Pharmacological Research - Natural Products最新文献_第10页

A review on the ethnopharmacology, anticancer mechanism, toxicity and clinical application of andrographolide isolated from Andrographis paniculata (Burm.f.) Nees 穿心莲（Andrographis paniculata, Burm.f.）穿心莲内酯的民族药理学、抗癌机制、毒性及临床应用综述需要雇

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-18 DOI: 10.1016/j.prenap.2026.100518

Xiaohan Wu , Lee Suan Chua , Khairunadwa Jemon

Andrographis paniculata (Burm. f.) Nees (A. paniculata), commonly known as "King of Bitters," has been widely used in traditional medicine in Asia, primarily for its heat-clearing, detoxifying, anti-inflammatory hepatoprotective properties. Andrographolide (AG), a bioactive compound derived from A. paniculata has been extensively investigated for its anticancer potential. Numerous studies have demonstrated its efficacy across various cancers, highlighting the potential of AG as a promising drug for cancer therapy. This review aims to systematically summarize the ethnopharmacological uses of A. paniculata and its main compound AG, the anticancer mechanisms, preclinical toxicity analysis and clinical therapeutic potential of AG, focusing on its multi-targeted actions across various cancer types and its application in clinical trials. A comprehensive literature survey was conducted using English medium databases from 2015 to 2025. After applied the exclusion and inclusion criteria, 102 articles related to the keywords of “Andrographis paniculata”, “Andrographis paniculata traditional uses”, “andrographolide anticancer”, “andrographolide toxicity and safety”, “andrographolide adverse reactions” and “Andrographolide clinical trial” were compiled for critical review. AG exerts its anticancer effects in animal and different cancer cell lines via various mechanism inducing apoptosis, promoting autophagy, triggering ferroptosis, and arresting the cell cycle, etc. AG is relatively safe compound with less toxicity in vivo and in vitro. The clinical trials and findings for different disease have been investigated and summarized. Andrographolide has the potential to be a promising drug for cancer treatment. The combination with other drugs and natural compounds can improve therapy. The toxicity and clinical trials need further study.

穿心莲f。)苦楝（A. paniculata），俗称“苦楝之王”，在亚洲的传统医学中被广泛使用，主要是因为它具有清热、解毒、抗炎、保护肝脏的特性。穿心莲内酯（Andrographolide， AG）是一种从穿心莲中提取的生物活性化合物，因其抗癌潜力而被广泛研究。许多研究已经证明其对各种癌症的疗效，突出了AG作为一种有前景的癌症治疗药物的潜力。本文系统综述了金针叶及其主要化合物AG的民族药理学作用、抗癌机制、临床前毒性分析和临床治疗潜力，重点介绍了金针叶在不同肿瘤类型中的多靶点作用及其在临床试验中的应用。2015 - 2025年使用英文媒体数据库进行全面的文献调查。应用排除纳入标准，以“穿心莲”、“穿心莲传统用途”、“穿心莲内酯抗癌”、“穿心莲内酯毒性与安全性”、“穿心莲内酯不良反应”、“穿心莲内酯临床试验”为关键词，整理出102篇文献进行批判性评价。AG通过诱导细胞凋亡、促进细胞自噬、触发铁下垂、阻滞细胞周期等多种机制在动物及不同癌细胞系中发挥抗癌作用。AG是一种相对安全的化合物，体内外毒性较小。对不同疾病的临床试验和结果进行了调查和总结。穿心莲内酯有可能成为一种很有前途的癌症治疗药物。与其他药物和天然化合物联合使用可以改善治疗效果。毒性及临床试验有待进一步研究。

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引用次数: 0

An integrated binary classification and machine learning approach to decode curcumin's mitigation of cypermethrin-induced hepatorenal injury: Experimental and computational analysis 综合二进制分类和机器学习方法解码姜黄素减轻氯氰菊酯诱导的肝肾损伤：实验和计算分析

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-27 DOI: 10.1016/j.prenap.2026.100538

Hamid Rehman , Nida Gul , Khurshid Ahmad , Mazhar Iqbal , Aqib Hassan Ali Khan , Rehan Naeem

