Fitoterapia最新文献_第2页

Comparative analysis of phytochemical profile and traditional pharmacological activities of Fritillaria anhuiensis and five Chinese medicinal herbs Fritillariae Bulbus 安徽贝母与五种中草药贝母的植物化学特征及传统药理活性比较分析。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-22 DOI: 10.1016/j.fitote.2026.107108

Yufeng Zhang , Zeqian Ma , Lu Cheng , Chengwu Fang , Yuehao Zhu , Shoujin Liu , Han Luo

Background

More than two thousand years ago, the bulbs of vegetal species in the genus Fritillaria were used to relieve cough and expectoration, they are also used in clinical treatments for antitussive and expectoration and anti-inflammation due to their extensive pharmacological activities currently. This study aims to analyze the differences in bioactive characteristic metabolites and traditional pharmacological activity between F. anhuiensis and the other five types of Fritillaria species included in Pharmacopoeia of People's Republic of China.

Methods

UHPLC-Q-Orbitrap-MS was employed to acquire mass spectrometry data from six species of Fritillaria. Principal component analysis and multivariate statistical analysis were applied to compare the differences in bioactive characteristic components between F. anhuiensis and other Fritillaria species. For pharmacological evaluation, a mouse model was utilized to systematically assess the antitussive, expectorant, and anti-inflammatory effects of F. anhuiensis in comparison with other Fritillaria species, through ammonia-induced cough tests, tracheal phenol red excretion experiments, and auricle swelling assays.

Results

A total of 153 compounds were identified in six species of Fritillaria. Cluster analysis indicated that F. anhuiensis was segregated as a separate category. Comparative analysis revealed 28 differential metabolites in F. anhuiensis compared to other Fritillaria species, the number of alkaloid metabolites is the majority. In traditional pharmacological studies, F. anhuiensis exhibited antitussive effects comparable to that of F. cirrhosa and superior to that of other Fritillaria species. Its expectorant activity was comparable to that of F. thunbergii and more pronounced than that of other Fritillaria species. With regard to anti-inflammatory effects, F. anhuiensis demonstrated the most potent inhibition of xylene-induced auricle swelling and showed efficacy comparable to F. cirrhosa in reducing the levels of anti-inflammatory factors in the serum of mouse, significantly outperforming other species within the genus.

Discussion

In contrast to other Fritillaria species, F. anhuiensis presented specificity in its chemical characteristics and demonstrated excellent antitussive, expectorant, and anti-inflammatory effects in traditional pharmacological activity experiments. This study provides solid scientific evidence for the substitution of F. anhuiensis for other Fritillaria species.

背景：早在两千多年前，贝母属植物的球茎就被用于止咳祛痰，目前由于其广泛的药理活性，也被用于临床治疗止咳祛痰和抗炎。本研究旨在分析安徽贝母与中华人民共和国药典收录的其他五种贝母在生物活性特征代谢物和传统药理活性方面的差异。方法：采用UHPLC-Q-Orbitrap-MS对6种贝母进行质谱分析。采用主成分分析和多元统计分析比较安徽贝母与其他贝母品种生物活性特征成分的差异。药理学评价方面，采用小鼠模型，通过氨致咳嗽实验、气管酚红排泄实验和耳廓肿胀实验，系统评价安徽贝母与其他贝母的止咳、祛痰、抗炎作用。结果：从贝母属6种中共鉴定出153个化合物。聚类分析表明，安徽赤杨被分离为一个单独的分类。对比分析发现安徽贝母的28种代谢物与其他贝母种类相比存在差异，其中生物碱代谢物数量最多。在传统药理学研究中，安徽贝母的止咳作用与肝硬化贝母相当，优于其他贝母品种。其祛痰作用与浙贝母相当，比其他贝母品种更明显。在抗炎作用方面，安徽黄芪对二甲苯诱导的耳膜肿胀的抑制作用最强，其降低小鼠血清中抗炎因子水平的效果与肝硬化黄芪相当，明显优于属内其他物种。讨论：与其他贝母物种相比，安徽贝母具有特异性的化学特性，在传统药理活性实验中表现出优异的止咳、祛痰、抗炎作用。本研究为安徽贝母替代其他贝母物种提供了坚实的科学依据。

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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 : 2026-01-21 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

