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Coumarins and the science of timeless beauty: A natural anti-skin aging solution 香豆素和永恒美丽的科学:一种天然的抗皮肤衰老的解决方案。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-03-01 Epub Date: 2025-12-22 DOI: 10.1016/j.fitote.2025.107053
Yasser Fakri Mustafa

Background

Coumarins, naturally occurring benzopyrone derivatives, have long been valued in traditional medicine, fragrance industries, and therapeutics. Recent interest has surged around their anti-aging properties, particularly in skincare, due to their antioxidant, anti-inflammatory, and photoprotective effects.

Objective

This review explores the role of coumarins as promising agents in combating skin aging, offering a natural alternative to synthetic cosmetics and contributing to the development of safe, effective anti-aging products.

Methods

An integrative analysis of historical, biochemical, pharmacological, and cosmetic perspectives was conducted, supported by traditional medicine records, modern preclinical studies, bioinformatics predictions, and formulation case studies. Emphasis was placed on coumarins' mechanisms of action, extraction methods, safety profiles, and their application in skincare formulations.

Results

Coumarins act through both direct and indirect antioxidant mechanisms, targeting pathways involved in oxidative stress, inflammation, collagen degradation, and skin barrier dysfunction. Studies show that certain derivatives can inhibit MMPs and modulate sirtuin and AMPK pathways, mechanisms vital in anti-aging interventions. Traditional medicine has long leveraged coumarin-rich herbs to treat dermatological, circulatory, and neurodegenerative conditions. Case studies confirmed favorable cosmetic properties in formulations containing coumarins and hyaluronic acid. Comparative analysis with existing anti-aging ingredients revealed that coumarins provide multi-targeted, dermo-compatible action with fewer adverse effects. Despite regulatory constraints, coumarins remain widely used in skincare and perfumes, with growing interest in sustainable sourcing and green synthesis.

