Journal of Natural Medicines最新文献_第10页

Extraction, characterization, and biological activities of a novel polysaccharide extract from Fructus caryophylli 一种新型石竹多糖提取物的提取、表征及生物活性研究。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-23 DOI: 10.1007/s11418-025-01891-w

Qingtao Yu, Wenzhi Li, Jieyi Long, Ming Liang, Lingli Jiang, Xiaoliang Lin, Dongqing He, Zhuoyan Wu, Xiaole Xia

This study showed that Polysaccharide-rich Fructus caryophylli extracts (FCE) were prepared for investigation through hot water extraction. Glucose was found to be the significant monosaccharide by chemical analysis, which included Fourier transform-infrared (FT-IR), high-performance liquid chromatography (HPLC), and high-performance gel permeation chromatography (HPGPC). The average molecular weight of FCE was ranged from 15.19 and 208.53 kDa. The bioactivities of FCE, including antioxidant, whitening, tissue regeneration, and anti-wrinkle properties, were evaluated using both in vitro and in vivo tests. In vitro antioxidant experiments demonstrated scavenging of 1,1-Diphenyl-2-picrylhydrazyl (DPPH), 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), hydroxyl radicals, and strong reducing power. FCE treatment effectively reduced oxidative stress in an in vivo antioxidant experiment involving zebrafish embryos exposed to a nonlethal dose of LPS, demonstrating its potent antioxidant potential. Furthermore, FCE exhibited promise in decreasing tyrosinase activity and total melanin content in zebrafish embryos, while promoting the relative expression levels of the elastin-regulating gene Eln1 RNA and the collagen-related gene col1a1a, thereby facilitating the positive stimulation of wound healing. This research provides valuable insights into the development of FCE as a novel functional raw material for applications in the food and cosmetics industries.

Graphical abstract

本研究采用热水浸提法制备了富含多糖的山核桃提取物（FCE）。通过傅里叶变换红外（FT-IR）、高效液相色谱（HPLC）和高效凝胶渗透色谱（HPGPC）分析，发现葡萄糖是主要的单糖。FCE的平均分子量为15.19 ~ 208.53 kDa。FCE的生物活性，包括抗氧化、美白、组织再生和抗皱性能，通过体外和体内试验进行了评估。体外抗氧化实验表明，其具有清除1,1-二苯基-2-吡啶肼（DPPH）、2,2'-氮基-双（3-乙基苯并噻唑-6-磺酸）、羟基自由基和较强的还原能力。在一项体内抗氧化实验中，FCE处理有效地降低了暴露于非致死剂量LPS的斑马鱼胚胎的氧化应激，证明了其强大的抗氧化潜力。此外，FCE有可能降低斑马鱼胚胎中酪氨酸酶活性和总黑色素含量，同时促进弹性蛋白调节基因Eln1 RNA和胶原相关基因col1a1a的相对表达水平，从而促进伤口愈合的积极刺激。该研究为FCE作为一种新型功能性原料在食品和化妆品行业的应用提供了有价值的见解。

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引用次数: 0

Multi-omics analysis reveals tissue-specific biosynthesis and accumulation of diterpene alkaloids in Aconitum japonicum 多组学分析揭示了日本乌头中二萜生物碱的组织特异性生物合成和积累。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-20 DOI: 10.1007/s11418-025-01881-y

Megha Rai, Amit Rai, Tetsuya Mori, Ryo Nakabayashi, Michimi Nakamura, Marsheige Kojoma, Hideyuki Suzuki, Kazuki Saito, Mami Yamazaki

Aconitum japonicum, native to the mountainous regions of Japan, is a toxic perennial plant widely recognized for its therapeutic potential. Despite its pharmacological importance, the complete biosynthetic pathway of diterpene alkaloids, bioactive compounds with significant pharmaceutical implications and derived from Aconitum species, remains elusive. In this study, leveraging high-throughput metabolome and transcriptome analyses, we conducted a comprehensive investigation using four tissues of A. japonicum, including leaf, mother root, daughter root, and rootlet. By integrating these multi-omics datasets, we achieved a holistic insight into the gene expression patterns and metabolite profiles intricately linked with diterpene alkaloid biosynthesis. Our findings unveil potential regulatory networks and pinpoint key candidate genes pivotal in diterpene alkaloid synthesis. Through comparative analyses across tissues, we delineate tissue-specific variations in gene expression and metabolite accumulation, shedding light on the spatial regulation of these biosynthetic pathways within the plant. Furthermore, this study contributes to a deeper understanding of the molecular mechanisms dictating the production of diterpene alkaloids in A. japonicum. Besides advancing our knowledge of plant secondary metabolism in A. japonicum, this study also provides a high-quality multi-omics resource for future studies aimed at functionally characterizing the target genes involved in different metabolic processes.

