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Recent advances in Chinese phytopharmacology for female infertility: A systematic review of high-quality randomized controlled trials 中药治疗女性不孕症的最新进展:高质量随机对照试验的系统回顾
Pub Date : 2024-11-04 DOI: 10.1016/j.prmcm.2024.100539
Rodrigo Aguiar , Samantha Gehlen , Rui Oliveira , Jorge Magalhães Rodrigues

Introduction

Infertility is a significant reproductive health issue affecting millions worldwide. Traditional Chinese Medicine (TCM), particularly Chinese phytopharmacology, has garnered attention as a potential complementary treatment. This systematic review aims to evaluate the efficacy and safety of Chinese phytopharmacology interventions for female infertility, focusing on recent randomized controlled trials (RCTs).

Methods

A comprehensive literature search was conducted in major databases to identify relevant RCTs published between 2019 and July 2024. Studies were assessed for quality, which also served as an inclusion/exclusion criterion. Data extraction focused on study characteristics, interventions, comparators, and outcomes.

Results

Nine good-quality RCTs were included, evaluating various Chinese phytopharmacology interventions for infertility. Positive effects were observed in several studies, particularly for the Zishen Yutai pill, Dingkun pill, Erzhi Tiangui granules, and ginger-isolated moxibustion. These interventions demonstrated potential benefits in improving pregnancy rates, embryo quality, and endometrial receptivity.

Conclusion

Chinese phytopharmacology interventions show promise in improving fertility outcomes when used in conjunction with conventional fertility treatments. While the findings are encouraging, more research is warranted to confirm the efficacy and safety of these interventions.
导言不孕症是影响全球数百万人的重大生殖健康问题。作为一种潜在的辅助治疗方法,传统中医药,尤其是中药已引起人们的关注。本系统综述旨在评估中药干预治疗女性不孕症的有效性和安全性,重点关注近期的随机对照试验(RCT)。对研究进行了质量评估,这也是纳入/排除标准。数据提取的重点是研究特点、干预措施、比较对象和结果。结果纳入了九项质量较好的 RCT,评估了针对不孕症的各种中药干预措施。几项研究都观察到了积极的效果,尤其是紫参玉台丸、定坤丸、二至天玑颗粒和隔姜灸。这些干预措施在提高妊娠率、胚胎质量和子宫内膜接受能力方面显示出潜在的益处。尽管研究结果令人鼓舞,但仍需开展更多研究,以确认这些干预措施的有效性和安全性。
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引用次数: 0
Synergistic effect between vancomycin and traditional Chinese medicine (TCM) herbs against methicillin-resistant Staphylococcus aureus (MRSA) infections 万古霉素与中药对耐甲氧西林金黄色葡萄球菌(MRSA)感染的协同作用
Pub Date : 2024-11-04 DOI: 10.1016/j.prmcm.2024.100538
Prateek Porwal, Satish Kumar Sharma

Introduction

Methicillin-resistant Staphylococcus aureus (MRSA) poses a significant challenge to global health due to its resistance to many conventional antibiotics. Emerging resistance increasingly compromises the efficacy of vancomycin, a glycopeptide antibiotic, which remains a critical treatment option for MRSA infections. Traditional Chinese Medicine (TCM), with its rich history and diverse pharmacopoeia, offers potential complementary therapies. This review explores the synergistic effects of combining vancomycin with TCM to enhance antibacterial efficacy against MRSA.

Method

We conducted a comprehensive literature review using databases such as PubMed, Scopus, and Web of Science. Studies included were those that evaluated the combined effects of vancomycin and Traditional Chinese Medicine (TCM) on MRSA in vitro, in vivo, and in clinical settings. Our selection criteria focused on peer-reviewed articles published in the last two decades. We included studies that provided clear methodologies for assessing bacterial inhibition rates, synergy assessments (using methods such as the checkerboard assay and time-kill curves), and mechanisms of action. Additionally, studies were required to detail the specific TCM components used, dosages, and outcomes. We excluded studies that did not specifically assess the combination of vancomycin with TCM, lacked a control group, or did not provide sufficient methodological details for assessing the synergy between the treatments. Data extraction was standardized to include study design, TCM components used, dosages, and outcomes.

Results

The review identified several TCM herbs and formulations that exhibited synergistic effects when combined with vancomycin. Notable examples include Huang Lian (Coptis chinensis), which demonstrated enhanced bacterial inhibition through disruption of bacterial cell walls and biofilm reduction. The combination therapy not only improved bacterial clearance but also reduced the required dosage of vancomycin, potentially mitigating adverse effects. Mechanistic studies showed that TCM compounds could make bacterial cell membranes more permeable and stop efflux pumps from working, which raised the concentration of vancomycin inside cells.

