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New 3-acyl derivatives of glaucocalyxin A: designed, synthesis and in vitro antibacterial activities. 琉璃苣毒素 A 的新 3-酰基衍生物:设计、合成和体外抗菌活性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-11-20 DOI: 10.1080/10286020.2024.2429136
Wei-Xian Yang, Wei-Qing Zhang, Mei-Qi Wei, Mei-Hui Duan, Xian-Ji Liu, Chen Yan

To discover novel antimicrobial drug, 22 novel acylated derivatives were synthesized by A-ring modification of glaucocalyxin A. The structures of these derivatives were confirmed by NMR and MS data. In vitro antimicrobial activity of these compounds was evaluated against E. faecium, E. faecalis, MRSA, E. coli, A. baumannii and K. pneumoniae. The results showed compound 3d against E. faecium, E. faecalis and MRSA with a minimum inhibitory concentration of 4 μg/ml. And further molecular docking revealed that compound 3d has a higher binding affinity. In conclusion, compound 3d has the potential to develop into a new drug against drug-resistant bacteria.

为了发现新型抗菌药物,研究人员通过对琉璃苣毒素 A 进行 A 环修饰,合成了 22 种新型酰化衍生物。评估了这些化合物对粪大肠杆菌、粪肠球菌、MRSA、大肠杆菌、鲍曼不动杆菌和肺炎双球菌的体外抗菌活性。结果表明,化合物 3d 对粪肠球菌、屎肠球菌和 MRSA 的最低抑制浓度为 4 μg/ml。进一步的分子对接显示,化合物 3d 具有更高的结合亲和力。总之,化合物 3d 有潜力发展成为一种抗耐药细菌的新药。
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引用次数: 0
Medicinal plants or bioactive components with antioxidant/anti-apoptotic effects as a potential therapeutic approach in heart failure prevention and management: a literature review 将具有抗氧化/抗细胞凋亡作用的药用植物或生物活性成分作为预防和治疗心力衰竭的潜在治疗方法:文献综述。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-11-20 DOI: 10.1080/10286020.2024.2414196
Atefeh Jalali , Maryam Kabiri , Shima Hashemi , Alireza Abdi Ardekani , Mohammad M. Zarshenas
Heart failure is described as a complicated syndrome, which is estimated that 56.2 million people were living with HF globally in 2019. Oxidative stress and apoptosis play a major role on HF development via targeting several signaling pathways in cardiac cells. This study investigated medicinal plants or their bioactive components with positive effects on HF management. In this research, keywords “heart failure,” “plant,” “antioxidant” or “radical scavenging,” “herbal” and “apoptosis” were synchronously searched through popular databases from 1990 up to 2023. Finally, the role of oxidative stress and apoptosis in HF development was searched and related signaling pathways were investigated.
心力衰竭是一种复杂的综合征,据估计,2019 年全球有 5620 万人患有心力衰竭。氧化应激和细胞凋亡通过靶向心脏细胞中的几种信号通路,对高血压的发展起着重要作用。本研究调查了对心房颤动治疗有积极作用的药用植物或其生物活性成分。在这项研究中,从 1990 年到 2023 年,我们通过流行数据库同步检索了 "心衰"、"植物"、"抗氧化 "或 "自由基清除"、"草药 "和 "细胞凋亡 "等关键词。最后,检索了氧化应激和细胞凋亡在心力衰竭发病中的作用,并研究了相关的信号通路。
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引用次数: 0
Two new quinazolinone alkaloids from Aspergillus udagawae. 来自乌达加瓦埃曲霉的两种新的喹唑啉酮生物碱。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-11-18 DOI: 10.1080/10286020.2024.2424910
Lin Liang, Xi Yuan, Xiao-Ya Xian, Xian-Li Zhou, Tong-Dong Kuang, Jin-Tao Gao, Li-Sheng Wang, Cheng-Qin Liang

Two new quinazolinone alkaloids, benzomalvin F (1), and quinadoline C (2), along with four known quinazolinones (3-6), were isolated from cultures of the wetland-soil-derived fungus Aspergillus udagawae from the Huixian wetland in Guilin. Their structures were elucidated based on detailed spectroscopic analysis, including 1D, 2D NMR, mass spectrometry, and IR spectra. In addition, the anti-inflammatory results showed that compounds 1, 2, 4, and 5 had significant inhibitory effects on NO production in RAW264.7 cells activated by lipopolysaccharide (LPS), with IC50 values of 24.5 ± 0.1, 29.7 ± 0.1, 29.4 ± 0.1, and 31.0 ± 0.1 µM respectively, compared with the positive control indomethacin (IC50 = 31.6 ± 0.4 μM).

