Fitoterapia最新文献_第6页

Bee bread as a natural shield against genetic damage: Investigation of antigenotoxic and antimutagenic potential 蜜蜂面包作为抗基因损伤的天然屏障：抗基因毒性和抗诱变潜力的研究。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-27 DOI: 10.1016/j.fitote.2025.107077

Karolina Matejczuk , Piotr M. Kuś , Piotr Szweda

Bee bread (BB), a fermented bee product rich in bioactive compounds, such as aminoacids and peptides, vitamins and polyphenols, has garnered attention for its potential health benefits, particularly high antioxidant potential. However, its role in protecting genetic material from damage (antigenotoxic and antimutagenic activity) remains largely unexplored. This study provides the first comprehensive evaluation of both antigenotoxic and antimutagenic activities of Polish bee bread extracts in human HEK293 cells, integrating functional assays with advanced chemical profiling.

Twenty Polish BB samples were analyzed for antioxidant activity using DPPH Radical Scavenging Assay and Cellular Antioxidant Activity assays, revealing significant radical scavenging and intracellular ROS reduction capacities. UHPLC-DAD-QqTOF-MS profiling identified 71 compounds, predominantly flavonoids and phenolamides, known for their cytoprotective roles.

Importantly, comet assay results demonstrated that BB extracts significantly reduced methyl methanesulfonate (MMS)-induced DNA strand breaks, while cytokinesis-block micronucleus assay confirmed up to 91 % reduction in mutagenicity without intrinsic genotoxicity. Unlike previous studies that focused primarily on antioxidant activity, our work establishes bee bread as a natural chemoprotective agent against DNA damage and chromosomal instability, highlighting its potential in disease prevention. These findings expand the current understanding of bee bread bioactivity and position it as a promising candidate for functional food and nutraceutical applications.

蜜蜂面包（BB）是一种富含生物活性化合物的发酵蜂产品，如氨基酸和多肽、维生素和多酚，因其潜在的健康益处，特别是高抗氧化潜力而受到关注。然而，它在保护遗传物质免受损害（抗基因毒性和抗诱变活性）方面的作用在很大程度上仍未被探索。该研究首次综合评价了波兰蜜蜂面包提取物对人HEK293细胞的抗基因毒性和抗诱变活性，将功能分析与先进的化学分析相结合。使用DPPH自由基清除实验和细胞抗氧化活性实验分析了20个波兰BB样品的抗氧化活性，揭示了显著的自由基清除和细胞内ROS还原能力。UHPLC-DAD-QqTOF-MS分析鉴定了71种化合物，主要是类黄酮和酚酰胺，已知具有细胞保护作用。重要的是，彗星试验结果表明，BB提取物显著降低了甲基甲烷磺酸盐（MMS）诱导的DNA链断裂，而细胞分裂阻断微核试验证实，在没有内在遗传毒性的情况下，致突变性降低了91% %。与以往主要关注抗氧化活性的研究不同，我们的工作确定了蜜蜂面包是一种天然的化学保护剂，可以防止DNA损伤和染色体不稳定，突出了它在疾病预防方面的潜力。这些发现扩大了目前对蜜蜂面包生物活性的理解，并将其定位为功能性食品和营养保健应用的有希望的候选者。

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引用次数: 0

Progress of anti-tumor research on natural products combined with doxorubicin 天然产物联合阿霉素抗肿瘤研究进展。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-27 DOI: 10.1016/j.fitote.2025.107076

Yanqing Wu, Jianguo Gao, Yuwei Zhao, Yingzhi Lu, Xiaoqing Cai

Cancer represents a major global public health challenge, with its incidence and mortality rates increasing annually. Doxorubicin (DOX) is a commonly used chemotherapeutic agent. Despite its marked antitumor efficacy, the clinical application of DOX is limited by drug resistance and cumulative toxicity. Numerous natural products have garnered significant attention owing to their favorable antitumor, antioxidant, anti-inflammatory, and anti-apoptotic properties, and are increasingly being developed as adjuvant agents in combination therapy with DOX. The co-administration of natural products with DOX has emerged as a promising strategy to enhance therapeutic outcomes while mitigating adverse effects. However, this combination approach is constrained by poor drug solubility and disparate pharmacokinetic profiles. The advent of multifunctional nanodelivery systems has improved drug bioavailability and tumor targeting, thereby laying the groundwork for synergistic interactions between natural products and DOX. This review systematically summarizes the antitumor mechanisms and toxic side effects of DOX, elucidates the mechanisms of action and structure-activity relationships of certain natural products serving as DOX sensitizers and protective agents, and highlights recent advances in nano-platform-based co-delivery strategies, offering valuable insights for future cancer therapeutics.

