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A Systematic Review of Neuroprotective Effects of Mangosteen and its Xanthones Against Oxidative Stress and Inflammation. 山竹果及其山酮抗氧化应激和炎症神经保护作用的系统综述。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-08-22 DOI: 10.1055/a-2665-2226
Hin Yee Thew, Yong Chiang Tan, Yong Sze Ong, Bey Hing Goh, Kooi Yeong Khaw

Mangosteen has garnered increasing attention for its medicinal properties against oxidative stress and inflammation-two major causative and progressive agents of neurodegenerative diseases. This systematic review explores the antioxidative and anti-inflammatory effects of mangosteen crude extracts and their purified bioactive compounds, highlighting their neuroprotective potential against neurodegenerative conditions.The Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) strategy was used to identify studies published in English up to July 2024 across five databases (Cochrane, PubMed, Scopus, Web of Science, and Google Scholar). The Population, Intervention, Comparison, and Outcome (PICO) framework guided the search strategy, and duplicate records were removed using Covidence software. Of the 149 studies screened, 40 met the predefined inclusion criteria and were included in the review. The quality of the included studies was assessed using criteria adapted from the Cochrane Handbook, focusing on risk of bias and methodological rigor.Mangosteen extract and xanthones consistently reduced oxidative markers in various models. Anti-inflammatory effects were evident as mangosteen extract reduced pro-inflammatory cytokines and modulated the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and cyclooxygenase-2 (COX-2) pathways in neuroinflammation models. Xanthones further suppressed inflammatory mediators and enhanced cellular resilience.The in vitro and in vivo results suggested the neuroprotective capabilities of mangosteen extracts and its purified bioactives. Despite that, gaps remain in understanding the potential synergistic effects of these bioactives, their druggability properties, and clinical applicability. Further research, especially clinical trials, will be necessary to further impel mangosteen and its derivatives into therapeutic applications.

山竹果因其抗氧化应激和炎症的药用特性而受到越来越多的关注,氧化应激和炎症是神经退行性疾病的两种主要病因和进行性因素。这篇系统综述探讨了山竹果粗提取物及其纯化的生物活性化合物的抗氧化和抗炎作用,强调了它们对神经退行性疾病的神经保护潜力。系统评价和荟萃分析首选报告项目(PRISMA)策略用于识别截至2024年7月在五个数据库(Cochrane, PubMed, Scopus, Web of Science和谷歌Scholar)中发表的英文研究。人口、干预、比较和结果(PICO)框架指导了搜索策略,并使用covid - ence软件删除了重复记录。在筛选的149项研究中,有40项符合预先确定的纳入标准并纳入了本综述。纳入研究的质量采用Cochrane手册的标准进行评估,重点关注偏倚风险和方法的严谨性。山竹提取物和山酮在各种模型中一致降低氧化标志物。在神经炎症模型中,山竹提取物降低促炎细胞因子,调节活化B细胞的核因子κB轻链增强子(NF-κB)和环氧化酶-2 (COX-2)通路,具有明显的抗炎作用。山酮进一步抑制炎症介质,增强细胞恢复力。体外和体内实验结果表明山竹提取物及其纯化的生物活性物质具有一定的神经保护作用。尽管如此,在了解这些生物活性物质的潜在协同作用、它们的药物特性和临床适用性方面仍然存在差距。进一步的研究,特别是临床试验,将有必要进一步推动山竹果及其衍生物进入治疗应用。
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引用次数: 0
Local and Systemic Effects of Topical Betulinic Acid in a Psoriasis-like Inflammation Model in Mice. 局部白桦酸对银屑病样炎症模型小鼠的局部和全身作用。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-06-27 DOI: 10.1055/a-2644-8732
Flávia S Fernandes, Gustavo S Silva, Rafael V Soares, Fabiana Ourique, Tiziane L D R Nakagawa, Daniel F Martins, Ariane Zamoner, Maicon R Kviecinski

