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Synthesis, anti-oomycete and anti-fungal activities of novel paeonol ester derivatives containing a schiff base 含席夫碱的新型丹皮酚酯衍生物的合成及其抗卵霉菌和抗真菌活性。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2024.2426205
Xiaofang Zhang , Xiaolong Guo , Wanying Yin , Ruiguang Wang , Yuee Tian , Huilu Sun , Shaobin Xu , Shaoyan Shuang , Xiaobo Huang , Genqiang Chen , Zhiping Che
To discover biorational natural product-based pesticides, a series of paeonol ester derivatives containing a Schiff base (6a-j, 7i,j, 8i,j, and 9i,j) were prepared, and their structures were well characterised by 1H NMR and HRMS. Furthermore, bioactivities of these compounds as anti-oomycete and anti-fungal agents against two serious agricultural diseases, Phytophthora capsici and Fusarium graminearum we assessed. Amongst evaluated compounds, 1) Compounds 6a and 6e displayed good anti-oomycete against P. capsici, with EC50 values of 116.50 and 88.86 mg/L, respectively. 2) Compounds 6e and 7i exhibited prominent anti-fungal against F. graminearum, with EC50 values of 66.73 and 29.33 mg/L, respectively. 3) This study suggested that the introduction of nitro at the C5 position of paeonol could improve its bioactivity against P. capsici and F. graminearum. The results of this study pave the way for further design and development of paeonol derivatives as plant anti-oomycetes and anti-fungal agents in crop protection.
为了发现生物天然产物型农药,制备了一系列含有希夫碱的丹皮酚酯衍生物(6a-j, 7i,j, 8i,j和9i,j),并通过1H NMR和HRMS对其结构进行了表征。此外,我们还评价了这些化合物作为抗卵霉菌剂和抗真菌剂对辣椒疫霉和谷物镰刀菌两种严重农业病害的生物活性。1)化合物6a和6e对辣椒辣椒粉有较好的抑制作用,EC50值分别为116.50和88.86 mg/L。2)化合物6e和7i对小麦赤霉病菌的抑菌效果较好,EC50值分别为66.73和29.33 mg/L。3)本研究表明,在丹皮酚的C5位点引入硝基可以提高其抗辣椒疫病毒和禾谷镰刀菌的活性。本研究结果为丹皮酚衍生物作为植物抗卵菌剂和抗真菌剂在作物保护中的进一步设计和开发奠定了基础。
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引用次数: 0
Curculigosides J–K and curcorchidihydrobenzofuran A, a dihydrobenzofuran with anti-proliferative properties from Curculigo orchioides 莪术苷 J-K 和莪术二氢苯并呋喃 A,一种来自莪术兰的具有抗增殖特性的二氢苯并呋喃。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2024.2426064
Phornnapa Saentao , Florian T. Schevenels , Jantana Yahuafai , Anupong Joompang , Thanapat Suebrasri , Sophon Boonlue , Sarawut Tontapha , Ratsami Lekphrom
Phytochemical investigation of the rhizomes and the leaves of Curculigo orchioides led to the isolation of fourteen compounds. They consist of one undescribed dihydrobenzofuran, curcorchidihydrobenzofuran A (1), two undescribed benzyl benzoate glycosides, curculigoside J (2) and K (3), and eleven known compounds (414). The structures of the isolated compounds were elucidated by thorough analysis of spectroscopic (IR, NMR and ECD) and spectrometric (MS) data. Compound 1 displayed significant anti-proliferative activities against cervical cancer cells (HelaS3, IC50 = 3.6 µM) and breast cancer cells (MCF-7, IC50 = 13.9 µM) while showing moderate activities against lung cancer cells (A549, IC50 = 29.8 µM). Importantly, it was non-toxic to Vero cells. Compound 1 also inhibited the tyrosinase enzyme in a moderate manner (IC50 = 120.8 µM). Eventually, its permethylated synthetic analog 1a showed a significant suppression of lipopolysaccharide (LPS)-induced NO production in murine macrophage RAW 264.7 (IC50 = 23.4 µM).
