Acyclic Monoterpenes

无环单萜
  • 文章类型: Journal Article
    柠檬醛,在许多植物中发现的一种常见的单萜,是一种有趣的化合物,已被证明具有各种生物活性。尽管它在自然界中分布广泛,并且有许多研究表明其生物学活性,它的抗神经变性活性,特别是在体内条件下,是非常了解的。因此,本文旨在加深对柠檬醛对神经变性的影响因素和症状的认识。要做到这一点,进行了几次全面的测试,包括丁酰胆碱酯酶抑制的估计,肝毒性的评估以及体外氧化应激和脂质过氧化的检测,以及使用小鼠模型的体内行为评估。此外,离体测定受试动物的脑和血液中化合物的水平。结果表明,柠檬醛能够抑制丁酰胆碱酯酶的活性,并在体外保护肝细胞免受氧化应激和脂质过氧化。此外,体内行为测试表明柠檬醛(50mg/kg)可改善与获取相关的记忆过程(被动回避测试),急性和亚慢性给药。此外,我们发现25mg/kg和50mg/kg柠檬醛的给药对运动活性没有显着影响。除了前面提到的,气相色谱-质谱分析显示,亚慢性给予柠檬醛后,血液和大脑中存在该化合物。一起来看,在体外获得的结果,在体内和离体清楚地表明柠檬醛是一种有前途的单萜,可潜在地用于认知改善。
    Citral, a common monoterpene found in numerous plants, is an interesting compound that has been shown to have various biological activities. Although it is widely distributed in nature and there are many studies presenting its biological activities, its anti-neurodegenerative activity, especially under in vivo conditions, is very poorly understood. Thus, this paper aimed to deepen knowledge about citral activity towards factors and symptoms of neurodegeneration. To accomplish this, several comprehensive tests were conducted, including the estimation of butyrylcholinesterase inhibition, the evaluation of hepatotoxicity and the detection of oxidative stress and lipid peroxidation in vitro, as well as an in vivo behavioral assessment using mice models. Additionally, ex vivo determination of level of the compound in the brain and blood of a tested animal was undertaken. The results obtained revealed that citral is able to inhibit butyrylcholinesterase activity and protect hepatic cells against oxidative stress and lipid peroxidation in vitro. Moreover, behavioral tests in vivo indicated that citral (50 mg/kg) improves memory processes associated with acquisition (passive avoidance test), both in acute and subchronic administration. Additionally, we found that the administration of citral at 25 mg/kg and 50 mg/kg did not significantly affect the locomotor activity. Beyond the aforementioned, gas chromatography-mass spectrometry analysis revealed the presence of the compound in the blood and brain after subchronic administration of citral. Taken together, the results obtained in vitro, in vivo and ex vivo clearly indicate that citral is a promising monoterpene that can potentially be used towards cognition improvement.
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  • 文章类型: Journal Article
    背景:苦橙(柑橘)是一种水果灌木,原产于世界各地的热带和亚热带国家,由于其营养保健价值而在许多地区种植。目前的研究调查了通过三种不同的提取方法从埃及栽培的金盏花果皮中提取的挥发性成分的代谢谱和酶抑制活性。
    方法:使用三种方法分离了乌兰果皮的挥发性化学成分;蒸汽蒸馏(SD),加氢蒸馏(HD),和微波辅助加氢蒸馏(MAHD),然后通过GC-MS进行研究。通过不同的测定如DPPH,ABTS,FRAP,CUPRAC,以及磷钼和金属螯合潜力。此外,使用BChE测试了三种精油的酶抑制作用,AChE,酪氨酸酶,葡萄糖苷酶,以及淀粉酶测定。
    结果:GC/MS分析共检测到6个化合物。通过所有三种提取方法获得的主要成分是柠檬烯(SD为98.86%,98.68%的高清,和99.23%由MAHD)。观察到三种油的化合物的组成差异。加氢蒸馏技术产生的化合物数量最多,值得注意的是两种含氧单萜:芳樟醇(0.12%)和α-松油醇乙酸酯(0.1%)。
    结论:在我们的研究中,金盏花果皮油的提取方法的差异导致了油的化学组成的差异。柑橘精油及其成分显示出潜在的抗氧化剂,抗胆碱酯酶,抗黑素生成,和抗糖尿病活性。芳樟醇和α-松油醇乙酸酯的存在可以解释在自由基清除和AChE抑制测定中HD分离的油所观察到的优异活性。以及在酶抑制试验中。
    BACKGROUND: Bitter orange (Citrus aurantium) is a fruiting shrub native to tropical and subtropical countries around the world and cultivated in many regions due to its nutraceutical value. The current study investigated the metabolic profiling and enzyme inhibitory activities of volatile constituents derived from the C. aurantium peel cultivated in Egypt by three different extraction methods.