Potential of ethyl acetate and acetone extracts from Montrichardia linifera leaves: Chemical characterization, in vitro study, molecular docking ad ADME-TOX 蒙地茅叶乙酸乙酯和丙酮提取物的潜力：化学表征、体外研究、分子对接和ADME-TOX

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-20 DOI: 10.1016/j.fitote.2026.107094

Cleiane Dias Lima , Marcelo da Costa Mota , Raimundo Leilton Santos Sousa , Luma Brisa Pereira dos Santos , Paulo Sérgio de Araujo Sousa , Raiza Raianne Luz Rodrigues , Klinger Antônio da Franca Rodrigues , Md Shimul Bhuia , Muhammad Torequl Islam , Alyne Rodrigues de Araújo-Nobre , Cláudia Quintino da Rocha , Jefferson Almeida Rocha

Leishmaniasis is a neglected tropical disease that affects millions of people worldwide, and current treatments are limited by toxicity and increasing parasite resistance, highlighting the need for new therapeutic agents. Montrichardia linifera, a plant used in traditional medicine, has shown relevant antiparasitic potential. This study evaluated the antileishmanial activity of acetone (EAMl), ethyl acetate (EAEMl), and ethanolic (EEMl) extracts of M. linifera. Chemical characterization was performed by liquid chromatography–mass spectrometry (LC–MS), and complementary in silico ADME/Tox predictions and molecular docking analyses were conducted. Antileishmanial activity was assessed against Leishmania (L.) major promastigotes using the MTT assay, and ultrastructural alterations were analyzed by atomic force microscopy (AFM). LC–MS results showed that EAEMl was the most chemically diverse extract, with quercetin identified as a major constituent. EAEMl exhibited the highest antipromastigote activity, with an IC₅₀ value of 20.30 μg/mL. AFM analysis revealed severe morphological damage in treated parasites, including membrane disruption and cell retraction. In silico analyses indicated favorable pharmacokinetic profiles for the main compounds. Molecular docking identified corilagin as the compound with the strongest affinity for pteridine reductase 1 (PTR1; PDB ID: 1E7W), with a binding energy of –10.9 kcal/mol. Overall, these findings demonstrate that M. linifera extracts, particularly those rich in phenolic compounds, exhibit promising antileishmanial activity, supporting their potential as sources of new therapeutic candidates.

利什曼病是一种被忽视的热带病，影响着全世界数百万人，目前的治疗受到毒性和寄生虫耐药性增加的限制，这突出表明需要新的治疗药物。传统药用植物蒙卡迪亚（Montrichardia linifera）显示出相应的抗寄生虫潜力。摘要本研究评价了黄皮草丙酮（EAMl）、乙酸乙酯（EAEMl）和乙醇（EEMl）提取物的抗利什曼原虫活性。通过液相色谱-质谱（LC-MS）进行化学表征，并进行互补的计算机ADME/Tox预测和分子对接分析。采用MTT法测定其抗利什曼原虫（L.）的活性，并用原子力显微镜（AFM）观察其超微结构变化。LC-MS结果表明，EAEMl是化学成分最多样化的提取物，槲皮素是其主要成分。EAEMl具有最高的抗promastigote活性，IC₅0值为20.30 μg/mL。AFM分析显示，处理后的寄生虫出现了严重的形态学损伤，包括膜破坏和细胞收缩。硅分析表明，主要化合物具有良好的药代动力学特征。分子对接鉴定出corilagin是对蝶啶还原酶1 （PTR1; PDB ID: 1E7W）亲和力最强的化合物，结合能为-10.9 kcal/mol。总的来说，这些发现表明，亚麻荠提取物，特别是那些富含酚类化合物的提取物，表现出有希望的抗利什曼原虫活性，支持它们作为新治疗候选物的潜力。

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引用次数: 0

Bioprospecting of endophytic fungi from medicinal plants as a source of antimicrobial agents: In vitro evaluation, metabolite profiling, and docking-based elucidation 药用植物内生真菌作为抗菌药物来源的生物勘探：体外评价、代谢物谱分析和基于对接的解析

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-20 DOI: 10.1016/j.fitote.2026.107104