Graphical abstract

Aconitum japonicum（日本乌头）原产于日本山区，是一种有毒的多年生植物，其治疗潜力得到广泛认可。尽管乌头具有重要的药理作用，但从乌头中提取的具有重要药用价值的生物活性化合物--二萜生物碱的完整生物合成途径仍然难以确定。在本研究中，我们利用高通量代谢组和转录组分析，对日本牡丹的四个组织（包括叶、母根、子根和小根）进行了全面研究。通过整合这些多组学数据集，我们全面了解了与二萜生物碱生物合成密切相关的基因表达模式和代谢物谱。我们的研究结果揭示了潜在的调控网络，并确定了在二萜生物碱合成过程中起关键作用的候选基因。通过对不同组织的比较分析，我们划定了基因表达和代谢物积累的组织特异性变化，揭示了植物内部这些生物合成途径的空间调控。此外，这项研究还有助于加深对日本椿生产二萜生物碱的分子机制的理解。除了增进我们对日本鸦胆子植物次生代谢的了解外，本研究还为今后旨在从功能上鉴定参与不同代谢过程的靶基因的研究提供了高质量的多组学资源。

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引用次数: 0

Correlation between the metabolic profile of Nelumbo Seed, a component of Seishinrenshiin, and its inhibitory activity on bladder smooth muscle contraction 参参仁心素成分莲子代谢谱与膀胱平滑肌收缩抑制活性的相关性研究。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-19 DOI: 10.1007/s11418-025-01889-4

Kazuo Harada, Yuki Fukuda, Takahiro Ohkubo, Kimio Sugaya, Yukihiko Osaki

Seishinrenshiin (SRI), a Kampo formula, is often used for frequent urination. Nelumbo Seed, a crude-drug component of SRI was reported to inhibit bladder smooth muscle contraction using excised rat bladder tissues. However, the active ingredients of Nelumbo Seed have not yet been identified. In this study, we investigated the active ingredients of Nelumbo Seed that inhibit bladder smooth muscle contraction. We obtained liquid chromatography/mass spectrometry profiles of extracts prepared from five types of Nelumbo Seed materials from different production areas and evaluated their inhibitory effects on excised rat bladder smooth muscle contraction. Analysis of these data using orthogonal projections to latent structures revealed neferine (Nef) as the compound with the highest variable influence on projection. Among the Nelumbo Seed materials processed using different methods, the Nef content was the highest in ‘Sekirenshi’, when embryo and pericarp were not removed at all. We determined the effects of administering Nelumbo Seed extracts with different Nef content on frequent-urination model rats. The Nef content in rat plasma was the highest when the Sekirenshi extract was administered, but Nef was not detected when seed embryos were removed. In this model, administration of the Nelumbo Seed extract improved the maximum bladder contraction pressure and bladder contraction interval, albeit not significantly. In particular, Sekirenshi tended to reduce the maximum bladder contraction pressure compared to other Nelumbo Seed. Our results indicate that although Nef in Nelumbo Seed does not clearly improve frequent urination, it might contribute to the improvement of urination disorder.

Graphical Abstract

Seishinrenshiin （SRI）是一种柬埔寨配方，常用于尿频。Nelumbo Seed是SRI的一种原料药成分，据报道可以抑制切除的大鼠膀胱组织的膀胱平滑肌收缩。然而，莲蓬籽的有效成分尚未被确定。在本研究中，我们研究了莲籽抑制膀胱平滑肌收缩的有效成分。我们获得了不同产地五种莲属植物种子材料提取物的液相色谱/质谱分析，并评价了其对大鼠膀胱平滑肌收缩的抑制作用。利用对潜在结构的正交投影对这些数据进行分析，发现碱（Nef）是对投影变量影响最大的化合物。在不同处理方法的莲蓬种子材料中，未去胚和未去果皮的“塞克仁石”的Nef含量最高。研究了不同Nef含量的莲子提取物对尿频模型大鼠的影响。大鼠血浆中Nef含量在给药时最高，但在去胚时未检测到Nef。在该模型中，给药莲籽提取物改善了膀胱最大收缩压力和膀胱收缩间隔，但不显著。特别是，与其他莲子相比，Sekirenshi倾向于降低膀胱最大收缩压力。我们的研究结果表明，虽然莲子中的Nef对尿频没有明显的改善作用，但它可能有助于改善排尿障碍。