通过对 Curculigo orchioides 根茎和叶片进行植物化学研究,分离出了 14 种化合物。这些化合物包括一种未曾描述过的二氢苯并呋喃--莪术二氢苯并呋喃 A (1)、两种未曾描述过的苯甲酸苄酯苷--莪术苷 J (2) 和 K (3),以及 11 种已知化合物 (4-14)。通过对光谱(红外光谱、核磁共振和电离辐射)和质谱(MS)数据的全面分析,阐明了分离出的化合物的结构。化合物 1 对宫颈癌细胞(HelaS3,IC50 = 3.6 µM)和乳腺癌细胞(MCF-7,IC50 = 13.9 µM)具有明显的抗增殖活性,而对肺癌细胞(A549,IC50 = 29.8 µM)则表现出中等活性。重要的是,它对 Vero 细胞无毒。化合物 1 对酪氨酸酶也有一定的抑制作用(IC50 = 120.8 µM)。最终,它的过甲基化合成类似物 1a 显示出对小鼠巨噬细胞 RAW 264.7 中脂多糖(LPS)诱导的氮氧化物生成有显著抑制作用(IC50 = 23.4 µM)。
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引用次数: 0
Crystal structure and the degradation products of Tenvermectin B 天维菌素 B 的晶体结构和降解产物。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2024.2429110
Zhen-Yu Wang , Chun-Hui Wu , Xiao-Han Ren , Wei Zhang , Shao-Yong Zhang , Huan Qi , Jun Huang , Ji-Dong Wang , Hui Zhang
The purpose of this work was to investigate the crystal structure and degradant products (DPs) of tenvermectin B (TVM B). A suitable crystal of TVM B was obtained from a solvent system (MeOH:formamide:H2O = 2:5:2) and its absolute configuration was unambiguously established by single-crystal X-ray diffraction analysis. Meanwhile, a formamide-assisted crystallisation method for the purification of TVM B was developed. During the stress degradation studies of TVM B, four DPs (DPs 1-4) were prepared and characterised by MS and NMR. Among them, DP 2 and DP 3 have not been reported previously. In addition, the nematocidal activity of these DPs were evaluated.
这项工作的目的是研究十维菌素B(TVM B)的晶体结构和降解产物(DPs)。在溶剂体系(MeOH:甲酰胺:H2O=2:5:2)中获得了合适的 TVM B 晶体,并通过单晶 X 射线衍射分析明确了其绝对构型。同时,还开发了一种甲酰胺辅助结晶方法来纯化 TVM B。在 TVM B 的应力降解研究中,制备了四种 DPs(DPs 1-4),并通过 MS 和 NMR 对其进行了表征。其中,DP 2 和 DP 3 以前从未报道过。此外,还对这些 DPs 的杀线虫活性进行了评估。
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引用次数: 0
Novel curcumin derivatives as potential anticancer agents: design, synthesis and biological evaluation 新型姜黄素衍生物的设计、合成及生物学评价。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2024.2429112
Wenqing Liu , Sha Yang , Yongchun Pan , Bingliang Wei , Mingsong Liu , Huajie Zhu , Zhidong Xu
Curcumin, originally isolated as natural product from the rhizome of Curcuma longa L., is widely known for its anticancer properties. However, the clinical application of curcumin is still limited due to its poor absorption and rapid metabolism. In this study, structural modification of curcumin by introducing active small organic acids into its pyrazole ring intermediate, was employed to yield five curcumin derivatives 5a-5e. All the target compounds were characterised by 1H NMR,13C NMR and ESI-MS. Biological evaluation through the CCK-8 method indicated that nearly all these derivatives displayed higher proliferation inhibitory effect on A549 cells than that of curcumin. Among them, 5d bearing biotin moiety exhibited even stronger cytotoxicity action (2.25 μmol/L) than the positive control drug Doxorubicin (3.99 μmol/L) and therefore became the most promising lead compound for further investigation. Our findings provided a potential approach for the structural optimisation of curcumin derivatization in cancer treatment.