Conclusion

Coumarins represent a scientifically grounded, culturally enriched, and biologically potent class of compounds that align with modern demands for natural and effective anti-aging solutions. Their multifunctionality, favorable safety profile, and dermo-pharmacological compatibility support their potential as key agents in next-generation beauty products. Further interdisciplinary research and regulatory harmonization are essential for optimizing their use in cosmetic and therapeutic contexts.
背景:香豆素是天然存在的苯并吡酮衍生物,长期以来在传统医学、香料工业和治疗学中受到重视。由于其抗氧化、抗炎和光保护作用,最近对其抗衰老特性的兴趣激增,特别是在护肤方面。目的:探讨香豆素在抗皮肤衰老方面的作用,为合成化妆品提供一种天然的替代品,为开发安全、有效的抗衰老产品做出贡献。方法:结合传统医学记录、现代临床前研究、生物信息学预测和配方案例研究,从历史、生化、药理学和美容角度进行综合分析。重点介绍了香豆素的作用机制、提取方法、安全性及其在护肤配方中的应用。结果:香豆素通过直接和间接的抗氧化机制起作用,靶向氧化应激、炎症、胶原降解和皮肤屏障功能障碍等途径。研究表明,某些衍生物可以抑制MMPs并调节sirtuin和AMPK途径,这是抗衰老干预的重要机制。传统医学长期以来一直利用富含香豆素的草药来治疗皮肤病、循环系统和神经退行性疾病。案例研究证实含有香豆素和透明质酸的配方具有良好的化妆品特性。与现有抗衰老成分的对比分析表明,香豆素具有多靶向,皮肤相容的作用,副作用小。尽管受到监管限制,香豆素仍然广泛应用于护肤品和香水中,人们对可持续采购和绿色合成的兴趣日益浓厚。结论:香豆素代表了一种科学基础、文化丰富、生物有效的化合物,符合现代对天然有效抗衰老解决方案的需求。它们的多功能性、良好的安全性和皮肤-药理相容性支持它们作为下一代美容产品的关键制剂的潜力。进一步的跨学科研究和监管协调对于优化其在化妆品和治疗环境中的使用至关重要。
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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 Pub Date : 2026-03-01 Epub 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
Topical application of Calvatia lilacina ethanol extract-derived fraction promotes diabetic wound healing 局部应用丁香花乙醇提取物衍生部分促进糖尿病伤口愈合。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-03-01 Epub Date: 2026-01-02 DOI: 10.1016/j.fitote.2026.107087
Yan Li , Tiantian Dong , Tangtang He , Yurong Zhao , Chenxi Yang , Hanlu Xiao , Ruiwen Mo , Jun Chen , Jie Dong
Calvatia lilacina (CL), a traditional Chinese medicinal fungus, has been extensively used for wound healing for centuries. However, the specific effective components of CL remain unclear. This study investigated the phytochemical composition and diabetic wound healing activities of a novel ethanol extract-derived fractions from CL (CLP2). UHPLC-TOF-MS/MS phytochemical analysis revealed 14 active components in CLP2. HPLC analysis showed that ergosterol was the most prevalent component in CLP2, with a content of 837.3 μg/mg. CLP2 significantly accelerated wound healing in db/db diabetic mice, facilitated re-epithelialization and inhibited the polarization of M1 macrophages, downregulated the transcription levels of the inflammatory cytokines, and promoted the expression of anti-inflammatory factors. In vitro tests indicated that CLP2 can promote the proliferation and migration of mouse skin fibroblasts, suppress the expression of M1 macrophage-associated pro-inflammatory cytokines, and enhance M2 polarization. Additionally, in vivo and in vitro experiments confirmed that CLP2 accelerated diabetic wound healing by suppressing M1 macrophages and promoting the polarization of macrophages towards the M2 phenotype, facilitating a faster transition from the inflammatory stage to the proliferative stage. These results highlight CLP2 as a potential therapeutic intervention for diabetic wound healing.
丁香花(calvara lilacina, CL)是一种传统的中药真菌,几个世纪以来一直被广泛用于伤口愈合。然而,CL的具体有效成分尚不清楚。本研究研究了一种新型乙醇提取物(CLP2)的植物化学成分和糖尿病创面愈合活性。UHPLC-TOF-MS/MS植物化学分析显示,CLP2中有14种有效成分。HPLC分析显示,麦角甾醇是CLP2中含量最高的成分,含量为837.3 μg/mg。CLP2显著加速db/db糖尿病小鼠创面愈合,促进M1巨噬细胞再上皮化,抑制M1巨噬细胞极化,下调炎症因子转录水平,促进抗炎因子表达。体外实验表明,CLP2能促进小鼠皮肤成纤维细胞的增殖和迁移,抑制M1巨噬细胞相关的促炎细胞因子的表达,增强M2极化。此外,体内和体外实验证实,CLP2通过抑制M1巨噬细胞,促进巨噬细胞向M2表型极化,促进炎症期向增殖期更快过渡,从而加速糖尿病创面愈合。这些结果突出了CLP2作为糖尿病伤口愈合的潜在治疗干预。
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引用次数: 0
Botrychium ternatum, the Hmong medicinal flora, improves acetaminophen-induced hepatic injury by inhibiting the abnormal activation of the B cell receptor signaling pathway Botrychium ternatum是一种苗族药用植物,通过抑制B细胞受体信号通路的异常激活来改善对乙酰氨基酚诱导的肝损伤。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-03-01 Epub Date: 2026-01-23 DOI: 10.1016/j.fitote.2026.107096
Tao Chen , Ya-Ru Yang , Ming-Hui He , Xu Zhang , Shang-Gao Liao , Zhu Zeng , Yun-Guang Long , Yan Lin , Bo Tu

Aim of study

This study investigated the hepatoprotective effects of BT, its chemical composition, correlations with target components, and mechanisms underlying acetaminophen (APAP)-induced liver injury.

Materials and methods

APAP-induced injury models were established using HepG2 cells and C57BL/6 mice. Cell viability, cytotoxicity, levels of pro-inflammatory cytokines (IL-1β, TNF-α), apoptosis, and proliferation were evaluated through CCK-8, ELISA, flow cytometry, and EDU staining. In C57BL/6 mice model, measurements included body weight, liver index, serum levels of transaminases (ALT, AST) and ALP, and hepatic histopathology via H&E staining. Key signaling pathways were identified through RNA sequencing, KEGG/GO enrichment analyses, RT-qPCR, and Western blotting (WB). Chemical components of BT were analyzed using UHPLC-QE-Orbitrap HRMS, with subsequent molecular docking and dynamics simulations for studying component-target interactions.