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引用次数: 0

New oxepin and dihydrobenzofuran derivatives from Bauhinia saccocalyx roots and their anti-inflammatory, cytotoxic, and antioxidant activities 从洋紫荆根中提取的新氧杂卓素和二氢苯并呋喃衍生物及其抗炎、细胞毒性和抗氧化活性。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-14 DOI: 10.1007/s11418-025-01888-5

Lueacha Tabtimmai, Thanyathon Phonchan, Natrinee Thongprik, Sutin Kaennakam, Nuttapon Yodsin, Kiattawee Choowongkomon, Chanikan Sonklin, Supachai Jadsadajerm, Awat Wisetsai

Four new oxepin and dihydrobenzofuran derivatives, saccoxepins A–C (1–3) and saccobenzofurin A (4), along with one known compound, bauhinoxepin A (5), were isolated from the roots of Bauhinia saccocalyx. The structures were elucidated by extensive analysis of spectroscopic data in combination with ECD analysis. The EtOAc extract exhibited significant NO inhibition (94.4 ± 0.35%, 50 μg/mL), and saccoxepin A and bauhinoxepin A demonstrated strong NO suppression, with IC₅₀ values of 49.35 µM and 30.28 µM, respectively, alongside notable antioxidant activity. Saccoxepin A and bauhinoxepin A selectively reduced interleukin-6 (IL-6) levels, while bauhinoxepin A slightly lowered tumor necrosis factor-alpha (TNF-α) at a low dose. Furthermore, bauhinoxepin A exhibited cytotoxicity against HCT-116 cells, with an IC₅₀ of 8.88 µM. These findings suggest that the roots of B. saccocalyx possess potent antioxidant, anti-inflammatory, and anticancer activities, supporting its traditional medicinal applications and highlighting its potential as a source of therapeutic agents.

Graphical abstract

从洋紫荆（Bauhinia saccocalyx）的根部分离出了四种新的氧西平和二氢苯并呋喃衍生物，即囊果西平 A-C (1-3) 和囊果苯并呋喃 A (4)，以及一种已知化合物，即洋紫荆氧西平 A (5)。通过结合 ECD 分析对光谱数据进行广泛分析，阐明了这些化合物的结构。EtOAc 提取物对 NO 有明显的抑制作用（94.4 ± 0.35%，50 μg/mL），Saccoxepin A 和 bauhinoxepin A 对 NO 有很强的抑制作用，IC50 值分别为 49.35 µM 和 30.28 µM，同时还具有显著的抗氧化活性。Saccoxepin A 和 bauhinoxepin A 选择性地降低了白细胞介素-6（IL-6）的水平，而 bauhinoxepin A 则在低剂量时略微降低了肿瘤坏死因子-α（TNF-α）的水平。此外，牛黄解毒片 A 对 HCT-116 细胞具有细胞毒性，IC50 为 8.88 µM。这些研究结果表明，B. saccocalyx 的根具有强大的抗氧化、抗炎和抗癌活性，支持其传统医学应用，并突出了其作为治疗药物来源的潜力。

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引用次数: 0

Growth characteristics, optimal harvest timing, and quality assessment of three Evodia species cultivated in Japan 日本栽培的三种吴茱萸的生长特性、最佳采收时机及品质评价。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-12 DOI: 10.1007/s11418-025-01886-7

