Pharmacological Research - Natural Products最新文献_第4页

Seasonal variation in phytochemical composition, quantitative analysis, and antioxidant activity of bulb extract from Urginea indica (Roxb.) Kunth 印楝球茎提取物植物化学成分、定量分析及抗氧化活性的季节变化肯

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-22 DOI: 10.1016/j.prenap.2026.100529

Uday Sahu , Shriram Kunjam

Background

Urginea indica (Roxb.) Kunth is an important medicinal geophyte that has been traditionally used to treat a wide range of ailments, particularly cardiac and respiratory disorders. Its therapeutic value is largely attributed to the rich diversity of bioactive secondary metabolites present in the plant.

Aim

The aim of this study is to investigate the seasonal effect in the phytochemical constituents of the bulb of Urginea indica (Roxb.) Kunth, both qualitatively and quantitatively, as well as the antioxidant activity of the methanolic plant extract.

Materials and methods

In this study, bulb samples were collected across three distinct seasons (rainy, winter, and summer) and then extracted using aqueous, acetone, and methanol solvents through the Soxhlet apparatus. The antioxidant activity was analyzed by the DPPH assay.

Results

Quantitative analysis revealed that phenolic (3.799 mg GAE/g) and flavonoid (0.922 mg QE/g) contents were highest in winter, followed by summer (1.550 mg GAE/g and 0.800 mg QE/g, respectively), and their lowest concentrations in the rainy season (0.547 mg GAE/g and 0.405 mg QE/g). On the other hand, steroid (7.6 µg/g) and alkaloid (43.94 %) content were highest in the rainy season, reflecting their role in plant defense and growth. Antioxidant activity, determined by the DPPH assay, was concentration-dependent, scavenging activity with the methanolic extract having an IC₅₀ value of 584.172 µg/ml, although less potent than ascorbic acid (IC₅₀ = 36.961 µg/ml). The observed activity supports the potential medicinal relevance of U. indica as a natural source of bioactive compounds.

Conclusion

This research highlights the seasonal and solvent-dependent variation in the distribution of bioactive compounds in U. indica bulbs, indicating their potent antioxidant activity and potential medicinal value.

背景：紫荆（Roxb.）Kunth是一种重要的药用地植物，传统上用于治疗各种疾病，特别是心脏和呼吸系统疾病。其治疗价值很大程度上归因于植物中存在的丰富多样的生物活性次生代谢物。目的研究不同季节对印楝球茎植物化学成分的影响。在定性和定量上，以及对植物甲醇提取物的抗氧化活性进行了研究。材料和方法在本研究中，球茎样品在三个不同的季节（雨季、冬季和夏季）采集，然后通过索氏装置用水溶液、丙酮和甲醇溶剂提取。DPPH法测定其抗氧化活性。结果结果表明，冬小麦中酚类（3.799 mg GAE/g）和黄酮类（0.922 mg QE/g）含量最高，夏季次之（分别为1.550 mg GAE/g和0.800 mg QE/g），雨季最低（0.547 mg GAE/g和0.405 mg QE/g）。另一方面，类固醇（7.6 µg/g）和生物碱（43.94 %）含量在雨季最高，反映了它们在植物防御和生长中的作用。DPPH测定的抗氧化活性与浓度有关，甲醇提取物的清除活性IC50值为584.172 µg/ml，但不如抗坏血酸（IC50 = 36.961 µg/ml）。所观察到的活性支持作为生物活性化合物的天然来源的潜在药用价值。结论本研究揭示了籼稻鳞茎中生物活性物质分布的季节和溶剂依赖性，表明其具有较强的抗氧化活性和潜在的药用价值。

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引用次数: 0

Phytoconstituents of Centella asiatica (L.) as dual BACE1 and AChE inhibitors: An in silico molecular interaction approach for Alzheimer’s disease therapy 积雪草植物成分作为BACE1和AChE双抑制剂：一种用于阿尔茨海默病治疗的硅分子相互作用方法

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-13 DOI: 10.1016/j.prenap.2026.100506

Renuka Ekka, Bharti Ahirwar, Sumathi Poleboina

Background

Alzheimer’s disease (AD) is characterized by cognitive decline and behavioural impairments, with β-amyloid (Aβ) plaque accumulation and cholinergic dysfunction as key pathological features. Targeting β-secretase (BACE1) and acetylcholinesterase (AChE) represents a promising therapeutic strategy.

