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Natural anti-neuroinflammatory inhibitors from Aglaia odorata 天然抗神经炎抑制剂,从香木莲。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2025.2492355
Xin-Yang Liu , Jing-Jing Zhang , Qian-Qian Yin , Yan-Ping Zhang , Chen Zhao , Ming-Xia Fang , Qing-Qi Meng , Yue Hou , Di Zhou , Ning Li
Eleven compounds were isolated from the n-butanol extract of Aglaia odorata Lour, including one undescribed lignan, curlignan-4-O-β-D-glucopyranoside (1), and ten known compounds (2–11). Their structures were characterized by comprehensive spectral analysis, nuclear magnetic resonance (1D and 2D NMR), mass spectrometry (MS), and electronic circular dichroism (ECD). The inhibitory effects of these compounds on nitric oxide (NO) production in lipopolysaccharide (LPS) stimulated BV-2 microglia were evaluated. The experimental results indicated that the anti-neuroinflammatory activities of compounds 1, 3, 4, 6, 7, 9 and 10 were significantly better than those of the positive control minocycline (IC50 = 41.34 ± 3.55 μM), with IC50 values ranging from 1.31 to 15.70 μM.
从香木莲正丁醇提取物中分离得到11个化合物,包括1个未描述的木脂素,curlignan-4-O-β-D-glucopyranoside(1)和10个已知化合物(2-11)。通过综合光谱分析、核磁共振(1D和2D NMR)、质谱(MS)和电子圆二色性(ECD)对其结构进行了表征。研究了这些化合物对脂多糖(LPS)刺激BV-2小胶质细胞一氧化氮(NO)产生的抑制作用。实验结果表明,化合物1、3、4、6、7、9、10的抗神经炎活性显著优于阳性对照米诺环素(IC50 = 41.34±3.55 μM), IC50值为1.31 ~ 15.70 μM。
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引用次数: 0
Exploring the mechanism of daphne-type diterpenes against gastric cancer cells 探索达芙妮类二萜对胃癌细胞的作用机制
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2311149
Yu-Jue Wang , Xin-Ye Wang , Zi-Nuo Yang , Xin-Yue Shang , Si-Hui Mi , Qingbo Liu , Guo-Dong Yao , Shao-Jiang Song
Gastric cancer is one of the common malignant tumors. It is reported that daphne-type diterpenes have inhibitory effects on gastric cancer cells, but the mechanism is still unknown. To explore the detailed mechanism of the anticancer effect of daphne-type diterpenes, we carried out an integrated network pharmacology prediction study and selected an effective component (yuanhuacine, YHC) for the following validation in silico and in vitro. The result showed that daphne-type diterpenes exerted an anti-tumor effect by targeting proto-oncogene tyrosine-protein kinase SRC as well as regulating the Ras/MAPK signaling pathway, which caused the apoptosis and mitochondrial damage in gastric cancer cells.
胃癌是常见的恶性肿瘤之一。据报道,达芙妮类二萜对胃癌细胞有抑制作用,但其机制尚不清楚。为了探索达芙妮型二萜抗癌作用的详细机制,我们开展了一项综合网络药理学预测研究,并选择了一种有效成分(元胡素,YHC)进行了后续的硅学和体外验证。结果表明,二萜通过靶向原癌基因酪氨酸蛋白激酶SRC和调控Ras/MAPK信号通路,引起胃癌细胞凋亡和线粒体损伤,从而发挥抗肿瘤作用。
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引用次数: 0
Two new Nb-oxide indole alkaloids with β-hematin inhibitory activity from the stems and leaves of Rauvolfia dichotoma 从 Rauvolfia dichotoma 的茎和叶中提取出两种具有 β-血金抑制活性的新 Nb-oxide 吲哚生物碱。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2302825
Jing-Ru Fang , Yu-Jie Zhang , Xiao Meng , Yi Chen , Xue Zhang , Ling-Juan Zhu , Xin-Sheng Yao
Rauvolfia dichotoma, a shrub of Apocynaceae, was collected from the Islands of SAO Tome and Principe and cultivated locally for medicinal purpose. Phytochemical investigation of 95% ethanol extract from the stems and leaves of R. dichotoma led to the isolation of two new Nb-oxide indole alkaloids, namely Nb-oxide-mitoridine (1) and Nb-oxide-raucaffricine (2), together with two known alkaloids (3–4) and eleven known lignans (5–15). Their chemical structures were elucidated by extensive NMR and HR-ESI-MS data analysis. All compounds (except 13) were tested for their β-hematin inhibitory activity. Compounds 2, 4, 14, and 15 showed certain inhibitory activity, indicating that they may have an antimalarial effect.