Koji Sugimura, Raju Aedla, Hiroyuki Fuchino, Osamu Iida, Takashi Watanabe

Immature Evodia fruits are used in herbal medicine for their analgesic properties; however, determining the appropriate time for harvesting these fruits remains challenging. Here, we investigated the growth characteristics and optimal timing for collecting the immature fruits of three Evodia species—E. rutaecarpa (Juss.) Benth., E. officinalis Dode, and E. hupehensis Dode—cultivated at the Tanegashima Division of the Research Center for Medicinal Plant Resources, Japan. Evodiamine and rutaecarpine content in the three species were measured across different collection seasons, and the relationship between time elapsed from the start of flowering and the levels of these active ingredients was determined. We found that the optimal time to collect the immature fruits of E. officinalis for use in herbal medicine was 2 weeks after flowering, when the fruit was heavier, contained more active ingredients, and had not yet dehisced. E. rutaecarpa fruits were heavier, contained more active ingredients, and retained their color (orange) until 3 weeks post-flowering. This suggests that the optimal collection time varied among species. Overall, E. rutaecarpa was the most suitable species for cultivation in Japan for use in herbal medicines because its optimal collection time was easier to determine, and its pericarp and seeds did not separate during drying. Therefore, to efficiently harvest Evodia fruits, cultivation methods should be optimized to leverage the specific growth characteristics of each species, with particular emphasis on accurately determining the optimal harvest time.

Graphical abstract

未成熟的吴茱萸果实因其镇痛特性而被用作草药；然而，确定收获这些水果的适当时间仍然具有挑战性。本文研究了三种吴茱萸的生长特性和最佳采收时机。rutaecarpa(权利)。Benth。日本药用植物资源研究中心种子岛分所栽培的黄芪、黄芪和黄芪。在不同的采收季节测量了3种植物中Evodiamine和rutaecarpine的含量，并确定了开花时间与这些活性成分含量的关系。我们发现，在开花后的2周内，是采收officinalis未成熟果实的最佳时间，此时果实较重，含有较多的有效成分，并且尚未开裂。芦杉果实较重，含有较多的有效成分，并保持其颜色（橙色），直到开花后3周。这表明最佳采集时间因物种而异。综上所述，因其最佳采收时间较易确定，且干燥过程中果皮和种子不分离，是最适合在日本种植的中药材品种。因此，为了有效地收获吴茱萸果实，应优化栽培方法，充分利用每个物种的特定生长特性，特别注重准确确定最佳采收时间。

{"title":"Growth characteristics, optimal harvest timing, and quality assessment of three Evodia species cultivated in Japan","authors":"Koji Sugimura, Raju Aedla, Hiroyuki Fuchino, Osamu Iida, Takashi Watanabe","doi":"10.1007/s11418-025-01886-7","DOIUrl":"10.1007/s11418-025-01886-7","url":null,"abstract":"<div><p>Immature <i>Evodia</i> fruits are used in herbal medicine for their analgesic properties; however, determining the appropriate time for harvesting these fruits remains challenging. Here, we investigated the growth characteristics and optimal timing for collecting the immature fruits of three <i>Evodia</i> species—<i>E. rutaecarpa</i> (Juss.) Benth.<i>, E. officinalis</i> Dode<i>,</i> and <i>E. hupehensis</i> Dode—cultivated at the Tanegashima Division of the Research Center for Medicinal Plant Resources, Japan. Evodiamine and rutaecarpine content in the three species were measured across different collection seasons, and the relationship between time elapsed from the start of flowering and the levels of these active ingredients was determined. We found that the optimal time to collect the immature fruits of <i>E. officinalis</i> for use in herbal medicine was 2 weeks after flowering, when the fruit was heavier, contained more active ingredients, and had not yet dehisced. <i>E. rutaecarpa</i> fruits were heavier, contained more active ingredients, and retained their color (orange) until 3 weeks post-flowering. This suggests that the optimal collection time varied among species. Overall, <i>E. rutaecarpa</i> was the most suitable species for cultivation in Japan for use in herbal medicines because its optimal collection time was easier to determine, and its pericarp and seeds did not separate during drying. Therefore, to efficiently harvest <i>Evodia</i> fruits, cultivation methods should be optimized to leverage the specific growth characteristics of each species, with particular emphasis on accurately determining the optimal harvest time.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"79 3","pages":"656 - 665"},"PeriodicalIF":2.5,"publicationDate":"2025-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s11418-025-01886-7.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143612916","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Leptomonines A and B, two novel rare benzyltetrahydroisoquinoline N-oxides from the aerial parts of Leptopyrum fumarioides as potential COX-2 inhibitors: in vitro and in silico studies Leptomonines A和B，两种新的稀有苯四氢异喹啉n -氧化物作为潜在的COX-2抑制剂：体外和硅研究。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-07 DOI: 10.1007/s11418-025-01882-x

