herbal extract

草药提取物
  • 文章类型: Journal Article
    目的在本研究中,斑马鱼胚胎用于研究基于氧化锌纳米颗粒(ZnONPs)的新型肛门内药物(ICM)的细胞毒性作用。负载有多草药提取物(Azadirachtaindica和Solanumxanthocarpum)。材料和方法在本研究中,采用绿色和可持续的方法合成ZnONPs,并将其与印su的树皮和种子提取物混合,以用作多草药ICM。在将二水合乙酸锌溶解在蒸馏水中,随后缓慢加入氢氧化钠溶液和草药提取物后,产生混合物的颜色变化,证实了ZnO纳米颗粒的制剂。通过斑马鱼胚胎毒性测试评估了这些绿色合成的ZnONP的作用。将胚胎暴露于不同浓度(25、50和100µg/mL)的合成实验剂量的ZnONP中,并与对照胚胎进行比较。毒理学终点,如斑马鱼胚胎的存活率,孵化率,和心率,被记录和描述。结果在绿色合成的ZnONP处理的胚胎中观察到死亡率和孵化延迟的浓度依赖性增加,随后心率下降。随着实验剂量的100µg/mL浓度的增加,观察到最大毒性,在25µg/mL的低浓度下,它没有有效地显示斑马鱼胚胎的任何发育改变。结论负载ZnONPs的新型多草药ICM对心率表现出剂量依赖性作用,孵化,和胚胎的死亡率。在最佳浓度下,这种药物表现出最小的发育畸形和细胞毒性作用,表明其使用的安全性。然而,药物浓度的增加导致严重的发育畸形。
    Objective In this study, zebrafish embryos are used to study the cytotoxic effects of a novel intracanal medication (ICM) based on zinc oxide nanoparticles (ZnO NPs) loaded with polyherbal extracts (Azadirachta indica and Solanum xanthocarpum). Material and methods In the present study, a green and sustainable method was employed for the synthesis of ZnO NPs mixed with bark and seed extracts of Azadirachta indica and Solanum xanthocarpum to be used as a polyherbal ICM. Formulation of ZnO NPs was confirmed with color change in mixture produced upon dissolving zinc acetate dihydrate in distilled water followed by slow addition of sodium hydroxide solution and herbal extracts. The effects of these green synthesized ZnO NPs were evaluated through a zebrafish embryo toxicity test. Embryos were exposed to different concentrations (25, 50, and 100 µg/mL) of synthesized experimental doses of ZnO NP and compared with the control embryos. Toxicological endpoints, such as the zebrafish embryo\'s survival rate, hatching rate, and heart rate, were noted and described. Results A concentration-dependent increase in mortality rate and hatching delay followed by declined heart rate was observed in green synthesized ZnO NP-treated embryos. The maximum toxicity was observed with an increase in the concentration of 100 µg/mL of the experimental dose, and at a low concentration of 25 µg/mL, it does not effectively show any developmental alteration in zebrafish embryos. Conclusion A novel polyherbal ICM loaded with ZnO NPs exhibited a dose-dependent effect on the heart rate, hatching, and mortality rate of the embryos. At optimal concentrations, the medication demonstrated minimal developmental malformations and cytotoxic effects, indicating its safety for use. However, increasing concentrations of the medication resulted in severe developmental malformations.
