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Molecular docking studies of Triphala with catalytic portion of HMG-CoA reductase enzyme Triphala与HMG-CoA还原酶催化部分的分子对接研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.28
P. Rinthong, P. Pulbutr, Chawannuch Mudjupa
Introduction: Triphala, consisting of three fruits, Phyllanthus emblica L. (Phyllanthaceae), Terminalia bellirica (Gaertn.) Roxb. (Combretaceae), and T. chebula Retz, is a well-recognized Ayurvedic herbal formulation, used for various therapeutic purposes, including the treatment of dyslipidemia. Inhibitory activity against 3‑hydroxy‑3‑methylglutaryl‑coenzyme A (HMG‑CoA) reductase, a rate-limiting enzyme in the endogenous cholesterol synthesis pathway, is an essential target for the management of hypercholesterolemia. This in silico study aimed to investigate the HMG-CoA reductase inhibitory activity of the phytochemical compounds derived from Triphala formulation by employing molecular docking analysis. Methods: Ten phytochemical constituents of Triphala formulation were selectively used for docking study by using the HMG-CoA reductase template (PDB: 1HWK). Docking analysis was performed using AutoDock 4.2. The candidates were ranked by the binding energy parameters. Results: From the docking studies, the phytochemical compounds with HMG-CoA reductase inhibition could be classified into 4 groups, including phytosterols, polyphenols, tannins, and flavonoids. Beta-sitosterol exhibited the highest binding affinity to HMG-CoA reductase with a binding energy of -7.75 kcal/mol. Conclusion: These 10 phytochemical compounds in Triphala potentially exert their cholesterol-lowering effects via inhibition against HMG-CoA reductase. Nonetheless, further in vitro and in vivo experiments should be conducted subsequently to confirm this finding.
简介:triphia,由三种果实组成,Phyllanthus emblica L. (Phyllanthaceae), Terminalia bellirica (Gaertn.)。Roxb。(combretacae)和T. chebula Retz,是一种公认的阿育吠陀草药配方,用于各种治疗目的,包括治疗血脂异常。3 -羟基- 3 -甲基戊二酰辅酶A (HMG - CoA)还原酶的抑制活性是内源性胆固醇合成途径中的限速酶,是治疗高胆固醇血症的重要目标。本研究旨在通过分子对接分析的方法,研究从Triphala制剂中提取的植物化学物质对HMG-CoA还原酶的抑制活性。方法:采用HMG-CoA还原酶模板(PDB: 1HWK),对Triphala制剂中的10种植物化学成分进行选择性对接研究。使用AutoDock 4.2进行对接分析。根据结合能参数对候选粒子进行排序。结果:通过对接研究,对HMG-CoA还原酶具有抑制作用的植物化学物质可分为4类,包括植物甾醇类、多酚类、单宁类和黄酮类。β -谷甾醇对HMG-CoA还原酶的结合亲和力最高,结合能为-7.75 kcal/mol。结论:这10种化合物可能通过抑制HMG-CoA还原酶发挥降胆固醇作用。尽管如此,还需要进一步进行体内和体外实验来证实这一发现。
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引用次数: 1
The modulatory effects of black chia (Salvia hispanica) and garden cress (Lepidium sativum) seeds on Nε-CML formation in streptozotocin-injected rats 丹参和水芹种子对链脲佐菌素注射大鼠Nε-CML形成的调节作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.27
Hadeer Saad Mohamed, Tahany Kholief, Radwan Mohamed, Amira Abd El-Rhman
Introduction: Antioxidant and hypoglycemic properties of some plant seeds are considered natural preventives for diabetic-associated glycation. This study is concerned with the evaluation of the bioactive components of black chia and garden cress seeds and the examination of their modulatory effects on hyperglycemia and associated glycation induced by streptozotocin (STZ) injection. Methods: Forty male rats were divided into 4 groups, 10 rats each: Group 1 (healthy control group); group 2 (diabetic group): rats injected STZ intraperitoneally to induce hyperglycemia; group 3 and group 4: rats treated (after diabetic induction) with 1 mL (20% w/w) black chia and garden cress seed extract, respectively. Results: STZ injection caused marked hyperglycemia, oxidative stress, glycation, and inflammation condition with disturbance in organs functions and structural alterations in pancreatic tissue, while; treatment with black chia and garden cress seed extracts showed remarkable (P < 0.05) modulatory effects on hyperglycemia and associated disorders. Conclusion: Black chia and garden cress seeds might be used in the management of diabetes and associated glycation.
