567-75-9Relevant academic research and scientific papers
Rhodomentosones A and B: Two Pairs of Enantiomeric Phloroglucinol Trimers from Rhodomyrtus tomentosa and Their Asymmetric Biomimetic Synthesis
Bai, Yang-Ting-Zhi,Deng, Lu-Ming,Hu, Li-Jun,Huang, Xiao-Jun,Jiang, Ren-Wang,Li, Chuang-Chuang,Li, Yao-Lan,Qin, Guan-Qiu,Song, Qiao-Yun,Su, Jun-Cheng,Tang, Wei,Wang, Jie,Wang, Ying,Ye, Wen-Cai
, p. 4499 - 4504 (2021/06/28)
Rhodomentosones A and B (1 and 2), two pairs of novel enantiomeric phloroglucinol trimers featuring a unique 6/5/5/6/5/5/6-fused ring system were isolated from Rhodomyrtus tomentosa. Their structures with absolute configurations were elucidated by NMR spe
Polycyclic benzodifuran compound and application thereof as anti-RSV drug
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, (2021/01/04)
The invention discloses a polycyclic benzodifuran compound with a formula (I), a preparation method thereof and an application of the polycyclic benzodifuran compound as an anti-respiratory syncytialvirus (RSV) drug. The polycyclic benzodifuran compound d
Synthesis and P-glycoprotein induction activity of colupulone analogs
Bharate, Jaideep B.,Batarseh, Yazan S.,Wani, Abubakar,Sharma, Sadhana,Vishwakarma, Ram A.,Kaddoumi, Amal,Kumar, Ajay,Bharate, Sandip B.
, p. 5488 - 5496 (2015/05/20)
Brain amyloid-beta (Aβ) plaques are one of the primary hallmarks associated with Alzheimer's disease (AD) pathology. Efflux pump proteins located at the blood-brain barrier (BBB) have been reported to play an important role in the clearance of brain Aβ, among which the P-glycoprotein (P-gp) efflux transporter pump has been shown to play a crucial role. Thus, P-gp has been considered as a potential therapeutic target for treatment of AD. Colupulone, a prenylated phloroglucinol isolated from Humulus lupulus, is known to activate pregnane-X-receptor (PXR), which is a nuclear receptor controlling P-gp expression. In the present work, we aimed to synthesize and identify analogs of colupulone that are potent P-gp inducer(s) with an ability to enhance Aβ transport across the BBB. A series of colupulone analogs were synthesized by modifications at both prenyl as well as acyl domains. All compounds were screened for P-gp induction activity using a rhodamine 123 based efflux assay in the P-gp overexpressing human adenocarcinoma LS-180 cells, wherein all compounds showed significant P-gp induction activity at 5 μM. In the western blot studies in LS-180 cells, compounds 3k and 5f were able to induce P-gp as well as LRP1 at 1 μM. The effect of compounds on the Aβ uptake and transport was then evaluated. Among all tested compounds, diprenylated acyl phloroglucinol 5f displayed a significant increase (29%) in Aβ transport across bEnd3 cells grown on inserts as a BBB model. The results presented here suggest the potential of this scaffold to enhance clearance of brain Aβ across the BBB and thus its promise for development as a potential anti-Alzheimer agent.
Virucidal activity of a β-triketone-rich essential oil of Leptospermum scoparium (manuka oil) against HSV-1 and HSV-2 in cell culture
Reichling, Juergen,Koch, Christine,Stahl-Biskup, Elisabeth,Sojka, Cornelia,Schnitzler, Paul
, p. 1123 - 1127 (2007/10/03)
The inhibitory activity of manuka oil against Herpes simplex virus type 1 (HSV-1) and Herpes simplex virus type 2 (HSV-2) was tested in vitro on RC-37 cells (monkey kidney cells) using a plaque reduction assay. In order to determine the mode of antiviral
β-triketones from Myrtaceae: Isoleptospermone from Leptospermum scoparium and papuanone from Corymbia dallachiana
Van Klink, John W.,Brophy, Joseph J.,Perry, Nigel B.,Weavers, Rex T.
, p. 487 - 489 (2007/10/03)
Naturally occurring β-triketones, isoleptospermone [3, 5-hydroxy-4-(2- methyl-1-oxopentyl)-2,2,6,6-tetramethyl-4-cyclohexene-1,3-dione) from Leptospermum scoparium] and papuanone [6, 5-hydroxy-4-(1-oxohexyl)-2,2,6,6- tetramethyl-4-cyclohexene-1,3-dione fr
