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Berberin

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https://www.readbyqxmd.com/read/29158264/azole-resistance-in-a-candida-albicans-mutant-lacking-the-abc-transporter-cdr6-roa1-depends-on-tor-signaling
#1
Nitesh Kumar Khandelwal, Neeraj Chauhan, Parijat Sarkar, Brooke D Esquivel, Paola Coccetti, Ashutosh Singh, Alix T Coste, Meghna Gupta, Dominique Sanglard, Theodore C White, Murielle Chauvel, Christophe dEnfert, Amitabha Chattopadhyay, Naseem A Gaur, Alok Kumar Mondal, Rajendra Prasad
ATP-binding cassette (ABC) transporters help export various substrates across the cell membrane and significantly contribute to drug resistance. However, a recent study reported an unusual case in which the loss of an ABC transporter in Candida albicans, orf19.4531 (previously named ROA1), increases resistance against antifungal azoles, which was attributed to an altered membrane potential in the mutant strain. To get further mechanistic insights into this phenomenon, here we confirmed that the plasma membrane localized transporter (renamed CDR6/ROA1 for consistency with C...
November 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29154866/activation-of-igf-1-igfbp-3-signaling-by-berberine-improves-intestinal-mucosal-barrier-of-rats-with-acute-endotoxemia
#2
Yan He, Xiaoming Yuan, Guangrong Zhou, Aiwen Feng
Insulin-like growth factor I (IGF-I) and binding protein 3 (IGFBP-3) play a role in the maintenance of gut mucosal barrier function. Nevertheless, IGF-I/IGFBP-3 and tight junction protein (TJP) expression in small intestinal mucosa are often impaired during endotoxemia. In this model of acute endotoxemia, the regulatory effect of berberine on IGF-I/IGFBP-3 and TJP expression in ileal mucosa was evaluated. The findings revealed systemic injection of lipopolysaccharide (LPS) suppressed mRNA and protein expression of IGF-I and IGFBP-3, but berberine ameliorated their production...
November 14, 2017: Fitoterapia
https://www.readbyqxmd.com/read/29148767/role-of-the-benzodioxole-group-in-the-interactions-between-the-natural-alkaloids-chelerythrine-and-coptisine-and-the-human-telomeric-g-quadruplex-dna-a-multiapproach-investigation
#3
F Papi, M Ferraroni, R Rigo, S Da Ros, C Bazzicalupi, C Sissi, P Gratteri
The binding properties toward the human telomeric G-quadruplex of the two natural alkaloids coptisine and chelerythrine were studied using spectroscopic techniques, molecular modeling, and X-ray diffraction analysis. The results were compared with reported data for the parent compounds berberine and sanguinarine. Spectroscopic studies showed modest, but different rearrangements of the DNA-ligand complexes, which can be explained considering particular stereochemical features for these alkaloids, in spite of the similarity of their skeletons...
November 17, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/29143794/berberine-activates-aryl-hydrocarbon-receptor-but-suppresses-cyp1a1-induction-through-mir-21-3p-stimulation-in-mcf-7-breast-cancer-cells
#4
Sheng-Nan Lo, Chun-Wei Wang, Yueh-Shieh Chen, Chiung-Chiao Huang, Tian-Shung Wu, Lih-Ann Li, I-Jung Lee, Yune-Fang Ueng
Berberine and the methylenedioxy ring-opening derivatives palmatine and jatrorrhizine are active ingredients in immunomodulatory plants, such as goldenseal. This study aimed to illustrate the effects of protoberberines on aryl hydrocarbon receptor (AhR) activation and cytochrome P450 (CYP) 1 in the estrogen receptor (ER)α(+) MCF-7 breast cancer cells. Among protoberberines at non-cytotoxic concentrations (≤10 μM), berberine had the most potent and statistically significant effects on AhR activation and CYP1A1/1A2/1B1 mRNA induction...