Conclusion

The synergistic use of vancomycin and TCM offers a promising strategy to combat MRSA infections, potentially addressing the limitations of vancomycin monotherapy. This review highlights the need for further clinical trials to validate these findings and optimise combination protocols. Integrating TCM with conventional antibiotics could lead to more effective, lower-dose treatments, reducing the risk of resistance development and improving patient outcomes. Future research should focus on elucidating the precise mechanisms of synergy and exploring the clinical applicability of these combinations.
导言由于耐甲氧西林金黄色葡萄球菌(MRSA)对许多常规抗生素具有耐药性,因此对全球健康构成了重大挑战。万古霉素是一种糖肽类抗生素,其疗效仍然是治疗 MRSA 感染的关键选择。中医药历史悠久,药典种类繁多,具有潜在的辅助治疗作用。本综述探讨了万古霉素与中药联合使用的协同作用,以增强对 MRSA 的抗菌效果。方法我们使用 PubMed、Scopus 和 Web of Science 等数据库进行了全面的文献综述。我们利用 PubMed、Scopus 和 Web Science 等数据库进行了全面的文献综述,纳入的研究均为评估万古霉素和中医药(TCM)在体外、体内和临床环境中对 MRSA 的联合作用的研究。我们的选择标准侧重于过去二十年中发表的经同行评审的文章。我们纳入的研究应提供明确的方法来评估细菌抑制率、协同作用评估(使用棋盘试验和时间杀伤曲线等方法)和作用机制。此外,研究还要求详细说明所使用的具体中药成分、剂量和结果。我们排除了那些没有专门评估万古霉素与中药联合治疗的研究、缺乏对照组的研究,或者没有提供足够的方法学细节来评估治疗之间的协同作用的研究。数据提取标准化,包括研究设计、使用的中药成分、剂量和结果。值得注意的例子包括黄连(黄连),它通过破坏细菌细胞壁和减少生物膜来增强抑菌作用。联合疗法不仅能提高细菌清除率,还能减少万古霉素的用量,从而减轻不良反应。机理研究表明,中药化合物可使细菌细胞膜更具渗透性,阻止外排泵工作,从而提高细胞内万古霉素的浓度。本综述强调了进一步临床试验的必要性,以验证这些研究结果并优化组合方案。将中药与传统抗生素结合使用,可实现更有效、剂量更低的治疗,降低耐药性产生的风险,改善患者预后。未来的研究应侧重于阐明协同作用的确切机制,并探索这些组合的临床适用性。
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引用次数: 0
Gut microbiota modulation through Traditional Chinese Medicine (TCM) - improving outcomes in Gastrointestinal (GI) cancer prevention and management 通过中医药(TCM)调节肠道微生物群--改善胃肠道(GI)癌症预防和管理的效果
Pub Date : 2024-11-02 DOI: 10.1016/j.prmcm.2024.100528
Yuying Wang , Yu Zeng , Xiaoli Chen , Aiping Lu , Wei Jia , Kenneth CP Cheung
<div><h3>Introduction</h3><div>Gastrointestinal (GI) cancers, such as colorectal cancer, pancreatic cancer and gastric malignancies, are increasing in prevalence and are notorious for poor prognosis and lack of satisfactory curative therapies. Emerging evidence indicates that the trillions of gut microbiotas in the GI tract play a crucial role in maintaining health and preventing disease, making it a promising target in GI cancer management. Additionally, the longstanding tradition and wisdom of Traditional Chinese medicine (TCM) are appreciated for offering valuable insights to complement current therapies against GI cancers. According to TCM principles, GI disorders are primarily attributed to ‘Qi-deficiency’ and disharmony among organs functions and Yin-yang imbalance. Treatment strategies not only include herbal formulations but also encompass non-pharmacological methods. For instance, well-known remedies such as Gegan Qing Lian Decoctions and Aidi injection have a long-standing history of treating GI disorders. These herbal combinations are considered Qi tonics which address the root causes of GI cancer. Furthermore, Reishi Mushroom and Ginseng are for their immune-supportive properties and ability to enhance overall vitality. Turmeric and Chinese rhubarb are noted for their anti-inflammatory, detoxifying and blood-nourishing effects. TCM also incorporates non-pharmacological interventions such as acupuncture and moxibustion, which may yield synergistic effects. The therapeutic benefits of these approaches, coupled with their symptom-relieving abilities, have provided insights for the potential integration with conventional treatments such as immunotherapy and chemotherapy. Several clinical trials have demonstrated positive outcomes, highlighting the involvement of gut microbiota in mediating the effects of these herbal interventions within the GI environment.</div></div><div><h3>Methods</h3><div>A comprehensive literature search was conducted using keywords including Traditional Chinese medicines (TCMs), Gastrointestinal (GI) cancers, gut microbiota, dysbiosis, GI disorders. Initially, a total of 300 articles published up to 2024 were identified, of which 180 articles were selected for inclusion in this review based on their relevance to TCM interventions and the modulation of gut microbiota in relation to GI cancer, either directly or indirectly. A variety of study designs including meta-analyses, systematic reviews, randomized controlled trials, and studies conducted on both human and rats are included.</div></div><div><h3>Results</h3><div>This review highlights the functions of gut microbiota and the implications of microbial dysbiosis in GI carcinogenesis, specifically focusing on the mechanisms that link disruptions in gut microbial communities to cancer progression. Additionally, it highlights the potential integration of Traditional Chinese Medicine into conventional cancer treatment and management by both pharmacological and non-pha
导言:胃肠道癌症(如结肠直肠癌、胰腺癌和胃恶性肿瘤)的发病率越来越高,而且因预后不良和缺乏令人满意的治疗方法而臭名昭著。新的证据表明,消化道中数以万计的肠道微生物在维持健康和预防疾病方面发挥着至关重要的作用,这使其成为消化道癌症治疗中一个前景广阔的靶点。此外,传统中医药的悠久传统和智慧为补充目前的消化道癌症疗法提供了宝贵的见解,值得赞赏。根据中医原理,消化道疾病主要归因于 "气虚"、脏腑功能失调和阴阳失衡。治疗策略不仅包括中药配方,还包括非药物治疗方法。例如,葛根清连煎和艾地注射液等著名疗法在治疗消化道疾病方面有着悠久的历史。这些中药组合被视为补气药,可从根本上治疗消化道癌症。此外,灵芝和人参具有增强免疫力和提高整体活力的作用。姜黄和大黄具有抗炎、解毒和养血的功效。中医还采用针灸等非药物干预措施,这些措施可能会产生协同效应。这些方法的治疗效果及其缓解症状的能力,为与免疫疗法和化疗等常规疗法的潜在结合提供了启示。几项临床试验显示了积极的结果,突出了肠道微生物群在消化道环境中参与介导这些中草药干预措施的效果。初步确定了截至 2024 年发表的 300 篇文章,根据这些文章与中医干预措施以及肠道微生物群与消化道癌症的直接或间接关系,从中选出 180 篇文章纳入本综述。结果本综述强调了肠道微生物群的功能以及微生物菌群失调对消化道癌症发生的影响,特别关注了肠道微生物群落紊乱与癌症进展之间的关联机制。讨论该综述讨论了基于中医药的干预措施在调节微生物组和缓解消化道癌症方面的潜力,以及中医药与肠道微生物群相互作用的机制。此外,它还强调了在消化道癌症治疗中采用基于微生物组的创新方法的必要性。总之,以微生物为基础、结合中医药的更有效策略亟待开发,这也凸显了临床试验的未来方向,即探索中医药参与消化道癌症治疗的更多可能性。尽管化疗和免疫疗法等传统疗法依然重要,但中医药的结合可作为消化道治疗的补充策略。为加深对中医药与微生物组相互作用的了解,应开展高质量、安慰剂对照、随机、双盲的临床试验。
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引用次数: 0
In-vitro modulation of glucose and lipid metabolism by Lentinula edodes extracts in obesity and type 2 diabetes models 在肥胖症和 2 型糖尿病模型中,小扁豆提取物对葡萄糖和脂质代谢的体外调节作用
Pub Date : 2024-11-01 DOI: 10.1016/j.prmcm.2024.100540
Jasmeet Kaur , Farheen Azad , Anish Murtaja Alam Khan , Mohd. Farzaan , Javed Ahmad , Humaira Farooqi , Kailash Chandra , Bibhu Prasad Panda

Introduction

Lentinula edodes (shiitake mushroom) has been integral to Traditional Chinese Medicine (TCM) for centuries, with its cultivation dating back to the Song dynasty (960–1127) in China. Traditionally valued for its immune-boosting properties, L. edodes is now being studied for its potential in managing metabolic disorders like obesity and type 2 diabetes. This study examines the effects of L. edodes fruiting body extract on key metabolic pathways related to glucose metabolism and lipid regulation.

Methods

Fruiting body extracts of Lentinula edodes including water, ethanolic, methanolic, and hydroalcoholic (50:50, 75:25, 25:75) were tested on L6 myoblasts. The study evaluated glucose uptake, GLUT4 expression, p-AMPK activation, and gene expression levels of PPARγ, AMPK, UCP-1, and FASN. Comparisons were made with control groups and standards like berberine and insulin.

Results

The hydroalcoholic extracts (50:50 and 75:25) significantly enhanced glucose uptake (p < 0.001) and GLUT4 translocation, similar to the effects of insulin (p < 0.0001) and berberine (p < 0.0001). These extracts also upregulated p-AMPK (p < 0.0001) and UCP-1 expression (7.621), indicating improved insulin sensitivity and thermogenic activity. Additionally, these extracts differentially regulated PPARγ and FASN, suggesting a complex interaction with lipid metabolism. Notably, FASN expression was highly upregulated in water extract (37.792), indicating potential implications for fatty acid synthesis and storage.