Rauvolfia dichotoma 是 Apocynaceae 的一种灌木,采集自圣多美和普林西比群岛,在当地种植用于药用。通过对 R. dichotoma 茎和叶 95% 的乙醇提取物进行植物化学研究,分离出两种新的 Nb-oxide 吲哚生物碱,即 Nb-oxide-mitoridine (1) 和 Nb-oxide-raucaffricine (2),以及两种已知生物碱 (3-4) 和 11 种已知木质素 (5-15)。通过大量的 NMR 和 HR-ESI-MS 数据分析,阐明了这些化合物的化学结构。对所有化合物(除 13 外)进行了 β-血蛋白抑制活性测试。化合物 2、4、14 和 15 显示出一定的抑制活性,表明它们可能具有抗疟作用。
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引用次数: 0
New aporphine alkaloids with antitumor activities from the roots of Thalictrum omeiense 从 Thalictrum omeiense 的根中提取的具有抗肿瘤活性的新卟吩生物碱。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2317826
Zhao-Jing Chen , Han-Gao Yang , Wen-Peng Zhu , Chun-Mei Xue , Hong-Mei Zhang , Yu-Ting Peng , Da-Hong Li , Hui-Ming Hua
Two new aporphine alkaloids, 6aR-2'-(3-oxobutenyl)-thaliadin (1) and N-methylthalisopynine (2), along with ten known analogs (312), were isolated from the roots of Thalictrum omeiense W. T. Wang et S. H. Wang. Their structures were determined by extensive spectroscopic and X-ray crystallographic analyses. Compounds 17 and 912 were tested for their antiproliferative effects in vitro against two human cancer cell lines (A549 and MCF-7). Among them, compounds 1, 3, and 7 exhibited moderate inhibitory activity against the tested cell lines with IC50 values ranging from 23.73 to 34.97 μM.
从 Thalictrum omeiense W. T. Wang et S. H. Wang 的根中分离出两种新的卟吩生物碱,6aR-2'-(3-氧代丁烯基)-thaliadin (1) 和 N-methylthalisopynine (2),以及十种已知的类似物 (3-12)。通过大量光谱和 X 射线晶体分析确定了它们的结构。体外测试了化合物 1-7 和 9-12 对两种人类癌细胞株(A549 和 MCF-7)的抗增殖作用。其中,化合物 1、3 和 7 对所测试的细胞株具有中等程度的抑制活性,IC50 值介于 23.73 到 34.97 μM 之间。
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引用次数: 0
Two pairs of bioactive cyclohexene alkaloid enantiomers from the roots of Piper nigrum 胡椒根中的两对具有生物活性的环己烯生物碱对映体
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2335279
Zhi-Yong Xu , Ning-Ning Du , Chang-Sheng La , Xiao-Xiao Huang , Shao-Jiang Song
Two pairs of cyclohexene amide alkaloid enantiomers were obtained from the root of Piper nigrum. Their plane structures were established by NMR and HRESIMS spectra. The absolute configurations of 1a/1b and 2a/2b were determined by the comparison between the experimental and calculated electronic circular dichroism (ECD) spectra. All identified compounds were tested for inhibitory effects on acetylcholinesterase (AChE) in vitro. Notably, compounds 1b and 2b showed strong inhibitory effects on AChE and the interaction between proteins and compounds was discussed by molecular docking studies.
从黑蒌根中获得了两对环己烯酰胺生物碱对映体。通过核磁共振和 HRESIMS 光谱确定了它们的平面结构。对映体 1 的绝对构型为...
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引用次数: 0
Target isolation of diverse sesquiterpenoid from the stems of Daphne genkwa based on molecular networking 基于分子网络从 Daphne genkwa 茎中定向分离出多种倍半萜类化合物。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2325033
Jia-Yi Li , Xin-Yi Wang , Mei-Juan Han , Ming Bai , Xiao-Xiao Huang
Guiding by LC-MS/MS analysis and the Global Natural Products Social (GNPS) Molecular Networking, three undescribed sesquiterpenoids, stedapgens A–C, and two known analogues were discovered in the barks of Daphne genkwa Sieb. et Zucc. The structures were determined by analysis of their spectroscopic data and quantum-chemical calculations. All the isolated novel compounds were tested for their acetylcholinesterase inhibitory activities with IC50 = 0.754 ± 0.059, 0.696 ± 0.026, and 0.337 ± 0.023 μg/ml. Among them, stedapgen A displayed promising inhibitory activities against AChE, and the binding sites were predicted by molecular docking.
