Natural Products and Bioprospecting最新文献

Dayuan Yin alleviates symptoms of HCoV-229E-induced pneumonia and modulates the Ras/Raf1/MEK/ERK pathway 大活络银可缓解 HCoV-229E 诱导的肺炎症状并调节 Ras/Raf1/MEK/ERK 通路。

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-11-04 DOI: 10.1007/s13659-024-00474-8

Rui Li, Wen Zhang, Bei Huang, Guotong Sun, Yifei Xie, Junke Song, Shumei Wang, Guanhua Du

Viral pneumonia is characterized by inflammation in the lungs triggered by respiratory viruses. Dayuan Yin (DYY), a traditional Chinese medicine formula known for treating infectious diseases, is hypothesized to offer therapeutic benefits in treating viral pneumonia, although its specific molecular impacts remain understudied. This study aimed to evaluate the therapeutic effects of DYY in mitigating HCoV-229E virus-induced pneumonia in mice. This study employed an HCoV-229E virus-infected mouse model to investigate the therapeutic potential and underlying molecular mechanisms of DYY on virus-induced pneumonia. The respiratory function and organ indices post-treatment were assessed. Lung tissue and tracheal lesions were evaluated via immunohistochemistry. Spleen immune cell composition was analyzed using flow cytometry. Inflammatory cytokines and viral loads were quantified using hypersensitive multiplex electrochemiluminescence method and PCR analysis, respectively. The expression levels of MAS1, Ras, Raf1, MEK1/2, and ERK1/2 in lung tissues were determined through western blot analysis. DYY significantly improved respiratory function, and reduced organ pathology in infected mice. It effectively decreased viral loads and inflammatory cytokines such as IL-6, IL-1β, and TNF-α in lung tissues. Enhancements in immune response were evidenced by increased CD4/CD8 ratios in the spleen. DYY also notably upregulated MAS1 protein levels and suppressed the activation of the Ras/Raf1/MEK/ERK signaling pathway. DYY enhanced respiratory function and exerted significant antiviral and immunomodulatory effects in mice infected with the HCoV-229E virus, primarily by modulating MAS1 expression and inhibiting the Ras/Raf1/MEK/ERK pathway.

Graphical Abstract

病毒性肺炎是由呼吸道病毒引发的肺部炎症。大活络银（DYY）是一种以治疗感染性疾病而闻名的传统中药配方，被认为对治疗病毒性肺炎有一定疗效，但其具体的分子影响仍未得到充分研究。本研究旨在评估 DYY 对减轻 HCoV-229E 病毒诱导的小鼠肺炎的治疗效果。本研究采用HCoV-229E病毒感染的小鼠模型，研究DYY对病毒诱导的肺炎的治疗潜力和潜在的分子机制。对治疗后的呼吸功能和器官指标进行了评估。通过免疫组化对肺组织和气管病变进行评估。使用流式细胞术分析了脾脏免疫细胞的组成。炎症细胞因子和病毒载量分别采用高敏多重电化学发光法和 PCR 分析法进行量化。通过 Western 印迹分析确定了肺组织中 MAS1、Ras、Raf1、MEK1/2 和 ERK1/2 的表达水平。DYY能明显改善感染小鼠的呼吸功能，减少器官病理变化。它能有效减少肺组织中的病毒载量和炎性细胞因子，如 IL-6、IL-1β 和 TNF-α。脾脏中 CD4/CD8 比率的增加证明了免疫反应的增强。DYY 还能显著上调 MAS1 蛋白水平，抑制 Ras/Raf1/MEK/ERK 信号通路的激活。DYY 主要通过调节 MAS1 的表达和抑制 Ras/Raf1/MEK/ERK 通路，增强了感染 HCoV-229E 病毒的小鼠的呼吸功能，并发挥了显著的抗病毒和免疫调节作用。

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引用次数: 0

Hypecotumines A-D, new isoquinoline alkaloids with potential PCSK9 inhibition activity from Hypecoum erectum L. 具有潜在 PCSK9 抑制活性的新异喹啉生物碱 Hypecotumines A-D from Hypecoum erectum L.