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  • 文章类型: Journal Article
    致畸和高尿酸血症是favipiravir的主要副作用,一种抗病毒药物最近发现可用于治疗轻度至中度冠状病毒(COVID-19)感染。这项研究调查了中药提取物如苦根(PK)和黄芩(SB)及其活性化学成分(黄芩苷和黄芩素)对法比拉韦诱导的大鼠肝毒性的有益作用。制剂组合包括favipiravir,favipirravir+PK提取物,法比拉韦+纯黄芩苷,法比拉韦+纯黄芩素,和分别指定为F1、F2、F3、F4和F5的faviravir+SB提取物,将其口服给予大鼠21天。Favipiravir导致SGOT水平升高,SGPT,ALP,总胆红素,和尿酸和肝脏重量降低,当使用法哌韦和黄芩素组合以及法哌韦和SB提取物的异草药制剂时,可以减轻。本文强调了使用肝保护剂改善favipirravir诱导的肝毒性的有吸引力的主张。
    Teratogenicity and hyperuricaemia are the main side effects of favipiravir, an antiviral drug recently found its use to treat mild to moderate coronavirus (COVID-19) infections. This study investigated the beneficial effect of herbal extracts like Picrorrhiza kurroa (PK) and Scutellaria baicalensis (SB) and their active chemical constituents (baicalin and baicalein) on favipiravir-induced hepatotoxicity in rats. The formulation combinations included favipiravir, favipiravir + PK extract, favipiravir + pure baicalin, favipiravir + pure baicalein, and favipiravir + SB extract designated as F1, F2, F3, F4 and F5 respectively that were administered to rats orally for 21 days. Favipiravir caused increased levels of SGOT, SGPT, ALP, total bilirubin, and uric acid and decreased liver weight which was alleviated when alloherbal formulation of favipiravir and baicalein combination and favipiravir and SB extract was used. This paper highlights an attractive proposition to ameliorate favipiravir-induced hepatotoxicity using hepatoprotective agents.
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  • 文章类型: Journal Article
    伤口愈合是一个复杂且连续的过程,受许多因素的影响,这些因素需要合适的环境来实现愈合。伤口愈合的自然能力经常被几个外部和内在因素改变,导致慢性伤口的发生。已经开发了许多伤口敷料,然而,目前可用的替代品无法合并所有必须快速皮肤再生的条件。
    使用PubMed对有关草药纳米复合伤口敷料的文章进行了广泛的评论,Scopus,和谷歌学者数据库,从2006年到2024年。这篇综述涉及导致伤口不愈合的病理生理学和因素,伤口敷料类型,草药生物活性物质对伤口愈合的作用,以及采用纳米技术提供草药活性物质的优势。许多纳米复合伤口敷料掺入植物成分,草药提取物,和精油进行了讨论。
    有一个强有力的证据表明,几种草药生物活性物质具有抗炎作用,抗菌,抗氧化剂,镇痛药,和加速伤口愈合过程的血管生成促进剂活性。纳米技术是一个有前途的战略,以提供草药生物活性,因为它确定他们的控制释放,提高生物利用度,改善对底层皮肤层的渗透性,促进伤口愈合.草药活性物质和基于纳米的敷料的组合为伤口管理提供了新的场所。
    UNASSIGNED: Wound healing is an intricate and continual process influenced by numerous factors that necessitate suitable environments to attain healing. The natural ability of wound healing often gets altered by several external and intrinsic factors, leading to chronic wound occurrence. Numerous wound dressings have been developed; however, the currently available alternatives fail to coalesce in all conditions obligatory for rapid skin regeneration.
    UNASSIGNED: An extensive review of articles on herbal nano-composite wound dressings was conducted using PubMed, Scopus, and Google Scholar databases, from 2006 to 2024. This review entails the pathophysiology and factors leading to non-healing wounds, wound dressing types, the role of herbal bio-actives for wound healing, and the advantages of employing nanotechnology to deliver herbal actives. Numerous nano-composite wound dressings incorporated with phytoconstituents, herbal extracts, and essential oils are discussed.
    UNASSIGNED: There is a strong substantiation that several herbal bio-actives possess anti-inflammatory, antimicrobial, antioxidant, analgesic, and angiogenesis promoter activities that accelerate the wound healing process. Nanotechnology is a promising strategy to deliver herbal bio-actives as it ascertains their controlled release, enhances bioavailability, improves permeability to underlying skin layers, and promotes wound healing. A combination of herbal actives and nano-based dressings offers a novel arena for wound management.
