GS) leaf extract is one of the most important functional food indicated for management of diabetes, obesity and associated disorders and is also indicated in Ayurveda for heart diseases. Although the plant is currently under intense exploration for its therapeutic potential in cardiometabolic diseases but efficacy against hypertension and in inducing vasorelaxation in vasculature was never well explored. The present study envisaged vasorelaxation and antihypertensive activity of biomarkers enriched extract (Gym-cit) in rodent model. When given at 30 mg kg⁻¹, 100 mg kg⁻¹ and 300 mg kg⁻¹ once orally for 14-days, Gym-cit significantly decreased the systolic, diastolic and mean arterial pressure in SHR. GS biomarkers like Gymnemagenin (GMN), Deacyl gymnemic acid (DAC), Gymnemic acid IV (GA IV) and standardized extract exhibited concentration dependent vasorelaxation in ex-vivo model in mesenteric artery. Gymnemagenin (GMN) exhibited maximum vasorelaxation potential (E_max; 59.44 ± 1.88; n = 6), putatively through opening of BK_Ca channel and blocking of L-type voltage dependent calcium channel in vascular smooth muscle. Gym-cit showed decent vasorelaxation response and significant antihypertensive activity in SHRs with significant decrease in systolic, diastolic and mean arterial pressure. The study suggests great promise in Gym-cit against cardiometabolic diseases associated with hypertension.

Gymnema sylvestre （GS）叶提取物是最重要的功能性食品之一，用于治疗糖尿病、肥胖和相关疾病，在阿育吠陀医学中也用于治疗心脏病。虽然目前对其治疗心脏代谢疾病的潜力进行了大量的探索，但对高血压和诱导血管舒张的功效却从未得到很好的探索。本研究设想了生物标志物富集提取物（Gym-cit）在啮齿动物模型中的血管松弛和降压活性。服用30 mg kg-1、100 mg kg-1和300 mg kg-1口服14天，Gym-cit可显著降低SHR的收缩压、舒张压和平均动脉压。在离体肠系膜动脉模型中，GS生物标志物如裸子素（GMN）、脱酰基裸子酸（DAC）、裸子酸IV （GA IV）和标准化提取物均表现出浓度依赖性血管松弛。Gymnemagenin （GMN）表现出最大的血管舒张电位（Emax; 59.44 ± 1.88;n = 6），推测是通过打开血管平滑肌BKCa通道和阻断l型电压依赖性钙通道实现的。gym - citit在shr患者中表现出良好的血管松弛反应和显著的降压活性，收缩压、舒张压和平均动脉压均显著降低。这项研究表明，gym - city对高血压相关的心脏代谢疾病有很大的帮助。

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引用次数: 0

Multi-faceted bioactivity of three unexplored Turkish plants: A comparative phytochemical and pharmacological profiling 三种未开发的土耳其植物的多方面生物活性：比较植物化学和药理学分析。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2025-12-25 DOI: 10.1016/j.fitote.2025.107066

Nilofar , Gunes Ak , Enver Saka , Gokhan Zengin , Cziaky Zoltan , Josef Jeko , Annalisa Chiavaroli , Simonetta Cristina Di Simone , Mariachiara Gabriele , Maria Loreta Libero , Giustino Orlando , Luigi Menghini , Claudio Ferrante , Jasmina Glamočlija , Mladen Rajaković , Evren Yildiztugay , Meng-Yao Li

