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Meet the Section Editors 与栏目编辑见面
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-04-01 DOI: 10.2174/221031551302230227115258
S. Gezici
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引用次数: 0
Review on Diabetic Complications and their Management by Flavonoids and Triterpenoids 黄酮类和三萜类药物治疗糖尿病并发症的研究进展
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-30 DOI: 10.2174/2210315513666230330082412
S. Shivam, Asheesh Kumar Gupta, Sushil Kumar
Diabetes mellitus, together with its numerous consequences, is rapidly becoming a major health issue. Natural products are secondary metabolites found in plants that have a wide range of biological functions. The development of anti-diabetic medications derived from natural compounds, particularly those derived from plants having a documented folk-use history in the treatment of diabetes, is gaining traction. Many studies have shown the usefulness of natural flavonoids with hypoglycemic properties in the management of diabetic problems, along with their advantages. This paper describes the mechanisms of action of several natural flavonoids whose hypoglycemic effects have been confirmed. Comprehensive lifestyle treatments can help those at high risk of diabetes to avoid or delay the start of the disease, according to the results of randomized controlled trials. Terpenoids are a type of natural substance that have been identified as an anti-diabetic agent in various studies. Some of them are in various phases of preclinical and clinical testing to conclude whether they can be used as anti-diabetic drugs. These compounds can block the enzymes involved in insulin resistance, facilitate glucose metabolism, and positively affect plasma glucose and insulin levels. By blocking multiple pathways implicated in diabetes and its consequences, flavonoids and triterpenes can operate as potential agents in the treatment of diabetic retinopathy, neuropathy, and nephropathy, as well as poor wound healing. However, there have been few attempts to investigate the biological effects of triterpenes and clinical research investigating their use in the treatment of diabetes. As a result, it is critical to pay close attention to these chemicals' therapeutic potential and to contribute fresh information to the scientific community. This review focuses on current advancements in flavonoids and triterpenes chemistry, derivatives, biological interventions, and therapeutic applications, with a focus on diabetes and related illnesses.
糖尿病及其众多后果正迅速成为一个主要的健康问题。天然产物是在植物体内发现的次生代谢产物,具有广泛的生物学功能。从天然化合物中提取的抗糖尿病药物,特别是从有文献记载的治疗糖尿病的民间使用历史的植物中提取的抗糖尿病药物,正在得到越来越多的关注。许多研究表明,具有降糖特性的天然类黄酮在治疗糖尿病方面的作用及其优势。本文介绍了几种已证实具有降血糖作用的天然黄酮类化合物的作用机理。根据随机对照试验的结果,全面的生活方式治疗可以帮助那些糖尿病高危人群避免或延迟疾病的开始。萜类化合物是一种天然物质,在各种研究中已被确定为抗糖尿病药物。其中一些药物正处于临床前和临床试验的不同阶段,以确定它们是否可以作为抗糖尿病药物使用。这些化合物可以阻断参与胰岛素抵抗的酶,促进葡萄糖代谢,并积极影响血浆葡萄糖和胰岛素水平。通过阻断与糖尿病及其后果相关的多种途径,类黄酮和三萜可以作为治疗糖尿病视网膜病变、神经病变和肾病以及伤口愈合不良的潜在药物。然而,很少有人尝试研究三萜的生物学效应,也很少有临床研究调查它们在糖尿病治疗中的应用。因此,密切关注这些化学物质的治疗潜力并为科学界贡献新的信息至关重要。本文综述了黄酮类化合物和三萜化合物的化学、衍生物、生物干预和治疗应用的最新进展,重点介绍了黄酮类化合物和三萜化合物在糖尿病及相关疾病中的应用。
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引用次数: 0
Trapa natans L.: A Journey from Traditional to Contemporary Therapies- A Review Trapa natans L.:从传统疗法到现代疗法的历程——综述
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-30 DOI: 10.2174/2210315513666230330182909
Zartaj Washmin Banu, D. Dasgupta, Iswar Hazarika, Damiki Laloo, Junmoni Kalita
Trapa natans (Family: Trapacea) is basically an edible and ornate plant found in warm, temperate regions of Asia and Europe. Extracts of different parts, as well as the whole herb itself, have been found to traditionally use for the treating many ailments.Current review aims at documenting, finding research gap, and critically appraising the contemporary information of T. natans based on botanical account, traditional use, reported bioactive constituents, toxicity, and therapeutic activities.We used several electronic databases, including scientific data from Pubmed, and Google scholar up to April 3, 2022, incorporating keywords- “Trapa natans,” and “Traditional use of Trapa natans.”The result suggested: a) The plant is used traditionally for treating burning sensation, dipsia, dyspepsia, haemorrhage, diarrhoea, dysentery, leprosy, weariness, inflammation, fractures, pharyngitis, urethrorrhea, bronchitis, and general debility. b) The phytoconstituents found in the plant include cycloucalenol, ursolic acid, ellagic acid, chlorogenic acid, gallic acid, syringic acid, quercetin and 2β, 3α, 23-trihydroxyurs-12-en-28-oic acid. The other phytoconstituents were protein, carbohydrates, starch, flavonoids, and essential vitamins like riboflavin, thiamine, pyridoxine, pantothenic acid, nicotinic acid, vitamin A, vitamin C and D-amylase. c) The plant was studied further for its pharmacological activity in antidiabetic property, antimicrobial potency, anti-inflammatory activity, analgesic activity, immunomodulatory effect, antiulcer activity, anticancer property and nootropic activity. d) Starch obtained from T. natans was also found to have good freeze thaw property, metal chelation property and youghurt stability which could be used for pharmaceutical preparations.e) The oral acute toxicity of hydroalcoholic, ethanolic and methanolic extracts of T. natans was reported to be safe up to a dose of 2000 mg/Kg.The present review suggests that T. natans needs to be explored for evaluation of mechanistic study of the reported activities, preclinical investigations, and evaluation of clinical studies on humans for its pharmacokinetics and pharmacodynamic actions as well as development dose-dependent formulations and routes of administration.