癌症是一项重大的全球公共卫生挑战，其发病率和死亡率每年都在上升。阿霉素（DOX）是一种常用的化疗药物。尽管DOX具有显著的抗肿瘤疗效，但其耐药和累积毒性限制了其临床应用。许多天然产物因其良好的抗肿瘤、抗氧化、抗炎和抗凋亡特性而受到广泛关注，并越来越多地被开发为与DOX联合治疗的佐剂。天然产物与DOX联合给药已成为一种有希望的策略，可以提高治疗效果，同时减轻不良反应。然而，这种联合方法受到药物溶解度差和不同药代动力学特征的限制。多功能纳米递送系统的出现改善了药物的生物利用度和肿瘤靶向性，从而为天然产物和DOX之间的协同相互作用奠定了基础。本文系统总结了DOX的抗肿瘤机制和毒副作用，阐明了某些天然产物作为DOX致敏剂和保护剂的作用机制和构效关系，并重点介绍了基于纳米平台的共给药策略的最新进展，为未来的癌症治疗提供了有价值的见解。

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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

Fitoterapia

Pub 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

Study on chemical composition, plasma-absorbed components, and anti-inflammatory and antibacterial activity of Hypericum patulum 金丝桃的化学成分、血浆吸收成分及抗炎、抗菌活性研究。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-26 DOI: 10.1016/j.fitote.2025.107044

Qiya Zhang , Meiqin Wang , Li Jiang , Yang Wang , Yuan Lu , Xue Ma , Yongjun Li

This study investigated the chemical composition of Hypericum patulum and its plasma metabolites in rats using ultra-high-performance liquid chromatography coupled to a Q-Exactive Plus Orbitrap mass spectrometer (UPLC-Q Exactive Plus Orbitrap MS). A total of 162 compounds were identified in the plant extract of H. patulum, encompassing 50 flavonoids, 32 organic acids, 26 xanthones, 12 polycyclic polyprenylated acylphloroglucinols (PPAPs), 10 amino acids, 8 coumarins, 5 alkaloids, 3 sugars, 2 terpenoids, 3 aldehydes, and 11 others. Analysis of rat plasma revealed 48 compounds, consisting of 20 prototypes (predominantly xanthones, organic acids, and flavonoids) and 28 metabolites generated via glucuronidation, methylation, and sulfation. In LPS-induced RAW 264.7 macrophages, H. patulum extract significantly inhibited NO release and suppressed the expression of pro-inflammatory mediators, including IL-6, TNF-α, COX-2, iNOS, and IL-1β. In vivo, quercetin and shikimic acid attenuated xylene-induced ear edema and inflammatory infiltration in mice, and also lowered serum levels of the pro-inflammatory cytokines TNF-α, IL-6, and IL-1β. Antibacterial testing revealed that shikimic acid demonstrated activity against a panel of pathogens, with minimum inhibitory concentration (MIC) of 13.00, 6.50, and 20.08 mg/mL against Staphylococcus aureus, Escherichia coli, and β-hemolytic Streptococcus, respectively. Vanillic acid showed MICs of 6.50 mg/mL against S. aureus and 3.25 mg/mL against E. coli, whereas quercetin inhibited S. aureus at a concentration of 3.25 mg/mL. These findings characterize the pharmacologically active components of H. patulum, thereby validating its traditional use and laying a foundation for future investigations into its therapeutic mechanisms.