    METHODS: The volatile chemical constituents of the peel of C. aurantium were isolated using three methods; steam distillation (SD), hydrodistillation (HD), and microwave-assisted hydrodistillation (MAHD), and then were investigated by GC-MS. The antioxidant potential was evaluated by different assays such as DPPH, ABTS, FRAP, CUPRAC, and phosphomolybdenum and metal chelating potential. Moreover, the effect of enzyme inhibition of the three essential oils was tested using BChE, AChE, tyrosinase, glucosidase, as well as amylase assays.
    RESULTS: A total of six compounds were detected by GC/MS analysis. The major constituent obtained by all three extraction methods was limonene (98.86% by SD, 98.68% by HD, and 99.23% by MAHD). Differences in the composition of the compounds of the three oils were observed. The hydrodistillation technique has yielded the highest number of compounds, notably two oxygenated monoterpenes: linalool (0.12%) and α-terpineol acetate (0.1%).
    CONCLUSIONS: In our study differences in the extraction methods of C. aurantium peel oils resulted in differences in the oils\' chemical composition. Citrus essential oils and their components showed potential antioxidant, anticholinesterase, antimelanogenesis, and antidiabetic activities. The presence of linalool and α-terpineol acetate may explain the superior activity observed for the oil isolated by HD in both radical scavenging and AChE inhibition assays, as well as in the enzyme inhibition assays.
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  • 文章类型: Journal Article
    干旱胁迫限制了无价药用植物次生代谢产物的开发和生产。MenthapulegiumL.属于唇形科,是地中海地区种植的重要植物,具有药用和美学特性。这项研究调查了三种聚乙二醇(PEG)(0、5和10%)作为干旱胁迫诱导剂和四种硅纳米颗粒(SiNP)(0、25、50和100ppm)浓度作为激发剂的作用,以克服干旱胁迫的不利影响,关于体外生长的M.pulegiumL.植物的生长参数和生物活性化学成分。该实验作为析因实验进行,使用完全随机设计(CRD),由12种具有两个因子(3PEG×4SiNPs浓度)的处理组成,每个处理使用6个重复,总共72个实验单元。芽形成的百分比与PEG浓度成反比;对于最高的PEG浓度,10%PEG时,芽形成的百分比最低(70.26%)。50ppm的SiNPs增强了芽的形成,射击的数量,射击高度,新鲜和干重,迷迭香酸,总酚,和2,2-二苯基-1-吡啶酰肼(DPPH)清除活性。使用气相色谱-质谱(GC-MS),从P中提取的甲醇提取物显示存在大量次生代谢产物。提取物的主要成分为柠檬烯(2.51,2.99%),芳樟醇(3.84,4.64%),香叶醇(6.49,8.77%),薄荷醇(59.73,65.43%),pulegone(3.76,2.76%)和十六烷酸甲酯或棕榈酸甲酯(3.2,4.71%)为0ppmSiNPs,PEG0%和50ppmSiNPs,和PEG10%,分别。在50ppmSiNP和10%PEG处理组中,甲醇提取物中通过GC-MS鉴定的大多数化学成分都比对照组高。SiNP通过调节生物合成和积累一些渗透压来提高耐旱性,并减轻聚乙二醇诱导的干旱胁迫的负面影响。根据结果,大多数参数的最佳处理是50ppmSiNPs与10%PEG组合,形态和化学特性与PEG浓度成反比,因为PEG浓度最高(10%)的结果最低。大多数参数在最高SiNP浓度(100ppm)时降低,除了DPPH清除百分比,因为50和100ppmSiNP之间没有显着差异。
    The development and production of secondary metabolites from priceless medicinal plants are restricted by drought stress. Mentha pulegium L. belongs to the Lamiaceae family and is a significant plant grown in the Mediterranean region for its medicinal and aesthetic properties. This study investigated the effects of three polyethylene glycol (PEG) (0, 5, and 10%) as a drought stress inducer and four silicon nanoparticle (SiNP) (0, 25, 50, and 100 ppm) concentrations as an elicitor to overcome the adverse effect of drought stress, on the growth parameters and bioactive chemical composition of M. pulegium L. plants grown in vitro. The experiment was performed as a factorial experiment using a completely randomized design (CRD) consisting of 12 treatments with two factors (3 PEG × 4 SiNPs concentrations), 6 replicates were used for each treatment for a total of 72 experimental units.The percentage of shoot formation was inversely proportional to the PEG concentration; for the highest PEG concentration, the lowest percentage of shoot formation (70.26%) was achieved