Aim

This study aimed to evaluate selected phytoconstituents from Centella asiatica, including madecassoside, madecassic acid, asiaticoside, asiatic acid, luteolin, rutin, naringin, and stigmasterol, as potential dual inhibitors of BACE1 and AChE using computational methods.

Material and methods

Molecular docking was performed against AChE and BACE1, followed by interaction analysis using Discovery Studio and LigPlot+ . Drug-likeness and pharmacokinetic properties were predicted using SwissADME and related in silico tools.

Results

Luteolin, madecassoside, and asiatic acid demonstrated the strongest binding affinities with both targets, supported by stable hydrogen bonding and hydrophobic interactions. Most compounds showed favorable ADMET characteristics, including good oral bioavailability, BBB permeability, and low toxicity.

Conclusion

This is the first comprehensive in silico evaluation of Centella asiatica phytoconstituents as dual BACE1 and AChE inhibitors. The findings suggest that these compounds hold potential as neuroprotective scaffolds for AD therapy, warranting further experimental validation.

阿尔茨海默病（AD）以认知能力下降和行为障碍为特征，β-淀粉样蛋白（Aβ）斑块积聚和胆碱能功能障碍是主要病理特征。靶向β-分泌酶（BACE1）和乙酰胆碱酯酶（AChE）是一种很有前景的治疗策略。目的本研究旨在通过计算方法评价积雪草中提取的植物成分，包括马鞭草苷、马鞭草酸、积雪草苷、积雪草酸、木犀草素、芦丁、柚皮苷和豆甾醇作为BACE1和AChE的潜在双重抑制剂。材料和方法对AChE和BACE1进行分子对接，然后使用Discovery Studio和LigPlot+ 进行相互作用分析。使用SwissADME和相关的硅工具预测药物相似性和药代动力学性质。结果石首草苷、马齿苋苷和亚细亚酸在稳定的氢键和疏水相互作用的支持下，与两个靶点的结合亲和性最强。大多数化合物表现出良好的ADMET特性，包括良好的口服生物利用度、血脑屏障通透性和低毒性。结论本研究首次对积雪草植物成分作为BACE1和AChE双抑制剂进行了计算机综合评价。研究结果表明，这些化合物具有作为AD治疗的神经保护支架的潜力，需要进一步的实验验证。

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引用次数: 0

Effect of gamma radiation on physical properties, chemical composition and antibacterial activity of the essential oil from Eucalyptus pellita F. Muell. 伽玛辐射对蓝桉精油物理性质、化学成分及抗菌活性的影响。

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-25 DOI: 10.1016/j.prenap.2026.100534

Yelina González Pérez , Ivan García-Fornaris , Daniel Milian Pérez , Abel Gámez Rodríguez , Raquel Milani , Antonio Celso Dantas Antonino , Yaicel Ge Proenza

The essential oils (EOs) from Eucalyptus species have high contents of oxygenated monoterpenes, demonstrated important antibacterial properties and are widely used in the pharmaceutical, cosmetic, and food industries. However, the stability and efficacy of EOs can be affected by environmental factors, such as exposure to radiation. The present study investigates the impact of gamma radiation on the chemical composition, physical properties and antibacterial activity of the essential oil (EO) from the leaves of Eucalyptus pellita F. Muell. The EO was extracted by hydro-distillation and analyzed by gas chromatography coupled mass spectrometry before and after exposure to 5–25 kGy of gamma radiation. The antibacterial activity of the EO was evaluated against two Gram-negative (G–), and two Gram-positive (G+) bacterial strains by the disk diffusion method. The gamma irradiation at the tested doses induced significant changes in the EO: reduction in monoterpenes such as eucalyptol and α-pinene, increase in sesquiterpenes, appearance of oxygenated compounds derived from radiolysis, and a notable increase in the density and refraction index. These modifications are further reflected in the antibacterial efficacy of the EO. The diameter of inhibition of the EO against the G– bacterial strains expands from average 9.9 to 13.2 ± 0.6 mm, and decreases from average 22.0 to 18.3 ± 0.8 mm against the G+ strains. These findings suggest that gamma radiation may be used to handle composition and antimicrobial properties of EOs for potential applications.

