Pedalitin
(Synonyms: 5,6,3',4'-四羟基-7-甲氧基黄酮) 目录号 : GC63497
Pedalitin 是酪氨酸酶（IC50=0.28 mM）和α-葡萄糖苷酶抑制剂（IC50=0.29 mM）。
Cas No.:22384-63-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pedalitin is a inhibitor of tyrosinase（IC50=0.28 mM） and α-glucosidase（IC50=0.29 mM）[1].
[1]. Lin L,et al.Comparative evaluation of rosmarinic acid, methyl rosmarinate and pedalitin isolated from Rabdosia serra (MAXIM.) HARA as inhibitors of tyrosinase and α-glucosidase. Food Chem. 2011;129(3):884-889.
| Cas No. | 22384-63-0 | SDF | |
| 别名 | 5,6,3',4'-四羟基-7-甲氧基黄酮 | ||
| 分子式 | C16H12O7 | 分子量 | 316.26 |
| 溶解度 | 储存条件 | Store at -20°C | |
| 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 | 3.162 mL | 15.8098 mL | 31.6196 mL |
| 5 mM | 0.6324 mL | 3.162 mL | 6.3239 mL |
| 10 mM | 0.3162 mL | 1.581 mL | 3.162 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 | ||||||||||
| 计算重置 | ||||||||||
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Synergistic effect of Pedalitin and amphotericin B against Cryptococcus neoformans by in vitro and in vivo evaluation
Int J Antimicrob Agents 2016 Nov;48(5):504-511.PMID:27742203DOI:10.1016/j.ijantimicag.2016.07.025.
Cryptococcosis is an opportunistic fungal infection responsible for high morbidity and mortality in immunocompromised patients. Combination of antifungal substances is a promising way to increase the percentage of successful treatment. Pedalitin (PED) is a natural substance obtained from Pterogyne nitens. The aim of this study was to verify the efficacy of PED alone and in combination with amphotericin B (AmB) in vitro and in vivo against Cryptococcus spp. In the in vitro assay, minimum inhibitory concentrations (MICs) of 0.125 mg/L for AmB and 3.9 mg/L for PED were found when the substances were tested alone, whilst in the combination treatment the active concentration of both decreased, with MICs of 0.03 mg/L for AmB and 1 mg/L for PED. In the survival assay, fungal burden study and histopathological assays it was possible to study the efficacy of the substances alone and in combination. The efficacy of combination therapy was considered better than monotherapy as evaluated in a Galleria mellonella model and a murine model. Thus, the combination of PED and AmB is an interesting alternative for anticryptococcal fungal treatment. Moreover, a correlation was observed between the invertebrate and murine models for this antifungal treatment combination.
Effect of traditionally used herb Pedalium murex L. and its active compound Pedalitin on urease expression - For the management of kidney stone
Saudi J Biol Sci 2020 Mar;27(3):833-839.PMID:32127759DOI:10.1016/j.sjbs.2020.01.014.
Pedalium murex L. is a medicinal herb that has been used for the treatment of diseases related to kidney in the traditional system of medicine. The current study aims to study the effect of ethyl acetate extract of P. murex (EAEP) and its fractionated compound Pedalitin against urease production and UreC gene expression in Proteus mirabilis. The selected reference strain Proteus mirabilis (MTCC 425) and the isolates culture of Proteus mirabilis were subjected to study the antibacterial efficacy of P. murex. Expression analysis of P. mirabilis urease gene was successfully done by QPCR. The ethyl acetate extract effectively inhibit the reference Proteus mirabilis and bacterial isolates of Proteus mirabilis in the clinical samples studied. EAEP has showed more potent activity (56.7%) against urease enzyme and Pedalitin also exhibited potent activity (30.1%). Using qPCR, the expression of UreC gene of P. mirabilis was controlled by EAEP and also its bioactive compound Pedalitin. The present study clearly demonstrated the potency of P. murex in controlling the growth of pathogenic P. mirabilis and to control the expression of urease enzyme production as well as to restrict the urease gene expression in P. mirabilis.