Shaymaa Ahmed Gouda , E.A. Gamal , Hanaa Mohamed Gouda , Ahmed A.M.A. Selim

The emergence of microbial resistance to antimicrobial agents emphasizes the need to discover new ones. The potential use of endophytic fungi as a source of antimicrobial agents and their mode of action has not been fully explored. Thus, this research aimed to evaluate the antimicrobial activity of 16 endophytic fungal species isolated from some plants collected from Wadi Hagul, Egypt, along with assessing the mechanism of action of the most active one. Alternaria E15 was the most effective fungus against S. aureus with an MIC of 321.5 μgmL⁻¹, E. coli, A. niger with MICs of 1250 μgmL⁻¹, and C. albicans with an MIC of 2500 μgmL⁻¹. It was identified morphologically and molecularly as Alternaria alternata (accession no. PX106371). Sorbitol protection and ergosterol-binding assays indicated that its ethyl acetate extract does not target the fungal cell wall but acts through direct ergosterol binding in the fungal membrane. LC/MS analysis of A. alternata extract revealed seventeen major compounds belonging to different antimicrobial chemical classes. The docking studies on CYP51 and Penicillin-Binding Protein 3 showed that Okanin4-(6-acetylglucoside) and alternariol (docking scores −11.957 and − 7.009, respectively) may inhibit fungal ergosterol biosynthesis, while Okanin4-(6-acetylglucoside) and altenusin may inhibit bacterial cell wall synthesis (docking scores −8.537 and − 8.019, respectively). This study highlights, for the first time to our knowledge, the investigation of Egyptian endophytic fungi isolated from certain plants as a potential source for antimicrobial products, with an understanding of the responsible compounds and their mechanisms supporting their potential use in developing novel medicinal applications.

微生物对抗菌素耐药性的出现强调了发现新抗菌素的必要性。内生真菌作为抗菌药物来源的潜在用途及其作用方式尚未得到充分探索。因此，本研究旨在评价从埃及Wadi Hagul部分植物中分离得到的16种内生真菌的抑菌活性，并对活性最强的一种真菌的作用机制进行评价。对金黄色葡萄球菌MIC为321.5 μgmL−1，对大肠杆菌、黑曲霉MIC为1250 μgmL−1，对白色念珠菌MIC为2500 μgmL−1效果最好。经形态学和分子鉴定为Alternaria alternata（品种号：Alternaria alternata）。PX106371)。山梨糖醇保护和麦角甾醇结合实验表明，其乙酸乙酯提取物不靶向真菌细胞壁，而是通过麦角甾醇在真菌膜上的直接结合起作用。液相色谱/质谱分析结果显示，花楸提取物中含有17种主要的抗菌化学成分。CYP51与青霉素结合蛋白3的对接研究表明，Okanin4-（6-乙酰葡萄糖苷）和alternariol（对接评分分别为- 11.957和- 7.009）可能抑制真菌麦角甾醇的生物合成，而Okanin4-（6-乙酰葡萄糖苷）和altenusin可能抑制细菌细胞壁的合成（对接评分分别为- 8.537和- 8.019）。据我们所知，这项研究首次强调了从某些植物中分离出来的埃及内生真菌作为抗菌产品的潜在来源的调查，并了解了相关化合物及其机制，支持了它们在开发新型药物应用方面的潜在用途。

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引用次数: 0

Vladimiria souliei alleviated ethanol induced gastric ulcer through inhibition of RIP1-RIP3-MLKL necrosome activation Vladimiria soulie通过抑制RIP1-RIP3-MLKL坏死体活化来缓解乙醇诱导的胃溃疡。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-19 DOI: 10.1016/j.fitote.2026.107102

Xiaojing Wei , Binjing Zhao , Xinyi Jiang , Lunli Lan , Rui Wang , Yuanyuan Li

Vladimiria souliei(Franch.)Ling is used as medicine with dried roots, which is a perennial herb in Asteraceae family. It has been generally applied as traditional Chinese medicine with relieving abdominal swelling or pain, and treatment of digestive system disease. However, the pharmacological mechanism of alleviating gastric ulcer (GU) for this herb were still unknown. UPLC-Q-TOF/MS was performed to analyze the main components of Vladimiria souliei extract (VSE). Based on the results of histopathological observation, cytokines assay, and immunohistochemistry staining, the therapeutic effect of VSE on ethanol-induced GU was appraised. Meanwhile, the CCK-8, LDH assay and crystal violet staining were assessed to evaluate the appropriate concentration of VSE in vitro. In GES-1 cells induced by ethanol, the cell viability, ROS and cell membrane damage assay were detected after the interference of VSE. Then, several pivotal proteins relating to necroptosis in GES-1 were evaluated through immunofluorescence staining to illustrate the further pharma-cological mechanisms. As a result, VSE significantly restrained the expansion of ulcer area, reduced the pepsin activity, restored the levels of SOD, decreased the levels of MDA, ROS, TNF-α, IL-1β, IL-6, and IL-18, ultimately ameliorated the gastric mucosa injury. Further analysis exhibited that VSE significantly inhibited the cellular necroptosis by down-regulating the levels of RIP1, RIP3 and MLKL. Conclusions: This research clarified that the VSE could improve gastric mucosal injury through inhibition of RIP1-RIP3-MLKL necrosome activation, which might provide scientific evidences on the application of Vladimiria souliei as a ethnic herb to ameliorate GU.