桉树精油富含氧合单萜烯，具有重要的抗菌性能，广泛应用于制药、化妆品和食品行业。然而，EOs的稳定性和有效性可能受到环境因素的影响，例如暴露于辐射。研究了伽玛辐射对桉叶精油化学成分、物理性质和抑菌活性的影响。在5-25 kGy γ射线照射前后，采用水蒸气蒸馏法提取EO，气相色谱耦合质谱法分析EO。采用纸片扩散法对2株革兰氏阴性菌（G -）和2株革兰氏阳性菌（G+）进行抑菌活性评价。在测试剂量下的伽马辐照引起了EO的显著变化：单萜烯（如桉树醇和α-蒎烯）减少，倍半萜烯增加，辐射分解产生的含氧化合物的出现，密度和折射率显著增加。这些修饰进一步体现在EO的抗菌效果上。EO对G -菌株的抑制直径从平均9.9增大到13.2 ± 0.6 mm，对G+菌株的抑制直径从平均22.0减小到18.3 ± 0.8 mm。这些发现表明，伽马辐射可用于处理EOs的组成和抗菌特性，具有潜在的应用价值。

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引用次数: 0

Quercetin and its derivatives as potent inhibitors of PilA protein of Streptococcus sanguinis: An in silico approach to combat infective endocarditis 槲皮素及其衍生物作为血链球菌PilA蛋白的有效抑制剂：对抗感染性心内膜炎的计算机方法

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-05 DOI: 10.1016/j.prenap.2026.100496

Bibhu Prasad Rath , Aurobinda Rout , Snehasish Mishra , Chandana Mohanty

Streptococcus sanguinis (S. sanguinis) is a leading cause of infective endocarditis (IE) that cause a wide range of clinical manifestations including death. It utilizes the PilA protein (a key component of type IV pili) to mediate strong adhesion and biofilm formation in heart tissues. Such biofilms exhibit resistance to traditional antibiotics like penicillin G and vancomycin. The standard treatment with these antibiotics are often ineffective owing to poor biofilm penetration leading to persistent infection and antibiotic resistance. Therefore, targeting PilA offers a potential strategy for disrupting biofilm formation and enhancement of IE treatment. The present in silico study is designed to evaluate Quercetin and its derivatives as a safer and alternative strategy to combat S. sanguinis-mediated biofilm formation. Molecular docking analyses demonstrated that Quercetin (-6.5 kcal/mol) and 8-prenylquercetin (-6.6 kcal/mol) exhibited stronger binding to the PilA protein of S. sanguinis compared to Penicillin G (-6.5 kcal/mol), indicating their superior potential in disrupting biofilm formation. Dynamic simulation further confirmed the stability of these complexes over time, suggesting persistent interaction with the target site. Pharmacokinetic evaluation also revealed favourable absorption, distribution, and metabolic properties, while toxicity prediction showed minimal adverse effects. Overall, the study highlights that Quercetin and its derivatives may serve as promising antibiofilm candidates against S. sanguinis. However, experimental validation through in vitro and in vivo studies is warranted to confirm their biological efficacy and safety.

血链球菌（S. sanguinis）是感染性心内膜炎（IE）的主要原因，可引起包括死亡在内的广泛临床表现。它利用PilA蛋白（IV型菌毛的关键成分）介导心脏组织的强粘附和生物膜形成。这种生物膜对青霉素G和万古霉素等传统抗生素具有耐药性。由于生物膜渗透性差，导致持续感染和抗生素耐药性，这些抗生素的标准治疗往往无效。因此，靶向PilA提供了破坏生物膜形成和增强IE治疗的潜在策略。目前的硅研究旨在评估槲皮素及其衍生物作为一种更安全的替代策略来对抗血葡萄球菌介导的生物膜形成。分子对接分析表明，槲皮素（-6.5 kcal/mol）和8-烯基槲皮素（-6.6 kcal/mol）比青霉素G（-6.5 kcal/mol）与血葡萄球菌PilA蛋白的结合更强，表明它们在破坏生物膜形成方面具有更强的潜力。动态模拟进一步证实了这些复合物随时间的稳定性，表明与目标位点的持续相互作用。药代动力学评价也显示了良好的吸收、分布和代谢特性，而毒性预测显示最小的不良反应。总之，该研究强调槲皮素及其衍生物可能作为抗血葡萄球菌的有前途的抗生素候选物。然而，通过体外和体内研究的实验验证是必要的，以确认其生物学有效性和安全性。

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引用次数: 0

Role of biochanin A in the treatment of diabetes and its complications 生物茶素A在糖尿病及其并发症治疗中的作用

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-03 DOI: 10.1016/j.prenap.2026.100491

