Paeoniflorin是一种从毛茛科植物芍药根中提取的蒎烷单萜糖苷，具有多种生物学活性。
Cas No.:23180-57-6
Sample solution is provided at 25 µL, 10mM.
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Paeoniflorin is a pinane monoterpene glycoside extracted from the roots of Paeonia plants of the Ranunculaceae family, possessing multiple biological activities[1-2]. Through mechanisms such as activating adenosine A1 receptors, inhibiting COX-2 expression, and downregulating HIF-1α, Paeoniflorin exerts anti-inflammatory, immunomodulatory, analgesic, anti-tumor, antioxidant stress, and anti-platelet aggregation effects. Paeoniflorin can be used in research related to rheumatoid arthritis, cardiovascular diseases, neurological disorders, and tumors[3-4].
In vitro, Paeoniflorin (60μM) pretreatment of ER-positive breast cancer cell lines T47D and MCF-7 for 48 hours, followed by combination treatment with Tamoxifen (8μM for T47D, 16μM for MCF-7), Paeoniflorin significantly enhanced Tamoxifen-induced apoptosis, upregulated the Bax/Bcl-2 protein expression ratio and Caspase 3 activity, while inhibiting STAT3 phosphorylation and its downstream target gene c-Myc expression by promoting SIRT4 expression[5]. Paeoniflorin (1-30μM) co-treatment with TGF-β1 (2ng/mL) in human alveolar epithelial cells A549 for 48 hours, Paeoniflorin significantly inhibited TGF-β1-induced epithelial-mesenchymal transition (EMT), reduced cell migration ability and Vimentin and α-SMA expression, while downregulating the transcription factor Snail expression through the Smad-dependent pathway and reducing type I and III collagen secretion[6].
In vivo, Paeoniflorin (50, 100, 200mg/kg/day) intraperitoneal injection in acetaminophen (APAP; 300mg/kg)-induced drug-induced liver injury C57BL/6J male mice (preventive administration starting 5 days before modeling, for 5 consecutive days), Paeoniflorin significantly reduced serum ALT, AST, ALP, γ-GT, and TBIL levels, alleviated liver tissue inflammation and edema, and protected hepatocytes from APAP damage by activating autophagy through inhibiting the MAPK/mTOR signaling pathway, reducing oxidative stress and apoptosis[7]. Paeoniflorin (5, 10mg/kg/day) intraperitoneal injection in LPS-induced cognitive dysfunction ICR male mice (starting after LPS injection, for 3 consecutive weeks), Paeoniflorin significantly improved spatial memory, recognition memory, and long-term learning ability in mice, and alleviated LPS-induced cognitive deficits by inhibiting the expression of APP, BACE, PS1, and PS2 proteins in the brain and reducing β-amyloid production[8].
References:
[1] Zhang L, Wei W. Anti-inflammatory and immunoregulatory effects of paeoniflorin and total glucosides of paeony. Pharmacol Ther. 2020 Mar;207:107452.
[2] Zhang XX, Zuo JQ, Wang YT, et al. Paeoniflorin in Paeoniaceae: Distribution, influencing factors, and biosynthesis. Front Plant Sci. 2022 Sep 2;13:980854.
[3] Ma Y, Lang X, Yang Q, et al. Paeoniflorin promotes intestinal stem cell-mediated epithelial regeneration and repair via PI3K-AKT-mTOR signalling in ulcerative colitis. Int Immunopharmacol. 2023 Jun;119:110247.
[4] Wang XL, Feng ST, Wang YT, et al. Paeoniflorin: A neuroprotective monoterpenoid glycoside with promising anti-depressive properties. Phytomedicine. 2021 Sep;90:153669.
[5] Zhang P, Wu N, Song ZJ, et al. Paeoniflorin Enhances the Sensitivity of ER-Positive Breast Cancer Cells to Tamoxifen through Promoting Sirtuin 4. Evid Based Complement Alternat Med. 2022 Jan 15;2022:6730559.
[6] Ji Y, Dou YN, Zhao QW, et al. Paeoniflorin suppresses TGF-β mediated epithelial-mesenchymal transition in pulmonary fibrosis through a Smad-dependent pathway. Acta Pharmacol Sin. 2016 Jun;37(6):794-804.
[7] Deng X, Li Y, Chen Y, et al. Paeoniflorin protects hepatocytes from APAP-induced damage through launching autophagy via the MAPK/mTOR signaling pathway. Cell Mol Biol Lett. 2024 Sep 7;29(1):119.
[8] Meng HW, Kim JH, Kim HY, et al. Paeoniflorin Attenuates Lipopolysaccharide-Induced Cognitive Dysfunction by Inhibition of Amyloidogenesis in Mice. Int J Mol Sci. 2023 Mar 2;24(5):4838.
