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Xanthohumol

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https://www.readbyqxmd.com/read/28858767/discovery-of-new-md2-targeted-anti-inflammatory-compounds-for-the-treatment-of-sepsis-and-acute-lung-injury
#1
Gaozhi Chen, Bing Xiao, Lingfeng Chen, Bin Bai, Yali Zhang, Zheng Xu, Lili Fu, Zhiguo Liu, Xiaokun Li, Yunjie Zhao, Guang Liang
Myeloid differentiation 2 (MD2) is essential to the recognition of lipopolysaccharide (LPS) and the subsequent mediation of toll-like receptor 4 (TLR4)-dependent acute inflammatory disorders including sepsis and acute lung injury. Inhibitors targeting MD2 may provide an alternative means to subdue acute inflammatory diseases. In the present study, 39 bisaryl-1,4-dien-3-one compounds with 5-carbon connection chains were designed and synthesized as MD2 inhibitors based on the analysis of the molecular docking of xanthohumol to MD2...
August 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28812892/designer-extracts-as-tools-to-balance-estrogenic-and-chemopreventive-activities-of-botanicals-for-women-s-health
#2
Birgit M Dietz, Shao-Nong Chen, René F Ramos Alvarenga, Huali Dong, Dejan Nikolić, Martin Biendl, Richard B van Breemen, Judy L Bolton, Guido F Pauli
Botanical dietary supplements contain multiple bioactive compounds that target numerous biological pathways. The lack of uniform standardization requirements is one reason that inconsistent clinical effects are reported frequently. The multifaceted biological interactions of active principles can be disentangled by a coupled pharmacological/phytochemical approach using specialized ("knock-out") extracts. This is demonstrated for hops, a botanical for menopausal symptom management. Employing targeted, adsorbent-free countercurrent separation, Humulus lupulus extracts were designed for pre- and postmenopausal women by containing various amounts of the phytoestrogen 8-prenylnaringenin (8-PN) and the chemopreventive constituent xanthohumol (XH)...
August 16, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28812343/xanthohumol-suppresses-mylip-idol-gene-expression-and-modulates-ldlr-abundance-and-activity-in-hepg2-cells
#3
Shih-Fen Chen, Pei-Yi Chen, Hao-Jen Hsu, Ming-Jiuan Wu, Jui-Hung Yen
Xanthohumol, a prenylated flavonoid found in hops (Humulus lupulus L.), exhibits multiple biological activities such as antiatherosclerosis and hypolipidemic activities. In this study, we aim to investigate the hypocholesterolemic effects and molecular mechanisms of xanthohumol in hepatic cells. We found that xanthohumol (10 and 20 μM) increased the amount of cell-surface low-density lipoprotein receptor (LDLR) from 100.0 ± 2.1% to 115.0 ± 1.3% and 135.2 ± 2.7%, and enhanced the LDL uptake activity from 100...
August 28, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28754033/the-influence-of-glycosylation-of-natural-and-synthetic-prenylated-flavonoids-on-binding-to-human-serum-albumin-and-inhibition-of-cyclooxygenases-cox-1-and-cox-2
#4
Tomasz Tronina, Paulina Strugała, Jarosław Popłoński, Aleksandra Włoch, Sandra Sordon, Agnieszka Bartmańska, Ewa Huszcza
The synthesis of different classes of prenylated aglycones (α,β-dihydroxanthohumol (2) and (Z)-6,4'-dihydroxy-4-methoxy-7-prenylaurone (3)) was performed in one step reactions from xanthohumol (1)-major prenylated chalcone naturally occurring in hops. Obtained flavonoids (2-3) and xanthohumol (1) were used as substrates for regioselective fungal glycosylation catalyzed by two Absidia species and Beauveria bassiana. As a result six glycosides (4-9) were formed, of which four glycosides (6-9) have not been published so far...
July 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28750311/synthesis-and-antiangiogenic-activity-study-of-new-hop-chalcone-xanthohumol-analogues
#5
Elisa Nuti, Barbara Bassani, Caterina Camodeca, Lea Rosalia, AnnaRita Cantelmo, Cristina Gallo, Denisa Baci, Antonino Bruno, Elisabetta Orlandini, Susanna Nencetti, Douglas M Noonan, Adriana Albini, Armando Rossello
Angiogenesis induction is a hallmark of cancer. Antiangiogenic properties of Xanthohumol (XN), a naturally occurring prenylated chalcone from hops, have been widely reported. Here we describe the synthesis and study the antiangiogenic activity in vitro of a series of XN derivatives, where different substituents on the B-ring of the chalcone scaffold were inserted. The new XN derivatives inhibited human umbilical-vein endothelial cell (HUVEC) proliferation, adhesion, migration, invasion and their ability to form capillary-like structures in vitro at 10 μM concentration...
