Pharmacological Research - Natural Products最新文献_第9页

Efficacy and safety of polyherbal Unani formulation in leucorrhoea – A prospective clinical trial 复方乌纳尼治疗白带的疗效和安全性——一项前瞻性临床试验

Pharmacological Research - Natural Products

Pub Date : 2025-12-20 DOI: 10.1016/j.prenap.2025.100472

Farhat Fathima , Zuha Umme Kulsum , Aarifa Sabreen , K. Kabiruddin Ahmed , Akhand Pratap Singh , N. Zaheer Ahmed , Farooqui Shazia Parveen

Background

Leucorrhoea is a common gynaecological condition characterized by excessive vaginal discharge, often accompanied by fatigue, pruritus, backache, and burning micturition. In Unani medicine, it is attributed to humoral imbalance and dysfunction of uterine faculties. Tiryāq-i-Raḥim, a polyherbal Unani formulation (PUF), is traditionally used for its tonic, astringent, analgesic, and phlegm-expelling properties.

Study objective

This study aimed to evaluate the safety and efficacy of PUF in women with leucorrhoea.

Methods

A prospective clinical study was conducted at Regional Research Institute of Unani Medicine, Chennai. The study was approved by the Institutional Ethics Committee on 08 September 2022 and registered with CTRI on 09 March 2023. A total of 117 female patients aged 18–40 years with symptoms of leucorrhoea were enrolled. The formulation was standardized through macroscopic, microscopic, and organoleptic evaluation of ingredients authenticated at RRIUM, Chennai. The botanical nomenclature of all plant components was verified using The Plant List (www.theplantlist.org) and compared with pharmacopoeial standards to ensure taxonomic accuracy. Quantitative phytochemical profiling (HPLC–MS) is proposed for future validation to strengthen reproducibility and quality control. PUF was administered orally (2 g twice daily) for 14 days. Symptom severity was assessed using a 10-point Visual Analogue Scale (VAS) and vaginal wet mount test. Safety was evaluated through laboratory tests. Statistical analysis was done using paired t-test and Wilcoxon signed-rank test, with p < 0.05 considered significant.

Results

After treatment, a significant reduction (p < 0.001) noted in VAS scores for all symptoms. Vaginal discharge reduced from 2.97 ± 0.15–0.52 ± 0.59, and general weakness from 5.81 ± 2.21–1.74 ± 1.28. No adverse events or laboratory abnormalities were noted. Complete relief was reported in 47.86 % of patients, with marked improvement in another 47.86 %.

Conclusion

This PUF is a safe and effective Unani formulation for managing leucorrhoea, warranting further trials for broader validation.

背景：白带是一种常见的妇科疾病，其特征是阴道分泌物过多，常伴有疲劳、瘙痒、背痛和排尿灼烧。在乌纳尼医学中，它被归因于体液失衡和子宫功能障碍。Tiryāq-i-Raḥim是一种多草药乌纳尼配方（PUF），传统上因其滋补、收敛、止痛和祛痰的特性而被使用。研究目的本研究旨在评价PUF治疗女性白带的安全性和有效性。方法在印度金奈地区医学研究所进行前瞻性临床研究。该研究于2022年9月8日获得机构伦理委员会批准，并于2023年3月9日在CTRI注册。共有117例年龄在18-40岁的女性白带患者被纳入研究。通过在金奈RRIUM认证的成分的宏观，微观和感官评价来标准化配方。使用植物目录（www.theplantlist.org）验证所有植物成分的植物学命名，并与药典标准进行比较，以确保分类准确性。提出了定量植物化学谱分析（HPLC-MS），以加强再现性和质量控制。PUF口服（2 g，每日2次），连续14天。采用10分视觉模拟量表（VAS）和阴道湿贴试验评估症状严重程度。通过实验室测试对安全性进行了评估。统计学分析采用配对t检验和Wilcoxon符号秩检验，p <； 0.05认为显著。结果治疗后，所有症状的VAS评分均显著降低（p <； 0.001）。阴道分泌物从2.97 ± 0.15-0.52 ± 0.59减少，全身无力从5.81 ± 2.21-1.74 ± 1.28减少。未发现不良事件或实验室异常。47.86 %的患者完全缓解，另有47.86 %的患者有显著改善。结论本品是一种安全有效的治疗白带的复方制剂，值得进一步试验验证。

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引用次数: 0

Effects of coenzyme Q10 on sexual behavior and hormonal profiles in male rats treated with trihexyphenidyl 辅酶Q10对经三己苯酯处理的雄性大鼠性行为和激素谱的影响

