Valepotriates

  • 文章类型: Journal Article
    药用植物是药学上重要的化合物的丰富来源,自古以来就被用于治疗各种疾病。Valerianajatamansi琼斯,也被称为印度缬草,在温带的喜马拉雅药用植物中占有特殊地位,并以其治疗各种疾病的治疗特性而闻名。V.jatamansi的治疗潜力归因于有价值的化合物,如戊酸盐的存在,倍半萜,戊酸类,jatamanins,木脂素,cryptomeridiol,maaliol,黄刺醇,以及在根茎和根中发现的广藿香醇。这项研究采用了各种治疗方法,包括通过接种真菌真菌来培养V.jatamansi,F.收缩,和丛枝菌根真菌(AMF)的财团,为了研究它们对生物质生产的影响,叶绿素含量,以及V.jatamansi中生物活性化合物的积累。结果显示在接种的植物中这些参数的显著改善。接种F.mosseae的植物参数最高,其次是接种F.strictus和AMFs混合物的植物。这项研究不仅强调了天然AMF促进V.jatamansi生长的潜力,而且阐明了它们在影响生物活性化合物合成中的作用。用本地AMF种植V.jatamansi已成为一种可持续和生态友好的方法,提供了双重好处,提高了这种有价值的植物的药用和经济价值。这项研究为菌根协会在药用植物种植中的实际应用提供了宝贵的见解,连接农业和制药领域。
    Medicinal plants are rich sources of pharmaceutically important compounds and have been utilized for the treatment of various diseases since ancient times. Valeriana jatamansi Jones, also known as Indian valerian, holds a special place among temperate Himalayan medicinal plants and is renowned for its therapeutic properties in addressing a variety of ailments. The therapeutic potential of V. jatamansi is attributed to the presence of valuable compounds such as valepotriates, sesquiterpenoids, valeriananoids, jatamanins, lignans, cryptomeridiol, maaliol, xanthorrhizzol, and patchouli alcohol found in its rhizome and roots. This study employed various treatments, including the cultivation of V. jatamansi with the inoculation of Funneliformis mosseae, F. constrictus, and a consortium of arbuscular mycorrhizal fungi (AMF), to investigate their influence on biomass production, chlorophyll content, and the accumulation of bioactive compounds in V. jatamansi. The results revealed significant improvement in these parameters in the inoculated plants. The parameters of plants inoculated with F. mosseae were the highest, followed by those of plants inoculated with F. constrictus and a mixture of AMFs. This study not only underscores the potential of native AMF for promoting the growth of V. jatamansi but also elucidates their role in influencing the synthesis of bioactive compounds. The cultivation of V. jatamansi with native AMF has emerged as a sustainable and eco-friendly approach, providing the dual benefit of enhancing both the medicinal and economic value of this valuable plant. This research contributes valuable insights into the practical application of mycorrhizal associations for the cultivation of medicinal plants, bridging the realms of agriculture and pharmaceuticals.