从桂林会仙湿地的湿地土源真菌乌达曲霉(Aspergillus udagawae)的培养物中分离出了两种新的喹唑啉酮生物碱--苯并马来文F(1)和喹唑啉C(2),以及四种已知的喹唑啉酮(3-6)。通过详细的光谱分析,包括一维、二维核磁共振、质谱和红外光谱,阐明了它们的结构。此外,抗炎结果表明,与阳性对照吲哚美辛(IC50 = 31.6 ± 0.4 μM)相比,化合物 1、2、4 和 5 对脂多糖(LPS)激活的 RAW264.7 细胞的 NO 生成具有显著的抑制作用,IC50 值分别为 24.5 ± 0.1、29.7 ± 0.1、29.4 ± 0.1 和 31.0 ± 0.1 μM。
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引用次数: 0
Evaluation of the potential anti-arthritic effects and evaluation of acute oral toxicity of the active fraction of Eclipta prostrata leaves in rat model. 在大鼠模型中评估 Eclipta prostrata 叶子活性成分的潜在抗关节炎作用和急性口服毒性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-11-13 DOI: 10.1080/10286020.2024.2422974
Anjoo Kamboj, Hitesh Malhotra, Himanshu Mukhija, Arockia Babu

The primary goal of this research was to isolate and assess the bioactive compounds within Eclipta prostrata Linn's chloroform extract, with a focus on their potential to combat arthritis, validating its traditional use. Initially, antioxidant characteristics were evaluated, followed by fractionation through column chromatography. The in-vivo safety assessment, following OECD TG 425 Guidelines, showed no mortality at doses up to 2000 mg/kg, confirming the fraction's safety. Subsequently, the active fraction was assessed in a complete Freund's adjuvant-induced arthritis model. It demonstrated a dose-dependent inhibitory effect on inflammation and improved various parameters, including thermal latency time, dorsal flexion, motility, and motor coordination. Active bio constituents like rutin, stigmasterol, quercetin, and beta-sitosterol were estimated in the active fraction. The findings provide validation for the traditional use of E. prostrata as a potential plant with anti-arthritic properties, suggesting its potential suitability for rheumatoid arthritis treatment.

这项研究的主要目的是分离和评估 Eclipta prostrata Linn 的氯仿提取物中的生物活性化合物,重点研究其抗击关节炎的潜力,从而验证其传统用途。首先对其抗氧化特性进行评估,然后通过柱层析法进行分馏。根据 OECD TG 425 准则进行的体内安全性评估显示,在剂量高达 2000 毫克/千克的情况下,没有人死亡,这证实了馏分的安全性。随后,在完全弗氏佐剂诱导的关节炎模型中对活性馏分进行了评估。它对炎症有剂量依赖性抑制作用,并改善了各种参数,包括热潜伏时间、背屈、运动能力和运动协调性。据估计,活性成分中含有芦丁、豆甾醇、槲皮素和 beta-谷甾醇等活性生物成分。研究结果验证了 E. prostrata 作为一种具有抗关节炎特性的潜在植物的传统用途,表明其可能适用于类风湿性关节炎的治疗。
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引用次数: 0
Two new glycosides and a new flavone from Gerbera delavayi. 来自非洲菊的两种新苷和一种新黄酮。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-11-09 DOI: 10.1080/10286020.2024.2420613
Yu-Shuang Wen, Li Jiang, Yang Wang, Ying-Jie Xu, Chun-Hua Liu, Yong Huang, Xue Ma, Yong-Jun Li

Three new compounds, including two glycosides, named gerbelavinsides E/G (1/2), and a flavone, named gerbelavin G (3), were isolated from 50% ethanol extract of Gerbera delavayi. Their structures were elucidated based on HR-ESI-MS, IR, UV and NMR spectral data, and the absolute configurations of 1 and 3 were determined by ECD spectra. Three compounds were tested for their inhibition effect against LPS-induced NO production in RAW 264.7 cells. They exhibited different degrees of inhibition activities with rates of 40.55 ± 1.65%, 70.13 ± 0.55%, 56.74 ± 1.15%, respectively.