Psoriasis patients often discontinue oral and injectable treatments due to concerns about both safety and efficacy. Issues such as adverse side effects, limited long-term effectiveness, and fear of potential complications contribute to non-adherence, impacting treatment outcomes and patients' quality of life. Betulinic acid (BA) forms supramolecular aggregates through self-assembly in a hydroalcoholic vehicle, which was hypothesized to have antipsoriatic activity when applied topically. To test this, imiquimod was applied to induce psoriasis-like skin inflammation in mice (except in the untreated group) every 24 hours for 5 days. Two hours after each imiquimod application, the groups received either 100 µL of vehicle (10% glycerol aqueous solution), 0.05 mg/mL clobetasol (Clo), or 0.5 mg/mL BA. At the end of the study, the Psoriasis Area and Severity Index (PASI) was evaluated (n = 12/group), and complete skin clearance time (CSC) was determined in six mice per group. The remaining six mice per group were used to assess acanthosis, lymphocyte and granulocyte infiltration, and Akt and ERK phosphorylation in skin samples, as well as TNFα, IL-17A, IFNγ, and TGFβ levels in serum. To assess treatment safety, we evaluated food and water intake, ambulation pattern, body weight gain, organ weights, and blood parameters. BA significantly reduced CSC time by up to 40% compared to the control and was 10% faster than Clo. Both BA and Clo reduced PASI and acanthosis to approximately one-third of control values, normalized immune cell infiltration and TNFα levels, decreased IL-17A by more than 30%, and reduced p-Akt and p-ERK2. BA uniquely normalized IFNγ levels without causing intolerable toxicity. Using an animal model of psoriatic skin inflammation, our findings support BA as a strong candidate for clinical translation, warranting further studies on its safety, pharmacokinetics, and optimal dosage in humans, potentially leading to randomized controlled trials in psoriasis patients.

白桦酸(BA)通过在氢酒精载体中的自组装形成超分子聚集体,假设局部应用时具有抗银屑病活性。应用咪喹莫特诱导小鼠(未给药组除外)每24小时出现牛皮癣样皮肤炎症,连续5天。每次咪喹莫特应用2小时后,各组分别给予100µL载体(10%甘油水溶液)、0.05 mg/mL氯倍他索(Clo)或0.5 mg/mL BA。在研究结束时,评估银屑病面积和严重程度指数(PASI) (n=12/组),并测定每组6只小鼠的完全皮肤清除时间(CSC)。每组剩余6只小鼠用于评估皮肤样本棘层增生、淋巴细胞和粒细胞浸润、Akt和ERK磷酸化以及血清中TNFα、IL-17A、IFNγ和TGFβ的水平。为了评估治疗的安全性,我们评估了食物和水的摄入量、活动方式、体重增加、器官重量和血液参数。与对照组相比,BA显著减少了CSC时间达40%,比Clo快10%。BA和Clo均可将PASI和棘层厚度降低至对照组的约三分之一,使免疫细胞浸润和TNFα水平正常化,IL-17A降低30%以上,p-Akt和p-ERK2降低。BA独特地使IFNγ水平正常化,而不会引起无法忍受的毒性。通过银屑病皮肤炎症的动物模型,我们的研究结果支持BA作为临床转化的强有力候选药物,值得进一步研究其安全性、药代动力学和人类最佳剂量,可能导致银屑病患者的随机对照试验。
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引用次数: 0
In silico and In vitro Screening of Medicinal Plants from Brazilian Traditional Medicine for Anti-Helicobacter pylori Activity. 巴西传统药用植物抗幽门螺杆菌活性的体外和室内筛选。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-06-13 DOI: 10.1055/a-2635-4268
Campili Mendes, Jéssica Raquel Borges Monteiro, Rodrigo de Almeida Romagna, Aliny Rodrigues de Jesus da Conceição, Pedro Henrique Tregnago, Amanda Eiriz Feu, Rita de Cássia Ribeiro Gonçalves, Warley de Souza Borges, Ricardo Machado Kuster, Rodrigo Rezende Kitagawa

