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Evaluation of the effect of milk casein on the pharmacokinetics of rutin 乳酪蛋白对芦丁药动学影响的评价
Pub Date : 2024-12-01 DOI: 10.1016/j.prenap.2024.100130
Ravindra Semwal , Ankit Kumar , Ruchi Badoni Semwal , Ashutosh Chauhan , Sunil Kumar Joshi , Kumud Upadhyaya , Deepak Kumar Semwal
Rutin, often referred to as vitamin P, possesses numerous pharmaceutical applications, yet its market availability is restricted due to poor bioavailability. Recent interest has focused on exploiting rutin's therapeutic potential, prompting efforts to enhance its bioavailability. This study aimed to enhance the bioavailability of rutin by formulating tablet dosage forms using cow milk casein as a matrix-forming agent. Tablet formulations containing rutin and milk casein were prepared, and their physicochemical properties were evaluated through in vitro tests, including hardness, friability, and dissolution. Pharmacokinetic studies were conducted using Wistar rat models, analyzing plasma drug concentrations and urine excretion. Stability studies were also performed to assess the tablets' shelf life under various conditions. The results of the study revealed that the incorporation of milk casein significantly improved the bioavailability of rutin, both in vitro and in vivo. Physicochemical evaluations demonstrated satisfactory tablet properties, while pharmacokinetic studies indicated enhanced plasma drug concentrations and reduced urine excretion of rutin with milk casein formulations. Stability studies further supported the suitability of the formulated tablets for long-term storage. In conclusion, milk casein proved effective as a matrix-forming agent for improving the bioavailability of rutin. The formulated tablets exhibited favorable physicochemical properties and enhanced drug absorption characteristics, suggesting the potential utility of milk casein in enhancing the therapeutic efficacy of rutin formulations.
芦丁通常被称为维生素P,具有许多制药应用,但由于生物利用度差,其市场供应受到限制。最近的兴趣集中在开发芦丁的治疗潜力,促使努力提高其生物利用度。本研究旨在以牛奶酪蛋白为基质形成剂,通过制定片剂剂型来提高芦丁的生物利用度。制备了含有芦丁和乳酪蛋白的片剂,并通过硬度、脆度、溶出度等体外理化指标对其进行了评价。采用Wistar大鼠模型进行药代动力学研究,分析血浆药物浓度和尿排泄情况。还进行了稳定性研究,以评估片剂在各种条件下的保质期。研究结果表明,乳酪蛋白的掺入显著提高了芦丁的体内和体外生物利用度。理化评价显示令人满意的片剂性质,而药代动力学研究表明,牛奶酪蛋白制剂提高了血浆药物浓度,减少了尿排泄。稳定性研究进一步支持了制剂长期储存的适宜性。综上所述,乳酪蛋白是提高芦丁生物利用度的有效基质形成剂。该制剂具有良好的理化性质和增强的药物吸收特性,提示乳酪蛋白在提高芦丁制剂疗效方面具有潜在的应用价值。
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引用次数: 0
Unveiling phytochemicals and antioxidant, cytotoxic, anti-thrombotic, anti-inflammatory, and antibacterial activities from the leaves of Dalbergia stipulacea (Roxb.)
Pub Date : 2024-12-01 DOI: 10.1016/j.prenap.2024.100126
Md. Jamal Hossain , Khandokar Nabila Sultana Amee , Md. Shohel Hossen , Afrin Rohoman , Mohammad Ibrahim Mondol , Mahfuza Afroz Soma , Mohammad A. Rashid
The study was aimed to conduct phytochemical investigation and assess the in vitro antioxidant, cytotoxic, anti-thrombotic, anti-inflammatory and antibacterial properties of crude methanol extract of Dalbergia stipulacea leaf and its various extractives. All the fractions contain quinines, alkaloids, flavonoids, tannins, resins, glycosides, and flavonoids, while crude methanol, petroleum ether, and ethyl acetate fractions contain saponins and steroids in qualitative phytochemical analysis. In GC-MS/MS technique, a total of 44 phytoconstituents were identified and characterized, where 3-O-Methyl-D-glucose (22.80 %), 8,11,14-Docosatrienoic acid, methyl ester (19.86 %), pentadecanoic acid, methyl ester (14.17 %), 13-docosenamide (6.62 %), nonadecanoic acid, methyl ester (4.62 %), and phytol (3.04 %) were most prominent. In addition, some promising bioactive constituents, such as pantolactone, aromandendrene, D-allose, loliolide, neophytadiene, dibutyl phthalate, kolavenol, and squalene are present in the leaf of D. stipulacea plant species. Petroleum ether soluble fraction (PESF) of the plant had the highest phenolic content (27.34 mg of GAE/gm) and showed the most effective DPPH free radical scavenger with a half maximal inhibitory concentration (IC50) value of 3.87 μg/mL. The PESF also exhibited cytotoxicity with median lethal dose (LC50) value of 2.76 μg/mL compared to the standard medication vincristine sulfate (LC50 = 0.45 μg/mL) in brine shrimp lethality bioassay. Compared to streptokinase (63.34 %), aqueous soluble fraction (AQSF) displayed the highest percentage of clot lysis (38.61 %). The PESF exhibited the most significant suppression of heat-induced hemolysis (32.61 %) and hypotonic solution-induced hemolysis (33.86 %), respectively, revealing promising anti-inflammatory properties. In addition, the methanol extract and its fractions exerted promising antibacterial properties with notable zone of inhibition (6–25 mm) compared to ciprofloxacin (17–37 mm). The current evidence supports the traditional medicinal applications of the plant, particularly its ability to act as an antioxidant, cytotoxic, thrombolytic, anti-inflammatory, and antibacterial agent. However, further phytochemical isolation and in vivo screening is necessary to discover new drugs from the leaf of D. stipulacea plant species based on the current evidence.
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引用次数: 0
Exploring the phytochemical and pharmacological insights of the plant Dolichandrone falcata
Pub Date : 2024-12-01 DOI: 10.1016/j.prenap.2024.100128
Suhas Dhaswadikar , Tanveer Shaikh , Yogesh Nikam , Natasha Akojwar , Rupali Prasad , Anil Badnale , Satish Meshram , Prakash Itankar , Satyendra Prasad
Dolichandrone falcata Seem. belonging to Bignoniaceae family is found in Malawi, Tanzania, South Africa, Bangladesh, Pakistan, and India. In Indian states, it is found in Maharashtra, Goa, Karnataka, and Bihar. This plant's anti-diabetic, anti-inflammatory, pain-relieving (analgesic), estrogen-blocking (antiestrogenic), antimicrobial, and pain-suppressing (antinociceptive) properties, antibacterial, anti-hemorrhoidal, and immunomodulatory qualities have been traditionally utilized in India to treat a variety of ailments. This plant contains a variety of phytochemicals, including steroids, amino acids, alkaloids, flavonoids, saponins, polyphenols, terpenoids, and cardiac glycosides. This review aims to provide comprehensive and up-to-date information on the traditional applications, phytochemistry, and pharmacology of the plant in order to better understand its phytochemistry and pharmacological effects. For this review, online databases such as ScifFnder, Scopus, Springer, ScienceDirect, Wiley, Web of Science, PubMed, and Google Scholar as well as a local library for relevant articles were searched. We discovered dolichandroside A, chrysin, chrysin-7-rutinoside, rutin, pinocembrin, α-Lapachone, lapachol, verbascoside, β-sitosterol, fatty acids, etc. during the plant's phytochemical analysis. Its anti-diabetic, anti-hemorrhoidal, anti-ulcer, anti-mycobacterial, anti-hyperlipidemic, antifungal, antimicrobial, antifertility, anti-inflammatory, and antinociceptive properties have also been demonstrated. This review has not only shed light on the latest scientific advancements related to this plant but has also underscored the pressing issue of its dwindling availability. The significance of this plant, particularly for its potential health benefits, cannot be overstated. Further, the information desiminated through this review may act as a knowledge source for researchers who wish to scientifically explore this plant
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引用次数: 0
Current trends in herbal medicines targeting to renal cell metabolic pathways in the treatment of cancer
Pub Date : 2024-12-01 DOI: 10.1016/j.prenap.2024.100129
Ashish Majumdar , Surendra Saraf , S.Prakash Rao