采用超高效液相色谱- Q-Exactive Plus Orbitrap质谱联用技术（UPLC-Q Exactive Plus Orbitrap MS）对大鼠血药金丝桃及其血浆代谢物的化学成分进行了研究。共鉴定出162种化合物，包括50种黄酮类化合物、32种有机酸、26种山酮类化合物、12种多环聚丙烯酰化酰基间苯三酚（PPAPs）、10种氨基酸、8种香豆素、5种生物碱、3种糖、2种萜类化合物、3种醛类化合物和11种其他化合物。对大鼠血浆的分析发现了48种化合物，包括20种原型化合物（主要是山酮类、有机酸和类黄酮）和28种通过葡萄糖醛酸化、甲基化和磺化产生的代谢物。在lps诱导的RAW 264.7巨噬细胞中，育兔草提取物显著抑制NO释放，抑制IL-6、TNF-α、COX-2、iNOS和IL-1β等促炎介质的表达。在体内，槲皮素和莽草酸可减轻二甲苯诱导的小鼠耳部水肿和炎症浸润，并降低血清中促炎细胞因子TNF-α、IL-6和IL-1β的水平。抑菌试验表明，莽草酸对多种病原菌均有抑制作用，对金黄色葡萄球菌、大肠杆菌和β-溶血性链球菌的最低抑制浓度（MIC）分别为13.00、6.50和20.08 mg/mL。香草酸对金黄色葡萄球菌的mic为6.50 mg/mL，对大肠杆菌的mic为3.25 mg/mL，槲皮素对金黄色葡萄球菌的mic为3.25 mg/mL。这些发现表征了黄菌的药理活性成分，从而验证了其传统用途，并为进一步研究其治疗机制奠定了基础。

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引用次数: 0

Screening 5-lipoxygenase inhibitors from Choerospondias axillaris via a novel enzyme immobilization targeted fishing technology 用一种新的酶固定化靶向捕捞技术筛选腋毛绒脊膜虫5-脂氧合酶抑制剂。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-26 DOI: 10.1016/j.fitote.2025.107047

Shiyu Li , Kai Xu , Shanpeng Ma , Xueying Qin , Li Jiang , Xiaohong Hou , Zibo Dong , Xun Gao , Lingling Huo

Currently, coronary heart disease (CHD) is prevalent worldwide, with its harmful impact second only to that of malignant tumors. A growing number of studies have confirmed that Choerospondias axillaris can significantly improve the therapeutic effect of CHD treatment and reduce the incidence of adverse reactions. However, its bioactive components and pharmacological mechanisms remain unclear. Based on a targeted fishing strategy, this study synthesized magnetic nanomaterials immobilized with 5-lipoxygenase (5-LOX) for screening and identifying 5-LOX inhibitors from the crude extract of Choerospondias axillaris. A total of 21 active components were identified and analyzed using ultra-high performance liquid chromatography-Q-Exactive Orbitrap tandem mass spectrometry (UHPLC-Q-Exactive Orbitrap-MS/MS). By comparing the screened active components with reported 5-LOX inhibitors, 9 novel 5-LOX inhibitors were discovered. Further molecular docking was performed on these 9 inhibitors, and the pharmacological activity of the selected ligands was verified using a 5-LOX inhibitor screening kit (fluorescence method).The compounds are ranked by activity from strongest to weakest: Lobetyolin (23.92 μM), Anhydroicaritin (29.55 μM), Narirutin(33.66 μM), Fisetin (47.28 μM) and Naringin(59.02 μM). This novel enzyme-immobilized targeted fishing technology is expected to efficiently and accurately screen bioactive components targeting different receptors from complex substrates.

目前，冠心病（冠心病）在世界范围内普遍存在，其危害仅次于恶性肿瘤。越来越多的研究证实，腋窝绒脊柱体能显著提高冠心病治疗的疗效，降低不良反应的发生率。然而，其生物活性成分和药理机制尚不清楚。本研究基于靶向捕捞策略，合成了5-脂氧合酶（5-LOX）固定化磁性纳米材料，用于筛选和鉴定腋毛绒海绵粗提物中5-LOX抑制剂。采用超高效液相色谱- q - exactive Orbitrap串联质谱（UHPLC-Q-Exactive Orbitrap-MS/MS）对21种有效成分进行了鉴定和分析。通过与已报道的5-LOX抑制剂进行比较，发现了9种新的5-LOX抑制剂。对这9种抑制剂进行进一步的分子对接，并使用5-LOX抑制剂筛选试剂盒（荧光法）验证所选配体的药理活性。活性由强到弱依次为：Lobetyolin（23.92 μM）、Anhydroicaritin（29.55 μM）、Narirutin（33.66 μM）、fissetin（47.28 μM）、Naringin（59.02 μM）。这种新型的酶固定化靶向捕捞技术有望有效、准确地从复杂底物中筛选针对不同受体的生物活性成分。

