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Ten limonoids and three protolimonoids from the Thai mangrove Xylocarpus moluccensis. 泰国红树林 Xylocarpus moluccensis 中的十种类柠檬素和三种原柠檬素。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-19 DOI: 10.1016/j.fitote.2024.106307
Li-Fu Liu, Wei Zhao, Patchara Pedpradab, Jun Wu, Li Shen

Ten new limonoids, named xylomolones E-N (1-10), and two new protolimonoids, named xylomolones O (11) and P (12), were isolated from seeds of the Thai mangrove Xylocarpus moluccensis, together with the known compound, hispidone acetonide (13). The structures of these compounds were established by extensive NMR spectroscopic data, single-crystal X-ray diffraction analysis, and comparison of experimental ECD spectra. The absolute configurations of xylomolones E (1) and L (8) were unambiguously determined by single-crystal X-ray diffraction analyses, conducted with Cu Kα radiation. Xylomolones E-L (1-8) are mexicanolide-type limonoids, among which xylomolones J (6) and K (7) contain a C7/C28δ-lactone ring, whereas xylomolones M (9) and N (10) are phragmalin-type limonoids. Xylomolones O (11) and P (12) are two new protolimonoids. In addition, the 1H and 13C NMR spectroscopic data for hispidone acetonide (13) was first assigned completely. In bioassay, xylomolones F (2), M (9), and P (12) exhibited moderate inhibitory activity against the production of NO in LPS-induced RAW 264.7 cells with IC50 values of 31.54 ± 7.27, 62.84 ± 17.62, and 22.7 ± 6.56 μM, respectively.

从泰国红树林 Xylocarpus moluccensis 的种子中分离出了 10 种新的柠檬醛类化合物,分别命名为木犀草酮 E-N (1-10),以及两种新的原木犀草酮类化合物,分别命名为木犀草酮 O (11) 和 P (12),还有已知的化合物--丙酮庚二酮 (13)。这些化合物的结构是通过大量的核磁共振光谱数据、单晶 X 射线衍射分析和实验 ECD 光谱对比确定的。通过使用 Cu Kα 辐射进行单晶 X 射线衍射分析,明确确定了木糖醇酮 E (1) 和 L (8) 的绝对构型。木糖醇内酯 E-L(1-8)属于墨西哥内酯型柠檬酸类化合物,其中木糖醇内酯 J(6)和 K(7)含有一个 C7/C28δ 内酯环,而木糖醇内酯 M(9)和 N(10)属于葭苷型柠檬酸类化合物。木糖醇酮 O (11) 和 P (12) 是两种新的原柠檬酸类化合物。此外,还首次完整地分配了丙酮桧酮(13)的 1H 和 13C NMR 光谱数据。在生物测定中,木犀草酮 F (2)、M (9) 和 P (12) 对 LPS 诱导的 RAW 264.7 细胞产生的 NO 具有中等程度的抑制活性,IC50 值分别为 31.54 ± 7.27、62.84 ± 17.62 和 22.7 ± 6.56 μM。
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引用次数: 0
Pharmacology, phytochemistry, and traditional uses of Huperzia serrata (Thunb. ex Murray) Trev. Huperzia serrata (Thunb. ex Murray) Trev.的药理学、植物化学和传统用途。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-19 DOI: 10.1016/j.fitote.2024.106304
Zhuoliang Chu, Qingmei Sun, Meiqin Mao, Yutong Wu, Le Yu, Jingyi Xu, Kaohua Liu, Luping Qin, Bo Zhu

