Alpinia galanga

高良姜高良姜
  • 文章类型: Journal Article
    胰高血糖素样肽-1(GLP-1)促分泌素是令人着迷的药物疗法,可克服GLP-1类似物和二肽基肽酶-4(DPP-4)抑制剂在治疗糖尿病和肥胖症中的缺陷。从天然来源发现新的GLP-1促分泌剂,AlpigalangolsA-Q(1-17),17种新的拉布丹二萜,包括四种不寻常的nor-labdane和含N的化合物,是从高良姜的果实中分离出来的。大多数分离株显示GLP-1在NCl-H716细胞中的促进作用,其中化合物3、4、12和14-17在50µM时具有246.0%-413.8%的高促进率。一项机制研究表明,最有效的化合物12上调了Gcg和Pcsk1的mRNA表达,以及PKA的蛋白磷酸化,CREB,和GSK3β,但对GPBAR和GPR119受体无活性。网络药理学分析表明,PI3K-Akt通路参与GLP-1刺激12,与AKT1、CASP3、PPARG、和ICAM1蛋白。这项研究表明,高良草富含多种具有GLP-1促进作用的拉丹二萜。代表一种来自天然来源的新型抗糖尿病候选药物。
    Glucagon-like peptide-1 (GLP-1) secretagogues are fascinating pharmacotherapies to overcome the defects of GLP-1 analogs and dipeptidyl peptidase-4 (DPP-4) inhibitors in treating diabetes and obesity. To discover new GLP-1 secretagogues from natural sources, alpigalangols A-Q (1-17), 17 new labdane diterpenoids including four unusual nor-labdane and N-containing ones, were isolated from the fruits of Alpinia galanga. Most of the isolates showed GLP-1 promotive effects in NCl-H716 cells, of which compounds 3, 4, 12, and 14-17 were revealed with high promoting rates of 246.0%-413.8% at 50 µM. A mechanistic study manifested that the most effective compound 12 upregulated the mRNA expression of Gcg and Pcsk1, and the protein phosphorylation of PKA, CREB, and GSK3β, but was inactive on GPBAR and GPR119 receptors. Network pharmacology analysis indicated that the PI3K-Akt pathway was involved in the GLP-1 stimulation of 12, which was highly associated with AKT1, CASP3, PPARG, and ICAM1 proteins. This study suggests that A. galanga is rich in diverse labdane diterpenoids with GLP-1 promoting effects, representing a new type of antidiabetic candidates from natural sources.
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  • 文章类型: Journal Article
    一种新的拉布丹二萜(1),两种新的降倍半萜(2-3),从高良姜(姜科)的种子中分离出八种已知的萜类化合物(4-11)。它们的结构和绝对构型由1D阐明,2DNMR,MS,以及他们的实验和计算电子圆二色性(ECD)的比较。对所有分离的化合物(1-11)的乙酰胆碱酯酶(AChE)抑制活性进行了评价,结果表明化合物6和9对AChE具有抑制活性,IC50值为295.70和183.91μM,而其他化合物没有显示任何抑制活性。
    A new labdane diterpene (1), two new norsesquiterpenoids (2-3), as well as eight known terpenoids (4-11) were isolated from the seeds of Alpinia galanga (Zingiberaceae). Their structures and absolute configurations were elucidated by 1D, 2D NMR, MS, and comparison of their experimental and calculated electronic circular dichroism (ECD). The acetylcholinesterase (AChE) inhibitory activities of all the isolated compounds (1-11) were evaluated and the result showed that compounds 6 and 9 had inhibitory activity against AChE, with IC50 values at 295.70 and 183.91 μM, whereas other compounds did not show any inhibitory activity.