Introduction

Renal cell carcinoma (RCC) is the most common form of kidney cancer, accounting for approximately 85 % of all malignant kidney tumors. Despite advances in targeted therapies, such as tyrosine kinase inhibitors (TKIs) and immune checkpoint inhibitors, the treatment of RCC remains challenging due to drug resistance, toxicity, and recurrence. These treatments, while effective initially, often lose efficacy over time and can lead to significant side effects, limiting their long-term use. Additionally, late-stage RCC is difficult to manage, and survival rates remain low for advanced cases. As the limitations of current treatments highlight the need for safer and more sustainable options, natural products have emerged as promising alternatives in RCC therapy.

Methods

For this article, authors used PubMed, PubMed Prime, Science direct, Medline, Scopus, and Google Scholar to obtain and screen the most recent literature on natural compounds having anti-renal-cancer characteristics. Therefore, the purpose of this review was to summarise the known phytochemistry and current state of the chosen plant species.

Results

Molecular mechanisms by which renal cell carcinoma evades the immune system are a topic of intense interest at the moment. Both basic and applied studies on RCC indicate that natural products have positive effects, such as inducing apoptosis, inhibiting tumour metabolism, motility, and active the progress of autophagy. One of the primary mechanisms is the inhibition of the PI3K/Akt/mTOR pathway, which is crucial for tumor cell survival, proliferation, and metabolism. Compounds like curcumin and silibinin inhibit this pathway, leading to reduced cancer cell growth and increased apoptosis. Another significant mechanism is the induction of apoptosis through modulation of proteins such as Bcl-2, Bax, and caspases. Several phytoconstituents have demonstrated potential against kidney cancer. These include kahweol acetate, honokiol, englerin A, and epigallocatechin-3-gallate. As a result, natural products may be more useful in the fight against kidney cancer and RCC than was previously thought.

