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Quercetin ameliorates depressive-like phenotypes and memory deficits in hypoxia-induced murine model of stress 槲皮素可改善缺氧诱导的小鼠应激模型中的抑郁样表型和记忆缺陷
Pub Date : 2024-10-05 DOI: 10.1016/j.prenap.2024.100104
Lily O. Otomewo , Anthony T. Eduviere , Olusegun A. Adeoluwa , Emuesiri G. Moke , Gladys O. Adeoluwa

Background

Hypoxia is believed to induce a form of stress that contributes to the exacerbation of certain disease conditions such as heart diseases. Most of these conditions revolve around the central nervous system (CNS) since the brain consumes a significant percentage of oxygen.

Purpose

This study aims to determine the specific effect of hypoxia on mood and cognitive behaviours using behavioural assessment and histological methods in mice. Additionally, this study investigated the counter effect of quercetin (QCN) on the hypoxia-induced changes.

Methods

A total of thirty (30) mice were equally divided into five (5) groups. Group 1 and 2 received 5 % DMSO while only the latter was subjected to the hypoxia protocol. Groups 3–5 received graded doses of quercetin (10, 20 and 40 mg/kg), respectively. Approximately 24 h after a consecutive seven-day treatment, the mice were tested for depressive-like symptoms as well as dysfunctional memory function using recognized pharmacological tests. Afterwards, histology of specific brain regions was conducted. Finally, the data were analysed by one-way ANOVA and statistical significance was set at p<0.05.

Results

In comparison with the normal control, mice of the model control group scored significantly (p<0.05) higher in the tests that assess depression and significantly (p<0.05) lower in the tests that assessed memory function, both indicators of adverse effects of hypoxia. Also, the contributing brain regions were also negatively affected by hypoxia. However, a significant attenuation of these effects was observed in the groups that received quercetin.

Conclusion

In conclusion, quercetin is a nutritional flavonoid that possesses the ability to improve behaviour and cognition in individuals regularly exposed to hypoxia or suffering from conditions that affect oxygen delivery within the body.
背景缺氧被认为会诱发一种压力,导致心脏病等某些疾病的恶化。本研究旨在通过行为评估和组织学方法确定缺氧对小鼠情绪和认知行为的具体影响。方法将三十(30)只小鼠平均分成五(5)组。第 1 组和第 2 组接受 5% 的二甲基亚砜(DMSO)治疗,只有后者接受缺氧治疗。第 3-5 组分别接受不同剂量的槲皮素(10、20 和 40 毫克/千克)。在连续七天的治疗后约 24 小时,使用公认的药理测试对小鼠进行抑郁症状和记忆功能障碍测试。随后,对特定脑区进行组织学检查。结果与正常对照组相比,模型对照组小鼠在评估抑郁的测试中得分明显较高(p<0.05),在评估记忆功能的测试中得分明显较低(p<0.05),这两项指标都表明小鼠受到了缺氧的不良影响。此外,缺氧也对脑区产生不利影响。总之,槲皮素是一种营养黄酮类化合物,能够改善经常暴露于缺氧环境或患有影响体内氧气输送的疾病的人的行为和认知能力。
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引用次数: 0
Unveiling the medicinal potential of Euonymus alatus (Thunb.) siebold: From traditional knowledge to mechanistic understanding 揭示西波德桉树的药用潜力:从传统知识到机理认识
Pub Date : 2024-10-05 DOI: 10.1016/j.prenap.2024.100102
Acharya Balkrishna , Pardeep Kaur , Deepika Srivastava , Priyanka Chaudhary , Nidhi Sharma , Vedpriya Arya
Euonymus alatus is an evergreen shrub of the Celastraceae family. It has been used in Asia for more than 2000 years, primarily in China, Japan, and Korea, to treat a variety of ailments including rheumatism, wounds, dysentery, pain, sores, gastrointestinal problems, skin problems, etc., and also kill insects. Web search engines such as PubMed, Science Direct Google Scholar, have been extensively searched using different keywords such as Euonymus alatus, ethnomedicinal, chemicals, etc. Some books and web sites were also included. A total of 51 relevant literature sources were included which met the inclusion criteria. This review aims to provide a botanical description, phytochemistry, pharmacology, and reported mechanisms of action. Plant includes 129 natural chemicals that have a range of biological effects, including hepatoprotective, antitumor, antioxidant, antidiabetic, and antitumor properties. The mechanisms of the unstudied phytochemicals should be further investigated since they may serve as a starting point for the development of new herbal medicines.
大叶女贞(Euonymus alatus)是天南星科常绿灌木。在亚洲,主要是在中国、日本和韩国,它已被用于治疗风湿、伤口、痢疾、疼痛、疮疡、肠胃问题、皮肤问题等多种疾病,还能杀虫,已有 2000 多年的历史。在 PubMed、Science Direct Google Scholar 等网络搜索引擎上,使用不同的关键词进行了广泛搜索,如白花蛇舌草、民族药用植物、化学物质等。此外,还包括一些书籍和网站。符合纳入标准的相关文献共有 51 篇。本综述旨在提供植物学描述、植物化学、药理学和报告的作用机制。植物包括 129 种天然化学物质,具有一系列生物效应,包括保肝、抗肿瘤、抗氧化、抗糖尿病和抗肿瘤特性。应进一步研究未研究过的植物化学物质的作用机制,因为它们可以作为开发新草药的起点。
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引用次数: 0
HPLC analysis and antibacterial activity of methanolic extract of Centella asiatica (L.) urban 积雪草(L.)甲醇提取物的高效液相色谱分析和抗菌活性
Pub Date : 2024-10-05 DOI: 10.1016/j.prenap.2024.100106
Vinod K. Bisht , Arvind K. Bhandari , Rakesh S. Bisht , L.S. Kandari , Subhash Chandra , T. Negi , Santwana Palai , Janini Filgueira Rosas , Jonas Ildefonso Junior , Davi Antas e Silva , Henrique Douglas Melo Coutinho