Pharmacological Research - Natural Products

Pub Date : 2025-12-20 DOI: 10.1016/j.prenap.2025.100469

Lateef Olabisi Okeleji , Ayoola Isaac Jegede , Ayodeji Folorunsho Ajayi

This study examined the impact of Coenzyme Q10 (CoQ10) on sexual behavior and reproductive hormone profiles in Trihexyphenidyl (THP)-treated male Wistar rats. The male pre-copulatory and copulatory behaviors were recorded and analyzed following the administration of CoQ10 (10 mg/kg b.w. p.o.), THP (1.5 mg/kg b.w. p.o.), and their combination [CoQ10 (10 mg/kg) + THP (1.5 mg/kg)]. Hormonal profiles, including serum levels of luteinizing hormone (LH), follicle-stimulating hormone (FSH), testosterone, estrogen, and prolactin, were also evaluated. Trihexyphenidyl treatment significantly increased mount latency (ML: 69.5 ± 6.36 s) and intromission latency (IL: 295 ± 14.8 s), while reducing ejaculation latency (EL: 167.3 ± 7.64 s), compared to the CoQ10 group (ML: 39.5 ± 2.12 s, p = 0.0033; IL: 157.7 ± 4.16 s, p < 0.0001; EL: 241.3 ± 9.45 s, p = 0.0008). CoQ10 administration to THP-treated rats significantly reduced ML (47.33 ± 4.04 s) and IL (195 ± 6 s), while increasing EL (305.3 ± 19.5 s), compared to THP alone (ML: 69.5 ± 6.36 s; IL: 295 ± 14.8 s; EL: 167.3 ± 7.64 s). In terms of frequency, THP significantly reduced mount frequency (MF: 3.67 ± 0.58) compared to the CoQ10 group (MF: 6.67 ± 0.58, p = 0.001) and the combination treatment of CoQ10 and THP (MF: 6.33 ± 0.58, p = 0.0021). However, no significant differences were observed in intromission and ejaculation frequencies across groups. The libido index was markedly reduced in THP-treated rats (60 %) but improved to 100 % with the addition of CoQ10. Similarly, the percentage of intromissions was higher in the THP + CoQ10 group (60 %) compared to THP alone (40 %). CoQ10 significantly increased copulatory efficiency (CE: 78 ± 3 %, p = 0.0006) and inter-copulatory efficiency (ICE: 12.84 ± 0.3) compared to THP-treated rats (CE: 38.1 ± 6.7 %; ICE: 11.08 ± 0.17). Hormonal analysis revealed that THP significantly decreased serum levels of LH (1.04 ± 0.7 mIU/mL, p = 0.0042), FSH (0.5 ± 0.05 mIU/mL, p < 0.0001), and testosterone (4.92 ± 0.6 ng/mL, p = 0.0001), while significantly increasing serum prolactin levels (3.6 ± 0.35 ng/dl, p < 0.0001). CoQ10 and the combination treatment were associated with normalization of these parameters, increasing LH, FSH, and testosterone levels while reducing prolactin in the THP + CoQ10 group. The findings suggest that CoQ10 enhances sexual behavior, particularly sexual drive and motivation, and is associated with improved reproductive hormonal profiles in male rats, potentially counteracting the inhibitory effects of THP. However, dose optimization studies are needed to establish optimal therapeutic regimens.