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  • 文章类型: Journal Article
    随着纳米技术的出现,癌症的治疗正在从传统的方法转变为基于纳米颗粒的方法。因此,开发纳米粒子来治疗癌症是一个非常重要的领域。我们从高良姜的甲醇提取物中制备了银纳米颗粒(AgNPs),并通过紫外-可见分光光度法对其进行了表征,傅里叶变换红外(FTIR)光谱,泽塔西泽,和透射电子显微镜(TEM)。UV-Vis分光光度法吸收光谱显示表面等离子体激元在400和480nm之间。FTIR光谱分析表明,各种植物化学物质/次生代谢产物参与了还原,caping,和稳定AgNPs。Zetasier结果表明,形成的颗粒尺寸小,多分散指数(PDI)低,表明颗粒分布的范围很窄。TEM图像表明,所形成的颗粒大部分具有接近20-25nm的球形形态。Further,选定区域电子衍射(SAED)图像显示五个电子衍射环,表明颗粒的多晶性质。纳米颗粒对宫颈癌(SiHa)细胞系显示出高抗癌功效。纳米结构显示出剂量依赖性抑制,在6.25μg/mL剂量下观察到40%的杀伤。该研究显示了合成AgNPs的生态友好且具有成本效益的方法,并提供了对抗氧化剂和抗癌剂开发的见解。
    With the advent of nanotechnology, the treatment of cancer is changing from a conventional to a nanoparticle-based approach. Thus, developing nanoparticles to treat cancer is an area of immense importance. We prepared silver nanoparticles (AgNPs) from methanolic extract of Alpinia galanga rhizome and characterized them by UV-Vis spectrophotometry, Fourier transform Infrared (FTIR) spectroscopy, Zetasizer, and Transmission electron Microscopy (TEM). UV-Vis spectrophotometry absorption spectrum showed surface plasmon between 400 and 480 nm. FTIR spectrum analysis implies that various phytochemicals/secondary metabolites are involved in the reduction, caping, and stabilization of AgNPs. The Zetasier result suggests that the particles formed are small in size with a low polydispersity index (PDI), suggesting a narrow range of particle distribution. The TEM image suggests that the particles formed are mostly of spherical morphology with nearly 20-25 nm. Further, the selected area electron diffraction (SAED) image showed five electron diffraction rings, suggesting the polycrystalline nature of the particles. The nanoparticles showed high anticancer efficacy against cervical cancer (SiHa) cell lines. The nanostructures showed dose-dependent inhibition with 40% killing observed at 6.25 µg/mL dose. The study showed an eco-friendly and cost-effective approach to the synthesis of AgNPs and provided insight into the development of antioxidant and anticancer agents.
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  • 文章类型: Journal Article
    SSRIs被认为是治疗抑郁症和焦虑症的第一线。他们最常见的副作用之一,性功能障碍,导致许多患者停止用药和治疗。高良姜,一种生姜家族的植物,已被证明可以增强雄激素活性和性功能。这项研究旨在评估在食用SSRIs的成年男性的治疗方案中添加高良姜提取物是否可以改善SSRI诱导的勃起功能障碍。
    这项三盲随机临床试验是对60名在研究时接受SSRIs治疗的成年男性进行的。参与者分为两组,一组30人接受500毫克高良姜提取物和一组30名受试者接受安慰剂。在研究的第2周和第4周使用国际勃起功能指数(IIEF)重新评估人群,贝克抑郁量表,还有贝克焦虑量表.在所有的测试中,0.05的p值被认为是显著性的截止值。
    在研究开始时,安慰剂组和干预组的IIEF评分分别为10.6±3.8和11.2±4.8,没有显着差异(p值=0.577)。在研究的第4周,对照组和高良姜组的IIEF评分分别提高到13.7±4.3和17.4±3.7,这表明与安慰剂组相比,接受高良姜提取物的组的增加明显更大(p值<0.001)。
    在这项研究中,在使用SSRIs的男性患者的治疗方案中添加高良姜提取物对该组患者所经历的性功能障碍的影响是有希望的。类似的结果,如果证明,可以帮助患者和临床医生制定和遵循更好的治疗计划,获得更愉快的结果。
    [https://clinicaltrials.gov/],标识符[IRCT201011100005280N41]。
    UNASSIGNED: SSRIs are considered the first line in the medical treatment of depression and anxiety disorders. One of their most common side effects, sexual dysfunction, has led many patients to discontinuing their medication and treatment course. Alpinia galanga, a plant from the ginger family, has been shown to enhance androgenic activity and sexual function. This study aimed to assess whether the addition of Alpinia galanga extract to the treatment regimen of adult males consuming SSRIs can improve SSRI-induced erectile dysfunction.
