trans-Chalcone
(Synonyms: 反-查耳酮) 目录号 : GC61896
Trans-Chalcone, the backbone of flavonoids, also is a potent fatty acid synthase (FAS) with IC50 of 17.1 μg/mL, and α-amylase inhibitor, causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7, exerting antifungal and anticancer activities.
Cas No.:614-47-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Trans-Chalcone, the backbone of flavonoids, also is a potent fatty acid synthase (FAS) with IC50 of 17.1 μg/mL, and α-amylase inhibitor, causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7, exerting antifungal and anticancer activities.
[1] Bitencourt TA, et al. BMC Complement Altern Med. 2013 Sep 17;13:229. [2] Najafian M, et al. Mol Biol Rep. 2011 Mar;38(3):1617-20. [3] Bortolotto LF, et al. Biomed Pharmacother. 2017 Jan;85:425-433.
| Cas No. | 614-47-1 | SDF | |
| 别名 | 反-查耳酮 | ||
| Canonical SMILES | O=C(C1=CC=CC=C1)/C=C/C2=CC=CC=C2 | ||
| 分子式 | C15H12O | 分子量 | 208.26 |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.8017 mL | 24.0085 mL | 48.0169 mL |
| 5 mM | 0.9603 mL | 4.8017 mL | 9.6034 mL |
| 10 mM | 0.4802 mL | 2.4008 mL | 4.8017 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。
trans-Chalcone inhibits transforming growth factor-β1 and connective tissue growth factor-dependent collagen expression in the heart of high-fat diet-fed rats
Arch Physiol Biochem 2022 Oct;128(5):1221-1224.PMID:32407146DOI:10.1080/13813455.2020.1764045.
Objective: Non-alcoholic fatty liver disease (NAFLD) is one of the main risk factors for cardiovascular mortality and morbidity. This study, for the first time, explored the effects of trans-Chalcone on cardiac expressions of myocardial fibrosis-related genes, including transforming growth factor -β1 (TGF-β1), connective tissue growth factor (CTGF/CCN2), and collagen type I.Materials and methods: Twenty-eight rats were randomly divided into four groups: control, received 10% tween 80; chalcone, received trans-Chalcone; HFD, received high-fat diet (HFD) and 10% tween 80; HFD + chalcone, received HFD and trans-Chalcone, by once-daily gavage for 6 weeks. Finally, cardiac expression levels of TGF-β1, CTGF, and collagen type I were determined.Results: HFD feeding increased mRNA levels of collagen type I, TGF-β1, and CTGF in the heart of rats. However, trans-Chalcone inhibited HFD-induced changes.Conclusions: trans-Chalcone can act as a cardioprotective compound by inhibiting TGF-β1 and CTGF-dependent stimulation of collagen type I synthesis in the heart of HFD-fed rats.
trans-Chalcone increases p53 activity via DNAJB1/HSP40 induction and CRM1 inhibition
PLoS One 2018 Aug 17;13(8):e0202263.PMID:30118500DOI:10.1371/journal.pone.0202263.
Naturally-occurring chalcones and synthetic chalcone analogues have been demonstrated to have many biological effects, including anti-inflammatory, anti-malarial, anti-fungal, and anti-oxidant/anti-cancerous activities. Compared to other chalcones, trans-Chalcone exhibits superior inhibitory activity in cancer cell growth as shown via in vitro assays, and exerts anti-cancerous effects via the activation of the p53 tumor suppressor protein. Thus, characterization of the specific mechanisms, by which trans-Chalcone activates p53, can aid development of new chemotherapeutic drugs that can be used individually or synergistically with other drugs. In this report, we found that trans-Chalcone modulates many p53 target genes, HSP40 being the most induced gene in the RNA-Seq data using trans-chalcone-treated cells. CRM1 is also inhibited by trans-Chalcone, resulting in the accumulation of p53 and other tumor suppressor proteins in the nucleus. Similar effects were seen using trans-Chalcone derivatives. Overall, trans-Chalcone could provide a strong foundation for the development of chalcone-based anti-cancer drugs.
trans-Chalcone enhances insulin sensitivity through the miR-34a/SIRT1 pathway
Iran J Basic Med Sci 2018 Apr;21(4):359-363.PMID:29796217DOI:10.22038/IJBMS.2018.24300.6063.
