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Withanolide derivatives from Physalis angulata var. villosa and their cytotoxic activities 长绒Physalis varululata vlolosa .绒毛中的Withanolide衍生物及其细胞毒活性
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60881-8
Peng Wang , Jue Yang , Yu Zhang , Jun Jin , Meijun Chen , Xiaojiang Hao , Chunmao Yuan , Ping Yi
A comprehensive phytochemical investigation of the leaves and twigs of Physalis angulata. var. villosa resulted in the isolation of 23 withanolide derivatives, including one novel 13,20-γ-lactone withanolide derivative (1) and three new withanolide derivatives (24). Architecturally, physalinin A (1) represents the first identified type B withanolide featuring a 13,20-γ-lactone moiety. The molecular structures of all isolates were elucidated using an integrated approach combining nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry (MS), infrared (IR) spectroscopy, and quantum chemical calculations to confirm structural assignments. The antiproliferative activities of all isolated withanolides were evaluated against four human cancer cell lines (HEL, HCT-116, Colo320DM, and MDA-MB-231). Among them, eight derivatives (2, 58, 14, 15, and 23) exhibited significant inhibitory effects, with half-maximal inhibitory concentration (IC50) values of 0.18 ± 0.03 to 17.02 ± 0.21 μmol·L−1. Structure-activity relationship (SAR) analysis suggested that the presence of an epoxide ring enhances anticancer activity, potentially through increased reactivity or specific interactions with molecular targets involved in cancer progression. These findings underscore the pharmacological potential of withanolides as promising lead compounds for the development of novel anticancer therapeutics.
角Physalis angulata叶片和细枝的植物化学研究。从Var. villosa中分离得到23个withanolide衍生物,包括1个新的13,20-γ-内酯withanolide衍生物(1)和3个新的withanolide衍生物(2−4)。在结构上,physalinin A(1)代表了第一个被鉴定的B型withanolide,具有13,20-γ-内酯片段。采用核磁共振(NMR)、质谱(MS)、红外(IR)光谱和量子化学计算相结合的方法对所有分离物的分子结构进行了鉴定。对提取的四种人癌细胞(HEL、HCT-116、Colo320DM和MDA-MB-231)的抗增殖活性进行了评价。其中,8个衍生物(2、5-8、14、15和23)表现出显著的抑制作用,半数最大抑制浓度(IC50)值为0.18±0.03 ~ 17.02±0.21 μmol·L−1。构效关系(SAR)分析表明,环氧环的存在增强了抗癌活性,可能是通过增加反应性或与参与癌症进展的分子靶点的特异性相互作用。这些发现强调了作为开发新型抗癌治疗药物的先导化合物的药物潜力。
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引用次数: 0
Deciphering the therapeutic potential and mechanisms of Artemisia argyit essential oil on flagellum-mediated Salmonella infections 解读艾叶精油对鞭毛介导的沙门氏菌感染的治疗潜力和机制
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60890-9
Linlin Ding , Lei Xu , Na Hu , Jianfeng Wang , Jiazhang Qiu , Qingjie Li , Xuming Deng
Salmonellosis represents a global epidemic, and the emergence of extensively drug-resistant (XDR) Salmonella and its sustained transmission worldwide constitutes a significant public health concern. Flagellum-mediated motility serves as a crucial virulence trait of Salmonella that guides the pathogen toward the epithelial surface, enhancing gut colonization. Artemisia argyit essential oil, a traditional herb extract, demonstrates efficacy in treating inflammation-related symptoms and diseases; however, its effects on flagellum assembly and expression mechanisms in anti-Salmonella activity remain inadequately explored. This study aimed to elucidate the mechanism by which Artemisia argyit essential oil addresses Salmonella infections. Network pharmacological analysis revealed that Traditional Chinese Medicine (TCM) Artemisia argyit exhibited anti-Salmonella infection potential and inhibited flagellum-dependent motility. The application of Artemisia argyit essential oil induced notable motility defects through the downregulation of flagellar and fimbriae expression. Moreover, it significantly reduced Salmonella-infected cell damage by interfering with flagellum-mediated Salmonella colonization. In vivo studies demonstrated that Artemisia argyit essential oil administration effectively alleviated Salmonella infection symptoms by reducing bacterial loads, inhibiting interleukin-1 beta (IL-1β), IL-6, and tumor necrosis factor-alpha (TNF-α) production, and diminishing pathological injury. Gas chromatography-mass spectrometry (GC-MS) analysis identified forty-three compounds in Artemisia argyit essential oil, with their corresponding targets and active ingredients predicted. Investigation of an in vivo model of Salmonella infection using the active ingredient demonstrated that alpha-cedrene ameliorated Salmonella infection. These findings suggest the potential application of Artemisia argyit essential oil in controlling Salmonella, the predominant food-borne pathogen.
