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Bilobetin Sale

(Synonyms: 白果素) 目录号 : GC35518

A biflavonoid with diverse biological activities

Bilobetin Chemical Structure

Cas No.:521-32-4

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产品描述

Bilobetin is a biflavonoid that has been found in G. biloba and has diverse biological activities.1,2,3 It is cytotoxic to HeLa, NCI-H460, Daudi, K562, SKOV3, MIA PaCa-2, and MCF-7 cells in vitro (IC50s = 14.79-97.28 μM).1 Bilobetin halts the cell cycle at the G2/M phase in HeLa cells in a concentration-dependent manner and induces apoptosis in HeLa cells when used at a concentration of 20 μM. It selectively inhibits matrix metalloproteinase-9 (MMP-9; IC50 = 10.33 μM) over MMP-2 and MMP-3 (IC50s = >100 μM).2 Bilobetin also inhibits aggregation of amyloid-β (1-40) peptide in vitro with an IC50 value of 4.7 μM.3

1.Li, M., Li, B., Xia, Z.-M., et al.Anticancer effects of five biflavonoids from Ginkgo Biloba L. male flowers in vitroMolecules24(8)E1496(2019) 2.Wang, C.G., Yao, W.N., Ahang, B., et al.Lung cancer and matrix metalloproteinases inhibitors of polyphenols from Selaginella tamariscina with suppression activity of migrationBioorg. Med. Chem. Lett.28(14)2413-2417(2018) 3.Sirimangkalakitti, N., Juliawaty, L.D., Hakim, E.H., et al.Naturally occurring biflavonoids with amyloid β aggregation inhibitory activity for development of anti-Alzheimer agentBioorg. Med. Chem. Lett.29(15)1994-1997(2019)

Chemical Properties

Cas No. 521-32-4 SDF
别名 白果素
Canonical SMILES O=C1C=C(C2=CC=C(O)C=C2)OC3=C(C4=CC(C5=CC(C6=C(O)C=C(O)C=C6O5)=O)=CC=C4OC)C(O)=CC(O)=C13
分子式 C31H20O10 分子量 552.48
溶解度 DMF: 10mg/mL,DMSO: 25mg/mL,DMSO:PBS (pH 7.2) (1:6): 0.14mg/mL,Ethanol: 2.5mg/mL 储存条件 Store at -20°C
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Research Update

Biological Importance of a Biflavonoid 'Bilobetin' in the Medicine: Medicinal Importance, Pharmacological Activities and Analytical Aspects

Infect Disord Drug Targets 2022;22(5):22-30.PMID:35319397DOI:10.2174/1871526522666220321152036.

Background: Flavonoid class phytochemicals are natural compounds present in different medicinal plants, vegetables and fruits. Ginkgo biloba contains significant amounts of bioflavonoid 'Bilobetin'. Bilobetin is an active phytochemical used for the treatment of human health complications due to its medicinal properties and therapeutic benefit. The purpose of this work is to collect and reviewed scientific data on Bilobetin from different literature sources; highlight their biological properties, pharmacological activities and analytical aspects. Methods: Health beneficial aspects of Bilobetin have been investigated in the present work through scientific data analysis. PubMed, Google Scholar, Google, Scopus, etc. have been searched in the present work in order to collect scientific information on Bilobetin. Medicinal importance and therapeutic benefit of Bilobetin has been searched in the present work through these databases of Bilobetin. Detailed pharmacological activities of Bilobetin have been reviewed in the present work through literature data analysis of various scientific research works. However, analytical data of Bilobetin were also collected and reviewed in the present reaserch. Results: Literature data analysis of Bilobetin in the present work revealed the medicinal properties and therapeutic potential of Bilobetin mainly due to its anti-fungal, anti-inflammatory, anti-oxidant, antihyperlipidemic, and anti-proliferative activities. Literature data analysis revealed the effectiveness of Bilobetin on osteoporosis, glucose metabolism, adipocytes, SARS CoV-2, Influenza A virus and human thrombin. Scientific data also revealed the importance of different analytical techniques for the isolation, separation, identification, and quantification of Bilobetin. Conclusion: Scientific data analysis revealed biological importance and pharmacological activities of Bilobetin in the health sector.

Bilobetin induces kidney injury by influencing cGMP-mediated AQP-2 trafficking and podocyte cell cycle arrest

Phytomedicine 2019 Nov;64:153073.PMID:31542661DOI:10.1016/j.phymed.2019.153073.