Discussion

Lentinula edodes shows significant potential as a functional food for managing obesity and diabetes, supporting traditional TCM practices with modern scientific evidence. The study suggests that L. edodes can modulate key metabolic pathways such as glucose uptake, AMPK signalling, PPARγ regulation, and upregulation of FASN and UCP-1, making it a promising natural therapeutic agent. Further research, including clinical trials, is necessary to confirm these benefits in humans and explore the underlying mechanisms.
导言:几个世纪以来,香菇一直是中药中不可或缺的成分,其栽培可追溯到中国宋朝(960-1127 年)。传统上,香菇具有增强免疫力的功效,现在,人们正在研究香菇在控制肥胖和 2 型糖尿病等代谢性疾病方面的潜力。本研究探讨了扁豆果实提取物对葡萄糖代谢和脂质调节相关的关键代谢途径的影响。方法在 L6 肌母细胞上测试了扁豆果实提取物,包括水、乙醇、甲醇和水醇(50:50、75:25、25:75)。研究评估了葡萄糖摄取、GLUT4 表达、p-AMPK 激活以及 PPARγ、AMPK、UCP-1 和 FASN 的基因表达水平。结果水醇提取物(50:50 和 75:25)显著增强了葡萄糖摄取(p < 0.001)和 GLUT4 转位,与胰岛素(p < 0.0001)和小檗碱(p < 0.0001)的效果相似。这些提取物还能上调 p-AMPK (p < 0.0001) 和 UCP-1 的表达 (7.621),表明胰岛素敏感性和生热活性得到改善。此外,这些提取物对 PPARγ 和 FASN 有不同的调节作用,表明它们与脂质代谢之间存在复杂的相互作用。值得注意的是,水提取物中 FASN 的表达高度上调(37.792),表明其对脂肪酸的合成和储存具有潜在影响。研究表明,龙胆草可调节葡萄糖摄取、AMPK 信号、PPARγ 调节、FASN 和 UCP-1 上调等关键代谢途径,使其成为一种有前景的天然治疗药物。要想在人体中证实这些益处并探索其潜在机制,还需要进一步的研究,包括临床试验。
{"title":"In-vitro modulation of glucose and lipid metabolism by Lentinula edodes extracts in obesity and type 2 diabetes models","authors":"Jasmeet Kaur ,&nbsp;Farheen Azad ,&nbsp;Anish Murtaja Alam Khan ,&nbsp;Mohd. Farzaan ,&nbsp;Javed Ahmad ,&nbsp;Humaira Farooqi ,&nbsp;Kailash Chandra ,&nbsp;Bibhu Prasad Panda","doi":"10.1016/j.prmcm.2024.100540","DOIUrl":"10.1016/j.prmcm.2024.100540","url":null,"abstract":"<div><h3>Introduction</h3><div><em>Lentinula edodes</em> (shiitake mushroom) has been integral to Traditional Chinese Medicine (TCM) for centuries, with its cultivation dating back to the Song dynasty (960–1127) in China. Traditionally valued for its immune-boosting properties, L. <em>edodes</em> is now being studied for its potential in managing metabolic disorders like obesity and type 2 diabetes. This study examines the effects of L. <em>edodes</em> fruiting body extract on key metabolic pathways related to glucose metabolism and lipid regulation.</div></div><div><h3>Methods</h3><div>Fruiting body extracts of <em>Lentinula edodes</em> including water, ethanolic, methanolic, and hydroalcoholic (50:50, 75:25, 25:75) were tested on L6 myoblasts. The study evaluated glucose uptake, GLUT4 expression, p-AMPK activation, and gene expression levels of PPARγ, AMPK, UCP-1, and FASN. Comparisons were made with control groups and standards like berberine and insulin.</div></div><div><h3>Results</h3><div>The hydroalcoholic extracts (50:50 and 75:25) significantly enhanced glucose uptake (<em>p</em> &lt; 0.001) and GLUT4 translocation, similar to the effects of insulin (<em>p</em> &lt; 0.0001) and berberine (<em>p</em> &lt; 0.0001). These extracts also upregulated p-AMPK (<em>p</em> &lt; 0.0001) and UCP-1 expression (7.621), indicating improved insulin sensitivity and thermogenic activity. Additionally, these extracts differentially regulated PPARγ and FASN, suggesting a complex interaction with lipid metabolism. Notably, FASN expression was highly upregulated in water extract (37.792), indicating potential implications for fatty acid synthesis and storage.</div></div><div><h3>Discussion</h3><div><em>Lentinula edodes</em> shows significant potential as a functional food for managing obesity and diabetes, supporting traditional TCM practices with modern scientific evidence. The study suggests that L. <em>edodes</em> can modulate key metabolic pathways such as glucose uptake, AMPK signalling, PPARγ regulation, and upregulation of FASN and UCP-1, making it a promising natural therapeutic agent. Further research, including clinical trials, is necessary to confirm these benefits in humans and explore the underlying mechanisms.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100540"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142593703","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Xylopia parviflora (A. rich.) benth. Mitigates anxiety behavior and chronic mild stress-induced depression-like behavior in mice: The involvement of biogenic amine neurotransmitters, cyclooxygenase-2 and stress biomarkers in its antidepressant activity Xylopia parviflora (A. rich.) benth.减轻小鼠的焦虑行为和慢性轻度应激诱发的抑郁样行为:生物胺神经递质、环氧化酶-2 和应激生物标志物参与其抗抑郁活性
Pub Date : 2024-11-01 DOI: 10.1016/j.prmcm.2024.100541
Abdullahi A. Murtala , Elijah O. Oyinloye , Farouk A. Oladoja , Samuel M. Fageyinbo , Holiness A. Olasore , Luqman O. Ogunjimi , Akinyinka A. Alabi , Wasiu E. Olooto , Oluwatosin O. Soyinka , Abayomi S. Faponle , Oluwatoyin O. Shonde , Luqmon E. Osipitan , Emmanuel O. Kasumu , Olusola O. Joseph , Emmanuel O. Olaniran , Esther F. Olatunji

Background

Xylopia parviflora is a novel botanical in Modern Chinese Medicine that contains bioactive constituents including alkaloids, flavonoids, and terpenoids, which are the pharmacologically active components in various Chinese herbal formulations such as Coptis chinensis (alkaloid-rich herbs), Ginkgo biloba (flavonoid-rich herbs) and Artemisia annua (terpenoid-rich herbs).

Objective

This investigation sought to evaluate the anxiolytic and antidepressant-like effects of the hydroethanol leaf extract of Xylopia parviflora using mouse models. We elucidated the roles of noradrenaline, serotonin, cyclooxygenase-2, and reactive oxidative species in mediating its antidepressant effects, providing a fresh perspective on the pharmacological activity of Xylopia parviflora.

Methods

The acute toxicity of XPE was assessed following OECD guideline 420. Established behavioral tests were used to evaluate the anxiolytic (including the hole-board, open field, elevated plus maze, and light/dark exploration assessments) and antidepressant (encompassing the forced swim and tail suspension tests) effects of the extract. Mice received treatments of distilled water (10 mL/kg, serving as the negative control), fluoxetine (20 mg/kg, acting as the reference medication), and XPE (at doses of 50, 100, and 200 mg/kg). The concentrations of noradrenaline, serotonin, and COX-2 within the brain tissue were quantified using ELISA kits. The levels of antioxidant biomarkers were evaluated using standardized commercial assay kits.

