Natural Products and Bioprospecting最新文献_第4页

Metabolomics reveal how strong water binding naturally enhances wheat seed longevity and Fusarium resistance 代谢组学揭示了强水结合如何自然增强小麦种子寿命和抗镰刀菌性

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2026-01-09 DOI: 10.1007/s13659-025-00559-y

Lorenzo Goglia, Vito Campanella, Agata Rascio

Seed water content affects wheat quality, storage, and food safety, influencing viability and fungal contamination risks. Grain moisture is influenced by both genetic and environmental factors, with agronomic practices aiming to optimize it. However, no genotype has been specifically developed for enhanced seed water properties, as the underlying biochemical and genetic mechanisms remain unclear. Using a durum wheat mutant (WM) with higher water affinity of leaves, compared to its wild-type cultivar, Trinakria (WT), this study investigates the biophysical and biochemical mechanisms affecting seed performance. Genotypic characterization of unaged seeds includes differential scanning calorimetry, metabolomic profiling, and functional analyses of water uptake rate, dehydration rate, and seed coat electrical resistance. Germination and Fusarium resistance were examined, too in both unaged and aged seeds. As for the leaves, WM seeds exhibit higher water-binding strength than WT. Metabolomic analysis revealed a higher polar/apolar ratio in WM (83 vs. 72 in WT), with significantly greater myo-inositol and raffinose content and lower levels of unsaturated fatty acids. No differences in seed imbibition velocity or dehydration velocity were observed, but WM showed lower seed coat electrical resistance, indicating greater free water retention on the seed surface. Under low Fusarium inoculum concentrations or in the absence of pathogens, aged WM seeds showed higher germination rates and vigor than WT. As an inherited trait, selecting for strong water-binding capacity, increased osmoprotective compounds, and lower unsaturated acid content could contribute sustainably improve seed longevity and Fusarium resistance.

Graphical Abstract

种子含水量影响小麦品质、贮藏和食品安全，影响种子活力和真菌污染风险。粮食水分受到遗传和环境因素的双重影响，农艺实践旨在优化粮食水分。然而，由于潜在的生化和遗传机制尚不清楚，没有专门开发用于增强种子水分特性的基因型。以叶片亲水性较高的硬粒小麦突变体（WM）为研究对象，探讨了影响其种子性能的生物物理和生化机制。未老化种子的基因型特征包括差示扫描量热法、代谢组学分析、吸水率、脱水率和种皮电阻的功能分析。对未老化和老化种子的萌发和抗镰刀菌性进行了研究。就叶片而言，WM种子的水结合强度高于WT。代谢组学分析显示WM种子的极性/极性比更高（83比72），肌醇和棉子糖含量显著增加，不饱和脂肪酸水平较低。籽粒吸胀速率和脱水速率无显著差异，但WM的种皮电阻较低，表明籽粒表面的自由水潴留量较大。在低镰刀菌接种浓度或无病原菌的情况下，老化WM种子的发芽率和活力高于WT。作为一种遗传性状，选择较强的水结合能力、增加渗透保护化合物和较低的不饱和酸含量可以持续提高种子的寿命和抗镰刀菌性。图形抽象

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引用次数: 0

Diverse phloroglucinols with hAChE inhibitory and anti-VRE effects from Rhodomyrtus tomentosa fruits 不同间苯三酚对毛蕊红果实hAChE抑制和抗vre作用的研究

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2026-01-08 DOI: 10.1007/s13659-025-00557-0

Ling-Yun Chen, Mu-Yuan Yu, E-E Luo, Wen-Ying Zong, Shu-Mei Lei, Yu Pan, Ai-Chun Lu, Cheng-Qin Liang, Xu-Jie Qin