Huperzia serrata (HS) has been a staple of traditional Chinese medicine for centuries, revered for its efficacy in treating various ailments such as pain relief, hemostasis, detoxification, dehumidification, and heat clearing. This review offers an in-depth summary of the botany, traditional utilization, pharmacology, pharmacokinetics, phytochemistry, and safety profile of HS and intends to shed light on potential future research directions and applications of this plant. Information on HS was gathered from ScienceDirect, PubMed, Springer, Sci Finder, Baidu Scholar, and Google Scholar. Over 94 compounds have been separated and identified from HS, including alkaloids, terpenoids, volatile oils, flavonoids, and polysaccharides. Both crude extracts and purified compounds from HS have shown promise in treating a spectrum of conditions, including Alzheimer's disease, epilepsy, pain, cancer, and inflammation. These extracts and compounds exhibit diverse pharmacological properties, including neuroprotective, anti-Alzheimer's, anti-epileptic, analgesic, cardioprotective, hepatoprotective, antioxidant, and anticancer activities. Pharmacological investigations support the traditional use of HS and may validate the folk medicinal use of HS to treat many chronic diseases. Current literature suggests that the bioactivity of HS is largely attributed to its alkaloids and polysaccharides. However, further exploration is warranted to comprehensively understand the structure-function relationship of these constituents, molecular mechanisms, and their potential synergistic and antagonistic interactions. Moreover, additional modern pharmacological explorations are necessary to validate the traditional use of HS such as promoting hemostasis, treating tuberculosis, hemorrhoids, and diarrhea. Therefore, there is a pressing need for comprehensive investigations to fully assess HS' medicinal properties and therapeutic potential.

几个世纪以来,蛇床子(Huperzia serrata,HS)一直是传统中药的主要成分,因其具有止痛、止血、解毒、除湿和清热等多种功效而备受推崇。本综述对 HS 的植物学、传统用途、药理学、药动学、植物化学和安全性进行了深入总结,旨在阐明这种植物未来潜在的研究方向和应用。有关 HS 的信息来自 ScienceDirect、PubMed、Springer、Sci Finder、百度学术和谷歌学术。目前已从 HS 中分离并鉴定出超过 94 种化合物,包括生物碱、萜类化合物、挥发油、黄酮类化合物和多糖。HS 的粗提取物和纯化化合物都显示出治疗各种疾病的前景,包括老年痴呆症、癫痫、疼痛、癌症和炎症。这些提取物和化合物具有多种药理特性,包括神经保护、抗老年痴呆、抗癫痫、镇痛、心脏保护、肝脏保护、抗氧化和抗癌活性。药理研究支持传统上对 HS 的使用,并可证实民间使用 HS 治疗多种慢性疾病。目前的文献表明,HS 的生物活性主要归功于其生物碱和多糖。然而,要全面了解这些成分的结构-功能关系、分子机制及其潜在的协同和拮抗作用,还需要进一步探索。此外,有必要进行更多的现代药理学探索,以验证 HS 的传统用途,如促进止血、治疗肺结核、痔疮和腹泻等。因此,迫切需要进行全面研究,以充分评估 HS 的药用特性和治疗潜力。
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引用次数: 0
Diterpenoids and lignans from the stems of Tripterygium wilfordii and their anti-inflammatory activities. 威灵仙茎中的二萜和木脂素及其抗炎活性。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-19 DOI: 10.1016/j.fitote.2024.106306
Yulu Tian, Yazi Wei, Haowen Luo, Xinyi Chen, Jie Ma, Yingda Zang, Tiantai Zhang, Dongming Zhang, Chuangjun Li

Two undescribed diterpenoids (1-2) and three lignans (3a/3b, 4a), together with sixteen known compounds (4b, 5-9, 10a/10b-14a/14b) were obtained from the stems of Tripterygium wilfordii (T. wilfordii). The structures of these new compounds were elucidated by detailed spectroscopic analyses, and their absolute configurations were estabished by ECD calculations. Some compounds exhibited moderate inhibitory activities against IL-6 production in LPS-stimulated RAW 264.7 macrophages in vitro. Compound 5 showed significant anti-inflammatory activity in vitro (IC50, 0.77 μM) and inhibited macrophage polarization towards a pro-inflammatory phenotype.

