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First total synthesis and antimicrobial evaluation of xanthone V1. 山酮V1的首次全合成及抗菌评价。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-03 DOI: 10.1080/10286020.2025.2581720
Fei Tan, Meng-Qi Wang, He-Fei Shi, Chun-Ran Zhang, De-Xiu Cui, Hong-Bo Dong

Antibiotic resistance demands new agents. We disclosed the first total synthesis of the natural xanthone V1 (1), which featured a regioselective Claisen cyclization and a Claisen/Cope rearrangement that installed the pyran ring and isopentenyl unit. The synthetic compound showed moderate antibacterial potency (MICs 16-64 μg/ml) across multiple strains and synergized with ciprofloxacin against MRSA. It exhibited low cytotoxicity toward mammalian cells and minimal hemolysis, thereby supporting xanthone V1 as a promising lead for anti-MRSA therapy.

抗生素耐药性需要新的药物。我们首次披露了天然山酮V1(1)的全合成,它具有区域选择性的Claisen环化和clisen /Cope重排,安装了吡喃环和异戊烯基单元。该化合物对多种菌株的抑菌效果中等(mic值为16 ~ 64 μg/ml),可与环丙沙星协同抑制MRSA。它对哺乳动物细胞具有较低的细胞毒性和最小的溶血作用,因此支持山酮V1作为抗mrsa治疗的有希望的先导物。
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引用次数: 0
A new verrucosane diterpenoid from the Vietnamese liverwort Plagiochila bantamensis. 越南板蓝藻中一个新的疣胞烷二萜。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-03 DOI: 10.1080/10286020.2025.2577286
Le Thi-Kim-Dung, Nguyen Thi-Nhu-Quynh, Le Thanh-Nguyen, Tram Nguyen-Khanh-Trinh, Nguyen Thi-Phuong, Thi-Hoai-Thu Nguyen, Ngoc-Hong Nguyen, Jirapast Sichaem, Thuc-Huy Duong

A new verrucosane-type diterpenoid, bantamenside (1), along with six known compounds (2-7), was isolated from the Vietnamese liverwort Plagiochila bantamensis. The structure of the new compound was determined using comprehensive spectroscopic methods, including 1D and 2D NMR techniques as well as high-resolution mass spectrometry. Furthermore, all isolated compounds were evaluated for their ability to inhibit nitric oxide (NO) production. Compounds 1-3 and 6-7 demonstrated notable NO inhibitory activity, with IC50 values ranging from 12.85 to 51.37 µM, outperforming or comparable to that of the positive control L-NMMA (IC50 41.30 ± 6.60 µM).

从越南苔类植物Plagiochila bantamensis中分离到一种新的疣胞烷型二萜类化合物bantamenside(1)和6个已知化合物(2-7)。新化合物的结构是通过综合光谱方法确定的,包括一维和二维核磁共振技术以及高分辨率质谱。此外,所有分离的化合物都对其抑制一氧化氮(NO)产生的能力进行了评估。化合物1-3和6-7具有显著的NO抑制活性,IC50值为12.85 ~ 51.37µM,优于或与阳性对照L-NMMA (IC50值为41.30±6.60µM)相当。
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引用次数: 0
Hongjingtian alleviates arsenic-induced hepatocyte injury by inhibiting oxidative stress and endoplasmic reticulum stress 红景天通过抑制氧化应激和内质网应激减轻砷诱导的肝细胞损伤。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2481290
Jiang-Tao Cao , Hai-Wen Li , Jia-Qi Chen , Hai-Long Lv , Yu-Feng Jiang
This study explored Hongjingtian’s (HJT) protective effects against arsenic-induced hepatotoxicity. NaAsO2 (8 μM, 24 h)-damaged hepatocytes treated with HJT (50/100 mg/L) showed restored cell viability via CCK-8/LDH assays. HJT reduced arsenic-induced ROS, improved mitochondrial membrane potential, elevated SOD/CAT activity, lowered MDA, and suppressed apoptosis by downregulating Caspase-3/Bax while upregulating Bcl-2. Additionally, HJT alleviated endoplasmic reticulum stress (ERS). Mechanistically, HJT attenuated arsenic-induced hepatocyte apoptosis by mitigating oxidative stress and ERS via ROS reduction.
