Asperuloside
(Synonyms: 车叶草苷) 目录号 : GC35411
An iridoid glycoside with diverse biological activities
Cas No.:14259-45-1
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.50%
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Asperuloside is an iridoid glycoside that has been found in G. tunetanum and has diverse biological activities, including anti-angiogenic, anti-inflammatory, and anti-obesity properties.1,2,3 It reduces microvessel formation by 67% in a chick embryo chorioallantoic membrane assay when used at a concentration of 2 μg/egg.1 Asperuloside (20, 40, and 80 mg/L) inhibits LPS-induced increases in TNF-α, IL-1β, and IL-6 production in RAW 264.7 macrophages in a concentration-dependent manner.2 It reduces lung myeloperoxidase (MPO) activity and bronchoalveolar lavage fluid (BALF) levels of TNF-α, IL-1β, and IL-6 in a mouse model of LPS-induced acute lung injury when administered at doses of 20, 40, and 80 mg/kg. Dietary administration of asperuloside decreases body weight gain, white adipose tissue (WAT) weight, and the ratio of WAT weight to body weight in a high-fat diet-induced mouse model of metabolic syndrome.3
1.Camero, C.M., Germanò, M.P., Rapisarda, A., et al.Anti-angiogenic activity of iridoids from Galium tunetanumBraz. J. Pharmacognosy28(3)374-377(2018) 2.Qiu, J., Chi, G., Wu, Q., et al.Pretreatment with the compound asperuloside decreases acute lung injury via inhibiting MAPK and NF-κB signaling in a murine modelInt. Immunopharmacol.31109-115(2016) 3.Hirata, T., Kobayashi, T., Wada, A., et al.Anti-obesity compounds in green leaves of Eucommia ulmoidesBioorg. Med. Chem. Lett.21(6)1786-1791(2011)
| Cas No. | 14259-45-1 | SDF | |
| 别名 | 车叶草苷 | ||
| Canonical SMILES | O=C1O[C@]2([H])[C@@]3([H])[C@](C(COC(C)=O)=C2)([H])[C@H](O[C@H]4[C@@H]([C@H]([C@@H]([C@@H](CO)O4)O)O)O)OC=C13 | ||
| 分子式 | C18H22O11 | 分子量 | 414.36 |
| 溶解度 | DMF: 5mg/mL,DMSO: 5mg/mL,Ethanol: 2mg/mL,PBS (pH 7.2): 3mg/mL | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4134 mL | 12.0668 mL | 24.1336 mL |
| 5 mM | 0.4827 mL | 2.4134 mL | 4.8267 mL |
| 10 mM | 0.2413 mL | 1.2067 mL | 2.4134 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Asperuloside inhibited epithelial-mesenchymal transition in colitis associated cancer via activation of vitamin D receptor
Phytomedicine 2022 Jul;101:154070.PMID:35523114DOI:10.1016/j.phymed.2022.154070.
Background: Asperuloside is a natural compound extracted from various herbs with several bioactivities. Its effects on anti-inflammation and anti-tumor indicated that Asperuloside might prevent colorectal cancer developing from inflammatory bowel diseases (IBD). But there were few reports about the efficacy and mechanism of Asperuloside on improving colorectal cancer. It has been reported that vitamin D receptor (VDR) could regulate the expression of SMAD3. In previous study, Asperuloside could significantly improve the expression of VDR and reduced Smad3 mRNA in IEC-6 cell. Purpose: The present study was aimed to investigate the potential mechanism of Asperuloside on inhibiting epithelial-mesenchymal transition (EMT) in colitis associated cancer. Study design: First, in LPS-injured IEC-6 cell, Asperuloside inhibited phosphorylated p65 (p-p65) level, improved VDR expression and reduced Smad3 mRNA. Second, we wonder the relationship between VDR signaling and nucleus factor-kappaB (NF-κB) signaling during Asperuloside on reducing Smad3 mRNA. And then, the effect of Asperuloside on inhibiting EMT development through VDR/Smad3 was investigated. Finally, we testified the effect of Asperuloside on protecting against colitis associated cancer (CAC) by inhibiting EMT development through VDR/Smad3. Methods: Pyrrolidinedithiocarbamate ammonium (PDTC) was used for established NF-κB-inhibited IEC-6 cell. This cell was applied for investigating the relationship between NF-κB and VDR of Asperuloside on inhibiting Smad3. VDR-inhibited cell was established by small