Objectives

Increasingly resistant antibiotics and new bacteria have fueled the demand for herbal remedies. Our current study aimed to find out whether the methanolic extract from Centella asiatica aerial parts contained asiatic acid and madecassoside, as well as their antibacterial properties.

Methods

A high-performance liquid chromatography (HPLC) technique was used to measure asiatic acid and madecassoside. We assessed the antibacterial activity of both compounds and crude aerial methanolic extract using the agar-well diffusion method.

Results

As identified through HPLC analysis, madecassoside was found to be 1.89 % and asiatic acid to be 0.35 %. C. asiatica had strong inhibitory activity against E. coli (MIC of 6.25 mg ml-1 and ZOI of 9 mm) and S. aureus (MIC of 3.12 mg ml-1 and ZOI of 8 mm). The ZOI for S. typhimurium, P. vulgaris, and B. subtilis was 7, 6, and 10 mm, respectively, and the MIC was 12.5 mg ml-1. Comparing asiatic acid to madecassoside, it has a potent antibacterial effect.

Conclusions

The methanolic crude extract and measured compounds of C. asiatica exhibit strong antibacterial activity, especially against S. typhimurium and E. coli. The asiatic acid and madecassoside identified by HPLC analysis could potentially be associated with this activity. These compounds exhibit antimicrobial activity can be found and employed as low-resistance, multi-target antibacterial drugs to treat a range of bacterial and fungal infections that have become resistant to existing antibiotics.
目的抗生素耐药性和新型细菌的增加刺激了对草药的需求。我们目前的研究旨在了解积雪草气生部分的甲醇提取物中是否含有积雪草酸和积雪草苷,以及它们的抗菌特性。方法采用高效液相色谱(HPLC)技术测定积雪草酸和积雪草苷。结果经高效液相色谱分析确定,积雪草苷的含量为 1.89%,积雪草酸的含量为 0.35%。积雪草对大肠杆菌(MIC 为 6.25 mg ml-1,ZOI 为 9 mm)和金黄色葡萄球菌(MIC 为 3.12 mg ml-1,ZOI 为 8 mm)具有很强的抑制活性。鼠伤寒杆菌、寻常鼠和枯草杆菌的 ZOI 分别为 7、6 和 10 毫米,MIC 为 12.5 毫克毫升-1。结论茜草的甲醇粗提取物和测定的化合物具有很强的抗菌活性,尤其是对伤寒杆菌和大肠杆菌。通过高效液相色谱分析确定的积雪草酸和积雪草苷可能与这种活性有关。这些具有抗菌活性的化合物可作为低抗药性、多靶点抗菌药物用于治疗对现有抗生素产生抗药性的各种细菌和真菌感染。
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引用次数: 0
Anticancer activity of Nigella sativa and its bioactive compounds: An update 黑麦草及其生物活性化合物的抗癌活性:最新进展
Pub Date : 2024-10-05 DOI: 10.1016/j.prenap.2024.100100
Mst.Asma Aktar , Md.Shimul Bhuia , Raihan Chowdhury , Shrabonti Biswas , Mst.Rifah Sanzida , Fatema Akter Sonia , Jannatul Ferdous , Razina Rouf , Mohammad S. Mubarak , Lucia Raquel de Lima , Henrique Douglas Melo Coutinho , Edinardo F.F. Matias , João Paulo Martins Lima , Janini Filgueira Rosas , Muhammad Torequl Islam
Nigella sativa (black cumin) is a widely recognized medicinal plant in traditional medicine, and its seeds and seed oil are used in the treatment of various diseases. This plant and its bioactive compounds exhibit numerous biological activities such as anti-diabetic, anticancer, antimicrobial, and anti-inflammatory, among others. N. sativa contains many bioactive compounds, including important antineoplastic agents such as thymoquinone, α-hederin, carvacrol, and thymol. This review focuses on and discusses the medicinal and health-promoting effects of N. sativa and covers the recent developments that deal with the anticancer activity of this medicinal plant and its bioactive compounds, with an emphasis on the mechanism of action. The findings demonstrated that the preventive effect of N. sativaand its bioactive phytochemicals are associated with its ability to decrease inflammation and exert immune-enhancing actions. The plant and its phytochemicals also enhance natural killer (NK) cell cytotoxicity, apoptotic effects on carcinoma cells, and control signal transduction pathways including caspases, p53, ROS, AMPK/mTOR, NF-κB, JAK2/STAT3, and PI3K/Akt in suppressing cancer and tumorigenesis. However, this suggests the use of the plant as a chemotherapeutic agent and further clinical assessment of the bioactive phytochemicals to establish a reliable anticancer drug.