沙门氏菌病是一种全球性流行病,广泛耐药沙门氏菌的出现及其在世界范围内的持续传播构成了一个重大的公共卫生问题。鞭毛介导的运动性是沙门氏菌的一个重要毒力特征,它引导病原体向上皮表面移动,增强肠道定植。艾叶精油是一种传统的草药提取物,对治疗炎症相关症状和疾病有疗效;然而,其对鞭毛组装的影响及其在抗沙门氏菌活性中的表达机制仍未得到充分探讨。本研究旨在阐明艾叶精油治疗沙门氏菌感染的作用机制。网络药理分析显示,中药艾叶具有抗沙门氏菌感染的潜力,并能抑制鞭毛依赖性运动。艾叶精油通过下调鞭毛和毛的表达诱导了明显的运动性缺陷。此外,它通过干扰鞭毛介导的沙门氏菌定植显著减少沙门氏菌感染的细胞损伤。体内研究表明,艾叶精油通过降低细菌负荷、抑制白细胞介素-1β (IL-1β)、IL-6和肿瘤坏死因子-α (TNF-α)的产生、减轻病理性损伤,有效缓解沙门氏菌感染症状。气相色谱-质谱联用(GC-MS)分析鉴定了艾叶精油中的43种化合物,并预测了它们对应的靶点和有效成分。利用活性成分对沙门氏菌感染的体内模型进行的研究表明,-柏木烯可改善沙门氏菌感染。这些发现提示艾叶精油在控制主要食源性病原菌沙门氏菌方面具有潜在的应用前景。
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引用次数: 0
Bioactivity-guided discovery of antiviral templichalasins A‒C from the endophytic fungus Aspergillus templicola 从内生真菌templicola Aspergillus templichalasins A-C中生物活性导向的抗病毒药物的发现
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60880-6
Teng Cai , Jingzu Sun , Wenxuan Chen , Qiang He , Baosong Chen , Yulong He , Peng Zhang , Yanhong Wei , Hongwei Liu , Xiaofeng Cai
The bioactivity-guided isolation of potentially active natural products has been widely utilized in pharmaceutical discovery. In this study, by screening fungal extracts against coxsackievirus B3 (CVB3), three new aspochalasins, templichalasins A‒C (13), along with six known aspochalasins (49) were isolated from an active extract derived from the endophytic fungus Aspergillus templicola LHWf045. Compound 1 features a unique 5/6/5/7/5 pentacyclic ring system, while compounds 2 and 3 possess unusual 5/6/6/7 tetracyclic skeletons. Their structures were characterized through extensive spectroscopic analyses, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. Additionally, we demonstrated that compound 4 can be readily converted into compounds 13 under mild acidic conditions and proposed a plausible mechanism for this conversion. Bioactivity evaluation of compounds 19 against CVB3 revealed the inhibitory effects of all compounds against the virus. Notably, compound 9 exhibited superior antiviral activity, surpassing the commercial drug ribavirin in selectivity index (SI) value.