简介:一些植物种子的抗氧化和降糖特性被认为是糖尿病相关糖基化的天然预防剂。本文对黑奇亚籽和芥蓝籽的生物活性成分进行了评价,并研究了其对链脲佐菌素(STZ)诱导的高血糖和相关糖基化的调节作用。方法:40只雄性大鼠随机分为4组,每组10只:第一组(健康对照组);2组(糖尿病组):大鼠腹腔注射STZ诱导高血糖;第3组和第4组:糖尿病诱导后大鼠分别给予黑籽提取物1 mL (20% w/w)和芥蓝籽提取物。结果:STZ注射液引起明显的高血糖、氧化应激、糖基化和炎症反应,器官功能紊乱,胰腺组织结构改变;黑奇亚和芥蓝籽提取物对高血糖及相关疾病的调节作用显著(P < 0.05)。结论:黑奇亚、芥蓝籽可用于糖尿病及相关糖基化的治疗。
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引用次数: 1
Co-administration of herbal inhibitors of P-glycoprotein with renal drugs enhance their bioavailability– In silico approach p -糖蛋白草药抑制剂与肾脏药物联合使用可提高其生物利用度
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.26
C. Roy, P. Ghosh
Introduction: Multidrug resistance (MDR) is primarily associated with reduced intracellular drug accumulation owing to overexpression of p-glycoprotein, an active efflux transporter. Competitive inhibition or allosteric modulation of p-glycoprotein may alter the pharmacokinetics of the drugs that serve as substrates, resulting in enhanced drug bioavailability and tissue penetration. This study endeavors to assess the efficacy of the components of reno-protective herbs in the inhibition of p-glycoprotein activity thereby enhancing the possibility of the retention of co-administered renal medications inside the target cells. Methods: Drug-likeness and pharmacokinetic properties were determined to ensure the safety and efficacy of herbal constituents. Molecular docking employing the CDOCKER module of Discovery Studio was performed to investigate the binding affinity between the active constituents and the p-glycoprotein receptor (6C0V). Molecular dynamics simulation was utilized to further assess the stability of the complex of receptors with the component bearing its maximal affinity. Results: The analyses suggested that the inhibitors viz., atisine, kutkin, and embelin from Aconitum heterophyllum, phylloquinone from Calendula officinalis, stigmasterol from Paederia foetida, and convallamarogenin from Convallaria majalis demonstrated maximum binding affinity towards p-glycoprotein. Conclusion: Atisine may thus be identified as the lead compound in the augmentation of drug bioavailability inside the cell, along with its reno-protective efficacy.
多药耐药(MDR)主要与细胞内药物积累减少有关,这是由于p糖蛋白(一种主动外排转运体)的过度表达。p糖蛋白的竞争性抑制或变构调节可能改变作为底物的药物的药代动力学,从而提高药物的生物利用度和组织渗透能力。本研究旨在评估肾保护草药成分在抑制p-糖蛋白活性方面的功效,从而提高共同给药的肾脏药物在靶细胞内保留的可能性。方法:测定中药成分的药物相似性和药动学性质,确保其安全性和有效性。利用Discovery Studio的CDOCKER模块进行分子对接,研究活性成分与p-糖蛋白受体(6C0V)的结合亲和力。利用分子动力学模拟进一步评估具有最大亲和力组分的受体复合物的稳定性。结果:分析表明,与p-糖蛋白结合最密切的抑制剂为乌头碱、库特金、栓塞素、金盏花叶黄醌、黄花拟南芥豆甾醇、康麻原素。结论:鸢尾碱可作为提高细胞内药物生物利用度的先导化合物,并具有免疫保护作用。
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引用次数: 0
Volkameria inermis: An overview of its chemical constituents and pharmacological properties, notably the amelioration of motor tics 藜草:概述其化学成分和药理特性,特别是改善运动性抽搐
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.18
E. Chan, S. Wong, H. T. Chan