Rhodomyrtus tomentosa fruits serve as both functional food and medicinal resources due to their rich bioactive constituents and manifold pharmacological effects. Phytochemical exploration of the R. tomentosa fruits led to the identification of eight new polymethylated phloroglucinols, designated as rhodotomentodione F (1) and rhodotomentodimers H‒N (2‒8), along with six previously described congeners (9‒14). Based on the detailed inspection of comprehensive spectroscopic data, electronic circular dichroism (ECD) simulations, and nuclear magnetic resonance (NMR) calculations, and DP4+ analyses, the structures of phloroglucinols 1‒8 were determined. Heterodimeric phloroglucinols 3‒14 exhibited human acetylcholinesterase (hAChE) inhibitory activities, with 13 exhibiting the highest potency (IC₅₀ = 1.04 μM). Moreover, molecular docking analysis clarified the potential binding interactions between the most active phloroglucinol 13 with hAChE. In addition, phloroglucinols 11 and 12 displayed significant anti-VRE (vancomycin-resistant Enterococci) activities, with MIC values reaching as low as 1 μg/mL.

Graphical Abstract

毛蕊红果实具有丰富的生物活性成分和多种药理作用，是功能性食品和药用资源。对红毛蕊花果实的植物化学研究鉴定出8种新的多甲基化间苯三酚，命名为红毛蕊花二聚体F(1)和红毛蕊花二聚体H-N(2-8)，以及6种先前描述的同系物（9-14）。基于综合光谱数据、电子圆二色性（ECD）模拟、核磁共振（NMR）计算和DP4+分析，确定了间苯三酚1-8的结构。异二聚体间苯三酚3-14具有抑制人乙酰胆碱酯酶（hAChE）的活性，其中13的抑制作用最强（IC50 = 1.04 μM）。此外，分子对接分析明确了最活跃的间苯三酚13与hAChE之间潜在的结合相互作用。此外，间苯三酚11和12具有明显的抗万古霉素耐药肠球菌活性，MIC值低至1 μg/mL。

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引用次数: 0

Advances in natural product discovery: strategies, technologies, and insights 天然产物发现的进展：策略、技术和见解。

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2026-01-07 DOI: 10.1007/s13659-025-00556-1

Buddha Bahadur Basnet, Zhen-Yi Zhou, Rajesh Basnet, Bin Wei, Hong Wang

Natural products (NPs) and their analogues have long underpinned therapies in humans, animals, and plants health, yet, discovering truly novel scaffolds remains a formidable challenge, even with the enormous diversity offered. Over the last two decades, breakthroughs in bioinformatics, cheminformatics, advanced analytical methods, synthetic biology toolkits, and optimized microbial culture have surmounted many of the bottlenecks that stalled NP research in the 1990s and 2000s. Researchers now deploy innovative extraction and purification protocols alongside high-throughput dereplication tools to fish trace metabolites out of complex matrices. These combined approaches not only enable the discovery and rigorous characterization of biosynthesized metabolites, bio-transformed analogues and new chemical entities but also allow precise tuning of biosynthetic gene clusters (BGCs) and culture conditions- modulation and optimization, dramatically improving yield, scalability, and cost-efficiency. Several of these newly unearthed compounds exhibit unique bioactivities that directly inspire drug-development programs against metabolic disorders, cancer drug resistance, and infectious diseases. In this review, we present an up-to-date, concise roadmap of natural product discovery (NPD), majorly covering strategies for awakening silent BGCs, genome mining, and late-stage diversification systems, and we discuss the current limitations and perspectives of rational NPD.

Graphical Abstract

天然产物（NPs）及其类似物长期以来一直是人类、动物和植物健康治疗的基础，然而，即使提供了巨大的多样性，发现真正新颖的支架仍然是一个艰巨的挑战。在过去的二十年中，生物信息学、化学信息学、先进的分析方法、合成生物学工具包和优化的微生物培养方面的突破已经克服了20世纪90年代和21世纪初停滞NP研究的许多瓶颈。研究人员现在采用创新的提取和纯化方案以及高通量去复制工具，从复杂的基质中提取痕量代谢物。这些综合方法不仅可以发现和严格表征生物合成代谢物，生物转化类似物和新的化学实体，还可以精确调整生物合成基因簇（bgc）和培养条件-调节和优化，显着提高产量，可扩展性和成本效益。这些新发现的化合物中有几种表现出独特的生物活性，直接激发了针对代谢紊乱、癌症耐药性和传染病的药物开发项目。在这篇综述中，我们提出了一个最新的、简明的天然产物发现（NPD）路线图，主要包括唤醒沉默的bgc、基因组挖掘和后期多样化系统的策略，并讨论了目前理性NPD的局限性和前景。