生物活性引导分离潜在活性天然产物已广泛应用于药物发现。在本研究中,通过筛选抗柯萨奇病毒B3 (CVB3)的真菌提取物,从内生真菌Aspergillus templicola LHWf045的活性提取物中分离到3个新的aspochalasins, templichalasins A-C(1-3)和6个已知的aspochalasins(4-9)。化合物1具有独特的5/6/5/7/5五环体系,而化合物2和3具有不寻常的5/6/6/7四环骨架。通过广泛的光谱分析、电子圆二色性(ECD)计算和单晶x射线衍射分析对其结构进行了表征。此外,我们证明了化合物4在温和的酸性条件下可以很容易地转化为化合物1-3,并提出了这种转化的合理机制。化合物1 ~ 9对CVB3的生物活性评价表明,所有化合物对病毒均有抑制作用。值得注意的是,化合物9表现出优异的抗病毒活性,其选择性指数(SI)值超过了市售药物利巴韦林。
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引用次数: 0
The potential therapeutic role of ginsenosides on fibrosis-associated diseases: a review on molecular mechanisms and call for further research 人参皂苷对纤维化相关疾病的潜在治疗作用:分子机制综述及进一步研究的展望
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60817-X
Mengguang Wei , Yue Zhang , Xiaomeng Sun , Lianwen Qi , Qun Liu
Fibrosis is characterized as an aberrant reparative process involving the direct replacement of damaged or deceased cells with connective tissue, leading to progressive architectural remodeling across various tissues and organs. This condition imposes a substantial burden, resulting in considerable morbidity and mortality. Ginseng (Panax ginseng C. A. Meyer), renowned for its medicinal properties, has been incorporated as a key component in Chinese patent medicines to mitigate fibrotic diseases. Ginsenosides, the primary bioactive compounds in ginseng, have garnered significant attention. Over the past five years, extensive research has explored the pharmaceutical potential of ginsenosides in diverse organ fibrosis conditions, including liver, myocardial, renal, and pulmonary fibrosis. Studies have elucidated that ginsenosides demonstrate potential effects on inflammatory responses stemming from parenchymal cell damage, myofibroblast activation leading to extracellular matrix (ECM) production, and myofibroblast apoptosis or inactivation. Additionally, potential downstream targets and pathways associated with these pathological processes have been identified as being influenced by ginsenosides. This review presents a comprehensive overview of the efficacious treatments utilizing ginsenosides for various tissue fibrosis types and their potential anti-fibrotic mechanisms. Furthermore, it offers a reference for the development of novel candidate drugs for future organ fibrosis therapies.
纤维化的特征是一种异常的修复过程,涉及结缔组织直接替代受损或死亡的细胞,导致各种组织和器官的进行性建筑重塑。这种情况造成了沉重的负担,导致相当高的发病率和死亡率。人参(Panax Ginseng C. a . Meyer)以其药用特性而闻名,已被纳入中成药的关键成分,以减轻纤维化疾病。人参皂苷作为人参中的主要生物活性物质,受到了广泛的关注。在过去的五年中,广泛的研究已经探索了人参皂苷在不同器官纤维化条件下的药物潜力,包括肝、心肌、肾和肺纤维化。研究表明,人参皂苷对实质细胞损伤、导致细胞外基质(ECM)产生的肌成纤维细胞激活、肌成纤维细胞凋亡或失活等炎症反应有潜在影响。此外,与这些病理过程相关的潜在下游靶点和途径已被确定为受人参皂苷的影响。本文综述了利用人参皂苷治疗各种类型组织纤维化的有效方法及其潜在的抗纤维化机制。为未来器官纤维化治疗的新型候选药物的开发提供参考。
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引用次数: 0
Intervention of natural products targeting novel mechanisms after myocardial infarction 针对心肌梗死新机制的天然产物干预
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60816-8
Guangjie Tai , Renhua Liu , Tian Lin , Jiancheng Yang , Xiaoxue Li , Ming Xu
Myocardial infarction is a cardiovascular disease (CVD) with high morbidity and mortality, which can trigger a cascade of cardiac pathophysiological changes, including fibrosis, inflammation, ischemia-reperfusion injury (IRI), and ventricular remodeling, ultimately leading to heart failure (HF). While conventional pharmacological treatments and clinical reperfusion therapy may enhance short-term prognoses and emergency survival rates, both approaches have limitations and adverse effects. Natural products (NPs) are extensively utilized as therapeutics globally, with some demonstrating potentially favorable therapeutic effects in preclinical and clinical pharmacological studies, positioning them as potential