Tserendorj Solongo, Tran Thu Huong, Erdenetsogt Purevdorj, Amgalan Solongo, Battsagaan Bayasgalan, Vu Thanh Loc, Nguyen Xuan Ha, Vu Thi Ha, Nguyen Phi Hung, Do Thi Thao, Nguyen Thi Nga, Hai Pham- The, Pauline Stark, Nguyen Manh Cuong

Leptomonines A and B, two novel rare benzyltetrahydroisoquinoline N-oxides, were isolated from the aerial parts of Leptopyrum fumarioides (L.) Reichenb. collected in Tuv province, Mongolia. Their chemical structures, absolute configurations, and conformations were established by 2D-NMR and CD spectral analyses. Leptomonine A (1) can suppress TNF-α production and COX-2 expression in LPS-stimulated RAW 267.4 cells. This compound at a concentration of 100 µM significantly reduced the TNF-α and COX-2 levels by 36.43% and 47.10%, respectively, compared with the negative control. Moreover, leptomonine B (2) remarkably lowers COX-2 levels at the highest concentration. The docking simulations were conducted with the COX-2 enzyme and revealed the binding ability of leptomonine A (1) and leptomonine B (2) with binding energies of − 9.03 and − 8.96 kcal/mol, respectively. The interactions of these alkaloids with the targets were mainly with the hydrophobic and hydrophilic sites, which are quite similar to rofecoxib. Phytochemical investigation revealed the diversity and novelty of the natural isoquinoline alkaloids in Leptopyrum fumarioides. Two new benzyltetrahydroisoquinoline N-oxides were identified as the bioactive constituents of Leptopyrum fumarioides by assessing its anti-inflammatory effects. The findings provide scientific justification to support the traditional application of Leptopyrum fumarioides for treating liver diseases associated with inflammation.

Graphical Abstract

从黄缕草（Leptopyrum fumarioides， L.）的地上部分中分离到两种新的稀有苯四氢异喹啉n -氧化物——Leptomonines A和B。Reichenb。采自蒙古图夫省。通过二维核磁共振和CD谱分析确定了它们的化学结构、绝对构型和构象。Leptomonine A(1)可以抑制lps刺激的RAW 267.4细胞中TNF-α的产生和COX-2的表达。该化合物浓度为100µM时，与阴性对照相比，TNF-α和COX-2水平分别降低36.43%和47.10%。此外，leptomonine B(2)在最高浓度下显著降低COX-2水平。通过与COX-2酶的对接模拟，揭示了leptomonine A(1)和leptomonine B(2)的结合能力，结合能分别为- 9.03和- 8.96 kcal/mol。这些生物碱与靶标的相互作用主要是在疏水性和亲水性位点，这与罗非昔布非常相似。植物化学研究揭示了黄缕草中天然异喹啉类生物碱的多样性和新颖性。通过对两种新型苯四氢异喹啉n -氧化物的抗炎活性评价，鉴定出两种新型的苯四氢异喹啉n -氧化物为富马黄芪的生物活性成分。该研究结果为支持传统应用瘦毒治疗与炎症相关的肝脏疾病提供了科学依据。

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引用次数: 0

Grandifolins A–D: three 6/6/5 abietane diterpenes and an abietane diterpene from Salvia grandifolia 桔梗苷A-D：三种6/6/5枞烷二萜和一种来自桔梗的枞烷二萜。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-02 DOI: 10.1007/s11418-025-01884-9

Hiroshi Kawabe, Teppei Komiyama, Yoshinori Saito, Yasuko Okamoto, Emi Hara, Keiichi Matsuzaki, Motoo Tori, Ryo Hanai, Hiroshi Hirota, Xun Gong, Chiaki Kuroda, Hiroyuki Kagechika, Ayumi Ohsaki

The genus Salvia is a well-established source of biologically active compounds with beneficial health effects. In this study, we aimed to isolate and structurally characterize novel compounds from Salvia grandifolia and evaluate their cytotoxic activity against human promyelocytic leukemia (HL-60) and cervical cancer (HeLa) cell lines. Three new rearranged abietane-type diterpenes, grandifolins A–C (1–3) and a new abietane diterpene, grandifolin D (4), were isolated from the roots of Salvia grandifolia, along with 12 known compounds (5–16). Their structures were determined by combining extensive ¹H and ¹³C spectroscopy, X-ray crystallography, and electronic circular dichroism spectra (ECD). The skeletons of 1–3 had a rearranged structure with a 6/6/5 ring from an abietane-type diterpene. A plausible biosynthetic pathway for the rearranged skeleton was also proposed. Many of the isolated compounds showed weak cytotoxicity against HeLa or HL-60 cell lines.