姜黄素最初是从姜黄根中分离出来的天然产物,因其抗癌特性而广为人知。但由于姜黄素吸收差、代谢快,其临床应用仍受到限制。本研究通过在吡唑环中间体中引入活性小有机酸对姜黄素进行结构修饰,得到5个姜黄素衍生物5a-5e。所有目标化合物均通过1H NMR、13C NMR和ESI-MS进行了表征。CCK-8法生物学评价表明,这些衍生物对A549细胞的增殖抑制作用几乎都高于姜黄素。其中,含5d生物素片段比阳性对照药物阿霉素(3.99 μmol/L)表现出更强的细胞毒作用(2.25 μmol/L),是最有希望进一步研究的先导化合物。我们的发现为姜黄素衍生化在癌症治疗中的结构优化提供了一种潜在的方法。
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引用次数: 0
First report on the chemical composition of volatile compounds in the essential oils and aromas of Senega adenophora, Senega appressa, and Senega longicaulis (Polygalaceae) 本文首次报道了三种植物(蓼科植物)挥发油和香气中挥发性化合物的化学成分。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2025.2480669
Layse Kristine Corrêa Lopes , Eloisa Helena de Aguiar Andrade , Mozaniel Santana de Oliveira , Diego Demarco , José Floriano Barêa Pastore , Ana Cristina Andrade de Aguiar Dias
This study presents a comprehensive chemical analysis of the essential oil isolated from Senega longicaulis, and aroma analysis of Senega adenophora and Senega appressa, employing both fresh and dried samples. Notable differences were observed between the fresh and dried samples of essential oil from S. longicaulis. In the fresh sample, the predominant compounds were (E,E)-geranyl linalool (33.21%) and dendrolasin (19.64%), whereas in the dried sample, (E,E)-geranyl linalool increased to 39.19% and dendrolasin to 18.83%. The oxygenated sesquiterpenes were found to be more abundant in the dried sample (81.52%) than in the fresh sample (69.96%). In the case of S. adenophora and S. appressa, the aroma analysis indicated that β-elemene (49.05%) and methyl salicylate (31.13%), respectively, were the primary compounds present in the fresh samples. These findings illustrate how the drying process has the effect of intensifying certain chemical components in the samples of S. longicaulis.
本研究采用新鲜样品和干燥样品,对长尾草精油的化学成分进行了综合分析,并对腺瘤草和小叶草进行了香气分析。鲜、干两种样品的精油含量差异显著。在新鲜样品中,主要化合物为(E,E)-香叶基芳樟醇(33.21%)和松木松素(19.64%),而在干燥样品中,(E,E)-香叶基芳樟醇增加到39.19%,松木松素增加到18.83%。氧化倍半萜在干燥样品中的含量(81.52%)高于新鲜样品(69.96%)。香气分析结果表明,新鲜样品中主要成分为β-榄香烯(49.05%)和水杨酸甲酯(31.13%)。这些发现说明了干燥过程是如何增强龙葵样品中某些化学成分的。
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引用次数: 0
Triterpenoid saponins from the fruit pulp of Tetrapleura tetraptera (Fabaceae) 从四叶草(豆科植物)果肉中提取的三萜类皂甙。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2024.2426072
G. Fru Chi , Serab Khan , Jenifer R. N. Kuete , Valaire Y. Matieta , Japheth. O. Ombito , Alfred. N. Tamfu , Junior F. Megaptche , Melvis A. Chongong , Taye B. Demissie , Victor Kuete , Farzana Shaheen
Tetrapleura tetraptera fruit, used as spice in West Africa was studied chemically; five previously undescribed triterpenoid saponins 15 and four known compounds 69 were isolated from the n-Butanol fraction. The chemical structures of all nine isolates were determined by comprehensive analysis of HRMS, 1D & 2D NMR experiments and by comparison with data in the literature. All nine compounds were evaluated for antibacterial activity by the broth microdilution through the rapid p-iodonitrotetrazolium chloride (INT) colorimetric technique. The results showed that only compounds 5 (MIC = 64 µg/mL against P. aeruginosa and P. stuartii) and 8 (MIC = 64 µg/mL against E. coli) exhibited moderate antibacterial activity. The rest of the compounds displayed weak antibacterial activity against the tested organisms. Molecular docking studies was used to comprehend antibacterial activities.