alternatives to modern drugs. This review comprehensively elucidates the pathophysiological mechanisms during myocardial infarction and summarizes the mechanisms by which NPs exert cardiac beneficial effects. These include classical mechanisms such as inhibition of inflammation and oxidative stress, alleviation of cardiomyocyte death, attenuation of cardiac fibrosis, improvement of angiogenesis, and emerging mechanisms such as cardiac metabolic regulation and histone modification. Furthermore, the review emphasizes the modulation by NPs of novel targets or signaling pathways in classical mechanisms, including other forms of regulated cell death (RCD), endothelial-mesenchymal transition, non-coding ribonucleic acids (ncRNAs) cascade, and endothelial progenitor cell (EPC) function. Additionally, NPs influencing a particular mechanism are categorized based on their chemical structure, and their relevance is discussed. Finally, the current limitations and prospects of NPs therapy are considered, highlighting their potential for use in myocardial infarction management and identifying issues that require urgent attention.
心肌梗死是一种高发病率和死亡率的心血管疾病(CVD),可引发一系列心脏病理生理变化,包括纤维化、炎症、缺血再灌注损伤(IRI)和心室重构,最终导致心力衰竭(HF)。虽然传统的药物治疗和临床再灌注治疗可以提高短期预后和急诊生存率,但这两种方法都有局限性和副作用。天然产物(NPs)在全球范围内被广泛用作治疗药物,其中一些在临床前和临床药理学研究中显示出潜在的良好治疗效果,将其定位为现代药物的潜在替代品。本文综述了心肌梗死的病理生理机制,并对NPs对心脏有益作用的机制进行了综述。这些包括经典机制,如抑制炎症和氧化应激,减轻心肌细胞死亡,减轻心脏纤维化,改善血管生成,以及新兴机制,如心脏代谢调节和组蛋白修饰。此外,该综述还强调了NPs在经典机制中对新靶点或信号通路的调节,包括其他形式的细胞死亡调节(RCD)、内皮-间质转化、非编码核糖核酸(ncrna)级联和内皮祖细胞(EPC)功能。此外,影响特定机制的NPs根据其化学结构进行了分类,并讨论了它们的相关性。最后,考虑了NPs治疗目前的局限性和前景,强调了它们在心肌梗死治疗中的应用潜力,并确定了需要紧急关注的问题。
{"title":"Intervention of natural products targeting novel mechanisms after myocardial infarction","authors":"Guangjie Tai ,&nbsp;Renhua Liu ,&nbsp;Tian Lin ,&nbsp;Jiancheng Yang ,&nbsp;Xiaoxue Li ,&nbsp;Ming Xu","doi":"10.1016/S1875-5364(25)60816-8","DOIUrl":"10.1016/S1875-5364(25)60816-8","url":null,"abstract":"<div><div>Myocardial infarction is a cardiovascular disease (CVD) with high morbidity and mortality, which can trigger a cascade of cardiac pathophysiological changes, including fibrosis, inflammation, ischemia-reperfusion injury (IRI), and ventricular remodeling, ultimately leading to heart failure (HF). While conventional pharmacological treatments and clinical reperfusion therapy may enhance short-term prognoses and emergency survival rates, both approaches have limitations and adverse effects. Natural products (NPs) are extensively utilized as therapeutics globally, with some demonstrating potentially favorable therapeutic effects in preclinical and clinical pharmacological studies, positioning them as potential alternatives to modern drugs. This review comprehensively elucidates the pathophysiological mechanisms during myocardial infarction and summarizes the mechanisms by which NPs exert cardiac beneficial effects. These include classical mechanisms such as inhibition of inflammation and oxidative stress, alleviation of cardiomyocyte death, attenuation of cardiac fibrosis, improvement of angiogenesis, and emerging mechanisms such as cardiac metabolic regulation and histone modification. Furthermore, the review emphasizes the modulation by NPs of novel targets or signaling pathways in classical mechanisms, including other forms of regulated cell death (RCD), endothelial-mesenchymal transition, non-coding ribonucleic acids (ncRNAs) cascade, and endothelial progenitor cell (EPC) function. Additionally, NPs influencing a particular mechanism are categorized based on their chemical structure, and their relevance is discussed. Finally, the current limitations and prospects of NPs therapy are considered, highlighting their potential for use in myocardial infarction management and identifying issues that require urgent attention.</div></div>","PeriodicalId":10002,"journal":{"name":"Chinese Journal of Natural Medicines","volume":"23 6","pages":"Pages 658-672"},"PeriodicalIF":4.0,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144331402","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Oroxylin A inhibits UVB-induced non-melanoma skin cancer by regulating XPA degradation Oroxylin A通过调节XPA降解抑制uvb诱导的非黑色素瘤皮肤癌