This study investigated the protective role of Curcuma longa L. extract (curcumin, CMN) against cypermethrin (CYP)-induced hepatic and renal injury in male albino rabbits. Animals were divided into four groups: control, CYP (25 mg kg⁻¹), CMN (50 mg kg⁻¹), and combined CYP + CMN, treated orally for 45 days. CYP administration markedly reduced hepatic and renal antioxidant enzymes, including SOD (47 %), CAT (39 %), and GPx (42 %), while elevating lipid peroxidation (61 %) and serum markers of liver (ALT 2.6-fold, AST 2.3-fold, ALP 2.1-fold) and kidney dysfunction was also increased (urea 58 %, creatinine 52 %). Co-treatment with CMN significantly restored antioxidant enzyme activities toward control levels (p < 0.01), normalized lipid profile indices, and improved histopathological architecture of hepatic and renal tissues. To complement experimental results, a computational regression model was trained on data to identify major predictors of CYP-induced oxidative stress. Binary classification model was developed to distinguish CYP-exposed (toxic) from CMN-protected (non-toxic) conditions using the same biochemical and enzymatic feature set. The classifier achieved outstanding performance, with overall accuracy of 100 %, area under the ROC curve (AUC = 1.0), precision (0.96), and recall (0.94), confirming a clear separation between the two physiological states. The Random forest model showed high predictive accuracy (R² = 0.98, RMSE = 29.20, MAPE = 1.1 %) The most discriminative predictors included SOD, GPX, and VLDL, of liver which consistently ranked among the top features in both regression and classification analyses. These results reinforce the experimental observations that hepatic antioxidant enzymes and lipid-associated parameters serve as reliable biomarkers for distinguishing oxidative injury from curcumin-mediated protection.

研究了姜黄素对氯氰菊酯（CYP）致雄性白化兔肝、肾损伤的保护作用。动物被分为四组：对照组，CYP（25 mg kg⁻¹），CMN（50 mg kg⁻¹）和CYP + CMN联合治疗，口服45天。CYP显著降低肝脏和肾脏抗氧化酶，包括SOD（47 %）、CAT（39 %）和GPx(42 %)，同时升高脂质过氧化（61 %）、肝脏血清标志物（ALT 2.6倍、AST 2.3倍、ALP 2.1倍）和肾功能障碍（尿素58 %、肌酐52 %）。与CMN共同治疗可显著恢复抗氧化酶活性至控制水平（p <； 0.01），使血脂指数正常化，并改善肝和肾组织的组织病理结构。为了补充实验结果，对数据进行了计算回归模型的训练，以确定cypp诱导的氧化应激的主要预测因素。使用相同的生化和酶学特征集，建立了二元分类模型来区分cyp暴露（有毒）和cmn保护（无毒）条件。该分类器表现出色，总体准确率为100 %，ROC曲线下面积（AUC = 1.0），精密度（0.96），召回率（0.94），证实了两种生理状态的明显分离。随机森林模型具有较高的预测准确率（R²= 0.98,RMSE = 29.20, MAPE = 1.1 %），最具判别性的预测因子为肝脏SOD、GPX和VLDL，在回归分析和分类分析中均名列前茅。这些结果加强了实验观察，肝脏抗氧化酶和脂质相关参数可作为区分氧化损伤和姜黄素介导的保护的可靠生物标志物。

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引用次数: 0

Biological and Computational Exploration of Ulva flexuosa: Antioxidant, Anti-inflammatory, Antidiabetic, Antipyretic, and Cytotoxic Insights for Drug Discovery 曲叶草的生物学和计算探索：抗氧化、抗炎、降糖、解热和细胞毒性药物发现的见解

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-25 DOI: 10.1016/j.prenap.2026.100533

Md. Jahirul Islam Mamun , Md. Hossain Rasel , Md. Tanvir Chowdhury , Md. Mahmudul Hasan , Miton Chowdhury , Thamjeed Mohaimeen , Md Anower Kader , Mohammad Wahiduzzaman , Mohammad Forkanul Hamid , S. M. Moazzem Hossen

Over the past decade, Ulva flexuosa, a green tide seaweed, has proliferated in China's Yellow Sea. This study evaluated the pharmacological potential of its acetone extract (AEUF) through in vitro, in vivo, and computational methods. AEUF exhibited moderate to significant antioxidant activity with IC₅₀ values of 194.53 µg/mL (DPPH) and 50.78 µg/mL (ABTS). It showed notable anti-inflammatory effects in both HRBC membrane stabilization and carrageenan-induced paw edema models. For antidiabetic assessment, AEUF demonstrated strong α-amylase inhibition (IC₅₀ = 65.9 µg/mL) and significant hypoglycemic activity (p < 0.001) in the oral glucose tolerance test (OGTT). Cytotoxicity evaluation via brine shrimp lethality assay revealed mild toxicity (LC₅₀ = 407.24 µg/mL), indicating a favorable safety profile. Molecular docking, PASS prediction, and ADME/T analyses supported the experimental results, highlighting the bioactive compounds’ binding affinity and drug-like properties. Overall, AEUF displays promising antioxidant, anti-inflammatory, antidiabetic, and hypoglycemic activities, with low cytotoxicity. These findings suggest that U. flexuosa is a valuable natural resource with significant pharmacological potential, particularly for managing oxidative stress, inflammation, and diabetes. Further studies are warranted to isolate active constituents and explore their mechanisms of action. This work underscores the importance of underutilized marine algae as a source of novel therapeutic agents.