This overview on Volkameria inermis (Lamiaceae) is the first in updating information on the chemical constituents and pharmacological properties of the species, notably on its unique ability in ameliorating motor tics. The information was procured from Google, Google Scholar, PubMed, PubMed Central, Science Direct, J-Stage, and PubChem. Previously named Clerodendrum inerme (Verbenaceae), V. inermis is a scrambling or scandent coastal shrub in the tropics and sub-tropics. From different parts of the plant, compounds such as flavonoids, diterpenes/diterpenoids, sterols, triterpenes/triterpenoids, iridoid glycosides, phenolic glycosides, phenylethanoid glycosides (PEGs), phenylpropanoid glycosides (PPGs), chalcones, and sesquiterpenes have been reported. Major pharmacological properties of V. inermis include anti-cancer, anti-inflammatory, antioxidant, hepatoprotective, analgesic, and antibacterial activities. Other properties include anti-tyrosinase, antifungal, neuroprotective, hypotensive, hypoglycemic, amyloid-β aggregation, wound healing, antipyretic, and larvicidal activities. A unique pharmacological property of V. inermis leaf extract, discovered by scientists from Taiwan, is the amelioration of motor tic disorders, a spectrum of Tourette syndrome. This property included a case report, three in vivo studies, and one patent. Areas of further research of V. inermis are suggested.
本综述首次更新了该物种的化学成分和药理学特性,特别是其改善运动抽搐的独特能力。这些信息来自谷歌、谷歌学者、PubMed、PubMedCentral、Science Direct、J-Stage和PubChem。以前被命名为Clerodendrum inerme(马鞭草科),V.inermis是热带和亚热带的一种攀援或攀缘海岸灌木。从植物的不同部位,已经报道了类黄酮、二萜/二萜、甾醇、三萜/三萜、环烯醚萜苷、酚苷、苯乙醇苷(PEG)、苯丙烷苷(PPG)、查尔酮和倍半萜等化合物。无尾V.inermis的主要药理特性包括抗癌、抗炎、抗氧化、保肝、镇痛和抗菌活性。其他特性包括抗酪氨酸酶、抗真菌、神经保护、降压、降血糖、淀粉样蛋白-β聚集、伤口愈合、解热和杀幼虫活性。台湾科学家发现的无尾蛇叶提取物的一个独特药理特性是改善运动障碍,这是一种图雷特综合征。该财产包括一份案例报告、三项体内研究和一项专利。文中提出了进一步研究伊纳灭活病毒的领域。
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引用次数: 0
Spatial memory-enhancing effects and antioxidant activities of leaf and stem bark methanol extracts of Prunus africana in scopolamine-treated mice 非洲李叶和茎皮甲醇提取物对东莨菪碱处理小鼠的空间记忆增强作用及抗氧化活性
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.33
D. Ngai, C. Kibiti, M. Ngugi
Introduction: Conventional medicines for Alzheimer’s disease (AD) have little efficacy and are linked to several severe effects, necessitating alternative therapy. The current study investigated the memory-enhancing effects and antioxidant activities of stem bark and leaf MeOH extracts of Prunus africana in scopolamine-induced amnesic mice. Several inclusions build up in brain tissue during AD progression and the brain clears them oxidatively. This makes the antioxidant activity a vital requirement for plant extracts that are used with great success to manage AD. Methods: In this study, for each plant extract, thirty Swiss albino mice were randomly assigned to six groups; extract-treated, reference drug control, normal control, and negative control groups. The mice were then subjected to the Morris water maze task for four consecutive days, euthanized and their whole brains were assessed for antioxidant activities. Results: The studied extracts significantly (P < 0.01) reduced escape latencies of experimental mice in a dose-related manner, depicting their considerable memory-enhancing effects. The extracts also displayed significant (P < 0.01) enzymatic and non-enzymatic antioxidant activities. Conclusion: The leaf and stem bark MeOH extracts of P. africana possess phytocompounds with spatial memory-enhancing effects and antioxidant activities.