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60893-4
Renjie Dou , Jiarui Sun , Hang Yang , Yufen Zheng , Kang Yuan , Lei Qiang , Run Ma , Yunyao Liu
Oroxylin A (OA), a natural compound extracted from Scutellaria baicalensis, demonstrates preventive potential against ultraviolet B (UVB)-induced non-melanoma skin cancer (NMSC), the most prevalent cancer worldwide with increasing incidence. Utilizing SKH-1 hairless mice exposed to UVB, this study showed that OA delayed NMSC onset and alleviated acute skin damage. Mechanistic investigations revealed its dual action: inhibiting inflammation and enhancing nucleotide excision repair (NER) by stabilizing XPA, a crucial deoxyribonucleic acid (DNA) repair protein. This stabilization occurred through OA’s interaction with glucose-regulated protein 94 (GRP94), which disrupted murine double minute 2 (MDM2)-mediated XPA ubiquitination and proteasomal degradation. By maintaining XPA levels, OA expedited photoproduct clearance and diminished genomic instability, ultimately impeding NMSC development. These findings suggest OA as a promising chemopreventive agent targeting the GRP94/MDM2-XPA axis to counteract UVB-induced carcinogenesis.
Oroxylin A (OA)是一种从黄芩中提取的天然化合物,对紫外线B (UVB)诱导的非黑色素瘤皮肤癌(NMSC)具有潜在的预防作用,NMSC是世界上最常见的癌症,发病率不断上升。利用暴露于UVB的SKH-1无毛小鼠,本研究表明OA延缓了NMSC的发生并减轻了急性皮肤损伤。机制研究揭示了其双重作用:抑制炎症和通过稳定XPA(一种关键的脱氧核糖核酸(DNA)修复蛋白)来增强核苷酸切除修复(NER)。这种稳定是通过OA与葡萄糖调节蛋白94 (GRP94)的相互作用发生的,这破坏了小鼠双分钟2 (MDM2)介导的XPA泛素化和蛋白酶体降解。通过维持XPA水平,OA加速了光产物清除,减少了基因组不稳定性,最终阻碍了NMSC的发展。这些发现表明OA是一种很有前景的化学预防剂,可以靶向GRP94/MDM2-XPA轴来对抗uvb诱导的致癌作用。
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引用次数: 0
Advancements and applications in radiopharmaceutical therapy 放射性药物治疗的进展与应用
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60887-9
Shiya Wang , Mingyi Cao , Yifei Chen , Jingjing Lin , Jiahao Li , Xinyu Wu , Zhiyue Dai , Yuhan Pan , Xiao Liu , Xian Liu , Liang-Ting Lin , Jianbing Wu , Ji Liu , Qifeng Zhong , Zhenwei Yuan
Radiopharmaceuticals operate by combining radionuclides with carriers. The radiation energy emitted by radionuclides is utilized to selectively irradiate diseased tissues while minimizing damage to healthy tissues. In comparison to external beam radiation therapy, radionuclide drugs demonstrate research potential due to their biological targeting capabilities and reduced normal tissue toxicity. This article reviews the applications and research progress of radiopharmaceuticals in cancer treatment. Several key radionuclides are examined, including 223Ra, 90Y, Lutetium-177 (177Lu), 212Pb, and Actinium-225 (225Ac). It also explores the current development trends of radiopharmaceuticals, encompassing the introduction of novel radionuclides, advancements in imaging technologies, integrated diagnosis and treatment approaches, and equipment-medication combinations. We review the progress in the development of new treatments, such as neutron capture therapy, proton therapy, and heavy ion therapy. Furthermore, we examine the challenges and breakthroughs associated with the clinical translation of radiopharmaceuticals and provide recommendations for the research and development of novel radionuclide drugs.