Aminu Mohammed , Nasir Tajuddeen , Murtala Bindawa Isah , Mohammed Auwal Ibrahim

Biochanin A is a dietary isoflavone with several pharmacological effects, like anticancer, antimicrobial, and antidiabetic properties. Herein, the antidiabetic activities of biochanin A using various diabetes models, including cell line-based, in vivo, and in vitro assays, were reviewed. Relevant articles were sourced from the major scientific databases (Scopus, PubMed, and Google Scholar). The studies included were those that reported the effects of biochanin A on key diabetes markers, such as glucose utilisation and insulin sensitivity, in vitro and in vivo models, as well as in cell-based studies. Collectively, the data revealed that biochanin A has a potential to reduce hyperglycemia, insulin resistance, and diabetes-induced oxidative stress. Such activities were linked, among others, to the activation of Nrf2 and PI3K/Akt pathways, increasing adiponectin level and visfatin expressions as well as inhibitions of NF-κB, GSK3β and serum resistin. With the current available studies, biochanin A showed promising antidiabetic activity in several diabetes models with relatively no adverse side effects, although no study is available to confirm the efficacy in human volunteers. Detailed clinical trials and toxicological studies are warranted to validate the preclinical data.

生物茶素A是一种膳食异黄酮，具有多种药理作用，如抗癌、抗菌和抗糖尿病特性。本文综述了生物茶素A在各种糖尿病模型中的抗糖尿病活性，包括基于细胞系的、体内的和体外的实验。相关文章来源于主要的科学数据库（Scopus、PubMed和b谷歌Scholar）。这些研究包括那些在体外和体内模型以及基于细胞的研究中报道了生物茶素A对糖尿病关键标志物的影响，如葡萄糖利用和胰岛素敏感性。总的来说，数据显示生物茶素A具有降低高血糖、胰岛素抵抗和糖尿病诱导的氧化应激的潜力。这些活性与Nrf2和PI3K/Akt通路的激活、脂联素水平和visfatin表达的增加以及NF-κB、GSK3β和血清抵抗素的抑制有关。根据目前的研究，生物茶素A在几种糖尿病模型中显示出有希望的抗糖尿病活性，并且相对没有不良副作用，尽管没有研究证实其在人类志愿者中的功效。需要详细的临床试验和毒理学研究来验证临床前数据。

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引用次数: 0

Murraya koenigii as a phytotherapeutic agent in breast cancer: A comprehensive review Murraya koenigii作为一种植物治疗乳腺癌的药物：综述

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2025-12-30 DOI: 10.1016/j.prenap.2025.100487

Debalina Bose , Sachin Shetty , Anushree Udupi , Kishore Srinivasan

Murraya koenigii (MK), a medicinal plant long esteemed in traditional Asian medicine, is rich in pharmacologically active constituents, particularly carbazole alkaloids (e.g., mahanine, koenimbine, girinimbine), flavonoids (e.g., myricetin, quercetin), and terpenoids. These compounds exert potent anticancer effects, especially against breast cancer, by inducing apoptosis, inhibiting metastasis, and modulating oxidative stress and inflammation. Mahanine has been shown to downregulate CDK4/6 and estrogen receptor-α, while koenimbine activates cytochrome c-mediated intrinsic apoptosis via caspase-9. MK extracts inhibit multiple oncogenic signaling cascades including NF-κB, PI3K/Akt/mTOR, and MAPK, and suppress proteasomal function and ROS-mediated proliferation. In vitro studies report IC₅₀ values as low as 4.5 µM (mahanimbine) and 6.5 µg/mL (silver nanoparticle-formulated MK extract) against MDA-MB-231 breast cancer cells. In vivo, MK administered at 300 mg/kg significantly reduced tumor burden and elevated apoptotic markers in 7,12-dimethylbenz[a]anthracene (DMBA)-induced rodent models. This review highlights MK’s potential as a low-toxicity adjunctive therapy in breast cancer treatment. Future directions include subtype-specific clinical trials, nanocarrier-based delivery systems, and biomarker-driven therapeutic stratification to facilitate clinical translation.

龙葵（MK）是亚洲传统医学中一种备受推崇的药用植物，具有丰富的药理活性成分，特别是咔唑类生物碱（如马汗碱、龙葵碱、吉莉宁）、类黄酮（如杨梅素、槲皮素）和萜类化合物。这些化合物通过诱导细胞凋亡，抑制转移，调节氧化应激和炎症，具有有效的抗癌作用，特别是对乳腺癌。Mahanine下调CDK4/6和雌激素受体-α，而koenimine通过caspase-9激活细胞色素c介导的内在凋亡。MK提取物抑制NF-κB、PI3K/Akt/mTOR和MAPK等多种致癌信号级联，抑制蛋白酶体功能和ros介导的增殖。体外研究报告IC₅0值低至4.5 µM （mahanimbine）和6.5 µg/mL（银纳米颗粒配制的MK提取物），可对抗MDA-MB-231乳腺癌细胞。在体内，给药剂量为300 mg/kg的MK可显著降低7,12-二甲基苯[a]蒽（DMBA）诱导的啮齿动物模型的肿瘤负荷，并升高凋亡标志物。这篇综述强调了MK在乳腺癌治疗中作为一种低毒性辅助疗法的潜力。未来的方向包括亚型特异性临床试验，基于纳米载体的递送系统，以及生物标志物驱动的治疗分层，以促进临床转化。