简介:传统药物治疗阿尔茨海默病(AD)的疗效甚微,并且与几种严重的影响有关,需要替代治疗。本研究研究了非洲李茎皮和叶MeOH提取物对东莨菪碱致失忆症小鼠的记忆增强作用和抗氧化活性。在阿尔茨海默病的发展过程中,脑组织中会积聚一些内含物,大脑会氧化清除它们。这使得抗氧化活性成为植物提取物的重要要求,这些提取物在治疗AD方面取得了巨大的成功。方法:在本研究中,针对每种植物提取物,将30只瑞士白化小鼠随机分为6组;提取物组、对照药物组、正常对照组、阴性对照组。然后,这些小鼠连续四天接受莫里斯水迷宫任务,并对其实施安乐死,评估其整个大脑的抗氧化活性。结果:所研究的提取物显著(P < 0.01)降低了实验小鼠的逃避潜伏期,且呈剂量相关,说明其具有显著的记忆增强作用。提取物具有极显著(P < 0.01)的酶和非酶抗氧化活性。结论:非洲木犀叶和茎皮MeOH提取物具有空间记忆增强作用和抗氧化活性。
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引用次数: 0
Protective role of hispolon pyrazole and hispolon monomethyl ether pyrazole in electromagnetic radiation-induced behavioral, neurochemical, oxidative, and histological changes in rats hispolon pyrazole和hispolon单甲基醚吡唑对电磁辐射诱导大鼠行为、神经化学、氧化和组织学变化的保护作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.32
Vara Prasad Saka, Chitra Vellapandian, Damodharan Narayanasamy
Introduction: Radiofrequency electromagnetic radiation (RF-EMR) from mobile phones was reported to cause neurological damage. Hispolon pyrazole (HP) and hispolon monomethyl ether pyrazole (HMEP) were tested for their RF-EMR protection in rats. Methods: Juvenile Wistar albino rats were exposed to the mobile phone generating 2400 MHz radiation with a maximum power output of 2 W/kg (Specific absorption rate 1.6 W/kg) for 90 days at a rate of 2 hours/day, treated with HP and HMEP at 20 and 40 mg/kg body weight. The elevated plus maze (EMT) test was used for anxiety and exploration evaluation, the forced swim test (FST) for depression, the Morris water maze test and Y-maze test for learning and memory. The oxidative stress markers like glutathione, superoxide dismutase (SOD), catalase (CAT), and malonaldehyde (MDA), and the neurotransmitters such as gamma-aminobutyric acid, glutamate, dopamine, and acetylcholinesterase along with histopathology in the cortex, striatum, and hippocampus were evaluated to establish the mechanism of the neuronal alterations of HP and HMEP against RF-EMR-induced damage. Results: In the current investigation, HP at a higher dose of 40 mg/kg and HMEP at both doses significantly reduced the oxidative stress generated by RF-EMR from mobile phones and altered neurobehavioral, neurotransmitter, and histological alterations. Conclusion: Based on the findings, HP and HMEP at a dose of 40 mg/kg are protective agents against long-term, continuous mobile phone use and can be regarded viable therapeutic agents.
导读:据报道,来自移动电话的射频电磁辐射(RF-EMR)会导致神经损伤。对大鼠进行了Hispolon pyrazole (HP)和Hispolon monmethyl ether pyrazole (HMEP)的RF-EMR保护实验。方法:将幼年Wistar白化大鼠以2小时/天的速率暴露于产生2400 MHz最大功率输出2 W/kg(比吸收率1.6 W/kg)的手机辐射中90天,并给予HP和HMEP分别为20和40 mg/kg体重。焦虑和探索评价采用升高+迷宫(EMT)测验,抑郁评价采用强迫游泳测验(FST),学习记忆评价采用Morris水迷宫测验和y型迷宫测验。通过对皮层、纹状体和海马组织中谷胱甘肽、超氧化物歧化酶(SOD)、过氧化氢酶(CAT)、丙二醛(MDA)等氧化应激标志物和γ -氨基丁酸、谷氨酸、多巴胺、乙酰胆碱酯酶等神经递质及组织病理学的检测,探讨HP和HMEP对rf - emr损伤的神经元改变机制。结果:在目前的研究中,HP (40 mg/kg)和HMEP(两种剂量)均显著降低了手机射频emr产生的氧化应激,并改变了神经行为、神经递质和组织学改变。结论:40 mg/kg剂量的HP和HMEP是长期连续使用手机的保护剂,可以作为可行的治疗剂。
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引用次数: 0
Protective effect of almond oil and primrose oil on neurochemical and lipid profile in ovariectomized rats 杏仁油和月见草油对去卵巢大鼠神经化学和血脂的保护作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.25
E. A. M. Sharaf, E. Kamel, Marwa Mosaad Hassan