Background: Ginkgo biloba (Gb) extracts have been used as a traditional Chinese medicine. Gb contains flavonoids, which are considered to be its active ingredients and have been used in the treatment of a variety of diseases. However, few scientific research studies on the side effects of flavonoid in Gb have been reported. Purpose: The present study aimed to investigate the effect of Bilobetin on the kidney of Sprague-Dawley (SD) rats. Study design and result: In this study, rats were injected with 50 mg/kg of Bilobetin, a biflavone isolated from Gb, for 7 days and aristolochic acid was used as positive controls. The results showed that the body weight and urine output of the rats were dramatically decreased, and urinary protein increased after the intraperitoneal injection of Bilobetin compared with the control group. Bilobetin treatment showed vacuolar degeneration in the renal tubular epithelium, glomerular atrophy by histostaining, and podocyte fusion by electron microscopy. This study further showed that Bilobetin promoted the trafficking of aquaporin 2 (AQP-2) onto the plasma membrane to achieve the function of urine concentration by in vivo study in rats and in vitro study in IMCD-3 cells. The redistribution of AQP-2 is due to increased expression of cGMP in IMCD-3 cells, which in turn promoted the phosphorylation of AQP-2 at site Ser-256. The proteinuria caused by Bilobetin may be attributed to podocyte cell cycle arrest at G2/M transition, which is may associated with AKT and MAPK signaling. Conclusions: The current study showed that Bilobetin has some side effects on kidneys at a dose of 50 mg/kg in SD rats and provides insight into the potential detrimental effects of monomeric ingredients in Gb.

Quantitative determination of Bilobetin in rat plasma by HPLC-MS/MS and its application to a pharmacokinetic study

Biomed Chromatogr 2020 Apr;34(4):e4784.PMID:31853982DOI:10.1002/bmc.4784.

Although Bilobetin, a biflavone isolated from the leaves of Ginkgo biloba, represents a variety of pharmacological activities, to date there have been no validated determination methods for Bilobetin in biological samples. Thus, we developed a liquid chromatographic method using a tandem mass spectrometry for the determination of Bilobetin in rat plasma. After protein precipitation with acetonitrile including diclofenac (internal standard), the analytes were chromatographed on a reversed-phased column with a mobile phase of purified water and acetonitrile (3:7, v/v, including 0.1% formic acid). The ion transitions of the precursor to the product ion were principally deprotonated ions [M - H]- at m/z 551.2 → 519.2 for Bilobetin and 296.1 → 251.7 for the IS. The accuracy and precision of the assay were in accordance with US Food and Drug Administration regulations for the validation of bioanalytical methods. This analytical method was successfully applied to monitor plasma concentrations of Bilobetin over time following intravenous administration in rats.

The Mechanistic Perspective of Bilobetin Protective Effects against Cisplatin-Induced Testicular Toxicity: Role of Nrf-2/Keap-1 Signaling, Inflammation, and Apoptosis

Biomedicines 2022 May 13;10(5):1134.PMID:35625871DOI:10.3390/biomedicines10051134.

Cisplatin (CP) is a productive anti-tumor used to treat numerous tumors. However, multiple toxicities discourage prolonged use, especially toxicity on the reproductive system. This experiment was mapped out to determine the potential therapeutic impact of Bilobetin on CP-induced testicular damage. Herein, Bilobetin was isolated from Cycas thouarsii leaves R. Br ethyl acetate fractions for the first time. A single dose of CP (7 mg/kg, IP) was used to evoke testicular toxicity on the third day. Rats were classified into five groups; Normal control, Bilobetin 12 mg/kg, Untreated CP, and CP treated with Bilobetin (6 and 12 mg/kg, respectively) orally daily for ten days. Bilobetin treatment ameliorated testicular injury. In addition, it boosted serum testosterone levels considerably and restored relative testicular weight. Nevertheless, apoptosis biomarkers such as P53, Cytochrome-C, and caspase-3 decreased significantly. Additionally, it enhanced the testes' antioxidant status via the activation of Nrf-2, inhibition of Keap-1, and significant elevation of SOD activity in addition to a reduction in lipid peroxidation. Histopathologically, Bilobetin preserved testicular architecture and improved testicular immunostaining of Ki67 substantially, showing evidence of testicular regeneration. Bilobetin's beneficial effects on CP-induced testicular damage are associated with enhanced antioxidant effects, lowered apoptotic signals, and the restoration of testes' regenerative capability. In addition, Bilobetin may be used in combination with CP in treatment protocols to mitigate CP-induced testicular injury.

Bilobetin, a novel small molecule inhibitor targeting influenza virus polymerase acidic (PA) endonuclease was screened from plant extracts

Nat Prod Res 2021 Dec;35(24):5968-5971.PMID:32820654DOI:10.1080/14786419.2020.1808636.

The influenza A virus polymerase acidic (PA) endonuclease is an attractive target for anti-influenza drug development. In this study, plant extracts were used to screen the inhibitor against the PA endonuclease and its mutant. In 45 kinds of plant extracts, eight can effectively inhibit the PAN and PAN-I38T mutant in the primary screening. Dose-dependent inhibition assay showed that Epimedii folium can effectivity inhibit the PAN and PAN-I38T with IC50 of 11.23 and 26.03 μM, respectively. Furthermore, 130 ingredients of E. folium were virtually screened using the in silico method, and the compounds ginkgetin and Bilobetin bind to the active pocket of PAN and PAN-I38T with a strong interaction force. Gel-based PA endonuclease analysis and inhibition type analysis identified that Bilobetin can competitively inhibit the PA. Hence, Bilobetin, as an ingredient of E. folium, was screened through in vitro and in silico research.