Trapa natans(科:Trapacea)基本上是一种可食用且华丽的植物,分布在亚洲和欧洲的温暖温带地区。不同部位的提取物,以及整个草药本身,已被发现传统上用于治疗许多疾病。目前的综述旨在根据植物学描述、传统用途、已报道的生物活性成分、毒性和治疗活性,记录、发现研究空白,并批判性地评估纳他菌的当代信息。我们使用了几个电子数据库,包括Pubmed和谷歌学者截至2022年4月3日的科学数据,其中包含关键词-“Trapa natans”和“Trapa natans的传统用途”。结果表明:a)该植物传统上用于治疗烧灼感、dipsia、消化不良、出血、腹泻、痢疾、麻风病、疲劳、炎症、骨折,咽炎、尿道炎、支气管炎和全身虚弱。b) 在该植物中发现的植物成分包括环ucalenol、熊果酸、鞣花酸、绿原酸、没食子酸、丁香酸、槲皮素和2β,3α,23-三羟基urs-12-en-28酸。其他植物成分包括蛋白质、碳水化合物、淀粉、类黄酮和必需维生素,如核黄素、硫胺素、吡哆醇、泛酸、烟酸、维生素A、维生素C和D-淀粉酶。c) 进一步研究了该植物在抗糖尿病、抗菌、抗炎、镇痛、免疫调节、抗溃疡、抗癌和益智等方面的药理活性。d) 从T.natans中获得的淀粉还具有良好的冻融性、金属螯合性和稳定性,可用于药物制剂,据报道,T.natans的乙醇和甲醇提取物在高达2000mg/Kg的剂量下是安全的。本综述表明,需要对T.natanss进行探索,以评估所报道的活性的机制研究、临床前研究,以及对其药代动力学和药效作用的人体临床研究的评估,以及剂量依赖性制剂和给药途径的开发。
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引用次数: 0
Traditional Uses, Phytochemistry, Pharmacology, and Toxicology of Erigeron floribundus (Kunth) Sch. Bip.: a Review 花灯盏花的传统用途、植物化学、药理学和毒理学。:回顾
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-30 DOI: 10.2174/2210315513666230330082415
Stephanie Tamdem Guetchueng, Axel Tiwa Lontsi, Théodora Kopa Kowa, J. Tchamgoue, N. Tsabang, E. Nnanga
Erigeron floribundus (Kunth) Sch. Bip. is a reputed medicinal plant widespread all over the world and used traditionally in the treatment of several diseases and infections such as skin disorders, malaria, and gastrointestinal infections.The purpose of this review is to provide a comprehensive overview of traditional uses, phytochemistry, pharmacological activity, and toxicological profile of E. floribundus, and to direct further studies on aspects that have not yet been investigated in order to bring more scientific data for this plant and then give an opportunity for future exploitation in pharmaceutical industries.A meticulous and methodical analysis of the literature was conducted using various online scientific databases and all relevant abstracts and full text articles analyzed and included in the review.A wide range of traditional uses are cited in the literature with the plant mostly being used in African folk medicine for the treatment of malaria and skin diseases. Phytochemical investigations of E. floribundus have resulted in the isolation of several metabolites from different classes including acetylene-derivatives, phenolic compounds, triterpenoids, and steroids. Extracts and isolates from this species were reported to exhibit promising antimicrobial, anti-inflammatory, and analgesic properties. However, the plant has also demonstrated some toxicological activities and should be used with caution.Reported chemical and pharmacological investigations of E. floribundus support the traditional uses of this plant which deserves further attention for antimicrobial drug discovery. The in-depth study should be emphasized the in vitro and in vivo antimicrobial assessment of its extracts and isolated compounds.
