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Sophoraflavanone G Sale

(Synonyms: 槐黄烷酮G,Kushenol F) 目录号 : GC38970

A flavonoid with diverse biological activities

Sophoraflavanone G Chemical Structure

Cas No.:97938-30-2

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5mg
¥1,071.00
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20mg
¥3,087.00
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产品描述

Sophoraflavanone G is a flavonoid that has been found in S. flavescens and has diverse biological activities.1,2,3,4 It is active against 21 strains of methicillin-resistant S. aureus (MRSA; MICs = 3.13-6.25 ?g/ml) and inhibits the activities of α-glucosidase and β-amylase (Kis = 5.6 and 30.6 ?M, respectively).1,2 Sophoraflavanone G is cytotoxic to HL-60 and HepG2 cancer cells (IC50s = 12.5 and 13.3 ?M, respectively) and induces apoptosis in HL-60 cells when used at concentrations of 10 or 25 ?M.3 It reduces LPS-induced production of prostaglandin E2 in RAW 264.7 cells when used at concentrations ranging from 1 to 50 ?M.4 Sophoraflavanone G (250 mg/kg) inhibits carrageenan-induced paw edema in rats.

1.Sato, M., Tsuchiya, H., Takase, I., et al.Antibacterial activity of flavanone isolated from Sophora exigua against methicillin-resistant Staphylococcus aureus and its combination with antibioticsPhytother. Res.9(7)509-512(1995) 2.Kim, J.H., Ryu, Y.B., Kang, N.S., et al.Glycosidase inhibitory flavonoids from Sophora flavescensBiol. Pharm. Bull.29(2)302-305(2006) 3.Ko, W.G., Kang, T.H., Kim, N.Y., et al.Lavandulylfavonoids: A new class of in vitro apoptogenic agents from Sophora favescensToxicol. In Vitro14(5)429-433(2000) 4.Kim, D.W., Chi, Y.S., Son, K.H., et al.Effects of sophoraflavanone G, a prenylated flavonoid from Sophora flavescens, on cyclooxygenase-2 and in vivo inflammatory responseArch. Pharm. Res.25(3)329-335(2002)

Chemical Properties

Cas No. 97938-30-2 SDF
别名 槐黄烷酮G,Kushenol F
Canonical SMILES O=C1C[C@@H](C2=CC=C(O)C=C2O)OC3=C(C[C@H](C(C)=C)C/C=C(C)\C)C(O)=CC(O)=C13
分子式 C25H28O6 分子量 424.49
溶解度 DMSO: 250 mg/mL (588.94 mM) 储存条件 Store at -20°C
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1 mM 2.3558 mL 11.7788 mL 23.5577 mL
5 mM 0.4712 mL 2.3558 mL 4.7115 mL
10 mM 0.2356 mL 1.1779 mL 2.3558 mL
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Research Update

Sophoraflavanone G suppresses the progression of triple-negative breast cancer via the inactivation of EGFR-PI3K-AKT signaling

Drug Dev Res 2022 Aug;83(5):1138-1151.PMID:35426453DOI:10.1002/ddr.21938.

Sophoraflavanone G (SG), a prenylated flavonoid extracted from Sophora flavescens, has been found to possess antitumor activity in several types of human cancer. However, the biological functions and molecular mechanism of SG in triple-negative breast cancer (TNBC) are required to be investigated. On the basis of network pharmacology methods and molecular docking technology, estimated glomerular filtration rate (EGFR) was identified as a potential target, and phosphatidylinositol 3-kinase-protein kinase B (PI3K-AKT) signaling was demonstrated as an important signaling pathway for SG to treat breast cancer. TNBC cells (BT-549 and MDA-MB-231) were used to determine the effects of SG in vitro. Cell Counting Kit, 5-ethynyl-2'-deoxyuridine, and colony formation assays confirmed the proliferation inhibition of SG on TNBC cells. Moreover, SG administration promoted cell apoptosis by affecting Bax, Bcl-2, and cleaved caspase-3 expression. SG treatment also enhanced oxidative stress of TNBC cells by inducing reactive oxygen species production, increasing malondialdehyde (MDA) level, and decreasing superoxide dismutase activity. Additionally, SG suppressed cell migration, invasion, and epithelial-mesenchymal transition process. Inactivated EGFR-PI3K-AKT signaling was observed in TNBC cells after treatment with SG. Furthermore, the inhibitory effects of SG on cell proliferation and metastasis and the promotive effects of SG on cell apoptosis and oxidative stress were significantly attenuated due to the overexpression of EGFR. Mice experiments revealed the suppression of SG on tumor growth and EGFR-PI3K-AKT signaling. Together, SG repressed the proliferation and metastasis, and induced apoptosis and oxidative stress in TNBC by targeting the EGFR-PI3K-AKT signaling pathway. SG might serve as a promising therapeutic agent to combat TNBC.

Sophoraflavanone G from Sophora flavescens Ameliorates Allergic Airway Inflammation by Suppressing Th2 Response and Oxidative Stress in a Murine Asthma Model

Int J Mol Sci 2022 May 29;23(11):6104.PMID:35682783DOI:10.3390/ijms23116104.