at 10% PEG. SiNPs at 50 ppm enhanced shoot formation, the number of shoots, shoot height, fresh and dry weight, rosmarinic acid, total phenols, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity. The methanol extract from M. pulegium revealed the presence of significant secondary metabolites using gas chromatography‒mass spectrometry (GC-MS). The principal constituents of the extract were limonene (2.51, 2.99%), linalool (3.84, 4.64%), geraniol (6.49, 8.77%), menthol (59.73, 65.43%), pulegone (3.76, 2.76%) and hexadecanoic acid methyl ester or methyl palmitate (3.2, 4.71%) for the 0 ppm SiNPs, PEG 0% and 50 ppm SiNPs, and PEG 10%, respectively. Most of the chemical components identified by GC‒MS in the methanol extract were greater in the 50 ppm SiNP and 10% PEG treatment groups than in the control group. SiNP improves drought tolerance by regulating biosynthesis and accumulating some osmolytes and lessens the negative effects of polyethylene glycol-induced drought stress.Based on the results, the best treatment for most of the parameters was 50 ppm SiNPs combined with 10% PEG, the morphological and chemical characteristics were inversely proportional to the PEG concentration, as the highest PEG concentration (10%) had the lowest results. Most parameters decreased at the highest SiNP concentration (100 ppm), except for the DPPH scavenging percentage, as there was no significant difference between the 50 and 100 ppm SiNPs.
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  • 文章类型: Journal Article
    蜡状芽孢杆菌通过产生引起腹泻和呕吐的毒素而引起食物中毒,在严重的情况下,心内膜炎,脑膜炎,和其他疾病。它还倾向于形成生物膜和孢子,导致食品生产环境的污染。柠檬醛是一种有效的天然抗菌剂,但其对蜡样芽孢杆菌的抗菌活性尚未得到广泛研究。在这项研究中,我们首先确定了最低抑菌浓度和最低杀菌浓度,生长曲线,在不同介质中的杀伤效果,膜电位,细胞内三磷酸腺苷(ATP),活性氧水平,和营养细胞的形态,其次是发芽率,形态学,孢子的发芽状态,最后是生物膜清除作用。结果表明,柠檬醛对细菌的最低抑菌浓度和最低杀菌浓度范围为100~800μg/mL。柠檬醛有效地延长了细菌的滞后期,细菌的生长速度减慢。Luria-Bertani肉汤中的细菌在0.5h内被柠檬醛以800μg/mL降低到检测限以下。大米中的细菌在0.5h内被柠檬醛以4000μg/mL降低到3logCFU/g。细胞内ATP浓度降低,膜电位改变了,细胞内活性氧浓度增加,正常细胞形态发生改变。用400μg/mL的柠檬醛处理后,孢子萌发率降至16.71%,孢子形态受到影响,孢子萌发状态发生改变。对生物膜的去除也有很好的效果。本研究表明,柠檬醛对蜡样芽孢杆菌营养细胞及其孢子具有良好的抑菌活性,对其生物膜也有良好的清除作用。柠檬醛有可能在食品工业生产中用作控制蜡状芽孢杆菌的抑菌物质。
    Bacillus cereus causes food poisoning by producing toxins that cause diarrhea and vomiting and, in severe cases, endocarditis, meningitis, and other diseases. It also tends to form biofilms and spores that lead to contamination of the food production environment. Citral is a potent natural antibacterial agent, but its antibacterial activity against B. cereus has not been extensively studied. In this study, we first determined the minimum inhibitory concentrations and minimum bactericidal concentrations, growth curves, killing effect in different media, membrane potential, intracellular adenosine triphosphate (ATP), reactive oxygen species levels, and morphology of vegetative cells, followed by germination rate, morphology, germination state of spores, and finally biofilm clearance effect. The results showed that the minimum inhibitory concentrations and minimum bactericidal concentrations of citral against bacteria ranged from 100 to 800 μg/mL. The lag phase of bacteria was effectively prolonged by citral, and the growth rate of bacteria was slowed down. Bacteria in Luria-Bertani broth were reduced to below the detection limit by citral at 800 μg/mL within 0.5 h. Bacteria in rice were reduced to 3 log CFU/g by citral at 4000 μg/mL within 0.5 h. After treatment with citral, intracellular ATP concentration was reduced, membrane potential was altered, intracellular reactive