Vladimiria souliei(法语)。凌是菊科多年生草本植物，干根成药。它已被普遍应用为中药，缓解腹部肿胀或疼痛，并治疗消化系统疾病。但其缓解胃溃疡的药理机制尚不清楚。采用UPLC-Q-TOF/MS对Vladimiria souliei提取物（VSE）的主要成分进行了分析。通过组织病理学观察、细胞因子测定和免疫组化染色，评价VSE对乙醇性GU的治疗效果。同时通过CCK-8法、LDH法、结晶紫染色法评价体外适宜的VSE浓度。在乙醇诱导的GES-1细胞中，VSE干扰后检测细胞活力、ROS和细胞膜损伤测定。然后，通过免疫荧光染色评估GES-1中与坏死性下垂相关的几个关键蛋白，以进一步阐明药理学机制。结果表明，VSE能明显抑制溃疡面积扩大，降低胃蛋白酶活性，恢复SOD水平，降低MDA、ROS、TNF-α、IL-1β、IL-6、IL-18水平，最终改善胃黏膜损伤。进一步分析发现，VSE通过下调RIP1、RIP3和MLKL水平，显著抑制细胞坏死。结论：本研究阐明了VSE可通过抑制RIP1-RIP3-MLKL坏死体活化改善胃黏膜损伤，为红参作为民族药改善GU的应用提供科学依据。

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引用次数: 0

Identification of secondary metabolites in polar organic extract of the fungus Cladobotryum virescens (Hypocreaceae, Ascomycota) by UHPLC-ESI-MS/MS: Cytotoxic and mutagenic activity 超高效液相色谱- esi -MS/MS法鉴定真菌Cladobotryum virescens （Hypocreaceae, Ascomycota）极性有机提取物的次生代谢物：细胞毒和诱变活性

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-19 DOI: 10.1016/j.fitote.2026.107101

Giselle Hernández , Luis A. Osoria , Beatriz Ramos , Trina H. García , Yarelis Ortiz , Yamilet Coll , Angel D. Vizcaino , Melissa R. Dupuig , Rafael F. Castañeda , Jared S. Goldman , Iraida Spengler , Antonio Francioso

The genus Cladobotryum is known for causing cobweb disease in edible mushroom crops. Its parasitic nature has prompted interest in its biocontrol potential and ability to produce cytotoxic compounds. The aim of this study was to identify secondary metabolites in a metahnolic extract of Cladobotryum virescens G.R.W. Arnold, and to evaluate its cytotoxicity against four cancer cell lines and its mutagenic effect in vitro. The chemical identification of metabolites was conducted using ultra-high performance liquid chromatography electrospray ionization-tandem mass spectrometry (UHPLC-ESI-MS/MS) in negative ionization mode. Cytotoxicity was assessed via MTT assay on MCF-7, MDA-MB-231 (both breast cancer), H460 (lung cancer), and L1210 (murine lymphocytic leukemia line) cell lines. A bacterial reversion test using Salmonella typhimurium strains TA98 and TA100 (Ames' test) was carried out to evaluate mutagenicity. UHPLC-ESI-MS/MS analysis allowed us to tentatively identify a total of 13 compounds in the extract, including polyketides, anthraquinones, and polyphenols mainly glycosylated flavonoids, among others. The methanolic extract of C. virescens showed significant dose-dependent cytotoxic against various cancer cell lines (IC₅₀ = 5.02, 50.15, 12.05 μg/mL for MCF-7, MDA-MB-231, and L1210, respectively) and remarkable primary mutagenic potential. These findings highlight the bioactive potential of C. virescens as a promising source of secondary metabolites for cancer treatment. Particularly, antioxidants may play a role in their cytotoxic effect and support further exploration of Cladobotryum species as a source of biologically active compounds.