Medicinal plants and their phytocompounds are valuable shortcuts for discovering new, safer biologically active compounds or herbal medicines with reduced adverse effects. In this study, medicinal plant species were initially selected from Brazilian traditional medicine using a database of in silico and in vitro studies. A virtual screening study was carried out with a phytochemical database previously reported in the literature. The biological activity was evaluated in silico by PASS Online and molecular docking, then validated by in vitro anti-Helicobacter pylori assay. The chemical profile of the species was obtained by ESI(±)FT-ICR MS and LC-MS-DAD analysis. Vernonia condensata, Bauhinia forficata, Jatropha gossypiifolia, and Sonalum paniculatum were selected based on a survey of the literature for use of gastric diseases and anti-Helicobacter pylori potential. After PASS analysis, Jatropha gossypiifolia was selected for in vitro study because its compounds showed anti-H. pylori activity potential, inhibiting fumarate reductase enzyme. J. gossypiifolia extracted showed MIC of 64 µg/mL and MBC of 128 µg/mL in the in vitro anti-H. pylori assay. ESI(±)FT-ICR MS and LC-MS-DAD analysis showed compounds such as luteolin (1: ), isovitexin (2: ), luteolin-7-O-glucoside (3: ), isoorientin (4: ), and 3-genistein-8-C-glucoside (5: ). Molecular docking analysis showed a potential interaction of compounds in the enzyme active site such as hydrogen bonds with Arg404 and a similar interaction to fumaric acid, except for isoorientin (4: ). J. gossypiifolia showed promising activity and may represent a future alternative to treat H. pylori infections and their deleterious effects, reinforcing the therapeutic potential of this plant.

药用植物及其植物化合物是发现新的、更安全的生物活性化合物或副作用更小的草药的宝贵捷径。在这项研究中,药用植物物种最初从巴西传统医学中通过计算机和体外研究数据库选择。虚拟筛选研究是利用文献中先前报道的植物化学数据库进行的。通过PASS Online和分子对接对其生物活性进行了计算机评价,并通过体外抗幽门螺杆菌实验对其进行了验证。通过ESI(±)FT-ICR MS和LC-MS-DAD分析获得了该物种的化学特征。在查阅文献的基础上,筛选出水杨、紫荆花、麻疯树和细叶索纳姆,研究其在胃病中的应用和抗幽门螺杆菌的潜力。通过PASS分析,选择麻疯树进行体外研究,因为其化合物具有抗h。幽门螺杆菌活性电位,抑制富马酸还原酶。棉叶提取物抗h的MIC为64µg/mL, MBC为128µg/mL。螺杆菌化验。ESI(±)FT-ICR MS和LC-MS-DAD分析显示化合物为木犀草素(1∶)、异牡荆素(2∶)、木犀草素-7- o -葡萄糖苷(3∶)、异荭草苷(4∶)和3-染料木素-8- c -葡萄糖苷(5∶)。分子对接分析显示,除了异荭草苷外,该酶活性位点上的化合物可能与Arg404存在氢键等相互作用,与富马酸也存在类似的相互作用(3:)。棉叶棉显示出良好的活性,可能是治疗幽门螺杆菌感染及其有害影响的未来选择,增强了该植物的治疗潜力。
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引用次数: 0
Anti-inflammatory and Antioxidant Properties of Almond-Skin Acetonic Extract in Zebrafish (Danio rerio) Copper-Sulphate-induced Inflammation. 杏仁皮丙酮提取物对斑马鱼(Danio rerio)硫酸铜诱导炎症的抗炎和抗氧化作用。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-10-01 DOI: 10.1055/a-2654-9426
Rúben Barbosa, Ana Martins, Ivo Vaz Oliveira, Maria Inês Dias, Sandra M Monteiro, Carlos Venâncio, Luís Félix