Discussion

The promising anticancer effects of natural products in RCC highlight their potential as adjunctive or alternative therapies to conventional treatments. Their ability to target multiple pathways, including apoptosis, angiogenesis, and metastasis, offers a comprehensive approach to cancer management while minimizing toxicity. However, further clinical research is necessary to establish their efficacy and safety in long-term use for RCC patients.
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引用次数: 0
Allium cepa bioactive phytochemicals as potent ALK (Anaplastic lymphoma kinase) inhibitors and therapeutic agents against non-small cell lung cancer (NSCLC): A computational study 葱属植物活性化学物质作为有效的ALK(间变性淋巴瘤激酶)抑制剂和治疗非小细胞肺癌(NSCLC)的药物:一项计算研究
Pub Date : 2024-12-01 DOI: 10.1016/j.prenap.2024.100124
Md. Sakib Al Hasan , Emon Mia , Noshin Tasnim Yana , Imam Hossen Rakib , Md. Shimul Bhuia , Raihan Chowdhury , Salehin Sheikh , Muhammad Torequl Islam
Anaplastic lymphoma kinase (ALK) inhibitors go after and stop the ALK protein, which is very important for cancer growth, especially in ALK-positive cancers like non-small cell lung cancer (NSCLC). Lung cancer, particularly ALK-positive NSCLC prone to metastasis, is treated with ALK inhibitors targeting the cancer-driving ALK protein. This study explored the potential of onion (Allium cepa) phytochemicals as inhibitors of ALK for NSCLC treatment using computational methods. The in silico study evaluated the binding affinity of all phytochemicals of A. cepa and also predicted pharmacokinetics, ADMET parameters, drug-likeness, anti-carcinogenic properties, and acute toxicity prediction to find reliable and safe ALK inhibitor agents for the treatment of NSCLC. The findings revealed that three phytochemicals, fisetin, quercetin, and tricetin demonstrated promising results with favorable drug-likeness profiles and strong binding affinities for the ALK receptors. Specifically, their binding affinities were –7.6, –7.7, and –7.8 kcal/mol for the 4ANQ receptor; –7.6, –7.6, and –8.0 kcal/mol for the 4ANS receptor, and –7.7, –7.6, and –7.7 kcal/mol for the 6MX8 receptor, respectively. Additionally, these compounds showed hydrogen bond formation, which is crucial for drug discovery against ALK and is comparable to the known ALK inhibitors crizotinib and alectinib. These findings also suggest their potential as therapeutic agents. Further, in vitro and in vivo studies are warranted to validate these results and elucidate their mechanisms of action. This study highlights the potential of natural compounds from A. cepa for the development of novel NSCLC therapies.
间变性淋巴瘤激酶(ALK)抑制剂追踪并阻止ALK蛋白,这对癌症生长非常重要,特别是在ALK阳性癌症如非小细胞肺癌(NSCLC)中。肺癌,尤其是易发转移的ALK阳性非小细胞肺癌(NSCLC),采用靶向驱动癌症的ALK蛋白的ALK抑制剂治疗。本研究利用计算方法探讨了洋葱(Allium cepa)植物化学物质作为ALK抑制剂在非小细胞肺癌治疗中的潜力。该计算机研究评估了A. cepa所有植物化学物质的结合亲和力,并预测了药代动力学、ADMET参数、药物相似性、抗癌特性和急性毒性预测,以寻找可靠和安全的ALK抑制剂用于治疗NSCLC。研究结果显示,三种植物化学物质,非瑟酮、槲皮素和三曲霉素显示出良好的药物相似谱和对ALK受体的强结合亲和力。具体来说,它们对4ANQ受体的结合亲和力分别为-7.6、-7.7和-7.8 kcal/mol;4ANS受体为-7.6、-7.6和-8.0 kcal/mol, 6MX8受体为-7.7、-7.6和-7.7 kcal/mol。此外,这些化合物显示了氢键形成,这对于发现抗ALK药物至关重要,并且与已知的ALK抑制剂克唑替尼和阿勒替尼相当。这些发现也表明了它们作为治疗药物的潜力。此外,体外和体内研究需要验证这些结果并阐明其作用机制。该研究强调了cepa天然化合物开发新型NSCLC治疗方法的潜力。
{"title":"Allium cepa bioactive phytochemicals as potent ALK (Anaplastic lymphoma kinase) inhibitors and therapeutic agents against non-small cell lung cancer (NSCLC): A computational study","authors":"Md. Sakib Al Hasan ,&nbsp;Emon Mia ,&nbsp;Noshin Tasnim Yana ,&nbsp;Imam Hossen Rakib ,&nbsp;Md. Shimul Bhuia ,&nbsp;Raihan Chowdhury ,&nbsp;Salehin Sheikh ,&nbsp;Muhammad Torequl Islam","doi":"10.1016/j.prenap.2024.100124","DOIUrl":"10.1016/j.prenap.2024.100124","url":null,"abstract":"<div><div>Anaplastic lymphoma kinase (ALK) inhibitors go after and stop the ALK protein, which is very important for cancer growth, especially in ALK-positive cancers like non-small cell lung cancer (NSCLC). Lung cancer, particularly ALK-positive NSCLC prone to metastasis, is treated with ALK inhibitors targeting the cancer-driving ALK protein. This study explored the potential of onion (<em>Allium cepa</em>) phytochemicals as inhibitors of ALK for NSCLC treatment using computational methods. The <em>in silico</em> study evaluated the binding affinity of all phytochemicals of <em>A. cepa</em> and also predicted pharmacokinetics, ADMET parameters, drug-likeness, anti-carcinogenic properties, and acute toxicity prediction to find reliable and safe ALK inhibitor agents for the treatment of NSCLC. The findings revealed that three phytochemicals, fisetin, quercetin, and tricetin demonstrated promising results with favorable drug-likeness profiles and strong binding affinities for the ALK receptors. Specifically, their binding affinities were –7.6, –7.7, and –7.8 kcal/mol for the 4ANQ receptor; –7.6, –7.6, and –8.0 kcal/mol for the 4ANS receptor, and –7.7, –7.6, and –7.7 kcal/mol for the 6MX8 receptor, respectively. Additionally, these compounds showed hydrogen bond formation, which is crucial for drug discovery against ALK and is comparable to the known ALK inhibitors crizotinib and alectinib. These findings also suggest their potential as therapeutic agents. Further, <em>in vitro</em> and <em>in vivo</em> studies are warranted to validate these results and elucidate their mechanisms of action. This study highlights the potential of natural compounds from <em>A. cepa</em> for the development of novel NSCLC therapies.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100124"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142744213","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
Reconnoitring antiepileptic and anxiolytic effects of Indian herbs: Findings from zebrafish behavioral research 重新认识印度草药的抗癫痫和抗焦虑作用:斑马鱼行为研究的发现
Pub Date : 2024-11-19 DOI: 10.1016/j.prenap.2024.100125
Srijan Bhattacharya , Debarpan Chatterjee , Rajdip Goswami , Bhaskar Pal , Susanta Paul , Nilanjan Sarkar , Mainak Chakraborty