Cladobotryum属因在食用菌作物中引起蛛网病而闻名。它的寄生特性引起了人们对其生物防治潜力和产生细胞毒性化合物的能力的兴趣。本研究旨在鉴定绿枝绿枝（Cladobotryum virescens G.R.W. Arnold）代谢提取物的次生代谢产物，并评价其对四种癌细胞的细胞毒性及其体外诱变作用。采用超高效液相色谱-电喷雾-串联质谱（UHPLC-ESI-MS/MS）负电离模式对代谢物进行化学鉴定。通过MTT法对MCF-7、MDA-MB-231（两种乳腺癌）、H460（肺癌）和L1210（小鼠淋巴细胞白血病系）细胞系进行细胞毒性评估。采用鼠伤寒沙门菌TA98和TA100菌株（Ames试验）进行细菌逆转试验，评价其致突变性。UHPLC-ESI-MS/MS分析初步鉴定出13种化合物，包括多酮类化合物、蒽醌类化合物和以糖基化黄酮类化合物为主的多酚类化合物等。绿草醇提物对多种肿瘤细胞系的细胞毒性表现出明显的剂量依赖性（MCF-7、MDA-MB-231和L1210的IC50分别为 = 5.02、50.15、12.05 μg/mL）和显著的初致突变潜力。这些发现突出了绿芽草作为癌症治疗次级代谢物的潜在生物活性。特别是，抗氧化剂可能在其细胞毒性作用中发挥作用，并支持进一步探索枝状纲物种作为生物活性化合物的来源。

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引用次数: 0

Quinones from Rubia manjith and their antitumor activity 芒草中醌类成分及其抗肿瘤活性研究。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-19 DOI: 10.1016/j.fitote.2026.107097

Yan-Fei Xu , Yun-Jie Wang , Zhuo-Tao Li , Li-Yuan Shi , Qia Wang , Ning-Hua Tan , Xue-Jia Zhang , Li Feng , Zhe Wang

Rubia plants, well-recognized as medicinal resources, are characterized by diverse phytoconstituents and a broad spectrum of biological activities, and have traditionally been employed in managing various diseases. R. manjith, a representative species of the genus Rubia enriched with quinone derivatives, has long been used in traditional Chinese medicine for the treatment of hematemesis, hematuria, inflammation, ulcers, and dermatological disorders. However, up to now, no research on the chemical components of this plant has been carried out. The present study focuses on the quinone constituents of R. manjith with the aim of identifying potential anti-tumor agents. From the roots and rhizomes of R. manjith, four previously undescribed anthraquinones (1–4), together with thirty-one known quinones (5–35), were successfully isolated and identified. Their cytotoxic activities were assessed against several colorectal cancer cell lines, among which 6 exhibited pronounced antiproliferative effects. Furthermore, network pharmacology analysis in combined with molecular docking was employed to elucidate the potential mechanisms underlying the anti-tumor activity of 6.

Rubia植物是公认的药用资源，具有多种植物成分和广泛的生物活性，传统上被用于治疗各种疾病。manjith是Rubia属的代表种，富含醌类衍生物，长期以来被用于治疗呕血、血尿、炎症、溃疡和皮肤病。然而，到目前为止，还没有对这种植物的化学成分进行研究。本文主要对蔓越藤中的醌类成分进行研究，以期发现潜在的抗肿瘤药物。从manjith的根和根茎中分离鉴定了4种未见的蒽醌类化合物（1-4）和31种已知的蒽醌类化合物（5-35）。对几种结直肠癌细胞株进行了细胞毒活性测定，其中6种具有明显的抗增殖作用。通过网络药理学分析结合分子对接，阐明了6。

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引用次数: 0

Chemical composition and evaluation of the antipsoriatic potential of Cistus sintenisii in mouse model 山楂的化学成分及抗银屑病作用的小鼠模型评价。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-19 DOI: 10.1016/j.fitote.2026.107103

Dionysia Alvanou , Ekaterina-Michaela Tomou , Maria Anagnostou , Christina Barda , Anastasia-Ioanna Papantonaki , Ioannis Sfiniadakis , Jane Anastassopoulou , Andreas Tzakos , Michail Rallis , Helen Skaltsa