从 Tripterygium wilfordii(T. wilfordii)的茎中获得了两种未被描述的二萜类化合物(1-2)和三种木脂素(3a/3b, 4a),以及 16 种已知化合物(4b, 5-9, 10a/10b-14a/14b)。通过详细的光谱分析阐明了这些新化合物的结构,并通过 ECD 计算确定了它们的绝对构型。一些化合物在体外对 LPS 刺激的 RAW 264.7 巨噬细胞产生的 IL-6 有中等程度的抑制作用。化合物 5 在体外表现出明显的抗炎活性(IC50,0.77 μM),并抑制巨噬细胞向促炎表型极化。
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引用次数: 0
Assessment of lapachol's anti-inflammatory effectiveness in mitigating sepsis-induced acute lung injury. 评估拉帕酚在减轻败血症引起的急性肺损伤方面的抗炎效果。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-17 DOI: 10.1016/j.fitote.2024.106298
Kavita Joshi, Vaishnavi Singh, Samit Chatterjee, Poonam Khandelwal, Rashmy Nair, Sameer Qureshi, Snigdha Siddh, Vandana Nunia

Sepsis-induced Acute Lung Injury (ALI) and Acute Respiratory Distress Syndrome (ARDS) pose life-threatening risks due to an excessive activation of proinflammatory cytokines via the JAK pathway. Currently, no confirmed drug treatment exists for ALI. In this study, we explored JAK1 as a potential therapeutic target to address this issue. This study evaluates lapachol, a bioactive secondary metabolite, for its potential in treating sepsis-induced Acute Lung Injury (ALI). Lapachol was selected based on in-silico analyses such as binding energy, RMSD, RMSF, H-bond graphs, and lig plots supported the hypothesis that Lapachol binds to JAK1 in a manner similar to Tofacitinib JAK1/3 inhibitor (Positive control). Lapachol, derived from the heartwood of Tecomella undulata, was used in this investigation. Swiss albino mice were categorized into control, LPS treated, positive control (Tofacitinib), and experimental groups (Lapachol at 20 and 40 mg/kg doses). Throughout the experiment, mice behaviour was monitored, and euthanasia was performed at 12 and 24-h intervals. Various analyses, including body weight, W/D ratio, lung weight/body weight ratio, flow cytometry of BAL fluid (at 12 and 24 h), histology, myeloperoxidase assays were performed. Results indicated that both Tofacitinib and Lapachol significantly reduced ALI markers, including lung weight/body weight ratio, cell counts, and granulocytes in bronchoalveolar lavage fluid. Moreover, histopathology and MPO analysis suggested that Lapachol, particularly at 40 mg/kg, exhibited anti-inflammatory effects comparable to Tofacitinib. Conclusively, the findings suggest that Lapachol possesses the potential to inhibit JAK1 kinase domains and mitigate ALI associated with sepsis similar to Tofacitinib.

脓毒症诱发的急性肺损伤(ALI)和急性呼吸窘迫综合征(ARDS)会通过 JAK 通路过度激活促炎细胞因子,从而危及生命。目前,尚无治疗 ALI 的药物。在本研究中,我们将 JAK1 作为潜在的治疗靶点来解决这一问题。本研究评估了生物活性次生代谢物拉帕酚治疗脓毒症诱发的急性肺损伤(ALI)的潜力。根据结合能、RMSD、RMSF、H 键图和 lig 图等室内分析结果,我们选择了拉帕酚,这些分析结果支持这样的假设:拉帕酚与 JAK1 的结合方式与托法替尼 JAK1/3 抑制剂(阳性对照)相似。本研究中使用的 Lapachol 提取自 Tecomella undulata 的心材。瑞士白化小鼠被分为对照组、LPS 处理组、阳性对照组(托法替尼)和实验组(拉帕酚剂量为 20 毫克/千克和 40 毫克/千克)。在整个实验过程中,对小鼠的行为进行监测,并在每隔 12 和 24 小时对小鼠实施安乐死。进行了各种分析,包括体重、W/D 比值、肺重量/体重比值、BAL 液流式细胞术(12 和 24 小时)、组织学、髓过氧化物酶测定。结果表明,托法替尼和拉帕酚都能显著降低ALI指标,包括肺重量/体重比、细胞计数和支气管肺泡灌洗液中的粒细胞。此外,组织病理学和MPO分析表明,拉帕酚(尤其是40毫克/千克的剂量)的抗炎效果与托法替尼相当。总之,研究结果表明,拉帕酚具有与托法替尼相似的抑制JAK1激酶域和减轻脓毒症相关ALI的潜力。
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引用次数: 0
Phytochemical characterization, toxicity and pharmacological profile of the central effects of the fixed fruit pulp oil of Mauritia flexuosa L.F. (buriti). Mauritia flexuosa L.F.(buriti)固定果肉油的植物化学特征、毒性和中枢效应药理学概况。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-17 DOI: 10.1016/j.fitote.2024.106303
Isaac Moura Araújo, Andressa de Alencar Silva, Luís Pereira-de-Morais, Debora de Menezes Dantas, Maysa de Oliveira Barbosa, Giovana Mendes Lacerda Leite, Carla de Fátima Alves Nonato, José Galberto Martins da Costa, Raimundo Luiz Silva Pereira, Marta Regina Kerntopf Mendonça, Henrique Douglas Melo Coutinho, Gyllyandeson de Araújo Delmondes