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引用次数: 0

Chemico-pharmacological evaluation of Ficus benjamina L. (Weeping Fig) leaf extracts: GC–MS/MS profiling, pharmacological screening, and computer-aided approaches 榕叶提取物的化学药理学评价：GC-MS /MS分析、药理学筛选和计算机辅助方法

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2025-12-20 DOI: 10.1016/j.prenap.2025.100473

Fahmida Tasnim Richi , Mohammad Abdullah Taher , Asaduzzaman , Sefat Hasan Sumaiya , Suriya Akter Shompa , Mahathir Mohammad , Hasin Hasnat , Mashiur Rahman , Safaet Alam

Ficus benjamina L., commonly known as the weeping fig, is a tropical Asian plant rich in bioactive compounds. This study focused on the identification and analytical characterization of phytoconstituents from its leaves using GC-MS/MS, identifying eighteen distinct compounds from a complex natural matrix. The methanolic extract also exhibited multifunctional biological activities through in vitro, in vivo and in silico evaluations relevant to functional food and phytotherapy applications. Total phenolic content was 39.15 mg GAE/g extract, and antioxidant capacity was demonstrated by a DPPH IC₅₀ of 66.89±0.41 μg/mL (compared to 22.14±0.001 μg/mL for BHT). Moderate cytotoxicity was observed in the brine shrimp lethality assay (LC₅₀ = 6.60±1.44 μg/mL). Antimicrobial activity showed inhibition zones of 9–14 mm against the tested microbes. Analgesic effects were confirmed by a 48.97±5.40 % reduction in acetic acid-induced writhing at 400 mg/kg, while the castor oil-induced diarrhea model revealed dose-dependent antidiarrheal activity, with 48.38 % inhibition at same dose. Molecular docking of the identified phytochemicals against kappa and mu-opioid receptors, epidermal growth factor receptor, dihydrofolate reductase, and urate oxidase receptor supported the observed bioactivities, and ADME/T analysis indicated favorable drug-likeness and safety profiles. These findings highlight Ficus benjamina as a promising natural source for developing phytotherapeutics, meriting further optimization and mechanistic studies.

榕树（Ficus benjamina L.），俗称垂枝榕，是一种富含生物活性化合物的亚洲热带植物。本研究利用GC-MS/MS技术对其叶中植物成分进行了鉴定和分析，从复杂的天然基质中鉴定出18种不同的化合物。通过体外、体内和计算机评价，甲醇提取物显示出与功能性食品和植物治疗应用相关的多功能生物活性。总酚含量为39.15 mg GAE/g提取物，DPPH IC₅₀为66.89±0.41 μg/mL (BHT为22.14±0.001 μg/mL)，证明了抗氧化能力。在卤虾致死试验中观察到中度细胞毒性（LC₅₀= 6.60±1.44 μg/mL）。抑菌活性为9 ~ 14 mm。在400 mg/kg剂量下，醋酸致扭体的镇痛作用降低48.97±5.40 %，而蓖麻油致腹泻模型显示出剂量依赖性的止泻活性，相同剂量下抑制48.38 %。鉴定的植物化学物质对kappa和mu-阿片受体、表皮生长因子受体、二氢叶酸还原酶和尿酸氧化酶受体的分子对接支持观察到的生物活性，ADME/T分析显示良好的药物相似性和安全性。这些发现突出了榕属植物作为一种有前景的天然植物资源，值得进一步优化和机制研究。

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引用次数: 0

Mucuna (Mucuna pruriens L.) seed-enriched diet suppresses ACE Gene expression and enhances antioxidant capacity in hypertensive rats Mucuna （Mucuna pruriens L.）富含种子的饮食抑制高血压大鼠ACE基因表达并增强抗氧化能力

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2025-12-24 DOI: 10.1016/j.prenap.2025.100481