Objectives: trans-Chalcone as the parent member of the chalcone series reduces circulating levels of insulin and glucose. However, the cellular mechanism of these effects is poorly understood. Sirtuin 1 (SIRT1) as a direct target of miR-34a controls homeostasis of glucose, and also improves insulin sensitivity. Therefore, the present study for the first time investigated the influence of trans-Chalcone on the miR-34a/SIRT1 pathway as a possible mechanism for its hypoglycemic and hypoinsulinemic effects. Materials and methods: In this study, thirty male rats were randomly divided into three groups (n=10): solvent control (NS), oral administration of trans-Chalcone for 2 (N2T) and 6 weeks (N6T) groups. Then, hepatic levels of miR-34a and SIRT1 were measured through the qRT-PCR method. Results: trans-Chalcone reduced food intake, body weight gain, and serum glucose as well as insulin levels. Also, this chalcone inhibited hepatic miR-34a expression and significantly elevated SIRT1 mRNA level. Conclusion: trans-Chalcone as an insulin-sensitizing chalcone partly acts through the miR-34a/SIRT1 pathway.
trans-Chalcone inhibits high-fat diet-induced disturbances in FXR/SREBP-1c/FAS and FXR/Smad-3 pathways in the kidney of rats
J Food Biochem 2020 Nov;44(11):e13476.PMID:32944984DOI:10.1111/jfbc.13476.
High-fat diet (HFD) intake is linked to chronic kidney disease. Farnesoid X receptor (FXR) controls the renal lipid metabolism and fibrosis. The purpose of the current study was to evaluate the possible impacts of trans-Chalcone on HFD-induced changes in renal lipid metabolism and Smad-3 expression through the regulation of FXR expression. To this aim, 28 rats were randomly divided into control, chalcone, HFD, and HFD + chalcone groups. At the end of treatments, renal FXR, sterol regulatory element-binding protein (SREBP)-1c, fatty acid synthase (FAS), Smad-3, and neutrophil gelatinase-associated lipocalin (NGAL) expression levels were assayed. Moreover, insulin sensitivity check index (QUICKI) was calculated. trans-Chalcone significantly inhibited HFD-induced reduction of insulin sensitivity. Moreover, HFD decreased the FXR expression, and trans-Chalcone reversed this change. trans-Chalcone also inhibited HFD-induced increases in expression levels of SREBP-1c, FAS, Smad-3, and NGAL. Therefore, trans-Chalcone, as a renoprotective agent, inhibits HFD-induced disturbances in FXR/SREBP-1c/FAS and FXR/Smad-3 pathways. PRACTICAL APPLICATIONS: Non-alcoholic fatty liver disease and metabolic syndrome, two health concerns with increasing prevalence, are known as important risk factors for chronic kidney disease. The current study indicated the preventive effect of trans-Chalcone administration on HFD-induced disturbances in renal FXR/SREBP-1c/FAS and FXR/Smad-3 pathways. According to these results, trans-Chalcone can be regarded as a renoprotective functional food component that can protect individuals with metabolic syndrome against chronic renal disease.
trans-Chalcone Attenuates Pain and Inflammation in Experimental Acute Gout Arthritis in Mice
Front Pharmacol 2018 Oct 2;9:1123.PMID:30333752DOI:10.3389/fphar.2018.01123.
Gouty arthritis is characterized by an intense inflammatory response to monosodium urate crystals (MSU), which induces severe pain and reduction in the life quality of patients. trans-Chalcone (1,3-diphenyl-2-propen-1-one) is a flavonoid precursor presenting biological activities such as anti-inflammatory and antioxidant proprieties. Thus, the aim of this work was to evaluate the protective effects of trans-Chalcone in experimental gout arthritis in mice. Mice were treated with trans-Chalcone (3, 10, or 30 mg/kg, per oral) or vehicle (Tween 80 20% plus saline) 30 min before intra-articular injection of MSU (100 μg/knee joint, intra-articular). We observed that trans-Chalcone inhibited MSU-induced mechanical hyperalgesia, edema, and leukocyte recruitment (total leukocytes, neutrophils, and mononuclear cells) in a dose-dependent manner. trans-Chalcone also decreased inflammatory cell recruitment as observed in Hematoxylin and Eosin (HE) staining and the intensity of fluorescence of LysM-eGFP+ cells in the confocal microscopy. trans-Chalcone reduced MSU-induced oxidative stress as observed by an increase in the antioxidant defense [Glutathione (GSH), Ferric Reducing (FRAP), and 2,2'-Azinobis-3-ethylbenzothiazoline 6-sulfonic acid (ABTS assays)] and reduction in reactive oxygen and nitrogen species production [superoxide anion (NBT assay) and nitrite (NO assay)]. Furthermore, it reduced in vivo MSU-induced interleukin-1β (IL-1β), Tumor necrosis factor-α (TNF-α), and IL-6 production, and increased Transforming growth factor-β (TGF-β) production. Importantly, trans-Chalcone reduced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) activation and thereby the mRNA expression of the inflammasome components Nlrp3 (cryopyrin), Asc (apoptosis-associated speck-like protein containing a CARD), Pro-caspase-1 and Pro-IL-1β. In vitro, trans-Chalcone reduced the MSU-induced release of IL-1β in lipopolysaccharide (LPS)-primed macrophages. Therefore, the pharmacological effects of trans-Chalcone indicate its therapeutic potential as an analgesic and anti-inflammatory flavonoid for the treatment of gout.