October 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29143468/predictive-qsar-modeling-study-on-berberine-derivatives-with-hypolipidemic-activity
#5
Pan Yu, Dongdong Li, Junjun Ni, Linguo Zhao, Gang Ding, Zhenzhong Wang, Wei Xiao
Berberine (BBR) isolated from a Chinese herb, is identified as a new cholesterol-lowering small molecule, and hundreds of berberine derivatives have been obtained for optimization of their hypolipidemic activities in recent years. However, so far there is no available quantitative structure-activity relationship (QSAR) model used for the development of novel BBR analogs with hypolipidemic activities, mainly due to lack of lipid-lowering molecular mechanisms and target identification of BBR. In this paper, the tactics using ligand efficiency indices instead of pIC50 as the activity could be adopted for the development of BBR QSAR models...
November 16, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29142419/antipsoriatic-and-anti-inflammatory-studies-of-berberis-aristata-extract-loaded-nanovesicular-gels
#6
Nimisha, Dilshad Ali Rizvi, Zeeshan Fatima, Neema, Chanchal Deep Kaur
Objective: Novel nanovesicular gel of Berberis aristata extract was developed and evaluated for its anti-inflammatory and antipsoriatic activity. Materials and Methods: Transferosomes were prepared using soya phosphatidylcholine and edge activators (Tween 80, Span 80, and sodium deoxycholate) by a modified lipid film hydration technique using rotary evaporator and evaluated for various parameters. The quantification and standardization of extract have been carried out using its alkaloid content as berberine as biomarker...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29138445/inhibition-activity-of-a-traditional-chinese-herbal-formula-huang-lian-jie-du-tang-and-its-major-components-found-in-its-plasma-profile-on-neuraminidase-1
#7
Xuelin Zhou, Haotian Li, Zhilong Shi, Sijia Gao, Shizhang Wei, Kun Li, Jiabo Wang, Jianyu Li, Ruilin Wang, Man Gong, Yanling Zhao, Xiaohe Xiao
Huang-Lian-Jie-Du-Tang (HLJDT), a traditional formula with four TCM herbs, has been used for hundred years for different diseases. The current study aimed to assess the inhibitory activity of HLJDT against H1N1 neuraminidase (NA-1), and identify potent NA-1 inhibitors from its plasma profile. The in vitro NA-1 study has shown that the water extract of HLJDT potently inhibited NA-1 (IC50 = 112.6 μg/ml; Ki = 55.6 μg/ml) in a competitive mode. The IC50 values of the water extracts of its four herbs were as follows: Coptidis Rhizoma, 96...
November 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29138118/8-cetylberberine-inhibits-growth-of-lung-cancer-in-vitro-and-in-vivo
#8
Yubo Xiao, Cheng Tian, Tao Huang, Bing Han, Meimei Wang, Hang Ma, Zhaoxing Li, Xiaoli Ye, Xuegang Li
AIMS: This study is aimed at detecting the anti-tumor efficacy of a new berberine (BBR) derivative 8-cetylberberine (HBBR), which has a significant improvement in hydrophobicity and pharmacological effects compared to BBR. MAIN METHODS: The human non-small lung cancer cell line A549 and normal human lung epithelial cells (MRC-5) were cultured to observe inhibition in vitro. Cell viability was analyzed via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay...
November 11, 2017: Life Sciences
https://www.readbyqxmd.com/read/29138046/novel-cremochylomicrons-for-improved-oral-bioavailability-of-the-antineoplastic-phytomedicine-berberine-chloride-optimization-and-pharmacokinetics
#9
Manal A Elsheikh, Yosra S R Elnaggar, Dalia A Hamdy, Ossama Y Abdallah
Berberine chloride (BER) is an antineoplastic phytomedicine that combat non-Hodgkin lymphoma. BER suffers from low oral bioavailability due to p-glycoprotein efflux and first-pass metabolism. Lymphatic drug targeting recently gained a profound attention due to circumventing hepatic first-pass metabolism and targeting lymph diseases. Therefore, novel BER-loaded cremochylomicrons were elaborated to mitigate BER drawbacks and enhance its lymphatic targeting and bioavailability. Optimized cremochylomicron was prepared with 2...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29133786/heterogeneity-in-the-drosophila-gustatory-receptor-complexes-that-detect-aversive-compounds
#10
Ha Yeon Sung, Yong Taek Jeong, Ji Yeon Lim, Hyeyon Kim, Soo Min Oh, Sun Wook Hwang, Jae Young Kwon, Seok Jun Moon
Animals must detect aversive compounds to survive. Bitter taste neurons express heterogeneous combinations of bitter receptors that diversify their response profiles, but this remains poorly understood. Here we describe groups of taste neurons in Drosophila that detect the same bitter compounds using unique combinations of gustatory receptors (GRs). These distinct complexes also confer responsiveness to non-overlapping sets of additional compounds. While either GR32a/GR59c/GR66a or GR22e/GR32a/GR66a heteromultimers are sufficient for lobeline, berberine, and denatonium detection, only GR22e/GR32a/GR66a responds to strychnine...