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引用次数: 0

Functional roles and regulatory mechanisms of paeonol in the treatment of liver disease 丹皮酚在肝病治疗中的功能作用及调控机制。

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2026-01-06 DOI: 10.1007/s13659-025-00554-3

Min Shu, Mengzhou Fang, Tao Xu, Qi Yan

Liver disease is a serious threat to human health, so its prevention and treatment have been the focus of medical research. In the past few years, natural products have proved to be promising and valuable in the treatment of liver diseases. The bioactive substance paeonol, extracted from the root bark of peony (Paeonia lactiflora) of the buttercup family, is a promising drug candidate because of its low toxicity and multifaceted pharmacological properties. This review comprehensively explored the therapeutic potential of paeonol in different liver pathologies as well as the regulatory mechanisms. Despite its promising potential, the poor solubility and rapid metabolism of paeonol hindered its clinical translation. To improve bioavailability and liver targeting, we highlighted the potential of paeonol as a next-generation therapy for liver diseases by integrating preclinical evidence and technological advances, while exploring key avenues for future research, such as metabolic regulation and smart nanocarrier design.

Graphical abstract

肝病是严重威胁人类健康的疾病，其防治一直是医学研究的重点。在过去的几年里，天然产物在肝脏疾病的治疗中被证明是有希望和有价值的。从毛茛科芍药（Paeonia lactiflora）的根皮中提取的生物活性物质丹皮酚因其低毒性和多方面的药理特性而成为一种很有前途的候选药物。本文综述了丹皮酚在不同肝脏病理中的治疗潜力及其调控机制。尽管丹皮酚具有广阔的应用前景，但其溶解性差、代谢速度快的特点阻碍了其临床应用。为了提高生物利用度和肝脏靶向性，我们通过整合临床前证据和技术进步，强调了丹皮酚作为下一代肝脏疾病治疗的潜力，同时探索了未来研究的关键途径，如代谢调节和智能纳米载体设计。

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引用次数: 0

First discovery of triterpenoids and sterols from Cotinus coggygria var. cinereus Engl. with anti-inflammatory and antibacterial activities 首次从黄连藤中发现三萜和甾醇。具有抗炎和抗菌活性

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2026-01-05 DOI: 10.1007/s13659-025-00553-4

Yue-Tong Zhu, Ze-Rui Li, Ren-Hao Chen, Jin-Hao Li, Wei Wang, Yu-Qi Gao, Chun-Huan Li, Jin-Ming Gao

This study led to the isolation of 17 triterpenoids, including two lanostane-type (1 and 2), two dammarane-type (3 and 7), ten tirucallane-type (4 and 8−16), and three oleanane-type (17−19) triterpenoids, as well as nine sterols (5, 6, and 20−26) from Cotinus coggygria var. cinereus Engl, which were first discovered from the genus Cotinus. Among them, coggygrenoids A−D (1−4), coggygrerol A (5), and coggygrerol B (6) are undescribed compounds. Additionally, seven flavonoids (27−33) were also isolated from this plant. Compound 15 displayed inhibitory activities in LPS-induced RAW 264.7 cells with an IC₅₀ value 6.81 ± 0.15 μM. Molecular docking demonstrated that 15 exhibited favorable affinity for NLRP3 and iNOS. In vitro and in vivo antibacterial evaluations indicated that coggygrnoid C (3) exhibited significant inhibitory activity against methicillin-resistant Staphylococcus aureus ATCC BAA-1717 (USA300), with An MIC of 8 μg/mL. Further mechanistic investigations demonstrated that 3 exerted antibacterial activity by compromising the integrity of the cell wall and membrane. Notably, the combination of 3 with ampicillin exhibited an additive antibacterial effect. In the Galleria mellonella infection model, compound 3 exhibited comparable activity to that of the positive control at 20 mg/kg. These findings suggest that triterpenoids of C. coggygria are potential antibacterial lead agents.

