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Cearoin Sale

(Synonyms: 2,5-二羟基-4-甲氧基二苯甲酮) 目录号 : GC61865

Cearoin 通过促进 ROS 产生和激活 ERK 来增强自噬 (autophagy) 和诱导细胞凋亡(apoptosis)。

Cearoin Chemical Structure

Cas No.:52811-37-7

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1 mg
¥2,250.00
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产品描述

Cearoin increases autophagy and apoptosis through the production of ROS and the activation of ERK[1].

Cearoin (10-80 µM) induces cell death in a dose-dependent manner[1]. Cearoin (10-80 µM) increases the phosporylation of ERK in SH-SY5Y cells[1]. Cearoin (5-80 µM) increases the conversion of LC3B-I to LC3B-II in SH-SY5Y cells. The expression of LC3B-II is a good marker for autophagosome formation in the autophagy process[1].

References:
[1]. Tonking Bastola, et al. Cearoin Induces Autophagy, ERK Activation and Apoptosis via ROS Generation in SH-SY5Y Neuroblastoma Cells. Molecules. 2017 Feb 6;22(2):242.

Chemical Properties

Cas No. 52811-37-7 SDF
别名 2,5-二羟基-4-甲氧基二苯甲酮
Canonical SMILES O=C(C1=CC(O)=C(OC)C=C1O)C2=CC=CC=C2
分子式 C14H12O4 分子量 244.24
溶解度 储存条件 4°C, protect from light
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1 mM 4.0943 mL 20.4717 mL 40.9433 mL
5 mM 0.8189 mL 4.0943 mL 8.1887 mL
10 mM 0.4094 mL 2.0472 mL 4.0943 mL
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Research Update

Cearoin Induces Autophagy, ERK Activation and Apoptosis via ROS Generation in SH-SY5Y Neuroblastoma Cells

Molecules 2017 Feb 6;22(2):242.PMID:28178193DOI:10.3390/molecules22020242.

Neuroblastomas are the most common solid extracranial tumors in childhood. We investigated the anticancer effect of Cearoin isolated from Dalbergia odorifera in human neuroblastoma SH-SY5Y cells. SH-SY5Y cells were treated with various doses of Cearoin. The viability was measured by MTT assay. DCFDA fluorescence assay and Griess assay were used for the measurement of intracellular reactive oxygen species (ROS) and nitric oxide (NO), respectively. Western blot analysis was performed to clarify the molecular pathway involved. Cearoin induced cell death in a dose-dependent manner. Cearoin increased the phosporylation of ERK, the conversion of LC3B-I to LC3B-II, decrease in Bcl2 expression, the activation of caspase-3, and the cleavage of PARP, indicating the induction of autophagy and apoptosis. Furthermore, Cearoin treatment increased the production of ROS and NO. Co-treatment with the antioxidant N-acetylcysteine completely abolished cearoin-mediated autophagy, ERK activation and apoptosis, suggesting the critical role of ROS in cearoin-induced anticancer effects. Moreover, co-treatment with ERK inhibitor PD98059 partially reversed cearoin-induced cell death, indicating the involvement of ERK in Cearoin anticancer effects. These data reveal that Cearoin induces autophagy, ERK activation and apoptosis in neuroblastoma SH-SY5Y cells, which is mediated primarily by ROS generation, suggesting its therapeutic application for the treatment of neuroblastomas.

Neoflavonoids as potential osteogenic agents from Dalbergia sissoo heartwood

Bioorg Med Chem Lett 2014 Jun 15;24(12):2664-8.PMID:24803361DOI:10.1016/j.bmcl.2014.04.056.

The present study was undertaken to investigate and rationalize the in vitro antiosteoporotic activity of neoflavonoids, isolated from Dalbergia sissoo heartwood. Neoflavonoids were isolated using extensive column chromatography and identified as dalsissooal (1) a new compound and Cearoin (2), dalbergin (3), 4-methoxy dalbergion (4), dalbergiphenol (5), dalbergichromene (6), methyl dalbergin (7) and latinone (8) as known compounds by comparison their spectroscopic data with those reported in the literature. Among the screened compounds, compounds 1, 3, 5-8 significantly increased proliferation as assessed by alkaline phosphatase activity and mineralization in calvarial osteoblast cells.