This study aimed to assess the properties of an acetone-based almond-skin (Prunus dulcis) extract and examine its effects on chemically induced inflammation by evaluating associated oxidative changes in an in vivo model. The phytochemical composition was analysed by LC-MS/MS while the antioxidant capacity was evaluated using DPPH, ABTS, and FRAP assays. The neutrophil migration was assessed using a CuSO4-induced inflammation model in a transgenic zebrafish line (Tg(mpx : GFP)i114). Three days post-fertilisation zebrafish larvae were treated with 5 and 25 µg/mL extract for 1 h and then exposed to 10 µM CuSO4 for 40 min. Following exposure, various biochemical markers were assessed, along with neurobehavioral effects. The polyphenolic profile revealed a high flavonoid content and good antioxidant properties confirmed by the DPPH, ABTS, and FRAP assays. The extract reduced neutrophil migration in a concentration-dependent manner, indicating anti-inflammatory activity. Additionally, it decreased reactive oxygen species (ROS) production and cell death without affecting mitochondrial membrane potential. The extract also mitigated oxidative damage, as shown by reduced malondialdehyde and protein carbonylation levels, alongside decreased antioxidant response markers. Neurobehavioral effects induced by CuSO4 were alleviated, as evidenced by improved touch-evoked responses. These findings suggest that almond-skin extract holds significant antioxidant and anti-inflammatory properties, possibly through modulation of ROS and calcium signalling pathways.

本研究旨在评估丙酮杏仁皮(Prunus dulcis)提取物的特性,并通过评估体内模型中相关的氧化变化来研究其对化学诱导炎症的影响。采用LC-MS/MS分析其植物化学成分,DPPH、ABTS和FRAP测定其抗氧化能力。在转基因斑马鱼系(Tg(mpx: GFP)i114)中,使用cuso4诱导的炎症模型评估中性粒细胞迁移。受精3天后,斑马鱼幼鱼分别用5和25µg/mL提取物处理1 h,然后用10µM CuSO4处理40 min。暴露后,评估了各种生化指标,以及神经行为影响。经DPPH、ABTS和FRAP检测证实,其多酚类化合物含量高,抗氧化性能好。提取物以浓度依赖的方式减少中性粒细胞迁移,表明抗炎活性。此外,它减少活性氧(ROS)的产生和细胞死亡,而不影响线粒体膜电位。通过降低丙二醛和蛋白质羰基化水平,以及降低抗氧化反应标志物,该提取物还可以减轻氧化损伤。CuSO4诱导的神经行为效应得到缓解,触觉诱发反应得到改善。这些发现表明杏仁皮提取物具有显著的抗氧化和抗炎特性,可能通过调节活性氧和钙信号通路。
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引用次数: 0
Therapeutic Potential of Carnosic Acid in Alopecia: A Mechanistic Perspective. 鼠尾草酸对脱发的治疗潜力:一个机制的观点。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-08-08 DOI: 10.1055/a-2665-2211
Priyanka Singh, Poonam Kushwaha, Mohammad Ahmad, Atif Husain

Alopecia, characterised by partial or complete hair loss, significantly affects the psychological and social well-being of individuals. Current FDA-approved treatments, such as topical minoxidil and oral finasteride, often present limitations, including skin irritation and suboptimal efficacy, compromising patient adherence. In recent years, natural compounds have garnered attention as potential alternatives, with carnosic acid emerging as a promising candidate due to its multifaceted biological activities. Carnosic acid, a diterpenic polyphenol predominantly found in rosemary (Rosmarinus officinalis) and sage (Salvia officinalis), exhibits potent antioxidant, anti-inflammatory, anti-androgenic, neuroprotective, and hair follicle-regenerative properties. Despite its therapeutic potential, its poor solubility and stability in conventional formulations limit its clinical application. This review comprehensively explores the mechanisms through which carnosic acid exerts its effects in alopecia management, focusing on its antioxidant capacity, anti-inflammatory responses, inhibition of dihydrotestosterone activity, promotion of hair follicle regeneration, and neuroprotective actions. The findings highlight carnosic acid's potential as a natural, effective, and safer alternative for alopecia treatment.