Introduction

In the 21st century, neuropsychological disorders such as anxiety, insomnia, and epilepsy have become increasingly prevalent due to irregular lifestyles, unhealthy food habits, and work pressure. These disorders significantly impact individuals' emotional, mental, and physical well-being, leading to decreased functionality and potential long-term health complications.

Materials and methods

The research project utilized zebrafish behavioral studies to investigate the effects of herbal extracts on anxiety-like behavior and stress levels. Specifically, the study focused on four herbal plants, Withania somnifera, Adiantumcapillus-veneris, Marsileaq uadrifolia Linn. and Nardostachys jatamansi, to assess their potential in managing neuropsychological disorders. The zebrafish were exposed to solutions or extracts of these plants, and standard doses of pentylenetetrazol (PTZ) were administered to induce seizures for anti-seizure tests. Additionally, six behavioural studies, including the Novel Tank Test and Open Field Test, were conducted to evaluate anxiety-like behaviour. The methods employed in this study aimed to provide insights into the potential anxiolytic and stress-reducing properties of the herbal extracts.

Results

The findings reveal that Withania somnifera and Marsilea quadrifolia Linn., demonstrate promising effects in reducing anxiety-like behaviour and stress levels in zebrafish compared toAdiantumcapillus-veneris and Nardostachys jatamansi. These results also show the potential to improve explorative behavior and reduce time spent in dark areas, indicating anxiolytic properties.

Conclusion

The study highlights the potential of herbal therapy in managing neuropsychological disorders and emphasizes the importance of exploring alternative treatment approaches. The results provide valuable insights into the potential use of Withania somnifera and Marsilea quadrifolia Linn extracts in alleviating anxiety and stress-related behaviours and mitigating seizures, paving the way for further research and potential therapeutic applications.
引言 在 21 世纪,由于不规律的生活方式、不健康的饮食习惯和工作压力,焦虑、失眠和癫痫等神经心理疾病越来越普遍。这些疾病严重影响了个人的情绪、精神和身体健康,导致机能下降和潜在的长期健康并发症。材料和方法该研究项目利用斑马鱼行为研究来探讨草药提取物对焦虑样行为和压力水平的影响。具体来说,该研究重点关注四种草本植物,即睡茄(Withania somnifera)、茵陈(Adiantumcapillus-veneris)、马钱子(Marsileaq uadrifolia Linn.)和桔梗(Nardostachys jatamansi),以评估它们在控制神经心理障碍方面的潜力。将斑马鱼暴露于这些植物的溶液或提取物中,并施用标准剂量的戊四唑(PTZ)诱发癫痫发作,以进行抗癫痫测试。此外,还进行了六项行为研究,包括新颖水槽测试和开放场地测试,以评估焦虑行为。结果研究结果表明,与Adiantumcapillus-veneris 和 Nardostachys jatamansi 相比,Withania somnifera 和 Marsilea quadrifolia Linn.这些结果还显示了改善探索行为和减少在黑暗区域停留时间的潜力,表明了抗焦虑特性。研究结果为了解睡茄和四叶马钱子提取物在缓解焦虑和压力相关行为以及减轻癫痫发作方面的潜在用途提供了宝贵的见解,为进一步研究和潜在治疗应用铺平了道路。
{"title":"Reconnoitring antiepileptic and anxiolytic effects of Indian herbs: Findings from zebrafish behavioral research","authors":"Srijan Bhattacharya ,&nbsp;Debarpan Chatterjee ,&nbsp;Rajdip Goswami ,&nbsp;Bhaskar Pal ,&nbsp;Susanta Paul ,&nbsp;Nilanjan Sarkar ,&nbsp;Mainak Chakraborty","doi":"10.1016/j.prenap.2024.100125","DOIUrl":"10.1016/j.prenap.2024.100125","url":null,"abstract":"<div><h3>Introduction</h3><div>In the 21st century, neuropsychological disorders such as anxiety, insomnia, and epilepsy have become increasingly prevalent due to irregular lifestyles, unhealthy food habits, and work pressure. These disorders significantly impact individuals' emotional, mental, and physical well-being, leading to decreased functionality and potential long-term health complications.</div></div><div><h3>Materials and methods</h3><div>The research project utilized zebrafish behavioral studies to investigate the effects of herbal extracts on anxiety-like behavior and stress levels. Specifically, the study focused on four herbal plants, <em>Withania somnifera</em>, <em>Adiantumcapillus-veneris</em>, <em>Marsileaq uadrifolia Linn.</em> and <em>Nardostachys jatamansi,</em> to assess their potential in managing neuropsychological disorders. The zebrafish were exposed to solutions or extracts of these plants, and standard doses of pentylenetetrazol (PTZ) were administered to induce seizures for anti-seizure tests. Additionally, six behavioural studies, including the Novel Tank Test and Open Field Test, were conducted to evaluate anxiety-like behaviour. The methods employed in this study aimed to provide insights into the potential anxiolytic and stress-reducing properties of the herbal extracts.</div></div><div><h3>Results</h3><div>The findings reveal that <em>Withania somnifera and Marsilea quadrifolia Linn.</em>, demonstrate promising effects in reducing anxiety-like behaviour and stress levels in zebrafish compared to<em>Adiantumcapillus-veneris and Nardostachys jatamansi</em>. These results also show the potential to improve explorative behavior and reduce time spent in dark areas, indicating anxiolytic properties.</div></div><div><h3>Conclusion</h3><div>The study highlights the potential of herbal therapy in managing neuropsychological disorders and emphasizes the importance of exploring alternative treatment approaches. The results provide valuable insights into the potential use of <em>Withania somnifera</em> and <em>Marsilea quadrifolia Linn</em> extracts in alleviating anxiety and stress-related behaviours and mitigating seizures, paving the way for further research and potential therapeutic applications.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100125"},"PeriodicalIF":0.0,"publicationDate":"2024-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142698204","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
Ethnobotanical knowledge and practices of pastoralist communities on plants used as repellents and/or insecticides against insect vectors in the Korahaye zone of the Somali Regional State, Eastern Ethiopia 埃塞俄比亚东部索马里州 Korahaye 地区牧民社区对用作驱虫剂和/或杀虫剂的植物的人种植物学知识和做法
Pub Date : 2024-11-05 DOI: 10.1016/j.prenap.2024.100122
Getu Alemayehu , Araya Gebresilassie , Desta Woldetsadik , Shushay Hagos , Moa Megersa , Patrick Van Damme , Solomon Yared