黑小茴香(Nigella sativa)是传统医学中广泛认可的药用植物,其种子和种子油被用于治疗各种疾病。这种植物及其生物活性化合物具有多种生物活性,如抗糖尿病、抗癌、抗菌和消炎等。荠菜含有许多生物活性化合物,其中包括重要的抗肿瘤物质,如胸腺醌、α-hederin、香芹酚和百里酚。这篇综述着重讨论了荠菜的药用和保健作用,并涵盖了有关这种药用植物及其生物活性化合物抗癌活性的最新进展,重点是其作用机制。研究结果表明,荠菜及其生物活性植物化学物质的预防作用与其减少炎症和发挥免疫增强作用的能力有关。该植物及其植物化学物质还能增强自然杀伤(NK)细胞的细胞毒性和对癌细胞的凋亡作用,并控制信号转导通路,包括抑制癌症和肿瘤发生的 caspases、p53、ROS、AMPK/mTOR、NF-κB、JAK2/STAT3 和 PI3K/Akt。不过,这表明可以将该植物用作化疗药物,并进一步对其生物活性植物化学物质进行临床评估,以确定可靠的抗癌药物。
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引用次数: 0
Phytochemical screening and evaluation of antibacterial, antipyretic, hypoglycemic, and anxiolytic effects of Adiantum philippense leaf extracts Philippense Adiantum 叶提取物的植物化学筛选及抗菌、解热、降血糖和抗焦虑作用评估
Pub Date : 2024-10-03 DOI: 10.1016/j.prenap.2024.100108
Farhana Sharmin Zumu , Md. Showkoth Akbor , Ahmed Al Amin , Mst. Farjanamul Haque , Irin Sultana , Abdullah Al Faruq , Carolina Bandeira Domiciano , Henrique Douglas Melo Coutinho , Muhammad Torequl Islam
Adiantum philippense (AP) is a source of various important phytochemicals and has been traditionally used to cure many diseases, including dysentery, ulcers, fevers, cooling, and elephantiasis. This study aimed to evaluate the anti-bacterial, anti-pyretic, analgesic, and anxiolytic effects of AP using a number of in vitro and in vivo test protocols. For this, dried leaves were extracted by the Soxhlet extractor using ethanol. The crude ethanol extract was then fractionated by treating with chloroform and n-hexane. A preliminary phytochemical screening was done for its crude extracts. The antibacterial activity of ethanol, chloroform, and n-hexane extracts of AP was tested against 10 pathogenic bacteria at concentrations of 500 µg/disc. The ethanol extract showed significant activity against Gram (+ve) and Gram (-ve) bacteria. In mice, the chloroform extracts showed significant (p <0.05) antipyretic and hypoglycemic effects, while the ethanol extract exerted significant anxiolytic effects on mice. The results obtained from this study indicate that AP leaf extracts contain important phytochemical groups and exert antibacterial, antipyretic, hypoglycemic, and anxiolytic effects. Further studies are required to isolate the bioactive compounds responsible for these claimed biological activities.
Adiantum philippense(AP)含有多种重要的植物化学物质,传统上被用于治疗多种疾病,包括痢疾、溃疡、发烧、感冒和象皮病。本研究旨在通过一系列体外和体内试验方案,评估 AP 的抗菌、解热、镇痛和抗焦虑作用。为此,使用索氏萃取器对干燥叶片进行乙醇萃取。然后用氯仿和正己烷对粗乙醇提取物进行分馏。对其粗提取物进行了初步的植物化学筛选。测试了 AP 的乙醇、氯仿和正己烷提取物在 500 µg/disc 浓度下对 10 种病原菌的抗菌活性。乙醇提取物对革兰氏(+ve)和革兰氏(-ve)细菌具有明显的活性。氯仿提取物对小鼠有明显的解热和降血糖作用(p <0.05),而乙醇提取物对小鼠有明显的抗焦虑作用。本研究结果表明,AP 叶提取物含有重要的植物化学组,具有抗菌、解热、降血糖和抗焦虑作用。还需要进一步研究,以分离出具有这些生物活性的化合物。
{"title":"Phytochemical screening and evaluation of antibacterial, antipyretic, hypoglycemic, and anxiolytic effects of Adiantum philippense leaf extracts","authors":"Farhana Sharmin Zumu ,&nbsp;Md. Showkoth Akbor ,&nbsp;Ahmed Al Amin ,&nbsp;Mst. Farjanamul Haque ,&nbsp;Irin Sultana ,&nbsp;Abdullah Al Faruq ,&nbsp;Carolina Bandeira Domiciano ,&nbsp;Henrique Douglas Melo Coutinho ,&nbsp;Muhammad Torequl Islam","doi":"10.1016/j.prenap.2024.100108","DOIUrl":"10.1016/j.prenap.2024.100108","url":null,"abstract":"<div><div><em>Adiantum philippense</em> (AP) is a source of various important phytochemicals and has been traditionally used to cure many diseases, including dysentery, ulcers, fevers, cooling, and elephantiasis<em><strong>.