Graphical Abstract

从Cotinus coggygria var. cinereus Engl中分离到17个三萜，包括2个羊毛甾烷型（1和2）、2个达玛烷型（3和7）、10个tirucallane型（4和8−16）和3个齐墩烷型（17−19）三萜，以及9个甾醇类（5、6和20−26）。其中，coggygrenoids A−D（1−4）、coggygreol A(5)和coggygreol B(6)为未描述的化合物。此外，还从该植物中分离到7种黄酮类化合物（27−33）。化合物15对lps诱导的RAW 264.7细胞有抑制作用，IC50值为6.81±0.15 μM。分子对接表明，其中15个对NLRP3和iNOS具有良好的亲和力。体外和体内抗菌评价表明，coggygrnoid C(3)对耐甲氧西林金黄色葡萄球菌ATCC BAA-1717 （USA300）具有显著的抑制活性，其MIC为8 μg/mL。进一步的机制研究表明，3通过破坏细胞壁和细胞膜的完整性来发挥抗菌活性。值得注意的是，3与氨苄西林合用具有加性抗菌作用。在mellonella感染模型中，化合物3在20 mg/kg时表现出与阳性对照相当的活性。这些结果表明，三萜是潜在的抗菌先导剂。图形抽象

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引用次数: 0

Preparation, physicochemical properties, and immunomodulatory activity of glycoproteins from Syngnathoides biaculeatus 双棘合藤糖蛋白的制备、理化性质及免疫调节活性研究。

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2025-12-01 DOI: 10.1007/s13659-025-00551-6

Xuewei Xia, Jieling Lin, Lihong Yang, Youhong Li, Wenshen Lin, Qingqing Wang, Jun Liu, Riming Huang

Syngnathoides biaculeatus, a potential functional food from marine sources, was found to enhance nonspecific immunity, but its functional ingredients have rarely been reported. Therefore, this study focused on the preparation and physicochemical properties of its water-soluble natural ingredients with their immunomodulatory activities and potential mechanisms. Firstly, we optimized the extraction method of glycoproteins from S. biaculeatus and prepared the crude glycoprotein SYB, from which the fraction glycoprotein SYB-1 was further purified. The carbohydrates of SYB-1 were 8.46% comprising mannose, glucose, and galactose, with an average molecular weight of 9.423 kDa. Amino acid analysis demonstrated that its major amino acids are glycine, glutamic acid, aspartic acid, and proline, with a total amino acid content of 88.81%. Furthermore, SYB-1 could significantly increase the cell viability of macrophages, and promote the release of NO, TNF-α, and IL-6. Metabolomics revealed that it was associated with arachidonic acid metabolism. The CYP450 enzyme family members and PTGS2 may be key targets for the regulatory role. These results suggested that the glycoprotein of S. biaculeatus may be an attractive functional food supplement from natural sources for immunocompromised populations.

Graphical Abstract

双棘合藤是一种具有增强非特异性免疫功能的潜在海洋功能性食品，但其功能成分鲜有报道。因此，本研究重点对其水溶性天然成分的制备、理化性质、免疫调节活性及其潜在机制进行了研究。首先，优化双歧杆菌中糖蛋白的提取方法，制备粗糖蛋白SYB，并对粗糖蛋白SYB-1进行进一步纯化。SYB-1的碳水化合物含量为8.46%，由甘露糖、葡萄糖和半乳糖组成，平均分子量为9.423 kDa。氨基酸分析表明，其主要氨基酸为甘氨酸、谷氨酸、天冬氨酸和脯氨酸，总氨基酸含量为88.81%。SYB-1能显著提高巨噬细胞的细胞活力，促进NO、TNF-α、IL-6的释放。代谢组学结果显示，它与花生四烯酸代谢有关。CYP450酶家族成员和PTGS2可能是调控作用的关键靶点。这些结果表明，双歧杆菌的糖蛋白可能是免疫功能低下人群的一种有吸引力的天然功能性食品补充剂。