研究人员对西非用作香料的 Tetrapleura tetraptera 果实进行了化学研究;从正丁醇馏分中分离出了五种以前未曾描述过的三萜类皂苷 1-5 和四种已知化合物 6-9。通过对 HRMS、1D 和 2D NMR 实验进行综合分析,并与文献数据进行比较,确定了所有九种分离物的化学结构。通过肉汤微量稀释法和快速对碘硝基氯化四氮唑(INT)比色法评估了所有九种化合物的抗菌活性。结果表明,只有化合物 5(对铜绿假单胞菌和沙门氏菌的 MIC = 64 µg/mL)和化合物 8(对大肠杆菌的 MIC = 64 µg/mL)具有中等抗菌活性。其余化合物对受试生物的抗菌活性较弱。分子对接研究用于理解抗菌活性。
{"title":"Triterpenoid saponins from the fruit pulp of Tetrapleura tetraptera (Fabaceae)","authors":"G. Fru Chi ,&nbsp;Serab Khan ,&nbsp;Jenifer R. N. Kuete ,&nbsp;Valaire Y. Matieta ,&nbsp;Japheth. O. Ombito ,&nbsp;Alfred. N. Tamfu ,&nbsp;Junior F. Megaptche ,&nbsp;Melvis A. Chongong ,&nbsp;Taye B. Demissie ,&nbsp;Victor Kuete ,&nbsp;Farzana Shaheen","doi":"10.1080/14786419.2024.2426072","DOIUrl":"10.1080/14786419.2024.2426072","url":null,"abstract":"<div><div><em>Tetrapleura tetraptera</em> fruit, used as spice in West Africa was studied chemically; five previously undescribed triterpenoid saponins <strong>1</strong>–<strong>5</strong> and four known compounds <strong>6</strong>–<strong>9</strong> were isolated from the <em>n</em>-Butanol fraction. The chemical structures of all nine isolates were determined by comprehensive analysis of HRMS, 1D &amp; 2D NMR experiments and by comparison with data in the literature. All nine compounds were evaluated for antibacterial activity by the broth microdilution through the rapid <em>p</em>-iodonitrotetrazolium chloride (INT) colorimetric technique. The results showed that only compounds <strong>5</strong> (MIC = 64 µg/mL against <em>P. aeruginosa</em> and <em>P. stuartii</em>) and <strong>8</strong> (MIC = 64 µg/mL against <em>E. coli</em>) exhibited moderate antibacterial activity. The rest of the compounds displayed weak antibacterial activity against the tested organisms. Molecular docking studies was used to comprehend antibacterial activities.</div></div>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":"40 3","pages":"Pages 826-838"},"PeriodicalIF":1.6,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142623730","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
In vitro, in silico and crystallographic-based identification of serine protease inhibitors 基于体外、硅学和晶体学鉴定丝氨酸蛋白酶抑制剂。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2024.2425793
Zeeshan Akbar , Malik Shoaib Ahmad
Serine proteases are involved in various ailments, including pancreatitis, and colon cancer. Based on substrate recognition serine proteases are classified into different groups. Trypsin and trypsin-like serine proteases are among most studied group of serine proteases. Trypsin is among the chief hydrolysing enzyme involved in the pathogenesis of pancreatitis. Its inhibition can help to manage the disease. Herein, we investigated the trypsin inhibitory effect of some arginine-based small molecules, through in vitro, in silico, and crystallographic methods. Compounds 1-3 were evaluated against bovine pancreatic trypsin (BPT). Compound 1 was found to be active against trypsin with IC50 value of 247.98 ± 2.44 μM. Molecular docking studies were used to investigate the binding energy and binding conformation of inhibitor. All three compounds were subjected to crystallisation with trypsin. Compounds 1-2 were successfully crystallised with BPT The crystal structures of trypsin in complexed with compounds 1, and 2 were determined at 2.30 and 2.50 Å resolution, respectively. Both molecules showed their binding affinity with the active site residues of trypsin. This study will provide insight into the binding mechanism of E-64 and arginine and might be useful in designing effective inhibitors of serine proteases.