Results

The findings indicated that BT (25/100 μg/mL in cells; 50/100/200 mg/kg in C57BL/6 mice model) significantly enhanced cell viability, reduced inflammatory cytokine levels and apoptosis, mitigated liver damage, and lowered serum enzyme levels in a dose-dependent manner. The B-cell receptor (BCR) signaling pathway emerged as crucial based on RNA sequencing, which was confirmed by WB and RT-qPCR. Analysis revealed forty-five compounds in BT, with kaempferitrin demonstrating consistent binding to LYN kinase (a key BCR pathway target) throughout 100 ns simulations.

Conclusions

In summary, BT demonstrates substantial hepatoprotective effects, potentially by suppressing the BCR signaling pathway, with kaempferitrin identified as a critical bioactive component targeting LYN kinase.
研究目的:本研究探讨了BT的肝保护作用、其化学成分、与靶成分的相关性以及对乙酰氨基酚(APAP)诱导肝损伤的机制。材料和方法:采用HepG2细胞和C57BL/6小鼠建立apap诱导的损伤模型。通过CCK-8、ELISA、流式细胞术和EDU染色评估细胞活力、细胞毒性、促炎细胞因子(IL-1β、TNF-α)水平、凋亡和增殖。C57BL/6小鼠模型测定体重、肝脏指数、血清转氨酶(ALT、AST、ALP)水平,H&E染色观察肝脏组织病理学变化。通过RNA测序、KEGG/GO富集分析、RT-qPCR和Western blotting (WB)鉴定关键信号通路。利用UHPLC-QE-Orbitrap HRMS分析了BT的化学成分,并进行了分子对接和动力学模拟,研究了组分与靶标的相互作用。结果:BT(细胞中25/100 μg/mL; C57BL/6小鼠模型中50/100/200 mg/kg)显著提高细胞活力,降低炎症细胞因子水平和细胞凋亡,减轻肝损伤,降低血清酶水平,呈剂量依赖性。基于RNA测序,WB和RT-qPCR证实了b细胞受体(BCR)信号通路是至关重要的。分析显示,在100次 ns模拟中,BT中有45种化合物,其中山柰素与LYN激酶(一个关键的BCR通路靶点)结合一致。结论:总之,BT显示出实质性的肝保护作用,可能是通过抑制BCR信号通路,山奈霉素被鉴定为针对LYN激酶的关键生物活性成分。
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引用次数: 0
Evaluation of sapogenin isolated from the defatted seeds of Camellia oleifera and its derivative as anti-breast cancer agents 油茶籽皂苷元及其衍生物抗乳腺癌作用的评价。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-03-01 Epub Date: 2025-12-27 DOI: 10.1016/j.fitote.2025.107075
Lu Li , Chuanqing Huang , Yunong Tian , Ying Wen , Meng Zhang , Yulin Liu , Shuhong Lin , Xianchun Hu , Yong Ye
The defatted seeds of Camellia oleifera are an underutilized resource that leads to poor economy. Saponins extracted from these seeds exhibit anti-breast cancer effects. To augment their anticancer efficacy, the saponins were structurally modified by the incorporation of a thiosemicarbazone moiety to yield the Camellia sapogenin thiosemicarbazone (CST). CST was subsequently complexed with zinc to form Zn-CST. This zinc complex demonstrated markedly enhanced antiproliferative and cytotoxic activity in ER+ / PR+ MCF-7 cells (IC₅₀ = 3.21 ± 0.44 μM) and HER2- T47D cells (IC₅₀ = 9.80 ± 1.31 μM), demonstrating greater potency than erlotinib. In MCF-7 cells, Zn-CST induced cell cycle arrest at the G₀ / G₁ phase and resulted in a 27-fold increase in apoptosis. Additionally, Zn-CST exhibited more potent inhibitory activity against EGFR kinase, with an IC₅₀ value of 0.25 ± 0.02 μM, compared to erlotinib. Molecular docking analysis confirmed Zn-CST's superior binding affinity for EGFR with a binding energy of −102.7 kcal/mol, predominantly due to a strong electrostatic interaction with Asp831. Collectively, these findings suggest that Zn-CST could be developed as anti ER+ / PR+ breast cancer candidate.
油茶的脱脂种子是一种未充分利用的资源,导致经济状况不佳。从这些种子中提取的皂苷具有抗乳腺癌的作用。为了增强其抗癌作用,我们对这些皂苷进行了结构修饰,加入了硫代氨基脲部分,得到了山茶皂苷基硫代氨基脲(CST)。CST随后与锌络合形成Zn-CST。这锌复杂了明显增强的抗增殖和细胞毒性活动ER + / PR + MCF-7细胞(IC₅₀ = 3.21 ±0.44  μM)和HER2 - T47D细胞(IC₅₀ = 9.80 ±1.31  μM),证明比埃罗替尼更大的力量。在MCF-7细胞中,Zn-CST诱导细胞周期阻滞在G 0 / G 1期,导致细胞凋亡增加27倍。此外,与厄洛替尼相比,Zn-CST对EGFR激酶表现出更强的抑制活性,IC₅₀值为0.25 ± 0.02 μM。分子对接分析证实,Zn-CST对EGFR具有较强的结合亲和力,结合能为-102.7 kcal/mol,这主要是由于与Asp831的强静电相互作用。总之,这些发现表明Zn-CST可以作为抗ER+ / PR+乳腺癌的候选药物。