多花飞蓬(Kunth)Sch。Bip。是一种著名的药用植物,广泛分布于世界各地,传统上用于治疗多种疾病和感染,如皮肤病、疟疾和胃肠道感染。本综述的目的是全面概述花叶E.floribundus的传统用途、植物化学、药理活性和毒理学特征,并指导对尚未研究的方面的进一步研究,为该植物带来更多的科学数据,为未来在制药工业中的开发提供机会。使用各种在线科学数据库以及分析并纳入综述的所有相关摘要和全文文章,对文献进行了细致而有条理的分析。文献中引用了广泛的传统用途,这种植物主要用于非洲民间医学,用于治疗疟疾和皮肤病。对花叶E.floribundus的植物化学研究已经从不同类别中分离出几种代谢产物,包括乙炔衍生物、酚类化合物、三萜类化合物和类固醇。据报道,该物种的提取物和分离物具有良好的抗菌、抗炎和镇痛特性。然而,该植物也显示出一些毒理学活性,应谨慎使用。据报道,花叶E.floribundus的化学和药理学研究支持了该植物的传统用途,值得进一步关注抗菌药物的发现。深入研究应强调对其提取物和分离化合物的体外和体内抗菌评价。
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引用次数: 0
Natural aphrodisiacs: traditional use, mechanism of action, clinical efficacy, and safety 天然春药:传统用法、作用机制、临床疗效和安全性
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-24 DOI: 10.2174/2210315513666230324111231
Galchenko Alexey Vladimirovich, Bubnova Anastasiia Mikhailovna
Since time immemorial, people have been trying to increase their sexuality. They seek ways to increase sexual activity or sexual desire in themselves and their partners. In addition to resorting to all sorts of mystical rituals, people were looking for various effects from the use of natural raw materials. Some plant, animal, or fungal products have been shown to affect libido, sexual arousal, erectile function, orgasm or erogenous zone sensitivity. Such substances have been called "aphrodisiacs" in honor of the ancient Greek goddess of love - Aphrodite. Most often, aphrodisiacs were taken orally, but some were smoked and others applied to the genitals.In modern clinical practice, phosphodiesterase type 5 inhibitors are used. These are substances, which enhance erection and prevent detumescence in the presence of sexual arousal. Another group of drugs is selective serotonin reuptake inhibitors, which reduce sexual arousal and sexual afferent from the genitals, thus preventing the premature onset of orgasm in men and prolonging sexual intercourse. However, drugs from other pharmacological groups have not found widespread clinical application. Another issue is a trend among young people taking drugs of natural origin, therefore, all kinds of traditional aphrodisiacs are actively used to the present day.Very little is known about almost all of them. Clinical trials are in most cases limited to a few, often not randomized, studies. In this regard, it is very difficult to evaluate the adequate therapeutic and toxic doses of remedies. The situation is complicated by the fact that those few clinical studies were based on questionnaires, that is, the indicators taken into statistical calculations were extremely subjective. Moreover, it was uncertain whether all patients could adequately assess their dynamics in terms of parameters such as sexual satisfaction, or clearly distinguish between libido and sexual arousal. Since the majority of the studies were not blinded, a psychogenic influence on the results of the investigations could not be eliminated, which in the sexual area may be huge. It is worth emphasizing the toxicity of many traditional aphrodisiacs.Of course, there is a serious deficit in the spectrum of pharmacotherapy for sexual disorders. Perhaps further large, randomized, placebo-controlled trials would add some of the traditional aphrodisiacs or their modifications to the arsenal of the clinical specialist.
