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Harnessing traditional chinese medicine for wound healing and modern wound models: An overview 中医药治疗创面愈合与现代创面模型:综述
Pub Date : 2025-09-01 Epub Date: 2025-07-23 DOI: 10.1016/j.prmcm.2025.100664
Vishwjeet Singh , Singh Khushbu Ravindranath , Harishchandra Verma , Shivang Shukla , Anjali Rai , Tejas Patani , Triveni Mishra , Anuradha Mishra , Ramesh Kumar Gupta

Introduction

This study delves into the intricate dynamics of wound healing, emphasizing the critical role of various wound healing models in advancing therapeutic interventions and the use of various Chinese medicines used in wound treatment. These models, ranging from abrasions to incision and dead space wound models, provide invaluable insights into chronic wounds like venous leg ulcers and diabetic foot ulcers.

Methods

A systematic literature search was conducted using PubMed, Scopus, Web of Science, and Google Scholar to identify studies published between 1994 and 2023 on the use of Traditional Chinese Medicines (TCMs) in wound healing. A total of 196 articles were retrieved, of which 161 were selected based on relevance, experimental evidence, and mechanistic insights. The review emphasizes TCM-based formulations evaluated in in vivo, in vitro, and preclinical models, with a focus on their therapeutic roles and underlying molecular pathways in skin repair and regeneration.

Results

Animal models, despite not perfectly replicating human chronic wounds, have been instrumental in studying wound healing mechanisms, particularly the inflammatory phase and factors like bacterial biofilms. The exploration of apoptosis and extracellular matrix alterations within these models sheds light on crucial cellular and molecular events essential for wound closure. Additionally, the article discusses models for burn wounds, skin aging, blister wounds, and back punch wounds, highlighting their significance in understanding wound pathophysiology and testing treatment efficacy. Furthermore, traditional remedies like Shiunko and Wuwei Xiaodu Yin are explored for their therapeutic properties in promoting granulation tissue formation, wound healing, and anti-inflammatory effects.

Conclusion

Overall, the study underscores the importance of these diverse wound healing models in unraveling the complexities of tissue repair and guiding the development of effective treatments for various types of wounds using Chinese medicine.

Significance statement

This article highlights the critical role of diverse wound healing models in advancing therapeutic interventions, particularly in studying chronic wounds and evaluating the efficacy of Chinese medicinal plant-based treatments. This study provides insights into wound pathophysiology, inflammation, and tissue repair mechanisms by analyzing various models, including burns, abrasions, and incisions, emphasizing the potential of traditional remedies like Shiunko and Wuwei Xiaodu Yin in promoting wound healing.
本研究深入探讨了伤口愈合的复杂动力学,强调了各种伤口愈合模型在推进治疗干预和各种中药在伤口治疗中的应用中的关键作用。这些模型,从擦伤到切口和死腔伤口模型,为静脉性腿部溃疡和糖尿病足溃疡等慢性伤口提供了宝贵的见解。方法采用PubMed、Scopus、Web of Science、b谷歌Scholar等数据库系统检索1994 ~ 2023年发表的有关中药在创面愈合中的应用的文献。共检索了196篇文章,其中161篇是根据相关性、实验证据和机制见解选择的。这篇综述强调了基于中药的制剂在体内、体外和临床前模型中的评估,重点是它们在皮肤修复和再生中的治疗作用和潜在的分子途径。结果尽管动物模型不能完美地复制人类慢性伤口,但在研究伤口愈合机制,特别是炎症期和细菌生物膜等因素方面具有重要意义。在这些模型中对细胞凋亡和细胞外基质改变的探索揭示了伤口愈合所必需的关键细胞和分子事件。此外,本文还讨论了烧伤创面、皮肤老化创面、水疱创面和背击创面的模型,强调了它们对了解创面病理生理和检验治疗效果的意义。此外,传统的药物如熏子和五味消毒饮在促进肉芽组织形成、伤口愈合和抗炎作用方面的治疗特性也被探索出来。总之,本研究强调了这些不同的伤口愈合模型在揭示组织修复的复杂性和指导开发有效的中药治疗各种类型伤口方面的重要性。本文强调了不同的伤口愈合模式在推进治疗干预方面的关键作用,特别是在研究慢性伤口和评估中药植物治疗的疗效方面。本研究通过对烧伤、擦伤、切口等多种模型的分析,对创面病理生理、炎症及组织修复机制进行了深入的研究,并强调了熏子、五味消毒饮等传统疗法在促进创面愈合方面的潜力。
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引用次数: 0
Aqueous extract of Hibiscus sabdariffa calyces offers neuroprotection against unpredictable chronic mild stress-induced neurobehavioral disorders and biochemical perturbations in male Swiss mice 芙蓉花萼水提物对瑞士雄性小鼠的慢性轻度应激性神经行为障碍和生化扰动具有神经保护作用
Pub Date : 2025-09-01 Epub Date: 2025-07-26 DOI: 10.1016/j.prmcm.2025.100665
Valiant Orodeh Adeoye , Abayomi Mayowa Ajayi , Peter Oghenebrorhie Orodeh , Joseph Chimezie , Love Enebeli , Paul Ademola Adeleke , Olatunde Owoeye , Solomon Umukoro

Introduction

Hibiscus sabdariffa (commonly known as roselle or Chinese rose tea) is widely known for its soothing effects, particularly during prolonged stress. In Traditional Chinese Medicine (TCM), it is valued for its therapeutic benefits, including antihypertensive, anti-inflammatory, and hepatoprotective effects. This study explores the neuroprotective potential of the aqueous extract of H. sabdariffa calyces (AEHS) in mitigating stress-induced neurobehavioral and biochemical changes in mice subjected to unpredictable chronic mild stress (UCMS).

Methods

Thirty male Swiss mice were randomly assigned to five groups (n = 6) and treated orally. Groups 1 (control) and 2 (UCMS-control) received distilled water, whereas group 3–5 received AEHS at doses of 50, 100, and 200 mg/kg, respectively. Group 2–5 were subjected to unpredictable chronic mild stress (UCMS) daily for 21 days. The neurobehavioral assessments including locomotor activity, memory, anxiety and depressive-like behaviors conducted on days 20 and 21. On day 22, blood glucose and serum corticosterone levels were analyzed alongside oxidative stress biomarkers, nitrites, pro-inflammatory cytokines (tumor necrosis factor-alpha and interleukin-6), and serotonin levels in the prefrontal cortex, amygdala, and hippocampus. The brain-derived neurotrophic factor (BDNF), nuclear factor kappa B (NF-κB), cyclic adenosine monophosphate (cAMP)-response element binding protein (CREB), and nuclear factor erythroid 2-related factor 2 (Nrf2) were evaluated. The enzymatic activities of acetylcholinesterase (AChE) and glutamic acid decarboxylase (GAD) as well as the histomorphological changes in the brain regions were also assessed.