Background

Combined efforts to combat both outdoor and indoor transmission of malaria parasites are hampered by emerging vector resistance in a wide range of endemic malaria settings in Ethiopia and the rest of the world, stressing the need to develop and implement alternative control measures. This study aimed to document indigenous pastoralist knowledge on the use of repellent and insecticidal plant species against insect vectors in a number of kebeles in the Somali Regional State, eastern Ethiopia.

Methods

Data were collected by interviewing a total of 120 participants (105 men and 15 women) through face-to-face interviews guided by a semi-structured questionnaire, observing information on the preparation method, and performing a guided field walk with a guide to collect plant specimens. The ethnobotanical survey was carried out from 5 May 2018–12 April 2019. Medicinal plant specimens were collected following a standard approach, and voucher specimens were deposited in the National Herbarium, Addis Ababa University. The data were analyzed using descriptive statistics, preference rankings, paired comparisons and direct matrix rankings.

Results

A total of 52 voucher specimens belonging to 47 genera and 31 families were obtained. Of these, 42 were reported to be repellents against mosquitoes or insects in general. Among the plant families recorded, Fabaceae had the highest number of plant species, at 6 (11.5 %). The most represented life forms were herbs (21, 40.38 %), followed by shrubs (17, 32.69 %). Leaves were the most commonly used plant part for remedy preparation and accounted for 14 (26.92 %) of the total plants. Among the repellent plant species documented, 57.68 % were reported to be burned to produce in-house smoke, 20.37 % were mashed, and the paste was applied on the human skin to repel insects. The plants that were commonly mentioned by respondents were Amaranthus sparganiocephalus (27, 22.5 %), Phytolacca dodecandra (18, 15 %), and Commiphora rostrata (26, 21.66 %) for repellent, insecticidal, and both repellent and insecticidal uses, respectively.