本研究检测了辅酶Q10 （CoQ10）对三己苯醚（THP）处理的雄性Wistar大鼠性行为和生殖激素谱的影响。用CoQ10（10 mg/kg b.w. p.o）、THP（1.5 mg/kg b.w. p.o）和它们的组合[CoQ10(10 mg/kg) + THP(1.5 mg/kg)]，记录并分析雄性交配前和交配行为。激素谱，包括黄体生成素（LH）、卵泡刺激素（FSH）、睾酮、雌激素和催乳素的血清水平也被评估。苯海索治疗显著增加延迟山(69.5毫升: ±6.36  s)和插入延时(IL): 295 ±14.8  s),同时减少射精延迟(EL: 167.3 ±7.64  s),相比辅酶q10组(ML: 39.5 ±2.12  s, p = 0.0033;IL: 157.7±4.16  s, p & lt; 0.0001;EL: 241.3±9.45  s, p = 0.0008)。辅酶q10政府THP-treated老鼠显著降低毫升(47.33 ±4.04  s)和IL(195 ± 6 年代),同时增加EL(305.3 ±19.5  s),相比THP独自(ML: 69.5 ±6.36  年代;IL: 295 ±14.8  年代;EL: 167.3±7.64  s)。在频率方面,THP显著降低频率山(MF: 3.67 ± 0.58)相比辅酶q10组(MF: 6.67 ± 0.58,p = 0.001)和辅酶q10的联合治疗,THP (MF: 6.33 ± 0.58,p = 0.0021)。然而，在射精频率和射精频率上各组间没有显著差异。thp处理大鼠的性欲指数明显降低（60 %），但添加辅酶q10后性欲指数提高到100 %。同样，THP + CoQ10组的插入率（60 %）高于THP单独组（40 %）。辅酶q10显著增加交配的效率(CE: 78 ± 3 % p = 0.0006)和inter-copulatory效率(冰:12.84 ± 0.3)相比THP-treated老鼠(CE: 38.1±6.7  %;冰: 11.08±0.17 )。荷尔蒙分析表明THP显著降低血清LH水平(1.04 ±0.7 /毫升、p = 0.0042),FSH( 0.5±0.05 /毫升、p & lt; 0.0001),和睾丸素( 4.92±0.6  ng / mL, p = 0.0001),同时显著提高血清泌乳素水平(3.6 ±0.35  毫微克/分升,p & lt; 0.0001)。辅酶q10和联合治疗与这些参数的正常化相关，THP + 辅酶q10组中LH、FSH和睾酮水平升高，而催乳素水平降低。研究结果表明，辅酶q10可以增强性行为，尤其是性冲动和动机，并与雄性大鼠生殖激素谱的改善有关，可能抵消THP的抑制作用。然而，剂量优化研究需要建立最佳的治疗方案。

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引用次数: 0

Antioxidant and inhibition of protein denaturation potential of essential oils of Ocimum tenuiflorum and Ocimum gratissimum: In vitro evaluation and In-silico PASS analysis 芦花和芦花精油的抗氧化和抑制蛋白质变性电位：体外评价和硅质PASS分析

Pharmacological Research - Natural Products

Pub Date : 2025-12-20 DOI: 10.1016/j.prenap.2025.100474

Shagun Sharma , Deeksha Salaria , Rajan Rolta , Ramesh Chandra Dubey

Medicinal plants have been an essential part of human society for the purpose of treating ailments since the dawn of civilization. With an extensive scope of biological pursuits, for almost 2000 years, Ocimum spp. have been considered among nearly all adaptable curative flora. Far from earlier studies, the present analysis combines both in vitro assays as well as PASS-dependent in silico prediction to recognize specific phytoconstituents from North-West Himalayan strains of Ocimum spp. which are less explored with favorable therapeutic properties and bioactivity. Examining antioxidant and protein denaturation inhibitory properties of essential oils derived from North-West Himalayan Ocimum spp. is the aim of the current study. O. gratissimum showed higher protein denaturation inhibitory and antioxidant potential as compared to O. tenuiflorum. The IC₅₀ of EO of O. tenuiflorum was observed to be 8.28 ± 0.070 μg/ml, 10.50 ± 0.77 μg/ml and 39.5 ± 1.3 μg ml⁻¹ whereas, IC₅₀ of EO of O. gratissimum was observed to be 5.9 ± 0.13 μg/ml, 6.26 ± 0.042 μg/ml and 32.86 ± 0.4 μg/ml with DPPH, ABTS and FRAP analysis, respectively. The IC₅₀ of EO of O. tenuiflorum was observed to be 30.76 ± 0.021 μg/ml whereas O. gratissimum EO was observed to be 29.31 ± 0.72 μg/ml analyzed as determined by egg albumin denaturation assay. Both O. gratissimum and O. tenuiflorum also met the Lipinski requirement and displayed traits associated with pharmaceuticals. Alpha-thujene showed the best protein denaturation potential accompanied by a P_a value of 0,807 whereas allocimene exhibited the leading antioxidant potential with a P_a value of 0,821. The present investigation’s conclusion is that EOs of O. tenuiflorum and O. gratissimum, as well as their active phytocompounds, may serve as potential sources of antioxidants and non-toxic protein denaturation inhibitory drugs.