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-10-15 DOI: 10.1007/s13659-024-00479-3

Yinling Wei, Hongyan Wen, Lian Yang, Bodou Zhang, Xiaoyu Li, Sheng Li, Jing Dong, Zhenzhen Liang, Yu Zhang

Four new isoquinoline alkaloids, hypecotumines A-D (1–4), were isolated and identified from the whole herbs of Hypecoum erectum L. Their structures were determined by a combination of HRESIMS, NMR, and X-ray diffraction analysis methods. Compounds 1–4 were characterized by a terminal double bond at C-9 and their plausible biosynthetic pathway was hypothesized. Since PCSK9 plays a key role in the development of cardiovascular disease (CVD), exploration of PCSK inhibitors from natural products are beneficial for drug discovery of CVD treatment. SPR and Western blot assays showed compound 4 had PCSK9 inhibition activity with K_D value of 59.9 µM and thus elevated the LDLR level. Further molecular docking studies demonstrated that 4 and PCSK9 could form stable interactions via key hydrogen bonds.

Graphical Abstract

结合 HRESIMS、核磁共振和 X 射线衍射分析方法确定了它们的结构。化合物 1-4 的特征是 C-9 上有一个末端双键，并假设了其合理的生物合成途径。由于 PCSK9 在心血管疾病（CVD）的发生发展中起着关键作用，因此从天然产物中探索 PCSK 抑制剂有利于发现治疗心血管疾病的药物。SPR 和 Western 印迹分析表明，化合物 4 具有 PCSK9 抑制活性，KD 值为 59.9 µM，从而提高了 LDLR 水平。进一步的分子对接研究表明，化合物 4 与 PCSK9 可通过关键氢键形成稳定的相互作用。

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引用次数: 0

Paeoniflorin mitigates insulin-like growth factor 1-induced lipogenesis and inflammation in human sebocytes by inhibiting the PI3K/Akt/FoxO1 and JAK2/STAT3 signaling pathways 芍药苷通过抑制PI3K/Akt/FoxO1和JAK2/STAT3信号通路，减轻胰岛素样生长因子1诱导的人皮脂细胞脂肪生成和炎症。

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-10-01 DOI: 10.1007/s13659-024-00478-4

Chuanchuan Cai, Si Liu, Yufeng Liu, Shaobin Huang, Shiya Lu, Fang Liu, Xiaohua Luo, Christos C. Zouboulis, Ge Shi

Insulin-like growth factor-1 (IGF-1) is considered as a pathogenic factor contributing to sebaceous gland dysfunction, which leads to acne vulgaris. Paeoniflorin (Pae), a bioactive monomer derived from total glycosides of paeony, has shown potential in treating various diseases. However, its anti-acne effects on human sebocytes are not well understood. In this study, we investigated the effects of Pae on acne development induced by IGF-1 in SZ95 sebocytes. Following IGF-1 stimulation, SZ95 sebocytes were exposed to Pae and then determined for proliferation, cell cycle, apoptosis, lipogenesis and pro-inflammatory cytokine secretion. We also analyzed the expression of proteins involved in the PI3K/Akt/FoxO1 and JAK2/STAT3 pathways. In vitro experiments demonstrated that Pae significantly inhibited colony formation, induced G1/S cell cycle arrest, promoted apoptosis, inhibited lipogenesis and cytokine synthesis in IGF-1-treated SZ95 sebocytes. Furthermore, Pae suppressed the phosphorylation of Akt, FoxO1, JAK2, and STAT3. Importantly, the sebo-suppressive and anti-inflammatory effects of Pae were enhanced by blocking PI3K and JAK2. In summary, our findings suggest that Pae has potent anti-proliferative and pro-apoptotic effects in SZ95 sebocytes. Additionally, Pae effectively protects against IGF-1-induced lipogenesis and inflammation by targeting the PI3K/Akt/FoxO1 and JAK2/STAT3 signaling pathways.