Sophoraflavanone G (SG), isolated from Sophora flavescens, has anti-inflammatory and anti-tumor bioactive properties. We previously showed that SG promotes apoptosis in human breast cancer cells and leukemia cells and reduces the inflammatory response in lipopolysaccharide-stimulated macrophages. We investigated whether SG attenuates airway hyper-responsiveness (AHR) and airway inflammation in asthmatic mice. We also assessed its effects on the anti-inflammatory response in human tracheal epithelial cells. Female BALB/c mice were sensitized with ovalbumin, and asthmatic mice were treated with SG by intraperitoneal injection. We also exposed human bronchial epithelial BEAS-2B cells to different concentrations of SG to evaluate its effects on inflammatory cytokine levels. SG treatment significantly reduced AHR, eosinophil infiltration, goblet cell hyperplasia, and airway inflammation in the lungs of asthmatic mice. In the lungs of ovalbumin-sensitized mice, SG significantly promoted superoxide dismutase and glutathione expression and attenuated malondialdehyde levels. SG also suppressed levels of Th2 cytokines and chemokines in lung and bronchoalveolar lavage samples. In addition, we confirmed that SG decreased pro-inflammatory cytokine, chemokine, and eotaxin expression in inflammatory BEAS-2B cells. Taken together, our data demonstrate that SG shows potential as an immunomodulator that can improve asthma symptoms by decreasing airway-inflammation-related oxidative stress.

Sophoraflavanone G Resensitizes ABCG2-Overexpressing Multidrug-Resistant Non-Small-Cell Lung Cancer Cells to Chemotherapeutic Drugs

J Nat Prod 2021 Sep 24;84(9):2544-2553.PMID:34496204DOI:10.1021/acs.jnatprod.1c00584.

Elevated expression of the ATP-binding cassette (ABC) drug transporter ABCG2 in cancer cells contributes to the development of the multidrug resistance phenotype in patients with advanced non-small-cell lung cancer (NSCLC). Due to the lack of U.S. Food and Drug Administration (FDA)-approved synthetic inhibitors of ABCG2, significant efforts have been invested in discovering bioactive compounds of plant origin that are capable of reversing ABCG2-mediated multidrug resistance in cancer cells. Sophoraflavanone G (SFG), a phytoncide isolated from the plant species Sophora flavescens, is known to possess a wide spectrum of pharmacological activities, including antibacterial, anti-inflammatory, antimalarial, and antiproliferative effects. In the present study, the chemosensitizing effect of SFG in ABCG2-overexpressing NSCLC cells was investigated. Experimental results demonstrate that at subtoxic concentrations SFG significantly reversed ABCG2-mediated multidrug resistance in a concentration-dependent manner. Additional biochemical data and in silico docking analysis of SFG to the inward-open conformation of human ABCG2 indicate that SFG inhibited the drug transport function of ABCG2 by interacting with residues within the transmembrane substrate-binding pocket of ABCG2. Collectively, these findings provide evidence that SFG has the potential to be further tested as an effective inhibitor of ABCG2 to improve the efficacy of therapeutic drugs in patients with advanced NSCLC.

Sophoraflavanone G induces apoptosis of human cancer cells by targeting upstream signals of STATs

Biochem Pharmacol 2013 Oct 1;86(7):950-9.PMID:23962443DOI:10.1016/j.bcp.2013.08.009.

Aberrantly activated signal transducer and activator of transcription (STAT) proteins are implicated with human cancers and represent essential roles for cancer cell survival and proliferation. Therefore, the development of small-molecule inhibitors of STAT signaling bearing pharmacological activity has therapeutic potential for the treatment of human cancers. In this study, we identified Sophoraflavanone G as a novel small-molecule inhibitor of STAT signaling in human cancer cells. Sophoraflavanone G inhibited tyrosine phosphorylation of STAT proteins in Hodgkin's lymphoma and tyrosine phosphorylation of STAT3 in solid cancer cells by inhibiting phosphorylation of the Janus kinase (JAK) proteins, Src family tyrosine kinases, such as Lyn and Src, Akt, and ERK1/2. In addition, Sophoraflavanone G inhibited STAT5 phosphorylation in murine-bone-marrow-derived pro-B cells transfected with translocated Ets Leukemia (TEL)-JAKs and cytokine-induced rat pre-T lymphoma cells, as well as STAT5b reporter activity in TEL-JAKs and STAT5b reporter systems. Sophoraflavanone G also inhibited nuclear factor-κB (NF-κB) signaling in multiple myeloma cells. Furthermore, Sophoraflavanone G inhibited cancer cell proliferation and induced apoptosis by regulating the expression of apoptotic and anti-apoptotic proteins. Our data suggest that Sophoraflavanone G is a novel small-molecule inhibitor of STAT signaling by targeting upstream signals of STATs that may have therapeutic potential for cancers caused by persistently activated STAT proteins.

Antiparasitical efficacy of Sophoraflavanone G isolated from Sophora flavescens against parasitic protozoa Ichthyophthirius multifiliis

Vet Parasitol 2022 Jun;306:109731.PMID:35643574DOI:10.1016/j.vetpar.2022.109731.

Ichthyophthirius multifiliis, a global distributed protozoan parasite, causes "White spot disease" and leads to serious mortality of freshwater fish in aquaculture. The present study was conducted to assess the anti-I. multifiliis efficacy of active compound isolated from Sophora flavescens. The isolated active compound was identified as Sophoraflavanone G (SG) with ESI-MS and NMR. In vitro tests, SG at concentrations of 0.5 mg/L and 2 mg/L resulted in death of all theronts and tomonts, respectively; SG at concentrations of 0.125 mg/L and 0.25 mg/L notably decreased theronts infectivity (p < 0.05). Additionally, the in vivo test results showed that a cumulative delivery of SG at concentration of 2 mg/L for 7 days protected fish from I. multifiliis infection. The 96-h LC50 (median lethal concentration) and safety concentration of SG to grass carp were 46.6 mg/L and 11.3 mg/L, respectively. The present work indicated that SG was a potential safe and effectively therapeutic agent in treating I. multifiliis.