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  • 文章类型: Journal Article
    ValerianajatamansiJones是一种常用的中药,拥有丰富的有效组合物,具有多功能的化学结构和广泛的极性,包括环烯醚萜类,绿原酸,和类黄酮.先前的报道表明,传统的高效液相色谱(HPLC)分析方法已证明在全面表征Valerianajatamansi中的成分方面表现不佳。在本研究中,已建立并验证了将超临界流体萃取与常规HPLC分离(反相)和超临界流体色谱(正相)相结合的混合在线分析平台。该系统可以提供具有两种不同色谱分离模式的在线提取,以提高分离能力,并已连接到质谱仪以获取高分辨率质谱数据。然后,将该在线平台应用于Valerianajatamansi中的成分筛选.共鉴定出117种化合物,包括五种木脂素类,18种有机酸,六种类黄酮,和88个环烯醚萜类。首次从Valerianajatamansi中报道了33个化合物。这些结果丰富了我们对Valerianajatamansi组件的理解,并证明了本研究中开发的在线平台是一种可靠的方法,可加快全面分析复杂样品的工作效率。
    Valeriana jatamansi Jones is a commonly used traditional Chinese medicine, boasting rich effective compositions with versatile chemical structures and wide polarity, including iridoids, chlorogenic acid, and flavonoids. Previous reports indicate that conventional high-performance liquid chromatography (HPLC) analytical methods have proven inefficient performance in comprehensively characterizing components in Valeriana jatamansi. In the present study, a hybrid online analytical platform combining supercritical fluid extraction with both conventional HPLC separation (reverse phase) and supercritical fluid chromatography (normal phase) has been established and validated. This system can provide online extraction with two different chromatographic separation modes to increase separation ability and has been connected to a mass spectrometer to acquire high-resolution mass spectrometry data. Then, the online platform was applied to screening components in Valeriana jatamansi. A total of 117 compounds were identified, including five lignans, 18 organic acids, six flavonoids, and 88 iridoids. Thirty-three compounds were reported from Valeriana jatamansi for the first time. These results enrich our understanding of the components of Valeriana jatamansi and prove that the developed online platform in this study is a robust approach for accelerating working efficiency in comprehensively analyzing complicated samples.
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  • 文章类型: Journal Article
    UNASSIGNED:缬草提取物胶囊(VEC)是一种有效的中成药,用于胃肠道(GI)疾病。
    未经批准:研究VEC在胃肠道疾病中临床作用的详细药理活性。
    UnASSIGNED:Sprague-Dawley大鼠分为六组:对照组,模型,和药物治疗(VEC-L,VEC-M,VEC-H,和teprenone)。连续3天口服给予大鼠VEC(124、248、496mg/kg)和替普瑞酮(21.43mg/kg)。1小时后,五组(对照组除外)口服乙醇(10mL/kg)1h或吲哚美辛(80mg/kg)7h。进行VEC(0.01-1mg/mL)对ACh/BaCl2诱导的新西兰兔平滑肌收缩的痉挛活性。C57BL/6小鼠碳推进试验评估了VEC(248-992mg/kg)对正常和新斯的明/肾上腺素诱导的小鼠肠运动的影响。
    UNASSIGNED:与模型组相比,VEC治疗降低了胃部病变指数和粘膜损伤。进一步的实验表明,VEC的病理改善作用伴随着酶促抗氧化系统和细胞保护标记的增强(COX-1,p<0.01;PGI2p<0.05;),随着MPO水平的减轻(乙醇:15.56±0.82vs.12.15±2.60,p<0.01;吲哚美辛:9.65±3.06vs.6.36±2.43,p<0.05),MDA(乙醇:1.66±0.44vs.0.81±0.58,p<0.01;吲哚美辛:1.71±0.87vs.1.09±0.43,p<0.05),和炎症介质。VEC降低了ACh/BaCl2诱导的高音调,并促进了正常和新斯的明/肾上腺素诱导的小鼠的肠道运输。
    未经授权:VEC显示出潜在的胃保护作用,表明VEC是治疗胃肠道疾病的有前途的植物药。
    UNASSIGNED: Valerian extract capsule (VEC) is an effective Chinese patent medicine used for gastrointestinal (GI) diseases.
    UNASSIGNED: To investigate the detailed pharmacological activity for VEC clinical effects in GI diseases.
    UNASSIGNED: Sprague-Dawley rats were divided into six groups: control, model, and drug-treated (VEC-L, VEC-M, VEC-H, and teprenone). Rats were orally administered VEC (124, 248, 496 mg/kg) and teprenone (21.43 mg/kg) for 3 consecutive days. After 1 h, the five groups (except the control group) were orally given ethanol (10 mL/kg) for 1 h or indomethacin (80 mg/kg) for 7 h. The spasmolytic activity of VEC (0.01-1 mg/mL) on ACh/BaCl2-induced New Zealand rabbit smooth muscle contraction was performed. The C57BL/6 mice carbon propelling test evaluated the effects of VEC (248-992 mg/kg) on intestinal motility in normal and neostigmine/adrenaline-induced mice.