自古以来,人们就一直在努力增强自己的性欲。他们寻求增加自己和伴侣的性活动或性欲的方法。除了求助于各种神秘的仪式,人们还在寻找使用天然原料的各种效果。一些植物、动物或真菌产品已被证明能影响性欲、性唤起、勃起功能、性高潮或性敏感区敏感性。这种物质被称为“催情剂”,以纪念古希腊的爱神阿芙罗狄蒂。大多数情况下,壮阳药是口服的,但有些是烟熏的,有些是用在生殖器上的。在现代临床实践中,磷酸二酯酶5型抑制剂被使用。这些物质可以在性唤起时促进勃起,防止水肿。另一组药物是选择性血清素再摄取抑制剂,它可以减少性唤起和生殖器的性传入,从而防止男性过早达到性高潮,延长性交时间。然而,从其他药理学组药物尚未发现广泛的临床应用。另一个问题是年轻人服用天然药物的趋势,因此,各种传统的春药被积极使用到今天。我们对它们几乎都知之甚少。在大多数情况下,临床试验仅限于少数研究,通常不是随机的。在这方面,很难评估适当的治疗剂量和毒性剂量。由于那些为数不多的临床研究是基于问卷调查的,也就是说,用于统计计算的指标是非常主观的,这一事实使情况更加复杂。此外,不确定是否所有患者都能充分评估他们的动态参数,如性满意度,或清楚区分性欲和性唤起。由于大多数研究不是盲法的,因此无法消除心理因素对调查结果的影响,这在性领域可能是巨大的。许多传统春药的毒性值得强调。当然,在治疗性功能障碍的药物治疗方面存在着严重的缺陷。也许进一步的大规模、随机、安慰剂对照试验将为临床专家的药库增加一些传统的壮阳药或它们的修改。
{"title":"Natural aphrodisiacs: traditional use, mechanism of action, clinical efficacy, and safety","authors":"Galchenko Alexey Vladimirovich, Bubnova Anastasiia Mikhailovna","doi":"10.2174/2210315513666230324111231","DOIUrl":"https://doi.org/10.2174/2210315513666230324111231","url":null,"abstract":"\u0000\u0000Since time immemorial, people have been trying to increase their sexuality. They seek ways to increase sexual activity or sexual desire in themselves and their partners. In addition to resorting to all sorts of mystical rituals, people were looking for various effects from the use of natural raw materials. Some plant, animal, or fungal products have been shown to affect libido, sexual arousal, erectile function, orgasm or erogenous zone sensitivity. Such substances have been called \"aphrodisiacs\" in honor of the ancient Greek goddess of love - Aphrodite. Most often, aphrodisiacs were taken orally, but some were smoked and others applied to the genitals.\u0000In modern clinical practice, phosphodiesterase type 5 inhibitors are used. These are substances, which enhance erection and prevent detumescence in the presence of sexual arousal. Another group of drugs is selective serotonin reuptake inhibitors, which reduce sexual arousal and sexual afferent from the genitals, thus preventing the premature onset of orgasm in men and prolonging sexual intercourse. \u0000However, drugs from other pharmacological groups have not found widespread clinical application. Another issue is a trend among young people taking drugs of natural origin, therefore, all kinds of traditional aphrodisiacs are actively used to the present day.\u0000Very little is known about almost all of them. Clinical trials are in most cases limited to a few, often not randomized, studies. In this regard, it is very difficult to evaluate the adequate therapeutic and toxic doses of remedies. The situation is complicated by the fact that those few clinical studies were based on questionnaires, that is, the indicators taken into statistical calculations were extremely subjective. Moreover, it was uncertain whether all patients could adequately assess their dynamics in terms of parameters such as sexual satisfaction, or clearly distinguish between libido and sexual arousal. Since the majority of the studies were not blinded, a psychogenic influence on the results of the investigations could not be eliminated, which in the sexual area may be huge. It is worth emphasizing the toxicity of many traditional aphrodisiacs.\u0000Of course, there is a serious deficit in the spectrum of pharmacotherapy for sexual disorders. Perhaps further large, randomized, placebo-controlled trials would add some of the traditional aphrodisiacs or their modifications to the arsenal of the clinical specialist.\u0000","PeriodicalId":56153,"journal":{"name":"Natural Products Journal","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42035901","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
Neuroprotective Activity of Blepharis maderaspatensis Against Colchicine Induced Alzheimer’s Disease Rat Model 马齿苋对秋水仙碱诱导的阿尔茨海默病大鼠模型的神经保护作用
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-16 DOI: 10.2174/2210315513666230316100124
Chandrashekhar V M, Lingaraj Anawal, M. Shalavadi, Shubham Teli
Traditionally, plants have been used for various diseases and neuronal disorders. The present study was designed to evaluate the neuroprotective effect of Blepharis maderaspatensis against a colchicine-induced Alzheimer’s disease rat model.Background and Objective: Traditionally, plants were used for various diseases and neuronal disorders. The present study was designed to evaluate the neuroprotective effect of Blepharis maderaspatensis against colchicine induced Alzheimer’s disease rat model.Neuroprotective activity was examined on colchicine-induced Alzheimer’s disease rats. Test group animals were administrated with ethanol extract of Blepharis maderaspatensis at doses of 200, 400, and 600mg/kg for 28 days. The behavioral parameters were assessed using the Morris water maze and a Digital actophotometer at days 0, 7, 14, and 28 on intracerebroventricular administration of colchicine for assessing the cognitive and gross behavioral activities in rats. Biochemical parameters like lipid peroxidation, glutathione, superoxide dismutase, catalase, total thiols, and acetylcholinesterase were assessed and histopathology of brain tissue was examined on the final day of the experiment.Ethanol extract of Blepharis maderaspatensis showed a dose-dependent neuroprotective activity with a significant decrease in time latency of the Morris water maze (p<0.001) and an increase in the locomotor activity (p<0.001) in the test group as compared to the control group. Biochemical parameters showed a significant decrease in lipid peroxidation (p<0.001) and acetylcholinesterase level (p<0.001) and an increase in superoxide dismutase (p<0.001), catalase (p<0.001), glutathione (p<0.001), and total thiols (p<0.001) in the test group as compared to the control group.In conclusion, the present study showed that the administration of ethanol extract of Blepharis maderaspatensis exerted neuroprotective activity against colchicine-induced cognitive impairment and associated oxidative stress.Ethanol extract of Blepharis maderaspatensis showed a dose dependent neuroprotective activity with significant decrease in time latency of Morris water maze (p<0.001) and increase in the locomotor activity (p<0.001) in test group as compared to control group. Biochemical parameters showed significant decreases in lipid peroxidation (p<0.001), acetylcholinesterase level (p<0.001) and increased in superoxide dismutase (p<0.001) catalase (p<0.001), glutathione (p<0.001) total thiols (p<0.001) in the test group as compared control group.In conclusion, the present study showed that administration of ethanol extract of Blepharis maderaspatensis possesses neuroprotective activity against colchicine induced cognitive impairment and associated oxidative stress.