Cistus species have been used in the treatment of various ailments, including skin disorders in the traditional medicine. The present study aimed to evaluate the antipsoriatic potential of Cistus sintenisii extracts, using an imiquimod-induced psoriasis mouse model. The most promising effects were observed in the highest concentrations of the extracts, which attenuated psoriatic alterations, such as hyperplasia of the epidermis and inflammation and improved epidermal structure. Furthermore, reduction of approximately 50% in the Psoriasis Area and Severity Index (PASI) score on day 6 indicated a favorable clinical response along with the histological outcomes. In addition, the chemical composition of the aqueous extract was studied, and nine compounds were isolated and identified, namely catechin, quercetin 3-O-α-L-rhamnoside, myricetin 3-O-α-L-rhamnoside, myricetin 3-O-α-L-arabinoside, myricetin 3-O-β-D-galactoside, gallic acid, shikimic acid, protocatechuic acid, and gentisic acid 5-O-β-D-xyloside. These findings may play a key role in the therapeutic potency of C. sintenisii against psoriasis, as well as support the traditional use of Cistus species in treating skin disorders.

山竹属植物已被用于治疗各种疾病，包括传统医学中的皮肤病。本研究旨在利用吡喹莫德诱导的银屑病小鼠模型，评价山竹提取物的抗银屑病潜力。在最高浓度的提取物中观察到最有希望的效果，它可以减轻银屑病的改变，如表皮增生和炎症，并改善表皮结构。此外，在第6天，银屑病面积和严重程度指数（PASI）评分减少了约50%，表明临床反应良好，组织学结果良好。此外，对水提物的化学成分进行了研究，分离鉴定出儿茶素、槲皮素3-O-α- l -鼠李糖、杨梅素3-O-α- l -鼠李糖、杨梅素3-O-α- l -阿拉伯糖、杨梅素3-O-β- d -半乳糖苷、没食子酸、草酸、原儿茶酸、龙胆酸5-O-β- d -木糖苷等9个化合物。这些发现可能在银屑病的治疗效力中发挥关键作用，并支持传统使用山竹属治疗皮肤病。

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引用次数: 0

Metabolomic and cheminformatic study of Sida hyssopifolia: A first record of potential multi-target antidiabetic compounds and chemotaxonomic comparison with Sida glabra and Sida rhombifolia 石竹的代谢组学和化学信息学研究：潜在的多靶点抗糖尿病化合物的首次记录以及与石竹和石竹的化学分类比较。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-19 DOI: 10.1016/j.fitote.2026.107100

Cecilia I. Mayo-Montor , Juan F. Avellaneda-Tamayo , Abraham Vidal-Limon , Oscar Carmona-Hernández , José Martín Barreda-Castillo , Víctor Manuel Loyola-Vargas , José L. Medina-Franco , Juan L. Monribot-Villanueva , José A. Guerrero-Analco

The Mexican cloud forest harbors an exceptional diversity of vascular plants, most of which remain unexplored. Sida hyssopifolia C.Presl (Malvaceae) is reported for the first time in this ecosystem and was chemically characterized in this study. S. hyssopifolia methanolic extract showed in vitro inhibitory activity to α-amylase (αA, IC₅₀ = 0.02 mg/mL), α-glucosidase (αG, IC₅₀ < 1 × 10⁻⁶ mg/mL), and dipeptidyl peptidase-IV (DPP-IV, IC₅₀ = 0.92 mg/mL), and low acute toxicity in the Artemia salina test (LC₅₀ = 1.33 mg/mL). Using UPLC-MS/MS-based untargeted metabolomics, 550 metabolites were putatively annotated (MSI-levels 2–4). Paired comparisons between S. hyssopifolia vs. S. glabra and S. hyssopifolia vs. S. rhombifolia allowed the identification of 54 metabolites as exclusively accumulated in S. hyssopifolia (fold change ≥2; P ≤ 0.05). In addition, 18 metabolites were determined by OPLS-DA as the most important compounds in S. hyssopifolia compared to the related species (VIP-scores >1). The Bemis-Murcko scaffold analysis revealed potential enrichment in flavonoid glycosides and triterpene-related metabolites. Additionally, by UPLC-MS/MS-based targeted metabolomics it was confirmed the differential accumulation of 19 phenolic compounds (MSI-level 1). Furthermore, 13 accumulated compounds of S. hyssopifolia (MSI-levels 1–2, fold change ≥2, P ≤ 0.05) stood out since have been reported as αA, αG, and/or DPP-IV in vitro inhibitors. Integration of metabolomics and cheminformatics suggested S. hyssopifolia as a potential source of multi-target antidiabetic natural products. These findings provide insights into its chemotaxonomic character and underscore the significance of the Mexican cloud forest as a potential source of biologically active plants.