Conclusions

The present study showed that pastoralist communities have valuable indigenous knowledge and practices related to the use of plants as repellents. This knowledge should be validated and confirmed experimentally and possibly promoted as a sustainable and ecosystem-friendly insect vector control tool.
背景由于在埃塞俄比亚和世界其他地方的多种疟疾流行环境中出现了病媒抗药性,防治疟疾寄生虫室外和室内传播的综合努力受到了阻碍,这就强调了开发和实施替代控制措施的必要性。本研究旨在记录埃塞俄比亚东部索马里州一些kebeles地区当地牧民使用驱虫和杀虫植物物种对付昆虫病媒的知识。方法通过半结构化问卷指导下的面对面访谈、观察配制方法信息以及在向导带领下实地走访采集植物标本,共访问了120名参与者(105名男性和15名女性),收集了数据。民族植物学调查于 2018 年 5 月 5 日至 2019 年 4 月 12 日进行。药用植物标本按照标准方法采集,凭证标本存放在亚的斯亚贝巴大学国家标本馆。数据分析采用了描述性统计、偏好排序、配对比较和直接矩阵排序等方法。结果 共获得 52 份凭证标本,隶属于 47 属 31 科。据报告,其中 42 种可驱蚊或驱虫。在记录的植物科中,豆科的植物物种数量最多,有 6 种(占 11.5%)。最多的生物形式是草本植物(21 种,占 40.38%),其次是灌木(17 种,占 32.69%)。叶子是最常用的药用植物部分,占植物总数的 14(26.92%)。在记录的驱虫植物种类中,57.68%的植物被报告用于燃烧以产生内部烟雾,20.37%的植物被捣碎并将糊状物涂抹在人体皮肤上以驱赶昆虫。受访者普遍提到的驱虫植物有马齿苋(27,22.5%)、十二芒草(18,15%)和萝藦(26,21.66%),分别用于驱虫、杀虫以及驱虫和杀虫。应通过实验对这些知识进行验证和确认,并在可能的情况下将其作为一种可持续的、对生态系统友好的病媒昆虫控制工具加以推广。
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引用次数: 0
Phytochemical compositions, antioxidant, anticholinesterase, and antibacterial properties of Clerodendrum thomsoniae Balf.f. leaves: In vitro and in silico analyses Clerodendrum thomsoniae Balf.f. 叶子的植物化学成分、抗氧化、抗胆碱酯酶和抗菌特性:体外和硅学分析
Pub Date : 2024-11-04 DOI: 10.1016/j.prenap.2024.100121
Shubham Bhattacharyya , Sovan Samanta , Mayukh Hore , Samir Barai , Sandeep Kumar Dash , Subhrajyoti Roy

Introduction

Clerodendrum thomsoniae Balf.f. (Family: Lamiaceae) is an ornamental plant with a high polyphenol content that has been extensively studied in traditional medicinal systems of several countries for a variety of important pharmacological properties. Present study is aimed to investigate the chemical constituents, and antioxidant, anticholinesterase, and antibacterial properties of methanolic leaf extract of Clerodendrum thomsoniae (MECT) using in vitro and in silico methods.

Methods

The phytochemical characterization of the crude methanolic leaves extract of Clerodendrum thomsoniae (MECT) was investigated using FT-IR and GC-MS studies. The biological evaluation of MECT was conducted using DPPH and β-carotene bleaching assays, acetyl- and butyrylcholinesterase inhibitory properties. The antibacterial effectiveness of the MECT was assessed against E. coli and S. aureus using MIC, MBC, and disc agar diffusion techniques. The bioactive compounds that were identified by GC-MS were subjected to docking studies with several proteins associated with antioxidants, anticholinesterase, and antibacterial properties.

Result

DPPH radical scavenging and β-carotene bleaching assays demonstrated significant antioxidant activities (IC50 values: 162.2±2.8 μg/mL and 179.7±5.1 μg/mL, respectively). The anticholinesterase activity of MECT was demonstrated by its efficient acetylcholinesterase- (132.8±2.3 μg/mL) and butyrylcholinesterase inhibitory (157.6±6.6 μg/mL) activities. MECT is also found to contain significant amounts of phenolics and flavonoids. Results also showed significant antibacterial capacity of MECT against both Gram-negative (E. coli) and Gram-positive (S. aureus) stains. FT-IR and GC-MS analyses revealed the presence of different functional groups with seven phytocompounds which were further used to evaluate the in silico properties of MECT. Molecular docking analysis revealed that 2,4-bis(1,1-dimethylethyl)-phenol has the highest binding affinities with different proteins. ADMET study including toxicity prediction analysis confirmed that most of the phytochemicals were non-toxic.

Conclusion

In conclusion, the findings of the present study suggest that MECT possesses potential antioxidant, anticholinesterase and antibacterial properties and may further be investigated as a therapeutic candidate against microbial infections and oxidative stress mediated neurodegenerative conditions.
导言:Clerodendrum thomsoniae Balf.f.(科属:唇形科)是一种多酚含量很高的观赏植物,在多个国家的传统医药系统中被广泛研究,具有多种重要的药理特性。本研究旨在采用体外和硅学方法,研究 Clerodendrum thomsoniae(MECT)甲醇叶提取物的化学成分、抗氧化、抗胆碱酯酶和抗菌特性。采用 DPPH 和 β-胡萝卜素漂白试验、乙酰胆碱酯酶和丁酰胆碱酯酶抑制特性对 MECT 进行了生物学评价。使用 MIC、MBC 和圆盘琼脂扩散技术评估了 MECT 对大肠杆菌和金黄色葡萄球菌的抗菌效果。结果DPPH 自由基清除和 β-胡萝卜素漂白试验显示了显著的抗氧化活性(IC50 值分别为 162.2±2.8 μg/mL 和 179.7±5.1 μg/mL)。MECT 的乙酰胆碱酯酶抑制活性(132.8±2.3 μg/mL)和丁酰胆碱酯酶抑制活性(157.6±6.6 μg/mL)证明了它的抗胆碱酯酶活性。还发现 MECT 含有大量酚类和黄酮类化合物。结果还显示,MECT 对革兰氏阴性(大肠杆菌)和革兰氏阳性(金黄色葡萄球菌)污渍都有明显的抗菌能力。傅立叶变换红外光谱(FT-IR)和气相色谱-质谱(GC-MS)分析表明,七种植物化合物含有不同的官能团。分子对接分析表明,2,4-双(1,1-二甲基乙基)苯酚与不同蛋白质的结合亲和力最高。总之,本研究的结果表明,MECT 具有潜在的抗氧化、抗胆碱酯酶和抗菌特性,可进一步研究作为治疗微生物感染和氧化应激介导的神经退行性疾病的候选药物。
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引用次数: 0
Phytochemical characterization and therapeutic potential of leaf of Emilia sonchifolia (L.) DC.: A comprehensive study on functional groups and bioactive compounds. Emilia sonchifolia (L.) DC.叶片的植物化学特征和治疗潜力:关于功能基团和生物活性化合物的综合研究。
Pub Date : 2024-11-02 DOI: 10.1016/j.prenap.2024.100120
Mahantesh Banni , M. Jayaraj

