Norathyriol
(Synonyms: Mangiferitin) 目录号 : GC67983Norathyriol (Mangiferitin) 是芒果苷的天然代谢物。 Norathyriol 以非竞争性方式抑制 α-葡萄糖苷酶 (α-glucosidase )，IC50 为 3.12 μM。Norathyriol 还抑制 PPARα、PPARβ 和 PPARγ，IC50 分别为 92.8 µM、102.4 µM 和 153.5 µM。具有抗氧化、抗癌、抗菌、抗炎、抗菌活性。
Cas No.:3542-72-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM[1]. Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively[2]. Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
Norathyriol (1-25 µM) inhibits growth by inducing cell cycle arrest in JB6 P+ cells. Norathyriol inhibits JB6 cell growth by inducing G2-M arrest[3].
Norathyriol suppresses UVB-induced phosphorylation of ERKs, AP-1 and NF-κB activation in JB6 P+ cells[3]Cell Growth Assay WB
Cell Viability Assay[3]
| Cell Line: | Mouse skin epidermal JB6 P+ cells |
| Concentration: | 0, 1, 10, or 25 µM |
| Incubation Time: | 24 or 72 hours |
| Result: | Inhibited cell growth in a dose- as well as time-dependent manner but does not cause cell death. |
Western Blot Analysis[3]
| Cell Line: | JB6 P+ cells |
| Concentration: | 0, 1, 10, or 25 µM |
| Incubation Time: | 2 hours |
| Result: | Inhibited UVB-induced phosphorylation of ERKs and p90RSK. |
Norathyriol is a natural metabolite of Mangifera in the human intestine with the oral availability and safety[1].
Norathyriol (0.92, 1.85 and 3.7 mg/kg) dose dependently decreased the serum urate levels by 27.0, 33.6 and 37.4%, respectively[4].
| Animal Model: | Adult Kunming mice weighing 18-22 g[4] |
| Dosage: | 0.92, 1.85 and 3.7 mg/kg |
| Administration: | Administered intragastrically; twice daily for five times |
| Result: | The serum uric acid levels were decreased by 27.0%, 33.6% and 37.4%. |
[1]. Zhi-Long Shi, et al. In Vitro and In Vivo Effects of Norathyriol and Mangiferin on α-Glucosidase. Biochem Res Int. 2017;2017:1206015.
[2]. Ashley S Wilkinson,et al. Effects of the mango components mangiferin and quercetin and the putative mangiferin metabolite norathyriol on the transactivation of peroxisome proliferator-activated receptor isoforms. J Agric Food Chem. 2008 May 14;56(9):3037-
[3]. Jixia Li, et al. Norathyriol suppresses skin cancers induced by solar ultraviolet radiation by targeting ERK kinases. Cancer Res. 2012 Jan 1;72(1):260-70.
[4]. Yanfen Niu, et al. Hypouricaemic action of mangiferin results from metabolite norathyriol via inhibiting xanthine oxidase activity. Pharm Biol. 2016 Sep;54(9):1680-6.
| Cas No. | 3542-72-1 | SDF | Download SDF |
| 别名 | Mangiferitin | ||
| 分子式 | C13H8O6 | 分子量 | 260.2 |
| 溶解度 | DMSO : 100 mg/mL (384.32 mM; Need ultrasonic) | 储存条件 | Store at -20°C, away from moisture |
| 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 | 3.8432 mL | 19.216 mL | 38.432 mL |
| 5 mM | 0.7686 mL | 3.8432 mL | 7.6864 mL |
| 10 mM | 0.3843 mL | 1.9216 mL | 3.8432 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
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。
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In Vitro and In Vivo Effects of Norathyriol and Mangiferin on α-Glucosidase
Biochem Res Int 2017;2017:1206015.PMID:28168055DOI:10.1155/2017/1206015.
Norathyriol is a metabolite of mangiferin. Mangiferin has been reported to inhibit α-glucosidase. To the best of our knowledge, no study has been conducted to determine or compare those two compounds on inhibiting α-glucosidase in vitro and in vivo by far. In this study, we determined the inhibitory activity of Norathyriol and mangiferin on α-glucosidase in vitro and evaluated their antidiabetic effect in diabetic mice. The results showed that Norathyriol inhibited α-glucosidase in a noncompetitive manner with an IC50 value of 3.12 μM, which is more potent than mangiferin (IC50 = 358.54 μM) and positive drug acarbose (IC50 = 479.2 μM) in the zymological experiment. Both of Norathyriol and mangiferin caused significant (p < 0.05) reduction in fasting blood glucose and the blood glucose levels at two hours after carbohydrate loading and it was interesting that mangiferin and Norathyriol can make the decline of the blood glucose earlier than other groups ever including normal group in the starch tolerance test. However, Norathyriol and mangiferin did not significantly influence carbohydrate absorption in the glucose tolerance test. Therefore, the antidiabetic effects of Norathyriol and mangiferin might be associated with α-glucosidase, and Norathyriol was more potent than mangiferin.
Norathyriol suppresses transformation in JB6 P+ cells by the inhibition of Akt
J Cancer Res Ther 2012 Oct-Dec;8(4):561-4.PMID:23361275DOI:10.4103/0973-1482.106537.