Inhibitory effects of flavonoids extracted from Nepalese propolis on the LPS signaling pathway

Int Immunopharmacol 2016 Nov;40:550-560.PMID:27770720DOI:10.1016/j.intimp.2016.10.008.

Flavonoids, particularly those derived from plants, harbor biological effects such as anti-inflammation and the inhibition of cancer progression. In the present study, we investigated the effects of 10 kinds of flavonoids isolated from Nepalese propolis on the LPS signaling pathway in order to clarify their anti-inflammatory activities. Five types of flavonoids: isoliquiritigenin, chrysin, 3',4'-dihydroxy-4-methoxydalbergione, 4-methoxydalbergion, and Cearoin, markedly inhibited inflammatory responses including LPS-induced NO production by suppressing the expression of iNOS mRNA and LPS-induced mRNA expression of TNFα and CCL2. Their inhibitory effects on LPS-induced inflammatory responses correlated with the intensities of these flavonoids to suppress the LPS-induced activation of nuclear factor κB (NF-κB), an essential transcription factor for the mRNA expression of iNOS, TNFα, and CCL2. Among these flavonoids, 3',4'-dihydroxy-4-methoxydalbergione and 4-methoxydalbergion markedly inhibited the LPS-induced activation of IKK, thereby abrogating the degradation of IκBα and nuclear localization of NF-κB. On the other hand, isoliquiritigenin, chrysin, and Cearoin failed to inhibit these signaling steps, but suppressed the transcriptional activity of NF-κB, which caused their anti-inflammatory effects. The results of the present study revealed that these five kinds of flavonoids are the components of Nepalese propolis that exhibit anti-inflammatory activities with a different regulatory mechanism for the activation of NF-κB.

Urease inhibitor from Datisca cannabina linn

J Enzyme Inhib Med Chem 2008 Jun;23(3):386-90.PMID:18569344DOI:10.1080/14756360701536513.

A new flavonoid datisdirin (1), along with eight known compounds tectochrysine, Cearoin, sideroxyline, ursolic acid, corosolic acid, arjunolic acid, erythrodiol and oleanolic acid, were isolated from the ethyl acetate fraction of D. cannabina Linn. The structure of compound 1 was deduced on the basis of its spectral data. Datisdirin showed activity against the ureases enzyme.

Anti-inflammatory activity of flavonoids in Nepalese propolis is attributed to inhibition of the IL-33 signaling pathway

Int Immunopharmacol 2015 Mar;25(1):189-98.PMID:25614224DOI:10.1016/j.intimp.2015.01.012.

Propolis has been used in folk medicine to improve health and prevent inflammatory diseases; however, the components that exhibit its anti-inflammatory activity remain unknown. We herein investigated the effects of flavonoids isolated from Nepalese propolis on the IL-33 signaling pathway to clarify the anti-inflammatory mechanism involved. Of the 8 types of flavonoids isolated from Nepalese propolis, 4 types of compounds, such as 3',4'-dihydroxy-4-methoxydalbergione, 4-methoxydalbergion, Cearoin, and chrysin, markedly inhibited the IL-33-induced mRNA expression of inflammatory genes including IL-6, TNFα and IL-13 in bone marrow-derived mast cells (BMMC). These four flavonoids also inhibited the IL-33-induced activation of nuclear factor κB (NF-κB), which was consistent with their inhibitory effects on cytokine expression. The effects of these flavonoids are attributed to inhibition of IL-33-induced activation of IKK, which leads to the degradation of IκBα and nuclear localization of NF-κB. On the other hand, other flavonoids isolated from Nepalese propolis, such as isoliquiritigenin, plathymenin, 7-hydroxyflavanone, and (+)-medicarpin, had no effect on the IL-33 signaling pathway or cytokine expression. Therefore, these results indicate that 3',4'-dihydroxy-4-methoxydalbergione, 4-methoxydalbergion, Cearoin, and chrysin are the substances responsible for the anti-inflammatory activity of Nepalese propolis.