传统上,植物被用于治疗各种疾病和神经紊乱。本研究旨在评价马氏眼睑草对秋水仙碱诱导的阿尔茨海默病大鼠模型的神经保护作用。背景与目的:传统上,植物被用于治疗各种疾病和神经紊乱。本研究旨在评价马氏眼睑草对秋水仙碱诱导的阿尔茨海默病大鼠模型的神经保护作用。观察秋水仙碱诱导的老年痴呆大鼠的神经保护作用。试验组动物分别以200、400、600mg/kg剂量给药28 d。在秋水仙碱脑室给药后的第0、7、14、28天,采用Morris水迷宫和数字体温计对大鼠的行为参数进行评估,以评估大鼠的认知和大体行为活动。在实验的最后一天,评估脂质过氧化、谷胱甘肽、超氧化物歧化酶、过氧化氢酶、总硫醇、乙酰胆碱酯酶等生化指标,并对脑组织进行组织病理学检查。与对照组相比,试验组大鼠Morris水迷宫潜伏期显著降低(p<0.001),运动活动显著增加(p<0.001),显示出剂量依赖性的神经保护活性。生化指标显示,与对照组相比,试验组的脂质过氧化(p<0.001)和乙酰胆碱酯酶(p<0.001)水平显著降低,超氧化物歧化酶(p<0.001)、过氧化氢酶(p<0.001)、谷胱甘肽(p<0.001)和总硫醇(p<0.001)水平显著升高。综上所述,本研究表明,对秋水仙碱诱导的认知功能障碍和相关氧化应激具有神经保护作用。马氏眼睑草乙醇提取物具有剂量依赖性的神经保护作用,实验组小鼠Morris水迷宫潜伏期显著降低(p<0.001),运动活性显著升高(p<0.001)。生化指标显示,试验组脂质过氧化(p<0.001)、乙酰胆碱酯酶(p<0.001)水平显著低于对照组,超氧化物歧化酶(p<0.001)、过氧化氢酶(p<0.001)、谷胱甘肽(p<0.001)、总硫醇(p<0.001)水平显著高于对照组。综上所述,本研究表明,对秋水仙碱诱导的认知功能障碍和相关氧化应激具有神经保护作用。
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引用次数: 0
Fenugreek (Trigonella foenum-graecum L.) modulates energy metabolism and anti-inflammatory response in obesity via combinatorial analysis 胡芦巴(Trigonella foenum-graecum L.)通过组合分析调节肥胖的能量代谢和抗炎反应
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-09 DOI: 10.2174/2210315513666230309105835
F. Liew, Theysshana Visuvanathan, Shalini Vellasamy
Since ancient times, fenugreek has been utilized as a dietary condiment as well as for its various therapeutic properties. The goal of this study is to look at the function of fenugreek in regulating obesity metabolism by providing a global picture of gene networks and pathways. The buildup of fat in adipose tissue and other internal organs is a hallmark of obesity, a long-term carbohydrate and lipid metabolic disorder. The fenugreek plant grows up to 60 cm tall, with golden-yellow rhomboidal seeds. Though the seeds of fenugreek are more well-known, the leaves and stems have also been suggested to have therapeutic properties. Various studies have shown that the secondary metabolites in the fenugreek plant are responsible for these properties. Several studies have shown that fenugreek has anti-obesity properties, making it a good plant candidate with a high prospect of being used to treat obesity. This review paper discusses the use of combinatorial analytic approaches to better understand the medicinal uses of fenugreek. Combinatorial analytical methods that use functional modulation and modelling may make it easier to come up with research strategies to fill in research gaps and find possible research niches.