墨西哥的云雾森林蕴藏着极其多样的维管植物，其中大部分尚未被探索过。本研究在该生态系统中首次报道并对其进行了化学表征。美国hyssopifolia methanolic提取显示体外抑制活性α淀粉酶(α,IC50 =  0.02毫克/毫升),α葡糖苷酶(αG, IC50 50 =  0.92毫克/毫升),卤虫盐沼和低的急性毒性试验(LC50 =  1.33毫克/毫升)。使用UPLC-MS/MS-based非靶向代谢组学，对550种代谢物进行了推定注释（MSI标准水平2-4）。通过对深槐与光叶深槐、深槐与弯叶深槐的配对比较，鉴定出54种代谢物仅在深槐中积累（倍差≥2；P ≤ 0.05）。此外，通过OPLS-DA测定，18种代谢物与近缘种相比是最重要的化合物（vip评分为>.1）。Bemis-Murcko支架分析显示黄酮类苷和三萜相关代谢物可能富集。此外，通过UPLC-MS/MS-based靶向代谢组学，证实了19种酚类化合物的差异积累（MSI标准1级）。此外，有13个累积化合物（msi水平为1-2，倍数变化≥2，P ≤ 0.05）作为αA、αG和/或DPP-IV的体外抑制剂被报道。代谢组学和化学信息学的综合研究表明，金丝桃是多靶点抗糖尿病天然产物的潜在来源。这些发现提供了对其化学分类特征的见解，并强调了墨西哥云雾林作为生物活性植物潜在来源的重要性。

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引用次数: 0

Alstotriamine A, a triamino monoterpene indole alkaloid with an unprecedented pentacyclic caged skeleton and anti-inflammatory alkaloids from Alstonia mairei Alstotriamine A，一种具有前所未有的五环笼状骨架的三氨基单萜吲哚生物碱和抗炎生物碱，来自Alstonia marei。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2026-01-18 DOI: 10.1016/j.fitote.2026.107099

Pengfei Jin , Guijuan Zheng , Yimiao Chen , Xinqiao Liu , Song Hu

A novel triamino monoterpene indole alkaloid, alstotriamine A (1), a new monoterpene indole alkaloid (2), and five known analogues (3–7) were isolated from the branches and leaves of Alstonia mairei. Their structures were elucidated via extensive spectroscopic methods and quantum chemical calculations including the ¹³C NMR-DP4+ analysis and electronic circular dichroism (ECD) calculations. Alstotriamine A (1), possessing an unprecedented pentacyclic caged skeleton incorporating with a third nitrogen atom, represents the first example of C-3 and C-17 cyclic corynanthe alkaloid, and a plausible biosynthetic pathway was proposed. Furthermore, compounds 1, 2, 5, and 7 displayed significant inhibitory effects on the LPS-induced NO production in RAW264.7 mouse macrophages with IC₅₀ values ranging from 4.6 to 16.2 μM, and the active compounds 2 and 5 dose-dependently decreased the levels of the pro-inflammatory cytokines TNF-α and IL-6.

从Alstonia marei的枝叶中分离得到了一种新的三氨基单萜吲哚生物碱alstotriamine A(1)、一种新的单萜吲哚生物碱alstotriamine A(2)和5种已知的类似物（3-7）。通过广泛的光谱方法和量子化学计算，包括13C NMR-DP4+分析和电子圆二色性（ECD）计算，阐明了它们的结构。Alstotriamine A(1)具有前所未有的含有第三个氮原子的五环笼状骨架，是第一个C-3和C-17环角缕草生物碱的例子，并提出了一种合理的生物合成途径。此外，化合物1、2、5和7对lps诱导的RAW264.7小鼠巨噬细胞NO生成具有显著的抑制作用，IC50值在4.6 ~ 16.2 μM之间，活性化合物2和5呈剂量依赖性地降低促炎细胞因子TNF-α和IL-6的水平。

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引用次数: 0