Herbacetin
(Synonyms: 草质素) 目录号 : GC38635
An ODC inhibitor
Cas No.:527-95-7
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
Herbacetin is a natural product that acts as a selective inhibitor of ornithine decarboxylase (ODC).1 It inhibits recombinant and HCT116 and HT29 colon cancer cell-derived ODC in a dose-dependent manner while having no effect on 13 tested kinases or S-adenosylmethionine decarboxylase in vitro. Herbacetin suppresses anchorage-independent growth, activation of activator protein-1 (AP-1), a MAP kinase transcription factor, and phosphorylation of ERK1/2 and p90RSK in vitro. It suppresses HCT116 xenograft tumor growth in mice without significant body weight loss when administered i.p. or orally. Herbacetin also inhibits acetylcholinesterase (AChE; IC50 = 1.37 μM) in vitro.2
1.Kim, D.J., Roh, E.J., Lee, M.-H., et al.Herbacetin is a novel allosteric inhibitor of ornithine decarboxylase with antitumor activityCancer Res.76(5)1146-1157(2016) 2.Li, F.J., Liu, Y., Yuan, Y., et al.Molecular interaction studies of acetylcholinesterase with potential acetylcholinesterase inhibitors from the root of Rhodiola crenulata using molecular docking and isothermal titration calorimetry methodsInt. J. Biol. Macromol.104(Pt. A)527-532(2017)
| Cas No. | 527-95-7 | SDF | |
| 别名 | 草质素 | ||
| Canonical SMILES | O=C1C(O)=C(C2=CC=C(O)C=C2)OC3=C(O)C(O)=CC(O)=C13 | ||
| 分子式 | C15H10O7 | 分子量 | 302.24 |
| 溶解度 | DMSO: 100 mg/mL (330.86 mM) | 储存条件 | Store at -20°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 | 3.3086 mL | 16.5431 mL | 33.0863 mL |
| 5 mM | 0.6617 mL | 3.3086 mL | 6.6173 mL |
| 10 mM | 0.3309 mL | 1.6543 mL | 3.3086 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。
Discovery of Herbacetin as a Novel SGK1 Inhibitor to Alleviate Myocardial Hypertrophy
Adv Sci (Weinh) 2022 Jan;9(2):e2101485.PMID:34761560DOI:10.1002/advs.202101485.
Cardiac hypertrophy is a pivotal pathophysiological step of various cardiovascular diseases, which eventually leads to heart failure and death. Extracts of Rhodiola species (Ext.R), a class of commonly used medicinal herbs in Europe and East Asia, can attenuate cardiac hypertrophy both in vitro and in vivo. Serum/glucocorticoid regulated kinase 1 (SGK1) is identified as a potential target of Ext. R. By mass spectrometry-based kinase inhibitory assay, Herbacetin (HBT) from Ext.R is identified as a novel SGK1 inhibitor with IC50 of 752 nmol. Thermal shift assay, KINOMEscan in vitro assay combined with molecular docking proves a direct binding between HBT and SGK1. Site-specific mutation of Asp177 in SGK1 completely ablates the inhibitory activity of HBT. The presence of OH groups at the C-3, C-8, C-4' positions of flavonoids is suggested to be favorable for the inhibition of SGK1 activity. Finally, HBT significantly suppresses cardiomyocyte hypertrophy in vitro and in vivo, reduces reactive oxygen species (ROS) synthesis and calcium accumulation. HBT decreases phosphorylation of SGK1 and regulates its downstream forkhead box protein O1 (FoxO1) signaling pathway. Taken together, the findings suggest that a panel of flavonoids structurally related to HBT may be novel leads for developing new therapeutics against cardiac hypertrophy.
A comprehensive review of Herbacetin: From chemistry to pharmacological activities
J Ethnopharmacol 2021 Oct 28;279:114356.PMID:34166735DOI:10.1016/j.jep.2021.114356.
Ethnopharmacological relevance: Herbacetin is an active constituent of traditional Chinese medicines such as Ephedra sinica Stapf (MaHuang) and Sedum roseum (L.). Scop. (Hong JingTian). MaHuang was used to treat cough, asthma, fever, and edema for more than 5000 years, while Hong JingTian was used to treat depression, fatigue, cancers, and cardiovascular disease. Recent studies indicate that Herbacetin and its glycosides play a critical role in the pharmacological activities of these herbs. However, currently, no comprehensive review on Herbacetin has been published yet. Aim of the study: This review aimed to summarize information on the chemistry, natural sources, and pharmacokinetic features of Herbacetin, with an emphasis on its pharmacological activities and possible mechanisms of action. Materials and methods: A literature search was performed on the Web of Science, PubMed, and China Knowledge Resource Integrated databases (CNKI) using the search term "Herbacetin" ("all fields") from 1935 to 2020. Information was also obtained from classic books of Chinese herbal medicine, Chinese pharmacopeia, and the database "The Plant List" (www.theplantlist.org). Studies have been analyzed and summarized in this review if they dealt with chemistry, taxonomy, pharmacokinetic, and pharmacological activity. Results: Herbacetin is distributed in various plants and can be extracted or synthesized. It showed diverse pharmacological activities including antioxidant, antiviral, anti-inflammatory, anticancer, antidiabetic, and anticholinesterase. It is thought to have great potential in cancer treatment, especially colon and skin cancers. However, the bioavailability of Herbacetin is low and the toxicity of Herbacetin has not been studied. Thus, more studies are required to solve these problems. Conclusions: Herbacetin shows promising pharmacological activities against multiple diseases. Future research should focus on improving bioavailability, further studying its pharmacological mechanism, evaluating its toxicity and optimal dose, and performing the clinical assessment. We hope that the present review will serve as a guideline for future research on Herbacetin.