在过去的十年里，绿潮藻弯尾藻在中国的黄海大量繁殖。本研究通过体外、体内和计算方法评价其丙酮提取物（AEUF）的药理潜力。AEUF具有中等到显著的抗氧化活性，IC₅₀值为194.53 µg/mL （DPPH）和50.78 µg/mL （ABTS）。在HRBC膜稳定和卡拉胶诱导的足跖水肿模型中均显示出明显的抗炎作用。在抗糖尿病评估中，AEUF在口服葡萄糖耐量试验（OGTT）中表现出强烈的α-淀粉酶抑制作用（IC₅₀= 65.9 µg/mL）和显著的降糖活性（p <； 0.001）。通过卤虾致死试验进行的细胞毒性评估显示毒性轻微（LC₅₀= 407.24 µg/mL），表明具有良好的安全性。分子对接、PASS预测和ADME/T分析支持实验结果，突出了生物活性化合物的结合亲和力和药物样特性。总之，AEUF具有良好的抗氧化、抗炎、抗糖尿病和降糖活性，并且具有较低的细胞毒性。这些研究结果表明，屈曲霉是一种有价值的天然资源，具有重要的药理潜力，特别是在控制氧化应激、炎症和糖尿病方面。进一步的研究是必要的，以分离有效成分和探索其作用机制。这项工作强调了未充分利用的海藻作为新型治疗剂来源的重要性。

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引用次数: 0

Integrated phytochemical, pharmacokinetic, and molecular docking analysis reveals Ficus religiosa seed extract as a multi-target inhibitor of calcium oxalate crystallization in urolithiasis 综合植物化学、药代动力学和分子对接分析显示，榕树种子提取物是尿石症中草酸钙结晶的多靶点抑制剂

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-02-03 DOI: 10.1016/j.prenap.2026.100552

Felicity Pinipay , Rajesh Rokkam , Satyanarayana Botcha , Raghava Rao Tamanam

Urolithiasis is a prevalent global health concern and third most common urinary disorder, with calcium oxalate (CaOx) stones representing the most common and therapeutically challenging form. The limitations of current treatments necessitate the exploration of safer phytotherapeutic alternatives. Based on prior antioxidant and in silico evidence, the present study evaluated the in-vitro antiurolithiatic potential of organic solvent extracts of Ficus religiosa seeds. The extracts were assessed for inhibition of CaOx nucleation, aggregation, and crystal growth, using Cystone as the reference standard. Among the tested extracts, the ethyl acetate extract exhibited the highest inhibitory activity, with 56.78 % nucleation inhibition, 71.34 % aggregation inhibition, and 70.69 % crystal growth inhibition at 500 µg/mL. Microscopic analysis revealed a dose-dependent reduction in crystal size and a shift from calcium oxalate monohydrate to the less adherent dihydrate form. LC-MS analysis of the ethyl acetate extract identified bioactive phytochemicals, which demonstrated favourable pharmacokinetic properties in ADMET profiling. Molecular docking further revealed strong binding affinities of top-performing phytochemicals, particularly apigenin, toward urolithiasis-related targets annexin II, α-enolase, and nucleolin. Overall, F. religiosa seed extracts, especially the ethyl acetate extract, exhibit promising antiurolithiatic potential and warrant further in-vivo and clinical investigations.

尿石症是全球普遍存在的健康问题，也是第三大常见泌尿系统疾病，草酸钙结石是最常见和治疗上最具挑战性的形式。当前治疗方法的局限性需要探索更安全的植物治疗替代品。基于已有的抗氧化和硅证据，本研究评估了榕种子有机溶剂提取物的体外抗尿石潜力。以Cystone为参比标准品，评价提取物对CaOx成核、聚集和晶体生长的抑制作用。其中，在500 µg/mL浓度下，乙酸乙酯对成核的抑制率为56.78 %，对聚集的抑制率为71.34 %，对晶体生长的抑制率为70.69 %。显微分析显示晶体大小的剂量依赖性减少，从一水草酸钙转变为较不粘连的二水形式。乙酸乙酯提取物的LC-MS分析鉴定出具有生物活性的植物化学物质，在ADMET分析中显示出良好的药代动力学特性。分子对接进一步揭示了表现最好的植物化学物质，特别是芹菜素，对尿石症相关靶标膜联蛋白II、α-烯醇酶和核蛋白具有很强的结合亲和力。总的来说，宗教花种子提取物，特别是乙酸乙酯提取物，显示出有希望的抗尿石潜力，值得进一步的体内和临床研究。