</strong></em> This study aimed to evaluate the anti-bacterial, anti-pyretic, analgesic, and anxiolytic effects of AP using a number of <em>in vitro</em> and <em>in vivo</em> test protocols. For this, dried leaves were extracted by the Soxhlet extractor using ethanol. The crude ethanol extract was then fractionated by treating with chloroform and n-hexane. A preliminary phytochemical screening was done for its crude extracts. The antibacterial activity of ethanol, chloroform, and n-hexane extracts of AP was tested against 10 pathogenic bacteria at concentrations of 500 µg/disc. The ethanol extract showed significant activity against Gram (+ve) and Gram (-ve) bacteria. In mice, the chloroform extracts showed significant (p &lt;0.05) antipyretic and hypoglycemic effects, while the ethanol extract exerted significant anxiolytic effects on mice. The results obtained from this study indicate that AP leaf extracts contain important phytochemical groups and exert antibacterial, antipyretic, hypoglycemic, and anxiolytic effects. Further studies are required to isolate the bioactive compounds responsible for these claimed biological activities.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100108"},"PeriodicalIF":0.0,"publicationDate":"2024-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142422207","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
A Comprehensive review on exploring Thymoquinone as novel therapeutic molecule for clinical management of Glioblastoma Multiforme 将胸腺醌作为新型治疗分子用于多形性胶质母细胞瘤临床治疗的综述
Pub Date : 2024-10-03 DOI: 10.1016/j.prenap.2024.100107
Sagar Trivedi , Ujban Hussain , Rishabh Agade , Veena Belgamwar
Glioblastoma Multiforme (GBM) is a deadly and aggressive brain cancer with rapid progression and resistance to conventional treatments. Patients suffering from GBM have a median survival of just over a year after diagnosis, and low potential of current treatments urges to discover novel molecules and therapies for its management. Thymoquinone (TH), a bioactive compound from Nigella sativa seeds, has shown potent antitumour effects in preclinical studies. TH's antioxidant properties are crucial in treating GBM, by oxidative stress-based treatment. Nanoparticles or nanocarriers entrapping TH's has substantially improved the efficacy of TH, and nanotechnology advancements can enhance targeted drug delivery. Combination therapy strategies with TH, targeting multiple vulnerabilities and disrupting pro-tumourigenic signalling cascades, may improve outcomes. TH has potential anti-GBM activity by modulating key signalling pathways, including NF-κB, PI3K/Akt, MAPK, and STAT3. It is an adjunctive in standard treatments for GBM, targeting residual tumour cells to inhibit postoperative growth and improve radiation therapy efficiency. Understanding TH-mediated immunosuppression in GBM and its effects on metabolic pathways and epigenetic regulation could lead to new therapeutic targets. This review gives a detail idea about the latest advancement made till date in the field of GBM treatment using TH as novel and potent molecule coupled with various immunology, nanotechnology, conventional therapies and other molecules.
多形性胶质母细胞瘤(GBM)是一种致命的侵袭性脑癌,病情发展迅速,对常规治疗具有抗药性。胶质母细胞瘤患者确诊后的中位生存期仅为一年多,而目前的治疗方法潜力较低,因此迫切需要发现新型分子和疗法来治疗这种疾病。胸腺醌(Thymoquinone,TH)是一种从黑麦草种子中提取的生物活性化合物,在临床前研究中显示出强大的抗肿瘤作用。胸腺醌的抗氧化特性对于通过基于氧化应激的治疗方法治疗脑胶质瘤至关重要。纳米颗粒或纳米载体包裹着 TH,这大大提高了 TH 的疗效,而纳米技术的进步可以加强靶向给药。针对多种薄弱环节和干扰促肿瘤发生信号级联的 TH 联合治疗策略可能会改善治疗效果。TH 通过调节关键信号通路,包括 NF-κB、PI3K/Akt、MAPK 和 STAT3,具有潜在的抗 GBM 活性。它是 GBM 标准治疗的一种辅助手段,可针对残余肿瘤细胞抑制术后生长并提高放疗效率。了解 TH 在 GBM 中介导的免疫抑制及其对代谢途径和表观遗传调控的影响,可以找到新的治疗靶点。这篇综述详细介绍了迄今为止利用 TH 这种新型强效分子结合各种免疫学、纳米技术、传统疗法和其他分子在 GBM 治疗领域取得的最新进展。