自文明出现以来，药用植物一直是人类社会治疗疾病的重要组成部分。由于其广泛的生物学研究，近2000年来，茜草属植物被认为是几乎所有适应性强的药用植物群之一。与早期的研究不同，本分析结合了体外实验和pass依赖的硅预测，以识别西北喜马拉雅地区的Ocimum spp菌株中较少探索的具有良好治疗特性和生物活性的特定植物成分。本研究的目的是研究西北喜马拉雅山茱萸精油的抗氧化和抑制蛋白质变性的特性。草叶草具有较强的蛋白质变性抑制和抗氧化能力。EO的IC50 o . tenuiflorum 被观察到8.28±0.070  μg / ml, 10.50±0.77   μg / ml和39.5±1.3  μg 毫升−1而IC50 EO o . gratissimum被观察到的5.9 ±0.13  μg / ml, 6.26±0.042   μg / ml和32.86±0.4  与DPPHμg / ml,分别abt和收紧分析。用蛋白蛋白变性法测定，黄花o的EO IC50为30.76 ± 0.021 μg/ml，黄花o的EO IC50为29.31 ± 0.72 μg/ml。黄草和黄草均符合利平斯基要求，并表现出与药物相关的性状。α -图烯表现出最佳的蛋白质变性潜能，Pa值为0.807，而异丙烯表现出最高的抗氧化潜能，Pa值为0.821。本研究的结论是，荆芥和荆芥的提取物及其活性化合物可能是抗氧化剂和无毒蛋白质变性抑制药物的潜在来源。

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引用次数: 0

Determination of antidiabetic property and liver-renal protective potential of aqueous extract of Annona reticulata Linn. leaves and its synergistic action with glibenclamide in alloxan-induced diabetes using animal model 番荔枝水提物抗糖尿病特性及肝肾保护作用的测定。四氧嘧啶诱导糖尿病的动物模型研究及其与格列本脲的协同作用

Pharmacological Research - Natural Products

Pub Date : 2025-12-18 DOI: 10.1016/j.prenap.2025.100470

Tasnia Binte Bari Kabbo , Md. Sohel Rana , Pritesh Ranjan Dash

Through this study, the antidiabetic activities of Annona reticulata L. (Annonaceae) leaves, as claimed by certain tribal communities, were investigated. The anti-diabetic and liver-renal protective properties of aqueous leaf extract and its combination with the standard drug glibenclamide were tested in rats with alloxan-induced diabetes at doses of 200 and 400 mg/kg body weight; both dosages were found to possess significant dose-dependent antidiabetic activity. After 21 days of treatment, standard medication glibenclamide (5 mg/kg) exhibited fasting blood glucose level of 5.91 ± 0.09 mmol/L, while aqueous leaf fraction (400 mg/kg); combination of extract (200 mg/kg) and glibenclamide (2.5 mg/kg) demonstrated fasting blood glucose levels of 5.13 ± 0.12 mmol/L and 5.21 ± 0.07 mmol/L. Additionally, the diabetic rats in the extract treated group (400 mg/kg dosage) and the combination group demonstrated 8.67 % and 6.19 % of body weight loss, respectively, which were less than the value observed from the group of rats treated with glibenclamide alone (12.31 %). Furthermore, the extract and its combination with glibenclamide were found to have beneficial effects on the liver and kidney (p < 0.001) and aided in the maintenance of healthy lipid profile even when diabetes was present; these effects were comparable to those of standard drug. Moreover, GC-MS analytical data aided in identification of potential components present in the test fraction that may be crucial in the achievement of these bioactivities.

通过本研究，对某些部落所宣称的番荔枝科植物番荔枝叶的抗糖尿病活性进行了调查。以四氧嘧啶诱导的糖尿病大鼠为实验对象，研究了叶水提物及其与标准药物格列本脲联用200、400 mg/kg体重的抗糖尿病和肝肾保护作用；两种剂量均具有显著的剂量依赖性抗糖尿病活性。治疗21天后，标准药物格列本脲（5 mg/kg）的空腹血糖水平为5.91 ± 0.09 mmol/L，而叶水馏分（400 mg/kg）；提取物（200 mg/kg）与格列本脲（2.5 mg/kg）联合使用，空腹血糖水平分别为5.13 ± 0.12 mmol/L和5.21 ± 0.07 mmol/L。此外，提取物处理组（400 mg/kg剂量）和联合处理组糖尿病大鼠的体重分别减轻8.67 %和6.19 %，低于格列本脲单独处理组（12.31 %）。此外，发现提取物及其与格列本脲的组合对肝脏和肾脏有有益作用（p <； 0.001），即使在患有糖尿病的情况下，也有助于维持健康的脂质状况；这些效果与标准药物相当。此外，GC-MS分析数据有助于鉴定测试分数中存在的潜在成分，这些成分可能对实现这些生物活性至关重要。

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引用次数: 0

Ethnopharmacological investigation of medicinal plants used by traditional healers in the treatment of malaria and HIV/AIDS in Meconta, Murrupula, and Ribaue districts, northern Mozambique 对莫桑比克北部Meconta、Murrupula和Ribaue地区传统治疗师用于治疗疟疾和艾滋病毒/艾滋病的药用植物进行民族药理学调查

Pharmacological Research - Natural Products

Pub Date : 2025-12-18 DOI: 10.1016/j.prenap.2025.100462

Bondy Lourenço , Asimbawe Kiza , Rodrigues Machude , Ngulwe Saide , Rachide Assane , Abrão João , Rodolfo Chissico , Abelardo Banze , Lázaro Cuinica

Background

Plants continue to provide humans with new remedies, as 50 % of all prescriptions from community pharmacies worldwide are derived from natural products, with higher plants contributing 25 % of the total. It is essential to globalize traditional medicine to establish evidence-based healthcare, considering its safety, efficacy, and therapeutic and clinical evidence.