本研究探讨红景天(HJT)对砷致肝毒性的保护作用。HJT (50/100 mg/L)处理NaAsO2 (8 μM, 24 h)损伤的肝细胞,CCK-8/LDH检测显示细胞活力恢复。HJT通过下调Caspase-3/Bax和上调Bcl-2,降低砷诱导的ROS,改善线粒体膜电位,提高SOD/CAT活性,降低MDA,抑制细胞凋亡。此外,HJT还能减轻内质网应激(ERS)。机制上,HJT通过减少ROS减少氧化应激和ERS来减轻砷诱导的肝细胞凋亡。
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引用次数: 0
Chemical constituents from Calophyllum polyanthum and their biological activity Calophyllum polyanthum的化学成分及其生物活性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2481274
Yin-Xia Yang , Li-Hua Gong , Fu-Hua Peng , Jian-Guo Hu , Tao Jiang , Bin Li , Yue Yang , Jing-Ying Peng , Xue-Mei Gao
Phytochemical investigation of Calophyllum polyanthum led to the isolation of six xanthones, six chromanone derivatives, one coumarin, one glycoside and one flavonoid, including two new xanthones named caledonixanthone M (1), caledonixanthone N (2) and thirteen known compounds (3–15). Among them, the structures of 1 and 2 were elucidated by analysis of spectroscopic data. Some known compounds showed potent α-glucosidase inhibitory and cytotoxic activity. Especially, compound 14 showed moderate inhibitory activities on α-glucosidase with IC50 value of 79.41 ± 0.22 µM, and compound 5 displayed anticancer effect on A549 non-small cell lung cancer cells.
通过对Calophyllum polyanthum的植物化学研究,分离得到6个口山酮、6个chromanone衍生物、1个香豆素、1个糖苷和1个黄酮类化合物,包括2个新的口山酮,分别命名为caledonixanthone M(1)、caledonixanthone N(2)和13个已知化合物(3-15)。其中,1号和2号的结构通过光谱数据进行了解析。一些已知的化合物显示出有效的α-葡萄糖苷酶抑制和细胞毒活性。其中,化合物14对α-葡萄糖苷酶具有中等抑制作用,IC50值为79.41±0.22µM;化合物5对A549非小细胞肺癌细胞具有抗肿瘤作用。
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引用次数: 0
Three new antinociceptive diterpenoids from the flowers of Rhododendron molle 从杜鹃花中分离出三个新的抗伤性二萜。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2527875
Yan Wang , Hui-Min Yan , Jin-Cai Lu , Shi-Shan Yu
Three new grayanane-type diterpenoids (1–3), together with eight known compounds, were isolated from the flowers of Rhododendron molle G. Don. The structures of new compounds were fully determined based on spectroscopic analysis, including HRESIMS, 1D, and 2D NMR data. The absolute configuration of the new compounds was confirmed by single-crystal X-ray diffraction. The analgesic activities of compounds 1–7 and 10–11 were evaluated by the acetic acid-induced writhing method in mice. Compounds 3 and 6 had significant analgesic effects at a low dose of 0.2 mg/kg, and the writhe inhibition rates were 66.3% and 82.9%, respectively. Compounds 3–4 and 10–11 also showed significant analgesic effects at a dose of 1 mg/kg (writhe inhibition rate was 66.8%–91.7%). Compounds 5, 7, and 10–11 showed significant analgesic effects at a dose of 5 mg/kg (writhe inhibition rate was 68.4%–83.4%).