Herbacetin Broadly Blocks the Activities of CYP450s by Different Inhibitory Mechanisms
Planta Med 2022 Jun;88(7):507-517.PMID:34116570DOI:10.1055/a-1502-7131.
Herbacetin is a bioactive flavanol compound that has various pharmacological effects. However, the pharmacokinetic characteristics have not been thoroughly investigated. Previously, we screened a natural compound library and identified Herbacetin as a potent CYP blocker. Herein, we aimed to mechanistically determine the inhibitory effects of Herbacetin on CYP450 and its potential application. A human liver microsome incubation system was developed based on a UPLC-MS/MS method. Moreover, an in silico docking assay and a human CYP recombinase reaction system were developed and used to investigate binding affinity and inhibitory efficacy. Subsequently, the effects of the combination of Herbacetin and sorafenib on HepG2 cells were assessed by MTT and immunoblotting assays. The concentration of sorafenib and its main metabolite were measured by UPLC-MS/MS after incubation with or without Herbacetin. As a result, we found Herbacetin almost completely inhibited the functions of major CYPs at 100 µM. Moreover, through analysis of the structure-activity relationship, we found 4-, 6-, and 8-hydroxyl were essential groups for the inhibitory effects. Herbacetin inhibited CYP3A4, CYP2B6, CYP2C9, and CYP2E1 in a mixed manner, but non-competitively blocked CYP2D6. These results are in good agreement with the recombinase reaction in vitro results, with an IC50 < 10 µM for each tested isoenzyme. Interestingly, the stimulatory effects of sorafenib on HepG2 cell apoptosis were significantly enhanced by combining with Herbacetin, which was associated with increased sorafenib exposure. In summary, Herbacetin is a potent inhibitor of a wide spectrum of CYP450s, which may enhance the exposure of drugs in vivo.
Herbacetin suppressed MMP9 mediated angiogenesis of malignant melanoma through blocking EGFR-ERK/AKT signaling pathway
Biochimie 2019 Jul;162:198-207.PMID:31075281DOI:10.1016/j.biochi.2019.05.003.
Malignant melanoma remains a challenge for clinical practice and novel therapeutic strategies are urgently needed. Herbacetin, a natural flavonoid compound that has multiple pharmacological activities, exerts anticancer effects on several human tumors. In this study, the anti-angiogenesis effect of Herbacetin in human malignant melanoma was investigated. The results indicated that Herbacetin treatment significantly suppressed tumor growth and angiogenesis of malignant melanoma both in vitro and in vivo. In melanoma A375 and Hs294T cells, Herbacetin treatment suppressed both EGF-induced and constitutive phosphorylation of EGFR, accelerated the internalization and degradation of EGFR, and subsequently suppressed the activation of the downstream kinases (AKT and ERK). Moreover, MMP9 was determined as a key angiogenic factor in Herbacetin treated melanoma cells. Knockdown of MMP9 suppressed the in vitro angiogenesis while overexpression of MMP9 in Herbacetin treated melanoma cells restored the angiogenesis ability. We concluded that Herbacetin suppressed melanoma angiogenesis through blocking EGFR-ERK/AKT-MMP9 signaling pathway and Herbacetin may be developed as a potential drug for melanoma treatment.
Inhibition of SARS-CoV 3CL protease by flavonoids
J Enzyme Inhib Med Chem 2020 Dec;35(1):145-151.PMID:31724441DOI:10.1080/14756366.2019.1690480.
There were severe panics caused by Severe Acute Respiratory Syndrome (SARS) and Middle-East Respiratory Syndrome-Coronavirus. Therefore, researches targeting these viruses have been required. Coronaviruses (CoVs) have been rising targets of some flavonoids. The antiviral activity of some flavonoids against CoVs is presumed directly caused by inhibiting 3C-like protease (3CLpro). Here, we applied a flavonoid library to systematically probe inhibitory compounds against SARS-CoV 3CLpro. Herbacetin, rhoifolin and pectolinarin were found to efficiently block the enzymatic activity of SARS-CoV 3CLpro. The interaction of the three flavonoids was confirmed using a tryptophan-based fluorescence method, too. An induced-fit docking analysis indicated that S1, S2 and S3' sites are involved in binding with flavonoids. The comparison with previous studies showed that Triton X-100 played a critical role in objecting false positive or overestimated inhibitory activity of flavonoids. With the systematic analysis, the three flavonoids are suggested to be templates to design functionally improved inhibitors.