脱发的特点是部分或完全脱发,严重影响个人的心理和社会福祉。目前fda批准的治疗方法,如局部米诺地尔和口服非那雄胺,通常存在局限性,包括皮肤刺激和次优疗效,影响患者的依从性。近年来,天然化合物作为潜在的替代品受到了人们的关注,鼠尾草酸因其多方面的生物活性而成为一个有希望的候选者。鼠尾草酸是一种二萜多酚,主要存在于迷迭香(Rosmarinus officinalis)和鼠尾草(Salvia officinalis)中,具有有效的抗氧化、抗炎、抗雄激素、神经保护和毛囊再生特性。尽管其具有治疗潜力,但其在常规配方中的溶解度和稳定性差限制了其临床应用。本文综述了鼠尾草酸在脱发治疗中的作用机制,重点介绍了鼠尾草酸的抗氧化能力、抗炎反应、抑制双氢睾酮活性、促进毛囊再生和神经保护作用。这些发现强调了鼠尾草酸作为一种天然、有效、安全的治疗脱发的替代品的潜力。
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引用次数: 0
Preclinical Evaluation of Baicalin for the Treatment of Diabetic Nephropathy: A Systematic Review and Meta-Analysis. 黄芩苷治疗糖尿病肾病的临床前评价:系统综述和荟萃分析。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-07-24 DOI: 10.1055/a-2615-8249
Hengtong An, Luyao Liu, Tongtong He, Xiaohan Chen, Xiaofei Jin, Xiaohong Zhou, Weijuan Gao

Scutellaria baicalensis, a widely used medicinal herb in traditional Chinese medicine, is frequently employed in the treatment of diabetic nephropathy (DN). Its primary active constituent, baicalin, has shown significant therapeutic potential in animal models of DN; however, no comprehensive and systematic evaluation of its therapeutic effects and underlying mechanisms in DN has yet been conducted. This meta-analysis aimed to assess the efficacy of baicalin in DN treatment and elucidate its pharmacological mechanisms. Relevant studies were retrieved from databases including Web of Science, PubMed, Embase, CNKI, Wanfang Data, and VPCS, covering the literature up to November 2024. Study quality was evaluated using SYRCLE's risk of bias tool, and statistical analyses were performed with STATA 12. Primary outcomes included blood urea nitrogen (BUN), serum creatinine (SCR), and fasting blood glucose (FBG), while secondary outcomes encompassed urinary protein (UP), triglycerides (TG), total cholesterol (TC), inflammatory markers, fibrosis indicators, and oxidative stress parameters. Subgroup analyses, publication bias assessments, and sensitivity analyses were conducted to ensure result reliability. A total of 14 studies involving 221 rodents met the inclusion criteria. Baicalin significantly reduced BUN, SCR, FBG, TG, TC, UP, interleukin-6 (IL-6), interleukin-1 beta (IL-1β), tumor necrosis factor-alpha (TNF-α), malondialdehyde (MDA), and fibronectin (FN) levels while enhancing superoxide dismutase (SOD) activity. These findings suggest that baicalin improves kidney function, reduces proteinuria, corrects lipid metabolism, and alleviates inflammation, oxidative stress, and fibrosis. This meta-analysis concludes that baicalin exhibits significant therapeutic potential in DN models, acting via anti-inflammatory, antioxidant, and antifibrotic mechanisms.

黄芩是一种应用广泛的中药,常用于治疗糖尿病肾病(DN)。其主要活性成分黄芩苷在DN动物模型中显示出显著的治疗潜力;然而,目前尚未对其治疗DN的效果和潜在机制进行全面系统的评价。本荟萃分析旨在评估黄芩苷治疗DN的疗效并阐明其药理机制。检索Web of Science、PubMed、Embase、CNKI、万方数据、VPCS等数据库,截止到2024年11月。使用sycle的偏倚风险工具评估研究质量,并使用STATA 12进行统计分析。主要结局包括血尿素氮(BUN)、血清肌酐(SCR)和空腹血糖(FBG),次要结局包括尿蛋白(UP)、甘油三酯(TG)、总胆固醇(TC)、炎症标志物、纤维化指标和氧化应激参数。进行亚组分析、发表偏倚评估和敏感性分析以确保结果的可靠性。共有涉及221只啮齿动物的14项研究符合纳入标准。黄芩苷显著降低BUN、SCR、FBG、TG、TC、UP、白细胞介素-6 (IL-6)、白细胞介素-1β (IL-1β)、肿瘤坏死因子-α (TNF-α)、丙二醛(MDA)、纤维连接蛋白(FN)水平,提高超氧化物歧化酶(SOD)活性。提示黄芩苷具有改善肾功能、减少蛋白尿、纠正脂质代谢、减轻炎症、氧化应激和纤维化的作用。本荟萃分析表明,黄芩苷在DN模型中表现出显著的治疗潜力,通过抗炎、抗氧化和抗纤维化机制发挥作用。
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引用次数: 0
Baicalein Alleviates Neuropathic Pain by Inhibiting Microglial Activation and Inflammation Via the TLR4/NF-κB p65 Pathway. 黄芩素通过TLR4/NF-κB p65通路抑制小胶质细胞激活和炎症,减轻神经性疼痛。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-07-25 DOI: 10.1055/a-2665-6684
Jieyi Cai, Ling Luo, Min Yuan, Hui Li, Lü Chen, Qianqian Peng, Changlai Zhu, Yun Gu