    UNASSIGNED: This triple-blind randomized clinical trial was conducted on 60 adult males who were being treated with SSRIs at the time of the study. The participants were divided into two groups, a group of 30 people receiving 500 mg of Alpinia galanga extract and a group of 30 subjects receiving placebo. The population were re-assessed on week 2 and week 4 of the study using the international index of erectile function (IIEF), the Beck Depression Inventory, and the Beck Anxiety Inventory. In all the tests, a p-value of 0.05 was considered as the cut-off for significance.
    UNASSIGNED: At the beginning of the study, the IIEF scores of the placebo group and the intervention group were 10.6 ± 3.8 and 11.2 ± 4.8, respectively, which were not significantly different (p-value = 0.577). By week 4 of the study, the IIEF scores of the control group and the Alpinia galanga group had increased to 13.7 ± 4.3 and 17.4 ± 3.7 respectively, which demonstrates a remarkably larger increase in the group receiving Alpinia galanga extract in comparison to the placebo group (p-value < 0.001).
    UNASSIGNED: In this study, the effect of the addition of Alpinia galanga extract to the treatment regimen of male patients using SSRIs on the sexual dysfunction experienced by this group has been promising. Similar results, if proven, can aid both patients and clinicians in making and following better treatment plans with more pleasant outcomes.
    UNASSIGNED: [https://clinicaltrials.gov/], identifier [IRCT20101130005280N41].
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  • 文章类型: Journal Article
    The objective of the current study was to investigate the influence of synergism of the dry powder of Alpinia galanga rhizomes (AGR) and/or zinc sulfate in the diet on semen quality and reproductive traits of California rabbit bucks. The study was conducted in two stages. First stage: appreciation of semen characteristics, 36 California rabbit bucks (aged 5 months) with average body weights of 2980 g were divided randomly into six treatments (six individuals each). The treatment groups were: first group, control fed basal diet (C); second group, fed basal diet plus 1 g AGR/kg dry matter (DM) (AGR1); third group, fed basal diet plus 2 g AGR/kg DM (AGR2); fourth group, fed basal diet plus 200 mg Zn/litre drinking water (Zn); fifth group, fed basal diet plus 1 g AGR/kg DM and 200 mg Zn/litre drinking water (AGR1 + Zn); sixth group, fed basal diet plus 2 g AGR/kg DM and 200 mg Zn/litre drinking water (AGR2 + Zn). Second stage: the previous bucks were used to determine the efficiency of semen on reproductive fertility traits, 48 mature does (aged 6 months, nulliparous) with an average body weight of 3050 ± 20.7 g were divided randomly into six treatments and inseminated with previous groups of treated bucks. The results of the first stage, recorded high activity on gonadotropins hormones: follicle-stimulating hormone (FSH) and luteinizing hormone (LH), free testosterone (FT), progesterone (P4) and oestrogen (E217β) concentrations for AGR1 + Zn and AGR2 + Zn compared with the control group. Groups AGR1, AGR2, AGR1 + Zn and AGR2 + Zn had significantly lowered concentrations of triglycerides, total cholesterol, low-density lipoprotein, and malondialdehyde (MDA), whereas high-density lipoprotein and total antioxidant capacity (TAC) were increased significantly compared with the control group. The group supplemented with AGR with or without Zn had significantly improved ejaculate volume, advanced motility, sperm concentration, and cell integrity. Fertility rate and litter size were improved in all groups compared with the control. It was concluded that supplementing diets with Alpinia galanga and Zn significantly increased sperm percentage, motility and reproductive hormones (testosterone, FSH, LH, E217β, P4). This suggested that this plant when used may be favourable for improved sperm quality and fertility parameters.