Graphical Abstract

胰岛素样生长因子-1（IGF-1）被认为是导致皮脂腺功能障碍的致病因素，而皮脂腺功能障碍又会导致寻常痤疮。芍药苷（Pae）是从芍药总苷中提取的一种生物活性单体，已显示出治疗多种疾病的潜力。然而，芍药苷对人体皮脂细胞的抗痤疮作用还不甚了解。在这项研究中，我们研究了芍药对 IGF-1 诱导的 SZ95 皮脂细胞痤疮发展的影响。在 IGF-1 刺激下，SZ95 皮脂腺细胞暴露于 Pae，然后测定其增殖、细胞周期、细胞凋亡、脂肪生成和促炎细胞因子分泌。我们还分析了参与 PI3K/Akt/FoxO1 和 JAK2/STAT3 通路的蛋白质的表达。体外实验表明，Pae能明显抑制IGF-1处理的SZ95皮脂腺细胞的集落形成、诱导G1/S细胞周期停滞、促进细胞凋亡、抑制脂肪生成和细胞因子合成。此外，Pae 还能抑制 Akt、FoxO1、JAK2 和 STAT3 的磷酸化。重要的是，阻断 PI3K 和 JAK2 可增强 Pae 的皮脂抑制和抗炎作用。总之，我们的研究结果表明，Pae 在 SZ95 皮脂腺细胞中具有强大的抗增殖和促凋亡作用。此外，Pae 还能通过靶向 PI3K/Akt/FoxO1 和 JAK2/STAT3 信号通路，有效防止 IGF-1 诱导的脂肪生成和炎症。

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引用次数: 0

Expanding horizons of iminosugars as broad-spectrum anti-virals: mechanism, efficacy and novel developments 亚氨基糖作为广谱抗病毒药物的前景：机制、功效和新发展。

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-09-26 DOI: 10.1007/s13659-024-00477-5

Qiantong Liu, Yanyun Liu, Tingting Liu, Jinbao Fan, Zanxian Xia, Yingjun Zhou, Xu Deng

Iminosugars, a class of polyhydroxylated cyclic alkaloids with intriguing properties, hold promising therapeutic potentials against a broad spectrum of enveloped viruses, including DENV, HCV, HIV, and influenza viruses. Mechanistically, iminosugars act as the competitive inhibitors of host endoplasmic reticular α-glucosidases I and II to disrupt the proper folding of viral nascent glycoproteins, which thereby exerts antiviral effects. Remarkably, the glycoproteins of many enveloped viruses are significantly more dependent on the calnexin pathway of the protein folding than most host glycoproteins. Therefore, extensive interests and efforts have been devoted to exploit iminosugars as broad-spectrum antiviral agents. This review provides the summary and insights into the recent advancements in the development of novel iminosugars as effective and selective antiviral agents against a variety of enveloped viruses, as well as the understandings of their antiviral mechanisms.

Graphical Abstract

亚氨基糖苷是一类多羟基环状生物碱，具有引人入胜的特性，对包括 DENV、HCV、HIV 和流感病毒在内的多种包膜病毒具有良好的治疗潜力。从机理上讲，亚氨基糖苷是宿主内质网α-糖苷酶 I 和 II 的竞争性抑制剂，能破坏病毒新生糖蛋白的正常折叠，从而发挥抗病毒作用。值得注意的是，与大多数宿主糖蛋白相比，许多包膜病毒的糖蛋白更依赖于蛋白质折叠的钙粘蛋白途径。因此，人们对利用亚氨基糖作为广谱抗病毒剂投入了广泛的兴趣和努力。本综述总结并深入探讨了最近在开发新型亚氨基糖作为有效和选择性抗病毒药物以对抗多种包膜病毒方面取得的进展，以及对其抗病毒机制的理解。

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引用次数: 0

Recent advances in pharmaceutical cocrystals of theophylline 茶碱药用共晶体的最新进展

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-09-14 DOI: 10.1007/s13659-024-00470-y