Clinically, there is a significant unmet need for effective treatments for chronic neuropathic pain. Commonly used drugs, such as opioids, are primarily designed for acute pain management and are associated with substantial adverse effects, including tolerance and addiction. Therefore, the development of safe and effective therapies is of paramount importance. Baicalein (BA), a flavonoid compound extracted from Scutellaria baicalensis, has anti-inflammatory, antibacterial, and anti-proliferative activities against tumor cells and has been used to treat various acute and chronic conditions without notable side effects. In this study, we employed the spared nerve injury (SNI) pain model to investigate the therapeutic efficacy of BA on neuropathic pain and its underlying mechanisms. Results showed that BA effectively alleviated SNI-induced hyperalgesia and the progression of chronic pain in a dose-dependent manner by inhibiting glial cell activation, immune cell infiltration, and inflammatory responses. Additionally, using an in vitro microglial inflammation model, we further confirmed that BA inhibits M1 polarization of microglia and the expression of pro-inflammatory factors by modulating the TLR4/NF-κB p65 signaling pathway. Our results suggest that BA holds promise as a potential therapeutic agent for treating neuropathic pain caused by nerve injury or diseases.

临床上,对慢性神经性疼痛的有效治疗有显著的未满足的需求。常用药物,如阿片类药物,主要用于急性疼痛管理,并与严重的不良反应相关,包括耐受性和成瘾性。因此,开发安全有效的治疗方法至关重要。黄芩素(Baicalein, BA)是从黄芩中提取的一种黄酮类化合物,具有抗炎、抗菌和抗肿瘤细胞增殖的作用,已被用于治疗各种急慢性疾病,且无明显的副作用。本研究采用SNI疼痛模型,探讨BA对神经性疼痛的治疗效果及其机制。结果显示,BA通过抑制神经胶质细胞活化、免疫细胞浸润和炎症反应,以剂量依赖的方式有效缓解sni诱导的痛觉过敏和慢性疼痛的进展。此外,通过体外小胶质细胞炎症模型,我们进一步证实了BA通过调节TLR4/NF-κB p65信号通路抑制小胶质细胞M1极化和促炎因子的表达。我们的研究结果表明,BA有望成为治疗神经损伤或疾病引起的神经性疼痛的潜在治疗剂。
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引用次数: 0
The "Cancer Bush" Sutherlandia (syn. Lessertia) frutescens. An Example of Promotional Research, or Is There Scientific Merit? “癌症灌木”萨瑟兰属植物(同属小瑟兰属植物)。一个促销研究的例子,还是有科学价值?
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-08-05 DOI: 10.1055/a-2654-6280
Nicezelle Gernandt, Frank van der Kooy

Sutherlandia (syn. Lessertia) frutescens is indigenous to the drier regions of southern Africa. Sutherlandia frutescens has a long history of traditional medicinal use and is credited with antiviral, antibacterial, antifungal, and anticancer properties. It is a very popular phytomedicine and, as the common name implies, is used as a prophylaxis and treatment of cancer. The objective of this review was to collate all published scientific data on the genera Sutherlandia and Lessertia regarding their antiproliferative properties and critically evaluate the data against established guidelines. Despite its use as traditional medicine, the potential of S. frutescens as a cancer treatment remains highly questionable. While in vitro studies suggest some potential antiproliferative effects, many studies lack positive controls and selectivity studies or use excessively high dosages, well above established guidelines, translating into unrealistic clinical applications. Consequently, these studies often appear overly optimistic and biased. Very few well-designed studies are available, and most research fails to meet established guidelines for evaluating selective cytotoxicity. Given these limitations and the absence of rigorous in vivo studies and/or clinical trials, future research may first focus on identifying chemovars with acceptable bioactivity and/or investigating the possibility of the presence of prodrugs by simulated gastrointestinal tract studies. Based on available data, it must be concluded that S. frutescens does not exhibit acceptable levels of bioactivity/selectivity, and keeping in mind possible herb-drug interactions and the serious nature of cancer, which causes over 10 million deaths annually, S. frutescens should not currently be recommended for use.