Results

AEHS effectively modulated UCMS-induced neurobehavioral disorders, along with elevated blood glucose and plasma corticosterone levels. The extract mitigated UCMS-induced increases in malondialdehyde (MDA), nitrites, pro-inflammatory cytokines, NF-κB, and AChE. Additionally, AEHS restored the diminished levels of glutathione, catalase, superoxide dismutase, CREB, BDNF, Nrf2, serotonin, and GAD activity within the brain regions. Furthermore, AEHS ameliorated UCMS-induced histomorphological alterations in the brain.

Discussion/Conclusion

This study demonstrated that AEHS confers neuroprotection against chronic stress-induced neurobehavioral disorders, biochemical and histomorphological alterations by enhancing antioxidant defenses and modulating key signaling pathways, including BDNF, CREB, Nrf2 and NF-κB. These findings underscore the potential therapeutic applications of AEHS in mitigating chronic stress-related psychiatric disturbances within the framework of TCM.
芙蓉花茶(俗称玫瑰花茶或中国玫瑰花茶)因其舒缓作用而广为人知,特别是在长时间的压力下。在传统中医(TCM)中,它因其治疗益处而受到重视,包括抗高血压、抗炎和保护肝脏的作用。本研究探讨了沙达尼花萼水提物(AEHS)在缓解不可预测的慢性轻度应激(UCMS)小鼠应激诱导的神经行为和生化变化中的神经保护作用。方法30只雄性瑞士小鼠随机分为5组(n = 6),均给予口服治疗。1组(对照组)和2组(ucms -对照组)给予蒸馏水,3-5组分别给予剂量为50、100和200 mg/kg的AEHS。2 ~ 5组每天进行不可预测的慢性轻度应激(UCMS),持续21 d。在第20天和第21天进行神经行为评估,包括运动活动、记忆、焦虑和抑郁样行为。第22天,分析血糖和血清皮质酮水平以及氧化应激生物标志物、亚硝酸盐、促炎细胞因子(肿瘤坏死因子- α和白细胞介素-6)和前额皮质、杏仁核和海马中的血清素水平。检测脑源性神经营养因子(BDNF)、核因子κB (NF-κB)、环磷酸腺苷(cAMP)反应因子结合蛋白(CREB)、核因子红细胞2相关因子2 (Nrf2)。测定大鼠脑区乙酰胆碱酯酶(AChE)和谷氨酸脱羧酶(GAD)活性及组织形态学变化。结果saehs可有效调节ucms诱导的神经行为障碍,并可提高血糖和血浆皮质酮水平。该提取物减轻了ucms诱导的丙二醛(MDA)、亚硝酸盐、促炎细胞因子、NF-κB和AChE的升高。此外,AEHS恢复了大脑区域内谷胱甘肽、过氧化氢酶、超氧化物歧化酶、CREB、BDNF、Nrf2、血清素和广泛性焦虑症活性的降低水平。此外,AEHS改善了ucms诱导的脑组织形态学改变。讨论/结论本研究表明,AEHS通过增强抗氧化防御和调节BDNF、CREB、Nrf2和NF-κB等关键信号通路,对慢性应激性神经行为障碍、生化和组织形态学改变具有神经保护作用。这些发现强调了AEHS在中医框架内缓解慢性应激相关精神障碍方面的潜在治疗应用。
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引用次数: 0
Progress in the application of AI in the standardization of traditional Chinese medicine: A review based on machine learning and deep learning 人工智能在中医药标准化中的应用进展:基于机器学习和深度学习的综述
Pub Date : 2025-09-01 Epub Date: 2025-06-26 DOI: 10.1016/j.prmcm.2025.100639
Xianglong Meng , Yijing Lang , Xiaofen Li , Yuting Li , Zhulin Bu , Yuhui Wu , Shuosheng Zhang

Introduction

The Fourth Industrial Revolution, propelled by advancements in the internet, big data, robotics, and artificial intelligence (AI), has not only accelerated technological progress but also heralded a new era of intelligent healthcare. Nowadays, traditional Chinese medicine (TCM) is moving towards the road of intelligent transformation, in which the urgency of integrating the advanced insights of modern medicine is becoming more and more obvious. At the same time, with the full use of various types of artificial intelligence technology, to explore the potential of Chinese medicine, prompting it to embark on a standardized development track, in order to let the ancient Chinese medicine in the wave of modern science and technology renewed new life.

Methods

Through a systematic exploration utilizing keywords such as “AI”, “TCM”, and “Standardization”, we conducted an extensive search across major repositories including Web of Science, PubMed, CNKI, and other databases, analyzing approximately 1000 scholarly works. We strive to deepen our understanding of TCM while fully exploiting the integration potential of AI and TCM, and to effectively promote TCM to make great strides towards more scientific, standardized and efficient standardization.

Results

This review explores six critical areas where AI techniques such as machine learning (ML) and deep learning (DL) contribute: disease diagnosis, prevention and treatment, herbal medicine quality evaluation, pharmacokinetics, mechanisms of action, and non-drug therapy. Examples include: using ML to predict disease outcomes; modeling pharmacokinetics using DL; and using AI techniques to assess the quality grade of herbal medicines etc.. It examines the systemic responses driven by complex interactions between internal and environmental factors during disease progression, grounded in fundamental human biology. Through rigorous high-throughput screening and analysis, this review elucidates intricate biological interaction networks and achieves comprehensive holistic regulation, thereby furthering the standardization of Traditional Chinese Medicine.

Conclusion

This review explores the complex dimensions of TCM using cutting-edge AI techniques to provide strategic guidance for promoting standardization and evolutionary development in the field.
在互联网、大数据、机器人技术和人工智能(AI)的推动下,第四次工业革命不仅加速了技术进步,而且预示着智能医疗的新时代。如今,中医药正走向智能化转型之路,融合现代医学先进见解的迫切性越来越明显。同时,充分利用各类人工智能技术,挖掘中医的潜力,促使其走上规范化发展轨道,以让古老的中医在现代科技浪潮中焕发新生命。方法采用“人工智能”、“中医”、“标准化”等关键词,对Web of Science、PubMed、CNKI等主要数据库进行了广泛的检索,分析了约1000篇学术著作。我们努力深化对中医的认识,充分挖掘人工智能与中医药的融合潜力,切实推动中医药朝着科学化、规范化、高效化方向大步迈进。本综述探讨了人工智能技术(如机器学习(ML)和深度学习(DL))在疾病诊断、预防和治疗、草药质量评价、药代动力学、作用机制和非药物治疗等六个关键领域的贡献。示例包括:使用ML预测疾病结果;用DL建立药代动力学模型;利用人工智能技术评估中草药的质量等级等。它检查了疾病进展过程中由内部和环境因素之间复杂相互作用驱动的系统反应,以基本的人类生物学为基础。通过严格的高通量筛选和分析,阐明复杂的生物相互作用网络,实现全面的整体调控,从而进一步促进中医药规范化。结论运用尖端人工智能技术对中医复杂维度进行探索,为促进该领域规范化和进化发展提供战略指导。
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引用次数: 0
Network pharmacology-based toxicity, molecular docking, and molecular dynamics analysis of phytoconstituents from roots of Nerium indicum L 基于网络药理学的苦楝根成分毒性、分子对接及分子动力学分析
Pub Date : 2025-09-01 Epub Date: 2025-06-07 DOI: 10.1016/j.prmcm.2025.100640
Veerkumar P. Japti , Mrityunjaya B. Patil , Banappa S. Unger , Shamanand P. Mallapur , Akshay Shamnewadi , Vishal S. Patil , Sathgowda Patil , Anand V. Desai

Background

Herbal medicine plays a vital role in healthcare, but safety concerns arise due to potential toxicity risks. Nerium indicum (夹竹桃, jiā zhú táo) is used in Chinese herbal medicine for its therapeutic effects, yet it contains toxic cardiac glycosides. This study investigates its toxicity mechanisms using systems biology tools to support safer applications through comprehensive risk-benefit evaluation and detoxification strategies.