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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 Pub Date : 2026-03-01 Epub 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 (14), together with thirty-one known quinones (535), 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。
{"title":"Quinones from Rubia manjith and their antitumor activity","authors":"Yan-Fei Xu ,&nbsp;Yun-Jie Wang ,&nbsp;Zhuo-Tao Li ,&nbsp;Li-Yuan Shi ,&nbsp;Qia Wang ,&nbsp;Ning-Hua Tan ,&nbsp;Xue-Jia Zhang ,&nbsp;Li Feng ,&nbsp;Zhe Wang","doi":"10.1016/j.fitote.2026.107097","DOIUrl":"10.1016/j.fitote.2026.107097","url":null,"abstract":"<div><div><em>Rubia</em> 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. <em>R. manjith</em>, a representative species of the genus <em>Rubia</em> 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 <em>R. manjith</em> with the aim of identifying potential anti-tumor agents. From the roots and rhizomes of <em>R. manjith</em>, four previously undescribed anthraquinones (<strong>1</strong>–<strong>4</strong>), together with thirty-one known quinones (<strong>5</strong>–<strong>35</strong>), were successfully isolated and identified. Their cytotoxic activities were assessed against several colorectal cancer cell lines, among which <strong>6</strong> 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 <strong>6</strong>.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107097"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146017995","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
Involvement of the NO-sGC/cGMP signaling pathway in the vasodilator and hypotensive effects of the ethanol-soluble fraction from Citrullus lanatus (Thunb.) Matsum. & Nakai seeds in rats NO-sGC/cGMP信号通路参与甜瓜醇溶部分的血管扩张和降压作用(Thunb.)Matsum。& Nakai种子在老鼠体内。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-03-01 Epub Date: 2025-12-23 DOI: 10.1016/j.fitote.2025.107041
Aline Aparecida Macedo Marques , Karyne Garcia Tafarelo Moreno , Luciane Barbosa Pessoa , Luana Ale Bertoncello Pael , Katiana Simões Kittelson , Ariany Carvalho dos Santos , Gabriela Pereira da Silva , Bianca Viana Silva , Maria Luiza Fidelis da Silva , Luana Bonifácio Sanches , Denise Brentan da Silva , Arquimedes Gasparotto Junior
The therapeutic management of hypertension involves both pharmacological and non-pharmacological interventions. However, control remains inadequate despite effective treatments, often due to poor adherence. In this context, herbal medicines offer a complementary approach to conventional therapy. Citrullus lanatus (watermelon) seeds, frequently discarded as agricultural byproducts, represent a promising source of bioactive compounds. This study evaluated the cardiorenal properties of three extracts obtained from dried C. lanatus seeds, including an ethanol-soluble fraction from an aqueous extract (ESCL), a hydroethanolic extract, and an aqueous extract obtained by turbolysis. These extracts were chemically characterized using liquid chromatography coupled with diode array detection and mass spectrometry. Diuretic and hypotensive activities were assessed in vivo in normotensive female Wistar rats, while vasodilatory mechanisms were investigated ex vivo in isolated mesenteric vascular beds. Among the preparations screened, only the ESCL fraction displayed significant cardiorenal activity, reducing blood pressure and peripheral vascular resistance. Mechanistic investigation revealed that this vascular response is mediated via the nitric oxide/soluble guanylate cyclase/cyclic guanosine monophosphate signaling cascade. These findings highlight the pharmacological potential of ESCL as a candidate for the development of novel hypotensive agents.