oxygen species concentration was increased, and normal cell morphology was altered. After treatment with citral at 400 μg/mL, spore germination rate was reduced to 16.71%, spore morphology was affected, and spore germination state was altered. It also had a good effect on biofilm removal. The present study showed that citral had good bacteriostatic activity against B. cereus vegetative cells and its spores and also had a good clearance effect on its biofilm. Citral has the potential to be used as a bacteriostatic substance for the control of B. cereus in food industry production.
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  • 文章类型: Journal Article
    这项全面的审查努力阐明芳樟醇的细微差别,一种在精油中大量发现的突出的单萜,构成他们组成的很大一部分。芳樟醇的生物医学相关性是一个重点,突出其通过抗伤害性作用观察到的治疗属性,抗焦虑特性,和受痴呆症影响的个体的行为调节。这些发现强调了该化合物在生物医学应用中的潜在应用。这篇综述进一步探讨了当代的表述,描述芳樟醇在纳米乳液中的适应性,微乳液,生物胶囊,和各种局部配方,包括外用凝胶和乳液。这项审查涵盖了2018年至2024年之间已发布和授权的专利,并阐明了芳樟醇应用的不断发展的景观。揭示皮肤病学的进步,抗炎,和抗菌领域。
    This comprehensive review endeavors to illuminate the nuanced facets of linalool, a prominent monoterpene found abundantly in essential oils, constituting a massive portion of their composition. The biomedical relevance of linalool is a key focus, highlighting its therapeutic attributes observed through anti-nociceptive effects, anxiolytic properties, and behavioral modulation in individuals affected by dementia. These findings underscore the compound\'s potential application in biomedical applications. This review further explores contemporary formulations, delineating the adaptability of linalool in nano-emulsions, microemulsions, bio-capsules, and various topical formulations, including topical gels and lotions. This review covers published and granted patents between 2018-2024 and sheds light on the evolving landscape of linalool applications, revealing advancements in dermatological, anti-inflammatory, and antimicrobial domains.
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  • 文章类型: Journal Article
    在ESKAPE病原体中,铜绿假单胞菌是一种广为人知的超级细菌,可导致难以治疗的感染。由于群体感应(QS)直接促进假单胞菌毒力,靶向QS电路是解除表型毒力的一种有前途的方法。因此,这项研究仔细检查了反QS,抗毒力,柠檬醛(CiT;植物化学)和三氯生(TcN;消毒剂)的抗生物膜潜力,单独和组合,针对铜绿假单胞菌PAO1/PA14。研究结果证实了CiT和TcN之间的协同作用,并揭示了它们的群体猝灭(QQ)潜力。在亚抑制水平,CiT-TcN组合显着阻碍了绿脓苷,总细菌蛋白酶,溶血素,和pytochelin的产生以及抑制铜绿假单胞菌中生物膜的形成。此外,通过分子对接研究,预测药物与铜绿假单胞菌QS受体的强关联,CiT和TcN的QQ和抗毒力潜力呈正相关。总的来说,该研究将CiT-TcN确定为含有QQ的有效药物组合,抗毒力,和抗生物膜的前景。
    Among the ESKAPE pathogens, Pseudomonas aeruginosa is an extensively notorious superbug that causes difficult-to-treat infections. Since quorum sensing (QS) directly promotes pseudomonal virulence, targeting QS circuits is a promising approach for disarming phenotypic virulence. Hence, this study scrutinizes the anti-QS, antivirulence, and anti-biofilm potential of citral (CiT; phytochemical) and triclosan (TcN; disinfectant), alone and in combination, against P. aeruginosa PAO1/PA14. The findings confirmed synergism between CiT and TcN and revealed their quorum quenching (QQ) potential. At sub-inhibitory levels, CiT-TcN combination significantly impeded pyocyanin, total bacterial protease, hemolysin, and pyochelin production alongside inhibiting biofilm formation in P. aeruginosa. Moreover, the QQ and antivirulence potential of CiT and TcN was positively correlated by molecular docking studies that predicted strong associations of the drugs with QS receptors of P. aeruginosa. Collectively, the study identifies CiT-TcN as an effective drug combination that harbors QQ, antivirulence, and anti-biofilm prospects against P. aeruginosa.