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  • 文章类型: Journal Article
    弓形虫病是一种世界范围内分布的人畜共患寄生虫感染,对人类健康影响很大。它对现有药物的临床分辨率有限,使治疗具有挑战性。槲皮素,具有生物和药理特性,包括抗寄生虫,抗氧化剂,和抗癌活动,是当前药物的可能替代品。海洋无脊椎动物可以产生大量不同的分子,其中许多是具有独特特征的生物活性物质。在这项研究中,我们评估了槲皮素和仙女草(水母)的毒液对弓形虫第三幼虫的体外杀线虫作用。在罗斯威尔公园纪念研究所-1640培养基的微孔板中,将幼虫与槲皮素的乙醇提取物(0.01、0.02、0.05、0.08、0.1、0.25和0.5mM/mL)和仙女草毒的水提取物(15、20、25、30、35、40和60µg/mL)一起孵育,以评估其杀幼虫效果。扫描电子显微镜研究了两种提取物的致死浓度(LC90)对栽培幼虫体壁的可能影响,与在阿苯达唑中培养的相比。我们的研究表明,与对照组和阿苯达唑治疗组相比,槲皮素和仙女树毒液暴露对犬第三幼虫的死亡率和超微结构的影响。
    Toxocariasis is a zoonotic parasitic infection with worldwide distribution and high impact on human health. It has a limited clinical resolution with the available drugs, making it challenging to treat. Quercetin, which possesses biological and pharmacological qualities including antiparasitic, antioxidant, and anticancer activities, is a possible substitute for the current medications. Marine invertebrates can produce a vast array of different molecules, many of which are biologically active substances with distinct characteristics. In this study, we assessed the in vitro nematocidal effect of both quercetin and venom of Cassiopea andromeda (jellyfish) against third larvae of Toxocara canis. In microplates with Roswell Park Memorial Institute-1640 medium, larvae were incubated with ethanolic extract of quercetin (0.01, 0.02, 0.05, 0.08, 0.1, 0.25, and 0.5 mM/mL) and water extract of C. andromeda venom (15, 20, 25, 30, 35, 40, and 60 µg/mL) to evaluate their larvicidal effect. A scanning electron microscopy has investigated the possible effect of lethal concentration (LC90) of both extracts on the body wall of cultivated larvae, in comparison with those cultivated in albendazole. Our study revealed the effects of both quercetin and C. andromeda venom exposure on the mortality rate and the ultrastructure of T. canis third larva in comparison with control and albendazole-treated groups.
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  • 文章类型: Journal Article
    这项研究介绍了一种创新的磁性泡腾辅助微萃取方法,通过一锅法简化泡腾片的制备,该方法将CO2供体(Na2CO3)和H供体(NaH2PO4)与裸露的磁性颗粒(Fe3O4)和吸附剂(羟基化的多壁碳纳米管)混合,然后按。在提取过程中,裸磁性颗粒和吸附剂经历原位自组装以产生磁性吸附剂。泡腾产生气泡,增强有效提取和磁性促进磁性吸附剂从样品溶液中的容易分离,在4分钟内完成该过程。应用于果汁和草药提取物中的有机氯农药分析,该方法具有良好的线性(R2>0.993),灵敏度(检测限:0.010-0.125ng/mL),准确度(回收率:85.8-99.9%),和精密度(RSD<9.7%)与GC-ECD。总的来说,这种方法以其简单性脱颖而出,成本效益,以及现场分析的适用性,由于其操作简便和独立于专用设备。
    This study introduced an innovative magnetic effervescence-assisted microextraction method, streamlining the preparation of effervescent tablets through a one-pot method that blends a CO2 donor (Na2CO3) and an H+ donor (NaH2PO4) with bare magnetic particles (Fe3O4) and an adsorbent (hydroxylated multi-walled carbon nanotubes), followed by pressing. During the extraction process, the bare magnetic particles and adsorbent undergo in-situ self-assembly to create a magnetic adsorbent. The effervescence generates bubbles that enhance effective extraction and magnetism facilitates the easy separation of the magnetic adsorbent from the sample solution, completing the process within 4 min. Applied to organochlorine pesticide analysis in fruit juices and herbal extracts, the method exhibits excellent linearity (R2 > 0.993), sensitivity (detection limits: 0.010-0.125 ng/mL), accuracy (recoveries: 85.8-99.9%), and precision (RSDs < 9.7%) with GC-ECD. Overall, this approach stands out for its simplicity, cost-effectiveness, and suitability for on-site analysis, owing to its operational ease and independence from specialized equipment.