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引用次数: 0

Six undescribed diterpenoids from the aerial parts of Siegesbeckia pubescens Makino and their anti-inflammatory activity 六种未描述的三叶青花（Siegesbeckia pubescens Makino）地上部二萜类化合物及其抗炎活性。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-26 DOI: 10.1016/j.fitote.2025.107068

LingXia Qu, JinBo Li, Jiang Zhou, MeiHui Zhou, HaiXue Kuang, Liu Yang, Hai Jiang

Six novel diterpenoids (1–6) and seventeen known compounds (7–23) were isolated from the aerial parts of Siegesbeckia pubescens Makino. The chemical structures of the new compounds were established through comprehensive spectroscopic characterization, including HR-ESI-MS and 1D/2D NMR analyses, and their absolute configurations were determined by ECD calculations. The anti-inflammatory effect of all compounds against lipopolysaccharide (LPS)-induced RAW 264.7 cells was tested. The results indicated that compounds 2–18 and 20–23 significantly suppressed nitric oxide (NO) production.

从牧野野荆芥（Siegesbeckia pubescens Makino）地上部分离得到6个新化合物（1 ~ 6）和17个已知化合物（7 ~ 23）。通过HR-ESI-MS和1D/2D NMR等综合波谱表征，确定了新化合物的化学结构，并通过ECD计算确定了它们的绝对构型。检测各化合物对脂多糖（LPS）诱导的RAW 264.7细胞的抗炎作用。结果表明，化合物2-18和20-23能显著抑制一氧化氮（NO）的生成。

引用次数: 0

Fu Fang Sheng Mai capsules inhibit osteoclast formation and improve osteoporosis caused by oophorectomy in mice 扶方生脉胶囊抑制破骨细胞形成，改善小鼠卵巢切除所致骨质疏松症。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-25 DOI: 10.1016/j.fitote.2025.107070

Qiang-Qiang Zhao , Wei Deng , Bin Mai , Ya-Mei Liu , Shi-yin Zhang , Jia-min Yang , Feihong Che , Pan Kang , Yang Peng , Shun-Cong Zhang , Bin Wang , Qiu-shi Wei , Yong-Xian Li , Liang-Liang Xu

Background

Postmenopausal osteoporosis (PMOP) is a critical bone metabolic disorder marked by progressive bone loss and compromised bone microstructure. Empirical clinical observations suggest that Fu Fang Sheng Mai Capsules (FFSM) can effectively alleviate symptoms of osteoporosis; however, their underlying molecular mechanisms remain insufficiently defined. The present study was designed to investigate the regulatory effects of FFSM on osteoclast differentiation and to evaluate its therapeutic potential in PMOP.

Methods

Bone marrow-derived macrophages (BMMs) were isolated and induced to differentiate into osteoclasts in vitro. The impact of FFSM on osteoclastogenesis was assessed by tartrate-resistant acid phosphatase (TRAP) staining and F-ACTIN ring fluorescence staining. Subsequently, quantitative real-time PCR (qRT–PCR) and Western blot analyses were performed to evaluate the expression of osteoclast-specific genes, with further mechanistic investigations. For in vivo validation, a bilateral ovariectomy model was established in C57BL/6 mice, and bone quality was examined using micro-CT and histological analysis.

Results and conclusion

FFSM significantly suppressed osteoclast formation and F-ACTIN ring assembly, with notable downregulation of osteoclast differentiation markers NFATc1 and Acp5 observed at days 3–5. Mechanistically, FFSM reduced intracellular ROS levels within osteoclasts, and specifically inhibited the phosphorylation of key signaling proteins, p-P65 in the NF-κB pathway and p-JNK in the MAPK pathway, thus interfering with pathways critical for osteoclastogenesis. Consistent with in vitro findings, in vivo studies revealed that FFSM reduced osteoclastogenesis and effectively rescued bone mass loss.