Results

The oral/intraperitoneal LD50 for the extract was established at 2000 mg/kg. In the behavioral assessments designed to measure anxiolytic effects, XPE significantly mitigated anxiety levels in mice, as evidenced by an increase in exploratory behaviors (including head dips, sectional crossings, general square crossings, rearing, and assisted rearing) and an increased time spent in the brightly illuminated compartments. Concerning the antidepressant evaluations, XPE significantly reduced depression-like behaviors in mice, which was indicated by an increased latency to immobility and a decrease in the duration of immobility. XPE was found to modulate noradrenaline and serotonin transmissions, attenuate oxidative species, and inhibit COX-2 activity.

Conclusion

The findings above demonstrate that Xylopia parviflora possesses anxiolytic and antidepressant-like activities. The antidepressant property of XPE, as revealed in this study, may be attributable to the enhancement of biogenic amines (specifically noradrenaline and serotonin), the suppression of oxidative species, and the inhibition of COX-2 activity.
背景半枝莲是现代中药中的一种新植物,它含有生物活性成分,包括生物碱、黄酮类和萜类化合物,这些成分是各种中药配方(如富含生物碱的黄连、富含黄酮类的银杏叶和富含萜类化合物的黄花蒿)中的药理活性成分。本研究试图利用小鼠模型评估西洛巴叶的水乙醇叶提取物的抗焦虑和抗抑郁作用。我们阐明了去甲肾上腺素、5-羟色胺、环氧化酶-2 和活性氧化物在介导其抗抑郁作用中的作用,为研究西洋参的药理活性提供了一个全新的视角。使用既定的行为测试来评估该提取物的抗焦虑(包括洞穴板、开阔地、高架加迷宫和光/暗探索评估)和抗抑郁(包括强迫游泳和尾悬试验)作用。小鼠分别接受蒸馏水(10 毫升/千克,作为阴性对照)、氟西汀(20 毫克/千克,作为参考药物)和 XPE(剂量分别为 50、100 和 200 毫克/千克)的治疗。使用酶联免疫吸附试剂盒对脑组织中去甲肾上腺素、血清素和 COX-2 的浓度进行量化。使用标准化的商业检测试剂盒对抗氧化生物标志物的水平进行了评估。结果确定提取物的口服/腹腔半数致死剂量为 2000 毫克/千克。在旨在测量抗焦虑作用的行为评估中,XPE 显著减轻了小鼠的焦虑水平,表现为探索行为(包括头部下沉、断面穿越、一般方形穿越、饲养和辅助饲养)的增加以及在明亮照明隔间中停留时间的增加。在抗抑郁评估方面,XPE 显著减少了小鼠的抑郁样行为,表现为不动潜伏期延长,不动持续时间缩短。研究发现,XPE 可调节去甲肾上腺素和血清素的传递,减少氧化物种,抑制 COX-2 活性。本研究揭示的 XPE 抗抑郁特性可能归因于生物胺(特别是去甲肾上腺素和血清素)的增强、氧化物种的抑制以及 COX-2 活性的抑制。
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引用次数: 0
Virtual screening and lead optimization of Desmostachya bipinnata-derived FGFR inhibitors for oral squamous cell carcinoma management 用于口腔鳞状细胞癌治疗的 Desmostachya bipinnata 衍生 FGFR 抑制剂的虚拟筛选和先导优化
Pub Date : 2024-10-31 DOI: 10.1016/j.prmcm.2024.100534
Nitya Krishnasamy , Ramya Ramadoss , Swarnalakshmi Raman

Background

Oral cancer remains a major global health challenge with limited therapeutic options, highlighting the need for novel treatments. Phytochemicals derived from Desmostachya bipinnata (Db), a plant used in traditional Chinese medicine for its anti-inflammatory and analgesic properties, have demonstrated potential anti-cancer effects. However, their mechanisms of action, particularly in targeting Fibroblast Growth Factor Receptor (FGFR) in oral cancer, are not well characterized.

Objective

This study aimed to leverage in-silico drug design methodologies to identify bioactive compounds from Db with potential FGFR-inhibiting activity for the treatment of oral cancer.

Methodology

An MTT assay was conducted using KB cell lines to evaluate cytotoxic effects, while thirty-eight phytochemicals from Db were screened through in silico approaches for their pharmacokinetics, toxicity, and drug-likeness. Molecular docking studies were performed to assess binding affinities to the FGFR protein. The biological activity and toxicity of the compounds were predicted to prioritize candidates for further investigation.

Results

Fourteen compounds were identified as promising candidates based on their drug-like properties, favourable pharmacokinetic profiles, significant FGFR binding affinities, and predicted anti-cancer activity. These compounds also demonstrated potential for oral bioavailability and central nervous system penetration, supporting their candidacy for further drug development. Notably, the traditional use of Desmostachya bipinnata in TCM emphasizes its role in enhancing overall vitality and immune function, which may synergize with the identified FGFR-inhibiting properties in the context of oral cancer treatment

Conclusion

The phytochemicals from Desmostachya bipinnata exhibit significant potential as FGFR-targeted therapeutic agents for oral cancer. Further experimental validation and optimization of these lead compounds could contribute to the development of novel, effective treatments for oral cancer and related conditions
背景口腔癌仍然是全球健康面临的一个重大挑战,但治疗方法有限,这凸显了对新型治疗方法的需求。传统中药中使用的一种植物 Desmostachya bipinnata(Db)具有消炎和镇痛特性,从这种植物中提取的植物化学物质已被证明具有潜在的抗癌作用。然而,它们的作用机制,尤其是针对口腔癌中成纤维细胞生长因子受体(FGFR)的作用机制,还没有得到很好的表征。本研究旨在利用体内药物设计方法,从 Db 中鉴定出具有潜在 FGFR 抑制活性的生物活性化合物,用于治疗口腔癌。方法使用 KB 细胞系进行 MTT 试验以评估细胞毒性效应,同时通过硅学方法筛选 38 种来自 Db 的植物化学物质,以确定其药代动力学、毒性和药物相似性。分子对接研究评估了与表皮生长因子受体蛋白的结合亲和力。结果根据化合物的类药物特性、良好的药代动力学特征、明显的 FGFR 结合亲和力以及预测的抗癌活性,14 个化合物被确定为有希望的候选化合物。这些化合物还表现出了口服生物利用度和中枢神经系统渗透的潜力,为进一步的药物开发提供了支持。值得注意的是,传统中医使用双黄连强调其在增强整体活力和免疫功能方面的作用,在口腔癌治疗中,这可能与已发现的表皮生长因子受体抑制特性产生协同作用。对这些先导化合物的进一步实验验证和优化将有助于开发新型、有效的口腔癌及相关疾病的治疗方法。
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引用次数: 0
Exploration of the key active ingredients and mechanisms of Sparganii Rhizoma-Curcumae Rhizoma compatible formulation against human colorectal cancer through network pharmacology and in vitro experiments 通过网络药理学和体外实验,探索 Sparganii Rhizoma-Curcumae Rhizoma 兼容制剂的主要活性成分和抗人类结直肠癌的机制
Pub Date : 2024-10-30 DOI: 10.1016/j.prmcm.2024.100532
Hongyan Lin , Dongxuan Ai , Xinling Wang , Shuaijun Cui , Xinghong Li , Bangmei Ye , Lingyu Ruan , Jing Xu , Liqun Wang

Introduction

Sparganii Rhizoma-Curcumae Rhizoma (SR-CR) formulation may offer an effective treatment for human colorectal cancer (CRC). However, the active ingredients and underlying mechanisms of this herbal formulation remain unclear.