丝氨酸蛋白酶与多种疾病有关,包括胰腺炎和结肠癌。根据对底物的识别,丝氨酸蛋白酶可分为不同的类别。胰蛋白酶和胰蛋白酶样丝氨酸蛋白酶是研究最多的丝氨酸蛋白酶之一。胰蛋白酶是参与胰腺炎发病机制的主要水解酶之一。抑制胰蛋白酶有助于控制疾病。在此,我们通过体外、硅学和晶体学方法研究了一些基于精氨酸的小分子对胰蛋白酶的抑制作用。我们评估了化合物 1-3 对牛胰蛋白酶(BPT)的抑制作用。发现化合物 1 对胰蛋白酶具有活性,IC50 值为 247.98 ± 2.44 μM。分子对接研究用于研究抑制剂的结合能和结合构象。所有三种化合物都用胰蛋白酶进行了结晶。胰蛋白酶与化合物 1 和 2 复合物的晶体结构分辨率分别为 2.30 和 2.50 Å。这两种分子都显示出与胰蛋白酶活性位点残基的结合亲和力。这项研究将有助于深入了解 E-64 与精氨酸的结合机制,并可能有助于设计有效的丝氨酸蛋白酶抑制剂。
{"title":"In vitro, in silico and crystallographic-based identification of serine protease inhibitors","authors":"Zeeshan Akbar ,&nbsp;Malik Shoaib Ahmad","doi":"10.1080/14786419.2024.2425793","DOIUrl":"10.1080/14786419.2024.2425793","url":null,"abstract":"<div><div>Serine proteases are involved in various ailments, including pancreatitis, and colon cancer. Based on substrate recognition serine proteases are classified into different groups. Trypsin and trypsin-like serine proteases are among most studied group of serine proteases. Trypsin is among the chief hydrolysing enzyme involved in the pathogenesis of pancreatitis. Its inhibition can help to manage the disease. Herein, we investigated the trypsin inhibitory effect of some arginine-based small molecules, through <em>in vitro</em>, <em>in silico</em>, and crystallographic methods. Compounds <strong>1</strong>-<strong>3</strong> were evaluated against bovine pancreatic trypsin (BPT). Compound <strong>1</strong> was found to be active against trypsin with IC<sub>50</sub> value of 247.98 ± 2.44 <em>μ</em>M. Molecular docking studies were used to investigate the binding energy and binding conformation of inhibitor. All three compounds were subjected to crystallisation with trypsin. Compounds <strong>1</strong>-<strong>2</strong> were successfully crystallised with BPT The crystal structures of trypsin in complexed with compounds <strong>1</strong>, and <strong>2</strong> were determined at 2.30 and 2.50 Å resolution, respectively. Both molecules showed their binding affinity with the active site residues of trypsin. This study will provide insight into the binding mechanism of E-64 and arginine and might be useful in designing effective inhibitors of serine proteases.</div></div>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":"40 3","pages":"Pages 753-759"},"PeriodicalIF":1.6,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142624370","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Headspace solid phase microextraction combined with GC–MS for the analysis of volatile compounds of Calystegia silvatica (Kit.) Griseb. from Algeria 顶空固相微萃取-气相色谱-质谱联用分析银根(Kit.)挥发物Griseb。从阿尔及利亚。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-02-01 DOI: 10.1080/14786419.2025.2478297
Amina Boudjada , Amirat Mokhtar , Hamdi Bendif , Rebbas Khellaf , Guido Flamini , STefania Garzoli
This study represents the first investigation of the volatile composition of Calystegia silvatica (Convolvulaceae) collected in Algeria, using headspace solid-phase microextraction and gas chromatography/mass spectrometry (HS-SPME-GC/MS). This technique allowed the identification of 44 compounds, constituting 96.9% of the total components. These compounds belong to various chemical classes, including sesquiterpene hydrocarbons (22) and non-terpene derivatives (13), as major groups. Remarkably, the volatile profile of C. silvatica was dominated by sesquiterpenoids (87.1%), particularly sesquiterpene hydrocarbons (83%). Analysis of the aroma profile revealed that the main metabolites were β-caryophyllene, α-gurjunene and germacrene D. Oxygenated sesquiterpenes were present in a smaller proportion (4.1%), mostly represented by palustrol. Other chemical classes, such as monoterpene hydrocarbons, oxygenated monoterpenes, non-terpene derivatives and apocarotenes, have been found in limited quantities. It is worth noting that the data presented in this study have not previously been reported for Calystegia species.