Methods

Computational analyses were performed to predict drug-likeness, toxicity, LD₅₀, and blood-brain barrier (BBB) penetration. Key toxicity-related genes were identified using SwissTargetPrediction and GeneCards. Gene Ontology (GO) and pathway enrichment analyses further explored toxicity mechanisms, while molecular docking and dynamics simulations assessed interactions between core targets, Prostaglandin-endoperoxide synthase 2 (PTGS2) and Mitogen-Activated Protein Kinase 1 (MAPK1), offering deeper insights into toxicity modulation.

Results

Computational analyses identified oleandrin, and odoroside A as highly toxic, with significant cardiotoxic and hepatotoxic risks. Network analysis revealed PTGS2 and MAPK1 as key toxicity regulators, mediating pathways linked to inflammation and cellular stress. Molecular docking showed Oleandrin exhibiting the strongest binding affinities with PTGS2 (-8.5 kcal/mol) and MAPK1 (-9.2 kcal/mol), while molecular dynamics simulations confirmed its stable interactions, suggesting a critical role in toxicity modulation.

Conclusion

This study highlights Oleandrin and related compounds as major toxicity contributors in N. indicum, emphasizing their impact on cardiac, hepatic, and neurological pathways. The findings underscore the need for cautious therapeutic use and potential detoxification strategies for safer applications.
草药在医疗保健中起着至关重要的作用,但由于潜在的毒性风险,安全性问题也引起了关注。凤仙花(zhú táo)因其治疗作用而被用作中草药,但它含有有毒的心脏苷。本研究使用系统生物学工具研究其毒性机制,通过综合风险-效益评估和解毒策略来支持更安全的应用。方法进行计算分析以预测药物相似性,毒性,LD₅0和血脑屏障(BBB)渗透。使用SwissTargetPrediction和GeneCards鉴定关键毒性相关基因。基因本体(GO)和途径富集分析进一步探索了毒性机制,而分子对接和动力学模拟评估了核心靶点前列腺素内过氧化物合成酶2 (PTGS2)和丝裂原活化蛋白激酶1 (MAPK1)之间的相互作用,为毒性调节提供了更深入的了解。结果计算分析确定夹竹桃苷和气味苷A具有高毒性,具有显著的心脏毒性和肝毒性风险。网络分析显示PTGS2和MAPK1是关键的毒性调节因子,介导与炎症和细胞应激相关的途径。分子对接表明,夹竹桃苷与PTGS2 (-8.5 kcal/mol)和MAPK1 (-9.2 kcal/mol)的结合亲和性最强,分子动力学模拟证实了其稳定的相互作用,表明夹竹桃苷在毒性调节中起关键作用。结论夹竹桃素及其相关化合物是夹竹桃的主要毒性来源,并对心脏、肝脏和神经通路产生影响。研究结果强调需要谨慎的治疗使用和潜在的更安全的应用解毒策略。
{"title":"Network pharmacology-based toxicity, molecular docking, and molecular dynamics analysis of phytoconstituents from roots of Nerium indicum L","authors":"Veerkumar P. Japti ,&nbsp;Mrityunjaya B. Patil ,&nbsp;Banappa S. Unger ,&nbsp;Shamanand P. Mallapur ,&nbsp;Akshay Shamnewadi ,&nbsp;Vishal S. Patil ,&nbsp;Sathgowda Patil ,&nbsp;Anand V. Desai","doi":"10.1016/j.prmcm.2025.100640","DOIUrl":"10.1016/j.prmcm.2025.100640","url":null,"abstract":"<div><h3>Background</h3><div>Herbal medicine plays a vital role in healthcare, but safety concerns arise due to potential toxicity risks. <em>Nerium indicum</em> (夹竹桃, jiā zhú táo) is used in Chinese herbal medicine for its therapeutic effects, yet it contains toxic cardiac glycosides. This study investigates its toxicity mechanisms using systems biology tools to support safer applications through comprehensive risk-benefit evaluation and detoxification strategies.</div></div><div><h3>Methods</h3><div>Computational analyses were performed to predict drug-likeness, toxicity, LD₅₀, and blood-brain barrier (BBB) penetration. Key toxicity-related genes were identified using SwissTargetPrediction and GeneCards. Gene Ontology (GO) and pathway enrichment analyses further explored toxicity mechanisms, while molecular docking and dynamics simulations assessed interactions between core targets, Prostaglandin-endoperoxide synthase 2 (PTGS2) and Mitogen-Activated Protein Kinase 1 (MAPK1), offering deeper insights into toxicity modulation.</div></div><div><h3>Results</h3><div>Computational analyses identified oleandrin, and odoroside A as highly toxic, with significant cardiotoxic and hepatotoxic risks. Network analysis revealed PTGS2 and MAPK1 as key toxicity regulators, mediating pathways linked to inflammation and cellular stress. Molecular docking showed Oleandrin exhibiting the strongest binding affinities with PTGS2 (-8.5 kcal/mol) and MAPK1 (-9.2 kcal/mol), while molecular dynamics simulations confirmed its stable interactions, suggesting a critical role in toxicity modulation.</div></div><div><h3>Conclusion</h3><div>This study highlights Oleandrin and related compounds as major toxicity contributors in <em>N. indicum</em>, emphasizing their impact on cardiac, hepatic, and neurological pathways. The findings underscore the need for cautious therapeutic use and potential detoxification strategies for safer applications.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"16 ","pages":"Article 100640"},"PeriodicalIF":0.0,"publicationDate":"2025-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144263754","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Exploring the progress of the traditional Chinese medicine "Duhuo-Qianghuo" in targeting the PI3K-AKT pathway to alleviate knee osteoarthritis based on bioinformatics 基于生物信息学探索中药“多活强活”靶向PI3K-AKT通路缓解膝关节骨性关节炎的进展
Pub Date : 2025-09-01 Epub Date: 2025-06-06 DOI: 10.1016/j.prmcm.2025.100638
Likang Wang , Minqi Zhu , Rujie Zhuang
<div><h3>Objective</h3><div>This study aims to explore how the traditional Chinese medicine "<em>Du huo-Qiang huo</em>" targets the PI3K-AKT signaling pathway to alleviate knee osteoarthritis using network pharmacology, molecular docking technology, and experimental validation.</div></div><div><h3>Methods</h3><div>Active ingredients and target genes related to "<em>Du huo-Qiang huo</em>" and knee osteoarthritis were retrieved from relevant databases.Overlapping data were used to develop a protein-protein interaction (PPI) network model. Functional enrichment analyses, including Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways, were performed using the DAVID tool. The identification of core active components and target genes was based on their interaction intensity within the PPI network.These identified components and targets were subjected to molecular docking analysis via AutoDockTools-1.5.7.Furthermore, the therapeutic effects of "<em>Du huo-Qiang huo</em>" in reducing cartilage degradation and inhibiting inflammatory responses were assessed using a knee osteoarthritis mouse model.</div></div><div><h3>Results</h3><div>"<em>Du huo-Qiang huo</em>" comprises 65 bioactive components and 622 associated targets. Through the integration of several databases, 5215 target genes related to knee osteoarthritis were identified, among which 304 were shared between datasets. The primary active compounds implicated in the therapeutic effects of "<em>Du huo-Qiang huo</em>" include <em>homostephanoline, xanthoxyletin</em>, a<em>ngelicone</em>, and <em>ostruthin</em>. Critical therapeutic targets encompass tumor necrosis factor (TNF), protein kinase B1 (AKT1), glyceraldehyde-3-phosphate dehydrogenase (GAPDH), interleukin-1β (IL-1β), and albumin (ALB). GO functional enrichment analysis revealed 1231 results, comprising 917 biological processes, 106 cellular components, and 208 molecular functions.KEGG pathway enrichment analysis identified 176 pathways, with the top 20 ranked by P-values and presented in bubble plots. Molecular docking studies demonstrated robust binding affinities between <em>homostephanoline, xanthoxyletin</em>, and targets such as AKT1 and TNF. Additionally, "<em>Du huo-Qiang huo</em>" granules showed partial restorative effects on cartilage damage and a reduction in inflammatory markers.</div></div><div><h3>Conclusion</h3><div>This study offers a preliminary exploration of the mechanisms underlying the therapeutic effects of "<em>Du huo-Qiang huo</em>" in managing knee osteoarthritis. Through an analysis of its diverse components, molecular targets, and related pathways, the findings highlight that pivotal active compounds, such as <em>homostephanoline</em> and <em>xanthoxyletin</em>, engage with critical targets like TNF and AKT1.These molecular interactions modulate the PI3K-AKT signaling pathway, promoting cartilage regeneration and mitigating inflammatory responses,which collectively contribute to its therap