Aim of the study

To document the medicinal plants used by traditional medicine practitioners in the treatment of malaria and HIV/AIDS in Meconta, Murrupula, and Ribaué districts.

Materials and methods

This was an observational descriptive study with a qualitative–quantitative approach, conducted in July 2022 in the Meconta district and in August 2023 in the districts of Murrupula and Ribaué, involving 45 traditional medicine practitioners. Data were collected using a semi-structured questionnaire. Plant specimens were photographed, collected, and sent for scientific identification through the Herbarium of the Institute of Agricultural Research of Mozambique, in Maputo. The data were analyzed using SPSS version 20 and Excel 2007 software to characterize the number of plants mentioned and botanical families, frequency of citation (FC), relative frequency of citation (RFC), fidelity level (FL), use value (UV) and informant consensus factor (ICF), plants parts used in malaria and HIV/AIDS treatment and its mode of preparation and administration. A literature review was performed, in vitro and in vivo pharmacological action for antiplasmodial activity, anti-retroviral and phytochemical purposes were further assessed.

Results

Among 39 plants identified in this study, 23 species of plants were used in Meconta district (18 species to treat malaria, five species to treat HIV/AIDS, and two species were used for both diseases), 16 and six plant species were used to treat malaria in Murrupula and Ribaue districts, respectively. The most cited plant species were Eucalyptus resinifera J. White (FC=10, RFC=0.22), followed by Brackenridgea zanguebarica Oliv. (FC=6, RFC=0.13), Senna petersiana (Bolle) Lock, and Psidium guajava L. (FC=5 of each, RFC=0.11). Roots (26.5 %) and leaves (23.5 %) were the most used plant parts by traditional healers.The most frequent modes of administration for malaria remedies were oral (29.4 %), bathing (20.6 %), and inhalation (11.8 %), whereas for HIV/AIDS treatment, oral administration was most common (85.7 %).

In conclusion

According to the literature review, five species and one species warrant further investigation in antimalarial and antiretroviral assays, respectively.

植物继续为人类提供新的治疗方法，因为全球社区药房的所有处方中有50% %来自天然产品，其中更高的植物贡献了25% %。考虑到传统医学的安全性、有效性以及治疗和临床证据，必须使传统医学全球化，以建立循证卫生保健。本研究的目的：记录Meconta、Murrupula和ribau地区传统医学从业者在治疗疟疾和艾滋病毒/艾滋病中使用的药用植物。材料和方法这是一项采用定性-定量方法的观察性描述性研究，于2022年7月在Meconta地区和2023年8月在Murrupula和ribau地区进行，涉及45名传统医学从业者。使用半结构化问卷收集数据。通过位于马普托的莫桑比克农业研究所植物标本室，对植物标本进行了拍照、收集并送去进行科学鉴定。采用SPSS version 20和Excel 2007软件对数据进行分析，对文献中提及的植物数量、植物科数、被引频次（FC）、相对被引频次（RFC）、保真度（FL）、使用价值（UV）和知情者共识因子（ICF）、用于疟疾和艾滋病治疗的植物部位及其制备和给药方式进行表征。通过文献综述，进一步评价了其体内体外抗疟原虫活性、抗逆转录病毒和植物化学作用。结果在本研究鉴定的39种植物中，Meconta区有23种（治疗疟疾18种，治疗艾滋病5种，治疗两种），Murrupula区和Ribaue区分别有16种和6种治疗疟疾的植物。被引植物种类最多的是桉树（Eucalyptus resinifera J. White）（FC=10， RFC=0.22），其次是Brackenridgea zanguebarica Oliv。（FC=6， RFC=0.13），木犀草（Bolle） Lock，瓜爪哇Psidium guajava . （FC=5， RFC=0.11）。根（26.5% %）和叶（23.5% %）是传统治疗师使用最多的植物部位。疟疾药物最常见的给药方式是口服（29.4% %）、沐浴（20.6% %）和吸入（11.8% %），而艾滋病毒/艾滋病治疗最常见的是口服（85.7% %）。结论根据文献综述，在抗疟和抗逆转录病毒检测中分别有5种和1种值得进一步研究。