胡芦巴自古以来就被用作一种膳食调味品,并具有多种治疗特性。这项研究的目的是通过提供基因网络和途径的全球图片来观察胡芦巴在调节肥胖代谢中的作用。脂肪组织和其他内脏中脂肪的堆积是肥胖的标志,肥胖是一种长期的碳水化合物和脂质代谢紊乱。胡芦巴植株高达60厘米,种子呈金黄色菱形。尽管胡芦巴的种子更为人所知,但其叶和茎也被认为具有治疗作用。各种研究表明,胡芦巴植物中的次生代谢产物对这些特性负责。几项研究表明,胡芦巴具有抗肥胖特性,是一种很好的候选植物,用于治疗肥胖的前景很高。本文讨论了使用组合分析方法来更好地了解胡芦巴的药用价值。使用功能调节和建模的组合分析方法可以更容易地提出填补研究空白和寻找可能的研究利基的研究策略。
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引用次数: 0
Octyl Gallate, a Potential Therapeutic Candidate for Psoriasis: An In vitro and In silico Anti-Inflammatory approach 没食子酸辛酯,一种潜在的银屑病候选治疗药物:一种体外和体外抗炎方法
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-09 DOI: 10.2174/2210315513666230309141639
A. Jabeen, Syeda Farah Shah, Sidrah Shams, Z. Batool, Zaheer-ul-Haq, S. Faizi
Psoriasis is an inflammatory skin disease characterized by hyper-proliferating epidermal membrane and accumulation of dermal inflammatory cells. A profound understanding of mechanistic studies has revealed the potential role of TNF-α and IL-17a in disease pathogenesis.Psoriasis is an inflammatory skin disease labelled with hyper-proliferating epidermal membrane and accumulation of dermal inflammatory cells. Profound understanding of mechanistic studies revealed the potential role of TNF-α and IL-17a in the disease pathogenesis.The study aims to evaluate the inhibitory potential of octyl gallate on IL-17a through in silico analysis and validate its anti-inflammatory effects against oxidative stress and proinflammatory cytokines in vitro.The study aims to evaluate the inhibitory potential of octyl gallate on IL-17a through in silico analysis and validate its anti-inflammatory effects against oxidative stress and proinflammatory cytokines in vitro.The objective of the study is to evaluate the potential of octyl gallate for the treatment of psoriasis by targeting inflammatory mediators using in vitro and in silico approaches.The anti-oxidant potential of octyl gallate was evaluated through chemiluminescence and the Griess method. Cytotoxicity was evaluated via MTT assay. TNF-α levels were quantified through ELISA. Mechanistic studies were performed to recognize the inhibition of strong inflammatory mediators, such as TNF-α, IL-1β, IL-6, NCF-1, and NF-κB through gene expression analysis. Molecular docking was performed to study the underlying binding pattern of gallate inhibitor with IL-17a.Octyl gallate potently inhibited the TNF-α, reactive oxygen and nitrogen species while significantly reduces the expression of inflammatory genes. The docking analysis revealed that octyl gallate resides well in the binding pocket of IL17a. The physiochemical properties of gallate resulted good ADME profile.Octyl gallate potently inhibited TNF-α, reactive oxygen, and nitrogen species while significantly reducing the expression of inflammatory genes. The docking analysis revealed that octyl gallate resides well in the binding pocket of IL17a. The physicochemical properties of gallate resulted in a good ADME profile.Octyl gallate revealed significant antioxidant potential and downregulation of inflammatory genes principally involved in psoriasis. A new inhibitory target IL-17a of octyl gallate has been identified that together with TNF-α develops a feed forward state in disease pathogenesis. This study signifies the potential of octyl gallate to be a prospective lead molecule for treatment of psoriasis.Octyl gallate revealed a significant antioxidant potential and downregulation of inflammatory genes principally involved in psoriasis. A new inhibitory target IL-17a of octyl gallate has been identified that, together with TNF-α, develops a feed-forward state in disease pathogenesis. This study signifies the potential of octyl gall