Graphical abstract

鼠尾草属是一种公认的具有有益健康作用的生物活性化合物来源。在本研究中，我们旨在从大叶丹参中分离和结构表征新化合物，并评估其对人早幼粒细胞白血病（HL-60）和宫颈癌（HeLa）细胞系的细胞毒活性。从丹参的根中分离到3个新的重排枞烷型二萜，grandfolins a - c（1-3）和一个新的枞烷型二萜，grandfolin D(4)，以及12个已知化合物（5-16）。结合广泛的1H和13C光谱，x射线晶体学和电子圆二色性光谱（ECD）确定了它们的结构。1-3的骨架结构重排，其中6/6/5环为二萜型二萜。还提出了重组骨架的生物合成途径。许多分离的化合物对HeLa或HL-60细胞株显示弱的细胞毒性。

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引用次数: 0

New abietane-type diterpenoids from roots of Euonymus hamiltonianus and their cytotoxicity in human cancer cell 哈密卫矛根新发现的二萜及其对人癌细胞的细胞毒性。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-03-01 DOI: 10.1007/s11418-025-01887-6

Jungmoo Huh, Eun Jin Park, Jae Hyun Lee, Chan-Woong Park, Tae-Jin Yang, Won Keun Oh, Young-Won Chin

Two new abietane-type diterpenoids, 6β-(3-furoyloxy)ferruginol (1) and 6-chloro-6,7-dehydroferruginol (2), were isolated from the roots of Euonymus hamiltonianus along with five known diterpenoids (3–7). Their structures were characterized using various spectroscopic analysis including HRMS, 1D and 2D NMR, and ECD analysis. All isolated compounds (1–7) were evaluated for their cytotoxic activity against human colon cancer cell line, HCT116, and it was found to exhibit moderate cytotoxic activity with IC₅₀ values ranging from 4.5 to 22.9 μM. Among the isolated compounds, montbretol (4) displayed the most cytotoxic activity (IC₅₀ = 4.50 ± 0.29 μM) against HCT116 human colon cancer cells than the other isolated compounds.

Graphical abstract

从 Euonymus hamiltonianus 的根中分离出了两种新的阿比坦类二萜，即 6β-（3-呋喃基氧基）阿魏酰醇（1）和 6-氯-6,7-脱氢阿魏酰醇（2），以及五种已知的二萜（3-7）。通过各种光谱分析，包括 HRMS、1D 和 2D NMR 以及 ECD 分析，对这些化合物的结构进行了表征。评估了所有分离化合物（1-7）对人结肠癌细胞系 HCT116 的细胞毒性活性，发现它们具有中等程度的细胞毒性活性，IC50 值在 4.5 到 22.9 μM 之间。在分离出的化合物中，与其他分离出的化合物相比，montbretol (4) 对 HCT116 人结肠癌细胞的细胞毒活性最高（IC50 = 4.50 ± 0.29 μM）。

引用次数: 0

Potential α-glucosidase inhibitors from cultures of Biscogniauxia capnodes SWUF15-40 fungus 双头菌SWUF15-40培养物中潜在的α-葡萄糖苷酶抑制剂。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-02-26 DOI: 10.1007/s11418-025-01876-9

Audomsak Churat, Praewpan Katrun, Chittima Laohpongspaisan, Wiyada Mongkolthanaruk, Chamaiporn Champasri, Pairot Moontragoon, Nuttika Suwannasai, Ek Sangvichien, Pakarapon Poonsukkho, Sirirath McCloskey