Introduction: Ovariectomies rats were used to assess the preventive effects of almond and primrose oils on their lipid and neurochemical profiles. Methods: The experimental groups were as follows: Group 1: A negative control group. Group 2: Rats given an oral dose of almond oil (800 mg/kg/d) for 30 days. Group 3: Rats given an oral dose of primrose oil (500 mg/kg/d) for 30 days. Group 4: Untreated ovariectomized rats. Group 5: Ovariectomized rats given an oral dose of almond oil (800 mg/kg/d) for 30 days. Group 6: Ovariectomized rats given an oral dose (500 mg/kg/d) of primrose oil daily for 30 days. Results: Oral administration of almond and primrose oils significantly decreased mean (P < 0.05) serum total cholesterol (TC), triacylglycerol (TG), low-density lipoprotein cholesterol (LDL-C), and very low-density lipoprotein cholesterol (VLDL-C) concentrations and raised high-density lipoprotein cholesterol (HDL-C) in the ovariectomized groups compared to group 4 (P < 0.05). They also increased leptin and estradiol (E2) concentrations in groups 5 and 6. Administration of oils showed a marked increase in noradrenalin, dopamine, and 5-hydroxytyramin levels and a marked decrease in PGE2 and COX-2 levels (P < 0.05). Rats given almond and primrose oils revealed minor capillary congestion in the hippocampus in brain sections. Conclusion: Administration of almond or primrose oils may improve central nervous system functions and decrease the risk of cardiovascular illnesses. They also might be effective against atherosclerosis, inflammation, endocrine disorders, and cognitive impairments for women who undergo surgical menopause prior to their natural menopause.
引言:用去卵巢大鼠评估杏仁油和报春花油对其脂质和神经化学特征的预防作用。方法:实验组如下:第一组:阴性对照组。第2组:大鼠口服杏仁油(800mg/kg/d)30天。第3组:大鼠口服报春花油(500mg/kg/d)30天。第4组:未经处理的去卵巢大鼠。第5组:去卵巢大鼠口服杏仁油(800mg/kg/d)30天。第6组:去卵巢大鼠每天口服报春花油(500mg/kg/d),持续30天。结果:口服杏仁油和报春花油可显著降低(P<0.05)血清总胆固醇(TC)、三酰甘油(TG)、低密度脂蛋白胆固醇(LDL-C),与第4组相比,去卵巢组的极低密度脂蛋白胆固醇(VLDL-C)浓度和高密度脂蛋白蛋白胆固醇(HDL-C)升高(P<0.05)。它们还增加了第5组和第6组的瘦素和雌二醇(E2)浓度。服用杏仁油和报春花油的大鼠大脑切片显示,去甲肾上腺素、多巴胺和5-羟基酪胺水平显著升高,PGE2和COX-2水平显著降低(P<0.05)。结论:杏仁油或报春花油可改善中枢神经系统功能,降低心血管疾病的风险。对于在自然绝经前接受手术绝经的女性来说,它们也可能对动脉粥样硬化、炎症、内分泌紊乱和认知障碍有效。
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引用次数: 0
Potent anticancer effects of vitamin C and vitamin C-rich fruit extract (Citrus sinensis L.) on human lung cancer cells 富含维生素C和维生素C的果实提取物(Citrus sinensis L.)对人癌症细胞的有效抗癌作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.30
Mohaddeseh Kamranikheiri, M. Koşar
Introduction: Studies have shown that synthetic agents are connected with some complications. This work was designed to study the effects of vitamin C and Citrus sinensis fruit extract (CSFE) on viability, DNA synthesis, and apoptosis stimulation in human lung cancer cells (COR-L105). Methods: The total contents of the phenolics, flavonoids, and ascorbic acid in CSFE were assessed through the Folin-Ciocalteu, aluminum chloride, and dinitrophenyl hydrazine methods, respectively. The cytotoxicity of vitamin C and CSFE on COR-L105 cells was evaluated by the cell viability assay. Measurement of the DNA synthesis was done through the BrdU solution assay. The expression levels of some apoptosis regulatory genes were also evaluated. Results: The total phenolic, flavonoids, and ascorbic acid contents of CSFE were 94.31 ± 2.27 gallic acid equivalents (mg/g) of dry extract, 63.26 ± 2.86 quercetin equivalents (mg/g) of dry extract, and 59 mg/L, respectively. The 50% cytotoxicity concentration (CC50) values of vitamin C and CSFE on cancer cells were 54.6 and 82.7.6 μg/mL, respectively. Vitamin C and CSFE dose-dependently declined the amount of DNA production in the cancer cells. The expression levels of caspase-3 and Bax genes were markedly (P < 0.001) elevated by vitamin C and CSFE, while they reduced the level of Bcl-2 gene (P < 0.05). Conclusion: The findings showed the potent anticancer effects of vitamin C and CSFE against human lung cancer cell lines. DNA synthesis reduction and apoptosis induction can be considered as possible mechanisms of action. However, further surveys are necessary to clarify the accurate mechanism and their efficacy.