Opeyemi B. Ogunsuyi , Olufunke F. Ajeigbe , Idowu S. Oyeleye , Ganiyu Oboh

Hypertension and its associated conditions are major contributors to hypertension-related deaths. Mucuna (Mucuna pruriens L.) seeds are leguminous seeds, rich in protein and nutrients, with known medicinal and therapeutic properties in folklore. However, the specific chemistry of Mucuna seed' anti-hypertensive properties is not fully understood. In this study, we explored the impact of incorporating Mucuna seed into two different diets (5 % and 10 %) on blood pressure, redox status, enzyme activities, and gene expression level in Nω-nitro-L-arginine-methyl-ester hydrochloride (L-NAME)-induced hypertensive rats. The levels of nitric oxide (NO) were elevated, and arginase activity was significantly (P < 0.05) reduced in hypertensive rats (n = 7) fed diets supplemented with Mucuna seed (5 % and 10 %) when compared with the hypertensive rats’ group. We observed a notable reduction in elevated ACE activity and downregulation of the upregulated ACE-1 mRNA gene expressed in hypertensive rats fed diets supplemented with Mucuna seed. Notably, the antioxidant status of the hypertensive rats was improved in Mucuna seed-treated rats through the elevation in glutathione-S-transferase, superoxide dismutase, and catalase activities and subsequent significant upregulation in the expression level of regulator gene nuclear factor-erythroid factor 2-related factor 2 (Nrf-2). The HPLC–DAD screening revealed the presence of the major flavonoids gallic acid, quercetin, and rutin. This study identifies Mucuna as a potent inhibitor of the ACE-1 gene involved in improving an antioxidant system through interaction with the Nrf-2 gene.

高血压及其相关疾病是高血压相关死亡的主要原因。Mucuna （Mucuna pruriens L.）种子是豆科植物的种子，富含蛋白质和营养物质，在民间传说中具有已知的药用和治疗特性。然而，Mucuna种子抗高血压特性的具体化学成分尚不完全清楚。在这项研究中，我们探讨了在两种不同的饮食中添加粘豆籽（5 %和10 %）对n ω-硝基- l-精氨酸-甲基酯盐盐（L-NAME）诱导的高血压大鼠的血压、氧化还原状态、酶活性和基因表达水平的影响。与高血压大鼠组相比，饲粮中添加黏液籽（5 %和10 %）的高血压大鼠（n = 7）一氧化氮（NO）水平升高，精氨酸酶活性显著降低（P <； 0.05）。我们观察到，在添加了粘豆籽的饮食中，高血压大鼠升高的ACE活性显著降低，上调的ACE-1 mRNA基因表达下调。值得注意的是，通过提高谷胱甘肽- s转移酶、超氧化物歧化酶和过氧化氢酶的活性，并随后显著上调调节基因核因子-红细胞因子2相关因子2 （Nrf-2）的表达水平，粘豆种子处理的高血压大鼠的抗氧化状态得到改善。HPLC-DAD筛选显示主要黄酮类化合物没食子酸、槲皮素和芦丁的存在。本研究发现，Mucuna是一种有效的ACE-1基因抑制剂，通过与Nrf-2基因相互作用，参与改善抗氧化系统。

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引用次数: 0

Anti-diabetic effect of leaf extracts of Pongamia pinnata pierre: An in silico, in vitro and in vivo study 桄榔子叶提取物的抗糖尿病作用：体外、体内、体外研究

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-12 DOI: 10.1016/j.prenap.2026.100504

Jayshri Swarnkar , Saloni Rahi , Khushboo Pathania , Devendra Mishra , Mukesh Lal Sah , Sandip V. Pawar , Sangeeta Pilkhwal Sah

Aim

Pongamia pinnata (L.) Pierre (Fabacae) (P. pinnata), popularly known as “Karanja” (in Hindi) is traditionally used for many ailments due to the presence of diverse group of chemical constituents. The study aims to determine the chemical constituents of the leaves of P. pinnata, and to scientifically validate the plant for its anti-diabetic effect using in silico, in vitro, and in vivo studies.