Sutherlandia(同:Lessertia) frutescens是非洲南部干旱地区的本土植物。Sutherlandia frutescens有着悠久的传统药用历史,被认为具有抗病毒、抗菌、抗真菌和抗癌的特性。它是一种非常流行的植物药,顾名思义,它被用来预防和治疗癌症。本综述的目的是整理所有已发表的关于Sutherlandia属和Lessertia属抗增殖特性的科学数据,并根据既定指南对数据进行批判性评估。尽管它被用作传统药物,但它作为癌症治疗的潜力仍然非常值得怀疑。虽然体外研究显示了一些潜在的抗增殖作用,但许多研究缺乏阳性对照和选择性研究,或使用过高的剂量,远远高于既定的指导方针,转化为不切实际的临床应用。因此,这些研究往往显得过于乐观和有偏见。设计良好的研究很少,而且大多数研究都不能满足评估选择性细胞毒性的既定指导方针。考虑到这些限制以及缺乏严格的体内研究和/或临床试验,未来的研究可能首先集中在鉴定具有可接受生物活性的化学变体和/或通过模拟胃肠道研究调查前药存在的可能性。根据现有的数据,必须得出结论,果参没有表现出可接受的生物活性/选择性水平,并且考虑到可能的草药药物相互作用和每年导致1 000多万人死亡的癌症的严重性,目前不应建议使用果参。
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引用次数: 0
Withanolides as Prospective Drug Candidates: Production and Therapeutic Applications-A Review. 作为潜在候选药物的戊内酯:生产和治疗应用综述。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-11-01 Epub Date: 2025-07-18 DOI: 10.1055/a-2659-7263
Anu Gupta, M Vasundhara

Withanolides are a group of steroidal lactones predominantly present in the genus 'Withania'. These compounds exhibit cytotoxic, neurological, immunomodulatory, and anti-inflammatory activities. Structural diversity leads to various kinds of withanolides with different biological functionality. There is an increasing market demand for withanolides as they exhibit great therapeutic potential and can be explored for developing novel drug entities. Withanolides are primarily produced from plants that are more prone to diseases and are on the verge of endangerment. From the plant sources, the yield of withanolides is meagre (0.5 - 2%), which cannot meet the market demand, and the production cost is very high. This leads to the exploration of an alternative sustainable source for withanolide production. Endophytic fungi can produce host plant metabolites and can be investigated as an alternative source for withanolides production. Endophytic fungi can be isolated from the host plant species producing withanolides and cultured further for production. Studying the genes of the withanolides' biosynthetic pathway (their upregulation or downregulation), media optimisation, co-culture, and various elicitors may enhance withanolides production. In silico approaches like molecular docking and quantitative structure-activity relationship studies may also aid in understanding the mechanism of action of withanolides on a specific target to cure a disease. Nanotechnology techniques help in designing the formulation of withanolides so that they can cross the blood-brain barrier and improve therapeutic effectiveness. This article highlights the biochemistry, biosynthetic pathway, mode of action, therapeutic potential of withanolides, and exploration of endophytic fungi as an alternative source to produce withanolides cost-effectively.