Methods

This study integrates network pharmacology, molecular docking and experimental verification to identify key active ingredients and elucidate the mechanisms of SR-CR in CRC treatment.

Results

Twenty-three active components of SR-CR were identified using the TCMSP, UniProt and Gene Cards databases. These components were associated with 178 targets, of which 118 are directly related to CRC. Protein-protein interaction (PPI) network analysis identified protein kinase B (AKT) 1, epidermal growth factor receptor (EGFR), SRC, Bcl2 and CASP3 as core anti-CRC targets. Gene Ontology (GO) and KEGG pathway analyses were performed on these 178 intersecting targets, and the results showed that these targets are involved in EGFR tyrosine kinase inhibitor resistance and AGE-RAGE signaling pathway in diabetic complications. At the same time, five compounds, including bisdemethoxycurcumin, formononetin, β-sitosterol, stigmasterol and hederagenin, were selected based on the target number of effective components and tested for cytotoxicity against human CRC cell lines HT-29, HCT-8 and HCT-116 in vitro. The results showed that bisdemethoxycurcumin exhibited significant anti-proliferative activity against HCT-116 cells. Molecular docking results indicated that bisdemethoxycurcumin effectively binds with AKT, EGFR, Bcl-2 and CASP3. Further pharmacological experiments demonstrated that bisdemethoxycurcumin inhibits HCT-116 cell proliferation and migration via inhibiting EGFR-AKT pathway, and induces apoptosis by up-regulating Bcl-2 expression.