Yanxiao Jia, Dezhi Yang, Wenwen Wang, Kun Hu, Min Yan, Li Zhang, Li Gao, Yang Lu

Currently, cocrystallization is a promising strategy for tailoring the physicochemical properties of active pharmaceutical ingredients. Theophylline, an alkaloid and the most primary metabolite of caffeine, is a readily available compound found in tea and coffee. It functions primarily as a bronchodilator and respiratory stimulant, making it a mainstay treatment for lung diseases like asthma. Theophylline’s additional potential benefits, including anti-inflammatory and anticancer properties, and its possible role in neurological disorders, have garnered significant research interest. Cocrystal formation presents a viable approach to improve the physicochemical properties of theophylline and potentially mitigate its toxic effects. This review comprehensively explores several successful studies that utilized cocrystallization to favorably alter the physicochemical properties of theophylline or its CCF. Notably, cocrystals can not only enhance the solubility and bioavailability of theophylline but also exhibit synergistic effects with other APIs. The review further delves into the hydrogen bonding sites within the theophylline structure and the hydrogen bonding networks observed in cocrystal structures.

Graphical Abstract

目前，共晶是一种很有前途的定制活性药物成分理化特性的策略。茶碱是一种生物碱，也是咖啡因最主要的代谢产物，是一种在茶叶和咖啡中很容易找到的化合物。它的主要功能是支气管扩张剂和呼吸兴奋剂，是治疗哮喘等肺部疾病的主要药物。茶碱的其他潜在益处，包括抗炎和抗癌特性，以及在神经系统疾病中可能发挥的作用，引起了研究人员的极大兴趣。形成可可结晶是改善茶碱理化性质并减轻其毒性作用的一种可行方法。本综述全面探讨了几项成功利用共晶体化改变茶碱或其CCF理化性质的研究。值得注意的是，共晶体不仅能提高茶碱的溶解度和生物利用度，还能与其他原料药产生协同效应。本综述进一步探讨了茶碱结构中的氢键位点以及在共晶体结构中观察到的氢键网络。

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引用次数: 0

Grewiifopenes A–K, bioactive clerodane diterpenoids from Casearia grewiifolia Vent. Grewiifopenes A-K, bioactive clerodane diterpenoids from Casearia grewiifolia Vent.

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-09-14 DOI: 10.1007/s13659-024-00475-7

Phanruethai Pailee, Paratchata Batsomboon, Wiriya Yaosanit, Theerawat Thananthaisong, Chulabhorn Mahidol, Poonsakdi Ploypradith, Nanthawan Reuk-ngam, Panita Khlaychan, Supanna Techasakul, Somsak Ruchirawat, Vilailak Prachyawarakorn

Eleven novel clerodane-type diterpenoids, grewiifopenes A–K (1–4 and 12–18), along with nine known compounds (5–11, 19, and 20) were purified from the dichloromethane extract of the twigs and stems of Casearia grewiifolia Vent. (Salicaceae). Their spectroscopic data, including the NMR, HRESIMS, and electronic circular dichroism calculations were employed to completely characterize and elucidate the chemical structures and absolute configurations. The clerodane diterpenoids possessing a 6-OH group and no substitution at C-7 exhibited greater cytotoxic activity than others, with their IC₅₀ values ranging from 0.3 to 2.9 μM. Isocaseamembrin E (7) exhibited antibacterial activity against Staphylococcus aureus, while isocaseamembrin E (7), corymbulosin X (8), caseargrewiin A (9), kurzipene A (10), and balanspene F (11) exhibited antibacterial activity against Bacillus cereus.