Withanolides是一组甾体内酯,主要存在于Withania属中。这些化合物具有细胞毒性、神经、免疫调节和抗炎活性。结构的多样性导致了不同种类的金皂荚内酯具有不同的生物学功能。由于它们具有巨大的治疗潜力,可以开发新的药物实体,因此市场对它们的需求不断增加。Withanolides主要是从那些更容易患病和濒临灭绝的植物中生产出来的。从植物源上看,金戊内酯的产率很低(0.5-2%),不能满足市场需求,而且生产成本很高。这导致探索替代可持续来源的威纳醇内酯生产。内生真菌可以产生寄主植物的代谢物,可以作为一种替代来源进行研究。内生真菌可以从产生吲哚内酯的寄主植物中分离出来,并进一步培养用于生产。研究其生物合成途径的基因(上调或下调)、培养基优化、共培养和多种激发子可提高其产量。分子对接和定量构效关系研究等计算机方法也可能有助于理解糖醇内酯对特定靶点的作用机制,从而治疗疾病。纳米技术有助于设计金皂荚内酯的配方,使它们能够穿过血脑屏障,提高治疗效果。本文重点介绍了植物内酯的生物化学、生物合成途径、作用方式、治疗潜力,并探讨了内生真菌作为一种经济有效地生产植物内酯的替代来源。
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引用次数: 0
The Medicinal Chemistry of Cyanidin and its Glycoside Derivatives: Focus on the Antiproliferative and Potential Anticancer Activity. 花青素及其苷类衍生物的药物化学研究:以其抗增殖和潜在的抗癌活性为重点。
IF 2 4区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 Epub Date: 2025-06-12 DOI: 10.1055/a-2634-4300
Abdur Rauf, Ahmed Olatunde, Rahaf Ajaj, Nabia Hafeez, Mohamed Y Zaky, Md Rezaul Islam, Md Mozahidul Islam, Giovanni Ribaudo

Cyanidin and its glucosides are anthocyanins belonging to the class of flavonoid phytochemicals. These pigments give fruits and vegetables their typical reddish-purple nuance, and their peculiar chemical features result in a remarkable ability to neutralize reactive oxygen species and other mutagens. Thus, both cyanidin and its glycosides were proposed as candidates for chemoprevention, as anticancer agents, and as adjuvant therapies. Indeed, the compounds were investigated through various in vitro and in vivo models of colon, breast, kidney, prostate and liver cancer, and glioma. Cyanidin and its derivatives have been found to inhibit key signaling pathways, such as PI3K/Akt, MAPK, and NF-κB, which can reduce cancer cell growth, induce apoptosis, and suppress metastasis. In the first part of the review, the chemical properties of cyanidin and its glycoside analogues will be discussed. Then, an overview of in vitro evidence on activity will be presented, followed by a report on preclinical and clinical data together with comments on the mechanisms involved. Eventually, the aspect of pharmacokinetic properties, bioavailability, and formulation will be dissected. Overall, the review indicates that cyanidin and its derivatives could be effective anticancer agents but also calls for a deeper understanding of the molecular mechanisms underlying their bioactivity. Despite promising results, resolving issues like stability, absorption, and targeted distribution is crucial to maximize their therapeutic potential. More research is needed to develop innovative cyanidin-based formulations for efficient cancer treatment.

花青素及其糖苷是类黄酮类植物化学物质中的花青素类。这些色素使水果和蔬菜呈现出典型的红紫色,它们独特的化学特性使它们具有非凡的中和活性氧和其他诱变剂的能力。因此,花青素及其糖苷被认为是化学预防、抗癌和辅助治疗的候选药物。事实上,这些化合物通过各种体外和体内模型进行了结肠癌、乳腺癌、肾癌、前列腺癌、肝癌和胶质瘤的研究。研究发现,花青素及其衍生物可抑制PI3K/Akt、MAPK、NF-κB等关键信号通路,从而抑制癌细胞生长、诱导凋亡、抑制转移。第一部分综述了花青素及其糖苷类似物的化学性质。然后,将概述有关活性的体外证据,随后是临床前和临床数据的报告以及对相关机制的评论。最后,将对其药代动力学特性、生物利用度和配方进行分析。综上所述,该综述表明花青素及其衍生物可能是有效的抗癌药物,但也需要对其生物活性的分子机制有更深入的了解。尽管结果令人鼓舞,但解决稳定性、吸收和靶向分布等问题对于最大限度地发挥其治疗潜力至关重要。需要更多的研究来开发创新的基于花青素的配方,以有效地治疗癌症。
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