July 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28745504/xanthohumol-restores-hepatic-glucolipid-metabolism-balance-in-type-1-diabetic-wistar-rats
#6
Mário Lima-Fontes, Raquel Costa, Ilda Rodrigues, Raquel Soares
Diabetes exhibits increased inflammation, angiogenesis, and apoptosis, three processes attenuated by xanthohumol (XN). Herein, we evaluate the effect of XN-enriched stout beer consumption in hepatic glucolipid metabolism imbalance seen in type 1 diabetes (T1D). Five groups of Wistar rats were established: streptozotocin-induced diabetic rats drinking water, treated with 5% ethanol, stout beer, and stout beer supplemented with 10 mg of XN/L and healthy rats drinking water. Hepatic periodic acid-Schiff, reticulin, sirius red, and oil red O histological staining was performed...
August 30, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28674253/effect-of-valerian-hop-mixture-on-sleep-related-behaviors-in-drosophila-melanogaster
#7
Hyeon-Son Choi, Bong Soo Ko, Hae Dun Kim, Ki-Bae Hong, Hyung Joo Suh
The aim of this study was to investigate the sleep-promoting effect of a Valerian/Hops mixture in fruit flies. The HPLC analysis showed that Valerenic acid (1260.53 µg/g of extract) and Xanthohumol (Cascade: 827.49 µg/g, Hallertau: 763.60 µg/g, Saaz: 186.93 µg/g) were contained in Valerian and Hop, respectively. The sleep patterns of fruit flies on the Valerian/Hops were examined in both baseline and caffeine-treated conditions. Total activities of flies significantly decreased in 20 mg/mL Valerian (74%), 10 mg/mL Cascade (25%), and 5 mg/mL Hallertau (11%) during nighttime or daytime compared with the control...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28665345/in-vitro-effect-of-8-prenylnaringenin-and-naringenin-on-fibroblasts-and-glioblastoma-cells-cellular-accumulation-and-cytotoxicity
#8
Monika Stompor, Łukasz Uram, Rafał Podgórski
Gliomas are one of the most aggressive and treatment-resistant types of human brain cancer. Identification and evaluation of anticancer properties of compounds found in plants, such as naringenin (N) and 8-prenylnaringenin (8PN), are among the most promising applications in glioma therapy. The prenyl group seems to be crucial to the anticancer activity of flavones, since it may lead to enhanced cell membrane targeting and thus increased intracellular activity. It should be noted that 8PN content in hop cones is 10 to 100 times lower compared to other flavonoids, such as xanthohumol...
June 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28627872/xanthohumol-blocks-proliferation-and-migration-of-vascular-smooth-muscle-cells-in-vitro-and-reduces-neointima-formation-in-vivo
#9
Rongxia Liu, Elke H Heiss, Daniel Schachner, Baohong Jiang, Wanhui Liu, Johannes M Breuss, Verena M Dirsch, Atanas G Atanasov
Xanthohumol (1) is a principal prenylated chalcone found in hops. The aim of this study was to examine its influence on platelet-derived growth factor (PDGF)-BB-triggered vascular smooth muscle cell (VSMC) proliferation and migration in vitro and on experimentally induced neointima formation in vivo. Quantification of resazurin conversion indicated that 1 can inhibit PDGF-BB-induced VSMC proliferation concentration-dependently (IC50 = 3.49 μM). Furthermore, in a wound-healing assay 1 potently suppresses PDGF-BB-induced VSMC migration at 15 μM...
July 28, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28539058/the-role-of-chalcones-helichrysetin-xanthohumol-and-flavokawin-c-in-promoting-neurite-outgrowth-in-pc12-adh-cells
#10
Chia-Wei Phan, Vikineswary Sabaratnam, Wai-Kuan Yong, Sri Nurestri Abd Malek
Chalcones are a group of compounds widely distributed in plant kingdom. The aim of this study was to assess the neurite outgrowth stimulatory activity of selected chalcones, namely helichrysetin, xanthohumol and flavokawin-C. Using adherent rat pheochromocytoma (PC12 Adh) cells, the chalcones were subjected to neurite outgrowth assay and the extracellular nerve growth factor (NGF) levels were determined. Xanthohumol (10 μg/mL) displayed the highest (p < 0.05) percentage of neurite-bearing PC12 Adh cells and the highest (p < 0...