{"title":"A Comprehensive review on exploring Thymoquinone as novel therapeutic molecule for clinical management of Glioblastoma Multiforme","authors":"Sagar Trivedi ,&nbsp;Ujban Hussain ,&nbsp;Rishabh Agade ,&nbsp;Veena Belgamwar","doi":"10.1016/j.prenap.2024.100107","DOIUrl":"10.1016/j.prenap.2024.100107","url":null,"abstract":"<div><div>Glioblastoma Multiforme (GBM) is a deadly and aggressive brain cancer with rapid progression and resistance to conventional treatments. Patients suffering from GBM have a median survival of just over a year after diagnosis, and low potential of current treatments urges to discover novel molecules and therapies for its management. Thymoquinone (TH), a bioactive compound from <em>Nigella sativa</em> seeds, has shown potent antitumour effects in preclinical studies. TH's antioxidant properties are crucial in treating GBM, by oxidative stress-based treatment. Nanoparticles or nanocarriers entrapping TH's has substantially improved the efficacy of TH, and nanotechnology advancements can enhance targeted drug delivery. Combination therapy strategies with TH, targeting multiple vulnerabilities and disrupting pro-tumourigenic signalling cascades, may improve outcomes. TH has potential anti-GBM activity by modulating key signalling pathways, including NF-κB, PI3K/Akt, MAPK, and STAT3. It is an adjunctive in standard treatments for GBM, targeting residual tumour cells to inhibit postoperative growth and improve radiation therapy efficiency. Understanding TH-mediated immunosuppression in GBM and its effects on metabolic pathways and epigenetic regulation could lead to new therapeutic targets. This review gives a detail idea about the latest advancement made till date in the field of GBM treatment using TH as novel and potent molecule coupled with various immunology, nanotechnology, conventional therapies and other molecules.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100107"},"PeriodicalIF":0.0,"publicationDate":"2024-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142422699","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
Piper attenuatum leaves extract reduced renal crystallization formation in urolithiasis might be due to probable interaction with uromodulin protein: An evidence based in vivo and in silico studies Piper attenuatum 叶提取物可减少尿石症患者肾脏结晶的形成,这可能是由于它与尿调素蛋白发生了相互作用:基于体内和硅学研究的证据
Pub Date : 2024-10-02 DOI: 10.1016/j.prenap.2024.100101
Shikha Sharma , Gaurav Kumar , Monika Meghani , Nitin Kumar , Neeraj Kumar Sethiya , Dheeraj Bisht
Urolithiasis can cause excruciating pain and hardly managed by allopathic medicine without surgery. Recently, many of research on validation of traditional medicinal plants provided a hope for management of urolithiasis. In this context, we have found a gap between traditional claims and scientific validation on use of Piper attenuatum (P. attenuatum) towards mangement of renal caliculi. Therefore, present study was planned to determine anti-urolithiatic efficacy of ethanol extract of P. attenuatum (EEPA) leaves on ethylene glycol induced urolithiasis on male Wistar rats. Further, study pertaining to phytochemical analysis followed by molecular docking of selected bioactive phytochemicals of P. attenuatum against human uromodulin (a key potential biomarkers relevant for renal function and chronic kidney disease including urolithiasis) protein. As a result, EEPA (400 mg/kg/bw) was found to significantly improves various urinary (volume: 7.19 ± 0.11 ml/24 hr; calcium: 6.15 ± 0.51 mg/dl; phosphate: 7.83 ± 0.56 mg/dl and oxalate: 1.78 ± 0.03 mg/dl) and serum parameters (creatinine: 1.85 ± 0.04 mg/dl; uric acid: 1.65 ± 0.08 mg/dl and blood urea nitrogen or BUN: 32.20 ± 1.41 mg/dl), when compared with negative control group followed by reverse in changes as an evidence of histological studies. Additionally, molecular docking studies revealed higher binding affinity to some selected phytoconstituents against human uromodulin enzyme. It was further concluded that EEPA leaves exhibits significant antiurolithiatic activity due to presence of aristolactam A II, cepharadione A and B, piperolactam A, norcepharadione B and pipoxide chlorohydrin via strong binding efficiency with uromodulin protein.