Since ancient times, plants have been used as a valuable source for treating serious diseases. Three different plants, namely Aubrieta pinardii, Johrenia dichotoma, and Malabaila dasyantha were used and extracted using the extraction solvents ethyl acetate (EA), methanol (MeOH), and water. Antioxidant activity was determined using several in vitro assays. Subsequently, the enzyme inhibition activities of the extracts were evaluated against cholinesterases (AChE and BChE), tyrosinase, amylase, and glucosidase. The antibacterial and antifungal effects of the extracts were assessed. Methanol extracts of A. pinardii, J. dichotoma, and M. dasyantha yielded the highest total flavonoids (TFC) compared to EA and water extracts. The analysis using HPLC-ESI-Q-TOF-MS identified various classes of phytochemicals within the species examined. Aubrieta pinardii extracts were abundant in glucosinolates, whereas J. dichotoma and M. dasyantha extracts were characterized by the presence of coumarins and furanocoumarins. The EA extracts exhibited greater inhibition of microorganism growth compared with MeOH and water extracts. Notably, J. dichotoma showed similar or superior antifungal activity against A. niger (MIC/MFC 0.25/0.50 mg/mL) and M. dasyantha demonstrated comparable efficacy against T. viride (MIC/MFC 0.50/1.00 mg/mL) and P. verrucosum var. cyclopium (MIC/MFC 0.125/0.25 mg/mL) when benchmarked against the reference drug ketoconazole. These results provide valuable information about A. pinardii, J. dichotoma, and M. dasyantha chemical profiles and underline the importance of selecting appropriate solvents for the extraction of metabolites from plant matrix for potential applications in the treatment of various diseases.

自古以来，植物就被用作治疗严重疾病的宝贵资源。采用三种不同的植物，即红毛赤杨（Aubrieta pinardii）、二叉菊（Johrenia dichotoma）和马拉贝拉（Malabaila dasyantha），分别用乙酸乙酯（EA）、甲醇（MeOH）和水进行提取。采用几种体外测定法测定其抗氧化活性。随后，研究了提取物对胆碱酯酶（AChE和BChE）、酪氨酸酶、淀粉酶和葡萄糖苷酶的抑制活性。评价了各提取物的抗菌和抗真菌作用。与EA和水提取物相比，pinardii， J. dichotoma和M. dasyantha甲醇提取物的总黄酮（TFC）含量最高。HPLC-ESI-Q-TOF-MS分析鉴定出不同种类的植物化学物质。红毛紫苏提取物中硫苷含量较高，而双花紫苏和大花紫苏提取物中主要含有香豆素和呋喃香豆素。与MeOH和水提取物相比，EA提取物对微生物生长的抑制作用更大。值得注意的是，当与对照药物酮康唑作对照时，J. dichotoma对黑曲霉（MIC/MFC 0.25/0.50 mg/mL）和M. dasyantha对T. viride （MIC/MFC 0.50/1.00 mg/mL）和P. verrucosum var. cyclopium （MIC/MFC 0.125/0.25 mg/mL）表现出相似或更好的抗真菌活性。这些结果为pinardii， J. dichotoma和M. dasyantha的化学特征提供了有价值的信息，并强调了选择合适的溶剂从植物基质中提取代谢物的重要性，以潜在地应用于治疗各种疾病。

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引用次数: 0

A new antiviral isorhamnetin glycoside from the Tunisian plant Herniaria hirsuta L. 从突尼斯植物Herniaria hirsuta L.中获得一种新的抗病毒异鼠李素糖苷。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2026-01-11 DOI: 10.1016/j.fitote.2026.107092

Hana Slimi , Hayet Edziri , Fatma Nouira , Lamjed Bouslama , Maha Mastouri , Adele Cutignano

Herniaria hirsuta L. (Caryophyllaceae) is an annual herb known as hairy rupturewort. It is used in traditional medicine, particularly in North Africa, to prevent and cure kidney stones and as a diuretic. Rich in saponins, it possesses many other bioactive secondary metabolites including flavonoids and their glycosides. Plant specimens harvested in Tunisia were chemically investigated and their extracts tested for antiviral activity. Ethyl acetate and butanol extracts showed significant activity against Herpes Simplex type-2 (HSV-2) virus (IC₅₀ = 31.15 μg/mL, SI =10.97 and IC₅₀ = 46.04 μg/mL, SI = 6.44, respectively). Ultra-High Performance Liquid Chromatography-High Resolution ElectroSpray Ionization Mass Spectrometry (UHPLC-HRESIMS) analyses combined with Nuclear Magnetic Resonance (NMR) spectroscopy revealed the occurrence of a family of isorhamnetin glycosides, containing 1 to 3 sugar units. By using a bioassay guided fractionation approach, we identified a new flavonoid glycoside: its chemical structure was resolved by extensive use of NMR spectroscopy and HRESIMS/MS as isorhamnetin-3-O-(2-O-(4-acetyl)-α-L-rhamnopyranosyl, 6-O-α-L-rhamnopyranosyl)-β-D-galactopyranoside, which exhibited an IC₅₀ = 20.34 μM (SI >15). Notably, its co-occurring deacetyl derivative resulted inactive. In vitro assays suggested that the antiviral action is exerted during the early stages of the viral cycle, preventing HSV-2 from infecting target cells.