Anxiety and depression are mental disorders that have been exponentially increasing over the last decades. Psychopharmacology emerged to try to alleviate the symptoms of these disorders; however, the side effects and the time it takes to achieve the desired effect are factors that decrease the search for and adherence to treatment. To remedy this situation, new compounds capable of improving the performance of these medications and reducing their adverse effects have been sought. The use of medicinal plants has been widely employed for this purpose. Mauritia flexuosa F.L., a palm tree with high incidence in Brazil, has been heavily targeted as all its parts are usable. The objective of this study is to evaluate the effects of fixed oil from the fruit of the buriti palm in models of depression and anxiety. The phytochemical profile of this oil and its toxicity were also investigated. The experiments conducted included the open field, rotarod, forced swim, and elevated plus maze tests. As a result, it was observed that the fixed oil from buriti palm presented 18 compounds, with elaidic acid being the major one, and showed no signs of toxicity. However, it demonstrated a possible stimulating activity in the open field test and had no effect on the motor system in the rotarod test. Furthermore, it exhibited an antidepressant-like effect in the forced swim test but an anxiety-like effect in the elevated plus maze test. Therefore, buriti oil may potentially be used in new formulations to assist in the treatment of anxiety and depression.

焦虑症和抑郁症是过去几十年来呈指数增长的精神疾病。精神药理学的出现试图缓解这些疾病的症状;然而,副作用和达到预期效果所需的时间是减少寻求和坚持治疗的因素。为了改变这种状况,人们一直在寻找能够改善这些药物的疗效并减少其不良反应的新化合物。为此,人们广泛使用药用植物。Mauritia flexuosa F.L.是一种在巴西发病率很高的棕榈树,由于其所有部分都可以使用,因此被列为重点研究对象。本研究的目的是评估从布尔提棕榈果实中提取的固定油对抑郁和焦虑模型的影响。此外,还研究了这种油的植物化学成分及其毒性。实验包括开阔地、旋转木马、强迫游泳和高架加迷宫测试。结果表明,布里提棕榈的固定油中含有 18 种化合物,其中主要是依来地酸,并且没有显示出毒性迹象。不过,它在开阔地试验中表现出可能的刺激活性,而在旋转木马试验中对运动系统没有影响。此外,它在强迫游泳试验中表现出类似抗抑郁的效果,但在高架加迷宫试验中表现出类似焦虑的效果。因此,布里提油有可能被用于辅助治疗焦虑症和抑郁症的新配方中。
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引用次数: 0
Integrated workflows using metabolomics, genome mining, and biological evaluation reveal oxepine‑sulfur-containing anti-cryptococcal diketopiperazine produced by the endophyte Penicillium setosum. 利用代谢组学、基因组挖掘和生物评估的综合工作流程揭示了内生青霉 setosum 产生的含氧硫抗隐球菌二酮哌嗪。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-16 DOI: 10.1016/j.fitote.2024.106301
Cláudia Maria da Silva Costa de Oliveira, Milena Costa Bassicheto, Renan Santini Barbosa, Kiandro de Oliveira Gomes Neves, Caroline Dos Santos Monteiro, Miriam Uemi, Renata Castiglioni Pascon, Gilvan Ferreira da Silva, Hector Henrique Ferreira Koolen, Lívia Soman de Medeiros