    UNASSIGNED: Compared with the model group, VEC treatment reduced the gastric lesion index and mucosal damage. Further experiments showed that the pathological ameliorative effect of VEC was accompanied by augmentation of the enzymatic antioxidant system and cytoprotective marker (COX-1, p < 0.01; PGI2 p < 0.05;), along with the alleviation of the levels of MPO (ethanol: 15.56 ± 0.82 vs. 12.15 ± 2.60, p < 0.01; indomethacin: 9.65 ± 3.06 vs. 6.36 ± 2.43, p < 0.05), MDA (ethanol: 1.66 ± 0.44 vs. 0.81 ± 0.58, p < 0.01; indomethacin: 1.71 ± 0.87 vs. 1.09 ± 0.43, p < 0.05), and inflammatory mediators. VEC decreased the high tone induced by ACh/BaCl2 and promoted intestinal transit in normal and neostigmine/adrenaline-induced mice.
    UNASSIGNED: VEC showed a potential gastroprotective effect, suggesting that VEC is a promising phytomedicine for the treatment of GI diseases.
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  • 文章类型: Journal Article
    Considering chemical complexity of plant crude extracts, purification of natural products is a rate limiting process to identify new compounds as well as to obtain standard references for quantitative or qualitative purposes. In the present work, a centrifugal partition chromatography (CPC) method was developed to isolate and produce high quality reference standards of valtrate and 7-homovaltrate from Centranthus ruber L. roots. These two compounds are controversial aglycon iridioids regulated by the legislation on plant-based dietary supplements. A new biphasic solvent system suitable for CPC separation of valepotriates was developed. It was composed of methanol/hexane/water (5/5/0.8, v/v/v). It yielded a partition coefficient near 1 and a theoretical selectivity of 1.3 between both targeted compounds. Optimization of CPC experimental parameters at the analytical scale (50 mL- and 100 mL-column capacity) enabled compounds\' separation with a flow rate of 8 mL/min at 2500 rpm. Then a scale up from a 100 mL-column capacity to a 1000 mL-column capacity has been studied using the \"free-space between peaks\" concept. It allowed an injected quantity 16 times higher in comparison to the maximal loading capacity of the 100 mL-column. Both valtrate and 7-homovaltrate were recovered in one single step with a purity over 97%. Further MS and NMR characterization allowed to confirm unambiguously the compounds\' structures. The highly efficient CPC separation developed in this work provides valepotriates in amounts suitable for further study and strong bases for future industrial development.
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  • 文章类型: Journal Article
    Valeriana jatamansi Jones is an important medicinal plant and its quality is closely related to its region of origin. In the current study, we utilized a flexible and powerful strategy for comprehensive evaluation of the quality diversity for 15 regions in China. The method was based on a hybrid linear ion trap-Orbitrap mass spectrometry platform. For structure characterization, fragmentation patterns were detected by analyzing a series of standard compounds using data dependent multistage mass spectrometry acquisition. A fragment ion database for valepotriates was established, and the acquired data were high throughput filtered by fragment ion search for compound identification. For quantitative purposes, we normalized the mass spectrometry data of 15 samples using SIEVE 2.0 and the differences in composition were analyzed using principal component analysis combined with hierarchical clustering analysis. The results identified a total of 92 compounds from Valeriana jatamansi Jones. Samples from Dali, Kunming, and Baoshan have better qualities and concentrations of the main active constituents. To verify our strategy, we compared the valtrate, acevaltrate, and baldrinal contents using high-performance liquid chromatography with diode array detector. We developed and validated a comprehensive qualitative and quantitative analytical method to achieve quality control of Valeriana jatamansi Jones.
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  • 文章类型: Journal Article
    Three new minor valepotriate isomers, jatamanvaltrates Z1 (1), Z2 (2), and Z3 (3), have been isolated from the whole plants of Valeriana jatamansi (syn. Valeriana wallichii.). Their structures were elucidated by extensive spectroscopic analysis, especially 2D NMR and ESI-MS/MSn. All isolated compounds displayed moderate cytotoxicity against the lung adenocarcinoma (A549), metastatic prostate cancer (PC-3 M), colon cancer (HCT-8), and hepatoma (Bel7402) cell lines with IC50 values of 2.8-8.3 μM.