Graphical Abstract

从盐肤木（Casearia grewiifolia Vent.，莎草科）的小枝和茎的二氯甲烷提取物中纯化了 11 个新的萜类化合物，即 grewiifopenes A-K（1-4 和 12-18），以及 9 个已知化合物（5-11、19 和 20）。研究人员利用核磁共振、HRESIMS 和电子圆二色性计算等光谱数据，完整地描述和阐明了这些化合物的化学结构和绝对构型。与其他化合物相比，具有一个 6-OH 基团且 C-7 没有被取代的萜类二萜具有更强的细胞毒活性，其 IC50 值介于 0.3 至 2.9 μM 之间。Isocaseamembrin E (7) 对金黄色葡萄球菌具有抗菌活性，而 isocaseamembrin E (7)、corymbulosin X (8)、caseargrewiin A (9)、kurzipene A (10) 和 balanspene F (11) 对蜡样芽孢杆菌具有抗菌活性。

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引用次数: 0

Structure characterization and immunoactivity on dendritic cells of two neutral polysaccharides from Dictyophora rubrovalvata 红豆杉中两种中性多糖的结构特征及对树突状细胞的免疫活性

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-09-14 DOI: 10.1007/s13659-024-00476-6

Ni Huang, Yi-Na Yang, Jia Huang, Hui-Yan Shao, Yan-Lang Li, Shi-Hui Qin, Han-Fen Li, Xiao-Jiang Shen, Liu Yang, Jiang-Miao Hu

Dictyophora rubrovalvata is a valuable fungus homologous to food and medicine, and its polysaccharide have been gaining increasing attention because of its plentiful activity. However, the structure and activity of its homogeneous polysaccharide have not been studied enough. In this study, two polysaccharides DRP-I and DRP-II were purified from D. rubrovalvata. Their structures were characterized by chemical composition, monosaccharide composition analysis, methylation analysis and nuclear magnetic resonance spectroscopy. The results showed that DRP-I and DRP-II were neutral heteropolysaccharides with molecular weights of 5.79 × 10³ and 1.25 × 10⁴ Da, respectively, which were composed of mannose, galactose, glucose, xylose and fucose. The main chains were → 6)-α-D-Galp-(1 → 6)-α-D-Galp-(2,1 → 6)-α-D-Manp-(2,1 → 6)-α-D-Galp-(1, and branch chains were β-D-Xylp-(1 → 3)-α-L-Fucp-(1 → 4)-α-D-Manp-(1 → and α-D-Galp-(1 → 3)-α-D-Galp-(1 → . The in vitro immunoactivity assays on dendritic cells showed that DRP-I and DRP-II could up-regulate the expression of IL-10 and IL-6 and inhibit the expression of TNF-α in a concentration-dependent manner. This research indicated that DRP-I and DRP-II possessed immunoactivity by balancing the excessive inflammation, and molecular weight is an important factor affecting immunoactivity.

Graphical Abstract

红豆杉（Dictyophora rubrovalvata）是一种药食同源的珍贵真菌，其多糖因具有丰富的活性而日益受到人们的关注。然而，人们对其均质多糖的结构和活性研究还不够。本研究从 D. rubrovalvata 中纯化了两种多糖 DRP-I 和 DRP-II。通过化学成分、单糖成分分析、甲基化分析和核磁共振波谱对它们的结构进行了表征。结果表明，DRP-I 和 DRP-II 为中性杂多糖，分子量分别为 5.79 × 103 和 1.25 × 104 Da，由甘露糖、半乳糖、葡萄糖、木糖和岩藻糖组成。主链为 → 6）-α-D-Galp-（1 → 6）-α-D-Galp-（2,1 → 6）-α-D-Manp-（2,1 → 6）-α-D-Galp-（1），支链为β-D-Xylp-（1 → 3）-α-L-Fucp-（1 → 4）-α-D-Manp-（1 → 1）和α-D-Galp-（1 → 3）-α-D-Galp-（1 → 1）。对树突状细胞进行的体外免疫活性试验表明，DRP-I 和 DRP-II 能上调 IL-10 和 IL-6 的表达，并能抑制 TNF-α 的表达，其表达呈浓度依赖性。这项研究表明，DRP-I和DRP-II具有平衡过度炎症的免疫活性，而分子量是影响免疫活性的重要因素。图文摘要