Discussion

Based on our study, inhibiting the EGFR-AKT pathway and upregulating Bcl2 may be one of the mechanisms by which SR-CR inhibits the growth of CRC. The main active ingredients of SR-CR include bisdemethoxycurcumin, formononetin, β-sitosterol, stigmasterol and hederagenin, which may exert anti-colon cancer activity by targeting the regulation of AKT, EGFR, Bcl-2 and CASP3. However, we need more in vitro and in vivo evidence to confirm this conclusion. This study lays the foundation for further research on the pharmacological mechanism of SR-CR in the treatment of CRC.
引言 天冬-莪术(SR-CR)制剂可有效治疗人类结直肠癌(CRC)。方法本研究整合了网络药理学、分子对接和实验验证等方法,以确定SR-CR的关键活性成分,并阐明SR-CR治疗CRC的机制。这些成分与 178 个靶点相关,其中 118 个与 CRC 直接相关。蛋白-蛋白相互作用(PPI)网络分析发现蛋白激酶B(AKT)1、表皮生长因子受体(EGFR)、SRC、Bcl2和CASP3是抗CRC的核心靶点。对这178个交叉靶点进行了基因本体(GO)和KEGG通路分析,结果表明这些靶点参与了表皮生长因子受体酪氨酸激酶抑制剂耐药性和糖尿病并发症中的AGE-RAGE信号通路。同时,根据有效成分的靶点数量,筛选出双去甲氧基姜黄素、甲萘素、β-谷甾醇、豆甾醇和鸡豆皂苷(hederagenin)等5个化合物,并在体外测试了它们对人CRC细胞株HT-29、HCT-8和HCT-116的细胞毒性。结果表明,双去甲氧基姜黄素对 HCT-116 细胞具有显著的抗增殖活性。分子对接结果表明,双去甲氧基姜黄素能有效地与 AKT、表皮生长因子受体、Bcl-2 和 CASP3 结合。讨论根据我们的研究,抑制表皮生长因子受体-AKT通路和上调Bcl2可能是SR-CR抑制CRC生长的机制之一。SR-CR的主要活性成分包括双去甲氧基姜黄素、甲萘素、β-谷甾醇、豆甾醇和赤芍素,它们可能通过靶向调控AKT、EGFR、Bcl-2和CASP3而发挥抗结肠癌活性。然而,我们需要更多的体外和体内证据来证实这一结论。本研究为进一步研究 SR-CR 治疗 CRC 的药理机制奠定了基础。
{"title":"Exploration of the key active ingredients and mechanisms of Sparganii Rhizoma-Curcumae Rhizoma compatible formulation against human colorectal cancer through network pharmacology and in vitro experiments","authors":"Hongyan Lin ,&nbsp;Dongxuan Ai ,&nbsp;Xinling Wang ,&nbsp;Shuaijun Cui ,&nbsp;Xinghong Li ,&nbsp;Bangmei Ye ,&nbsp;Lingyu Ruan ,&nbsp;Jing Xu ,&nbsp;Liqun Wang","doi":"10.1016/j.prmcm.2024.100532","DOIUrl":"10.1016/j.prmcm.2024.100532","url":null,"abstract":"<div><h3>Introduction</h3><div><em>Sparganii Rhizoma</em>-<em>Curcumae Rhizoma</em> (SR-CR) formulation may offer an effective treatment for human colorectal cancer (CRC). However, the active ingredients and underlying mechanisms of this herbal formulation remain unclear.</div></div><div><h3>Methods</h3><div>This study integrates network pharmacology, molecular docking and experimental verification to identify key active ingredients and elucidate the mechanisms of SR-CR in CRC treatment.</div></div><div><h3>Results</h3><div>Twenty-three active components of SR-CR were identified using the TCMSP, UniProt and Gene Cards databases. These components were associated with 178 targets, of which 118 are directly related to CRC. Protein-protein interaction (PPI) network analysis identified protein kinase B (AKT) 1, epidermal growth factor receptor (EGFR), SRC, Bcl2 and CASP3 as core anti-CRC targets. Gene Ontology (GO) and KEGG pathway analyses were performed on these 178 intersecting targets, and the results showed that these targets are involved in EGFR tyrosine kinase inhibitor resistance and AGE-RAGE signaling pathway in diabetic complications. At the same time, five compounds, including bisdemethoxycurcumin, formononetin, β-sitosterol, stigmasterol and hederagenin, were selected based on the target number of effective components and tested for cytotoxicity against human CRC cell lines HT-29, HCT-8 and HCT-116 <em>in vitro</em>. The results showed that bisdemethoxycurcumin exhibited significant anti-proliferative activity against HCT-116 cells. Molecular docking results indicated that bisdemethoxycurcumin effectively binds with AKT, EGFR, Bcl-2 and CASP3. Further pharmacological experiments demonstrated that bisdemethoxycurcumin inhibits HCT-116 cell proliferation and migration via inhibiting EGFR-AKT pathway, and induces apoptosis by up-regulating Bcl-2 expression.</div></div><div><h3>Discussion</h3><div>Based on our study, inhibiting the EGFR-AKT pathway and upregulating Bcl2 may be one of the mechanisms by which SR-CR inhibits the growth of CRC. The main active ingredients of SR-CR include bisdemethoxycurcumin, formononetin, β-sitosterol, stigmasterol and hederagenin, which may exert anti-colon cancer activity by targeting the regulation of AKT, EGFR, Bcl-2 and CASP3. However, we need more <em>in vitro</em> and <em>in vivo</em> evidence to confirm this conclusion. This study lays the foundation for further research on the pharmacological mechanism of SR-CR in the treatment of CRC.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100532"},"PeriodicalIF":0.0,"publicationDate":"2024-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142553556","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Hypoglycemic and antihyperglycemic effects of Abelmoschus esculentus and Alchornea cordifolia in normal and alloxan-induced diabetic rats 阿贝摩斯和虫草对正常大鼠和阿脲诱导的糖尿病大鼠的降血糖和抗高血糖作用
Pub Date : 2024-10-29 DOI: 10.1016/j.prmcm.2024.100531
Barnabé Lucien Nkono Ya Nkono , Adjia Hamadjida , Damolai Gounkagou , Fidèle Ntchapda , Sélestin Sokeng Dongmo , Pierre Kamtchouing
<div><h3>Background</h3><div><em>Abelmoschus esculentus</em> and <em>Alchornea cordifolia</em> are commonly used in Traditional Chinese Medicine (TCM) to treat several diseases. <em>Abelmoschus esculentus</em> is used to treat infertility and menorrhagia, while <em>Alchornea cordifolia</em> is used for the treatment of venereal diseases, cough, and diarrhoea. However, very few studies assessed the antidiabetic effects of these plants. Therefore, this study aimed to investigate the hypoglycemic and antihyperglycemic effects of aqueous extract of <em>A. esculentus</em> fruits and <em>A. cordifolia</em> leaves.</div></div><div><h3>Material and Methods</h3><div>Fresh Abelmoschus esculentus fruits and the powder from the dried leaves of <em>Alchornea cordifolia</em> leaves were prepared by maceration in the aqueous phase (200 mg/100 mL and 50 mg/100 mL respectively) for 24 h, then filtered and concentrated in an oven at 45 °C. Diabete was induced to male Wistar rats by a single intraperitoneal injection of alloxan (150 mg kg<sup>−1</sup>, b.w). Rats with a blood glucose level greater than or equal to 200 mg/dL were selected, divided into groups and were daily administered orally with either aqueous extracts of <em>A. esculentus</em> at 30 mg kg<sup>−1</sup> (AEAE30) or <em>A. cordifolia</em> at 400 mg kg<sup>−1</sup> (AEAC400) for 14 consecutive days. For comparison, acarbose (100 mg kg<sup>−1</sup>), glibenclamide (5 mg kg<sup>−1</sup>), and 500 mg kg<sup>−1</sup> metformin (Glucophage) were administered orally as reference drugs. Moreover, insuline was also used as a positive control and administered intraperitoneally at a dose of 5 IU/kg. Then, blood glucose levels, oral glucose tolerance test, oral maltose tolerance club, body weight and hemoglobin were assessed. For evaluation of the aqueous extracts in the intestinal transit, imodium (2mg kg<sup>−1</sup>, p.o) and fructine (5 mg kg<sup>−1</sup>, p.o) were used as a positive control to determine the spasmolytic and laxative activities, respectively. The histopathological study of the liver, kidney, pancreas, testis, epididymis, and seminal vesicle was also carried out using the hematoxyline & eosin (H&E) technique.</div></div><div><h3>Results</h3><div>AEAE30 and AEAC400 significantly reduced (<em>P</em> < 0.001) fasting blood glucose (FBG) levels and significantly prevented (<em>P</em> < 0.001) postprandial glycemia in AI-db rats following oral glucose tolerance test (OGTT) and oral maltose tolerance test (OMTT) in alloxan-induced diabetic rats (AI-db). In normoglycemic and insulin-resistant (IR) rats, AEAE30 significantly prevented the post-prandial blood glucose level during the OGTT (<em>P</em> < 0.01) only in normoglycemic rats. At the end of treatment, AEAE30 significantly reduced the relative weight of the liver (<em>P</em> < 0.01) and significantly increased (<em>P</em> < 0.001) the relative weight of the testes and pancreas while AEAC400 significantly increased the
背景传统中医常用阿胶和蛇床子来治疗多种疾病。大腹皮用于治疗不孕症和月经过多,而蛇床子则用于治疗性病、咳嗽和腹泻。然而,很少有研究对这些植物的抗糖尿病作用进行评估。材料和方法将新鲜的阿贝莫斯(Abelmoschus esculentus)果实和堇菜(Alchornea cordifolia)干叶粉末分别浸泡在 200 毫克/100 毫升和 50 毫克/100 毫升的水溶液中 24 小时,然后过滤并在 45 °C的烘箱中浓缩。给雄性 Wistar 大鼠腹腔注射一次阿脲(150 毫克/千克-1,体重),诱发糖尿病。筛选出血糖水平大于或等于 200 mg/dL 的大鼠,将其分成若干组,每天口服 30 mg kg-1 的 A. esculentus 水提取物(AEAE30)或 400 mg kg-1 的 A. cordifolia 水提取物(AEAC400),连续 14 天。作为对比,口服阿卡波糖(100 毫克/千克)、格列本脲(5 毫克/千克)和 500 毫克/千克二甲双胍(Glucophage)作为参考药物。此外,还使用胰岛素作为阳性对照,以 5 IU/kg 的剂量腹腔注射。然后评估血糖水平、口服葡萄糖耐量试验、口服麦芽糖耐量俱乐部、体重和血红蛋白。为了评估水提取物在肠道转运中的作用,使用了易蒙停(2 毫克/千克,p.o)和果碱(5 毫克/千克,p.o)作为阳性对照,分别测定其解痉和通便活性。此外,还使用苏木精&伊红(H&E)技术对肝脏、肾脏、胰腺、睾丸、附睾和精囊进行了组织病理学研究。结果 AEAE30 和 AEAC400 能明显降低(P <0.001)空腹血糖(FBG)水平,并能明显防止(P <0.001)阿糖诱导糖尿病大鼠(AI-db)在进行口服葡萄糖耐量试验(OGTT)和口服麦芽糖耐量试验(OMTT)后出现餐后血糖。在正常血糖大鼠和胰岛素抵抗(IR)大鼠的 OGTT 试验中,AEAE30 仅在正常血糖大鼠中能显著降低餐后血糖水平(P < 0.01)。治疗结束时,与未治疗的 AI-db 大鼠相比,AEEAE30 能明显降低肝脏的相对重量(P < 0.01),明显增加睾丸和胰腺的相对重量(P < 0.001),而 AEAC400 能明显增加睾丸的相对重量。组织病理学研究表明,经植物提取物处理的 AI-db 动物阿脲诱导的组织损伤恢复到了接近正常对照组的水平,附睾中的精子密度也增加了,这与未经处理的 AI-db 组不同。
{"title":"Hypoglycemic and antihyperglycemic effects of Abelmoschus esculentus and Alchornea cordifolia in normal and alloxan-induced diabetic rats","authors":"Barnabé Lucien Nkono Ya Nkono ,&nbsp;Adjia Hamadjida ,&nbsp;Damolai Gounkagou ,&nbsp;Fidèle Ntchapda ,&nbsp;Sélestin Sokeng Dongmo ,&nbsp;Pierre Kamtchouing","doi":"10.1016/j.prmcm.2024.100531","DOIUrl":"10.1016/j.prmcm.2024.100531","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Background&lt;/h3&gt;&lt;div&gt;&lt;em&gt;Abelmoschus esculentus&lt;/em&gt; and &lt;em&gt;Alchornea cordifolia&lt;/em&gt; are commonly used in Traditional Chinese Medicine (TCM) to treat several diseases. &lt;em&gt;Abelmoschus esculentus&lt;/em&gt; is used to treat infertility and menorrhagia, while &lt;em&gt;Alchornea cordifolia&lt;/em&gt; is used for the treatment of venereal diseases, cough, and diarrhoea. However, very few studies assessed the antidiabetic effects of these plants. Therefore, this study aimed to investigate the hypoglycemic and antihyperglycemic effects of aqueous extract of &lt;em&gt;A. esculentus&lt;/em&gt; fruits and &lt;em&gt;A. cordifolia&lt;/em&gt; leaves.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Material and Methods&lt;/h3&gt;&lt;div&gt;Fresh Abelmoschus esculentus fruits and the powder from the dried leaves of &lt;em&gt;Alchornea cordifolia&lt;/em&gt; leaves were prepared by maceration in the aqueous phase (200 mg/100 mL and 50 mg/100 mL respectively) for 24 h, then filtered and concentrated in an oven at 45 °C. Diabete was induced to male Wistar rats by a single intraperitoneal injection of alloxan (150 mg kg&lt;sup&gt;−1&lt;/sup&gt;, b.w). Rats with a blood glucose level greater than or equal to 200 mg/dL were selected, divided into groups and were daily administered orally with either aqueous extracts of &lt;em&gt;A. esculentus&lt;/em&gt; at 30 mg kg&lt;sup&gt;−1&lt;/sup&gt; (AEAE30) or &lt;em&gt;A. cordifolia&lt;/em&gt; at 400 mg kg&lt;sup&gt;−1&lt;/sup&gt; (AEAC400) for 14 consecutive days. For comparison, acarbose (100 mg kg&lt;sup&gt;−1&lt;/sup&gt;), glibenclamide (5 mg kg&lt;sup&gt;−1&lt;/sup&gt;), and 500 mg kg&lt;sup&gt;−1&lt;/sup&gt; metformin (Glucophage) were administered orally as reference drugs. Moreover, insuline was also used as a positive control and administered intraperitoneally at a dose of 5 IU/kg. Then, blood glucose levels, oral glucose tolerance test, oral maltose tolerance club, body weight and hemoglobin were assessed. For evaluation of the aqueous extracts in the intestinal transit, imodium (2mg kg&lt;sup&gt;−1&lt;/sup&gt;, p.o) and fructine (5 mg kg&lt;sup&gt;−1&lt;/sup&gt;, p.o) were used as a positive control to determine the spasmolytic and laxative activities, respectively. The histopathological study of the liver, kidney, pancreas, testis, epididymis, and seminal vesicle was also carried out using the hematoxyline &amp; eosin (H&amp;E) technique.&lt;/div&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Results&lt;/h3&gt;&lt;div&gt;AEAE30 and AEAC400 significantly reduced (&lt;em&gt;P&lt;/em&gt; &lt; 0.001) fasting blood glucose (FBG) levels and significantly prevented (&lt;em&gt;P&lt;/em&gt; &lt; 0.001) postprandial glycemia in AI-db rats following oral glucose tolerance test (OGTT) and oral maltose tolerance test (OMTT) in alloxan-induced diabetic rats (AI-db). In normoglycemic and insulin-resistant (IR) rats, AEAE30 significantly prevented the post-prandial blood glucose level during the OGTT (&lt;em&gt;P&lt;/em&gt; &lt; 0.01) only in normoglycemic rats. At the end of treatment, AEAE30 significantly reduced the relative weight of the liver (&lt;em&gt;P&lt;/em&gt; &lt; 0.01) and significantly increased (&lt;em&gt;P&lt;/em&gt; &lt; 0.001) the relative weight of the testes and pancreas while AEAC400 significantly increased the ","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100531"},"PeriodicalIF":0.0,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142657241","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Clinical formulation Zhigan Oral Liquid intervenes in alcoholic liver injury by regulating the intestinal flora and PI3K⧵AKT⧵NF-κB pathway 临床配方志甘口服液通过调节肠道菌群和PI3K⧵AKT⧵NF-κB途径干预酒精性肝损伤
Pub Date : 2024-10-24 DOI: 10.1016/j.prmcm.2024.100537
Yahong Zhao (赵亚红) , Dongyang Li (李东阳) , Shengchao Wang (王胜超) , Wenxia Zhao (赵文霞) , Zhenling Zhang (张振凌) , Hongwei Zhang (张宏伟) , Ruisheng Wang (王瑞生) , Yafang Hou (侯娅芳) , Meng Zhao (赵萌)