泌尿系统结石会给患者带来剧烈疼痛,如果不进行手术,对抗疗法很难治愈。最近,许多关于传统药用植物验证的研究为治疗尿路结石带来了希望。在这种情况下,我们发现在使用 Piper attenuatum(欧蒌)治疗肾积水方面,传统说法与科学验证之间存在差距。因此,本研究计划确定欧蒌叶乙醇提取物(EEPA)对乙二醇诱导的雄性 Wistar 大鼠尿路结石症的抗尿路结石功效。此外,还进行了有关植物化学分析的研究,随后对所选的具有生物活性的 P. attenuatum 植物化学物质与人尿调素(一种与肾功能和慢性肾病(包括尿石症)相关的关键潜在生物标志物)蛋白进行了分子对接。结果发现,EEPA(400 毫克/千克/体重)能显著改善各种尿液(尿量:7.19 ± 0.11 毫升/24 小时;钙:6.15 ± 0.51 毫克/分升;磷酸盐:7.83 ± 0.56 毫克/分升;草酸盐:1.78 ± 0.03 毫克/分升):与阴性对照组相比,血清参数(肌酐:1.85±0.04 mg/dl;尿酸:1.65±0.08 mg/dl;血尿素氮或 BUN:32.20±1.41 mg/dl)和组织学研究显示的变化发生了逆转。此外,分子对接研究显示,一些选定的植物成分与人尿调素酶的结合亲和力更高。研究进一步得出结论,EEPA 树叶中的马兜铃内酰胺 A II、头抱茎二酮 A 和 B、哌啶内酰胺 A、去甲抱茎二酮 B 和哌啶氧化物氯醇与泌尿调节蛋白的结合力很强,因此具有显著的抗泌尿系结石活性。
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引用次数: 0
Chitosan nanoparticle-mediated drug delivery for linoleic acid isolated from Melastomastrum capitatum Fern. leaf extract against MCF-7 and OV7 cancer cells 壳聚糖纳米颗粒介导的从 Melastomastrum capitatum Fern. 叶提取物中分离出的亚油酸对 MCF-7 和 OV7 癌细胞的给药作用
Pub Date : 2024-10-02 DOI: 10.1016/j.prenap.2024.100105
C.A. Ukwubile , A. Ahmed , U.A. Katsayal , J. Ya’u , H. Nettey
The number of cancer cases worldwide is rising, resulting in approximately 40 million deaths each year due to the inability to effectively deliver drugs that specifically target cancer cells. The study's aim was to utilize chitosan nanoparticles containing linoleic acid extracted from Melastomastrum capitatum leaves to specifically target MCF-7 and OV7 cancer cells. The study conducted toxicity tests on Wistar rats to evaluate the potential harmful effects of the extract at different doses. It also examined the extract's impact on vital organs through histopathological analysis. Chitosan nanoparticles containing the extract were developed using the spray drying method. In addition, the study analyzed various characteristics of the chitosan-loaded extract, such as % yield, drug entrapment efficiency, morphology, particle size, thermal properties, drug release, and swelling index. In vitro studies were conducted on MCF-7 and OV7 cell lines to assess the extract's anticancer properties. In vivo studies were performed on tumor-induced Wistar rats, with five rats in each of the five groups, using hemocytometer trypan blue cell counting. The study found that the crude leaf extract of M. capitatum (MCE) was well tolerated at a dose of 5000 mg/kg in rats, with only partial congestion observed in the lungs and testis. The extract exhibited higher cytotoxicity against the ovarian cancer cell line OV7 compared to the breast cancer cell line MCF-7, with an IC50 value of 10.13±2.20. In vitro studies showed that a chitosan nanoparticle-loaded version of the extract (CSLA3) induced apoptosis and increased caspase-3 activity in OV7 cells. In vivo studies showed that treatment with the chitosan-loaded extract significantly increased mean survival time and percentage increase in life span in tumor-induced rats. Tumor cell volume and viable cell counts decreased, while non-viable cell count increased in the treated group. The study concluded that CSLA3 effectively inhibited the growth of ovarian cancer cells and demonstrated the potential of chitosan nanoparticles to deliver anticancer plant extracts. This also supports the traditional use of M. capitatum leaf extract as a treatment for ovarian cancer.