本研究首次采用顶空气固相微萃取-气相色谱-质谱联用技术(HS-SPME-GC/MS)研究了阿尔及利亚产的卷叶菊的挥发性成分。该方法鉴定出44个化合物,占总成分的96.9%。这些化合物属于不同的化学类别,包括倍半萜烃(22)和非萜烯衍生物(13),作为主要基团。值得注意的是,松木挥发物以倍半萜类化合物为主(87.1%),尤其是倍半萜类烃(83%)。香气谱分析表明,其主要代谢物为β-石竹烯、α-古朱烯和德国烯d,含氧倍半萜类成分较少(4.1%),以帕鲁甾醇为代表。其他种类的化学物质,如单萜烯碳氢化合物、氧化单萜烯、非萜烯衍生物和麻瓜烯,数量有限。值得注意的是,在这项研究中提出的数据以前没有报道过Calystegia物种。
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引用次数: 0
Therapeutic effects of wogonin on sepsis and its mechanisms of action: a comprehensive systematic review. 沃戈宁对脓毒症的治疗作用及其作用机制:一项全面的系统综述。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-01-30 DOI: 10.1080/14786419.2026.2613344
Husni Farah, Waleed K Abdulsahib, Ihsan Khudhair Jasim, Soumya V Menon, Pradeepta Sekhar Patro, A Sabarivani, Gunjan Mukherjee, Aashna Sinha, Jasur Rizaev

Wogonin, a flavonoid derived from the plant Scutellaria baicalinase's, has emerged as a promising candidate for sepsis management due to its multifaceted pharmacological properties. A comprehensive search of databases, including Google Scholar, Scopus, Web of Science, PubMed, and Embase, was conducted up to November 2025 using relevant keywords. In-vivo studies were assessed using the SYRCLE risk of bias tool, and in-vitro studies were evaluated with the OHAT risk of bias tool. A total of 449 articles were initially sourced, ultimately, 24 publications included in this systematic review. Evidence from various in-vivo and in-vitro studies indicates that wogonin exerts protective effects against sepsis-induced organ damage by modulating critical signalling pathways such as NF-κB, MAPK, and Nrf2/HO-1. Despite these promising findings, further clinical trials are necessary to establish the safety and efficacy of wogonin in human subjects suffering from sepsis.

黄芩苷是一种从黄芩苷中提取的黄酮类化合物,由于其多方面的药理特性,已成为脓毒症治疗的有希望的候选药物。我们使用相关关键词对谷歌Scholar、Scopus、Web of Science、PubMed和Embase等数据库进行了全面检索,检索时间截止到2025年11月。使用sycle偏倚风险工具评估体内研究,使用OHAT偏倚风险工具评估体外研究。总共有449篇文章最初被引用,最终有24篇出版物被纳入本系统综述。来自各种体内和体外研究的证据表明,wogonin通过调节NF-κB、MAPK和Nrf2/HO-1等关键信号通路,对败血症诱导的器官损伤具有保护作用。尽管有这些令人鼓舞的发现,但需要进一步的临床试验来确定沃戈宁对人类败血症患者的安全性和有效性。
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引用次数: 0
Two new clerodane diterpenoids and their anti-inflammatory activity from Callicarpa integerrima. 两种新氯烷二萜及其抗炎活性研究。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2026-01-30 DOI: 10.1080/14786419.2026.2622548
Muhammad Aurang Zeb, Xiao-Ying Ruan, Xing-Jie Zhang, Yu-Tong Xing, Meng-Ru Wang, Yuan-Lin Kong, Xiao-Li Li, Kai Jiang, Wei-Lie Xiao

A phytochemical investigation of Callicarpa integerrima resulted in the isolation of two previously undescribed clerodane diterpenoids, compounds 1 and 2, in addition to four known compounds (3-6). Structural determination of the new compounds was accomplished through a comprehensive investigation of their spectral data (1D and 2D NMR, HR-ESI-MS and UV/IR), and their absolute configurations were assigned by the comparison of the experimental and calculated ECD curves, supported by specific rotation data. LDH release in J774A.1 macrophages was used to evaluate the anti-inflammatory effects of compounds 1-6. Compound 2 revealed remarkable activity, with an IC50 of 5.12 ± 0.24 µM, compared to andrographolide (IC50 of 12.48 ± 0.60 µM), effectively inhibiting lipopolysaccharide and nigericin-induced pyroptosis in a dose-dependent manner, highlighting its potential as a promising NLRP3 inflammasome inhibitor for further development.

一项植物化学研究发现,除了四种已知化合物(3-6)外,还分离出两种先前未被描述的氯烷二萜化合物1和2。通过对新化合物的光谱数据(1D和2D NMR, HR-ESI-MS和UV/IR)进行综合研究,确定了新化合物的结构,并通过实验和计算ECD曲线的比较确定了它们的绝对构型,并提供了比旋转数据的支持。以J774A.1巨噬细胞LDH释放量评价化合物1-6的抗炎作用。与穿心莲内酯(IC50为12.48±0.60µM)相比,化合物2显示出显著的活性,IC50为5.12±0.24µM,有效抑制脂多糖和尼日利亚菌素诱导的焦凋亡,并呈剂量依赖性,显示出其作为NLRP3炎症小体抑制剂的潜力,值得进一步开发。
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引用次数: 0
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