Cryptococcosis is a fungal infection for which treatment relies on old antifungal agents usually leading to drawbacks such as high toxicity and mainly low efficiency since drug resistance of microorganisms is strongly widespread. The discovery of new antifungal agents is urgent and investigations about underexplored Natural Product (NP) can yield the necessary outcomes to guide the discovery of new prototypes to anti-cryptococcal molecules development. In this scenario, an integrated strategy involving metabolomic data analysis, biological assessement and genome mining of P. setosum CMLD 18, revealed the biosynthesis of bis(methyl-sulfanyl) oxepine-containing diketopiperazine derivative, the bisdethiobis(methylthio)acetylaranotine (1) by the endophyte. The molecule showed a minimum inhibitory concentration (MIC) value of 0.125 mM when tested against C. neoformans. Evidence about the corresponding biosynthetic gene cluster (BGC) responsible for the biosynthesis of (1) in P. setosum were found. Moreover, other putative analogues of (1) were also detected, suggesting this microorganism may represent an important source of likely anti-cryptococcal molecules to be further investigated.

隐球菌病是一种真菌感染,其治疗通常依赖于旧的抗真菌药物,但由于微生物的耐药性非常普遍,因此通常会导致高毒性和低效率等缺点。发现新的抗真菌剂迫在眉睫,而对尚未充分开发的天然产物(NP)的研究可以产生必要的成果,指导发现新的原型,以开发抗隐球菌分子。在这种情况下,一种涉及 P. setosum CMLD 18 的代谢组数据分析、生物评估和基因组挖掘的综合策略揭示了内生菌生物合成含双(甲硫基)氧杂环庚烷的二酮哌嗪衍生物--双硫代双(甲硫基)乙酰aranotine (1)。该分子对新变形杆菌的最低抑制浓度(MIC)值为 0.125 mM。研究还发现了 P. setosum 中负责生物合成(1)的相应生物合成基因簇(BGC)。此外,还检测到了(1)的其他假定类似物,这表明该微生物可能是抗隐球菌分子的重要来源,有待进一步研究。
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引用次数: 0
Kakuol and asarinin protecting liver injury via HSP90AA1/CDK2/mTOR signaling pathway. Kakuol和asarinin通过HSP90AA1/CDK2/mTOR信号通路保护肝损伤。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-15 DOI: 10.1016/j.fitote.2024.106297
Ling Jiang, Cai-Bo Tian, Rui-Han Ye, Nian Shi, Xing-Chao He, Yun-Li Zhao, Xiao-Dong Luo

Drug-induced liver injury caused acute hepatic failure and hepatitis frequently. In this investigation, kakuol and asarinin reduced the levels of serum alanine transaminase (ALT), aspartate transaminase (AST) and malondialdehyde (MDA) dramatically, and ameliorated the pathological damage of liver tissues in APAP-induced mice. Furthermore, both compounds increased the viabilities of APAP-induced L-O2 cells and extracellular glutathione (GSH) levels accompanied significantly by reducing the level of intracellular ROS in vitro. In addition, HSP90AA1/CDK2/mTOR signaling pathway and five target proteins (CDK2, HSP90AA1, HRAS, MMP1, mTOR) were proposed from network pharmacology and molecular docking prediction, and then the up-regulation of protein expression of CDK2, mTOR and down-regulation of HSP90AA1, HRAS, MMP1 by kakuol and asarinin in western blotting supported their mechanism.

