Dihydrokaempferol
(Synonyms: 香橙素) 目录号 : GC38617
Dihydrokaempferol(Aromadendrin)是一种天然存在的黄酮类化合物,具有清除自由基、抗炎、抗肿瘤等生物活性。
Cas No.:480-20-6
Sample solution is provided at 25 µL, 10mM.
Dihydrokaempferol (Aromadendrin) is a naturally occurring flavonoid compound with biological activities such as free radical scavenging, anti-inflammatory and anti-tumor[1, 2]. Dihydrokaempferol can activate the SIRT1 pathway, thereby activating cell autophagy, reducing oxidative stress damage and inhibiting inflammatory response[3].
In vitro, Dihydrokaempferol (10, 30μM) treatment of rheumatoid arthritis fibroblast-like synoviocytes (RA-FLSs) for 48h concentration-dependently inhibited cell viability, induced cell apoptosis and was able to express apoptosis-related proteins[4]. Dihydrokaempferol (0-200μM) pretreatment of RAW264.7 macrophages for 1h inhibited LPS-induced NO and PGE2 production in a concentration-dependent manner[5]. Dihydrokaempferol (20μM) pretreatment of SH-SY5y neuronal cells for 1h inhibited methamphetamine (METH)-induced cytotoxicity and enhanced cell confluence[6].
In vivo, oral administration of Dihydrokaempferol (80mg/kg) to treat severe acute pancreatitis (SAP) mice regulated the Keap1/Nrf2 pathway, reduced oxidative stress damage, and improved SAP-induced pancreatic damage[7].
References:
[1] Kim J K, Park S U. Recent studies on kaempferol and its biological and pharmacological activities[J]. EXCLI journal, 2020, 19: 627-634.
[2] Wang S H, Hu Y L, Liu T X. Plant distribution and pharmacological activity of flavonoids[J]. Tradit. Med. Res, 2019, 4: 269-287.
[3] Zhang J, Hu C, Li X, et al. Protective effect of dihydrokaempferol on acetaminophen-induced liver injury by activating the SIRT1 pathway[J]. The American Journal of Chinese Medicine, 2021, 49(03): 705-718.
[4] Zhang Y, Yan G, Sun C, et al. Apoptosis effects of dihydrokaempferol isolated from Bauhinia championii on synoviocytes[J]. Evidence‐Based Complementary and Alternative Medicine, 2018, 2018(1): 9806160.
[5] Lee J W, Kim N H, Kim J Y, et al. Aromadendrin inhibits lipopolysaccharide-induced nuclear translocation of NF-κB and phosphorylation of JNK in RAW 264.7 macrophage cells[J]. Biomolecules & Therapeutics, 2013, 21(3): 216.
[6] Lee H S, Kim E N, Jeong G S. Aromadendrin protects neuronal cells from methamphetamine-induced neurotoxicity by regulating endoplasmic reticulum stress and PI3K/Akt/mTOR signaling pathway[J]. International Journal of Molecular Sciences, 2021, 22(5): 2274.
[7] Liang X, Hu C, Liu C, et al. Dihydrokaempferol (DHK) ameliorates severe acute pancreatitis (SAP) via Keap1/Nrf2 pathway[J]. Life Sciences, 2020, 261: 118340.
Dihydrokaempferol(Aromadendrin)是一种天然存在的黄酮类化合物,具有清除自由基、抗炎、抗肿瘤等生物活性[1, 2]。Dihydrokaempferol能够激活SIRT1通路,从而激活细胞自噬、减少氧化应激损伤并抑制炎症反应[3]。
在体外,Dihydrokaempferol(10, 30μM)处理类风湿关节炎成纤维样滑膜细胞(RA-FLSs)48h,浓度依赖性地抑制了细胞活力,诱导了细胞凋亡并且能够凋亡相关蛋白表达[4]。Dihydrokaempferol(0-200μM)预处理RAW264.7巨噬细胞细胞1h,以浓度依赖性方式抑制了LPS诱导的NO和PGE2产生[5]。Dihydrokaempferol(20μM)预处理SH-SY5y神经元细胞1h,抑制了甲基苯丙胺(METH)诱导的细胞毒性,增强了细胞的汇合度[6]。
在体内,Dihydrokaempferol(80mg/kg)通过口服治疗重症急性胰腺炎(SAP)小鼠,调节了Keap1/Nrf2通路,减少了氧化应激损伤,改善了SAP引起的胰腺损伤[7]。
Cell experiment [1]: | |
Cell lines | Rheumatoid arthritis fibroblast-like synoviocytes (RA-FLSs) |
Preparation Method | RA-FLSs cultured in 96-well plates were treated with Dihydrokaempferol at various concentrations (0.3, 3, 30, 300μM) for 48h, followed by incubation with MTS for an additional 4h at 37°C. Then the absorbance at 570nm was taken by a microplate reader. |
Reaction Conditions | 0.3, 3, 30, 300μM; 48h |
Applications | Dihydrokaempferol (0.3, 3, 30, 300μM) had no significant effect of cell survival on normal synoviocytes. But Dihydrokaempferol (0.3, 3, 30, 300μM) concentration dependently decreased the viability of RA-FLSs. |
Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice were randomly divided into six distinct groups as follows: ad-control, ad-control+Severe acute pancreatitis (SAP), ad-control+SAP+Dihydrokaempferol (80mg/kg), ad-Keap1, ad- Keap1+SAP, and ad-Keap1+SAP+Dihydrokaempferol (80mg/kg). These mice received seven i.p. of 50μg/kg cerulein diluted in saline, with a 1 h interval between the injections. On the last injection, these mice received an injection that contained both cerulein and LPS (10mg/kg). Subsequently, these mice were intravenously (i.v.) injected with ad-Keap1 (5×108 pfu) or ad-control (5×108 pfu) to be infected and Dihydrokaempferol administered orally 1h after SAP induction. Lastly, these mice were sacrificed 6h after SAP induction and their plasma and pancreas tissues collected. |
Dosage form | 80mg/kg; p.o. |
Applications | Keap1 overexpression adenovirus (ad-Keap1) suppressed the nuclear translocation of Nrf2 which is enhanced by Dihydrokaempferol, and suppressed the antioxidant functionality of Dihydrokaempferol both in mice and cells models. |
References: |
Cas No. | 480-20-6 | SDF | |
别名 | 香橙素 | ||
Canonical SMILES | O=C1C2=C(O)C=C(O)C=C2O[C@H](C3=CC=C(O)C=C3)[C@H]1O | ||
分子式 | C15H12O6 | 分子量 | 288.25 |
溶解度 | DMSO: 10 mM | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
1 mM | 3.4692 mL | 17.3461 mL | 34.6921 mL |
5 mM | 0.6938 mL | 3.4692 mL | 6.9384 mL |
10 mM | 0.3469 mL | 1.7346 mL | 3.4692 mL |
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