放射性药物通过将放射性核素与载体结合而起作用。利用放射性核素发射的辐射能选择性地照射病变组织,同时尽量减少对健康组织的损害。与外束放射治疗相比,放射性核素药物由于其生物靶向能力和降低正常组织毒性而显示出研究潜力。本文综述了放射性药物在肿瘤治疗中的应用及研究进展。几个关键的放射性核素被检查,包括223Ra, 90Y,镥-177 (177Lu), 212Pb和锕-225 (225Ac)。它还探讨了当前放射性药物的发展趋势,包括新的放射性核素的引入,成像技术的进步,综合诊断和治疗方法,以及设备-药物组合。本文综述了中子俘获治疗、质子治疗和重离子治疗等新型治疗方法的研究进展。此外,我们还分析了与放射性药物临床转化相关的挑战和突破,并对新型放射性核素药物的研究和开发提出了建议。
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引用次数: 0
Harmonizing tradition and technology: Liposomal nanocarriers unlocking the power of natural herbs in Traditional Chinese Medicine 调和传统与技术:脂质体纳米载体释放天然中药的力量
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60889-2
Ibrahim Shaw , Aaron Albert Aryee , Yimer Seid Ali , George Frimpong Boafo , Jingjing Tian , Ronald Mlambo , Songwen Tan , Chuanpin Chen
Natural herbs demonstrate significant therapeutic potential in managing chronic and complex diseases; however, their clinical application faces limitations due to low bioavailability, instability, toxicity, and herb-drug interactions. Furthermore, insufficient standardized evidence and global acceptance impede their widespread adoption. Liposomes, nanocarriers consisting of a phospholipid bilayer enclosing an aqueous core, present a promising approach for enhancing the pharmacokinetics and therapeutic efficacy of herbal compounds. These adaptable systems can encapsulate both hydrophilic and hydrophobic agents, enabling targeted drug delivery and enhanced stability. Moreover, liposomes can be modified to carry diagnostic and imaging agents, enabling precise disease detection and monitoring. While liposomes offer potential as an innovative delivery technology for herbal remedies, their application in Traditional Chinese Medicine (TCM) remains relatively unexplored. TCM, with its holistic, energy-based approach to health and organ function, presents distinct challenges regarding formulation and delivery. This review examines the therapeutic potential of herbal medicines, emphasizing how liposomes address delivery challenges within the TCM framework. It also investigates the integration of TCM with Western medical practices, demonstrating how liposomal systems may bridge these approaches. The review analyzes key formulation techniques for TCM-loaded liposomes, particularly the microfluidic method, which demonstrates superior control over particle size and encapsulation efficiency compared to conventional methods. The analysis addresses barriers to integrating liposomal delivery systems with TCM, including physicochemical properties, scalability issues, and regulatory challenges. Finally, this review provides strategic recommendations for overcoming these obstacles and identifies future research directions to maximize the potential of liposomal technology in enhancing TCM therapies.