May 25, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28501703/xanthohumol-a-hop-derived-prenylated-flavonoid-promotes-macrophage-reverse-cholesterol-transport
#11
Hiroshi Hirata, Harumi Uto-Kondo, Masatsune Ogura, Makoto Ayaori, Kazusa Shiotani, Ami Ota, Youichi Tsuchiya, Katsunori Ikewaki
Xanthohumol, a prominent prenyl flavonoid from the hop plant (Humulus lupulus L.), is suggested to be antiatherogenic since it reportedly increases high-density lipoprotein (HDL) cholesterol levels. It is not clear whether xanthohumol promotes reverse cholesterol transport (RCT), the most important antiatherogenic property of HDL; therefore, we investigated the effects of xanthohumol on macrophage-to-feces RCT using a hamster model as a CETP-expressing species. In vivo RCT experiments showed that xanthohumol significantly increased fecal appearance of the tracer derived from intraperitoneally injected [(3)H]-cholesterol-labeled macrophages...
April 22, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28432774/comprehensive-two-dimensional-pc-3-prostate-cancer-cell-membrane-chromatography-for-screening-anti-tumor-components-from-radix-sophorae-flavescentis
#12
Qiang Wang, Junnan Xu, Xiang Li, Dawei Zhang, Yong Han, Xu Zhang
Radix Sophorae flavescentis is generally used for the treatment of different stages of prostate cancer in China. It has ideal effects when combined with surgical treatment and chemotherapy. However, its active components are still ambiguous. We devised a comprehensive two-dimensional PC-3 prostate cancer cell membrane chromatography system for screening anti-prostate cancer components in Radix Sophorae flavescentis. Gefitinib and dexamethasone were chosen as positive and negative drugs respectively for validation and optimization the selectivity and suitability of the comprehensive two-dimensional chromatographic system...
July 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28431322/xanthohumol-and-8-prenylnaringenin-ameliorate-diabetic-related-metabolic-dysfunctions-in-mice
#13
Raquel Costa, Ilda Rodrigues, Luísa Guardão, Sílvia Rocha-Rodrigues, Carolina Silva, José Magalhães, Manuel Ferreira-de-Almeida, Rita Negrão, Raquel Soares
Type 2 diabetes mellitus (T2DM) is a chronic disease characterized by metabolic disturbances in specific tissues. The present work aimed to analyze the effects of xanthohumol (XN) and 8-prenylnaringenin (8PN), two beer-derived polyphenols, in liver and skeletal muscle lipid and glycolytic metabolism in T2DM mice model. Thirty C57Bl/6 mice were randomly divided into five groups: standard diet (control), high-fat diet (DM), high-fat diet plus ethanol (DM-Ethanol), high-fat diet plus 10 mg/L XN (DM-XN) and high-fat diet plus 10 mg/L 8PN (DM-8PN) during 20 weeks...
July 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28415750/xanthohumol-induces-paraptosis-of-leukemia-cells-through-p38-mitogen-activated-protein-kinase-signaling-pathway
#14
Xiangquan Mi, Chunming Wang, Chao Sun, Xu Chen, Xiang Huo, Yiming Zhang, Gang Li, Bo Xu, Jun Zhang, Jianxin Xie, Zhenhua Wang, Ji Li
Xanthohumol as a natural polyphenol demonstrates an anticancer activity, but its underlying mechanism remains unclear. In this study, we showed that xanthohumol (XN) induces paraptosis of leukemia cells. The paraptosis is one cell death which is characterized by dilation of the endoplasmic reticulum and/or mitochondria. The results demonstrated that XN treatment significantly inhibited cell proliferation and triggered extensive cytoplasmic vacuolation of HL-60 leukemia cells, but it did not cause the cleavage of caspase-3 protein or apoptosis...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28413193/effect-of-dietary-purified-xanthohumol-from-hop-humulus-lupulus-l-pomace-on-adipose-tissue-mass-fasting-blood-glucose-level-and-lipid-metabolism-in-kk-ay-mice
#15
Koki Takahashi, Kyoichi Osada
We previously showed that xanthohumol-rich hop extract (XRHE, ~18% xanthohumol) exerts anti-obesity effects in rats fed a high-fat diet through regulation of fatty acid metabolism. In this study, we examined the effects of dietary purified xanthohumol from XRHE (PX, ~91.9% xanthohumol) in KK-Ay mice in order to understand the anti-obesity effects of xanthohumol alone because XRHE contains 82% unknown compounds. Dietary consumption of PX significantly inhibited an increase in the visceral fat weight of mice compared to those fed control diet without PX...