高血压的治疗管理包括药物和非药物干预。然而,尽管有有效的治疗,但控制仍然不足,这往往是由于依从性差。在这种情况下,草药为传统疗法提供了一种补充方法。作为农业副产品经常被丢弃的西瓜种子是一种很有前途的生物活性化合物来源。本研究评估了三种从干羊草种子中提取的提取物的心肾特性,包括水提取物(ESCL)的乙醇溶性部分,氢乙醇提取物和通过涡轮分解获得的水提取物。利用液相色谱、二极管阵列检测和质谱法对这些提取物进行了化学表征。在正常血压的雌性Wistar大鼠体内评估利尿和降压活性,并在离体肠系膜血管床中研究血管舒张机制。在筛选的制剂中,只有ESCL组分显示出显著的心肾活性,降低血压和外周血管阻力。机制研究表明,这种血管反应是通过一氧化氮/可溶性鸟苷环化酶/环鸟苷单磷酸信号级联介导的。这些发现突出了ESCL作为开发新型降压药物的候选药物的药理学潜力。
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引用次数: 0
A novel compound mixture mitigates hyperglycemia, insulin resistance, dyslipidemia, and oxidative stress in streptozotocin induced diabetic rats: A therapeutic drug lead for metabolic syndrome 一种新型化合物混合物可减轻链脲佐菌素诱导的糖尿病大鼠的高血糖、胰岛素抵抗、血脂异常和氧化应激:一种代谢综合征的治疗药物。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-03-01 Epub Date: 2026-01-11 DOI: 10.1016/j.fitote.2026.107091
Thushara Indika Sampath , Susanthi Jayasinghe , Anoja Priyadarshani Attanayake , Veranja Karunaratne
Plant-derived bioactive compounds play a crucial role in managing metabolic syndrome (MetS) components such as hyperglycemia, insulin resistance, and atherogenic dyslipidemia. The present study investigates the glucose and lipid lowering potential of a novel compound mixture composed of garcinol, piperine, butyl oleate, pipnoohine, and bismurrayanimbine (molar ratio of 9:33:1:4:1) and its effects on insulin resistance and atherogenic indices in streptozotocin induced (60 mgkg−1, ip) diabetic rats. The oral administration of the compound mixture at low (10 mgkg−1), therapeutic (25 mgkg−1), and high (50 mgkg−1) doses resulted in dose-dependent improvement in oral glucose tolerance with an increase of 6%, 9%, and 12%, respectively. There was a corresponding elevation in serum insulin (4%, 66%, 66%) and C-peptide (18%, 152%, 153%), along with reduction in serum fasting glucose (8%, 29%, 30%) and percentage of HbA1C (18%, 27%, 31%) compared to diabetic untreated rats (p < 0.05). Histopathological assessment of H and E-stained sections of the pancreatic tissue confirmed islet cell restoration. At the therapeutic dose, the mixture reduced homeostatic model assessment of insulin resistance (HOMA-IR) and increased homeostatic model assessment of β-cell functions (HOMA-β), aligning with pancreatic functions. Furthermore, all doses improved the antioxidant status and reversed atherogenic dyslipidemia in diabetic rats. Biochemical analysis revealed significant improvement in hepatic hexokinase activity at 25 and 50 mgkg−1 doses (p < 0.05). Overall, the compound mixture showed promising results as an adjunct therapy for managing hyperglycemia and atherogenic dyslipidemia associated with MetS, highlighting its potential to be developed as a therapeutic agent.
植物源性生物活性化合物在控制代谢综合征(MetS)成分(如高血糖、胰岛素抵抗和动脉粥样硬化性血脂异常)中起着至关重要的作用。本文研究了由garcinol、胡椒碱、油酸丁酯、胡椒碱和双氰胺(摩尔比为9:33:1:4:1)组成的新型复方降糖降脂潜能及其对链脲佐菌素(60 mg -1, ip)诱导的糖尿病大鼠胰岛素抵抗和动脉粥样硬化指标的影响。口服低剂量(10毫克-1)、治疗剂量(25毫克-1)和高剂量(50毫克-1)的复方混合物可导致口服葡萄糖耐量的剂量依赖性改善,分别增加6%、9%和12%。与未治疗的糖尿病大鼠相比,血清胰岛素(4%,66%,66%)和c肽(18%,152%,153%)相应升高,血清空腹血糖(8%,29%,30%)和HbA1C百分比(18%,27%,31%)降低(p -1剂量(p