天然草药在治疗慢性和复杂疾病方面显示出巨大的治疗潜力;然而,由于低生物利用度、不稳定性、毒性和草药相互作用,它们的临床应用面临限制。此外,缺乏标准化证据和全球接受程度阻碍了它们的广泛采用。脂质体是一种由包裹水核的磷脂双分子层组成的纳米载体,是一种很有前途的提高草药化合物药代动力学和治疗效果的方法。这些适应性强的系统可以封装亲水性和疏水性试剂,从而实现靶向药物递送和增强稳定性。此外,脂质体可以被修饰以携带诊断和显像剂,从而实现精确的疾病检测和监测。虽然脂质体作为一种创新的给药技术具有潜力,但它们在中药中的应用仍相对未被探索。中医以其整体的、以能量为基础的健康和器官功能方法,在配方和递送方面提出了独特的挑战。这篇综述探讨了草药的治疗潜力,强调了脂质体如何在中医框架内解决递送挑战。它还研究了中医与西方医学实践的整合,展示了脂质体系统如何连接这些方法。本文分析了中药脂质体的关键配方技术,特别是微流控法,与传统方法相比,微流控法在粒径和包封效率方面具有优越的控制能力。该分析解决了将脂质体递送系统与中药整合的障碍,包括物理化学性质、可扩展性问题和监管挑战。最后,本文提出了克服这些障碍的策略建议,并确定了未来的研究方向,以最大限度地发挥脂质体技术在中医治疗中的潜力。
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引用次数: 0
Diphenylemestrins A−E: diketopiperazine-diphenyl ether hybrids from Aspergillus nidulans Diphenylemestrins A−E:双酮哌嗪-二苯醚杂交种
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60891-0
Aimin Fu , Qin Li , Yang Xiao , Jiaxin Dong, Yuanyang Peng, Yu Chen, Qingyi Tong, Chunmei Chen, Yonghui Zhang, Hucheng Zhu
A chemical investigation of secondary metabolites (SMs) from Aspergillus nidulans resulted in the identification of five novel dioxopiperazine (DKP)-diphenyl ether hybrids, designated as diphenylemestrins A−E (15). These compounds 15 represent the first known dimers combining DKP and diphenyl ether structures, with compound 4 featuring an uncommon dibenzofuran as the diphenyl ether component. The structural elucidation and determination of absolute stereochemistry were accomplished through spectroscopic analysis and electronic circular dichroism (ECD) calculations. Notably, diphenylemestrin C (3) exhibited moderate cytostatic activity against NB4 cells, with a half maximal inhibitory concentration (IC50) value of 21.99 μmol·L−1, and induced apoptosis at higher concentrations.
通过对尼杜曲霉次生代谢产物(SMs)的化学分析,鉴定出5个新的二氧哌嗪(DKP)-二苯基醚杂交种,命名为diphenylemestrins A−E(1−5)。这些化合物1 ~ 5是已知的第一个结合DKP和二苯基醚结构的二聚体,其中化合物4以一种罕见的二苯并呋喃作为二苯基醚组分。通过光谱分析和电子圆二色性(ECD)计算完成了结构解析和绝对立体化学的测定。值得注意的是,二苯甲素C(3)对NB4细胞表现出中等的细胞抑制活性,其半数最大抑制浓度(IC50)值为21.99 μmol·L−1,高浓度时可诱导细胞凋亡。
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引用次数: 0
Combination of Astragalus−Salvia and Ophiopogon−Dendrobium herb pairs alleviates Sjögren’s Syndrome via inhibiting the JAK1/STAT3 and PI3K/AKT pathways in NOD/Ltj mice 黄芪-鼠尾草和麦冬-石斛组合通过抑制NOD/Ltj小鼠的JAK1/STAT3和PI3K/AKT通路减轻Sjögren 's综合征
IF 4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE Pub Date : 2025-06-01 DOI: 10.1016/S1875-5364(25)60892-2
Peng Sun , Lili Zhu , Yang Yu , Sijing Hu , Mengyi Shan , Xuan Zhao , Xinchang Wang , Qiaoyan Zhang , Luping Qin