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  • 文章类型: Journal Article
    高良姜在东亚被广泛用作香料或传统药物,通常被称为泰国姜。在本研究中,七种主要的苯丙素类化合物,(±)-1羟基查维考乙酸酯(1;HCA),(1\'S)-1\'-乙酰氧基查维考乙酸酯(2;ACA),(1'S)-1-乙酰氧基丁香酚乙酸酯(3;AEA),乙酸丁香酯(4),反式对香豆醛(5),反式-对-乙酰氧基肉桂醇(6),和反式对香豆基二乙酸酯(7),通过色谱法从高良姜根茎的95%EtOH和热水提取物中分离。评价苯丙烷1-7的葡萄糖刺激的胰岛素分泌(GSIS)效应和α-葡萄糖苷酶抑制活性。苯丙烷1-4增加大鼠INS-1胰腺β细胞的GSIS效应而无细胞毒性。此外,用AEA(3)处理INS-1细胞,以通过确定胰岛素受体底物2(IRS-2)的激活来确定β细胞功能和胰岛素分泌的合理机制,磷脂酰肌醇3-激酶(PI3K),Akt,胰腺和十二指肠同源盒-1(PDX-1)。在用AEA(3)治疗后,INS-1细胞显示这些蛋白质表达增加。同时,AEA(3)具有α-葡萄糖苷酶抑制活性。根据上述发现,我们建议AEA(3)作为一种潜在的抗糖尿病药物。
    Alpinia galanga have been widely used as spice or traditional medicine in East Asia, commonly known as Thai ginger. In the present study, seven major phenylpropanoids, (±)-1\'-hydoxychavicol acetate (1; HCA), (1\'S)-1\'-acetoxychavicol acetate (2; ACA), (1\'S)-1\'-acetoxyeugenol acetate (3; AEA), eugenyl acetate (4), trans-p-coumaraldehyde (5), trans-p-acetoxycinnamyl alcohol (6), and trans-p-coumaryl diacetate (7), were isolated from the 95% EtOH and hot water extracts of the rhizomes of A. galanga by chromatographic method. Phenylpropanoids 1-7 were evaluated for glucose-stimulated insulin secretion (GSIS) effect and α-glucosidase inhibitory activity. Phenylpropanoids 1-4 increase GSIS effect without cytotoxicity in rat INS-1 pancreatic β-cells. In addition, INS-1 cells were treated with AEA (3) to determine a plausible mechanism of β-cell function and insulin secretion through determining the activation of insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), Akt, and pancreatic and duodenal homeobox-1 (PDX-1). Upon treatment with AEA (3), INS-1 cells showed an increase in these protein expressions. Meanwhile, AEA (3) exhibited α-glucosidase inhibitory activity. On the basis of the above findings, we suggest AEA (3) as a potential antidiabetic agent.