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  • 文章类型: Journal Article
    Valepotriates, plant secondary metabolites of the family Valerianaceae, contain various acyloxy group linkages to the valepotriate nucleus and exhibit significant biological activities. Identification of valepotriates is important to uncover potential lead compounds for the development of new sedative and antitumor drugs. However, making their structure elucidation by nuclear magnetic resonance (NMR) experiments is too difficult to be realized because of the overlapped carbonyl carbon signals of acyloxy groups substituted at different positions. Thus, the mass spectrometric profiling of these compounds in positive ion mode was developed to unveil the exact linkage of acyloxy group and the core of valepotriate. In this study, electrospray ionization tandem multistage mass spectrometry (ESI-MS/MS(n)) in ion trap and collision-induced dissociation tandem MS were used to investigate the fragmentation pathways of four types of valepotriates in Valeriana jatamansi, including 5-hydroxy-5,6-dihydrovaltrate hydrin (5-hydroxy-5,6-dihydrovaltrate chlorohydrin), 5,6-dihydrovaltrate hydrin (5,6-dihydrovaltrate chlorohydrin), 5-hydroxy-5,6-dihydrovaltrate and valtrate hydrin (valtrate chlorohydrin). The high-resolution mass spectrum (HRMS) data of all the investigated valepotriates from quadrupole time-of-flight MS/MS were used as a supportive of the fragmentation rules we hypothesized from ion-trap stepwise MS(n). As a result, the loss sequence of acyloxy groups and the abundance of key product ions, in combination with the characteristic product ions corresponding to the valepotriate nucleus, could readily differentiate the four different types of valepotriates. The summarized fragmentation rules were also successfully exploited for the structural characterization of three new trace valepotriates from V. jatamansi. The results indicated that the developed analytical method could be employed as a rapid, effective technique for structural characterization of valepotriates, especially for the trace compounds that could not be identified by NMR techniques. This study may also arouse interest for further structural analysis of other valepotriate-containing type herbal medicines.
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  • 文章类型: Journal Article
    Three new decomposition products of valepotriates, valtrals A-C (1-3), and two known products, baldrinal and homobaldrinal, are formed during the isolation procedure of the ethanol extract of the whole plants of Valeriana jatamansi. Their structures were determined by spectroscopic methods including IR, MS, 1D, and 2D NMR experiments. Compounds 1-3 showed selective cytotoxicity against metastatic prostate cancer (PC-3M) and colon cancer (HCT-8) cell lines.
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  • 文章类型: Journal Article
    OBJECTIVE: Combinations of different classes of antidepressants (including herbal adjuvants) have been used as an alternative means of achieving better results in the treatment of depressed patients. However, studies characterizing the interactions between herbal adjuvants and antidepressants are lacking. This study is the first to investigate the interaction between diene valepotriates (VAL) from Valeriana glechomifolia, a species with antidepressant-like effects, and imipramine (IMI), desipramine (DESI) and bupropion (BUP). The interactions were assessed via isobolographic analyses, which represent a tool for evaluating interactions between drugs.
    METHODS: The interaction between VAL and each antidepressant was evaluated in mice given concurrent oral administration of each drug with fixed ED50 ratios and subjected to a forced swimming test (FST). Spontaneous locomotion was measured in the open field test.
    RESULTS: The drug combinations produced a dose-dependent anti-immobility effect in the FST without altering mouse locomotor activity. Isobolographic analysis revealed that VAL resulted in synergistic interactions in combination with each of the antidepressants tested.
    CONCLUSIONS: The synergistic interactions between VAL and IMI, DESI and BUP highlight the potential for VAL to serve as adjuvants to antidepressant drugs and suggest that VAL does not directly target the same sites on neuronal transporters as the antidepressants.
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