目的通过网络药理学、分子对接技术和实验验证,探讨中药“渡火强活”如何靶向PI3K-AKT信号通路缓解膝关节骨性关节炎。方法从相关数据库中检索“杜活强活”与膝关节骨性关节炎相关的有效成分和靶基因。利用重叠数据建立蛋白-蛋白相互作用(PPI)网络模型。使用DAVID工具进行功能富集分析,包括基因本体(GO)和京都基因与基因组百科全书(KEGG)途径。核心活性成分和靶基因的鉴定是基于它们在PPI网络中的相互作用强度。通过AutoDockTools-1.5.7进行分子对接分析。此外,通过膝关节骨性关节炎小鼠模型,评估了“笃火强活”在减少软骨退化和抑制炎症反应方面的治疗效果。结果“杜火强火”含有65种活性成分,622个伴生靶点。通过多个数据库的整合,共鉴定出5215个与膝关节骨关节炎相关的靶基因,其中304个基因在数据集之间共享。“渡火强火”的主要活性成分包括同stephanolin、xanthoxyletin、angelicone和ostrutin。关键的治疗靶点包括肿瘤坏死因子(TNF)、蛋白激酶B1 (AKT1)、甘油醛-3-磷酸脱氢酶(GAPDH)、白细胞介素-1β (IL-1β)和白蛋白(ALB)。氧化石墨烯功能富集分析揭示了1231个结果,包括917个生物过程、106个细胞组分和208个分子功能。KEGG通路富集分析鉴定出176条通路,其中p值排名前20位,以气泡图表示。分子对接研究表明,同型stephanolin、xanthoxyletin与靶标如AKT1和TNF之间具有很强的结合亲和力。此外,“渡火强活”颗粒对软骨损伤有部分修复作用,炎症标志物减少。结论本研究初步探讨了“笃活强活”治疗膝关节骨性关节炎的作用机制。通过对其多种成分、分子靶点和相关途径的分析,研究结果强调了关键活性化合物,如同stephananoline和xanthoxyletin,与TNF和AKT1等关键靶点相关。这些分子相互作用调节PI3K-AKT信号通路,促进软骨再生,减轻炎症反应,共同促进其治疗膝关节骨关节炎的疗效。
{"title":"Exploring the progress of the traditional Chinese medicine \"Duhuo-Qianghuo\" in targeting the PI3K-AKT pathway to alleviate knee osteoarthritis based on bioinformatics","authors":"Likang Wang ,&nbsp;Minqi Zhu ,&nbsp;Rujie Zhuang","doi":"10.1016/j.prmcm.2025.100638","DOIUrl":"10.1016/j.prmcm.2025.100638","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Objective&lt;/h3&gt;&lt;div&gt;This study aims to explore how the traditional Chinese medicine \"&lt;em&gt;Du huo-Qiang huo&lt;/em&gt;\" targets the PI3K-AKT signaling pathway to alleviate knee osteoarthritis using network pharmacology, molecular docking technology, and experimental validation.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Methods&lt;/h3&gt;&lt;div&gt;Active ingredients and target genes related to \"&lt;em&gt;Du huo-Qiang huo&lt;/em&gt;\" and knee osteoarthritis were retrieved from relevant databases.Overlapping data were used to develop a protein-protein interaction (PPI) network model. Functional enrichment analyses, including Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways, were performed using the DAVID tool. The identification of core active components and target genes was based on their interaction intensity within the PPI network.These identified components and targets were subjected to molecular docking analysis via AutoDockTools-1.5.7.Furthermore, the therapeutic effects of \"&lt;em&gt;Du huo-Qiang huo&lt;/em&gt;\" in reducing cartilage degradation and inhibiting inflammatory responses were assessed using a knee osteoarthritis mouse model.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Results&lt;/h3&gt;&lt;div&gt;\"&lt;em&gt;Du huo-Qiang huo&lt;/em&gt;\" comprises 65 bioactive components and 622 associated targets. Through the integration of several databases, 5215 target genes related to knee osteoarthritis were identified, among which 304 were shared between datasets. The primary active compounds implicated in the therapeutic effects of \"&lt;em&gt;Du huo-Qiang huo&lt;/em&gt;\" include &lt;em&gt;homostephanoline, xanthoxyletin&lt;/em&gt;, a&lt;em&gt;ngelicone&lt;/em&gt;, and &lt;em&gt;ostruthin&lt;/em&gt;. Critical therapeutic targets encompass tumor necrosis factor (TNF), protein kinase B1 (AKT1), glyceraldehyde-3-phosphate dehydrogenase (GAPDH), interleukin-1β (IL-1β), and albumin (ALB). GO functional enrichment analysis revealed 1231 results, comprising 917 biological processes, 106 cellular components, and 208 molecular functions.KEGG pathway enrichment analysis identified 176 pathways, with the top 20 ranked by P-values and presented in bubble plots. Molecular docking studies demonstrated robust binding affinities between &lt;em&gt;homostephanoline, xanthoxyletin&lt;/em&gt;, and targets such as AKT1 and TNF. Additionally, \"&lt;em&gt;Du huo-Qiang huo&lt;/em&gt;\" granules showed partial restorative effects on cartilage damage and a reduction in inflammatory markers.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Conclusion&lt;/h3&gt;&lt;div&gt;This study offers a preliminary exploration of the mechanisms underlying the therapeutic effects of \"&lt;em&gt;Du huo-Qiang huo&lt;/em&gt;\" in managing knee osteoarthritis. Through an analysis of its diverse components, molecular targets, and related pathways, the findings highlight that pivotal active compounds, such as &lt;em&gt;homostephanoline&lt;/em&gt; and &lt;em&gt;xanthoxyletin&lt;/em&gt;, engage with critical targets like TNF and AKT1.These molecular interactions modulate the PI3K-AKT signaling pathway, promoting cartilage regeneration and mitigating inflammatory responses,which collectively contribute to its therap","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"16 ","pages":"Article 100638"},"PeriodicalIF":0.0,"publicationDate":"2025-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144263755","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Trypanocidal potentials of Jatropha curcas L. 1753 leaf extracts and fractions in vivo 麻疯树(Jatropha curcas L. 1753)叶提取物及组分体内杀锥虫活性研究
Pub Date : 2025-09-01 Epub Date: 2025-08-27 DOI: 10.1016/j.prmcm.2025.100670
Haolat Yusuf , Abdulhakeem Binhambali , Mutiu Olawale Rahmon , Ridwan Bolaji Yusuf , Suleiman Garba Salihu , Barnabas Jarumi Musa