hirsuta L.（石竹科）是一种一年生草本植物，被称为毛破裂草。在传统医学中，特别是在北非，它被用来预防和治疗肾结石，并作为利尿剂。它富含皂苷，还具有许多其他生物活性次生代谢产物，包括黄酮类化合物及其苷类。对在突尼斯收获的植物标本进行了化学研究，并对其提取物进行了抗病毒活性测试。乙酸乙酯和丁醇提取物对2型单纯疱疹病毒（HSV-2）具有显著的抑制作用（IC50 = 31.15 μg/ml, SI =10.97; IC50 = 46.04 μg/ml, SI = 6.44）。超高效液相色谱-高分辨率电喷雾质谱分析（uhplc - hresms）结合核磁共振（NMR）光谱分析发现了一个异鼠李素糖苷家族，包含1至3个糖单位。采用生物测定指导分离的方法，鉴定出一种新的黄酮类苷类化合物，通过核磁共振光谱和HRESIMS/MS鉴定其化学结构为异鼠李糖素-3- o -(2-O-（4-乙酰基）-α- l -鼠李糖pyranosyl， 6-O-α- l -鼠李糖pyranosyl -β- d -半乳糖吡喃苷，IC50为 = 20.34 μM （SI bbb15）。值得注意的是，其共发生的脱乙酰衍生物导致失活性。体外实验表明，抗病毒作用在病毒周期的早期阶段发挥作用，阻止HSV-2感染靶细胞。

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引用次数: 0

Quinoline and para-aminobenzoic acid derivatives with anti-osteoclastic activity from a marine mesophotic zone Demosponge sponge-associated fungus Xylaria sp. NBUF245 海洋间孔区海绵相关真菌Xylaria sp. NBUF245的喹啉和对氨基苯甲酸衍生物具有抗破骨活性。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2025-12-23 DOI: 10.1016/j.fitote.2025.107046

Yu-Ying Liu , Chan-Ting Lai , Salman Khan , Qian-Jing Zheng , Rong Zhang , Wei-Yi Wang , Bin Wu , Shan He , Li Yang , Ting-Ting Wang

One undescribed quinoline derivative, xylaminoquin A (1), one new p-aminobenzoic acid derivative, xylamidate B (2), and methyl 4-(butanoylamino)-3-hydroxybenzoate, reported for the first time as a natural product and named xylamidate C (3), together with known alkaloids and diketopiperazines, methyl 4-acetylamino-3-hydroxybenzoate (4), methyl 4-[(1-oxobutyl)amino]benzoate (5), pseurotin A (6), azaspirofuran A (7), cyclo(l-Tyr-l-Leu) (8), and cyclo-(l-Tyr-l-Val) (9) were isolated from Xylaria sp. NBUF245, a fungus associated with a Demosponge sp. collected from the marine mesophotic zone. Structurally, compound 1 is the first example of 3,7-dissubstitented quinoline derivative isolated from fungi. The structures of all compounds were elucidated by combined analysis of spectroscopic data and X-ray crystallography. Bioassay results showed that compound 5 effectively prevented prednisolone-induced bone loss in zebrafish at a concentration of 30 μM, suggesting potential osteoprotective activity.