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  • 文章类型: Journal Article
    本研究旨在研究使用池塘苹果(Annonaglabra)化合物作为预防和治疗急性肝胰腺坏死病(AHPND)的新策略,并更好地了解虾健康改善的机制。使用各种溶剂提取光晕叶提取物,并检测抗副溶血弧菌菌株的体外和体内活性。与乙醇和水提取物相比,甲醇提取物杀菌效果最强(MBC/MIC比为2.50±1.00),最小抑菌浓度(MIC)为0.023±0.012mgml-1,最小杀菌浓度(MBC)为0.065±0.062mgml-1。白腿虾(P.南美白对虾,体重10.37±0.27g),以1%的量饲喂含A.glabra甲醇提取物的饮食(AMEDs),1.5%,和2.0%显示对存活率没有有害影响,并且在喂食30天后长度和体重显着增加。总血细胞水平,与对照组相比,饲喂AMEDs的虾在第15天的透明血细胞和第30天的粒细胞显着增加(p<0.05)。该发现表明粒细胞是时间依赖性诱导的。特别是,在1.5%和2.0%的AMED药物治疗下,副溶血性弧菌攻击虾的存活率显着高于对照组(p<0.05)。弧菌的细菌负荷减少。和副溶血性弧菌明显记录在肝胰腺虾AMEDs1.5%和2.0%,可能与草药特征有关,如抗菌活性,增强先天免疫,和它的潜力,以保持肝胰腺组织的完整性。我们的发现表明,草A提取物可用作商业养殖虾的健康增强剂。
    This study aims to investigate the use of pond apple (Annona glabra) compounds as a novel strategy to prevent and treat acute hepatopancreatic necrosis disease (AHPND) as well as to better understand the mechanism of health improvement in shrimp. The A. glabra leaf extracts were extracted using various solvents and examined for in vitro and in vivo activity against Vibrio parahaemolyticus strains. In comparison with ethanol and water extracts, methanol extract showed the strongest bactericidal effect (MBC/MIC ratio of 2.50 ± 1.00), with minimal inhibitory concentration (MIC) of 0.023 ± 0.012 mg ml-1 and minimum bactericidal concentration (MBC) of 0.065 ± 0.062 mg ml-1. White leg shrimp (P. vannamei, body weight 10.37 ± 0.27 g) fed A. glabra methanol extracts-containing diets (AMEDs) at 1 %, 1.5 %, and 2.0 % demonstrated no deleterious effects on survival and were significantly increased in length and weight after 30 days of feeding. The level of total haemocyte, hyaline haemocyte on day 15 and granulocyte on day 30 remarkably increased (p < 0.05) in shrimps fed AMEDs groups compared to those in the control group. The finding demonstrates that granulocyte was induced time dependently. In particular, the survival rate of V. parahaemolyticus challenged shrimps under medication with AMEDs at 1.5 % and 2.0 % was significantly higher (p < 0.05) than that of the control group. The decrease in bacterial load of Vibrio spp. and V. parahaemolyticus was obviously recorded in hepatopancreas shrimp given AMEDs 1.5 % and 2.0 % and may be linked to herb characteristics such as antibacterial activity, enhancing innate immunity, and its potential to maintain the integrity of hepatopancreatic tissue. Our findings suggest that A. glabra extract might be used as a health enhancer in commercial farmed shrimp.
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  • 文章类型: Journal Article
    所有肾结石病例中大多数为草酸盐尿石症,复发风险很高。除了它的广泛发生,肾结石的特点是并发症严重,治疗费用高。益生菌和草药可能是治疗草酸盐肾结石的治疗干预措施。
    在PubMed/MEDLINE数据库中搜索关键字\"产甲酸草酸杆菌\"和\"草酸盐\"或\"草酸盐降解\"和\"乳杆菌\"或\"双歧杆菌\"或\"重组乳杆菌\"或\"枯草芽孢杆菌\",和“尿石症”和“草药提取物”。搜索返回253个结果,其中38项列入审查。
    大多数降解草酸盐的益生菌属于产草酸杆菌,乳酸菌,双歧杆菌,和芽孢杆菌属,最低剂量为107CFU的胶囊形式,小袋,和冻干粉。培养基中的草酸盐浓度为5-50mM,孵育时间为24小时至14天。大多数研究表明,益生菌补充剂可能有助于减少草酸盐和尿素的尿排泄以及减轻结石形成。不同的草药提取物用于肾结石(由0.5-3%乙二醇诱导)的小鼠模型,减少肾脏炎症和泌尿参数,和草酸钙晶体.