银屑病是一种炎症性皮肤病,其特征是表皮膜过度增生和真皮炎症细胞积聚。对机制研究的深刻理解揭示了TNF-α和IL-17a在疾病发病机制中的潜在作用。牛皮癣是一种炎症性皮肤病,其特征是表皮膜过度增生和真皮炎症细胞积聚。对机制研究的深入了解揭示了TNF-α和IL-17a在疾病发病机制中的潜在作用。本研究旨在通过芯片分析评估没食子酸辛酯对IL-17a的抑制潜力,并验证其对氧化应激和促炎细胞因子的体外抗炎作用。本研究旨在通过芯片分析评估没食子酸辛酯对IL-17a的抑制潜力,并验证其对氧化应激和促炎细胞因子的体外抗炎作用。本研究的目的是评估没食子酸辛酯通过体外和计算机方法靶向炎症介质治疗牛皮癣的潜力。采用化学发光法和Griess法对没食子酸辛酯的抗氧化能力进行了评价。MTT法测定细胞毒性。ELISA法测定TNF-α水平。通过基因表达分析进行机制研究,以识别TNF-α、IL-1β、IL-6、NCF-1和NF-κB等强炎症介质的抑制作用。通过分子对接研究没食子酸酯抑制剂与IL-17a的潜在结合模式。没食子酸辛酯能有效抑制TNF-α、活性氧和氮,同时显著降低炎症基因的表达。对接分析表明,没食子酸辛酯存在于IL17a的结合口袋中。没食子酸酯的理化性质使其具有良好的ADME特性。没食子酸辛酯能有效抑制TNF-α、活性氧和氮,同时显著降低炎症基因的表达。对接分析表明,没食子酸辛酯存在于IL17a的结合口袋中。没食子酸酯的物理化学性质导致了良好的ADME分布。没食子酸辛酯显示显著的抗氧化潜力和下调炎症基因主要参与牛皮癣。没食子酸辛酯的一个新的抑制靶点IL-17a已被发现,它与TNF-α一起在疾病发病机制中形成前馈状态。本研究提示没食子酸辛酯有潜力成为治疗银屑病的先导分子。没食子酸辛酯显示出显著的抗氧化潜力和下调炎症基因主要参与牛皮癣。没食子酸辛酯的一个新的抑制靶点IL-17a已经被发现,它与TNF-α一起在疾病发病机制中形成前馈状态。本研究提示没食子酸辛酯有潜力成为治疗银屑病的先导分子。NA
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引用次数: 0
Modulatory Effects of Mangiferin Isolated from Aquilaria Plants on Human Cytochrome P450 Enzyme (CYP) Activities in Vitro and in Silico Studies 沉香芒果苷对人细胞色素P450酶(CYP)活性的调控作用
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-07 DOI: 10.2174/2210315513666230307115348
Yan Pan, Premika Jagadiah, Yee Tze Ung, Sharoen Yu Ming Lim, K. Lim, Jason Loo Siau Ee, Y. Pung, L. Chowdhury, Shang Tao
Mangiferin has been identified as one of the major active constituents of Aquilaria plants. It was reported to have several promising chemotherapeutic potentials. Our preliminary data suggested that Aquilaria plant water extracts inhibited several cytochrome P450 (CYP) isoenzymes in vitro.This study aimed to investigate the modulatory effects of mangiferin on six major drug metabolizing CYP enzymes including CYP2A6, CYP2B6, CYP2C9, CYP2D6, CYP3A4, and CYP3A5.The enzyme activities were measured using fluorescence-based assays and enzyme kinetic such as IC50 parameters and Ki values were calculated to evaluate inhibitory potencies and mechanisms. Moreover, for potent inhibitions, molecular docking studies were carried out to explore potential interactions of residues between mangiferin and CYP enzymes.Our findings suggested that mangiferin could inhibit CYP2D6, CYP3A4, and CYP3A5 in vitro with IC50 values of 9.2, 8.7, and 4.3µM, and Ki values of 3.8, 10.8, and 9.6µM, in a non-competitive inhibition pattern. Molecular docking studies using AutoDock 4.2 identified potential residues contained in mangiferin that interacted with CYP2D6, CYP3A4, and CYP3A5, resulting in the observed inhibitory effects.Mangiferin should be used carefully, in particular, with conventional drugs metabolized mainly by CYP2D6, CYP3A4, and CYP3A5. Further in vivo studies are recommended to evaluate the clinical relevance of these inhibitions.
芒果苷是沉香属植物的主要活性成分之一。据报道,它具有几种很有前途的化疗潜力。我们的初步数据表明,沉香水提物在体外抑制几种细胞色素P450 (CYP)同工酶。本研究旨在探讨芒果苷对CYP2A6、CYP2B6、CYP2C9、CYP2D6、CYP3A4和CYP3A5 6种主要药物代谢CYP酶的调节作用。采用荧光法测定酶活性,并计算酶动力学(如IC50参数和Ki值)以评估抑制效力和机制。此外,对于有效的抑制作用,进行了分子对接研究,以探索芒果苷与CYP酶之间残基的潜在相互作用。结果表明,芒果苷对CYP2D6、CYP3A4和CYP3A5具有非竞争性抑制作用,IC50值分别为9.2、8.7和4.3µM, Ki值分别为3.8、10.8和9.6µM。使用AutoDock 4.2进行分子对接研究,发现芒果苷中含有与CYP2D6、CYP3A4和CYP3A5相互作用的潜在残基,从而产生观察到的抑制作用。芒果苷应谨慎使用,特别是与主要由CYP2D6、CYP3A4和CYP3A5代谢的常规药物一起使用。建议进一步的体内研究来评估这些抑制的临床相关性。
{"title":"Modulatory Effects of Mangiferin Isolated from Aquilaria Plants on Human Cytochrome P450 Enzyme (CYP) Activities in Vitro and in Silico Studies","authors":"Yan Pan, Premika Jagadiah, Yee Tze Ung, Sharoen Yu Ming Lim, K. Lim, Jason Loo Siau Ee, Y. Pung, L. Chowdhury, Shang Tao","doi":"10.2174/2210315513666230307115348","DOIUrl":"https://doi.org/10.2174/2210315513666230307115348","url":null,"abstract":"\u0000\u0000Mangiferin has been identified as one of the major active constituents of Aquilaria plants. It was reported to have several promising chemotherapeutic potentials. Our preliminary data suggested that Aquilaria plant water extracts inhibited several cytochrome P450 (CYP) isoenzymes in vitro.\u0000\u0000\u0000\u0000This study aimed to investigate the modulatory effects of mangiferin on six major drug metabolizing CYP enzymes including CYP2A6, CYP2B6, CYP2C9, CYP2D6, CYP3A4, and CYP3A5.