<div><h3>Introduction</h3><div>Trypanosomiasis is a debilitating parasitic disease affecting both humans and animals, leading to substantial economic losses in the livestock sector due to reduced productivity and increased mortality. As resistance to conventional drugs escalates, interest in plant-based alternatives has grown. <em>Jatropha curcas</em> (JC), widely used in traditional medicine systems including Traditional Chinese Medicine (TCM), has demonstrated promising anti-trypanosomal activity. It is known as mǎfēng shù (麻风树) or “Leprosy Tree’’ in TCM and its varies potential has been widely described in various studies. However, this study specifically evaluated the therapeutic potential of various JC aqueous extracts on weight, body temperature, and parasitaemia levels in <em>Trypanosoma congolense</em>-infected mice.</div></div><div><h3>Methods</h3><div>Ninety mice were randomly assigned to 8 (groups 4–8 have 3 subgroups) experimental groups. Mice in all groups, except the control, were inoculated with <em>Trypanosoma congolense</em> (TC) and treated with Diminazene aceturate (DA) and varying doses of aqueous, methanol, and solvent fractions of JC extracts. Parasitaemia was monitored daily, and blood samples were collected for hematological analysis. Tissue (spleen and liver) were accessed for changes in microscopic examination.</div></div><div><h3>Result</h3><div>The results indicated no statistically significant weight changes between treatment groups (<em>p</em> > 0.05), although slight fluctuations in weight were observed across groups. Similarly, the treatment had minimal effects on body temperature, with no significant differences observed across groups (<em>p</em> > 0.05). On parasitaemia, aqueous extracts at higher doses (of 80 and 40 mg/kg) significantly reduced parasitaemia (<em>p</em> < 0.05) compared to controls, particularly between 2–6 days. Methanol and ethyl acetate extracts also showed significant parasitaemia reduction (<em>p</em> < 0.05), with the 15 mg/kg methanol dose demonstrating the highest efficacy. However, butanol and hexane extracts did not significantly reduce parasitaemia (<em>p</em> > 0.05) and many of the tissues showed different changes on histological analysis.</div></div><div><h3>Conclusion</h3><div>This study demonstrates that JC extracts, particularly aqueous, methanol, and ethyl acetate, exhibit significant anti-trypanosomal activity, by reducing parasitaemia levels in infected mice, likely due to the presence of bioactive phytochemicals such as alkaloids, flavonoids, and saponins. Although the extracts did not completely eliminate the parasites like common drug, however they contributed to improvements in weight, packed cell volume (PCV), red blood cell counts and histological changes, proving their potential therapeutic effects when used appropriately. Also, toxicity concerns, evidenced by the observed histology changes in higher-dose groups, warrant further investigation. The study s
锥虫病是一种影响人类和动物的使人衰弱的寄生虫病,由于生产力下降和死亡率增加,导致畜牧业遭受重大经济损失。随着对传统药物的耐药性不断升级,人们对植物替代品的兴趣也在增长。麻疯树(Jatropha curcas, JC)广泛应用于包括中药在内的传统医学体系中,具有良好的抗锥虫活性。它在中医中被称为mǎfēng shù或“麻风树”,其各种潜力在各种研究中被广泛描述。然而,本研究专门评估了各种JC水提取物对刚果锥虫感染小鼠体重、体温和寄生虫血症水平的治疗潜力。方法90只小鼠随机分为8个实验组(4 ~ 8组共3个亚组)。除对照组外,所有组小鼠均接种刚果锥虫(TC),并用乙酸迪咪那烯(DA)和不同剂量的JC提取物的水、甲醇和溶剂部分处理。每天监测寄生虫血症,并采集血样进行血液学分析。取组织(脾和肝)进行镜下检查。结果各组患者体重差异无统计学意义(p > 0.05),但组间体重有轻微波动。同样,治疗对体温的影响很小,各组间无显著差异(p > 0.05)。在寄生虫血症方面,与对照相比,较高剂量(80和40 mg/kg)的水提取物显著降低了寄生虫血症(p < 0.05),特别是在2-6天之间。甲醇和乙酸乙酯提取物也有显著的降低寄生虫率的作用(p < 0.05),其中甲醇剂量为15 mg/kg时效果最好。然而,丁醇和己烷提取物并没有显著降低寄生虫血症(p > 0.05),许多组织在组织学分析上表现出不同的变化。本研究表明,JC提取物,特别是水、甲醇和乙酸乙酯提取物,通过降低感染小鼠的寄生虫血症水平,表现出显著的抗锥虫活性,可能是由于生物碱、类黄酮和皂苷等生物活性植物化学物质的存在。虽然提取物不能像普通药物那样完全消除寄生虫,但它们有助于改善体重、堆积细胞体积(PCV)、红细胞计数和组织学变化,证明如果使用得当,它们具有潜在的治疗效果。此外,高剂量组观察到的组织学变化证明了毒性问题,值得进一步研究。该研究支持对JC作为潜在的抗锥虫药物的优化配方和给药方案的需求。
{"title":"Trypanocidal potentials of Jatropha curcas L. 1753 leaf extracts and fractions in vivo","authors":"Haolat Yusuf ,&nbsp;Abdulhakeem Binhambali ,&nbsp;Mutiu Olawale Rahmon ,&nbsp;Ridwan Bolaji Yusuf ,&nbsp;Suleiman Garba Salihu ,&nbsp;Barnabas Jarumi Musa","doi":"10.1016/j.prmcm.2025.100670","DOIUrl":"10.1016/j.prmcm.2025.100670","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Introduction&lt;/h3&gt;&lt;div&gt;Trypanosomiasis is a debilitating parasitic disease affecting both humans and animals, leading to substantial economic losses in the livestock sector due to reduced productivity and increased mortality. As resistance to conventional drugs escalates, interest in plant-based alternatives has grown. &lt;em&gt;Jatropha curcas&lt;/em&gt; (JC), widely used in traditional medicine systems including Traditional Chinese Medicine (TCM), has demonstrated promising anti-trypanosomal activity. It is known as mǎfēng shù (麻风树) or “Leprosy Tree’’ in TCM and its varies potential has been widely described in various studies. However, this study specifically evaluated the therapeutic potential of various JC aqueous extracts on weight, body temperature, and parasitaemia levels in &lt;em&gt;Trypanosoma congolense&lt;/em&gt;-infected mice.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Methods&lt;/h3&gt;&lt;div&gt;Ninety mice were randomly assigned to 8 (groups 4–8 have 3 subgroups) experimental groups. Mice in all groups, except the control, were inoculated with &lt;em&gt;Trypanosoma congolense&lt;/em&gt; (TC) and treated with Diminazene aceturate (DA) and varying doses of aqueous, methanol, and solvent fractions of JC extracts. Parasitaemia was monitored daily, and blood samples were collected for hematological analysis. Tissue (spleen and liver) were accessed for changes in microscopic examination.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Result&lt;/h3&gt;&lt;div&gt;The results indicated no statistically significant weight changes between treatment groups (&lt;em&gt;p&lt;/em&gt; &gt; 0.05), although slight fluctuations in weight were observed across groups. Similarly, the treatment had minimal effects on body temperature, with no significant differences observed across groups (&lt;em&gt;p&lt;/em&gt; &gt; 0.05). On parasitaemia, aqueous extracts at higher doses (of 80 and 40 mg/kg) significantly reduced parasitaemia (&lt;em&gt;p&lt;/em&gt; &lt; 0.05) compared to controls, particularly between 2–6 days. Methanol and ethyl acetate extracts also showed significant parasitaemia reduction (&lt;em&gt;p&lt;/em&gt; &lt; 0.05), with the 15 mg/kg methanol dose demonstrating the highest efficacy. However, butanol and hexane extracts did not significantly reduce parasitaemia (&lt;em&gt;p&lt;/em&gt; &gt; 0.05) and many of the tissues showed different changes on histological analysis.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Conclusion&lt;/h3&gt;&lt;div&gt;This study demonstrates that JC extracts, particularly aqueous, methanol, and ethyl acetate, exhibit significant anti-trypanosomal activity, by reducing parasitaemia levels in infected mice, likely due to the presence of bioactive phytochemicals such as alkaloids, flavonoids, and saponins. Although the extracts did not completely eliminate the parasites like common drug, however they contributed to improvements in weight, packed cell volume (PCV), red blood cell counts and histological changes, proving their potential therapeutic effects when used appropriately. Also, toxicity concerns, evidenced by the observed histology changes in higher-dose groups, warrant further investigation. The study s","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"16 ","pages":"Article 100670"},"PeriodicalIF":0.0,"publicationDate":"2025-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144988225","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Mechanism of Tetrastigma hemsleyanum extracts on diabetic retinopathy based on network pharmacology and experimental verification 基于网络药理学和实验验证的红四头草提取物治疗糖尿病视网膜病变的机制
Pub Date : 2025-09-01 Epub Date: 2025-06-14 DOI: 10.1016/j.prmcm.2025.100646
Jie Zhou , Xuan Chen , Baisheng Xu , Xuechun Jiang , Jie Wang , Huan An