Introduction

Zhigan Oral Liquid (ZOL) was developed from the empirical formulation of Professor Zhao Wenxia, a nationally renowned practitioner of Chinese medicine, and it has been used in Chinese medicine for many years for the effective treatment of alcoholic liver damage (ALD). However, the interventional mechanism of action of the dosage indications for different stages of ALD pathogenesis is not clear.

Methods

The main chemical components of ZOL were qualitatively analyzed by ultra-high performance liquid chromatography (UHPLC-Q-Orbitrap HRMS) in tandem with quadrupole electrostatic field orbital well high resolution mass spectrometry and quantitatively analyzed by high-performance liquid chromatography (HPLC). Network pharmacological analysis was performed to predict the targets and pathways of the potential pharmacodynamic components. The pharmacodynamic effects and potential target mechanisms were verified in a murine model of ALD. To observe the effect of ZOL on the intestinal flora, 16s rDNA sequencing was performed on ALD mice.

Results

ZOL can achieve alcohol detoxification by increasing the activity of ALDH and other detoxification enzymes and can intervene in the process of alcoholic liver injury and liver fibrosis by regulating the alcohol-induced bacterial dysbiosis, increasing the level of antioxidants, and inhibiting the activation of the PI3KAKTNF-κB signaling pathway. Kakkalide, Luteolin, Puerarin, tectoridin, and dihydromyricetin are related to the flavonoids that may be the main pharmacodynamic components that exert their medicinal effects.

Conclusions

The findings have significant implications for the development of Empirical treatments for alcoholic liver injury. Furthermore, the study contributes to promoting development and utilization of new dosage forms of hospital preparations by emphasizing the composition identification and animal experimental efficacy of ZOL. Overall, this study provides valuable insights into establishing an alcohol-induced liver injury model, and demonstrates the potential of ZOL as a common treatment for alcoholic liver injury a rich source.
引言 滋肝口服液(Zhigan Oral Liquid,ZOL)是在全国著名中医赵文霞教授的经验方基础上研制而成的,多年来一直用于中医有效治疗酒精性肝损伤(ALD)。方法采用超高效液相色谱法(UHPLC-Q-Orbitrap HRMS)串联四极静电场轨道井高分辨率质谱法对 ZOL 的主要化学成分进行定性分析,并采用高效液相色谱法(HPLC)对其进行定量分析。进行了网络药理学分析,以预测潜在药效成分的靶点和途径。药效学效应和潜在靶点机制在小鼠 ALD 模型中得到了验证。结果ZOL能通过提高ALDH和其他解毒酶的活性实现解酒,并能通过调节酒精诱导的细菌失调、提高抗氧化剂水平和抑制PI3KAKTNF-κB信号通路的激活,干预酒精性肝损伤和肝纤维化的过程。Kakkalide、木犀草素、葛根素、桔梗苷和二氢杨梅素与黄酮类化合物有关,它们可能是发挥药效的主要药效学成分。此外,该研究通过强调 ZOL 的成分鉴定和动物实验疗效,有助于促进医院制剂新剂型的开发和利用。总之,本研究为建立酒精诱导的肝损伤模型提供了有价值的见解,并证明了 ZOL 作为酒精性肝损伤常用治疗方法的潜力。
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引用次数: 0
Green synthesis of Au nanoparticles by Scutellaria barbata extract for chemo-photothermal anticancer therapy 利用黄芩提取物绿色合成金纳米粒子用于化疗光热抗癌疗法
Pub Date : 2024-10-23 DOI: 10.1016/j.prmcm.2024.100536
Yinchuan Wang , Jia Chen , Yifan Bo , Jiacheng Chen , Yuan Liu , Zhanglong Li , Changyuan Yu , Jiahui Liu , Shihui Wang

Introduction

The combination of photothermal therapy and chemotherapy has emerged as a promising strategy for cancer treatment. The green synthesis of gold nanoparticles (Au NPs) using extracts from traditional Chinese medicine Scutellaria barbata D. Don (Scu) has revealed an economical, sustainable, and eco-friendly approach for the outstanding anticancer activities.