    几种益生菌和草药提取物对肾结石/肾结石具有保护作用,表明它们有希望被视为预防/辅助治疗策略的要素。
    UNASSIGNED: The majority of all kidney stone cases are oxalate urolithiasis with a high risk of recurrence. Beside its widespread occurrence, kidney stones are characterized by severe complications and high treatment costs. Probiotics and herbal medications could be forthcoming therapeutic interventions in the management of oxalate kidney stones.
    UNASSIGNED: The PubMed/MEDLINE database was searched for keywords \"Oxalobacter formigenes\" AND \"Oxalate\" OR \"oxalate degradation\" AND \"Lactobacillus\" OR \"Bifidobacterium\" OR \"recombinant Lactobacillus\" OR \"Bacillus subtilis\", and \"urolithiasis\" AND \"herbal extract\". The search returned 253 results, 38 of which were included in the review.
    UNASSIGNED: Most of the oxalate-degrading probiotics belong to the Oxalobacter formigenes, Lactobacillus, Bifidobacterium, and Bacillus genus with a minimum dosage of 107 CFU in the form of capsules, sachets, and lyophilized powder. Oxalate concentration in media was 5-50mM with an incubation time ranging from 24h to 14 days. The majority of the studies suggested that probiotic supplementation might be useful for reducing urinary excretion of oxalate and urea and alleviation of stone formation. Different herbal extracts were used on murine models of nephrolithiasis (induced by 0.5-3% ethylene glycol) with reduction of renal inflammation and urinary parameters, and calcium oxalate crystals.
    UNASSIGNED: Several strains of probiotics and herbal extracts confer protective effects against kidney stone/nephrolithiasis, indicating their promising nature for being considered as elements of preventive / adjuvant therapeutic strategies.
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  • 文章类型: Journal Article
    双盲,安慰剂对照,随机化,概念验证试验旨在评估VerbasnolTM[地黄叶基提取物(RGLE)]在女性中的疗效和安全性,中度至重度寻常痤疮。
    22名年龄在18至35岁之间的中度至重度痤疮,全球痤疮分级系统(GAGS)评分为19至38的女性被纳入研究,并以1:1的比例随机分配,早餐后口服1粒RGLE胶囊(100mg/天)或安慰剂56天。主要结果是在第56天与安慰剂相比,通过GAGS测量的痤疮严重程度的变化。次要结果是炎性痤疮病变数量的变化,面部皮脂分泌,生活质量,局部疼痛和瘙痒,皮肤皱纹严重程度,和其他皮肤特征,包括辐射,光度,平滑度,纹理,坚定,和水合作用。此外,评估了应答者的百分比以及总体耐受性和疗效.
    在RGLE(n=10)和安慰剂组(n=12)第28天,平均GAGS评分分别降低了21.72%和14.20%,分别,在第56天,两组进一步减少。RGLE组在第56天报告了其他皮肤特征的更好改善。未报告提取物的安全性或耐受性问题。早在补充28天,与安慰剂相比,RGLE减少了女性的痤疮并改善了皮肤质量。
    剂量为100mg/天的RGLE补充剂在56天的剂量给药后,临床上可降低痤疮严重程度,并改善痤疮参与者的皮肤水合作用和生活质量。
    UNASSIGNED: A double-blind, placebo-controlled, randomized, proof-of-concept trial aimed to evaluate the efficacy and safety of VerbasnolTM [Rehmannia glutinosa Libosch leaf-based extract (RGLE)] in females, with moderate to severe acne vulgaris.
    UNASSIGNED: Twenty-two females aged 18 to 35 years having moderate to severe acne with Global Acne Grading System (GAGS) scores of 19 to 38 were included in the study and were randomized in a 1:1 ratio to receive either one capsule (100 mg/day) of RGLE or placebo orally after breakfast for 56 days. The primary outcome was a change in acne severity measured by the GAGS compared to the placebo on day 56. The secondary outcomes were changes in the number of inflammatory acne lesions, facial sebum secretion, quality of life, local pain and itching, skin wrinkle severity, and other skin characteristics, including radiance, luminosity, smoothness, texture, firmness, and hydration. Additionally, the percentage of responders and global tolerability and efficacy were evaluated.