Paeoniflorin是一种从毛茛科植物芍药根中提取的蒎烷单萜糖苷，具有多种生物学活性[1-2]。Paeoniflorin通过激活腺苷A1受体、抑制COX-2表达和下调HIF-1α等机制，发挥抗炎、免疫调节、镇痛、抗肿瘤、抗氧化应激、抗血小板聚集等功能，Paeoniflorin可用于类风湿关节炎、心血管疾病、神经系统疾病和肿瘤等相关研究[3-4]。
在体外，Paeoniflorin（60μM）预处理ER阳性乳腺癌细胞系T47D和MCF-7 48小时，随后与Tamoxifen（8μM for T47D，16μM for MCF-7）联合处理，Paeoniflorin显著增强Tamoxifen诱导的细胞凋亡，并上调Bax/Bcl-2蛋白表达比例及Caspase 3活性，同时通过促进SIRT4表达抑制STAT3磷酸化及其下游靶基因c-Myc的表达[5]。Paeoniflorin（1-30μM）与TGF-β1（2ng/mL）处理人肺泡上皮细胞A549 48小时，Paeoniflorin显著抑制TGF-β1诱导的上皮-间质转化（EMT），降低细胞迁移能力及波形蛋白（Vimentin）和α-SMA表达，同时通过Smad依赖性途径下调转录因子Snail表达，减少I型和III型胶原分泌[6]。
在体内，Paeoniflorin（50，100，200mg/kg/day）腹腔注射处理Administered acetaminophen (APAP； 300mg/kg)诱导的药物性肝损伤C57BL/6J雄性小鼠（从造模前5天开始预防性给药，连续5天），Paeoniflorin显著降低血清ALT、AST、ALP、γ-GT和TBIL水平，减轻肝组织炎症和水肿，并通过抑制MAPK/mTOR信号通路激活自噬、减少氧化应激和细胞凋亡，从而保护肝细胞免受APAP损伤[7]。Paeoniflorin（5，10mg/kg/day）腹腔注射处理LPS诱导的认知功能障碍ICR雄性小鼠（从LPS注射后开始，连续3周），Paeoniflorin显著改善小鼠的空间记忆、识别记忆以及长期学习能力，并通过抑制脑内APP、BACE、PS1和PS2蛋白表达，减少β-淀粉样蛋白生成，从而缓解LPS诱导的认知缺陷[8]。
| Cell experiment [1]: | |
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Cell lines |
A549 cells (human type II alveolar epithelial cell line) |
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Preparation Method |
A549 cells were maintained in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. For EMT induction, cells were incubated with TGF-β1 (2ng/mL). Paeoniflorin was co-incubated with TGF-β1 at 1-30μM. |
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Reaction Conditions |
1-30μM; 48h |
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Applications |
Paeoniflorin significantly inhibited TGF-β1-induced epithelial-mesenchymal transition (EMT) in A549 cells, as evidenced by the reversal of morphological changes to a mesenchymal phenotype, reduction of cell migration, up-regulation of epithelial marker E-cadherin, and down-regulation of mesenchymal markers Vimentin and α-SMA. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6J mice |
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Preparation Method |
Mice were intraperitoneally Administered acetaminophen (APAP; 300mg/kg) to induce acute liver injury. Paeoniflorin (50, 100, 200mg/kg) was administered intraperitoneally once daily for 5 consecutive days before APAP injection. Mice were sacrificed 24 hours after APAP administration for serum and liver tissue collection. |
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Dosage form |
50, 100, 200mg/kg; i.p.; Once daily for 5 days. |
|
Applications |
Paeoniflorin pretreatment significantly attenuated APAP-induced acute liver injury, as evidenced by reduced serum levels of ALT, AST, ALP, γ-GT, and TBIL, and ameliorated liver histopathological changes including hepatocyte necrosis, inflammatory cell infiltration, and congestion. Paeoniflorin also suppressed oxidative stress by decreasing MDA levels and increasing SOD and GSH activities, and inhibited apoptosis by regulating the Bax/Bcl-2 ratio and cleaved caspase-3 expression. Mechanistically, Paeoniflorin activated autophagy through the MAPK/mTOR signaling pathway, which contributed to its hepatoprotective effects against APAP-induced liver damage. |
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References: |
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| Cas No. | 23180-57-6 | SDF | |
| 别名 | 芍药苷; Peoniflorin | ||
| 化学名 | ((2S,2aR,2a1S,3aR,4R,5aR)-4-hydroxy-2-methyl-2a-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-1,5-dioxa-2,4-methanocyclobuta[cd]pentalen-2a1-yl)methyl benzoate | ||
| Canonical SMILES | O=C(C1=C([H])C([H])=C([H])C([H])=C1[H])OC([H])([H])[C@@]2([C@@]3([H])C4([H])[H])[C@]4([C@@](C5([H])[H])(C([H])([H])[H])O[C@]2([H])O[C@@]35O[H])O[C@]([C@]([C@@]6([H])O[H])([H])O[H])([H])O[C@@](C([H])([H])O[H])([H])[C@@]6([H])O[H] | ||
| 分子式 | C23H28O11 | 分子量 | 480.47 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,PBS (pH 7.2): 10 mg/mL | 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 | 2.0813 mL | 10.4065 mL | 20.813 mL |
| 5 mM | 416.3 μL | 2.0813 mL | 4.1626 mL |
| 10 mM | 208.1 μL | 1.0406 mL | 2.0813 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。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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