全球癌症病例数量不断上升,每年造成约 4000 万人死亡,原因是无法有效提供专门针对癌细胞的药物。这项研究的目的是利用壳聚糖纳米粒子,其中含有从 Melastomastrum capitatum 叶子中提取的亚油酸,从而特异性地靶向 MCF-7 和 OV7 癌细胞。研究对 Wistar 大鼠进行了毒性测试,以评估不同剂量提取物的潜在有害影响。研究还通过组织病理学分析检验了萃取物对重要器官的影响。采用喷雾干燥法研制出了含有该提取物的壳聚糖纳米粒子。此外,该研究还分析了壳聚糖负载提取物的各种特性,如产量百分比、药物包载效率、形态、粒度、热性能、药物释放和膨胀指数。对 MCF-7 和 OV7 细胞系进行了体外研究,以评估提取物的抗癌特性。在肿瘤诱导的 Wistar 大鼠身上进行了体内研究,五组中每组五只大鼠,使用血细胞计数器进行胰蓝细胞计数。研究发现,大鼠对毛果芸香科植物粗叶提取物(MCE)的耐受性良好,剂量为 5000 毫克/千克,仅在肺部和睾丸观察到部分充血。与乳腺癌细胞株 MCF-7 相比,该提取物对卵巢癌细胞株 OV7 的细胞毒性更高,IC50 值为 10.13±2.20。体外研究表明,壳聚糖纳米粒子负载型提取物(CSLA3)可诱导 OV7 细胞凋亡,并提高 Caspase-3 的活性。体内研究表明,壳聚糖载体提取物能显著延长肿瘤诱导大鼠的平均存活时间,并增加其寿命百分比。治疗组的肿瘤细胞体积和存活细胞数减少,而非存活细胞数增加。研究得出结论,CSLA3 能有效抑制卵巢癌细胞的生长,证明了壳聚糖纳米颗粒具有递送抗癌植物提取物的潜力。这也为传统上使用毛果芸香叶提取物治疗卵巢癌提供了支持。
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引用次数: 0
Natural products as a source of cholinesterase inhibitors 天然产品作为胆碱酯酶抑制剂的来源
Pub Date : 2024-10-01 DOI: 10.1016/j.prenap.2024.100099
Pamella Christina Ortega de Oliveira , Gabriel Matias da Silva , Quezia Bezerra Cass , Marcela Cristina de Moraes , Carmen Lúcia Cardoso
As the global population ages, the incidence of neurodegenerative diseases such as Parkinson’s disease and dementia including Alzheimer's disease (AD) rises. The characteristic cognitive, behavioral, and motor impairments of these conditions are often linked to dysregulated cholinergic system. Various neurodegenerative diseases have been associated with altered levels of the neurotransmitter acetylcholine (ACh) and changes in the expression and function of receptors in specific areas of the nervous system. For instance, while AD development is not fully understood, the AD cholinergic hypothesis considers that AD patients exhibit low ACh concentrations, and that many dementia symptoms could potentially stem from this deficiency. Moreover, it has been speculated that acetylcholine dysfunction might not be the primary pathological cause but rather a consequence of AD. Hence, one approach to developing new drugs to treat AD involves identifying compounds that can inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the two enzymes underlying ACh hydrolysis. Natural products offer wide structural diversity, which makes them an important source of bioactive compounds. This article reviews the literature on how natural compounds have contributed to the discovery and design of new cholinesterase inhibitors over the past two decades. The review encompasses a brief historical overview of inhibitors that are used to treat AD in clinical settings, a discussion of the different classes of natural products that act to inhibit AChE and BChE, and a concise presentation of the screening assays that are employed to identify AChE and BChE ligands.
随着全球人口的老龄化,帕金森病和包括阿尔茨海默病(AD)在内的痴呆症等神经退行性疾病的发病率也在上升。这些疾病特有的认知、行为和运动障碍往往与胆碱能系统失调有关。各种神经退行性疾病都与神经递质乙酰胆碱(ACh)水平的改变以及神经系统特定区域受体表达和功能的变化有关。例如,虽然人们对注意力缺失症的发展还不完全清楚,但注意力缺失症胆碱能假说认为,注意力缺失症患者的乙酰胆碱浓度较低,许多痴呆症状可能源于乙酰胆碱的缺乏。此外,还有人推测,乙酰胆碱功能障碍可能不是主要的病理原因,而是AD的后果。因此,开发治疗注意力缺失症新药的一种方法是找出能够抑制乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)这两种乙酰胆碱水解酶的化合物。天然产品具有广泛的结构多样性,因此是生物活性化合物的重要来源。本文回顾了过去二十年来天然化合物如何促进新胆碱酯酶抑制剂的发现和设计的文献。该综述简要概述了临床上用于治疗注意力缺失症的抑制剂的历史,讨论了抑制 AChE 和 BChE 的不同天然产物类别,并简明扼要地介绍了用于鉴定 AChE 和 BChE 配体的筛选方法。
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引用次数: 0
Zootherapeuticals of the three geo-political regions of Southern Nigeria 尼日利亚南部三个地缘政治地区的动物疗法
Pub Date : 2024-09-28 DOI: 10.1016/j.prenap.2024.100095
Olayide Muideen Oladepo , Waheed Adeola Adedeji , Musa Oladejo , Mohammed Wulgo Ali , Oyindamola Olajumoke Abiodun , Oluwakanyinsola Salawu