背景：绝经后骨质疏松症（PMOP）是一种严重的骨代谢紊乱，其特征是进行性骨质流失和骨微结构受损。临床经验观察表明，扶方生脉胶囊能有效缓解骨质疏松症的症状；然而，其潜在的分子机制仍不明确。本研究旨在探讨FFSM对破骨细胞分化的调节作用，并评价其治疗ppu的潜力。方法：分离骨髓源性巨噬细胞，体外诱导其向破骨细胞分化。通过抗酒石酸酸性磷酸酶（TRAP）染色和F-ACTIN环荧光染色评估FFSM对破骨细胞生成的影响。随后，采用定量实时PCR （qRT-PCR）和Western blot分析来评估破骨细胞特异性基因的表达，并进一步进行机制研究。为了在体内验证，我们建立了C57BL/6小鼠双侧卵巢切除模型，并通过显微ct和组织学分析检查了骨质量。结果与结论：FFSM明显抑制破骨细胞形成和F-ACTIN环组装，在第3-5天观察到破骨细胞分化标志物NFATc1和Acp5明显下调。从机制上看，FFSM降低了破骨细胞内的ROS水平，并特异性抑制了关键信号蛋白NF-κB通路中的p-P65和MAPK通路中的p-JNK的磷酸化，从而干扰了破骨细胞发生的关键通路。与体外研究结果一致，体内研究表明，FFSM可以减少破骨细胞的发生，有效地挽救骨量损失。

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引用次数: 0

Gut microbiota combined with metabolomics approach to investigate the processing-based detoxification mechanism of processed cream of Croton tiglium L. seeds 肠道菌群结合代谢组学方法研究巴豆种子加工奶油的加工解毒机制。

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-25 DOI: 10.1016/j.fitote.2025.107067

Wen Pan , Ze-Fei Jia , Xiao-Bin Deng , Liang-Ying Li , Shu-Li Man , Shi-Qiang Tan , Jing Hu

Croton tiglium L. (Crotonis Fructus, CF), a classic toxic but valued Chinese herb used for over 2000 years, requires detoxification processing for clinical safety. Crotonis Semen Pulveratum (CP) is the most common processed product of CF, which has been utilized since the Song Dynasty. Nevertheless, the detoxification mechanisms underlying CP processing is still unclear. Therefore, this study investigated toxicity differences between raw and processed CF in rats and preliminarily predicted the potential attenuation mechanism after processing. UPLC-Q-Exactive-MS characterized CF and CP constituents, and 16S rRNA sequencing analyzed gut microbiota changes. Additionally, serum metabolomics was adopted to identify differential biomarkers and principal metabolic pathways associated with CP toxicity attenuation. The results show that chemical profiling identified 18 compounds that differentiated CP from CF. Histopathology showed processing significantly alleviated CF-induced gut damage in normal rats. CP restored colonic mucosa, reversing CF-induced damage to epithelium, crypts, and goblet cells. Moreover, CP treatment exhibited substantial regulatory effects on inflammatory and oxidative markers. Gut microbiota studies revealed that processing-mediated toxicity attenuation was closely associated with the restoration of gut microbial diversity and specific modulation of key bacterial taxa, including Eubacterium_coprostanoligenes_group, Escherichia-Shigella and Lactobacillus. Processing ameliorated CF-induced serum metabolic disorders, identifying 12 biomarkers linked to glycerolipid, lysine, and arginine/proline metabolism pathways. Additionally, quantitative analysis indicated that the reduction of crotonane diterpenoids after processing might contribute to the observed detoxification effects of CP. This study provides new insights into the possible processing-mediated toxicity attenuation of CP, offering a scientific foundation for its quality optimization and safe clinical application.

Crotonis Fructus （Crotonis Fructus， CF）是一种经典的有毒但有价值的中药，使用了2000多年 年，为了临床安全，需要进行解毒处理。巴豆粉（CP）是巴豆粉最常见的加工产品，自宋代开始使用。然而，CP加工背后的解毒机制仍不清楚。因此，本研究考察了生的和加工的CF对大鼠的毒性差异，并初步预测加工后可能的衰减机制。UPLC-Q-Exactive-MS表征了CF和CP成分，16S rRNA测序分析了肠道微生物群的变化。此外，采用血清代谢组学方法鉴定与CP毒性衰减相关的差异生物标志物和主要代谢途径。结果表明，化学分析鉴定出18种化合物可区分CP和CF。组织病理学显示加工可显著减轻CF引起的正常大鼠肠道损伤。CP恢复结肠黏膜，逆转cf诱导的上皮、隐窝和杯状细胞损伤。此外，CP治疗对炎症和氧化标志物具有实质性的调节作用。肠道菌群研究表明，加工介导的毒性衰减与肠道微生物多样性的恢复和关键细菌类群的特异性调节密切相关，包括真杆菌群、志贺杆菌群和乳杆菌群。加工改善了cf诱导的血清代谢紊乱，确定了与甘油脂、赖氨酸和精氨酸/脯氨酸代谢途径相关的12种生物标志物。此外，定量分析表明，加工后的巴豆烷二萜的减少可能与观察到的CP解毒作用有关。本研究为CP加工介导的毒性衰减提供了新的见解，为其质量优化和安全临床应用提供了科学依据。