在 LC-MS/MS 分析和全球天然产品社会(GNPS)分子网络的指导下,在 Daphne genkwa Sieb. et Zucc. 的树皮中发现了三种未曾描述过的倍半萜类化合物 Stedapgens A-C 和两种已知的类似物。通过分析其光谱数据和量子化学计算,确定了它们的结构。对所有分离出的新化合物进行了乙酰胆碱酯酶抑制活性测试,其 IC50 = 0.754 ± 0.059、0.696 ± 0.026 和 0.337 ± 0.023 μg/ml。其中,stedapgen A 对 AChE 具有良好的抑制活性,其结合位点可通过分子对接进行预测。
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引用次数: 0
A new cassane diterpenoid from the seed of Caesalpinia sappan 从 Caesalpinia sappan 种子中提取的一种新的决明二萜。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2360640
Yue-Lin Zhao , Yue Jin , Zi-Ying Han , Wen-Han Song , Hui-Lin Zhu , Jian Zhang , Qian Wang , Miao Wang , Xiao-Wen Jiang , Hui-Yuan Gao
In this study, a previously undescribed cassane diterpenoid, named caesalpinin JF (1), along with two known cassane diterpenoids caesanine C (2) and tomocinol B (3), was isolated from 95% EtOH extract of the seeds of Caesalpinia sappan Linn. Additionally, three known compounds including pulcherrin R (4), syringaresinol-4'-O-β-D-glucopyranoside (5) and kaempferol (6) were also identified. The structures of the isolated compounds were elucidated by comprehensive 1D and 2D NMR spectroscopic analyses. Additionally, electronic circular dichroism (ECD) calculation was used to identify the absolute structure of compound 1. Among the isolated compounds, compound 1 displayed a potent anti-neuroinflammation with an IC50 value of 9.87 ± 1.71 μM.
在这项研究中,从红豆杉种子 95% 的 EtOH 提取物中分离出了一种之前未曾描述过的决明子二萜,命名为 Caesalpinin JF (1),以及两种已知的决明子二萜 caesanine C (2) 和 tomocinol B (3)。此外,还鉴定出三种已知化合物,包括 Pulcherrin R (4)、Syringaresinol-4'-O-β-D-吡喃葡萄糖苷 (5) 和山奈酚 (6)。通过全面的一维和二维核磁共振光谱分析,阐明了这些分离化合物的结构。在分离出的化合物中,化合物 1 具有很强的抗神经发炎作用,其 IC50 值为 9.87 ± 1.71 μM。
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引用次数: 0
Synthesis of sinomenine derivatives with potential anti-leukemia activity 具有潜在抗白血病活性的西乃咪宁衍生物的合成
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2327524
Xiang Gao , Hao-Nan Li , Peng-Ju Liu , Xiao-Kang Long , Xue-Hai Guo , Hui-Ming Hua , Da-Hong Li
In recent years, with sinomenine hydrochloride as the main ingredient, Qingfengteng had been formulated as various dosage forms for clinical treatment. Subsequent findings confirmed a variety of biological roles for sinomenine. Here, 15 H2S-donating sinomenine derivatives were synthesized. Target hybrids a11 displayed substantial cytotoxic effects on cancer cell lines, particularly against K562 cells, with an IC50 value of 1.36 μM. In-depth studies demonstrated that a11 arrested cell cycle at G1 phase, induced apoptosis via both morphological changes in nucleus and membrane potential collapse in mitochondria. These results indicated a11 exerted an antiproliferative effect through apoptosis induction via mitochondrial pathway.
近年来,以盐酸西诺明为主要成分的青风藤被配制成各种剂型用于临床治疗。随后的研究结果证实,清风藤具有多种生物活性。
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引用次数: 0
Two new cassane diterpenoids from the seed kernels of Caesalpinia sinensis 从中华桫椤种仁中提取的两种新的决明二萜。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-02 DOI: 10.1080/10286020.2024.2317841
Lian Lian , Yue-Lin Zhao , Tian-Jian Zhang , Miao Wang , Hui-Yuan Gao
Two new cassane diterpenoids, sucupiranin MN (1) and sucupiranin ML (2), together with two known compounds sucutinirane C (3) and deacetylsucutinirane C (4) were isolated from the seed kernels of Caesalpinia sinensis. Their structures were elucidated by means of analysis of comprehensive spectroscopic data, especially HRESIMS and 1D/2D NMR spectroscopy. Compounds 1–4 are typical furan-type cassane derivatives with an aromatized C ring. Biological evaluation revealed that compounds 1–4 at the concentration of 10 μM could inhibit the overproduction of NO in LPS-stimulated RAW 264.7 macrophages.
从中华皂荚的种仁中分离出了两种新的皂荚烷二萜类化合物:琥珀烷宁 MN (1) 和琥珀烷宁 ML (2),以及两种已知化合物琥珀烷宁 C (3) 和脱乙酰基琥珀烷宁 C (4)。通过分析全面的光谱数据,特别是 HRESIMS 和 1D/2D NMR 光谱,阐明了它们的结构。化合物 1-4 是具有芳香化 C 环的典型呋喃型卡桑烷衍生物。生物学评价显示,浓度为 10 μM 的化合物 1-4 可抑制 LPS 刺激的 RAW 264.7 巨噬细胞中 NO 的过度产生。
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引用次数: 0
Special issue commemorating the 40th anniversary of the College of Traditional Chinese Medicine, Shenyang Pharmaceutical University. 纪念沈阳药科大学中医药学院建校四十周年特刊。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-01 Epub Date: 2025-11-17 DOI: 10.1080/10286020.2025.2588076
Shao-Jiang Song
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引用次数: 0
期刊
Journal of Asian Natural Products Research
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