Background

Emilia sonchifolia (L.) DC is an annual herbaceous plant used in the Ayurveda and Unani therapeutic systems. It treats various conditions such as diarrhea, sore throat, night blindness, rashes, fever, measles, earache, eye inflammation, ophthalmia, asthma, malaria, stomach tumors, chest pain, liver diseases, cuts, and wounds.

Purpose

This study aimed to assess the functional groups and bioactive compounds present in the leaves of E. sonchifolia using FT-IR and GC-MS analyses and explore their antioxidant, antidiabetic and anticancer effects.

Materials and methods

Different leaf extracts of E. sonchifolia were subjected to Fourier transform infrared (FT-IR) and gas chromatography-mass spectrometry (GC-MS) analyses to determine the presence of functional groups and for chemical characterization. Biological evaluations such as antioxidant (DPPH and ABTS assays) and antidiabetic (α-amylase enzyme inhibition and glucose uptake using yeast cell assays) and anticancer (HepG2 cell lines) potentials were also analyzed.

Results

FT-IR analysis revealed the presence of various functional groups such as amines, alcohols, alkanes, alkenes, halo compounds, aldehydes, sulfates, esters, phenols, and carboxylic acids. GC-MS analysis revealed the presence of 32 bioactive compounds in different leaf extracts. Among the extracts, petroleum ether (16) contained the highest number of chemical compounds, followed by ethanol (14), chloroform (9), and acetone (4). Lanosterol was the most significant compound in petroleum ether extract, whereas phytol (44.05 %) in the acetone extract and 1,2-benzenedicarboxylic acid in the chloroform (82.47 %) and ethanol (50.49 %) extracts. The ethanol leaf extract showed the highest antioxidant potential in DPPH (63.38±0.46 µg/mL) and ABTS (60.74±0.59 µg/mL) assays. It also showed better results in antidiabetic activity in both α-amylase enzyme inhibition (135.69±2.08 µg/mL) and glucose uptake using yeast cell (114.37±1.71 µg/mL) assays. Ethanol leaf extract exhibits good anticancer activity with 59.52±0.76 µg/mL against HepG2 cell line.

Conclusion

FTIR and GC-MS analyses confirmed the presence of bioactive functional groups and phytoconstituents. These results justify the leaves as a traditional remedy in Ayurveda and Unani therapeutic systems. Antioxidant, antidiabetic and anticancer assays suggested that E. sonchifolia leaves have good antioxidant, antidiabetic and anticancer potential compared to standards. Further studies are required to identify the chemical compounds responsible for these activities.
背景Emilia sonchifolia (L.) DC 是一种一年生草本植物,用于阿育吠陀和尤那尼治疗系统。它可治疗各种疾病,如腹泻、咽喉肿痛、夜盲症、皮疹、发烧、麻疹、耳痛、眼部炎症、眼炎、哮喘、疟疾、胃肿瘤、胸痛、肝病、割伤和伤口。材料和方法对不同的 E. sonchifolia 叶提取物进行傅立叶变换红外光谱(FT-IR)和气相色谱-质谱联用仪(GC-MS)分析,以确定功能团的存在和化学特征。此外,还分析了抗氧化(DPPH 和 ABTS 试验)、抗糖尿病(α-淀粉酶酶抑制作用和酵母细胞葡萄糖吸收试验)和抗癌(HepG2 细胞系)潜力等生物学评价。气相色谱-质谱分析显示,不同的叶片提取物中含有 32 种生物活性化合物。在各种提取物中,石油醚(16)含有最多的化合物,其次是乙醇(14)、氯仿(9)和丙酮(4)。石油醚提取物中含量最高的化合物是羊毛甾醇,丙酮提取物中含量最高的化合物是植物醇(44.05%),氯仿(82.47%)和乙醇(50.49%)提取物中含量最高的化合物是 1,2-苯二甲酸。乙醇叶提取物在 DPPH(63.38±0.46 µg/mL)和 ABTS(60.74±0.59 µg/mL)检测中显示出最高的抗氧化潜力。在α-淀粉酶抑制(135.69±2.08 µg/mL)和酵母细胞葡萄糖吸收(114.37±1.71 µg/mL)试验中,它也显示出较好的抗糖尿病活性。结论FTIR 和 GC-MS 分析证实了生物活性官能团和植物成分的存在。这些结果证明阿育吠陀和尤那尼治疗系统中的传统疗法是正确的。抗氧化、抗糖尿病和抗癌检测表明,与标准物质相比,E. sonchifolia 叶子具有良好的抗氧化、抗糖尿病和抗癌潜力。还需要进一步研究来确定这些活性的化学成分。
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引用次数: 0
Ameliorative effect of Ferula Asafoetida oleo-gum-resin (Asafin) against cisplatin induced functional dyspepsia condition 阿魏油胶树脂(Asafin)对顺铂引起的功能性消化不良的改善作用
Pub Date : 2024-11-01 DOI: 10.1016/j.prenap.2024.100117
Svenia P. Jose , Ratheesh M , Sheethal S , Sony Rajan , Krishnakumar IM , Sandya S

Background

Functional dyspepsia (FD), affecting over 30 % of the global population, manifests with symptoms like fullness, bloating, epigastric pain, early satiety, and gastric motility issues. In the current study, we investigated the efficacy and mechanism of action of a water-soluble powder formulation of Ferula Asafoetida oleo-gum-resin (Asafin) in an animal model of Cisplatin-induced (CP) FD.