    UNASSIGNED: The mean GAGS score was reduced by 21.72% and 14.20% on day 28 in RGLE (n=10) and placebo groups (n=12), respectively, which further reduced in both groups on day 56. The RGLE group reported better improvement in other skin characteristics on day 56. No safety or tolerability concerns were reported for the extract. RGLE reduced acne and improved the skin quality in females compared to placebo as early as 28 days of supplementation.
    UNASSIGNED: RGLE supplementation at a dose of 100 mg/day has provided a clinically relevant decrease in acne severity and improved the skin hydration and quality of life of the participants with acne after 56 days of dose administration.
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  • 文章类型: Journal Article
    背景:作为中国生产的代表性地方药材,VladimiriaeRadix(VR)已被证明具有保护肝脏和胆汁的作用,在胆汁淤积性肝损伤(CLI)中具有特殊的治疗效果,如VR提取物(VRE)所示。然而,VRE治疗CLI的质量标记(Q标记)尚不清楚.
    目的:提出了一种基于“功效”核心要素的新策略,利用光谱-效应关系的组合,药代动力学,和分子对接方法选择和确认VRE的Q标记。
    方法:首先,研究了10批VRE的HPLC指纹图谱,并测定了大鼠体内抗CLI的药理指标。光谱-效应关系被用作鉴定VRE的Q标记的筛选方法。其次,Q标记用作VRE药代动力学标记,以测量其在正常和CLI大鼠血浆中的浓度,分析他们的性格。最后,利用分子对接来预测已鉴定的Q标记与CLI关键靶标之间的潜在相互作用。
    结果:建立了10批VRE的指纹图谱。大鼠体内药理评价显示VRE对CLI有显著的治疗作用。谱-效应相关分析表明,谷草内酯(COS)和去氢木霉内酯(DEH)是VRE抗CLI的Q标记。药动学结果显示,AUC(0-t),Cmax,CLZ/F,COS和DEH在CLI大鼠中的VZ/F差异有统计学意义(P<0.01)。它们被有效地吸收到CLI大鼠的血浆中,确保理想的生物利用度,并确认它们作为Q标记的作用。分子对接结果表明,COS,DEH与关键靶标(FXR,汽车,PXR,MAPK,TGR5,NRF2)用于CLI处理(结合能<-4.52kcalmol-1),进一步验证了Q标记选择的正确性。
    结论:在这项研究中,通过实验和理论相结合的方法,从药效学表达方面,体内过程规则,和相互作用力预测,阐明了VRE和Q标记(COS,DEH)的治疗效果。此外,成功提出了一种基于“功效”原理的新思想,用于筛选和评估Q标记。
    BACKGROUND: As a representative local medicinal herb produced in China, Vladimiriae Radix (VR) has been proven to exert hepatoprotective and choleretic effects, with particular therapeutic efficacy in cholestatic liver injury (CLI), as demonstrated by the VR extract (VRE). However, the quality markers (Q-markers) of VRE for the treatment of CLI remain unclear.
    OBJECTIVE: A new strategy based on the core element of \"efficacy\" was proposed, using a combination of spectrum-effect relationship, pharmacokinetics, and molecular docking methods to select and confirm Q-markers of VRE.
    METHODS: First, the HPLC fingerprinting of 10 batches of VRE was studied, and the in vivo pharmacological index of anti-CLI in rats was determined. The spectrum-effect relationship was utilized as a screening method to identify the Q-markers of VRE. Secondly, Q-markers were used as VRE pharmacokinetic markers to measure their concentrations in normal and CLI rat plasma, and to analyze their disposition. Finally, molecular docking was utilized to predict the potential interaction between the identified Q-markers and crucial targets of CLI.