Materials and Methods

n-hexane, ethyl acetate and ethanolic leaf extracts of P.pinnata were screened using spectroscopic and chromatographic analysis, followed by in silico molecular docking studies. The extracts were further evaluated for their in vitro antioxidant and antidiabetic activities, which were subsequently validated in a streptozotocin-induced diabetic rodent model

Results

The Gas chromatography-Mass Spectroscopy investigation revealed the presence of total 3, 7 and 48 peaks, respectively in chromatograms of n-hexane, ethyl acetate and ethanolic extracts respectively. The compound 2,7-diphenyl-1,6-dioxopyridazino [4,5:2’,3’] pyrrolo[ 4’,5’-d] pyridazine present in ethanolic extract, exhibited lowest binding energies for α-amylase and α-glucosidase enzyme targets suggesting antidiabetic potential comparable to acarbose. All the extracts demonstrated in vitro antidiabetic effect, with ethanolic extract having the most significant one. However, a weak antioxidant effect was seen with all the extracts. In streptozotocin induced diabetic rats, ethanolic and ethyl acetate extracts produced more significant antihyperglycemic effect than the standard drug metformin. The results correlated well with the findings of histopathological studies.

Conclusion

In a nutshell the antidiabetic effect of P. pinnata leaf extracts may be primarily attributed to mechanisms beyond antioxidant activity, such as the inhibition of enzymes involved in carbohydrate metabolism, warranting further extensive studies.

凤尾花（L.）皮埃尔（Fabacae）（P. pinnata），俗称“Karanja”（印地语），传统上用于治疗许多疾病，因为它含有多种化学成分。本研究旨在通过硅片、体外和体内研究，确定桄榔子叶的化学成分，科学验证其抗糖尿病作用。材料与方法采用光谱学和色谱学方法对桄榔子叶的正己烷、乙酸乙酯和乙醇提取物进行筛选，并进行硅分子对接研究。结果发现，正己烷、乙酸乙酯和乙醇提取物的色谱中分别存在3个、7个和48个峰。乙醇提取物中的化合物2,7-二苯基-1,6-二氧吡啶基[4,5:2 ',3 ']吡啶基[4 ',5 ' -d]吡啶基对α-淀粉酶和α-葡萄糖苷酶的结合能最低，表明其抗糖尿病潜力与阿卡波糖相当。所有提取物均有抗糖尿病作用，其中乙醇提取物的抗糖尿病作用最显著。然而，所有提取物的抗氧化作用都很弱。在链脲佐菌素诱导的糖尿病大鼠中，乙醇和乙酸乙酯提取物的降糖作用比标准药物二甲双胍更显著。该结果与组织病理学研究结果吻合良好。结论桄榔子叶提取物的抗糖尿病作用可能主要与抗氧化作用以外的机制有关，如抑制碳水化合物代谢酶，值得进一步深入研究。

{"title":"Anti-diabetic effect of leaf extracts of Pongamia pinnata pierre: An in silico, in vitro and in vivo study","authors":"Jayshri Swarnkar , Saloni Rahi , Khushboo Pathania , Devendra Mishra , Mukesh Lal Sah , Sandip V. Pawar , Sangeeta Pilkhwal Sah","doi":"10.1016/j.prenap.2026.100504","DOIUrl":"10.1016/j.prenap.2026.100504","url":null,"abstract":"<div><h3>Aim</h3><div><em>Pongamia pinnata</em> (L.) Pierre (Fabacae) (P. pinnata), popularly known as “Karanja” (in Hindi) is traditionally used for many ailments due to the presence of diverse group of chemical constituents. The study aims to determine the chemical constituents of the leaves of <em>P. pinnata</em>, and to scientifically validate the plant for its anti-diabetic effect using <em>in silico</em>, <em>in vitro</em>, and <em>in vivo</em> studies.</div></div><div><h3>Materials and Methods</h3><div>n-hexane, ethyl acetate and ethanolic leaf extracts of <em>P.pinnata</em> were screened using spectroscopic and chromatographic analysis, followed by <em>in silico</em> molecular docking studies. The extracts were further evaluated for their <em>in vitro</em> antioxidant and antidiabetic activities, which were subsequently validated in a streptozotocin-induced diabetic rodent model</div></div><div><h3>Results</h3><div>The Gas chromatography-Mass Spectroscopy investigation revealed the presence of total 3, 7 and 48 peaks, respectively in chromatograms of n-hexane, ethyl acetate and ethanolic extracts respectively. The compound 2,7-diphenyl-1,6-dioxopyridazino [4,5:2’,3’] pyrrolo[ 4’,5’-d] pyridazine present in ethanolic extract, exhibited lowest binding energies for α-amylase and α-glucosidase enzyme targets suggesting antidiabetic potential comparable to acarbose. All the extracts demonstrated <em>in vitro</em> antidiabetic effect, with ethanolic extract having the most significant one. However, a weak antioxidant effect was seen with all the extracts. In streptozotocin induced diabetic rats, ethanolic and ethyl acetate extracts produced more significant antihyperglycemic effect than the standard drug metformin. The results correlated well with the findings of histopathological studies.</div></div><div><h3>Conclusion</h3><div>In a nutshell the antidiabetic effect of <em>P. pinnata</em> leaf extracts may be primarily attributed to mechanisms beyond antioxidant activity, such as the inhibition of enzymes involved in carbohydrate metabolism, warranting further extensive studies.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"10 ","pages":"Article 100504"},"PeriodicalIF":0.0,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145977482","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