Sjögren’s syndrome (SS) is an autoimmune disease characterized primarily by oral and periocular dryness. Astragalus-Salvia (AS) and Ophiopogon-Dendrobium (OD) represent two frequently utilized herb pairs in SS treatment. While the combination of AS-OD herb pairs demonstrates clinical efficacy in alleviating SS symptoms, its underlying mechanism remains unclear. This investigation sought to assess the therapeutic effects and elucidate the potential mechanisms of AS-OD in non-obese diabetic (NOD)/Ltj mice with SS. The study utilized NOD/Ltj mice as SS models, administering AS-OD treatment for 10 weeks at doses of 113.1, 226.2, and 339.3 mg·d−1·20 g−1. Results demonstrated that AS-OD improved SS symptoms, evidenced by enhanced salivary flow rate, decreased anti-SSA/Ro and anti-SSB/La antibody levels, increased swimming duration, and reduced lactate (LA) and blood urea nitrogen (BUN) levels in NOD/Ltj mice. AS-OD reduced lymphocyte infiltration, enhanced Aquaporin-5 (AQP5) expression in the submandibular gland, decreased inflammatory cytokine levels in the submandibular gland, and reduced the T helper type 17/regulatory T lymphocyte (Th17/Treg) cell ratio in the spleen. Transcriptomic and proteomic analyses indicated AS-OD’s involvement in regulating phosphatidylinositol-3-kinase/protein kinase B (PI3K/AKT) and Janus kinase 3/signal transducer and activator of transcription 3 (JAK1/STAT3) pathways, with inhibitory effects validated in both NOD/Ltj mice submandibular gland and A-253 cells. Furthermore, AS-OD enhanced cell viability and reduced A-253 cell apoptosis through the PI3K/AKT pathway. In A-253 cells, AS-OD reduced inflammatory cytokine levels, CXC chemokine ligand 9/10 (CXCL9/10), and T-cell chemotaxis by inhibiting the JAK1/STAT3 pathway. AS-OD mitigates SS by suppressing inflammation and immune responses through the PI3K/AKT and JAK1/STAT3 pathways.
Sjögren综合征(SS)是一种以口腔和眼周干燥为主要特征的自身免疫性疾病。黄芪-鼠尾草(AS)和麦冬-石斛(OD)是SS治疗中常用的两对草本植物。虽然AS-OD中药组合在缓解SS症状方面具有临床疗效,但其潜在机制尚不清楚。本研究旨在评估as - od对患有SS的非肥胖糖尿病(NOD)/Ltj小鼠的治疗效果,并阐明其潜在机制。本研究以NOD/Ltj小鼠作为SS模型,分别以113.1、226.2和339.3 mg·d - 1·20 g - 1剂量给予as - od治疗10周。结果表明,AS-OD改善了NOD/Ltj小鼠的SS症状,表现为唾液流速增加,抗ssa /Ro和抗ssb /La抗体水平降低,游泳时间延长,乳酸(La)和血尿素氮(BUN)水平降低。AS-OD可减少淋巴细胞浸润,增强颌下腺水通道蛋白-5 (AQP5)表达,降低颌下腺炎性细胞因子水平,降低脾脏T辅助型17/调节性T淋巴细胞(Th17/Treg)细胞比例。转录组学和蛋白质组学分析表明,AS-OD参与调节磷脂酰肌醇-3激酶/蛋白激酶B (PI3K/AKT)和Janus激酶3/信号转导和转录激活因子3 (JAK1/STAT3)通路,在NOD/Ltj小鼠颌下腺和A-253细胞中均有抑制作用。此外,AS-OD通过PI3K/AKT通路增强细胞活力,减少A-253细胞凋亡。在A-253细胞中,AS-OD通过抑制JAK1/STAT3通路降低炎症细胞因子水平、CXC趋化因子配体9/10 (CXCL9/10)和t细胞趋化性。AS-OD通过PI3K/AKT和JAK1/STAT3通路抑制炎症和免疫反应,从而减轻SS。
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Chinese Journal of Natural Medicines
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