药物引起的肝损伤经常导致急性肝功能衰竭和肝炎。在这项研究中,卡枯酚和皂苷能显著降低 APAP 诱导的小鼠血清丙氨酸转氨酶(ALT)、天门冬氨酸转氨酶(AST)和丙二醛(MDA)的水平,改善肝组织的病理损伤。此外,这两种化合物通过降低细胞内 ROS 水平,显著提高了 APAP 诱导的 L-O2 细胞的活力和细胞外谷胱甘肽(GSH)水平。此外,通过网络药理学和分子对接预测,提出了HSP90AA1/CDK2/mTOR信号通路和五个靶蛋白(CDK2、HSP90AA1、HRAS、MMP1、mTOR),然后通过Western blotting检测卡枯酚和asarinin对CDK2、mTOR蛋白表达的上调和对HSP90AA1、HRAS、MMP1蛋白表达的下调支持了它们的作用机制。
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引用次数: 0
Antidiabetic and antioxidant profiling of 67 African trifoliate yam accessions by planar on-surface assays versus in vitro assays 通过平面表面试验和体外试验对 67 个非洲三叶山药品种进行抗糖尿病和抗氧化分析。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-14 DOI: 10.1016/j.fitote.2024.106299
Priscilla O. Aiyedun , Mubo A. Sonibare , Badara Gueye , Dirk C. Albach , Julia Heil , Gertrud E. Morlock
Trifoliate yam (Dioscorea dumetorum) is traditionally used to treat diabetics in Nigeria. However, almost no information is available on its antidiabetic constituents and their natural variance. Hence, the activity of methanolic tuber extracts of 67 trifoliate yam accessions from the largest collection in Africa was proven by four colorimetric antidiabetic and antioxidant in vitro assays, as diabetes is also linked with oxidative stress. For the first time, selected accessions were also analyzed by planar bioactivity profiling. It has a comparatively higher, more differentiated information content, is more sustainable in terms of material consumption, and enables straightforward compound prioritization and characterization. Up to a dozen individual antioxidant zones were revealed as well as one prominent zone inhibiting α-glucosidase and α-amylase. The latter inhibition zone was tentatively assigned to palmitic, linoleic, oleic, linolenic, oxo-nonanoic fatty acids by direct elution to heated electrospray ionization high-resolution mass spectrometry.
在尼日利亚,三叶山药(Dioscorea dumetorum)传统上用于治疗糖尿病。然而,几乎没有关于其抗糖尿病成分及其天然差异的信息。因此,通过四种比色法进行体外抗糖尿病和抗氧化试验,证明了非洲最大的 67 种三叶山药品种的甲醇块茎提取物的活性,因为糖尿病也与氧化应激有关。此外,还首次对所选品种进行了平面生物活性分析。这种方法的信息含量相对更高,区分度更大,在材料消耗方面更具可持续性,而且可以直接确定化合物的优先次序和特征。研究发现了多达十几个单独的抗氧化区,以及一个显著的α-葡萄糖苷酶和α-淀粉酶抑制区。通过直接洗脱到加热电喷雾离子化高分辨率质谱仪,后一个抑制区被初步归类为棕榈酸、亚油酸、油酸、亚麻酸和氧化壬酸脂肪酸。
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引用次数: 0
Synthesis and pharmacological activity evaluation of 2-(2-Phenylethyl)chromone analogues: The principal components in agarwood 2-(2-苯基乙基)铬酮类似物的合成和药理活性评价:沉香中的主要成分。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-13 DOI: 10.1016/j.fitote.2024.106296
Mingliang Zhang , Mengrong Niu , Jiangping Fan , Zihan Lu , Zhixiang Zhu , Bowen Gao , She-Po Shi
2-(2-Phenylethyl)chromones (PECs), the pivotal constituents responsible for the distinctive aroma and pharmacological potential of agarwood, are primarily obtained through extraction from natural materials. The restricted availability of agarwood has, however, hindered a comprehensive and systematic evaluation of their biological properties. In this study, we have chemically synthesized a total of 38 PEC derivatives, including 23 new compounds that had not been previously isolated from agarwood. These compounds were then evaluated for their inhibitory effects on nitric oxide release, neutrophil superoxide production, as well as their activities against tyrosinase, acetylcholinesterase, and α-glucosidase. The preliminary screening resulted in the identification of promising leads with potential therapeutic activities, and the structure-activity relationship of the synthesized PECs have also been briefly discussed. The results provide a foundation for the synthesis and pharmacological exploration of PECs, which sheds light on the pharmacological potential of agarwood's secondary metabolites.