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引用次数: 0

Bioprospecting diverse natural product components as potential source of proton pump inhibitors: A systematic review 生物勘探多种天然产物成分作为质子泵抑制剂的潜在来源：系统综述

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-11 DOI: 10.1016/j.prenap.2026.100505

Partha Pratim Thakuria , Bedanta Bhattacharjee , Shatabdi Ghose , Lima Patowary , Junmoni Nath , Dinesh Kumar Patel , Ghanshyam R. Parmar , Damiki Laloo

Despite advances in modern therapy, gastro-duodenal ulcers, due to their recurrence and relapse, remains one of the most common health issues in the world, posing considerable therapeutic challenges. This issue is further exacerbated by the adverse effects associated with conventional therapy, particularly proton pump inhibitors (PPIs). Although PPIs are widely prescribed drugs for the management of gastric ulcers owing to their proven efficacy and therapeutic benefits, their prolonged use has been linked to a variety of health risks. This review aimed to present a comprehensive information on natural compounds with H⁺,K⁺-ATPase inhibitory activity, supported by database evidence from in vitro, in vivo and in silico studies. A comprehensive and systematic literature search, conducted by PRISMA guidelines, identified 36 potential natural substances derived from plants, marines (sponges, corals etc.), and microorganisms that exhibited inhibitory effects on H⁺,K⁺-ATPase. In conclusion, findings from the current review indicate that natural products may offer considerable potential as proton pump inhibitors for treating gastro-duodenal ulcers. However, further extensive research and clinical assessments are necessary to facilitate the development of safe, effective and sustainable natural compounds for future clinical management of gastric ulcer.

尽管现代治疗取得了进步，但胃-十二指肠溃疡由于其复发和复发，仍然是世界上最常见的健康问题之一，对治疗提出了相当大的挑战。常规治疗，特别是质子泵抑制剂（PPIs）的副作用进一步加剧了这一问题。虽然质子泵抑制剂因其已被证实的疗效和治疗益处而被广泛用于治疗胃溃疡，但长期使用与各种健康风险有关。该综述旨在提供具有H +、K + - atp酶抑制活性的天然化合物的全面信息，并得到体外、体内和计算机研究的数据库证据的支持。根据PRISMA指南进行了全面、系统的文献检索，发现了36种来自植物、海洋生物（海绵、珊瑚等）和微生物的潜在天然物质，这些物质对H +、K + - atp酶具有抑制作用。总之，目前的研究结果表明，天然产物作为质子泵抑制剂治疗胃-十二指肠溃疡可能具有相当大的潜力。然而，需要进一步的广泛研究和临床评估，以促进开发安全、有效和可持续的天然化合物，用于未来的胃溃疡临床治疗。

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引用次数: 0

Neuroprotective potential of Gerbera lanuginosa phytochemicals through multitarget modulation of DYRK1A, BACE1, and GABA-A in down syndrome 通过多靶点调节DYRK1A、BACE1和GABA-A对唐氏综合征患者的神经保护作用

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-10 DOI: 10.1016/j.prenap.2026.100500

Nitya Krishnasamy

Background

Down-syndrome-related neurodegeneration involves simultaneous dysregulation of DYRK1A-mediated tau phosphorylation, BACE1-driven amyloidogenesis, and GABA-A imbalance. Natural multitarget modulators could offer superior neuroprotection.

Methods

Five Gerbera lanuginosa phytochemicals (taraxerol, taraxerol acetate, gerberinol, scopoletin, and coumarin) were evaluated against DYRK1A (PDB 4AZE), BACE1 (4COF), and GABRA1 (5HU1) using AutoDock 4.2, PyMOL, and Discovery Studio 2023. ADMET and Boiled-Egg models (SwissADME, pkCSM) assessed pharmacokinetics; protein–protein interactions (STRING v12, Cytoscape 3.9.1) mapped functional links; and 100-ns GROMACS molecular-dynamics with MMPBSA free-energy estimation validated complex stability.

Results

Taraxerol and taraxerol acetate displayed the strongest affinities (−10.1 and −9.6 kcal/mol) for DYRK1A/BACE1, while gerberinol bound GABRA1 (−8.3 kcal/mol). Boiled-Egg analysis predicted high GI absorption and moderate BBB permeability. MD trajectories maintained RMSD < 2 Å with binding energies ≈ −72 to −60 kJ mol⁻¹ . Network-pharmacology revealed high-degree centrality of taraxerol connecting kinase, secretase, and receptor pathways.