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引用次数: 0

Phytochemical profiling and In Vitro and In Silico evaluation of antioxidant and antimicrobial activities of Papaver rhoeas L. seed extracts obtained by microwave-assisted extraction and maceration 微波浸渍法提取的罂粟籽提取物的植物化学特征及体外和室内抗氧化和抗菌活性评价

Pharmacological Research - Natural Products

Pub Date : 2025-12-17 DOI: 10.1016/j.prenap.2025.100467

Anouar Hmamou , Abdelouahid Laftouhi , Hamza Bouakline , Oussama Khibech , Mostafa El Khomsi , Ahmed Bendaoud , Nabil El Brahmi , Amal Lahkimi

The roots, stems, leaves, and flowers of Papaver rhoeas L. (P. rhoeas) are well known for their medicinal properties, yet the seeds remain largely underexplored. This study provides the first detailed evaluation of antioxidant and antimicrobial activities of seed extracts obtained by microwave-assisted extraction (SEMi) and maceration (SEMa). Total phenolic content (TPC) was measured using the Folin–Ciocalteu method, and total flavonoid content (TFC) by the aluminum chloride assay. HPLC-DAD analysis identified the main phenolic compounds in each extract. Antioxidant activity was assessed via total antioxidant capacity (TAC) and DPPH scavenging assays, while antimicrobial efficacy was tested against Escherichia coli, Klebsiella pneumoniae, and Staphylococcus aureus by agar diffusion and broth microdilution. Molecular docking supported these biological activities in silico. SEMi extraction was more efficient (7.08 %) than SEMa (3.95 %). Both extracts had similar TPC, but SEMi showed slightly higher TFC. TAC values were comparable, yet SEMi displayed superior DPPH scavenging. SEMi exhibited stronger antimicrobial activity, reflected by larger inhibition zones and lower MIC values. HPLC-DAD revealed SEMi contained a wider range of phenolics, including gallic acid, epicatechin, and p-coumaric acid, absent in SEMa, which was richer in quercetin and (+)-catechin. Docking analysis showed quercetin and (+)-catechin had the strongest affinities, particularly for Keap1 (–9.6 and –9.5 kcal/mol) and DNA-gyrase B (–8.7 and –8.4 kcal/mol), highlighting their pivotal contributions to antioxidant and antibacterial activities. In conclusion, microwave-assisted extraction enhances both the chemical diversity and bioactivity of P. rhoeas seed extracts, emphasizing their promise for pharmaceutical and cosmetic uses.

罂粟花的根、茎、叶和花因其药用特性而闻名，但其种子仍未得到充分开发。本研究首次详细评价了微波辅助提取（SEMi）和浸渍（SEMa）方法获得的种子提取物的抗氧化和抗菌活性。用Folin-Ciocalteu法测定总酚含量（TPC），用氯化铝法测定总黄酮含量（TFC）。HPLC-DAD分析鉴定了各提取物的主要酚类化合物。通过总抗氧化能力（TAC）和DPPH清除率测定抗氧化活性，通过琼脂扩散法和肉汤微量稀释法检测对大肠杆菌、肺炎克雷伯菌和金黄色葡萄球菌的抑菌效果。分子对接支持了这些生物活性。SEMi萃取效率（7.08 %）高于SEMa（3.95 %）。两种提取物的TPC相似，但半提取物的TFC略高。TAC值具有可比性，但SEMi显示出更好的DPPH清除能力。SEMi表现出较强的抑菌活性，表现为较大的抑菌区和较低的MIC值。HPLC-DAD显示SEMi含有更多的酚类物质，包括没食子酸、表儿茶素和对香豆酸，而SEMa则含有更丰富的槲皮素和(+)-儿茶素。对接分析显示，槲皮素和(+)-儿茶素的亲和力最强，特别是对Keap1（-9.6和-9.5 kcal/mol）和DNA-gyrase B（-8.7和-8.4 kcal/mol）的亲和力最强，突出了它们在抗氧化和抗菌活性中的关键作用。综上所述，微波辅助提取提高了红缨种子提取物的化学多样性和生物活性，强调了其在制药和化妆品方面的应用前景。

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引用次数: 0

Computational study of binding affinity and ADMET properties of Leonurus cardiaca phytoconstituent on the serotonin transporter (SERT) for antidepressant activity 益母草植物成分对血清素转运体（SERT）抗抑郁活性的结合亲和力和ADMET特性的计算研究