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  • 文章类型: Journal Article
    背景:药用植物的植物化学研究正在迅速普及,具有许多药理作用。本研究旨在确定由五种药用植物组成的ClearbresiblePlus提取物(CBL-P)的抗氧化能力以及抗癌和抗迁移活性,高良姜,PiperNigrum,金叶柑橘,Tiliacoratriandra,和大麻对人结肠癌细胞SW620和HCT116细胞系,和人非小细胞肺癌细胞A549和NCI-H460细胞系。
    方法:在本研究中,使用90%乙醇提取干燥植物粉末。此外,通过DPPH和ABTS测定法研究CBL-P的抗氧化活性,并使用Griess反应使用一氧化氮测定法研究抗炎活性。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基-2H-四唑溴化物(MTT)和划痕测定法研究了CBL-P的抗增殖和抗迁移。
    结果:结果显示,对于所有四种细胞系,CBL-P具有有效的抗增殖活性,IC50值呈浓度和时间依赖性。CBL-P还对所有研究的癌细胞具有有效的抗迁移活性。CBL-P在孵育48小时后对四种不同类型的癌细胞(A549,NCI-H460,HCT116和SW620)具有抗迁移活性,在A549细胞(伤口闭合的10.23%)和NCI-H460细胞(伤口闭合的9.16%)中,在最高测试浓度(15μg/mL)下观察到最大的效果。CBL-P还有效减少HCT116和SW620细胞的迁移,闭合面积范围为10-50%。此外,CBL-P具有抗氧化活性,DPPH和ABTS测定的IC50值分别为8.549±0.241mg/mL和2.673±0.437mg/mL。分别。CBL-P在40μg/mL的浓度下也显示出抗炎活性,对NO产生具有最佳抑制活性。
    结论:结论:混合物提取物具有抗氧化和抗炎活性。此外,混合植物提取物对SW620,HCT116,A549和NCI-H460细胞显着表现出抗增殖和抗迁移活性(P≤0.05)。一起来看,我们的研究结果表明,药用植物可能具有协同作用,当用作佐剂时,可能会增强癌症治疗的有效性.这些发现为今后努力探索作用机制提供了坚实的科学基础。
    BACKGROUND: The phytochemical study of medicinal plants is rapidly gaining popularity with many pharmacologic effects. This study aims to determine the antioxidant capacity as well as anticancer and antimigration activities of Clear belongs Plus extract (CBL-P) which consisted of five medicinal plants namely, Alpinia galanga, Piper nigrum, Citrus aurantifolia, Tiliacora triandra, and Cannabis sativa on human colon cancer cells SW620 and HCT116 cell lines, and human non-small cell lung cancer cells A549 and NCI-H460 cell lines.
    METHODS: In this study the dried-plant powder was extracted using 90% ethanol. Additionally, CBL-P was studied antioxidative activity via DPPH and ABTS assays and anti-inflammatory activities using nitric oxide assay using Griess reaction. Antiproliferation and antimigration of CBL-P were investigated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) and scratch assay.
    RESULTS: The results showed that CBL-P had potent antiproliferative activity with IC50 values in a concentration- and time-dependent manners for all four cell lines. CBL-P also possessed potent antimigration activity against all studied cancer cells. CBL-P demonstrated antimigration activity on four different types of cancer cells (A549, NCI-H460, HCT116, and SW620) after 48 h of incubation, with the greatest effect seen at the highest concentration tested (15 μg/mL) in A549 cells (10.23% of wound closure) and NCI-H460 cells (9.16% of wound closure). CBL-P was also effective in reducing migration in HCT116 and SW620 cells, with a range of closure area from 10-50%. In addition, CBL-P had antioxidant activity with IC50 values of 8.549 ± 0.241 mg/mL and 2.673 ± 0.437 mg/mL for DPPH and ABTS assays, respectively. CBL-P also showed anti-inflammatory activity with the best inhibitory activity on NO production at a concentration of 40 μg/mL.
    CONCLUSIONS: In conclusion, the mixture extract possessed antioxidant and anti-inflammatory activity. Furthermore, the mixture plant extract significantly exhibited antiproliferative and antimigration activities on SW620, HCT116, A549, and NCI-H460 cells (P ≤ 0.05). Taken together, our results suggest that medicinal plants may have synergistic effects that could potentially enhance the effectiveness of cancer treatment when used as adjuvants. These findings provide a solid scientific foundation for future efforts to explore the mechanism of action.