Conclusion

G. lanuginosa triterpenoids exhibit stable multitarget inhibition of DYRK1A, BACE1, and GABA-A, favorable pharmacokinetics, and mechanistic coherence, positioning them as lead scaffolds for developing neuroprotective therapeutics in Down-syndrome-associated cognitive decline.

背景：唐氏综合征相关的神经退行性变包括dyrk1a介导的tau磷酸化、bace1驱动的淀粉样蛋白形成和GABA-A失衡的同时失调。天然多靶点调节剂可以提供更好的神经保护。方法采用AutoDock 4.2、PyMOL和Discovery Studio 2023对5种非洲菊植物化学物质（taraxerol、taraxerol acetate、gerberinol、东莨菪碱和香豆素）对DYRK1A （PDB 4AZE）、BACE1 （4COF）和GABRA1 （5HU1）的抗性进行检测。ADMET和煮蛋模型（SwissADME, pkCSM）评估药代动力学；蛋白-蛋白相互作用（STRING v12, Cytoscape 3.9.1）映射的功能链接；100-ns GROMACS分子动力学与MMPBSA自由能估计验证了配合物的稳定性。结果staraxerol和taraxerol醋酸酯对DYRK1A/BACE1的亲和力最强（−10.1和−9.6 kcal/mol），而gerberinol对GABRA1的亲和力最强（−8.3 kcal/mol）。煮蛋分析预测高GI吸收和中度血脑屏障通透性。MD轨迹保持RMSD <； 2 Å，结合能≈ −72至−60 kJ mol⁻¹ 。网络药理学研究显示，taraxerol连接激酶、分泌酶和受体通路具有高度的中心性。杉木三萜对DYRK1A、BACE1和GABA-A具有稳定的多靶点抑制作用，良好的药代动力学和机制一致性，使其成为开发唐氏综合征相关认知衰退神经保护疗法的先导支架。

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引用次数: 0

Ethnopharmacological survey of local medicinal plants used against schistosomiasis in the Moungo division, littoral region of Cameroon: Cercaricidal, antioxidant and anti-inflammatory activities, cytotoxicity and phytochemical profile of some selected plants 喀麦隆沿海地区蒙戈省用于治疗血吸虫病的当地药用植物的民族药理学调查：某些选定植物的杀虫、抗氧化和抗炎活性、细胞毒性和植物化学特征

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-06 DOI: 10.1016/j.prenap.2026.100492

Dongmo Nguepi Mireille Sylviane , Ngachou Nebot Floride , Tincho Marius Belmondo , Itoe Ubre Sicca , Noubissi Paul Aime , Dongmo Nanfack Christelle , Madjougne Foudjo Domiriane Ornela , Dize Darline , Woutouoba Ntieche David , Wendji Monkam Diana Sandra , Sofeu Feugaing David Denis , Ayiseh Rene Bilingwe , Ghogomu Stephen Mbigha

Introduction

Schistosomiasis, a neglected tropical disease remains a major public health challenge in sub-Saharan Africa despite widespread use of Praziquantel. In Cameroon, various remedies are traditionally employed for treatment. This study aimed to document such remedies in Loum and Njombe-Penja and evaluate their biological activities against Schistosoma mansoni, with the goal of identifying affordable, community-based antischistosomal agents.

Methods

An ethnobotanical survey conducted in Loum and Njombe Penja identified 11 herbalists who reported nine medicinal plants from seven families. The Euphorbiaceae family was most represented, and Euphorbia hirta, Euphorbia prostrata, and Alchornea cordifolia were selected for further analysis. Cercaricidal activity was assessed by exposing S. mansoni cercariae to plant extracts (0.4 – 250 µg/ml). Antioxidant potential was evaluated using DPPH and FRAP assays, while anti-inflammatory activity was measured via albumin denaturation inhibition. Cytotoxicity was tested on LLC-MK2 cells, and phytochemical composition was analyzed using LC-MS and HPLC-UV-ESI-TOF-MS.

Results

Methanolic and hexane extracts of E. hirta showed most potent cercaricidal activity with LC₅₀ values of 0.07569 and 0.7994 µg/ml, respectively. E. hirta and A. cordifolia showed strong radical scavenging potential (SC₅₀: 0.3012 – 203.7 µg/ml). A dose-dependent inhibition of albumin denaturation, with plant extracts outperforming Diclofenac at low concentrations was observed. Cytotoxicity assays indicated low toxicity (IC₅₀: 325.7 – 550.8 µg/ml). The Phytochemical screenings identified metabolites as polyphenols, terpenoids, and steroids.