从非洲菊 50%的乙醇提取物中分离出了三种新化合物,包括两种苷类化合物,命名为非洲菊苷 E/G (1/2),以及一种黄酮类化合物,命名为非洲菊苷 G (3)。根据 HR-ESI-MS、IR、UV 和 NMR 光谱数据阐明了它们的结构,并通过 ECD 光谱确定了 1 和 3 的绝对构型。测试了三种化合物对 RAW 264.7 细胞中 LPS 诱导的 NO 生成的抑制作用。它们表现出不同程度的抑制活性,抑制率分别为 40.55 ± 1.65%、70.13 ± 0.55%、56.74 ± 1.15%。
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引用次数: 0
Taxifolin ameliorates the D-galactose-induced aging of mouse hippocampal neurons HT-22 cells through modulating SIRT1/p53 and PI3K/AKT signaling pathways. 紫杉叶素通过调节SIRT1/p53和PI3K/AKT信号通路改善D-半乳糖诱导的小鼠海马神经元HT-22细胞衰老。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-11-01 DOI: 10.1080/10286020.2024.2421925
Xing-Long Liu, Shuang Zu, Hao Yue, An-Ning Li, Ping-Ping Sun, Jian-Guo Li, Li Yan, Li-Na Ma, Shuai Zhang

By establishing an in vitro model of D-Gal-induced brain neuronal cell (HT-22) senescence, it was found that TAX treatment significantly increased the activities of SOD and GSH, while decreasing MDA levels in aging HT-22 cells, indicating that TAX effectively restored the total antioxidant capacity and antioxidant enzyme activity of aging HT-22 cells induced by D-Gal, and attenuated cellular oxidative stress injury. In addition, taxifolin could also protect HT-22 cells from aging by up-regulating SIRT1 while reducing the expression of Ac-p53, indicating that TAX may be an active substance that can effectively delay cell aging.

通过建立体外D-Gal诱导的脑神经细胞(HT-22)衰老模型,发现TAX处理可显著提高衰老HT-22细胞的SOD和GSH活性,同时降低MDA水平,表明TAX能有效恢复D-Gal诱导的衰老HT-22细胞的总抗氧化能力和抗氧化酶活性,减轻细胞氧化应激损伤。此外,Taxifolin还能通过上调SIRT1而降低Ac-p53的表达,从而保护HT-22细胞免于衰老,这表明TAX可能是一种能有效延缓细胞衰老的活性物质。
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引用次数: 0
Recent advances in natural products and derivatives with antiviral activity against respiratory syncytial virus (RSV). 具有抗呼吸道合胞病毒(RSV)病毒活性的天然产品和衍生物的最新进展。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-10-19 DOI: 10.1080/10286020.2024.2417211
Ameena Tur Rasool, Erguang Li, Ahsan Nazir

Respiratory syncytial virus (RSV) is a widespread viral infection that causes millions of high-risk illnesses annually. Medicinal herbs such as ginseng root, echinacea purpurea, and radix astragali have a positive effect on antiviral activity by preventing viral adhesion, syncytial development, inhibiting viral internalization, relieving respiratory inflammation, strengthening the immune system, and stimulating the release of interferons. The potential benefits of natural products in terms of lower costs, better patient outcomes, and fewer adverse effects are discussed. This review examines the current evidence on the prevention and control of RSV with natural ingredients and the challenges and opportunities in clinical practice.

呼吸道合胞病毒(RSV)是一种广泛传播的病毒感染,每年导致数百万人患上高危疾病。人参根、紫锥菊和黄芪等药草通过防止病毒粘附、合胞体发育、抑制病毒内化、缓解呼吸道炎症、增强免疫系统和刺激干扰素释放,对抗病毒活性有积极作用。文中讨论了天然产品在降低成本、改善患者疗效和减少不良反应方面的潜在益处。本综述探讨了利用天然成分预防和控制 RSV 的现有证据以及临床实践中的挑战和机遇。
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引用次数: 0
Caenorhabditis elegans as in vivo model for the screening of natural plants-derived novel anti-aging compounds: a short introduction. 作为体内模型筛选天然植物提取的新型抗衰老化合物的草履虫:简短介绍。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-10-15 DOI: 10.1080/10286020.2024.2414189
Samah H O Zarroug

The global aging population highlights the need for effective anti-aging treatments. Natural products show promise, but thorough evaluation requires in vivo models due to the complexity of aging. Ethical concerns are driving a shift from traditional models like rabbits and mice to alternatives such as Caenorhabditis elegans. This microscopic nematode, with its short life cycle, genetic similarities to humans, and cost-effectiveness, is ideal for testing anti-aging compounds. We review studies using C. elegans to assess natural products, suggesting it could serve as a primary model for -evaluating the safety and efficacy of plant-derived anti-aging compounds.