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引用次数: 0

Preparation of polysaccharide derivatives from the stems of Pleurotus geesteranus and antioxidant and hypoglycemic activities 平菇茎多糖衍生物的制备及其抗氧化和降血糖活性

IF 2.6 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia

Pub Date : 2025-12-25 DOI: 10.1016/j.fitote.2025.107054

Shiyang Zhou , Wenbin Wang , Jie Zhao , Fengming Ren

This study focused on Pleurotus geesteranus stem polysaccharide (PSP), successfully established and optimized their derivatives preparation process. The structures of these derivatives were characterized using ultraviolet spectroscopy, infrared spectroscopy, and ion chromatography-techniques that enabled identification of substituent types, determination of substitution degrees, analysis of monosaccharide compositions, and quantification of molecular weight variations. For antioxidant activity assessment, in vitro chemical models and H₂O₂-induced RAW264.7 cell model confirmed that PSP derivatives exhibit significant antioxidant capacity. Specifically, phosphorylated PSP (PPSP) at a concentration of 3.2 mg/mL exhibited scavenging rates of 98.5 %, 98.4 %, and 96.7 % against DPPH, ABTS, and hydroxyl radicals, respectively, with a total reducing capacity absorbance of 0.96. Additionally, PPSP significantly increased the levels of CAT, SOD, and GSH-Px enzymes in RAW264.7 cells while decreasing MDA content. Hypoglycemic activity was evaluated via α-glucosidase inhibition, α-amylase inhibition, and glucose consumption assays using insulin-resistant HepG2 cells as a model. Results demonstrated that PSP derivatives exerted strong inhibitory effects on α-glucosidase and α-amylase, and dose-dependently enhanced glucose consumption in insulin-resistant HepG2 cells. At 5 mg/mL, PPSP inhibited α-glucosidase and α-amylase activities by 87.3 % and 90.3 %, respectively. This study was systematically investigate their biological activities, thereby providing a novel strategy for the efficient and in-depth utilization of Pleurotus geesteranus resources. The prepared derivatives hold potential applications in functional foods and the pharmaceutical industry. However, the current research was limited to in vitro experiments. Thus, subsequent animal studies and clinical trials were warranted to further explore their in vivo mechanisms of action, pharmacokinetic profiles, and safety characteristics.

本研究以平菇茎多糖（PSP）为研究对象，成功建立并优化了其衍生物的制备工艺。利用紫外光谱、红外光谱和离子色谱技术对这些衍生物的结构进行了表征，这些技术可以识别取代基类型、确定取代度、分析单糖组成和量化分子量变化。体外化学模型和h2o2诱导的RAW264.7细胞模型证实PSP衍生物具有显著的抗氧化能力。在3.2 mg/mL浓度下，磷酸化PSP （PPSP）对DPPH、ABTS和羟基自由基的清除率分别为98.5%、98.4%和96.7%，总还原容量吸光度为0.96。此外，PPSP显著提高RAW264.7细胞中CAT、SOD和GSH-Px酶的水平，降低MDA含量。以胰岛素抵抗型HepG2细胞为模型，通过α-葡萄糖苷酶抑制、α-淀粉酶抑制和葡萄糖消耗测定来评估降糖活性。结果表明，PSP衍生物对胰岛素抵抗的HepG2细胞α-葡萄糖苷酶和α-淀粉酶具有较强的抑制作用，并呈剂量依赖性地增加葡萄糖消耗。在5 mg/mL浓度下，PPSP对α-葡萄糖苷酶和α-淀粉酶活性的抑制作用分别为87.3%和90.3%。本研究旨在系统地研究其生物活性，从而为高效、深入地利用杏鲍菇资源提供新的策略。所制备的衍生物在功能性食品和制药工业中具有潜在的应用前景。然而，目前的研究仅限于体外实验。因此，后续的动物研究和临床试验有必要进一步探索其体内作用机制、药代动力学特征和安全性。

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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

Fitoterapia

Pub 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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