Palbinone
(Synonyms: 芍药二酮) 目录号 : GC34701
Palbinone是从芍药中提取的萜类物质，有效抑制3α羟基类固醇脱氢酶(3α-HSD)的活性，IC50值为46nM。具有抗炎功效。
Cas No.:139954-00-0
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
Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity[1]. IC50: 46 nM (3α-HSD)[1]
[1]. Kadota S, et al. Palbinone, a novel terpenoid from Paeonia albiflora; potent inhibitory activity on 3 alpha-hydroxysteroid dehydrogenase. Chem Pharm Bull (Tokyo). 1993 Mar;41(3):487-90.
| Cas No. | 139954-00-0 | SDF | |
| 别名 | 芍药二酮 | ||
| Canonical SMILES | C[C@]1([C@@]2(C3=O)C)[C@@](C=CC2=C(O)C3=O)([H])[C@@]4([C@@](C(C)([C@@H](O)CC4)C)([H])CC1)C | ||
| 分子式 | C22H30O4 | 分子量 | 358.47 |
| 溶解度 | Soluble in DMSO | 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 | 2.7896 mL | 13.9482 mL | 27.8963 mL |
| 5 mM | 0.5579 mL | 2.7896 mL | 5.5793 mL |
| 10 mM | 0.279 mL | 1.3948 mL | 2.7896 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。
Palbinone alleviates diabetic retinopathy in STZ-induced rats by inhibiting NLRP3 inflammatory activity
J Biochem Mol Toxicol 2020 Jul;34(7):e22489.PMID:32202043DOI:10.1002/jbt.22489.
Diabetic retinopathy (DR) is the primary cause of blindness and visual impairment in diabetes patients worldwide. However, laser and surgical therapies at DR have short-term effectiveness and cause side effects. Treatment with natural products is a reasonable alternative treatment for DR. The main objective of this investigation is to explore the efficacy of a bioactive compound such as Palbinone (PB) in DR. Experimental rats were injected intraperitoneally with streptozotocin (STZ, 65 mg/kg), and these established experimental rats were treated with PB (20 mg/kg/bw) for 42 days. The observed results showed that PB considerably reduced the proinflammatory cytokine (interleukin-18 [IL-18] and IL-1β) production as well as improved the activities of antioxidant enzymes (superoxide dismutase, catalase, and glutathione peroxidase) particularly in the retinal region of STZ-induced DR rats. In addition, PB treatment improved nuclear factor erythroid 2-related factor 2 (Nrf2) accumulation and enhanced the heme oxygenase-1 expression, and major antioxidants downregulated Nrf2 in the damaged retina. Also, the expression levels of nod-like receptor family pyrin domain containing 3 (NLRP3), cleaved-caspase-1, IL-1β, and apoptosis-associated speck-like protein containing CARD in the retinal region were notably upregulated in STZ-induced DR, which was eliminated by PB interference. PB administration exerted efficient antioxidant activities, Nrf2 pathway activation, and inhibition of NLRP3 inflammasome. This current investigation concluded that PB considerably reduced the retinal inflammation and oxidative stress stimulated via high glucose, and also activated the antioxidative Nrf2 pathway and inhibited the NLRP3 inflammasome formation in rats.
Palbinone from Paeonia suffruticosa protects hepatic cells via up-regulation of heme oxygenase-1
Phytother Res 2014 Feb;28(2):308-11.PMID:23595773DOI:10.1002/ptr.4993.
Paeonia suffruticosa has been traditionally employed for vitalizing blood circulation and alleviating liver and inflammatory diseases. The pathways by which Palbinone (PB) isolated from P. suffruticosa mediates heme oxygenase-1 (HO-1) induction were investigated using the specific inhibitors for PI3K and mitogen activated protein kinases pathways. The effect of PB-treatment on Nrf2 translocalization and HO-1-antioxidant response element (ARE) regulation was examined employing Western blot and luciferase assays. PB induced HO-1 expression via the activation of Nrf2 in the hepatic cells, and ARE-dependent genes were stimulated via the PB-mediated Nrf2 activation. PB-mediated HO-1 expression could be involved with PI3K/Akt and ERK1/2 pathways. Our study suggests the mechanism by which PB induces HO-1 expression in the hepatic cells. This might substantiate the traditional applications of P. suffruticosa for the treatment of oxidative stress-related diseases including oxidant and inflammatory-mediated vascular and liver diseases.
Palbinone, a novel terpenoid from Paeonia albiflora; potent inhibitory activity on 3 alpha-hydroxysteroid dehydrogenase
Chem Pharm Bull (Tokyo) 1993 Mar;41(3):487-90.PMID:8477499DOI:10.1248/cpb.41.487.
Palbinone, a novel terpenoid isolated from the roots of Paeonia albiflora, showed a strong inhibitory activity on the reduced form of nicotinamide adenine dinucleotide phosphate (NADPH)-linked 3 alpha-hydroxysteroid dehydrogenase (3 alpha-HSD) of rat liver cytosol. The structures of Palbinone and a known compound, paeonilactone-B isolated from the active fraction of this plant were determined by the use of 2D NMR techniques (1H-1H COSY, 1H-13C COSY, 1H-13C long-range COSY, and HMBC).
Palbinone and triterpenes from Moutan Cortex (Paeonia suffruticosa, Paeoniaceae) stimulate glucose uptake and glycogen synthesis via activation of AMPK in insulin-resistant human HepG2 Cells
Bioorg Med Chem Lett 2009 Oct 1;19(19):5556-9.PMID:19716700DOI:10.1016/j.bmcl.2009.08.048.
Moutan Cortex is a well-known herb in traditional Korean, Chinese, and Japanese anti-diabetic formulae. In the current study, we investigated the metabolic effects of isolated triterpenes (1-7) in HepG2 cells under high glucose conditions. These compounds remakably stimulated AMP-activated protein kinase (AMPK), GSK-3beta, and ACC phosphorylation. The compounds also increased glucose uptake and enhanced glycogen synthesis. Among these, compound 1 displayed the greatest potential anti-diabetic activity though the AMPK activation pathway. Compound 1 significantly increased the levels of phospho-AMPK, phospho-ACC, and phospho-GSK-3beta and stimulated glucose uptake and glycogen synthesis in a dose-dependent manner. In conclusion, our results suggest that these compounds, especially compound 1, may have beneficial roles in glucose metabolism via the AMPK pathway.
Paeonone A, a novel nonanortriterpenoid from the roots of Paeonia lactiflora
Bioorg Chem 2021 May;110:104783.PMID:33714021DOI:10.1016/j.bioorg.2021.104783.
Paeonone A (1), a unique nonanortriterpenoid, and a new octanortriterpenoid, paeonone B (2), were isolated from the roots of Paeonia lactiflora, together with a known analogue, Palbinone (3). Paeonone A (1) is the first example of naturally occurring nonanortriterpenoid with a diketo acid group. Extensive NMR and HRESIMS experiments were applied to identify the structures of 1 and 2, and their absolute configurations were solved by single-crystal X-ray diffraction and ECD data. Biological properties of 1-3 were explored against pancreatic lipase and cancer cell lines.