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  • 文章类型: Journal Article
    背景:在巴西流行医学中,Lippiaalba叶用于茶治疗疼痛和炎症性疾病。
    目的:评价化学成分,抗伤害性,和抗炎活性羊皮脂精油及其主要化合物香叶醇。
    方法:在帕拉州收集Lippiaalba叶,巴西。使用改良的Clevenger型提取器获得叶精油。然后,通过GC和GC-MS分析对油进行分析。为了评估LaEO和香叶醇的毒性,在小鼠模型中使用50,300和2000mg/kg的剂量。对于镇痛试验,腹部扭曲,热板,和福尔马林试验;所有组均接受LaEO和香叶醇治疗,剂量为25,50和100mg/kg;并使用耳水肿模型评估炎症.
    结果:含量最高的成分是含氧单萜:香叶醇(37.5%),geranial(6.7%)和neral(3.8%)。用LaEO和香叶醇治疗的动物表现出非典型行为,表现出嗜睡和嗜睡。处于镇静状态的动物的特征;相对重量与对照组相比没有显着差异。在腹部扭曲试验中,LaEO在25mg/kg,50mg/kg剂量,100毫克/千克减少扭曲的数量,减少了84.64%,81.23%,和分别为66.21%。在热板测试中,在所有测试期间,LaEO和香叶醇以25、50和100mg/kg的剂量增加了潜伏期;LaEO和香叶醇之间没有统计学差异。在福尔马林测试的第一阶段,只有25mg/kg和100mg/kg剂量的LaEO显示出显著的活性,减少了53.40%和58.90%的延迟时间。25mg/kg和100mg/kg剂量的LaEO减少了水肿的大小,显示59.38%(25mg/kg)和50%(100mg/kg)的抗炎活性。
    结论:唇皮精油和香叶醇具有中枢/外周镇痛和抗炎潜力,可作为常规药物的替代或补充治疗。需要更多的研究来评估其作用机制及其镇痛作用。
    BACKGROUND: In Brazilian popular medicine, Lippia alba leaves are used in teas to treat pain and inflammatory diseases.
    OBJECTIVE: to evaluate the chemical composition, antinociceptive, and anti-inflammatory activities of Lippia alba essential oil and its major compound geraniol.
    METHODS: Lippia alba leaves were collected in Pará state, Brazil. The leaf essential oil was obtained using a modified Clevenger-type extractor. Then, the oil was analyzed by GC and GC-MS analyses. To evaluate the toxicity of LaEO and geraniol, the doses of 50, 300, and 2000 mg/kg were used in a mouse model. For antinociception tests, abdominal contortion, hot plate, and formalin tests were used; all groups were treated with LaEO and geraniol at doses of 25, 50, and 100 mg/kg; and to evaluate inflammation using the ear edema model.
    RESULTS: The constituents identified in the highest content were oxygenated monoterpenes: geraniol (37.5%), geranial (6.7%) and neral (3.8%). The animals treated with LaEO and geraniol demonstrated atypical behaviors with aspects of lethargy and drowsiness, characteristics of animals in a state of sedation; the relative weights showed no significant difference compared to the controls. In the abdominal contortion test, LaEO at 25 mg/kg, 50 mg/kg doses, and 100 mg/kg reduced the number of contortions, representing a percentage reduction of 84.64%, 81.23%, and 66.21% respectively. In the hot plate test, LaEO and geraniol increased the latency time at doses of 25, 50, and 100 mg/kg in all test periods; there was no statistical difference between LaEO and geraniol. In the first phase of the formalin test, only doses of 25 mg/kg and 100 mg/kg of LaEO showed significant activity, reducing the latency time by 53.40% and 58.90%. LaEO at doses of 25 mg/kg and 100 mg/kg reduced the size of the edema, demonstrating an anti-inflammatory activity of 59.38% (25 mg/kg) and 50% (100 mg/kg).