从杜鹃(Rhododendron molle G. Don)花中分离到了3个新的灰烷型二萜类化合物(1-3)和8个已知化合物。新化合物的结构完全确定基于光谱分析,包括hremsims, 1D和2D NMR数据。单晶x射线衍射证实了新化合物的绝对构型。采用醋酸扭体法对化合物1-7、10-11的镇痛作用进行了评价。化合物3和6在0.2 mg/kg低剂量下具有明显的镇痛作用,扭曲抑制率分别为66.3%和82.9%。化合物3-4和10-11在1 mg/kg剂量下也有明显的镇痛作用(扭曲抑制率为66.8% ~ 91.7%)。化合物5、7和10-11在5 mg/kg剂量下表现出明显的镇痛作用(扭曲抑制率为68.4% ~ 83.4%)。
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引用次数: 0
Three new shikimate-conjugated meroterpenoids from Alternaria alternata isolated from an entomopathogenic fungus Apis mellifera 从昆虫病原真菌蜜蜂中分离得到的三个新的莽草碱共轭角萜类化合物。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2521542
Ya-Nan Tian , Yu-Wei Niu , Ke-Liang Chen , Yang Liu , Chen-Yu Yang , Xing-Bao Jia , Yang Yang , Yun-Bao Liu
Three new shikimate-conjugated meroterpenes, tricycloalternarenes Z1–Z3 (13), were isolated from Alternaria alternate, an endophytic fungus residing in Apis mellifera. The structures of new compounds were characterized by analyses of their NMR and HRESIMS data. The absolute configurations were assigned through electronic circular dichroism (ECD) calculations and CD spectra. Bioassay results showed that tricycloalternarene Z1 (1) exhibited moderate anti-inflammatory activity against the LPS-induced production of NO in RAW 264.7 cells, with an IC50 value of 0.93 µM.
从亚洲蜜蜂内生真菌Alternaria alternarenes中分离到3个新的牛草酸共轭二萜类化合物tricycloalternarenes Z1-Z3(1-3)。新化合物的结构通过NMR和hresms数据进行了表征。通过电子圆二色性(ECD)计算和CD光谱确定了绝对构型。生物实验结果显示,三环交替芳烃Z1(1)对lps诱导的RAW 264.7细胞NO生成具有中等抗炎活性,IC50值为0.93µM。
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引用次数: 0
Discovery of immunosuppressive secondary metabolites from Hypericum patulum 金丝桃免疫抑制次生代谢物的发现。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2481285
Fei Song , Jie Li , Bin-Bin Song , Zheng-Yi Shi , Zhang-Rong Hou , Ye-Ting Zhang , Yu-Lin Duan , Jian-Ping Wang , Chang-Xing Qi , Yong-Hui Zhang
The chemical study of Hypericum patulum provided a new degraded lupane-type triterpenoid, patutriter A (1), and seven known compounds (28). Their structures were identified by spectroscopic techniques and single crystal diffraction experiment. Structurally, patutriter A (1) was a new lupane with a 28-nor-skeleton. More importantly, compounds 35 exhibited moderate immunosuppressive effects that inhibit the anti-CD3/anti-CD28 monoclonal antibodies (mAbs) and concanavalin A (ConA) stimulated murine splenocytes proliferation, with IC50 values from (15.25 ± 1.78) μM to (22.58 ± 3.47) μM, disclosing that those compounds might serve as potential lead compounds in the development of new immunosuppressants.
对金丝桃的化学研究提供了一种新的降解的羽扇烷型三萜,patutriter a(1)和7个已知化合物(2-8)。通过光谱技术和单晶衍射实验对其结构进行了鉴定。在结构上,patutriter A(1)是一个具有28-no -skeleton的新lupane。更重要的是,化合物3-5表现出适度的免疫抑制作用,抑制抗cd3 /抗cd28单克隆抗体(mab)和ConA刺激小鼠脾细胞增殖,IC50值在(15.25±1.78)μM至(22.58±3.47)μM之间,表明这些化合物可能是开发新型免疫抑制剂的潜在先导化合物。
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引用次数: 0
Expanding the role of alpha lipoic acid for psychiatric and neurological health 扩大α硫辛酸对精神和神经健康的作用。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2509765
Ishu Garg , Harish Kumar , Raj Kumari , Anupama Singh , Ravi Maurya , Rashi Pandey , Shruti Bhatt
With the rise in health and neurological concerns around the globe, nutraceuticals are surpassing the harms of drug treatment. Alpha-lipoic acid, an organosulfur naturally abundant biomolecule that has potent protective and therapeutic effects in psychiatric and neurological disorders. Studies targeting alpha-lipoic acid in the brain have concluded that it modulates oxidative stress, neuronal aging, apoptosis, mitochondrial dysfunction, neuro-inflammation, cellular signaling, neurotransmission, and receptor functioning. Various clinical studies have been conducted, yielding satisfactory results indicating alpha-lipoic acid as a therapeutic agent for neurodegenerative and psychiatric disorders. However, further studies are still required to use alpha-lipoic acid as a monotherapeutic agent and to design a dosage regimen. The article aims to demonstrate alpha-lipoic acid as a potent biomolecule for curing and preventing psychiatric and neural disorders.