Pharmacological Research - Natural Products

Pub Date : 2025-12-15 DOI: 10.1016/j.prenap.2025.100466

Priyanka Khedekar , Shweta Rane , Kalpana Tirpude , Dhanashree Bawane , Alpana Asnani , Sapan Shah

Depression is a prevalent mental health disorder affecting over 300 million individuals worldwide, characterized by persistent sadness, loss of motivation, and dysphoria. In this in-silico study, the Leonurus cardiaca 34 phytoconstituents were screened for antidepressant potential through molecular docking against the serotonin transporter (SERT) using fluoxetine as a reference drug. Among these, twelve phytoconstituents, including ursolic acid, corosolic acid, euscaphic acid, and β-sitosterol, exhibited higher binding affinities (−9.4 to −12.4 kcal/mol) than fluoxetine (−8.9 kcal/mol). ADME analysis via SwissADME revealed high gastrointestinal absorption and favorable water solubility for several lead compounds. Toxicity prediction using pkCSM indicated no AMES toxicity or skin sensitivity, and none of the top compounds showed hERG inhibition, suggesting low cardiotoxic potential. Although these phytoconstituents exhibited limited BBB permeability compared to fluoxetine, their physicochemical and pharmacokinetic profiles suggest potential for further optimization. Overall, L. cardiaca phytoconstituents may serve as promising lead scaffolds for the development of safer antidepressant agents, following experimental validation.

抑郁症是一种普遍存在的精神健康障碍，影响着全世界超过3亿人，其特征是持续悲伤、失去动力和烦躁不安。本研究以氟西汀为参比药物，通过对益母草血清素转运体（SERT）的分子对接，筛选了益母草34种植物成分的抗抑郁潜能。其中熊果酸、花冠果酸、桉叶酸和β-谷甾醇等12种植物成分的结合亲和力（−9.4 ~−12.4 kcal/mol）高于氟西汀（−8.9 kcal/mol）。通过SwissADME进行的ADME分析显示，几种先导化合物具有较高的胃肠道吸收和良好的水溶性。使用pkCSM进行毒性预测显示没有AMES毒性或皮肤敏感性，并且没有一种顶级化合物显示hERG抑制，表明低心脏毒性潜力。尽管与氟西汀相比，这些植物成分表现出有限的血脑屏障通透性，但它们的理化和药代动力学特征表明它们有进一步优化的潜力。总的来说，经实验验证，心草植物成分可能作为开发更安全的抗抑郁药物的有前途的铅支架。

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引用次数: 0

Ganoderma lucidum protects estrogen-deficient hearts from ischemia-reperfusion injury via mitochondrial and estrogen receptor pathways 灵芝通过线粒体和雌激素受体途径保护雌激素缺乏的心脏免受缺血再灌注损伤

Pharmacological Research - Natural Products

Pub Date : 2025-12-15 DOI: 10.1016/j.prenap.2025.100461

Sri Rahavi Boovarahan , Priyanka N. Prem , Akshayakeerthi Arthanarisami , Saranyasri santhanam , Srijan Jayaraman , Gino A. Kurian

Ischemic heart disease (IHD) risk increases in postmenopausal women due to estrogen deficiency, highlighting the need for non-hormonal cardioprotective therapies. This study investigates the cardioprotective potential of Ganoderma lucidum ethanolic extract (GL) against ischemia-reperfusion (IR) injury in an estrogen-deficient rat model. Ovariectomized (Ovx) female Wistar rats were used to mimic postmenopausal conditions. After 12 weeks, isolated hearts were subjected to IR injury via the Langendorff system, with GL administered through the Krebs Henseleit buffer. Cardiac function (LVDP, RPP), infarct size, oxidative stress markers, and mitochondrial complex activities were assessed. GC-MS analysis identified key bioactives such as linoleic acid, ergosterol, and dehydroergosterol. In silico docking revealed moderate to strong binding affinities of these compounds to cardioprotective targets including estrogen receptor β (ERβ), sirtuin-3 (SIRT3), and Caspase-3. GL treatment significantly improved post-ischemic recovery (RPP = 17.10 ± 0.29 in OVX vs. 22.62 ± 0.36 mmHg*BPM × 10 ³ in SHAM), reduced cardiac enzyme leakage, attenuated oxidative stress, and restored mitochondrial function. Notably, linoleic acid and ergosterol derivatives showed promising interactions with ERβ and SIRT3, implicating estrogenic and mitochondrial pathways in the observed cardioprotection. These findings suggest that GL exerts a multifaceted protective effect in estrogen-deficient hearts through antioxidant, mitochondrial, and receptor-mediated mechanisms. The study gives preclinical support to the potential of GL as a safe, non-hormonal therapeutic strategy for mitigating IHD risk in postmenopausal women.