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引用次数: 0

Advancement in nanocarrier-mediated delivery of herbal bioactives: from bench to beside 纳米载体介导的草药生物活性递送研究进展：从工作台到旁边

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2025-11-01 DOI: 10.1007/s13659-025-00550-7

Fatemeh Najafi, Negar Farrokhzad, Amirhossein Ghaemi, Dorsa Azizi Khezri, Mohammadali Hajiabbas, Amirhossein Khanizadeh, Nasim Kaveh Farsani, Mahsa Khoramipour, Niloofar Fatemipayam, Elham Seyyedi Zadeh, Arash Goodarzi, Behnoosh Khodadadi, Fatemeh Moradbeygi, Ahmad Reza Farmani, Mohammad Tavakkoli Yaraki, Martin Federico Desimone

The resurgence of interest in traditional herbal remedies stems from an increasing appreciation for their complex phytochemical profiles and potential for synergistic therapeutic effects. However, the therapeutic potential of plant extracts is often limited by poor absorption and potential toxicity related to conventional delivery methods. This review explores the application of nanocarrier-mediated delivery systems, such as nanoparticles (NPs), liposomes, and nanoemulsions, to address these challenges. These biocompatible carriers offer enhanced stability and targeted delivery of herbal compounds, improving their efficacy and reducing unwanted side effects. By enabling precise distribution, nanotechnology optimizes the potency of herbal medicine across diverse applications, including regenerative medicine, wound healing, anticancer, and infection treatment. This review provides a systematic description of successful applications of nano-delivery technologies, nanoparticles, liposomes, nanoemulsions, and hybrid carriers, for the targeted delivery of some well-characterized herbal bioactives (curcumin, allicin, berberine, resveratrol etc.) and the enhanced therapeutic performance of herbal bioactives across a variety of preclinical models.

Graphical Abstract

对传统草药疗法的兴趣的复苏源于对其复杂的植物化学特征和潜在的协同治疗效果的日益重视。然而，植物提取物的治疗潜力往往受到吸收不良和与传统给药方法相关的潜在毒性的限制。这篇综述探讨了纳米载体介导的递送系统的应用，如纳米颗粒（NPs）、脂质体和纳米乳液，以解决这些挑战。这些生物相容性载体提供了增强的稳定性和靶向输送草药化合物，提高其功效和减少不必要的副作用。通过精确分配，纳米技术优化了草药在多种应用中的效力，包括再生医学、伤口愈合、抗癌和感染治疗。本文综述了纳米递送技术、纳米颗粒、脂质体、纳米乳剂和杂交载体的成功应用，用于靶向递送一些具有良好特征的草药生物活性物质（姜黄素、大蒜素、小檗碱、白藜芦醇等），并在各种临床前模型中增强了草药生物活性物质的治疗性能。图形抽象

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引用次数: 0

Kaemphenolide: a cyclobutane-bearing phenylpropanoid from Kaempferia galanga L. with nitric oxide inhibitory activity 山柰酚内酯：从山柰中提取的含环丁烷的苯丙素，具有抑制一氧化氮的活性。

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2025-10-02 DOI: 10.1007/s13659-025-00547-2

Syarifatul Mufidah, Yusaku Miyamae, Hiroyuki Fuchino, Nobuo Kawahara

An undescribed phenylpropanoid dimer featuring a rare cyclobutane ring was isolated from the rhizomes of Kaempferia galanga L., a medicinal plant traditionally used in Southeast Asia for its anti-inflammatory and therapeutic properties. Kaemphenolide (1), along with five known constituents, was obtained by separations of methanolic extract using chromatography. The presence of a cyclobutane ring within the phenylpropanoid scaffold represents an unusual structural motif among natural products and underscores the chemical uniqueness of this molecule. To evaluate its biological relevance, 1 was tested for its ability to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. The compound exhibited anti-inflammatory activity, with an IC₅₀ value of 23.1 ± 6.40 µM.