Methods

The animals were divided into four groups: Group I - Normal, Group II - Cisplatin control, Group III - Cisplatin + Standard drug, and Group IV - Cisplatin + Asafin. Various parameters including body weight, food intake, hematological markers, biochemical markers, and histopathology were analyzed during and after a 30-day study period.

Results

It was observed that CP-treated animals exhibited a marked reduction in food intake and body weight, which significantly improved or reversed when treated with Asafin. Further analysis of gut peptide hormones (Leptin, Ghrelin, GLP-1) and their gene expressions confirmed delayed gastric emptying and impaired gastric motility in CP rats. However, co-administration of Asafin with CP showed a significant improvement in these markers, indicating the normalization of the symptoms. These results were also consistent with the observed gene expressions of appetite-regulating GI peptide hormones CCK, POMC, MTL, NPY, and CART, which returned to normal levels. Histopathology results further supported the significant improvement provided by Asafin in CP rats

Conclusions

Our findings suggest that Asafin may mitigate FD risk by modulating the gut-brain axis via gut peptide hormones and neurotransmitters.
背景功能性消化不良(FD)影响着全球30%以上的人口,表现为饱胀、腹胀、上腹痛、早饱和胃蠕动问题等症状。在本研究中,我们研究了阿魏油胶树脂水溶性粉剂(Asafin)在顺铂诱导(CP)FD 动物模型中的疗效和作用机制:I组为正常组,II组为顺铂对照组,III组为顺铂+标准药物组,IV组为顺铂+Asafin组。在 30 天的研究期间和之后,对体重、食物摄入量、血液标记物、生化标记物和组织病理学等各种参数进行了分析。结果表明,CP 治疗动物的食物摄入量和体重明显减少,而使用阿沙芬治疗后,情况明显好转或逆转。对肠道肽类激素(Leptin、Ghrelin、GLP-1)及其基因表达的进一步分析证实,CP 大鼠的胃排空延迟,胃蠕动受损。然而,阿沙芬与氯化石蜡联合给药后,这些指标均有明显改善,表明症状趋于正常。这些结果也与观察到的食欲调节消化道肽类激素CCK、POMC、MTL、NPY和CART的基因表达相一致,它们都恢复到了正常水平。结论我们的研究结果表明,阿萨芬可以通过肠道肽类激素和神经递质调节肠道-大脑轴,从而降低FD风险。
{"title":"Ameliorative effect of Ferula Asafoetida oleo-gum-resin (Asafin) against cisplatin induced functional dyspepsia condition","authors":"Svenia P. Jose ,&nbsp;Ratheesh M ,&nbsp;Sheethal S ,&nbsp;Sony Rajan ,&nbsp;Krishnakumar IM ,&nbsp;Sandya S","doi":"10.1016/j.prenap.2024.100117","DOIUrl":"10.1016/j.prenap.2024.100117","url":null,"abstract":"<div><h3>Background</h3><div>Functional dyspepsia (FD), affecting over 30 % of the global population, manifests with symptoms like fullness, bloating, epigastric pain, early satiety, and gastric motility issues. In the current study, we investigated the efficacy and mechanism of action of a water-soluble powder formulation of Ferula Asafoetida oleo-gum-resin (Asafin) in an animal model of Cisplatin-induced (CP) FD.</div></div><div><h3>Methods</h3><div>The animals were divided into four groups: Group I - Normal, Group II - Cisplatin control, Group III - Cisplatin + Standard drug, and Group IV - Cisplatin + Asafin. Various parameters including body weight, food intake, hematological markers, biochemical markers, and histopathology were analyzed during and after a 30-day study period.</div></div><div><h3>Results</h3><div>It was observed that CP-treated animals exhibited a marked reduction in food intake and body weight, which significantly improved or reversed when treated with Asafin. Further analysis of gut peptide hormones (Leptin, Ghrelin, GLP-1) and their gene expressions confirmed delayed gastric emptying and impaired gastric motility in CP rats. However, co-administration of Asafin with CP showed a significant improvement in these markers, indicating the normalization of the symptoms. These results were also consistent with the observed gene expressions of appetite-regulating GI peptide hormones CCK, POMC, MTL, NPY, and CART, which returned to normal levels. Histopathology results further supported the significant improvement provided by Asafin in CP rats</div></div><div><h3>Conclusions</h3><div>Our findings suggest that Asafin may mitigate FD risk by modulating the gut-brain axis via gut peptide hormones and neurotransmitters.</div></div>","PeriodicalId":101014,"journal":{"name":"Pharmacological Research - Natural Products","volume":"5 ","pages":"Article 100117"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142592783","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
期刊
Pharmacological Research - Natural Products
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