\u0000\u0000\u0000\u0000The enzyme activities were measured using fluorescence-based assays and enzyme kinetic such as IC50 parameters and Ki values were calculated to evaluate inhibitory potencies and mechanisms. Moreover, for potent inhibitions, molecular docking studies were carried out to explore potential interactions of residues between mangiferin and CYP enzymes.\u0000\u0000\u0000\u0000Our findings suggested that mangiferin could inhibit CYP2D6, CYP3A4, and CYP3A5 in vitro with IC50 values of 9.2, 8.7, and 4.3µM, and Ki values of 3.8, 10.8, and 9.6µM, in a non-competitive inhibition pattern. Molecular docking studies using AutoDock 4.2 identified potential residues contained in mangiferin that interacted with CYP2D6, CYP3A4, and CYP3A5, resulting in the observed inhibitory effects.\u0000\u0000\u0000\u0000Mangiferin should be used carefully, in particular, with conventional drugs metabolized mainly by CYP2D6, CYP3A4, and CYP3A5. Further in vivo studies are recommended to evaluate the clinical relevance of these inhibitions.\u0000","PeriodicalId":56153,"journal":{"name":"Natural Products Journal","volume":" ","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45653042","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
Pharmacology, Ethnopharmacology, and Phytochemistry of Medicinally Active Moringa oleifera: A Review 药用辣木的药理学、民族药理学和植物化学研究进展
IF 0.8 Q4 CHEMISTRY, MEDICINAL Pub Date : 2023-03-01 DOI: 10.2174/2210315513666230301094259
N. Kumar, Shikha Sharma
Moringa oleifera (MO), which belongs to the family Moringaceae, is a significant medicinal plant that is also one of the species farmed in the greatest quantity worldwide. All its components, including its leaves, roots, seeds, flowers, bark, stems, and green pods, have a wide range of medicinal properties and are exceptionally high in nutritional content. Some of the important medicinal properties of the plant include anticancer, antiasthmatic, antipyretic, antiepileptic, anti-inflammatory, antiulcerative, cholesterol-lowering, antioxidant, antidiabetic, hepatoprotective, diuretic, CNS depressant, antibacterial, antifungal, anthelmintic, antibiotic, analgesic, antimalarial, antispasmodic, etc. Its nutritional value is attributed to the presence of proteins, carbohydrates, minerals, vitamins, amino acids, α-carotene, and various phenolic compounds. The purpose of this review is to present a synopsis of the ethnobotany, nutritive, and phytochemical profiles of various parts as well as the pharmacological properties of MO, with a particular emphasis on the several processes that are responsible for its multispectral activity. Additionally, it highlights studies on the safety profile, medication interactions, and relevant clinical trials. MO is used in pharmaceutics as an active extract in metallic nanoparticles and as an excipient in different pharmaceutical products. Other applications related to its water-purifying features, such as biodiesel, biogas, and biopesticide, are also discussed in the present article. Thus, the review provides necessary information proving that each part of MO has beneficial effects, and the plant can be studied extensively for many research aspects.
辣木(Moringa oleifera,MO)属于辣木科,是一种重要的药用植物,也是世界上种植量最大的物种之一。它的所有成分,包括叶子、根、种子、花、树皮、茎和绿荚,都具有广泛的药用特性,营养含量极高。该植物的一些重要药用特性包括抗癌、平喘、解热、抗癫痫、抗炎、抗溃疡、降胆固醇、抗氧化、抗糖尿病、保肝、利尿、中枢神经系统抑制剂、抗菌、抗真菌、驱虫、抗生素、镇痛、抗疟、抗痉挛等。它的营养价值归因于蛋白质、碳水化合物、矿物质、维生素、氨基酸、α-胡萝卜素和各种酚类化合物的存在。这篇综述的目的是介绍MO的民族植物学、营养和植物化学概况,以及MO的药理学特性,特别强调其多光谱活性的几个过程。此外,它还强调了对安全性、药物相互作用和相关临床试验的研究。MO在药学中被用作金属纳米颗粒中的活性提取物和不同医药产品中的赋形剂。本文还讨论了其净水特性的其他应用,如生物柴油、沼气和生物农药。因此,该综述提供了必要的信息,证明MO的每一部分都具有有益的效果,并且可以在许多研究方面对植物进行广泛的研究。
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引用次数: 0
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