May 1, 2017: Journal of Oleo Science
https://www.readbyqxmd.com/read/28330519/insecticidal-effects-of-extracts-of-humulus-lupulus-hops-l-cones-and-its-principal-component-xanthohumol
#16
T Aydin, N Bayrak, E Baran, A Cakir
Insecticidal effects of the dichloromethane, ethyl acetate, acetone, ethanol and methanol extracts of Humulus lupulus (hops) L. cones and its principal components, xanthohumol was investigated on five stored pests, Sitophilus granarius (L.), Sitophilus oryzae (L.), Acanthoscelides obtectus (Say.), Tribolium castaneum (Herbst) and Lasioderma serricorne (F.). The mortality of adults of the insects treated with 2, 5, 5, 10 and 20 mg ml̠-1 concentrations of the extracts and xanthuhumol was counted after 24, 48, 72, 96 and 120 h...
March 23, 2017: Bulletin of Entomological Research
https://www.readbyqxmd.com/read/28285192/xanthohumol-ameliorates-lipopolysaccharide-lps-induced-acute-lung-injury-via-induction-of-ampk-gsk3%C3%AE-nrf2-signal-axis
#17
Hongming Lv, Qinmei Liu, Zhongmei Wen, Haihua Feng, Xuming Deng, Xinxin Ci
Abundant natural flavonoids can induce nuclear factor-erythroid 2 related factor 2 (Nrf2) and/or AMP-activated protein kinase (AMPK) activation, which play crucial roles in the amelioration of various inflammation- and oxidative stress-induced diseases, including acute lung injury (ALI). Xanthohumol (Xn), a principal prenylflavonoid, possesses anti-inflammation and anti-oxidant activities. However, whether Xn could protect from LPS-induced ALI through inducing AMPK/Nrf2 activation and its downstream signals, are still poorly elucidated...
August 2017: Redox Biology
https://www.readbyqxmd.com/read/28188927/xanthohumol-isolated-from-humulus-lupulus-prevents-thrombosis-without-increased-bleeding-risk-by-inhibiting-platelet-activation-and-mtdna-release
#18
Guang Xin, Zeliang Wei, Chengjie Ji, Huajie Zheng, Jun Gu, Limei Ma, Wenfang Huang, Susan L Morris-Natschke, Jwu-Lai Yeh, Rui Zhang, Chaoyi Qin, Li Wen, Zhihua Xing, Yu Cao, Qing Xia, Ke Li, Hai Niu, Kuo-Hsiung Lee, Wen Huang
AIM: As the global population has reached 7 billion and the baby boom generation reaches old age, thrombosis has become the major contributor to the global disease burden. It has been reported that, in moderate doses, beer may protect against thrombosis. Xanthohumol (XN), an antioxidant, is found at high concentrations in hop cones (Humulus lupulus L.) and is a common ingredient of beer. Here, the aim of the present work was to investigate the effects of XN on antithrombotic and antiplatelet activities, and study its mechanism...
July 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28122154/protein-kinase-a-inhibition-facilitates-the-antitumor-activity-of-xanthohumol-a-valosin-containing-protein-inhibitor
#19
Yuki Shikata, Tetsuro Yoshimaru, Masato Komatsu, Hiroto Katoh, Reiko Sato, Shuhei Kanagaki, Yasumasa Okazaki, Shinya Toyokuni, Etsu Tashiro, Shumpei Ishikawa, Toyomasa Katagiri, Masaya Imoto
Xanthohumol (XN), a simple prenylated chalcone, can be isolated from hops and has the potential to be a cancer chemopreventive agent against several human tumor cell lines. We previously identified valosin-containing protein (VCP) as a target of XN; VCP can also play crucial roles in cancer progression and prognosis. Therefore, we investigated the molecular mechanisms governing the contribution of VCP to the antitumor activity of XN. Several human tumor cell lines were treated with XN to investigate which human tumor cell lines are sensitive to XN...
April 2017: Cancer Science
https://www.readbyqxmd.com/read/28105237/xanthohumol-inhibits-proliferation-of-laryngeal-squamous-cell-carcinoma
#20
Yan Li, Kai Wang, Shankai Yin, Hongliang Zheng, Daliu Min
Xanthohumol is a flavonoid compound that exhibits antioxidant and anticancer effects, and is used to treat atherosclerosis. The aim of the present study was to investigate the effect of xanthohumol on the cell proliferation of laryngeal squamous cell carcinoma and to understand the mechanism of its action. The effects of xanthohumol on the cell viability and apoptosis rate of laryngeal squamous cell carcinoma SCC4 cells were assessed by Annexin V-fluorescein isothiocyanate/propidium iodide staining. In addition, the expression levels of pro-apoptotic proteins, caspase-3, caspase-8, caspase-9, poly ADP ribose polymerase (PARP) p53 and apoptosis-inducing factor (AIF), as well as anti-apoptotic markers, B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia 1 (Mcl-1), were analyzed by western blotting...
December 2016: Oncology Letters
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