    RESULTS: The fingerprints of 10 batches of VRE was established. The in vivo pharmacological evaluation of rats showed that VRE had a significant therapeutic effect on CLI. The spectrum-effect correlation analysis showed that costunolide (COS) and dehydrocostus lactone (DEH) were the Q-markers of VRE anti-CLI. The pharmacokinetic results showed that AUC(0-t), Cmax, CLZ/F, and VZ/F of COS and DEH in CLI rats had significant differences (P < 0.01). They were effectively absorbed into the blood plasma of CLI rats, ensuring ideal bioavailability, and confirming their role as Q-markers. Molecular docking results showed that COS, DEH had good affinity with key targets (FXR, CAR, PXR, MAPK, TGR5, NRF2) for CLI treatment (Binding energy < -4.52 kcal mol-1), further verifying the correctness of Q-marker selection.
    CONCLUSIONS: In this study, through the combination of experimental and theoretical approaches from the aspects of pharmacodynamic expression, in vivo process rules, and interaction force prediction, the therapeutic effect of VRE and Q-markers (COS、DEH) were elucidated. Furthermore, a new idea based on the principle of \"efficacy\" was successfully proposed for screening and evaluating Q-markers.
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  • 文章类型: Journal Article
    cimicifugaraceemosa提取物(CREs)已获得公认的用于治疗更年期症状,例如潮热和出汗过多,和体重增加。虽然CREs的临床效果已经得到了很好的证明,这些影响的潜在机制在很大程度上是未知的。最近,在体外培养细胞和体内肥胖小鼠模型中证明了CREZe450的代谢作用。在分子水平上,代谢调节,增强胰岛素敏感性,葡萄糖摄取的增加与AMP激活的蛋白激酶(AMPK)的激活有关。因此,我们测试了Ze450对AMPK磷酸化的影响,从而在来自不同组织的细胞中激活,即,鼠C2C12成肌细胞,人HEPG2肝细胞,小鼠HT22神经元细胞,和鼠3T3L1脂肪细胞。使用基于FRET的HTRF测定,我们发现,Ze450诱导AMPK磷酸化和激活的这种关键酶的代谢调节在细胞从各种不同的组织,包括C2C12(肌肉),HEPG2(肝脏),HT22(海马),和3T3-L1(脂肪细胞)细胞。在C2C12肌肉细胞中,AMPK激活增强伴随着线粒体呼吸减少和葡萄糖摄取增强.Further,Ze450增强了细胞抵抗铁凋亡诱导剂erastin或RSL3诱导的氧化死亡的弹性。我们的发现表明,消旋升麻对不同组织和跨物种的AMPK活化具有一般作用。这可能对Ze450的扩展治疗应用具有显著影响,因为AMPK激活和相关的代谢作用先前已经与抗衰老作用和代谢综合征的预防相关联。
    Cimicifuga racemosa extracts (CREs) have gained well-established use for the treatment of menopausal symptoms such as hot flushes and excessive sweating, and weight gain. While the clinical effects of CREs have been well documented, the mechanisms underlying these effects are largely unknown. More recently, the metabolic effects of the CRE Ze 450 were demonstrated in cultured cells in vitro and in mouse models of obesity in vivo. At the molecular level, metabolic regulation, enhanced insulin sensitivity, and increased glucose uptake were linked to the activation of AMP-activated protein kinase (AMPK). Therefore, we tested the effects of Ze 450 on AMPK phosphorylation and thus activation in cells from different tissues, i.e., murine C2C12 myoblast cells, human HEPG2 liver cells, mouse HT22 neuronal cells, and in murine 3T3L1 adipocytes. Using a FRET-based HTRF-assay, we found that Ze 450 induced AMPK phosphorylation and the activation of this key enzyme of metabolic regulation in cells from various different tissues including C2C12 (muscle), HEPG2 (liver), HT22 (hippocampal), and 3T3-L1 (adipocyte) cells. In C2C12 muscle cells, enhanced AMPK activation was accompanied by reduced mitochondrial respiration and enhanced glucose uptake. Further, Ze 450 enhanced the resilience of the cells against oxidative death induced by ferroptosis inducers erastin or RSL3. Our findings suggest a general effect of Cimicifuga racemosa on AMPK activation in different tissues and across species. This may have a significant impact on expanded therapeutic applications of Ze 450, since AMPK activation and the related metabolic effects have been previously associated with anti-aging effects and the prevention of the metabolic syndrome.
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