Conclusion

These findings suggest that E. hirta, E. prostrata, and A. cordifolia possess cercaricidal, antioxidant, and anti-inflammatory properties. Their rich phytochemical profiles support their potential as effective, low-toxicity antischistosomal remedies suitable for integration into primary health care systems in endemic regions

血吸虫病是一种被忽视的热带病，尽管吡喹酮被广泛使用，但在撒哈拉以南非洲仍是一项重大的公共卫生挑战。在喀麦隆，传统上采用各种疗法进行治疗。本研究旨在记录Loum和Njombe-Penja的这些药物，并评估它们对曼氏血吸虫的生物活性，目的是确定负担得起的、基于社区的抗血吸虫药物。方法在卢姆和恩琼贝Penja进行民族植物学调查，鉴定了11名草药医师，他们报告了7科9种药用植物。以大戟科植物为代表，选取大戟属（Euphorbia hirta）、大戟属（Euphorbia prostrata）和大戟属（Alchornea cordifolia）进行分析。将曼氏尾蚴暴露于植物提取物（0.4 - 250 µg/ml）中，评估其杀灭尾蚴的活性。通过DPPH和FRAP测定抗氧化潜力，通过白蛋白变性抑制测定抗炎活性。采用LC-MS和HPLC-UV-ESI-TOF-MS对lc - mk2细胞进行细胞毒性检测和植物化学成分分析。结果香茅的甲醇和己烷提取物具有最强的杀菌活性，LC₅0值分别为0.07569和0.7994 µg/ml。E. hirta和A. cordifolia显示出很强的自由基清除潜力（SC₅₀：0.3012 - 203.7 µg/ml）。剂量依赖性抑制白蛋白变性，植物提取物在低浓度下优于双氯芬酸。细胞毒性试验表明毒性较低（IC₅₀：325.7 - 550.8 µg/ml）。植物化学筛选鉴定代谢物为多酚、萜类和类固醇。结论hirta、proprota和cordifolia具有抗氧化、抗炎和杀虫作用。其丰富的植物化学特征支持其作为有效、低毒性抗血吸虫药物的潜力，适合纳入流行地区的初级卫生保健系统

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引用次数: 0

Deciphering the phytochemical and pharmacological potential of Syzygium grande (Wight) Walp. through in vivo, in vitro, and computational approaches 解读大白穗的植物化学和药理潜力。通过体内，体外和计算方法

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-13 DOI: 10.1016/j.prenap.2026.100509

Md. Jahirul Islam Mamun , Sifatul Islam Mizan , Mahathir Mohammad , Md. Hossain Rasel , Mohi Uddin

Syzygium grande (Wight) Walp., a member of the Myrtaceae family, has been traditionally used to address various health conditions. This research aimed to assess the phytochemical composition and the potential antioxidant, anti-inflammatory, antidiabetic, and thrombolytic properties of the methanolic leaf extract of S. grande (MESG). MESG exhibited mild antioxidant activity in the DPPH assay, with an IC₅₀ value of 238 µg/mL, compared to the standard ascorbic acid (IC₅₀ = 95.85 µg/mL). However, it was less potent than the reference ascorbic acid, which had an IC₅₀ value of 95.85 µg/mL. MESG at 200 mg/kg significantly (p < 0.001) reduced ear edema in mice compared to the control in the xylene-induced ear edema test (78.89 % inhibition). The extract also exhibited notable anti-inflammatory effects, with 73.12 ± 0.98 % protection at 1000 µg/mL in the HRBC test and an IC₅₀ value of 246.67 µg/mL in the protein denaturation assay. MESG showed a strong antidiabetic effect in the alpha-amylase inhibitory test, with an IC₅₀ value of 51.22 µg/mL, compared to the reference acarbose (IC₅₀ = 36.95 µg/mL). Furthermore, the extract displayed considerable thrombolytic activity, achieving 65.2 ± 4.66 % clot lysis in the human blood clot lysis test. Molecular docking studies provided further support for our findings, confirming the predicted interactions and binding affinities of the identified compounds with their respective target proteins. These results indicate that MESG may have potential applications in addressing oxidative stress, inflammation, diabetes, and thrombosis-related conditions. However, further research is necessary to confirm these outcomes and explore their therapeutic potential.