The search for a potent α-glucosidase inhibitor from the fungus Biscogniauxia capnodes SWUF15-40 yielded eighteen compounds. A comprehensive analysis from NMR and MS data revealed three new α-pyrones, biscogniapyrones A–C (1–3), two new isocoumarins (5 and 6), and thirteen known compounds. The configurations were assigned from calculated ¹³C NMR chemical shifts and ECD spectra, together with ¹H NMR analysis of Mosher esters. Several compounds exhibited effective inhibitory activity against α-glucosidase with IC₅₀ values in the range of 0.041–0.257 mM, which are lower than the positive control, acarbose (IC₅₀ 0.713 mM). The proposed non-competitive mode of inhibition was deduced from Lineweaver–Burk plots together with K_m and V_max values. In silico dockings of the strongest inhibitor, compound 3 were studied. Three out of the five determined allosteric sites of the enzyme model were favorable, with closed free binding energies of roughly − 4.00 kcal/mol. The binding interactions observed between 3 and amino acids in the pocket sites were hydrogen bonding and hydrophobic interactions. These findings, therefore, provide opportunities for drug development processes to be carried out.

Graphical abstract

从真菌Biscogniauxia capnodes SWUF15-40中寻找有效的α-葡萄糖苷酶抑制剂，共获得18个化合物。通过核磁共振和质谱的综合分析，发现了3个新的α-吡酮类化合物，biscogniapyrones A- c(1-3)， 2个新的异香豆素（5和6），以及13个已知化合物。根据计算的13C NMR化学位移和ECD光谱以及Mosher酯的1H NMR分析确定了构型。部分化合物对α-葡萄糖苷酶的IC50值在0.041 ~ 0.257 mM之间，均低于阳性对照阿卡波糖（IC50为0.713 mM）。提出的非竞争性抑制模式是由Lineweaver-Burk图以及Km和Vmax值推导出来的。对最强抑制剂化合物3的硅对接进行了研究。该酶模型的5个变构位点中有3个是有利的，其闭合自由结合能约为- 4.00 kcal/mol。在口袋位点上观察到3和氨基酸之间的结合相互作用是氢键和疏水相互作用。因此，这些发现为开展药物开发过程提供了机会。

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引用次数: 0

SIRT5: a potential target for discovering bioactive natural products SIRT5：发现生物活性天然产物的潜在靶标。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Journal of Natural Medicines

Pub Date : 2025-02-20 DOI: 10.1007/s11418-024-01871-6

Yuwei Xie, Nali Cai, Xiaohua Liu, Liangliang He, Yiming Ma, Changyu Yan, Juan Liang, Shu-Hua Ouyang, Ao Luo, Yingzhi He, Jun Lu, Dang Ao, Jia Liu, Zhonglv Ye, Bin Liu, Rong-Rong He, Wen Li

Silent information regulator 5 (SIRT5) is the fifth member of the sirtuin family, which is mainly expressed in mitochondrial matrix. SIRT5 plays a key role in metabolism and antioxidant responses, and is an important regulator for maintaining intracellular homeostasis. Given its involvement in multiple cellular processes, dysregulation of SIRT5 activity is associated with a variety of diseases. This review explores the structural characteristics of SIRT5 that influence its substrate specificity, highlights recent research advances, and summarizes its four key enzymatic activities along with their corresponding substrates in disease contexts. We also discuss the natural products that modulate SIRT5 activity and identify potential targets of SIRT5 through virtual docking, which may provide new therapeutic avenues. Although the mechanism of SIRT5 in diseases needs to be further elucidated and deglutathionylation activities are still at an early stage, targeting SIRT5 and its substrates holds significant promise for the development of novel therapeutics.

Graphical abstract

沉默信息调节因子5 （Silent information regulator 5, SIRT5）是sirtuin家族的第五个成员，主要表达于线粒体基质中。SIRT5在代谢和抗氧化反应中起关键作用，是维持细胞内稳态的重要调节因子。考虑到SIRT5参与多种细胞过程，SIRT5活性失调与多种疾病有关。本文探讨了影响SIRT5底物特异性的结构特征，重点介绍了最近的研究进展，并总结了SIRT5在疾病背景下的四种关键酶活性及其相应的底物。我们还讨论了调节SIRT5活性的天然产物，并通过虚拟对接确定了SIRT5的潜在靶点，这可能为治疗提供新的途径。虽然SIRT5在疾病中的作用机制有待进一步阐明，去谷胱甘肽化活性仍处于早期阶段，但靶向SIRT5及其底物对开发新的治疗方法具有重要的前景。

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