Context: Chemoprevention has been acknowledged as an important and practical strategy for the management of skin cancer. Norathyriol, a naturally occurring compound present in various plants, has a potent anticancer-promoting activity. Aims: The aim was to investigate the chemopreventive activity of Norathyriol on JB6 P+ cells. Materials and methods: A soft agar assay was used to detect the effect of Norathyriol on cell transformation. The activator protein-1 (AP-1) transactivation activity was examined by the luciferase assay. Results: Norathyriol inhibited epidermal growth factor (EGF)- and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced neoplastic cell transformation in a dose-dependent manner. The activation of activator protein-1 was dose dependently suppressed by Norathyriol treatment. Western blot data revealed that Norathyriol attenuated the phosphorylation of Akt. Conclusions: Norathyriol exerts a potent chemopreventive activity by inhibiting Akt activation in neoplastic cell transformation.
Norathyriol suppresses skin cancers induced by solar ultraviolet radiation by targeting ERK kinases
Cancer Res 2012 Jan 1;72(1):260-70.PMID:22084399DOI:10.1158/0008-5472.CAN-11-2596.
Ultraviolet (UV) irradiation is the leading factor in the development of skin cancer, prompting great interest in chemopreventive agents for this disease. In this study, we report the discovery of Norathyriol, a plant-derived chemopreventive compound identified through an in silico virtual screening of the Chinese Medicine Library. Norathyriol is a metabolite of mangiferin found in mango, Hypericum elegans, and Tripterospermum lanceolatum and is known to have anticancer activity. Mechanistic investigations determined that Norathyriol acted as an inhibitor of extracellular signal-regulated kinase (ERK)1/2 activity to attenuate UVB-induced phosphorylation in mitogen-activated protein kinases signaling cascades. We confirmed the direct and specific binding of Norathyriol with ERK2 through a cocrystal structural analysis. The xanthone moiety in Norathyriol acted as an adenine mimetic to anchor the compound by hydrogen bonds to the hinge region of the protein ATP-binding site on ERK2. Norathyriol inhibited in vitro cell growth in mouse skin epidermal JB6 P+ cells at the level of G(2)-M phase arrest. In mouse skin tumorigenesis assays, Norathyriol significantly suppressed solar UV-induced skin carcinogenesis. Further analysis indicated that Norathyriol mediates its chemopreventive activity by inhibiting the ERK-dependent activity of transcriptional factors AP-1 and NF-κB during UV-induced skin carcinogenesis. Taken together, our results identify Norathyriol as a safe new chemopreventive agent that is highly effective against development of UV-induced skin cancer.
Norathyriol reverses obesity- and high-fat-diet-induced insulin resistance in mice through inhibition of PTP1B
Diabetologia 2014 Oct;57(10):2145-54.PMID:24985145DOI:10.1007/s00125-014-3315-8.
Aim/hypothesis: Protein tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signalling. PTP1B deficiency improves obesity-induced insulin resistance and consequently improves type 2 diabetes in mice. Here, the small molecule Norathyriol reversed obesity- and high-fat-diet-induced insulin resistance by inhibiting PTP1B. Methods: The inhibitory mode of PTP1B was evaluated by using the double-reciprocal substrate in the presence of Norathyriol. Primary cultured hepatocytes, myoblasts and white adipocytes were used to investigate the effect of Norathyriol on insulin signalling. Glucose homeostasis and insulin sensitivity were characterised by glucose and insulin tolerance tests. Results: Norathyriol was identified as a competitive inhibitor of PTP1B, with an IC50 of 9.59 ± 0.39 μmol/l. In cultured hepatocytes and myoblasts, Norathyriol treatment blocked the PTP1B-mediated dephosphorylation of the insulin receptor. Intraperitoneal injection of Norathyriol inhibited liver and muscle PTP1B activity in mice, thus contributing to the improved glucose homeostasis and insulin sensitivity. However, these beneficial effects were abolished in PTP1B-deficient mice. Notably, oral administration of Norathyriol protected mice from diet-induced obesity and insulin resistance through inhibition of hypothalamic PTP1B activity. Conclusions/interpretation: Our results indicate that the small molecule Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.
Absorption, Metabolism, and Pharmacokinetics Profiles of Norathyriol, an Aglycone of Mangiferin, in Rats by HPLC-MS/MS
J Agric Food Chem 2018 Nov 21;66(46):12227-12235.PMID:30298742DOI:10.1021/acs.jafc.8b03763.
Norathyriol, an aglycone of mangiferin, is a bioactive tetrahydroxyxanthone present in mangosteen and many medicinal plants. However, the biological fate of Norathyriol in vivo remains unclear. In this study, the absorption and metabolism of Norathyriol in rats were evaluated through HPLC-MS/MS. Results showed that Norathyriol was well absorbed, as indicated by its absolute bioavailability of 30.4%. Besides, a total of 21 metabolites of Norathyriol were identified in rats, including methylated, glucuronidated, sulfated and glycosylated conjugates, which suggested Norathyriol underwent extensive phase II metabolism. Among those metabolites, 15 metabolites were also identified in hepatocytes incubated with Norathyriol, indicating the presence of hepatic metabolism. Furthermore, glucuronide and sulfate conjugates, rather than their parent compound, were found to be the main forms existing in vivo after administration of Norathyriol, as implicated by the great increase of exposure of Norathyriol determined after hydrolysis with β-glucuronidase and sulfatase. The information obtained from this study contributes to better understanding of the pharmacological mechanism of Norathyriol.