interfering RNA (siRNA) of VDR and was employed to investigate the role of VDR for Asperuloside on decreasing Smad3. Transforming growth factor β1 (TGFβ1) was used for inducing EMT/fibrosis in IEC-6 cell. TGFβ1-stimulated cell was used for testifying the effect of Asperuloside on inhibiting EMT development. AOM/DSS-induced CAC was established to investigate the effect of Asperuloside on suppressing cancer development. Results: Asperuloside inhibited the level of p-p65 which was up-regulated by LPS. Asperuloside could up-regulate VDR signaling and reduce Smad3 mRNA in NF-κB-knockdown IEC-6 cells. Asperuloside failed to reduce Smad3 mRNA due to VDR knockdown, which implied that Asperuloside might down-regulate Smad3 mRNA dependently on activation of VDR signaling and independently on inhibiting NF-κB signaling. Asperuloside exhibited significant prevention of EMT development in TGFβ1-induced IEC-6 cell (EMT cell) and mice CAC. Asperuloside reduced the transform of epithelial phenotype into motile mesenchymal phenotype in EMT cell along with decreasing levels of EMT markers by inhibiting Smad3 mRNA via activation of VDR. In mice with CAC, expression of VDR in colon was improved by Asperuloside. Symptoms of colitis, tumor number and tumor size were significantly inhibited by Asperuloside. Suppressed EMT development was determined by reduced α-SMA expression and decreased mRNAs of several EMT markers. Conclusion: Asperuloside might prevent CAC through inhibiting EMT development via regulation of VDR/Smad3 pathway.
Asperuloside suppressing oxidative stress and inflammation in DSS-induced chronic colitis and RAW 264.7 macrophages via Nrf2/HO-1 and NF-κB pathways
Chem Biol Interact 2021 Aug 1;344:109512.PMID:33974900DOI:10.1016/j.cbi.2021.109512.
Background: Inflammatory bowel diseases (IBDs), which mainly include Crohn's disease (CD) and ulcerative colitis (UC), are chronic idiopathic inflammatory disease of the gastrointestinal tract for which effective pharmacological treatments are lacking or options are very limited. Purpose: Here, we aim to investigate the therapeutic effects of an iridoid glycoside, Asperuloside (ASP) on mice experimental chronic colitis induced by dextran sulfate sodium (DSS) and further explore underlying mechanisms in vitro and in vivo. Methods: LPS-treated RAW 264.7 cells showed inflammation and were assessed for various physiological, morphological and biochemical parameters in the absence or presence of ASP. Chronic colitis was induced by 2% DSS in mice, which were used as an animal model to explore the pharmacodynamics of ASP. We detected p65 and Nrf2 pathway proteins via Western blot and RT-PCR analysis, assessed the cytokines TNF-α and IL-6 via ELISA, tested p65 and Nrf2 nuclear translocation via fluorescence. In addition, the docking affinity of ASP and p65 or Nrf2 proteins in the MOE 2015 software. Results: We found that ASP attenuated weight loss, disease activity index (DAI) and colonic pathological damage in colitis mice and restored the expressions of inflammatory cytokines in the colon. In addition, ASP restored antioxidant capacity in DSS-induced chronic colitis mice and lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Furthermore, ASP suppressed oxidative stress through increasing Nrf2, HO-1 and NQO-1 proteins expressions, and down-regulated nuclear levels of p65 to inhibit DSS-induced colonic oxidative stress and inflammation. Validation of the molecular docking results also indicated that ASP interacts with Nrf2 or p65 proteins. In summary, ASP improved DSS-induced chronic colitis by alleviating inflammation and oxidative stress, activating Nrf2/HO-1 signaling and limiting NF-κB signaling pathway, which may be an effective candidate for the treatment of IBD.
Asperuloside Enhances Taste Perception and Prevents Weight Gain in High-Fat Fed Mice
Front Endocrinol (Lausanne) 2021 Apr 13;12:615446.PMID:33927690DOI:10.3389/fendo.2021.615446.