2-(2-苯基乙基)色酮(PECs)是沉香木独特香气和药理潜力的关键成分,主要通过从天然材料中提取获得。然而,由于沉香的可获得性有限,阻碍了对其生物特性进行全面系统的评估。在这项研究中,我们用化学方法合成了 38 种 PEC 衍生物,其中包括 23 种以前从未从沉香木中分离出来的新化合物。然后对这些化合物对一氧化氮释放、中性粒细胞超氧化物生成的抑制作用,以及对酪氨酸酶、乙酰胆碱酯酶和α-葡萄糖苷酶的活性进行了评估。通过初步筛选,确定了具有潜在治疗活性的有希望的先导化合物,并简要讨论了合成的 PECs 的结构-活性关系。这些结果为 PECs 的合成和药理探索奠定了基础,从而揭示了沉香次生代谢物的药理潜力。
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引用次数: 0
Chemical profiles and antibacterial actions of Zanthoxylum acanthopodium DC. Essential oil growing in Indonesia Zanthoxylum acanthopodium DC.精油生长在印度尼西亚。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2024-11-12 DOI: 10.1016/j.fitote.2024.106300
Abdi Wira Septama , Eldiza Puji Rahmi , Aprilia Nur Tasfiyati , Nur Aini Khairunnisa , Halimah Raina Nasution , Nilesh Nirmal , Sofna Dewita Sari Banjarnahor , Nurhadi , Dadang Priyatmojo
Foodborne illness caused by pathogens has been a major health problem. Antibacterial resistance renders therapeutic options for treating the condition more limited, hence there is a growing interest in finding novel antibacterial alternatives. Zanthoxylum acanthopodium (Rutaceae) essential oil (ZAEO) has a substantial potential to suppress the growth of bacterial infections. This study was conducted to evaluate antibacterial activity of ZAEO against four species of foodborne pathogens that cause potential infections. The checkerboard assay was used to identify synergistic effect of ZAEO and tetracycline, while bacteriolysis test was applied to evaluate the ability of ZAEO releasing material genetics of bacteria, inhibiting biofilm formation, and suppressing efflux pump. The oils of Z. acanthopodium was evaluated and showed that the highest constituents were limonene and geranyl acetate at 47.13 % and 23.84 %, respectively. These oils have the strongest ability to inhibit Escherichia coli compared to other pathogens with MIC value of 62.5 μg/mL. ZAEO and tetracycline also presented a synergistic effect against E. coli with FICI value of 0.37. Moreover, this combination of ZAEO and antibiotic shown as potential antibacterial agent by several mechanisms such as, decreasing biofilm formation, releasing ions, rupturing membrane cells, and suppressing the efflux pump of E. coli. It can be concluded that ZAEO and tetracycline presented a promising antibacterial activity, which can be explored further to develops antibacterial agents against foodborne pathogens.
由病原体引起的食源性疾病一直是一个重大的健康问题。抗菌药的耐药性使治疗这种疾病的方法更加有限,因此人们对寻找新的抗菌替代品越来越感兴趣。Zanthoxylum acanthopodium(芸香科)精油(ZAEO)具有抑制细菌感染生长的巨大潜力。本研究评估了ZAEO对四种可能引起感染的食源性病原体的抗菌活性。采用棋盘试验来确定ZAEO和四环素的协同作用,同时采用细菌溶解试验来评估ZAEO释放细菌遗传物质、抑制生物膜形成和抑制外排泵的能力。对刺五加油进行了评估,结果表明,含量最高的成分是柠檬烯和乙酸香叶酯,分别为 47.13 % 和 23.84 %。与其他病原体相比,这些油对大肠杆菌的抑制能力最强,其 MIC 值为 62.5 μg/mL。ZAEO和四环素对大肠杆菌也有协同作用,FICI值为0.37。此外,ZAEO 和抗生素的组合通过多种机制显示出潜在的抗菌作用,如减少生物膜的形成、释放离子、破坏膜细胞和抑制大肠杆菌的外排泵。由此可以得出结论,ZAEO 和四环素具有良好的抗菌活性,可以进一步开发针对食源性病原体的抗菌剂。
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Fitoterapia
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