由于雌激素缺乏，绝经后妇女患缺血性心脏病（IHD）的风险增加，强调需要非激素心脏保护疗法。本研究探讨了灵芝乙醇提取物（GL）对雌激素缺乏大鼠模型缺血-再灌注（IR）损伤的心脏保护作用。卵巢切除（Ovx）雌性Wistar大鼠被用来模拟绝经后的状况。12周后，通过Langendorff系统对离体心脏进行IR损伤，并通过Krebs Henseleit缓冲液给予GL。评估心功能（LVDP、RPP）、梗死面积、氧化应激标志物和线粒体复合物活性。GC-MS分析确定了关键的生物活性，如亚油酸、麦角甾醇和脱氢麦角甾醇。硅对接显示，这些化合物与雌激素受体β (ERβ)、sirtuin-3 （SIRT3）和Caspase-3等心脏保护靶点具有中等至强的结合亲和力。GL治疗显著改善缺血后恢复（OVX组RPP = 17.10 ± 0.29 vs. SHAM组RPP = 22.62 ± 0.36 mmHg*BPM × 10 ³），减少心肌酶渗漏，减轻氧化应激，恢复线粒体功能。值得注意的是，亚油酸和麦角甾醇衍生物显示出与ERβ和SIRT3有良好的相互作用，暗示观察到的心脏保护的雌激素和线粒体途径。这些发现表明GL通过抗氧化、线粒体和受体介导的机制对雌激素缺乏的心脏发挥多方面的保护作用。该研究为GL作为一种安全的、非激素治疗策略的潜力提供了临床前支持，以减轻绝经后妇女IHD的风险。

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引用次数: 0

Co-administration of phytochemicals and anti-melanoma drugs: Mechanisms, metastasis prevention, and regulatory challenges 植物化学物质和抗黑色素瘤药物的联合施用：机制、转移预防和监管挑战

Pharmacological Research - Natural Products

Pub Date : 2025-12-15 DOI: 10.1016/j.prenap.2025.100465

Irem Beyza Huner, Muge Kasim Kirac, Kutlu O. Ulgen

This review focuses on the pharmacokinetic effects of phytochemicals or foods on drugs currently used for melanoma therapy or those with the potential to prevent melanoma metastasis. The pharmacokinetic effects of piperine, Eurycoma longifolia, and garlic co-administered with propranolol, as well as carvone and orange juice co-administered with ivermectin, are investigated, along with the impact of imperatorin on dabrafenib pharmacokinetic parameters. Upon research suggesting that platelet inhibition may be useful for preventing melanoma metastases, the pharmacokinetic parameters of ticagrelor are examined in the context of grapefruit juice consumption or the administration of conventional anticancer drugs. Across the reviewed studies, piperine and garlic increased propranolol bioavailability up to twofold, while imperatorin elevated dabrafenib plasma exposure by more than threefold through CYP3A4 inhibition. Conversely, Eurycoma longifolia and orange juice decreased drug absorption, illustrating the dual modulatory potential of dietary agents on melanoma therapies. The possible drawbacks and advantages of these synergistic phytochemical-drug combinations are discussed, along with regulatory and ethical challenges. The mechanistic and molecular aspects of reshaping therapeutic dynamics upon coadministration of drugs and phytochemicals are deliberated. Precision medicine and phytochemical delivery technologies are highlighted.

本文综述了植物化学物质或食物对目前用于黑色素瘤治疗或具有预防黑色素瘤转移潜力的药物的药代动力学影响。研究了胡椒碱、长叶Eurycoma和大蒜与心得安共给药，香芹酮和橙汁与伊维菌素共给药的药代动力学效应，以及欧前胡素对dabrafenib药代动力学参数的影响。在研究表明血小板抑制可能有助于预防黑色素瘤转移的基础上，在饮用葡萄柚汁或服用常规抗癌药物的背景下，研究了替格瑞洛的药代动力学参数。在回顾的研究中，胡椒碱和大蒜将心得安的生物利用度提高了两倍，而欧前胡素通过抑制CYP3A4使达非尼的血浆暴露率提高了三倍以上。相反，长叶Eurycoma和橙汁减少药物吸收，说明了膳食剂对黑色素瘤治疗的双重调节潜力。讨论了这些协同植物化学药物组合可能存在的缺点和优点，以及监管和伦理挑战。在药物和植物化学物质共同管理重塑治疗动力学的机制和分子方面进行了审议。重点介绍了精准医疗和植物化学输送技术。

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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 : 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