Ethnopharmacological relevance

Drug bioprospecting from natural products is arguably a gold mine. Ethnopharmacological studies have primarily focused on the use of plant materials for drug discovery, though other natural products including animal species are commonly used for managing diseases in Nigeria. Review and documentation of zootherapy studies in Southern Nigeria are scattered, and inventory and cross-indexing of zootherapeutics in the region are scarce.

Aim of the study

We reviewed and inventoried studies on the practice of zootherapy in managing diseases in the three geopolitical regions of Southern Nigeria.

Materials and methods

Inclusion criterion for the papers used was limiting utilization of animal species to medicinal purposes only. Publications between 1988 and 2021 were examined using databases like Google Scholar, Scopus, Web of Science, PubMed and Medline. Popularity ratio (P.R) and impart factor (IF) were assigned to an animal family to denote number of places in the Southern Nigeria where it is used and number of diseases it is used to manage respectively.

Results

Data were gathered from 81 published papers or books out of which 26 were on the practices of zootherapy in different states of Southern Nigeria, 45 were on the practices of zootherapy in other parts of the world for correlations and cross indexing, 8 were referenced for natural medicines generally while the remaining two were relevant literatures. Ninety-eight (98) species of medicinal animals and products were used in the South-Western, seventy-nine (79) in the South-Southern and twenty (20) in the South-Eastern regions of Nigeria. Oyo State was reported for the highest therapeutic usage while Abia State has the lowest value. The animal product with the most medicinal usage in Southern Nigeria are Bovidae with an impart factor (IF) of 100 while Anatidae, Osteridae and Colubrida each has an impart factor of 4.76. The animal parts (bone, tail, head, skin, fur, milk, hoof, horn, egg and honey; skull and teeth) are the most commonly used in the South-East, whole animal in the South-West and flesh in the South-South.

Conclusions

This review of the zootherapy practices in Nigeria may further enhance the study and development of new drugs by researchers interested in ethnopharmacology.
从天然产品中进行药物生物勘探可以说是一座金矿。尽管包括动物物种在内的其他天然产品通常用于治疗尼日利亚的疾病,但人种药理学研究主要侧重于利用植物材料进行药物开发。对尼日利亚南部动物疗法研究的回顾和记录比较零散,对该地区动物疗法的盘点和交叉索引也很少。研究目的我们回顾并盘点了尼日利亚南部三个地缘政治地区动物疗法治疗疾病的研究。使用谷歌学术、Scopus、Web of Science、PubMed 和 Medline 等数据库对 1988 年至 2021 年间的论文进行了研究。结果从 81 篇已发表的论文或书籍中收集了数据,其中 26 篇涉及尼日利亚南部各州的动物疗法实践,45 篇涉及世界其他地区的动物疗法实践,以便进行关联和交叉索引,8 篇参考了一般的天然药物,其余 2 篇为相关文献。尼日利亚西南部地区使用了 98 种药用动物和产品,南部地区使用了 79 种,东南部地区使用了 20 种。据报告,奥约州的药用率最高,而阿比亚州的药用率最低。尼日利亚南部地区药用价值最高的动物产品是牛科动物,其传授系数(IF)为 100,而羊科动物、牡蛎科动物和疣螈科动物的传授系数均为 4.76。动物器官(骨、尾、头、皮、毛、乳、蹄、角、蛋和蜜;头骨和牙齿)在东南部最常用,整只动物在西南部最常用,肉在南部最常用。
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引用次数: 0
期刊
Pharmacological Research - Natural Products
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