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  • 文章类型: Journal Article
    <b>背景和目的:</b>AL22菌株从<i>Alpiniagalanga</i>的根际土壤中分离得到(L.)威尔德(姜科),并被鉴定为<i>微双孢菌</i>sp。,通过分析它的形态,趋化性和16SrDNA序列。先前的研究证明了其粗提物对&lt;i&gt;蜡状芽孢杆菌&lt;/i&gt;的杀菌作用,<i>枯草芽孢杆菌</i>,<i>金黄色葡萄球菌</i>和耐甲氧西林金黄色葡萄球菌</i>本研究旨在分离主要化合物并评估其生物学特性。<b>材料与方法:</b>硅胶柱色谱和薄层色谱用于3,4-二氢-lactucin(化合物<b>1</b>)和伞形酮(化合物<2</b>)的质谱鉴定,分别。进行了抗菌和抗癌活性。<b>结果:</b>生物测定研究表明化合物<b>1</b>对革兰氏阳性菌具有抗菌活性,其最低抑菌浓度和最低杀菌浓度为16-32和64-128μgmL<sup></sup><sup>1</sup>,分别。粗提取物和纯化的化合物对L929和Vero细胞显示弱的细胞毒性活性,IC<sub>50</sub>值>512.00μgmL<sup>/sup><sup>1</sup>。在MDA-MB-231和HeLa细胞中观察到化合物<b>1</b>的细胞毒性,IC<sub>50</sub>值为37.62和75.34μgmL<sup></sup>1<分别,而其针对HepG2细胞的IC<sub>50</sub>值为456.67μgmL<sup>/sup><1</sup><b>结论:</b>这些发现表明<i>的化合物<b>1</b>,AL22具有抗菌和抗癌活性。对3,4-二氢-lactucin的广泛研究可能导致开发用于管理细菌感染和癌症的有益方法。
    <b>Background and Objective:</b> The AL22 strain was isolated from the rhizosphere soil of <i>Alpinia galanga</i> (L.) Willd (Zingiberaceae) and identified as <i>Microbispora</i> sp., by analysing its morphology, chemotaxonomy and 16S rDNA sequence. Previous studies demonstrated the bactericidal effects of its crude extract against <i>Bacillus cereus</i>, <i>Bacillus subtilis</i>, <i>Staphylococcus aureus</i> and methicillin-resistant <i>Staphylococcus aureus</i>. The present study aimed to isolate the major compounds and evaluate their biological properties. <b>Materials and Methods:</b> Silica gel column chromatography and thin-layer chromatography were used for the purification and identification of 3,4-dihydro-lactucin (compound <b>1</b>) and umbelliferone (compound <b>2</b>) by NMR and mass spectrometry, respectively. Antibacterial and anticancer activities were carried out. <b>Results:</b> The bioassay studies illustrated that compound <b>1</b> had antibacterial activity against gram-positive bacteria, with its minimum inhibitory concentration and minimum bactericidal concentration of 16-32 and 64-128 μg mL<sup></sup><sup>1</sup>, respectively. The crude extract and purified compounds showed weak cytotoxic activity on the L929 and Vero cells with IC<sub>50</sub> values >512.00 μg mL<sup></sup><sup>1</sup>. The cytotoxicity of compound <b>1</b> was observed in the MDA-MB-231 and HeLa cells with IC<sub>50</sub> values of 37.62 and 75.34 μg mL<sup></sup><sup>1</sup>, respectively, while its IC<sub>50</sub> value against the HepG2 cells was 456.67 μg mL<sup></sup><sup>1</sup>. <b>Conclusion:</b> These findings showed that compound <b>1</b> of <i>Microbispora</i> sp., AL22 exhibited antibacterial and anticancer activities. Extensive studies on 3,4-dihydro-lactucin could lead to the development of beneficial approaches for managing bacterial infections and cancer.