Asperuloside is an iridoid glycoside found in many medicinal plants that has produced promising anti-obesity results in animal models. In previous studies, three months of Asperuloside administration reduced food intake, body weight, and adipose masses in rats consuming a high fat diet (HFD). However, the mechanisms by which Asperuloside exerts its anti-obesity properties were not clarified. Here, we investigated homeostatic and nutrient-sensing mechanisms regulating food intake in mice consuming HFD. We confirmed the anti-obesity properties of Asperuloside and, importantly, we identified some mechanisms that could be responsible for its therapeutic effect. Asperuloside reduced body weight and food intake in mice consuming HFD by 10.5 and 12.8% respectively, with no effect on mice eating a standard chow diet. Fasting glucose and plasma insulin were also significantly reduced. Mechanistically, Asperuloside significantly reduced hypothalamic mRNA ghrelin, leptin, and pro-opiomelanocortin in mice consuming HFD. The expression of fat lingual receptors (CD36, FFAR1-4), CB1R and sweet lingual receptors (TAS1R2-3) was increased almost 2-fold by the administration of Asperuloside. Our findings suggest that Asperuloside might exert its therapeutic effects by altering nutrient-sensing receptors in the oral cavity as well as hypothalamic receptors involved in food intake when mice are exposed to obesogenic diets. This signaling pathway is known to influence the subtle hypothalamic equilibrium between energy homeostasis and reward-induced overeating responses. The present pre-clinical study demonstrated that targeting the gustatory system through Asperuloside administration could represent a promising and effective new anti-obesity strategy.
Asperuloside Prevents Peri-Implantitis via Suppression of NF-κB and ERK1/2 on Rats
Pharmaceuticals (Basel) 2022 Aug 20;15(8):1027.PMID:36015175DOI:10.3390/ph15081027.
Peri-implantitis is characterized by inflammatory cell infiltration and hyperactivation of the osteoclasts surrounding dental implants which can result in bone resorption and ultimately implant failure. Therefore, coordinating the activity of inflammatory response and bone-resorbing osteoclasts is crucial for the prevention of peri-implantitis. Asperuloside (ASP), an iridoid glycoside, has significant anti-inflammatory activities, suggesting the great potential in attenuating peri-implantitis bone resorption. A ligature-induced peri-implantitis model in the maxilla of rats was established, and the effects of ASP on preventing peri-implantitis were evaluated after four weeks of ligation using micro-CT and histological staining. RT-PCR, western blotting, tartrate-resistant acid phosphatase (TRAP), and immunofluorescent staining were conducted on osteoclasts to confirm the mechanisms of ASP on osteoclastogenesis. The results show that ASP could lead to attenuation of alveolar bone resorption in peri-implantitis by inhibiting osteoclast formation and decreasing pro-inflammatory cytokine levels in vivo. Furthermore, ASP could inhibit osteoclastogenesis by downregulating expression levels of transcription factors nuclear factor of activated T-cell (NFATc1) via restraining the activations of nuclear factor kappa beta (NF-κB) and the phosphorylation of extracellular signal-related kinase 1/2 (ERK1/2). In conclusion, ASP could significantly attenuate bone resorption in peri-implantitis via inhibition of osteoclastogenesis by suppressing NF-κB and ERK1/2 signaling pathways activations.
Emerging therapeutic potential of the iridoid molecule, Asperuloside: A snapshot of its underlying molecular mechanisms
Chem Biol Interact 2020 Jan 5;315:108911.PMID:31786185DOI:10.1016/j.cbi.2019.108911.
Over the years, the attention of researchers in the field of modern drug discovery and development has become further intense on the identification of active compounds from plant sources and traditional remedies, as they exhibit higher therapeutic efficacies and improved toxicological profiles. Among the large diversity of plant extracts that have been discovered and explored for their potential therapeutic benefits, Asperuloside, an iridoid glycoside, has been proven to provide promising effects as a therapeutic agent for several diseases. Although, this potent substance exists in several genera, it is primarily found in plants belonging to the genus Eucommia. Recent decades have seen a surge in the research on Asperuloside, making it one of the most studied natural products in the field of medicine and pharmacology. In this review, we have attempted to study the various reported mechanisms of Asperuloside that form the basis of its wide spectrum of pharmacological activities.