全球人口老龄化凸显了对有效抗衰老疗法的需求。天然产品大有可为,但由于衰老的复杂性,彻底评估需要体内模型。出于伦理方面的考虑,人们正在从兔子和小鼠等传统模型向 elegans 线虫等替代模型转变。这种微小的线虫生命周期短,基因与人类相似,成本效益高,是测试抗衰老化合物的理想选择。我们回顾了利用秀丽隐杆线虫评估天然产品的研究,认为它可以作为评估植物抗衰老化合物安全性和有效性的主要模型。
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引用次数: 0
A regio-specific 4'-O-methyltransferase from Epimedium pseudowushanense regiospecifically catalyzing 8-prenylkeampferol to icaritin. 一种来自淫羊藿的区域特异性 4'-O-甲基转移酶,可将 8-异戊烯基莰菲醇催化为冰片苷。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-10-07 DOI: 10.1080/10286020.2024.2411710
Ke-Ping Feng, Ji-Mei Liu, Ri-Dao Chen, Qiao-Man Fei, Ke-Bo Xie, Da-Wei Chen, Jun-Gui Dai

Epimedium is widely used in traditional Chinese medicine and contains rich bioactive compounds. These compounds often have a methyl group at their 4'-OH position catalyzed by methyltransferases. Therefore, studying methyltransferases in Epimedium plants is of great significance. In this study, a flavonol methyltransferase, EpOMT4, was isolated from Epimedium pseudowushanense B.L. Guo. The recombinant enzyme regiospecifically transferred a methyl group to the 4'-OH position of 8-prenylkaempferol forming icaritin. The study demonstrates that enzymatic methylation of flavonoids in Epimedium plants holds significant potential and could provide a promising alternative method for the biosynthetic production of bioactive methylated prenylflavonoids.

淫羊藿被广泛用于传统中药,含有丰富的生物活性化合物。在甲基转移酶的催化下,这些化合物的 4'-OH 位置通常带有一个甲基。因此,研究淫羊藿植物中的甲基转移酶具有重要意义。本研究从 Epimedium pseudowushanense B.L. Guo 分离出了一种黄酮醇甲基转移酶 EpOMT4。该重组酶能将一个甲基特异性地转移到 8-异戊烯基山奈酚的 4'-OH 位置,形成冰片黄酮素。该研究表明,淫羊藿植物中黄酮类化合物的酶法甲基化具有很大的潜力,可为生物合成生产具有生物活性的甲基化前酰基黄酮类化合物提供一种很有前途的替代方法。
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引用次数: 0
Potential benefits of marine-derived compounds for slowing the advancement of Alzheimer's disease. 海洋萃取化合物对延缓阿尔茨海默氏症发展的潜在益处。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-10-07 DOI: 10.1080/10286020.2024.2409869
Aditya Malan, Manjusha Choudhary, Prabhjeet Kaur Bamrah, Dipender Kumari

The incidence of Alzheimer's is increasing and poses a significant social and economic burden. The pathogenesis involved in the expansion of AD includes neuronal oxidative damage, tau phosphorylation, amyloid beta aggregation, neuroinflammation, etc. Despite enormous efforts, there is currently no effective treatment or cure for this condition in the allopathic system. Marine compounds are appealing options and have a strong neuroprotective impact. Marine-derived compounds from sponges, algae, and marine invertebrates can be used for neuroprotection, with fewer adverse effects than synthetic drugs. Various compounds such as bryostatin-1, docosahexaenoic acid, spirolides, and astaxanthin, GV-971, have demonstrated outstanding activity and bioavailability.

阿尔茨海默氏症的发病率在不断上升,给社会和经济造成了巨大负担。阿兹海默症的发病机制包括神经元氧化损伤、tau 磷酸化、淀粉样蛋白 beta 聚集、神经炎症等。尽管付出了巨大的努力,但目前在对抗疗法系统中还没有有效的治疗或治愈方法。海洋化合物是很有吸引力的选择,具有很强的神经保护作用。从海绵、藻类和海洋无脊椎动物中提取的海洋化合物可用于神经保护,与合成药物相比,其不良反应较少。各种化合物,如白僵菌素-1、二十二碳六烯酸、螺内酯和虾青素 GV-971 等,都已证明具有出色的活性和生物利用度。
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引用次数: 0
期刊
Journal of Asian Natural Products Research
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