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  • 文章类型: Journal Article
    AlpiniagalangaWild.,更大的高良姜,几千年来一直被用作香料和传统医学。其中枢神经系统(CNS)刺激活性和神经保护作用已在动物模型和人体试验中得到证实。然而,造成这些影响的化合物尚未确定。因此,主要成分(对羟基苯甲醛(1),反式-对-香豆醇(2),对香豆醛(4),高良姜醇A(5),高良姜醇B(6),反式-对-乙酰氧基肉桂醇(7),1\'S-1\'-乙酰氧基查维考乙酸酯(ACA,9),和1'S-1'-乙酰氧基丁香酚乙酸酯(AEA,10))通过平行人工膜通透性测定(PAMPA)分离以研究其水性稳定性和跨胃肠道(GIT)膜和血脑屏障(BBB)的被动扩散。我们对化合物1、2、4、7、9和10的积极结果表明良好的渗透性,因此,对中枢神经系统中更大的高良姜的影响有潜在的贡献。PAMPA-BBB的结果通过基于计算机化学成像的ChemGPS-NP框架实验得到证实。此外,检查高良姜化合物相对于已知精神兴奋剂的化学空间位置,发现附近的所有分子都是NET/SERT抑制剂。由于ACA和AEA与任何一种化合物都没有太多接近,进一步研究其降解产物的重要性变得更加明显。
    Alpinia galanga Willd., greater galangal, has been used for thousands of years as a spice as well as in traditional medicine. Its central nervous system (CNS) stimulant activity and neuroprotective effects have been proved both in animal models and human trials. However, the compounds responsible for these effects have not been identified yet. Therefore, the main constituents (p-OH-benzaldehyde (1), trans-p-coumaryl-alcohol (2), p-coumaryl-aldehyde (4), galanganol A (5), galanganol B (6), trans-p-acetoxycinnamyl alcohol (7), 1\'S-1\'-acetoxychavicol acetate (ACA, 9), and 1\'S-1\'-acetoxyeugenol acetate (AEA, 10)) were isolated to investigate their aqueous stability and passive diffusion across the gastro-intestinal tract (GIT) membrane and the blood-brain barrier (BBB) by the parallel artificial membrane permeability assay (PAMPA). Our positive results for compounds 1, 2, 4, 7, 9, and 10 suggest good permeability, thus potential contribution to the effects of greater galangal in the CNS. The results of the PAMPA-BBB were corroborated by in silico chemography-based ChemGPS-NP framework experiments. In addition, examination of the chemical space position of galangal compounds in relation to known psychostimulants revealed that all the molecules in proximity are NET/SERT inhibitors. As ACA and AEA did not show much proximity to either compound, the importance of further investigation of their degradation products becomes more pronounced.
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  • 文章类型: Journal Article
    本研究旨在研究高良姜的化学成分并揭示高良姜的选择性抑制活性(L.)威尔德。精油(AGO)对乙酰胆碱酯酶(AChE)的比较丁酰胆碱酯酶(BChE)。通过气相色谱-质谱法研究了AGO的化学成分。采用Ellman法测定其对AChE和BChE的抑制活性。开发了具有理想的抗胆碱酯酶作用的微乳液系统。据报道,肉桂酸甲酯和1,8-桉树脑是AGO的主要成分。A.galanga油对AChE和BChE的IC50值分别为24.6±9.6和825.4±340.1µg/mL,分别。与加兰他敏氢溴酸盐(6.4±1.5)相比,AGO对AChE的选择性(34.8±8.9)更高,这表明AGO是一种有效成分,对阿尔茨海默病的治疗副作用较少。有趣的是,AGO的微乳剂具有比单独的天然油明显更高的抗胆碱酯酶活性。因此,AGO微乳剂是治疗阿尔茨海默病的一种有前途的替代方法。
    This study aimed to investigate the chemical composition and reveal the selective inhibitory activity of Alpinia galanga (L.) Willd. essential oil (AGO) on acetylcholinesterase (AChE) compared to butyrylcholinesterase (BChE). The chemical composition of AGO was investigated by means of gas chromatography-mass spectrometry. Ellman\'s method was used to determine the inhibitory activities against AChE and BChE. Microemulsion systems with desirable anticholinesterase effects were developed. Methyl cinnamate and 1,8-cineole were reported as the major component of AGO. The IC50 values of A. galanga oil against AChE and BChE were 24.6 ± 9.6 and 825.4 ± 340.1 µg/mL, respectively. The superior selectivity of AGO on AChE (34.8 ± 8.9) compared to galantamine hydrobromide (6.4 ± 1.5) suggested AGO to be an effective ingredient with fewer side effects for Alzheimer\'s treatment. Interestingly, the microemulsion of AGO possessed significantly higher anticholinesterase activity than that of native oil alone. Therefore, microemulsion of AGO is a promising alternative approach for the treatment of Alzheimer\'s disease.
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