    CONCLUSIONS: Lippia alba essential oil and geraniol showed central/peripheral analgesic and anti-inflammatory potential and can be used as an alternative or complementary treatment to conventional drugs. More studies are needed to evaluate its action mechanisms and its analgesic effects.
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  • 文章类型: Journal Article
    HemerocallisL.拥有丰富的种质资源,在观赏方面具有重要的价值,可食用,和医药方面。然而,不同品种的品质特征差异很大。选择具有特征香气的优质品种可以增加红花的经济价值。层次分析法(AHP)是比较评价多个特征维度的有效决策方法。通过应用层次分析法,本研究对60个月季花品种的芳香特性进行了分析和评价。采用顶空固相微萃取气相色谱-质谱联用(HS-SPME-GC-MS)技术对花中的挥发性成分进行了鉴定。发现有13种挥发性成分有助于Hemerocallis花的香气,这有助于评估它们在精油中的潜在应用,芳香疗法,和医疗。这些成分包括2-苯基乙醇,香叶醇,芳樟醇,非肛门,decanal,(E)-β-辛烯,α-法尼烯,吲哚,Nerolidol,3-呋喃甲醇,3-carene,苯甲醛和苯甲醇。使用AHP模型可以从大量数据中选择具有较好芳香潜力的品种。这项研究提供了一个全面的了解的香气成分的特点,在春花,为育种提供指导,提高了鲜花的经济价值。
    Hemerocallis L. possesses abundant germplasm resources and holds significant value in terms of ornamental, edible, and medicinal aspects. However, the quality characteristics vary significantly depending on different varieties. Selection of a high-quality variety with a characteristic aroma can increase the economic value of Hemerocallis flowers. The analytic hierarchy process (AHP) is an effective decision-making method for comparing and evaluating multiple characteristic dimensions. By applying AHP, the aromatic character of 60 varieties of Hemerocallis flowers were analyzed and evaluated in the present study. Headspace solid-phase microextraction gas chromatography-mass spectrometry (HS-SPME-GC-MS) was employed to identify volatile components in Hemerocallis flowers. Thirteen volatile components were found to contribute to the aroma of Hemerocallis flowers, which helps in assessing their potential applications in essential oil, aromatherapy, and medical treatment. These components include 2-phenylethanol, geraniol, linalool, nonanal, decanal, (E)-β-ocimene, α-farnesene, indole, nerolidol, 3-furanmethanol, 3-carene, benzaldehyde and benzenemethanol. The varieties with better aromatic potential can be selected from a large amount of data using an AHP model. This study provides a comprehensive understanding of the characteristics of the aroma components in Hemerocallis flowers, offers guidance for breeding, and enhances the economic value of Hemerocallis flowers.