Introduction

Diabetic retinopathy (DR) is a prevalent ocular complication of diabetes, with advanced stages potentially leading to blindness. Tetrastigma hemsleyanum (San ye qing, SYQ) has traditionally been employed in addressing ailments such as fever, asthma, hepatitis, infantile febrile seizures, pneumonia, rheumatism, and sore throats. Initial animal studies have suggested that SYQ may significantly curb the progression of DR. This study utilized network pharmacology to explore the mechanism of Tetrastigma hemsleyanum (San ye qing, SYQ) in diabetes retinopathy (DR), with subsequent validation through molecular docking and experiments.

Methods

Male C57BL/6 J mice were applied to establish a type Ⅰ diabetes model. Hemoxylin & eosin staining and western blotting were then used to evaluate the efficacy of SYQ. Databases including Swiss Target Prediction, GeneCards, and DisGeNet were used to filter targets related to DR. The STRING database and Cytoscape software were used to create a protein-protein interaction network. The Metascape database was used to conduct Gene Ontology and Kyoto Encyclopedia of Genes and Genomes pathway enrichment analyses of mutual targets. The active compounds were subjected to molecular docking with core targets using AutoDock software, and the predicted outcomes from network pharmacology were verified in vitro. Tube formation and migration experiments were conducted to evaluate the anti-angiogenic effect and mechanism of SYQ on high glucose-induced EA.hy926 cells.

Results

SYQ demonstrated an inhibitory effect on angiogenesis within the DR model and decreased the expression of proteins related to angiogenesis. Network pharmacology analyses revealed that SYQ targeted 127 proteins, with implications for pathways including the HIF-1 signaling pathway. Molecular docking illuminated that β-sitosterol, Procyanidin-B1, and Emodion-1-O-β-d-glucopyranoside exhibited strong binding affinities with AKT1 core target proteins. In vitro experiments corroborated that SYQ diminished tube formation and migration of EA.hy926 cells under high glucose conditions, in a dose-dependent manner. The pro-angiogenic influence of an AKT1 agonist was counteracted by SYQ. Additionally, administration of SYQ led to reduced expression of p-AKT, HIF-1, and angiogenesis-related proteins, suggesting an inhibitory mechanism via AKT1 against high glucose-induced angiogenesis. These observations confirmed the network pharmacology insights.