大（重）臀。是桃金娘科的一员，传统上被用来治疗各种健康问题。摘要本研究旨在研究大叶青醇提物（MESG）的植物化学成分及其潜在的抗氧化、抗炎、抗糖尿病和溶栓活性。与标准抗坏血酸（IC50 = 95.85 µg/mL）相比，MESG在DPPH实验中表现出温和的抗氧化活性，IC50值为238 µg/mL。但IC50值为95.85 µg/mL，低于对照抗坏血酸。在二甲苯诱导的耳部水肿试验中，与对照组相比，200 mg/kg的MESG显著（p <； 0.001）减少了小鼠的耳部水肿（抑制率为78.89 %）。该提取物还具有显著的抗炎作用，在1000 µg/mL的HRBC试验中，其保护作用为73.12 ± 0.98 %，在蛋白质变性试验中，其IC50值为246.67 µg/mL。MESG在α -淀粉酶抑制试验中显示出较强的降糖作用，IC50值为51.22 µg/mL，而对照品阿卡波糖的IC50值为36.95 µg/mL。此外，提取物显示出相当大的溶栓活性，在人血凝块溶解试验中达到65.2 ± 4.66 %的凝块溶解。分子对接研究为我们的发现提供了进一步的支持，证实了所鉴定的化合物与各自靶蛋白的预测相互作用和结合亲和力。这些结果表明，MESG可能在解决氧化应激、炎症、糖尿病和血栓相关疾病方面有潜在的应用。然而，需要进一步的研究来证实这些结果并探索其治疗潜力。

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引用次数: 0

Comprehensive evaluation of isogarcinol from Garcinia cambogia: Extraction, characterization, and docking-based insights into anti-hyperlipidemic potential via HMG-CoA reductase inhibition 从黄藤中提取的异氨基酚的综合评价：提取、表征和通过HMG-CoA还原酶抑制抗高脂血症潜力的对接

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2025-12-15 DOI: 10.1016/j.prenap.2025.100463

N. Surendra Chowdary , Rajeshwari S , Suresh J , B.M. Gurupadayya , Erica Alves

This study presents a comprehensive evaluation of isogarcinol extracted from Garcinia cambogia for its anti-hyperlipidemic potential targeting 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Sequential aqueous and n-hexane extraction followed by column chromatography yielded 4 % w/w pure isogarcinol crystals, confirmed by TLC (Rf = 0.69), FT-IR, ¹H/¹ ³C NMR, MS (m/z 603.4 [M + H]⁺), and HPLC analysis. The compound showed a retention time of 5.43 min with excellent linearity in the range of  mL⁻¹ (R² = 0.9927). Validation according to ICH Q2(R2) demonstrated high precision (%RSD < 0.5 %), accuracy (99.2–102.0 % recovery), robustness (%RSD < 0.3 %), and a limit of detection/quantification of 0.216 µg mL⁻¹ and 0.655 µg mL⁻¹ , respectively. Forced-degradation studies indicated limited degradation (< 17 %) under acid, alkali, oxidative, photolytic, and thermal stress. Molecular docking revealed a Glide score of –5.3 kcal mol⁻¹ for isogarcinol versus –5.6 kcal mol⁻¹ for the reference drug fenofibrate, with stable hydrogen-bond interactions involving Tyr479, Asn529, Asn567, and Ala478. MM-GBSA free-energy calculations indicated a total ΔG_bind of –0.49 kcal mol⁻¹ for isogarcinol and –41.16 kcal mol⁻¹ for fenofibrate, while 100 ns molecular dynamics simulations confirmed complex stability (RMSD < 0.7 Å). These findings collectively establish isogarcinol as a computationally and experimentally validated natural scaffold with potential lipid-lowering activity meriting further in-vitro and in-vivo investigation.

本研究综合评价了从藤黄果中提取的异丙二醇对3-羟基-3-甲基戊二酰辅酶a （HMG-CoA）还原酶的抗高脂血症潜力。通过TLC （Rf = 0.69）、FT-IR、¹H/¹ ³C NMR、MS （m/z 603.4 [m + H] +）和HPLC验证，得到4 % w/w纯异己醇晶体。该化合物在 mL⁻¹ 范围内呈良好的线性关系（R²= 0.9927），保留时间为5.43 min。验证据我Q2 (R2)演示了高精度(% RSD = & lt; 0.5 %),精度(99.2 - -102.0 %恢复),鲁棒性(% RSD = & lt; 0.3 %),和一个检测极限/量化0.216 µg 毫升⁻¹ 和0.655 µg 毫升⁻¹ ,分别。强制降解研究表明，在酸、碱、氧化、光解和热胁迫下，降解有限（< 17 %）。分子对接发现，异氨基甲酸酯的Glide分数为-5.3 kcal mol⁻¹ ，对照药物非诺贝特的为-5.6 kcal mol⁻¹ ，与Tyr479、Asn529、Asn567和Ala478有稳定的氢键相互作用。MM-GBSA自由能计算表明总Δ G_bind -0.49千卡 摩尔⁻¹ isogarcinol为-41.16 千卡 摩尔⁻¹ 非诺贝特,而100 ns分子动力学模拟证实了复杂的稳定(RMSD & lt; 0.7 )。这些发现共同建立了异氨基甲酸酯作为一种计算和实验验证的天然支架，具有潜在的降脂活性，值得进一步的体外和体内研究。