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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 Pub Date : 2026-03-01 Epub 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 (37) 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。
{"title":"Alstotriamine A, a triamino monoterpene indole alkaloid with an unprecedented pentacyclic caged skeleton and anti-inflammatory alkaloids from Alstonia mairei","authors":"Pengfei Jin ,&nbsp;Guijuan Zheng ,&nbsp;Yimiao Chen ,&nbsp;Xinqiao Liu ,&nbsp;Song Hu","doi":"10.1016/j.fitote.2026.107099","DOIUrl":"10.1016/j.fitote.2026.107099","url":null,"abstract":"<div><div>A novel triamino monoterpene indole alkaloid, alstotriamine A (<strong>1</strong>), a new monoterpene indole alkaloid (<strong>2</strong>), and five known analogues (<strong>3</strong>–<strong>7</strong>) were isolated from the branches and leaves of <em>Alstonia mairei</em>. Their structures were elucidated <em>via</em> extensive spectroscopic methods and quantum chemical calculations including the <sup>13</sup>C NMR-DP4+ analysis and electronic circular dichroism (ECD) calculations. Alstotriamine A (<strong>1</strong>), 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 <strong>1</strong>, <strong>2</strong>, <strong>5</strong>, and <strong>7</strong> displayed significant inhibitory effects on the LPS-induced NO production in RAW264.7 mouse macrophages with IC<sub>50</sub> values ranging from 4.6 to 16.2 μM, and the active compounds <strong>2</strong> and <strong>5</strong> dose-dependently decreased the levels of the pro-inflammatory cytokines TNF-<em>α</em> and IL-6.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107099"},"PeriodicalIF":2.6,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146009450","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
Astracondensatols F–L, cycloartane triterpenoids from Astragalus condensatus with their anti-inflammatory potential astracondensatol F-L:从黄芪中提取的环artane三萜,具有抗炎作用。
IF 2.6 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2026-03-01 Epub Date: 2025-12-25 DOI: 10.1016/j.fitote.2025.107071
Fadime Aydoğan , Merve Inci Camci , Jin Zhang , Jianping Zhao , Nirmal D. Pugh , Ikhlas A. Khan , Zulfıqar Ali
Phytochemical investigation on the roots of Astragalus condensatus (Fabaceae) led to the isolation of seven previously undescribed cycloartane-type triterpenoids, named astracondensatols F–L (1–7), alongside twelve known cycloartane derivatives (8–19) and fifteen other known secondary metabolites (20–34). The structures of these compounds were elucidated through comprehensive spectroscopic analysis, including 1D and 2D NMR, as well as high-resolution electrospray ionization mass spectrometry (HRESIMS). The isolated triterpenoids were evaluated for their effect on nuclear factor kappa B (NF-κB)-driven luciferase expression in THP-1 monocytes stimulated with Escherichia coli lipopolysaccharide (LPS). Five compounds (3, 4, 8, 10, and cyclocephagenol) demonstrated a dose-dependent suppression of NF-κB activation. Notably, these effects were non-selective, as they also inhibited Sp-1 control activity similarly.
通过对豆科植物黄芪(Astragalus consatus)根的植物化学研究,分离出7种以前未被描述的环artane-type三萜,命名为astracondensatols F-L(1-7),以及12种已知的环artane衍生物(8-19)和15种其他已知的次生代谢产物(20-34)。这些化合物的结构通过综合光谱分析,包括一维和二维核磁共振,以及高分辨率电喷雾电离质谱(hresms)进行了阐明。用大肠杆菌脂多糖(LPS)刺激THP-1单核细胞,观察分离得到的三萜对核因子κB (NF-κB)驱动的荧光素酶表达的影响。5种化合物(3、4、8、10和环肾上腺素)显示出对NF-κB活化的剂量依赖性抑制。值得注意的是,这些影响是非选择性的,因为它们也同样抑制了Sp-1的控制活性。
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