Discussion

SYQ emerged as a potential therapeutic agent for DR, primarily by inhibiting angiogenesis. Its anti-angiogenetic effect was mediated via the AKT1/HIF-1/VEGF pathway, indicating a promising avenue for further research and potential clinical application in DR management.
糖尿病视网膜病变(DR)是一种常见的糖尿病眼部并发症,晚期可能导致失明。三叶青传统上被用于治疗发烧、哮喘、肝炎、婴儿热性癫痫、肺炎、风湿病和喉咙痛等疾病。初步的动物研究表明SYQ可能显著抑制DR的进展。本研究利用网络药理学方法探讨了Tetrastigma hemsleyanum(三叶清,SYQ)在糖尿病视网膜病变(DR)中的作用机制,并通过分子对接和实验进行验证。方法采用C57BL/ 6j小鼠建立Ⅰ型糖尿病模型。Hemoxylin,采用伊红染色和免疫印迹法评价SYQ的疗效。使用Swiss Target Prediction、GeneCards和DisGeNet等数据库筛选与dr相关的靶标。使用STRING数据库和Cytoscape软件创建蛋白-蛋白相互作用网络。利用metscape数据库进行基因本体(Gene Ontology)和京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes)通路富集分析。利用AutoDock软件将活性化合物与核心靶点进行分子对接,并在体外验证网络药理学的预测结果。通过成管和迁移实验,探讨SYQ对高糖诱导的EA.hy926细胞的抗血管生成作用及其机制。结果syq对DR模型血管生成有抑制作用,降低血管生成相关蛋白的表达。网络药理学分析显示SYQ靶向127个蛋白,其中包括HIF-1信号通路。分子对接表明,β-谷甾醇、原花青素- b1和Emodion-1-O-β-d-glucopyranoside与AKT1核心靶蛋白具有较强的结合亲和力。体外实验证实,SYQ在高糖条件下以剂量依赖的方式减少EA.hy926细胞的管形成和迁移。AKT1激动剂的促血管生成作用被SYQ抵消。此外,SYQ可降低p-AKT、HIF-1和血管生成相关蛋白的表达,表明AKT1可抑制高糖诱导的血管生成。这些观察结果证实了网络药理学的见解。syq主要通过抑制血管生成而成为DR的潜在治疗剂。其抗血管生成作用是通过AKT1/HIF-1/VEGF通路介导的,在DR治疗中具有进一步的研究和潜在的临床应用前景。
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引用次数: 0
The study of the cold and heat properties of Dianthus superbus and Odontites vulgaris based on multi-sample metabolomics and gut microbiota analysis: Exploring material and energy metabolism mechanisms 基于多样本代谢组学和肠道菌群分析的石竹和齿齿石冷热特性研究:探索物质和能量代谢机制
Pub Date : 2025-09-01 Epub Date: 2025-07-03 DOI: 10.1016/j.prmcm.2025.100654
Yafeng Zhuang , Xiangxi Meng , Jiayin Chang , Xiaolei Jiang , Hong Chang , Minhui Li

Objective

Dianthus superbus (DS)and Odontites vulgaris (OV) are crucial components of the Mongolian medicine "Bashaga", each possessing unique efficacy. However, their cold and heat natures remain to be experimentally verified. The aim of this study is to validate the medicinal natures of DS and OV and to elucidate the underlying mechanisms from the perspectives of substance and energy metabolism as well as gut microbiota.

Methods

In this study, Anemarrhena asphodeloides (AA, a cold-natured traditional Chinese medicine) and Cinnamomum cassia (CC,a heat-natured traditional Chinese medicine) were used as references to explore the impacts of DS and OV on the material and energy metabolism, multi-sample metabolomics, and gut microbiota in normal rats. This method aims to evaluate the medicinal properties of these plants and clarify their underlying mechanisms.

Results

In terms of material and energy metabolism, the content of Sodium-Potassium Adenosine Triphosphatase (Na⁺/ K⁺ -ATP) in DS and OV was lower than the normal level (p < 0.05). In DS, Pyruvate Kinase (PK) was significantly decreased (p < 0.01), Adenylate Kinase (ADK) was decreased (p < 0.001), and Citrate Synthase (CS) was increased (p < 0.05). In OV, ADK was decreased (p < 0.01) and Glycogen Synthase Kinase 3 Alpha (GSK - 3α) was increased (p < 0.05). AA showed a similar situation. In terms of metabolomics, the metabolic profiles and clustering heatmaps of DS, OV, and AA were similar. AA affected the tryptophan-related metabolic pathways, while CC affected the glutamate-related metabolic pathways. Regarding the gut microbiota, DS, OV, and AA all increased the diversity and richness of the microbiota. At the phylum and genus levels, the composition of the microbiota was similar, and the abundances of various microbiota changed differently.

Conclusion

DS and OV exhibit cold-natured characteristics, as evidenced by their impacts on metabolism and gut microbiota. These findings provide preliminary insights into the potential mechanisms underlying their medicinal properties.
目的:石竹(DS)和牙齿石(OV)是蒙药“巴沙加”的重要成分,各自具有独特的功效。然而,它们的冷热性质仍有待实验验证。本研究的目的是验证DS和OV的药用特性,并从物质和能量代谢以及肠道菌群的角度阐明其潜在机制。方法本研究以寒性中药麻风(Anemarrhena aspholoides, AA)和热性中药肉桂(Cinnamomum cassia, CC)为对照,探讨DS和OV对正常大鼠物质和能量代谢、多样本代谢组学和肠道微生物群的影响。本方法旨在评价这些植物的药用特性并阐明其作用机制。结果在物质和能量代谢方面,DS和OV中钠钾腺苷三磷酸酶(Na + / K + -ATP)含量均低于正常水平(p <;0.05)。在DS中,丙酮酸激酶(PK)显著降低(p <;0.01),腺苷酸激酶(ADK)降低(p <;0.001),柠檬酸合酶(CS)升高(p <;0.05)。OV患者ADK降低(p <;0.01),糖原合成酶激酶3α (GSK - 3α)升高(p <;0.05)。AA也显示了类似的情况。在代谢组学方面,DS、OV和AA的代谢谱和聚类热图相似。AA影响色氨酸相关代谢途径,CC影响谷氨酸相关代谢途径。在肠道菌群方面,DS、OV和AA均增加了肠道菌群的多样性和丰富度。在门和属水平上,微生物群的组成相似,各微生物群的丰度变化不同。结论ds和OV对代谢和肠道菌群的影响表明它们具有冷性特征。这些发现为其药用特性的潜在机制提供了初步的见解。
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引用次数: 0
Melanogenesis inhibition by (2-Methylbutyryl) Shikonin, a naturally occurring naphthoquinone potentiates dacarbazine anti-melanoma efficacy via ROS mediated apoptotic pathway 天然萘醌(2-甲基丁基)紫草素通过ROS介导的凋亡途径增强达卡巴嗪抗黑色素瘤的作用
Pub Date : 2025-09-01 Epub Date: 2025-06-27 DOI: 10.1016/j.prmcm.2025.100651
Aalim Maqsood Bhat , Irshad Ahmad Bhat , Sheikh Tasduq Abdullah

Introduction

Melanoma is a highly aggressive skin cancer with strong metastatic potential and resistance to conventional chemotherapy. Dacarbazine (DTIC) is widely used for melanoma treatment, but its effectiveness is often compromised by acquired resistance, resulting in relapse and poor prognosis. (2-Methylbutyryl) Shikonin (BSHK), a naturally derived naphthoquinone pigment isolated from Lithospermum erythrorhizon, is a bioactive derivative of shikonin—an established compound in Traditional Chinese Medicine (TCM). In TCM, shikonin and its derivatives are key constituents of formulations such as Zicao (purple gromwell root), traditionally used for detoxification, reducing inflammation, and treating skin disorders, including eczema, burns, and malignancies. BSHK has demonstrated broad anti-cancer activity by inhibiting cancer cell proliferation and possesses the ability to suppress tyrosinase enzyme activity, a key enzyme in melanogenesis. This study investigates whether BSHK can enhance the therapeutic efficacy of dacarbazine in melanoma cells and explores the molecular mechanisms underlying their combined effect, while also highlighting its traditional use and therapeutic relevance in Chinese herbal medicine.