Graphical Abstract

从东南亚传统药用植物山柰（Kaempferia galanga L.）根茎中分离出一种具有罕见环丁烷环的苯丙二聚体。山柰具有抗炎和治疗特性。Kaemphenolide(1)，连同五个已知的成分，得到分离甲醇提取物使用色谱法。苯基丙烷支架内的环丁烷环的存在代表了天然产物中不寻常的结构基序，并强调了该分子的化学独特性。为了评估其生物学相关性，1测试了其抑制脂多糖（LPS）刺激的RAW264.7巨噬细胞中一氧化氮（NO）产生的能力。化合物具有抗炎活性，IC50值为23.1±6.40µM。

引用次数: 0

Neuroprotective effects of chemical constituents from Nicotiana tabacum L. in Parkinson’s disease 烟草化学成分对帕金森病的神经保护作用。

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2025-10-01 DOI: 10.1007/s13659-025-00541-8

Hao-Jing Zang, Xiao-Lin Bai, Xue-Yi Sui, Xiao-Rui Zhai, Yong-Cui Wang, Zhong-Quan Xin, Qiu-Yuan Yin, Xiao-Jiang Hao, Yue-Hu Wang, Xun Liao, Ying-Tong Di

Parkinson’s disease (PD), the second most common neurodegenerative disorder globally, arises from selective dopaminergic neuron degeneration. While current therapies address symptoms, disease-modifying agents remain an unmet need. Herein, we investigated Nicotiana tabacum L. (Solanaceae), a plant linked epidemiologically to reduced PD risk, as a source of multi-target neuroprotective compounds. From ultra-low nicotine (< 0.04%) tobacco leaves, we isolated 22 molecules, including a novel 21-norsesterterpenoid (Nicotiazanorpenoid A) and eight previously unreported compounds. Systematic evaluation revealed three synergistic neuroprotective mechanisms: (1) Antioxidant activity: Scopoletin (3) and isoferulic acid (6) showed significant radical scavenging capacity (ABTS assay; IC₅₀ = 27.74, and 18.13 μM, respectively); (2) Neuronal protection: cis-11,14,17-Eicosatrienoic acid methyl ester (14) enhanced survival (93.94% vs. control) in 6-OHDA-induced PC12 cells, surpassing rasagiline (88.36% at equivalent concentrations); (3) MAO-B inhibition: five compounds displayed selective inhibition, with scopoletin (3) exhibiting highest potency (K_i = 20.7 μM). Notably, plant prostaglandins (10/11) were identified as competitive MAO-B inhibitors first time through molecular docking and 100-ns MD simulations, revealing stable binding at the FAD site (ΔG = − 10.42, and − 9.75 kcal/mol, respectively).

Graphical Abstract

帕金森病（PD）是全球第二大最常见的神经退行性疾病，由选择性多巴胺能神经元变性引起。虽然目前的治疗方法解决了症状，但疾病调节剂仍然是一个未满足的需求。在此，我们研究了烟草（Nicotiana tabacum L.），一种与降低PD风险相关的植物，作为多靶点神经保护化合物的来源。来自超低尼古丁（50 = 27.74 μM, 18.13 μM）；(2)神经元保护作用：顺式-11,14,17-二十碳三烯酸甲酯（14）可提高6- ohda诱导的PC12细胞的存活率（93.94%），超过同等浓度的雷沙吉兰（88.36%）；(3)抑制MAO-B: 5种化合物表现出选择性抑制作用，其中东莨菪碱(3)的抑制作用最强（Ki = 20.7 μM）。值得注意的是，通过分子对接和100-ns MD模拟，植物前列腺素（10/11）首次被鉴定为具有竞争性的MAO-B抑制剂，显示其在FAD位点的稳定结合（ΔG = - 10.42和- 9.75 kcal/mol）。