引言:研究表明,合成药物与一些并发症有关。本研究旨在研究维生素C和香茅果实提取物(CSFE)对人癌症细胞(COR-L105)活力、DNA合成和凋亡刺激的影响。方法:分别采用Folin-Ciocalteu法、氯化铝法和二硝基苯肼法测定CSFE中酚类化合物、黄酮类化合物和抗坏血酸的总含量。通过细胞活力测定评估维生素C和CSFE对COR-L105细胞的细胞毒性。通过BrdU溶液测定法进行DNA合成的测量。还评估了一些细胞凋亡调控基因的表达水平。结果:CSFE的总酚类、黄酮类和抗坏血酸含量分别为94.31±2.27没食子酸当量(mg/g)、63.26±2.86槲皮素当量(mg/g)和59mg/L。维生素C和CSFE对癌症细胞的50%细胞毒性浓度(CC50)值分别为54.6和82.7.6μg/mL。维生素C和CSFE剂量依赖性地降低癌症细胞中DNA的产生量。维生素C和CSFE能显著提高胱天蛋白酶-3和Bax基因的表达(P<0.001),降低Bcl-2基因的表达水平(P<0.05)。DNA合成减少和细胞凋亡诱导可以被认为是可能的作用机制。然而,有必要进行进一步的调查,以澄清准确的机制及其功效。
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引用次数: 0
Antibacterial and cytotoxicity of chitosan nanocomposite loaded with thymol against some cariogenic bacteria 载百里香酚壳聚糖纳米复合材料对致龋细菌的抗菌及细胞毒性研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.23
Matin Kordestani, M. Rashidipour, H. Mahmoudvand, Shoukofeh Jalali, F. Kooshki
Introduction: Tooth decay as the most common infectious-nutritional disease in the world. The current work aims to investigate the antibacterial effect of thymol-loaded chitosan nanocomposite (TLCN) against Streptococcus mutans and Actinomyces viscosus as the main cariogenic bacteria. Methods: Antibacterial activity of TLCN was assessed on S. mutans and A. viscosus. The effects on protein leakage in the tested bacteria, as well as its cytotoxicity, were studied by Bradford’s method and cell viability assay, respectively. Results: The size of the nanocomposite varied from 100 to 600 nm. The best minimum inhibitory concentration (MIC) related to nanocomposite + chlorhexidine was reported 2.66 for both bacteria. TLCN dose-dependently increased the protein leakage (P < 0.05). The 50% cytotoxic concentration (CC50) of nanocomposite against on normal (HGF1-PI1) and cancer (KB) cells were 149.6 and 68.4 μg/mL, respectively. Conclusion: TLCN, especially in combination with chlorhexidine, displayed potent antibacterial effects against the main cariogenic bacterial causes. Nevertheless, other examinations are required to illuminate the precise mechanisms and its toxicity mainly in clinical settings.