Methods

Melanoma cells were treated with BSHK, dacarbazine, or their combination. Cell viability was assessed by MTT assay. Apoptosis was analyzed using Annexin-V/FITC staining and flow cytometry. Protein expression levels of key Oxidative stress, apoptotic and melanogenic markers such as SOD, Catalase, Nrf-2 Bcl-2, BAX, Caspase-3, and MITF was evaluated by immunoblotting.

Results

BSHK significantly enhanced the anti-proliferative effect of dacarbazine on melanoma cells. Co-treatment increased apoptotic cell populations and ROS levels compared to single treatments. Western blot analysis revealed that combination therapy downregulated MITF and Bcl-2, while upregulating BAX and cleaved Caspase-3, indicating enhanced apoptotic signaling and melanogenesis inhibition.

Discussion

In conclusion, (2-Methylbutyryl) Shikonin sensitizes melanoma cells to dacarbazine by inhibiting melanogensis thereby increasing their susceptibility to apoptosis. The synergistic anticancer effects of (2-Methylbutyryl) Shikonin and dacarbazine suggest that their combination could be a promising therapeutic strategy for treating melanoma
黑色素瘤是一种高度侵袭性的皮肤癌,具有很强的转移潜力,对常规化疗有耐药性。达卡巴嗪(DTIC)广泛用于黑色素瘤的治疗,但其有效性往往受到获得性耐药的影响,导致复发和预后不良。(2-甲基丁基)紫草素(BSHK)是从紫草中分离得到的萘醌类天然色素,是紫草素的生物活性衍生物。在中医中,紫草素及其衍生物是紫草等制剂的关键成分,紫草传统上用于解毒、消炎和治疗皮肤疾病,包括湿疹、烧伤和恶性肿瘤。BSHK已显示出广泛的抗癌活性,可以抑制癌细胞增殖,并具有抑制酪氨酸酶活性的能力,酪氨酸酶是黑色素形成的关键酶。本研究探讨BSHK是否能增强达卡巴嗪对黑色素瘤细胞的治疗作用,并探讨其联合作用的分子机制,同时强调其在中草药中的传统应用和治疗意义。方法分别用BSHK、达卡巴嗪或两者联合治疗黑色素瘤细胞。MTT法测定细胞活力。Annexin-V/FITC染色及流式细胞术分析细胞凋亡。免疫印迹法检测各组氧化应激、凋亡和黑色素生成标志物(SOD、过氧化氢酶、Nrf-2 Bcl-2、BAX、Caspase-3和MITF)的蛋白表达水平。结果bshk能显著增强达卡巴嗪对黑色素瘤细胞的抗增殖作用。与单独处理相比,共处理增加了凋亡细胞群和ROS水平。Western blot分析显示,联合治疗下调了MITF和Bcl-2,上调了BAX和裂解Caspase-3,表明增强了凋亡信号传导和黑色素生成抑制。总之,(2-甲基丁基)紫草素通过抑制黑素生成从而增加其对凋亡的敏感性,从而使黑色素瘤细胞对达卡巴嗪敏感。(2-甲基丁基)紫草素和达卡巴嗪的协同抗癌作用表明,它们的联合治疗可能是治疗黑色素瘤的一种有前途的治疗策略
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引用次数: 0
Unveiling polyphyllin's role in neuroprotection: A pharmacological perspective 揭示多叶磷脂在神经保护中的作用:药理学观点
Pub Date : 2025-09-01 Epub Date: 2025-06-07 DOI: 10.1016/j.prmcm.2025.100641
Md Sadique Hussain , Amita Joshi Rana , Mudasir Maqbool , Nasreen Sulthana , Ayesha Sultana , Sumel Ashique , Yumna Khan , Prasanna Srinivasan Ramalingam , Sushil S. Burle , Vikas Jakhmola , Gaurav Gupta

Introduction

Polyphyllins are bioactive steroidal saponins predominantly derived from Paris polyphylla (Chinese: Chonglou, 重楼), an herb long employed in Traditional Chinese Medicine (TCM) for detoxification, inflammation control, and pain relief, commonly administered as decoctions or powdered Rhizoma Paridis. Beyond these traditional uses, growing evidence supports their neuroprotective efficacy, especially in the context of neurodegenerative diseases (NDs), where inflammation, oxidative stress, and dysregulated cell death are central to disease progression.

Methods

A comprehensive literature search was conducted up to March 2025. Out of 423 initially retrieved articles, 143 were included based on relevance to neuroprotective mechanisms, pharmacokinetics, and translational potential. Reviews, non-English articles, and studies not focused on brain-related mechanisms were excluded.

Results

Polyphyllins demonstrate potent neuroprotective activities through anti-inflammatory, antioxidant, and autophagy-modulating mechanisms. PP-II interrupts the KEAP1-NRF2 interaction, activating antioxidant gene expression, while PP-I induces mitophagy via the PINK1-Parkin pathway. PP-VII modulates neuroinflammation through activation of the cGAS-STING axis. These actions collectively protect neurons, preserve mitochondrial function, and reduce pathological cascades associated with NDs. However, poor solubility and limited blood-brain barrier permeability remain key translational barriers.

Discussion

The promising therapeutic effects of polyphyllins in ND models align with their historical use in TCM. Advances in nanomedicine, including lipid nanoparticles and carbon dots; have improved polyphyllin delivery to the central nervous system. Nevertheless, the absence of clinical trials and the need for safety profiling require resolution before clinical adoption. Future investigations should prioritize optimized drug formulations and validation in human models to bridge preclinical evidence with therapeutic applications.
总黄酮是一种具有生物活性的甾体皂苷,主要从巴黎总黄酮(中文:重楼)中提取,是一种长期用于解毒,控制炎症和缓解疼痛的中药,通常作为煎剂或粉末给药。除了这些传统用途,越来越多的证据支持其神经保护作用,特别是在神经退行性疾病(NDs)的背景下,炎症、氧化应激和细胞死亡失调是疾病进展的核心。方法进行截至2025年3月的综合文献检索。在最初检索的423篇文章中,143篇基于神经保护机制、药代动力学和翻译潜力的相关性被纳入。综述、非英文文章和不关注大脑相关机制的研究被排除在外。结果多叶磷脂通过抗炎、抗氧化和自噬调节机制显示出强大的神经保护作用。PP-II阻断KEAP1-NRF2相互作用,激活抗氧化基因表达,而PP-I通过PINK1-Parkin途径诱导线粒体自噬。PP-VII通过激活cGAS-STING轴调节神经炎症。这些作用共同保护神经元,保持线粒体功能,并减少与NDs相关的病理级联反应。然而,溶解度差和血脑屏障通透性有限仍然是主要的翻译障碍。多叶磷脂在ND模型中的良好治疗效果与其在中医中的历史应用相一致。纳米医学的进展,包括脂质纳米粒子和碳点;改善了向中枢神经系统输送多叶茶素。然而,临床试验的缺乏和安全性分析的需要需要在临床采用之前解决。未来的研究应优先考虑优化药物配方和人体模型验证,以弥合临床前证据与治疗应用之间的桥梁。
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Pharmacological Research - Modern Chinese Medicine
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