随着全球范围内对健康和神经系统的关注的增加,营养保健品正在超越药物治疗的危害。硫辛酸是一种天然丰富的有机硫生物分子,对精神和神经疾病具有有效的保护和治疗作用。针对大脑中α -硫辛酸的研究已经得出结论,它可以调节氧化应激、神经元衰老、细胞凋亡、线粒体功能障碍、神经炎症、细胞信号传导、神经传递和受体功能。已经进行了各种临床研究,取得了令人满意的结果,表明α -硫辛酸作为神经退行性疾病和精神疾病的治疗剂。然而,将α -硫辛酸作为单一治疗药物并设计给药方案仍需进一步研究。本文旨在证明α -硫辛酸作为一种有效的生物分子治疗和预防精神和神经疾病。
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引用次数: 0
Three new compounds from the roots of Rubia cordifolia 从芦花根中提取的三个新化合物。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2568630
Wan-Qi Zhang , Xin-Yue Li , Ming-Hui Sun , Jie Zhou , Guo-Ru Shi , De-Quan Yu , Yan-Fei Liu
Three new compounds (13), including two cyclopentanoid monoterpenes rubicoside A (1) and rubicocin A (2), and one naphthohydroquinone glycoside rubinaphthin E (3), together with six known analogues (49), were isolated from the roots of Rubia cordifolia. The structures of compounds 13 were established by chemical methods and spectroscopic analysis. Compounds 19 were tested for their cytotoxicity and screened for stable transfection of recombinant dopamine receptors in HEK293 cell lines.
从芦花根中分离得到3个新化合物(1-3),包括2个环戊类单萜rubicoside A(1)和rubicocin A(2), 1个萘对苯二酚糖苷rubbinaphthin E(3)和6个已知的类似物(4-9)。通过化学方法和光谱分析确定了化合物1 ~ 3的结构。化合物1-9在HEK293细胞系中进行了细胞毒性测试和筛选,以稳定转染重组多巴胺受体。
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引用次数: 0
Functional and biological characterization of Lactobacillus plantarum with isatin for use as probiotics for therapeutic options 植物乳杆菌与isatin作为益生菌治疗选择的功能和生物学特性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-11-02 DOI: 10.1080/10286020.2025.2475469
Ramya Ravindhiran , Mahalakshmi Subramanian , Madhumitha Rajalingam , Madhumitha Gunasekaran , Karthiga Sivarajan , Kumarappan Chidambaram , Kavitha Dhandapani
In our study, the functional and biological properties of the developed probiotic formulations containing Lactobacillus plantarum and isatin (Couroupita guianensis) have been evaluated. The developed probiotic formulations have demonstrated remarkable antioxidant, antimicrobial, and cholesterol-lowering properties (67.3 ± 0.57%). In addition, they exhibit high survivability in simulated oral fluid (98.8%). Furthermore, extracellular enzyme production iterates other health attributes of probiotic formulations to the human system by improving the utilization of nutrients in the intestine. In sum, the developed probiotic formulations have unveiled probiotic functions and safer applications, which could pave the way to develop functional foods or lead compounds for drug discovery.
本研究对已开发的植物乳杆菌和桂皮素(cououpita guianensis)益生菌制剂的功能和生物学特性进行了评价。所开发的益生菌制剂具有显著的抗氧化、抗菌和降胆固醇性能(67.3±0.57%)。此外,它们在模拟口腔液中表现出较高的存活率(98.8%)。此外,胞外酶生产通过提高肠道营养物质的利用率,使益生菌配方的其他健康属性迭代到人体系统。总之,开发的益生菌配方揭示了益生菌的功能和更安全的应用,为开发功能食品或药物开发的先导化合物铺平了道路。
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引用次数: 0
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Journal of Asian Natural Products Research
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