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引用次数: 0

Curcumin supplementation mitigates renal dysfunction via enhanced glucose metabolism and inflammatory regulation in alloxan-induced diabetic rats 姜黄素补充剂通过增强葡萄糖代谢和炎症调节来减轻四氧嘧啶诱导的糖尿病大鼠的肾功能障碍

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2025-12-15 DOI: 10.1016/j.prenap.2025.100464

Igbayilola Yusuff Dimeji , Saka Waidi Adeoye , Hamidu Lawan Jabba , Ngabea Murtala Audu , Adekola Saheed Ayodeji , Aina Olawale Samson , Agunbiade Mercy Oluwaseyi , Lawal Abdulmujeeb Abodunrin

Diabetic kidney disease (DKD), a major cause of end-stage renal disease, affects 30–40 % of individuals with diabetes, a condition projected to impact 783 million people by 2025. This study investigated the effects of curcumin supplementation on renal function and glucose metabolism in alloxan-induced diabetic male Wistar rats. Forty-five rats (150–200 g) were divided into five groups (n = 9): Group A (Control), Group B (Alloxan only), Group C (Alloxan + Metformin), Group D (Alloxan + Curcumin), and Group E (Curcumin only). Diabetes was induced by alloxan (150 mg/kg, intraperitoneally), and blood glucose levels were monitored after 72 h. Groups C, D, and E received metformin (100 mg/kg) or curcumin (100 mg/kg) daily for 4 weeks. Posttreatment, fasting blood samples were collected to assess blood glucose, insulin, and renal function markers, including serum urea, creatinine, and electrolytes (Na+, K+, Clˉ, and HCO3ˉ). Additionally, glucose metabolic enzymes—hexokinase, fructokinase, and pyruvate kinase—were analysed in liver and muscle tissues. The results revealed that alloxan-induced diabetes significantly elevated the serum urea, creatinine, and electrolytes. Curcumin treatment significantly reduced these markers and corrected electrolyte imbalances. It also increased glucose metabolic enzyme activities, increased GLUT4 protein expression in muscle tissues, and reduced insulin resistance, as indicated by the HOMA-IR scores. These findings suggest that curcumin supplementation improves glucose metabolism, reduces inflammation, and preserves renal function, making it a potential therapeutic approach for diabetic nephropathy and an adjuvant for diabetes treatment.

糖尿病肾病（DKD）是终末期肾病的主要病因，影响着30 - 40% %的糖尿病患者，预计到2025年糖尿病患者将达到7.83亿人。本研究探讨了补充姜黄素对四氧嘧啶诱导的糖尿病雄性Wistar大鼠肾功能和葡萄糖代谢的影响。将45只（150 ~ 200 g）大鼠分为5组（n = 9）：A组（对照组）、B组（单药四氧嘧啶）、C组（单药四氧嘧啶+二甲双胍）、D组（单药四氧嘧啶+姜黄素）、E组（单药姜黄素）。四氧嘧啶（150 mg/kg，腹腔注射）诱导糖尿病，72 h后监测血糖水平。C、D、E组每日给予二甲双胍（100 mg/kg）或姜黄素（100 mg/kg）治疗，连续4周。治疗后，采集空腹血液样本，评估血糖、胰岛素和肾功能指标，包括血清尿素、肌酐和电解质（Na+、K+、Cl - h和HCO3 - h）。此外，葡萄糖代谢酶——己糖激酶、果糖激酶和丙酮酸激酶——在肝脏和肌肉组织中被分析。结果显示，四氧嘧啶诱导的糖尿病显著升高血清尿素、肌酐和电解质。姜黄素治疗显著降低了这些指标并纠正了电解质失衡。HOMA-IR评分显示，它还能提高葡萄糖代谢酶活性，增加肌肉组织中GLUT4蛋白的表达，降低胰岛素抵抗。这些发现表明，补充姜黄素可以改善葡萄糖代谢，减少炎症，并保持肾功能，使其成为糖尿病肾病的潜在治疗方法和糖尿病治疗的辅助手段。

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引用次数: 0