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引用次数: 0

Strophioglandins A–C, highly rearranged norditerpenoids with an unusual tricyclo[6.4.1.04,13]tridecane core from Strophioblachia glandulosa var. cordifolia 含有一个不寻常的三环[6.4.1.4.04,13]三烷烃核的高度重排的北二萜类化合物

IF 4.9 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2025-09-15 DOI: 10.1007/s13659-025-00548-1

Jian-Kai Xia, Lei-Ming Wu, Wei-Ye Wu, Dong Huang, Fang-Yu Yuan, Lei Li, Shu-Qi Wu, Yan-Jiang Zhang, Tao Yuan, Xin Chen, Gui-Hua Tang, Jia-Luo Huang, Sheng Yin

Strophioglandins A−C (1−3), three highly rearranged norditerpenoids featuring an unusual tricyclo[6.4.1.0^4,13]tridecane core, were isolated from Strophioblachia glandulosa var. cordifolia. Integrated spectroscopic analyses, X-ray crystallography, and ECD calculations synergistically determined their molecular architectures. Remarkably, all compounds manifested potent anti-inflammatory effects in LPS-activated RAW264.7 cells with IC₅₀ values ranging from 7.83 ± 1.11 to 15.09 ± 1.21 μM. Mechanism study revealed that strophioglandin A (1), the most potent compound, could suppress the expression of multiple inflammatory factors by inhibiting the P38 and Erk1/2 MAPK signaling pathways.

Graphical Abstract

Strophioglandins A−C（1−3）是三个高度重排的北二萜类化合物，具有罕见的三环[6.4.1.04,13]三烷核心。综合光谱分析、x射线晶体学和ECD计算协同确定了它们的分子结构。值得注意的是，所有化合物对lps激活的RAW264.7细胞均表现出较强的抗炎作用，IC50值在7.83±1.11 ~ 15.09±1.21 μM之间。机制研究发现，其中最有效的化合物strophioglandin A(1)可通过抑制P38和Erk1/2 MAPK信号通路抑制多种炎症因子的表达。图形抽象

{"title":"Strophioglandins A–C, highly rearranged norditerpenoids with an unusual tricyclo[6.4.1.04,13]tridecane core from Strophioblachia glandulosa var. cordifolia","authors":"Jian-Kai Xia, Lei-Ming Wu, Wei-Ye Wu, Dong Huang, Fang-Yu Yuan, Lei Li, Shu-Qi Wu, Yan-Jiang Zhang, Tao Yuan, Xin Chen, Gui-Hua Tang, Jia-Luo Huang, Sheng Yin","doi":"10.1007/s13659-025-00548-1","DOIUrl":"10.1007/s13659-025-00548-1","url":null,"abstract":"<div><p>Strophioglandins A−C (<b>1</b>−<b>3</b>), three highly rearranged norditerpenoids featuring an unusual tricyclo[6.4.1.0<sup>4,13</sup>]tridecane core, were isolated from <i>Strophioblachia glandulosa</i> var. <i>cordifolia</i>. Integrated spectroscopic analyses, X-ray crystallography, and ECD calculations synergistically determined their molecular architectures. Remarkably, all compounds manifested potent anti-inflammatory effects in LPS-activated RAW264.7 cells with IC<sub>50</sub> values ranging from 7.83 ± 1.11 to 15.09 ± 1.21 μM. Mechanism study revealed that strophioglandin A (<b>1</b>), the most potent compound, could suppress the expression of multiple inflammatory factors by inhibiting the P38 and Erk1/2 MAPK signaling pathways.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"15 1","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-09-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13659-025-00548-1.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145057635","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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