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引用次数: 0

Micro-scale screening of genetically modified Fusarium fujikuroi strain extends the apicidin family 转基因 Fusarium fujikuroi 菌株的微尺度筛选扩展了凋萎素家族。

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-08-23 DOI: 10.1007/s13659-024-00473-9

Alica Fischle, Mika Lutsch, Florian Hübner, Linda Schäker-Hübner, Lina Schürmann, Finn K. Hansen, Svetlana A. Kalinina

Apicidins are a class of naturally occurring cyclic tetrapeptides produced by few strains within the Fusarium genus. These secondary metabolites have gained significant attention due to their antiprotozoal activity through HDAC inhibition, thereby highlighting their potential for the treatment of malaria. Predominantly, apicidins have been isolated from Fusarium semitectum, offering a deep insight into the biosynthetic pathway responsible for their formation. A similar biosynthetic gene cluster has also been identified in the rice pathogenic fungus F. fujikuroi, leading the discovery of three additional apicidins through genetic manipulation. Routine mass spectrometric screening of these compound-producing strains revealed another metabolite structurally related to previously studied apicidins. By optimizing culture conditions and developing an effective isolation method, we obtained a highly pure substance, whose chemical structure was fully elucidated using NMR and HRMS fragmentation. Further studies were conducted to determine cytotoxicity, antimalarial activity, and HDAC inhibitory activity of this new secondary metabolite alongside the previously known apicidins. This work not only expands the apicidin class with a new member but also provides extensive insights and comparative analysis of apicidin-like substances produced by F. fujikuroi.

Graphical Abstract

表皮苷是镰刀菌属中少数菌株产生的一类天然环状四肽。由于这些次生代谢物通过抑制 HDAC 而具有抗原虫活性，从而凸显了其治疗疟疾的潜力，因此备受关注。主要是从半知菌镰刀菌中分离出的芹菜苷，使人们对形成芹菜苷的生物合成途径有了深入的了解。在水稻致病真菌 F. fujikuroi 中也发现了一个类似的生物合成基因簇，从而通过基因操作发现了另外三种芹菜素。通过对这些产生化合物的菌株进行常规质谱筛选，发现了另一种与之前研究的芹菜素在结构上相关的代谢物。通过优化培养条件和开发有效的分离方法，我们获得了一种高纯度物质，并利用核磁共振和 HRMS 片段分析法完全阐明了其化学结构。我们还进一步研究了这种新的次生代谢物的细胞毒性、抗疟活性和 HDAC 抑制活性。这项研究不仅为蛛红素类化合物增加了一个新成员，而且还对由 F. fujikuroi 产生的蛛红素类物质进行了深入的了解和比较分析。

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引用次数: 0

Purification and immobilization of β-glucosidase using surface modified mesoporous silica Santa Barbara Amorphous 15 for eco-friendly preparation of sagittatoside A 利用表面改性介孔二氧化硅 Santa Barbara Amorphous 15 纯化和固定化β-葡萄糖苷酶，以环保方式制备沙葛苷 A。

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-08-23 DOI: 10.1007/s13659-024-00471-x

Ya-Ya Yang, Shun-Li Jing, Jia-Li Shao, Ji-Xuan Chen, Wei-Feng Zhang, Si-Yuan Wan, Yu-Ping Shen, Huan Yang, Wei Yu