简介:蛀牙是世界上最常见的营养性传染病。本工作旨在研究胸腺素负载的壳聚糖纳米复合材料(TLCN)对变形链球菌和粘放线菌作为主要致龋细菌的抗菌作用。方法:用TLCN对变形链球菌和粘球菌进行抗菌活性测定。分别用Bradford法和细胞活力测定法研究了对受试细菌蛋白质渗漏的影响及其细胞毒性。结果:纳米复合材料的尺寸在100~600nm之间。据报道,与纳米复合材料+氯己定相关的两种细菌的最佳最小抑制浓度(MIC)均为2.66。TLCN剂量依赖性地增加蛋白渗漏(P<0.05),纳米复合物对正常细胞(HGF1-PI1)和癌症细胞(KB)的50%细胞毒浓度(CC50)分别为149.6和68.4μg/mL。结论:TLCN,特别是与氯己定联合使用,对主要致龋细菌具有较强的抗菌作用。然而,主要在临床环境中,还需要进行其他检查来阐明确切的机制及其毒性。
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引用次数: 0
Chemical composition, anti-fungal and cytotoxic effects of Ferula macrecolea essential oil against Candida albicans resistant and sensitive strains 大阿魏精油对白色念珠菌耐药和敏感菌株的化学成分、抗真菌和细胞毒作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-18 DOI: 10.34172/jhp.2023.24
Nader Sadeghi, Hoda Sadeghi, Dharshini Nangaru Mohan, A. Sepahvand, Arash Alizadeh, Shirin Garavand
Introduction: Candidiasis therapy is a complicated concern because of the occurrence of resistance to antifungal agents. We studied the anti-fungal effects of Ferula macrecolea essential oil (FME) against Candida albicans resistant and sensitive strains, as well as its cytotoxic effects against normal and cancer cell lines. Methods: The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of F. macrecolea essential oil against C. albicans ATCC 5027 and C. albicans ATCC 76616 were studied by broth-microdilution approach. The cytotoxicities of FME on HGF1-PI (normal gingival cell line) and HepG2 (liver cancer cell line) cells were also studied. Results: The main components of essential oil were terpinolene (71.25%), n-nonanal (6.32%), and linalool (3.95%), respectively. The MIC and MFC of FME on C. albicans sensitive to nystatin were 1.6 and 2.0 μg/mL, respectively. The MIC and MFC of FME on nystatin-resistant strains were 3.3 and 4 μg/mL, respectively. The MIC and MFC of terpinolene on C. albicans sensitive to nystatin were 0.8 and 1.0 μg/mL, respectively. The MIC and MFC of terpinolene on nystatin-resistant strains were 2 and 2.4 μg/mL, respectively. The essential oil and terpinolene had no significant cytotoxic effects against normal cells. Conclusion: We revealed the promising antifungal effect of F. macrecolea essential oil and its main component, terpinolene, against C. albicans sensitive and resistant to nystatin with no significant toxicity on normal cells.
念珠菌病的治疗是一个复杂的问题,因为发生抗真菌药物的耐药性。研究了大阿魏精油(FME)对白色念珠菌耐药和敏感菌株的抗真菌作用,以及对正常细胞和癌细胞的细胞毒作用。方法:采用微液稀释法研究大黄油精油对白色念珠菌ATCC 5027和白色念珠菌ATCC 76616的最小抑菌浓度(MIC)和最小杀真菌浓度(MFC)。同时研究了FME对正常牙龈细胞系HGF1-PI和肝癌细胞系HepG2细胞的细胞毒性。结果:挥发油的主要成分为萜烯(71.25%)、正壬醛(6.32%)和芳樟醇(3.95%)。FME对制霉菌素敏感的白色念珠菌的MIC和MFC分别为1.6和2.0 μg/mL。FME对耐药菌株的MIC和MFC分别为3.3和4 μg/mL。萜烯对制霉菌素敏感的白色念珠菌的MIC和MFC分别为0.8和1.0 μg/mL。耐制氨抑素菌株对萜烯的MIC和MFC分别为2和2.4 μg/mL。精油和萜烯对正常细胞无明显的细胞毒作用。结论:大榄精油及其主要成分萜油烯对制霉菌素敏感和耐药的白色念珠菌具有良好的抗真菌作用,且对正常细胞无明显毒性。
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Journal of HerbMed Pharmacology
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