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  • 文章类型: Journal Article
    阿魏酸(Fer)和香叶醇(Ger)是天然化合物,其抗氧化和抗炎活性赋予有益的特性,如抗菌,抗癌,和神经保护作用。然而,常规给药后,这些化合物的短半衰期损害了它们的治疗活性。我们提议,因此,一种新的前药(Fer-Ger),通过Fer和Ger的生物催化酯缀合获得,以增强设计为Fer-Ger递送和靶向系统的固体脂质微粒(SLM)的负载。SLM是通过不含有机溶剂的热乳液技术获得的。HPLC-UV分析表明,Fer-Ger在人或大鼠全血和大鼠肝匀浆中水解,半衰期分别为193.64±20.93、20.15±0.75和3.94±0.33min,分别,但不是在大鼠大脑匀浆中。与活性氧(ROS)诱导剂H2O2孵育的神经元分化小鼠神经母细胞瘤N2a细胞的研究证明了Fer-Ger预防氧化损伤的能力,尽管它似乎促进了ROS。包封在三硬脂酸甘油酯SLM中的Fer-Ger的量,在不存在或存在葡萄糖的情况下获得,为1.5±0.1%,允许控制前药释放(葡萄糖不存在)或敏感地提高其水溶解速率(葡萄糖存在)。这些新的“绿色”载体可以潜在地延长Fer和Ger的有益作用,或作为鼻用制剂诱导神经保护。
    Ferulic acid (Fer) and geraniol (Ger) are natural compounds whose antioxidant and anti-inflammatory activity confer beneficial properties, such as antibacterial, anticancer, and neuroprotective effects. However, the short half-lives of these compounds impair their therapeutic activities after conventional administration. We propose, therefore, a new prodrug (Fer-Ger) obtained by a bio-catalyzed ester conjugation of Fer and Ger to enhance the loading of solid lipid microparticles (SLMs) designed as Fer-Ger delivery and targeting systems. SLMs were obtained by hot emulsion techniques without organic solvents. HPLC-UV analysis evidenced that Fer-Ger is hydrolyzed in human or rat whole blood and rat liver homogenates, with half-lives of 193.64 ± 20.93, 20.15 ± 0.75, and 3.94 ± 0.33 min, respectively, but not in rat brain homogenates. Studies on neuronal-differentiated mouse neuroblastoma N2a cells incubated with the reactive oxygen species (ROS) inductor H2O2 evidenced the Fer-Ger ability to prevent oxidative injury, despite the fact that it appears ROS-promoting. The amounts of Fer-Ger encapsulated in tristearin SLMs, obtained in the absence or presence of glucose, were 1.5 ± 0.1%, allowing the control of the prodrug release (glucose absence) or to sensibly enhance its water dissolution rate (glucose presence). These new \"green\" carriers can potentially prolong the beneficial effects of Fer and Ger or induce neuroprotection as nasal formulations.
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  • 文章类型: Journal Article
    经皮给药为布洛芬等药物的给药提供了一个有希望的替代方案,以其镇痛和抗炎特性而闻名,与口服相比,胃肠道副作用减少。这项研究探索了布洛芬与薰衣草精油(LEO)在透皮贴剂中的潜在协同作用。分析了LEO的组成,揭示了主要的化合物,如乙酸芳樟醇和芳樟醇,以其镇痛和抗炎特性而闻名。研究了贴片的物理化学性质,表明添加LEO改善了内聚力。此外,热稳定性评估表明,随着起始分解温度从49.0°C增加到67.9°C,LEO掺入的稳定性增强。与不含LEO的贴剂中的60%RSA相比,含LEO的贴剂的抗氧化活性显著更高,具有79.13%RSA的自由基清除能力。释放和渗透研究表明,具有LEO的贴剂显示布洛芬通过皮肤的渗透增加,24小时后,74.40%的药物从含有LEO的贴剂释放,而没有LEO的贴剂为36.29%。LEO的渗透速率明显更快,表明更快的治疗效果。在含有布洛芬的透皮贴剂中加入LEO有望提高药物递送效率和治疗效果,提供改善疼痛管理和减少副作用的潜在策略。
    Transdermal drug delivery offers a promising alternative for administering medications like ibuprofen, known for its analgesic and anti-inflammatory properties, with reduced gastrointestinal side effects compared to oral administration. This study explored the potential synergistic effects of combining ibuprofen with lavender essential oil (LEO) in transdermal patches. The composition of LEO was analyzed, revealing predominant compounds such as linalyl acetate and linalool, which are known for their analgesic and anti-inflammatory properties. The physicochemical properties of the patches were investigated, indicating improved cohesion with the addition of LEO. Additionally, thermal stability assessments demonstrated enhanced stability with LEO incorporation with an increase in onset decomposition temperature from 49.0 to 67.9 °C. The antioxidant activity of patches containing LEO was significantly higher with a free radical scavenging ability of 79.13% RSA compared to 60% RSA in patches without LEO. Release and permeation studies showed that patches with LEO exhibited an increased permeation of ibuprofen through the skin with 74.40% of the drug released from LEO-containing patches compared to 36.29% from patches without LEO after 24 h. Moreover, the permeation rate was notably faster with LEO, indicating quicker therapeutic effects. The inclusion of LEO in transdermal patches containing ibuprofen holds promise for enhancing drug delivery efficiency and therapeutic effectiveness, offering a potential strategy for improved pain management with reduced side effects.
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