Dose dependent behavioral effects of agmatine in rats 胍丁胺对大鼠的剂量依赖性行为影响

Pharmacological Research - Natural Products

Pub Date : 2026-03-01 Epub Date: 2026-01-21 DOI: 10.1016/j.prenap.2026.100528

Hira Rafi , Hamna Rafiq , Muhammad Farhan

Background

Agmatine, a decarboxylated metabolite of L-arginine, exhibits neuroprotective, antidepressant, and anxiolytic properties through its modulation of NMDA receptors, monoamine pathways, and antioxidant defenses. Although its therapeutic potential is well recognized, its dose-dependent behavioral and biochemical effects remain insufficiently characterized.

Objective

This study investigated the chronic, dose-dependent effects of agmatine on locomotor activity, anxiety-like and depressive-like behaviors, cognitive performance, and oxidative stress markers in rats.

Methods

albino Wistar rats (n = 24) received oral agmatine at 50, 100, or 200 mg/kg for 28 days, while controls received water. Behavioral assessments included the open field test, forced swim test, elevated plus maze, light/dark transition test, and Morri’s water maze. Oxidative stress markers (MDA, SOD, CAT, GSH, GPx) were quantified from brain homogenates. Statistical analysis was performed using one-way ANOVA (p < 0.05).

Results

Agmatine produced significant dose-dependent improvements in locomotion and exploration, with the most pronounced effects at 100 and 200 mg/kg. Antidepressant-like behavior was evident through increased struggling in the forced swim test (p < 0.01), while anxiolytic effects were observed across all doses in both the elevated plus maze and light/dark transition tasks (p < 0.01). Cognitive function improved significantly, as shown by reduced escape latencies during training, acquisition, and retention phases of the Morris water maze (p < 0.01). Biochemically, agmatine reduced lipid peroxidation and elevated enzymatic antioxidant activity in a dose-dependent manner. 100 mg/kg dose consistently produce the strongest behavioral and antioxidant responses.

Conclusion

Chronic agmatine administration exerts robust dose-dependent behavioral and neuroprotective effects, with 100 mg/kg identified as the optimal effective dose. These findings support agmatine as a safe candidate for therapeutic applications targeting anxiety, depression, cognitive impairment, and oxidative stress.

胍丁氨酸是l -精氨酸的一种脱羧代谢物，通过调节NMDA受体、单胺途径和抗氧化防御，具有神经保护、抗抑郁和抗焦虑的特性。虽然其治疗潜力已得到充分认识，但其剂量依赖性行为和生化效应仍未充分表征。目的研究胍丁胺对大鼠运动活动、焦虑样和抑郁样行为、认知表现和氧化应激标志物的慢性剂量依赖性影响。方法salbino Wistar大鼠（n = 24只）按50、100、200 mg/kg剂量口服胍丁胺28 d，对照组饮水。行为学评估包括开阔场地测试、强迫游泳测试、高架加迷宫、明暗转换测试和Morri水迷宫。从脑匀浆中定量测定氧化应激标志物（MDA、SOD、CAT、GSH、GPx）。统计学分析采用单因素方差分析（p <； 0.05）。结果胍丁氨酸对小鼠运动和探索能力有明显的剂量依赖性改善，其中以100和200 mg/kg的效果最为显著。在强迫游泳测试中，抗抑郁样行为通过增加挣扎表现明显（p <； 0.01），而在升高的迷宫和光/暗过渡任务中，所有剂量的抗焦虑作用都被观察到（p <； 0.01）。Morris水迷宫的训练、习得和保留阶段的逃避潜伏期减少，表明认知功能显著改善（p <； 0.01）。生物化学上，胍丁氨酸以剂量依赖的方式减少脂质过氧化和提高酶的抗氧化活性。100 mg/kg剂量持续产生最强的行为和抗氧化反应。结论慢性给药agmatine具有良好的剂量依赖性行为和神经保护作用，最佳有效剂量为100 mg/kg。这些发现支持agmatine作为治疗焦虑、抑郁、认知障碍和氧化应激的安全候选药物。

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引用次数: 0