Comparative evaluation of rosmarinic acid, methyl rosmarinate and Pedalitin isolated from Rabdosia serra (MAXIM.) HARA as inhibitors of tyrosinase and α-glucosidase
Food Chem 2011 Dec 1;129(3):884-9.PMID:25212314DOI:10.1016/j.foodchem.2011.05.039.
Rabdosia serra has been used in traditional Chinese medicine for centuries. In order to illustrate the pharmaceutical activity of R. serra as hypoglycaemic and skin-whitening agents, rosmarinic acid (confirmed as the major compound in R. serra), methyl rosmarinate and Pedalitin isolated from R. serra were evaluated for their inhibitory effects and mechanisms on tyrosinase and α-glucosidase. The inhibitory effects on both tyrosinase and α-glucosidase were in decreasing order, Pedalitin>methyl rosmarinate>rosmarinic acid. The IC50 values for the tyrosinase and α-glucosidase activity inhibited by Pedalitin were 0.28 and 0.29mM, respectively. Both rosmarinic acid and methyl rosmarinate were considered as noncompetitive inhibitors of tyrosinase, while Pedalitin was suggested to be a mixed-type inhibitor of tyrosinase. In the assay of α-glucosidase inhibition, rosmarinic acid was found to be a competitive inhibitor, whereas both methyl rosmarinate and Pedalitin were considered as mixed-type inhibitors.
Antioxidants from Rabdosia japonica
Phytother Res 2006 Mar;20(3):206-13.PMID:16521110DOI:10.1002/ptr.1835.
The antioxidant activities of phenolic compounds: Pedalitin, quercetin, rutin, isoquercitrin, and rosmarinic acid, isolated from the dried leaves of Rabdosia japonica Hara (Labiatae) were elucidated. All the phenolics tested exhibited superoxide scavenging activity and an inhibitory effect on xanthine oxidase (EC 1.1.3.22), and Pedalitin showed the most potent antioxidant activity. Pedalitin prevents the generation of superoxide radicals in part by inhibiting xanthine oxidase competitively. Both Pedalitin and quercetin inhibited uric acid formation by xanthine oxidase, and the inhibition kinetics analysed by Lineweaver-Burk plots found both flavonoids to be competitive inhibitors. On the other hand, isoquercitrin, rutin and rosmarinic acid were effective in scavenging superoxide radicals generated by the xanthine-xanthine oxidase system without inhibiting the enzyme.
Flavonoids from Pterogyne nitens as Zika virus NS2B-NS3 protease inhibitors
Bioorg Chem 2021 Apr;109:104719.PMID:33636437DOI:10.1016/j.bioorg.2021.104719.
Although the widespread epidemic of Zika virus (ZIKV) and its neurological complications are well-known there are still no approved drugs available to treat this arboviral disease or vaccine to prevent the infection. Flavonoids from Pterogyne nitens have already demonstrated anti-flavivirus activity, although their target is unknown. In this study, we virtually screened an in-house database of 150 natural and semi-synthetic compounds against ZIKV NS2B-NS3 protease (NS2B-NS3p) using docking-based virtual screening, as part of the OpenZika project. As a result, we prioritized three flavonoids from P. nitens, quercetin, rutin and Pedalitin, for experimental evaluation. We also used machine learning models, built with Assay Central® software, for predicting the activity and toxicity of these flavonoids. Biophysical and enzymatic assays generally agreed with the in silico predictions, confirming that the flavonoids inhibited ZIKV protease. The most promising hit, Pedalitin, inhibited ZIKV NS2B-NS3p with an IC50 of 5 μM. In cell-based assays, Pedalitin displayed significant activity at 250 and 500 µM, with slight toxicity in Vero cells. The results presented here demonstrate the potential of Pedalitin as a candidate for hit-to-lead (H2L) optimization studies towards the discovery of antiviral drug candidates to treat ZIKV infections.