Functionalized mesoporous materials have become a promising carrier for enzyme immobilization. In this study, Santa Barbara Amorphous 15 (SBA-15) was modified by N-aminoethyl-γ-aminopropyl trimethoxy (R). R-SBA-15 was employed to purify and immobilize recombinant β-glucosidase from Terrabacter ginsenosidimutans (BgpA) in one step for the first time. Optimum pH of the constructed R-SBA-15@BgpA were 7.0, and it has 20 ℃ higher optimal temperature than free enzyme. Relative activity of R-SBA-15@BgpA still retained > 70% at 42 ℃ after 8-h incubation. The investigation on organic reagent resistance revealed that the immobilized enzyme can maintain strong stability in 15% DMSO. In leaching test and evaluation of storage stability, only trace amount of protein was detected in buffer of the immobilized enzyme after storage at 4 ℃ for 33 days, and the immobilized BgpA still maintained > 50% relative activity. It also demonstrated good reusability, with 76.1% relative activity remaining after fourteen successive enzymatic hydrolyses of epimedin A to sagittatoside A. The newly proposed strategy is an effective approach for the purification and immobilization of BgpA concurrently. In addition, R-SBA-15@BgpA was demonstrated to have high efficiency and stability in this application, suggesting its great feasibility and potential to produce bioactive compounds such as secondary glycosides or aglycones from natural products.

Graphical Abstract

功能化介孔材料已成为一种很有前景的酶固定载体。在本研究中，Santa Barbara Amorphous 15（SBA-15）被 N-氨乙基-γ-氨丙基三甲氧基（R）修饰。R-SBA-15 首次被用于从 Terrabacter ginsenosidimutans（BgpA）中一次性纯化和固定重组β-葡萄糖苷酶。构建的 R-SBA-15@BgpA 的最适 pH 值为 7.0，最适温度比游离酶高 20 ℃。在 42 ℃ 下培养 8 h 后，R-SBA-15@BgpA 的相对活性仍保持在 70% 以上。对有机试剂耐受性的研究表明，固定化酶在 15%二甲基亚砜中能保持较强的稳定性。在浸出试验和贮存稳定性评价中，固定化酶在 4 ℃下贮存 33 天后，缓冲液中仅检测到微量蛋白质，固定化 BgpA 仍能保持大于 50%的相对活性。新提出的策略是同时纯化和固定 BgpA 的有效方法。此外，R-SBA-15@BgpA 在该应用中被证明具有高效性和稳定性，这表明它在从天然产物中生产次生苷或苷元等生物活性化合物方面具有极大的可行性和潜力。

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引用次数: 0

Harnessing the power of Arctium lappa root: a review of its pharmacological properties and therapeutic applications 利用牛蒡根的力量：药理特性和治疗应用综述。

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL

Natural Products and Bioprospecting

Pub Date : 2024-08-20 DOI: 10.1007/s13659-024-00466-8

Mukul Shyam, Evan Prince Sabina

Arctium lappa, widely recognized as burdock, is a perennial plant that is employed in the realm of traditional Chinese medicine for a wide range of medicinal applications. The herb is rich in bioactive metabolites with therapeutic potential, encompassing polyphenolic antioxidants in its leaves, and flavonoids and fructo-oligosaccharides in its underground parts. Nutraceuticals originating from botanical sources such as Arctium lappa provide supplementary health advantages alongside their nutritional content and have demonstrated effectiveness in the prevention and management of specific ailments. The utilization of Arctium lappa root extract has exhibited encouraging outcomes in addressing hepatotoxicity induced by cadmium, lead, chromium, and acetaminophen, ameliorating liver damage and oxidative stress. Additionally, the root extract displays properties such as antidiabetic, hypolipidemic, aphrodisiac, anti-rheumatic, anti-Alzheimer, and various other pharmacological actions.

Graphical abstract

牛蒡（Arctium lappa）被广泛认为是牛蒡，是一种多年生植物，在传统中药领域具有广泛的药用价值。牛蒡富含具有治疗潜力的生物活性代谢物，叶片中含有多酚抗氧化剂，地下部分含有类黄酮和果寡糖。源自牛蒡等植物资源的保健食品除营养成分外，还具有补充保健的优势，在预防和治疗特定疾病方面已证明十分有效。在解决镉、铅、铬和对乙酰氨基酚引起的肝毒性方面，使用牛蒡根提取物已取得令人鼓舞的成果，可改善肝损伤和氧化应激。此外，牛蒡根提取物还具有抗糖尿病、降血脂、壮阳、抗风湿、抗老年痴呆等多种药理作用。

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引用次数: 0