Methods

Scu extract was mixed with HAuCl4 solution to fabricate Scu-Au NPs. The synthesis process was optimized by varying the reaction temperature, reaction time, and HAuCl4 concentration. The changes in the components of Scu before and after synthesis were analyzed using the 3,5-dinitrosalicylic acid (DNS) reduction test, the rutin colorimetric method, and the Folin–Ciocalteu method. The morphology, size, and structure of Scu-Au NPs were characterized by TEM, DLS, XRD, and XPS. The photothermal characteristics induced by near-infrared (NIR) irradiation were assessed by continuously monitoring the temperature elevation. The anticancer activity and mechanisms of Scu-Au NPs were investigated using MTT assay, cell uptake studies, ROS level detection, cell apoptosis and necrosis assays, flow cytometry analysis, intracellular Caspase-3 protein activity fluorescence detection, and Western blot analysis on A549, 4T1, and RAW264.7 cells.

Results

Scu-Au NPs were successfully fabricated using Scu extract as a reducing agent. The Scu-Au NPs were spherical with a size of 50 nm. During the synthesis process, the levels of reducing sugars, flavonoids, and polyphenols in the Scu extract decreased by 80.8%, 54.3%, and 70.1%, respectively. Scu-Au NPs demonstrated excellent photothermal responsiveness, thermostability, and biocompatibility. For chemo-photothermal anticancer therapy, the cytotoxicity of Scu-Au NPs on 4T1 cells reached approximately 85% upon exposure to 808 nm NIR irradiation. The anticancer activity was attributed to the induction of apoptosis and necrosis, achieved by increasing intracellular ROS levels, causing cell cycle arrest at the S phase, and modulating the expression of apoptosis-related proteins.

Discussion

Our synthesized Scu-Au NPs exhibit favorable photothermal conversion characteristics, demonstrating excellent therapeutic efficacy and safety for cancer treatment.
导言:光热疗法与化疗的结合已成为一种前景广阔的癌症治疗策略。利用传统中药黄芩(Scutellaria barbata D. Don,Scu)提取物绿色合成金纳米粒子(Au NPs)是一种经济、可持续和生态友好的方法,具有显著的抗癌活性。通过改变反应温度、反应时间和 HAuCl4 浓度对合成过程进行了优化。采用 3,5-二硝基水杨酸(DNS)还原试验、芦丁比色法和 Folin-Ciocalteu 法分析了合成前后 Scu 成分的变化。TEM、DLS、XRD 和 XPS 对 Scu-Au NPs 的形貌、尺寸和结构进行了表征。通过连续监测温度升高,评估了近红外(NIR)照射诱导的光热特性。结果以 Scu 提取物为还原剂,成功制备了 Scu-Au NPs。Scu-Au NPs呈球形,大小为50 nm。在合成过程中,Scu 提取物中还原糖、黄酮类化合物和多酚类化合物的含量分别下降了 80.8%、54.3% 和 70.1%。Scu-Au NPs 具有优异的光热响应性、热稳定性和生物相容性。在化学光热抗癌疗法中,Scu-Au NPs 在 808 纳米近红外照射下对 4T1 细胞的细胞毒性达到约 85%。我们合成的 Scu-Au NPs 具有良好的光热转换特性,在癌症治疗中表现出卓越的疗效和安全性。
{"title":"Green synthesis of Au nanoparticles by Scutellaria barbata extract for chemo-photothermal anticancer therapy","authors":"Yinchuan Wang ,&nbsp;Jia Chen ,&nbsp;Yifan Bo ,&nbsp;Jiacheng Chen ,&nbsp;Yuan Liu ,&nbsp;Zhanglong Li ,&nbsp;Changyuan Yu ,&nbsp;Jiahui Liu ,&nbsp;Shihui Wang","doi":"10.1016/j.prmcm.2024.100536","DOIUrl":"10.1016/j.prmcm.2024.100536","url":null,"abstract":"<div><h3>Introduction</h3><div>The combination of photothermal therapy and chemotherapy has emerged as a promising strategy for cancer treatment. The green synthesis of gold nanoparticles (Au NPs) using extracts from traditional Chinese medicine <em>Scutellaria barbata D. Don</em> (Scu) has revealed an economical, sustainable, and eco-friendly approach for the outstanding anticancer activities.</div></div><div><h3>Methods</h3><div>Scu extract was mixed with HAuCl<sub>4</sub> solution to fabricate Scu-Au NPs. The synthesis process was optimized by varying the reaction temperature, reaction time, and HAuCl<sub>4</sub> concentration. The changes in the components of Scu before and after synthesis were analyzed using the 3,5-dinitrosalicylic acid (DNS) reduction test, the rutin colorimetric method, and the Folin–Ciocalteu method. The morphology, size, and structure of Scu-Au NPs were characterized by TEM, DLS, XRD, and XPS. The photothermal characteristics induced by near-infrared (NIR) irradiation were assessed by continuously monitoring the temperature elevation. The anticancer activity and mechanisms of Scu-Au NPs were investigated using MTT assay, cell uptake studies, ROS level detection, cell apoptosis and necrosis assays, flow cytometry analysis, intracellular Caspase-3 protein activity fluorescence detection, and Western blot analysis on A549, 4T1, and RAW264.7 cells.</div></div><div><h3>Results</h3><div>Scu-Au NPs were successfully fabricated using Scu extract as a reducing agent. The Scu-Au NPs were spherical with a size of 50 nm. During the synthesis process, the levels of reducing sugars, flavonoids, and polyphenols in the Scu extract decreased by 80.8%, 54.3%, and 70.1%, respectively. Scu-Au NPs demonstrated excellent photothermal responsiveness, thermostability, and biocompatibility. For chemo-photothermal anticancer therapy, the cytotoxicity of Scu-Au NPs on 4T1 cells reached approximately 85% upon exposure to 808 nm NIR irradiation. The anticancer activity was attributed to the induction of apoptosis and necrosis, achieved by increasing intracellular ROS levels, causing cell cycle arrest at the S phase, and modulating the expression of apoptosis-related proteins.</div></div><div><h3>Discussion</h3><div>Our synthesized Scu-Au NPs exhibit favorable photothermal conversion characteristics, demonstrating excellent therapeutic efficacy and safety for cancer treatment.</div></div>","PeriodicalId":101013,"journal":{"name":"Pharmacological Research - Modern Chinese Medicine","volume":"13 ","pages":"Article 100536"},"PeriodicalIF":0.0,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142593702","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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Pharmacological Research - Modern Chinese Medicine
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