一种未被描述的喹啉衍生物xylaminoquin A(1)，一种新的对氨基苯甲酸衍生物xylamidate B(2)和甲基4-（丁酰氨基）-3-羟基苯甲酸甲酯，首次作为天然产物报道并命名为xylamidate C(3)，以及已知的生物碱和二酮哌嗪，甲基4-乙酰氨基-3-羟基苯甲酸甲酯(4)，甲基4-[（1-氧丁基）氨基]苯甲酸甲酯(5)，假黄素A (6), azaspirofuran A(7)，环（l-Tyr-l-Leu） (8)，和cyclo-(l-Tyr-l-Val)(9)分别从海洋中孔带采集的与Demosponge sp.相关的Xylaria sp. NBUF245真菌中分离得到。结构上，化合物1是首次从真菌中分离得到的3,7-非取代喹啉衍生物。所有化合物的结构都通过光谱数据和x射线晶体学的结合分析得到了证实。生物测定结果表明，化合物5在浓度为30 μM时可有效预防强的松龙诱导的斑马鱼骨质流失，提示其具有潜在的骨保护作用。

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引用次数: 0

Nine feruloyltyramine derivatives and one pyrrole with hepatoprotective activity isolated from fresh Portulaca oleracea L. 新鲜马蹄苋中具有保肝活性的9个阿魏酰基胺衍生物和1个吡咯。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-03-01 Epub Date: 2026-01-18 DOI: 10.1016/j.fitote.2026.107098

Hongqing Wang , Yaru Jiao , Jianbo Liu, Junhua Sun, Zhanrong Zhou, Ruoyun Chen, Jie Kang

Nine feruloyltyramine derivatives (1, 2, 4–10) and one pyrrole (3) were isolated from 70% EtOH extract of fresh Portulaca oleracea L.. Among them, compounds 1, 2 and 4 were cyclized feruloyltyramine derivatives, the other feruloyltyramine derivatives (5–10) were non-cyclized. Compounds 1 and 2 were racemic mixtures, and were separated into enantiomers 1-a (R), 1-b (S), 2-a (R) and 2-b (S), respectively. Three compounds (1–3) were new, and their structures were elucidated by UV, IR, HRESIMS, 1D and 2D NMR, and ECD spectra, as well as optical rotations. All the compounds (1−10) were tested for their hepatoprotective activity in vitro. At a concentration of 10 μM, three cyclized feruloyltyramine derivatives (1-a, 2-a and 4) possessed significant hepatoprotective activity against the damage induced by N-acetyl-para-aminophenol (APAP) in human HepG2 liver cancer cells, with cell survival rates of 63.61, 65.44 and 65.52%. It was suggested that the cyclized feruloyltyramine derivatives with R configuration had better hepatoprotective activity than that of S configuration and non-cyclized feruloyltyramine derivatives.

从新鲜马蹄苋70% EtOH提取物中分离得到9个阿魏乙胺衍生物（1,2,4 -10）和1个吡咯(3)。其中化合物1、2、4为环化阿魏酰乙胺衍生物，其余化合物（5 ~ 10）为非环化阿魏酰乙胺衍生物。化合物1和2为外消旋混合物，分别分离为对映体1-a (R)、1-b (S)、2-a (R)和2-b (S)。其中3个化合物（1-3）为新化合物，其结构通过UV、IR、hresms、1D和2D NMR、ECD光谱以及旋光性进行了鉴定。所有化合物（1-10）均进行了体外保肝活性试验。在10 μM浓度下，3种环化阿魏酰乙胺衍生物（1-a、2-a和4）对n -乙酰对氨基酚（n -acetyl-para- aminhenol， APAP）对人HepG2肝癌细胞的损伤具有显著的肝保护作用，细胞存活率分别为63.61、65.44和65.52%。结果表明，具有R构型的环化阿魏酰乙胺衍生物比S构型和非环化阿魏酰乙胺衍生物具有更好的肝保护活性。

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引用次数: 0