November 14, 2017: Nature Communications
https://www.readbyqxmd.com/read/29133053/synthesis-and-biological-evaluation-of-new-berberine-derivatives-as-cancer-immunotherapy-agents-through-targeting-ido1
#11
Yan-Xiang Wang, Wei-Qiang Pang, Qing-Xuan Zeng, Zhe-Song Deng, Tian-Yun Fan, Jian-Dong Jiang, Hong-Bin Deng, Dan-Qing Song
To discover small-molecule cancer immunotherapy candidates through targeting Indoleamine 2,3-dioxygenase 1 (IDO1), twenty-five new berberine (BBR) derivatives defined with substituents on position 3 or 9 were synthesized and examined for repression of IFN-γ-induced IDO1 promoter activities. Structure-activity relationship (SAR) indicated that large volume groups at the 9-position might be beneficial for potency. Among them, compounds 2f, 2i, 2n, 2o and 8b exhibited increased activities, with inhibition rate of 71-90% compared with BBR...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29132092/berberine-attenuates-cognitive-impairment-and-ameliorates-tau-hyperphosphorylation-by-limiting-the-self-perpetuating-pathogenic-cycle-between-nf-%C3%AE%C2%BAb-signaling-oxidative-stress-and-neuroinflammation
#12
Wenbo He, Chuanling Wang, Yi Chen, Yongli He, Zhiyou Cai
BACKGROUND: Berberine (BBR) plays an important role in the prevention and treatment of Alzheimer's disease (AD). The present work was to explore whether BBR ameliorates cognitive deficits in AD and to investigate whether its underlying mechanism involves inhibiting hyperphosphorylated tau protein. METHODS: The cognitive function was measured by the Morris water maze (MWM) test. The levels of hyperphosphorylated tau proteins were determined by Western blot. The biomarkers of NF-κB signaling pathway and oxidative stress were detected by Western blot and biochemical assays...
June 15, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29130448/a-review-on-the-effects-of-current-chemotherapy-drugs-and-natural-agents-in-treating-non-small-cell-lung-cancer
#13
Chih-Yang Huang, Da-Tong Ju, Chih-Fen Chang, P Muralidhar Reddy, Bharath Kumar Velmurugan
Lung cancer is the leading cause of cancer deaths worldwide, and this makes it an attractive disease to review and possibly improve therapeutic treatment options. Surgery, radiation, chemotherapy, targeted treatments, and immunotherapy separate or in combination are commonly used to treat lung cancer. However, these treatment types may cause different side effects, and chemotherapy-based regimens appear to have reached a therapeutic plateau. Hence, effective, better-tolerated treatments are needed to address and hopefully overcome this conundrum...
December 2017: BioMedicine
https://www.readbyqxmd.com/read/29125225/baicalein-reduces-oxidative-stress-in-cho-cell-cultures-and-improves-recombinant-antibody-productivity
#14
Tae Kwang Ha, Anders Holmgaard Hansen, Stefan Kol, Helene Faustrup Kildegaard, Gyun Min Lee
Oxidative stress that naturally accumulates in the endoplasmic reticulum (ER) as a result of mitochondrial energy metabolism and protein synthesis can disturb the ER function. Because ER has a responsibility on the protein synthesis and quality control of the secreted proteins, ER homeostasis has to be well maintained. When H2O2, an oxidative stress inducer, was added to recombinant Chinese hamster ovary (rCHO) cell cultures, it reduced cell growth, monoclonal antibody (mAb) production, and galactosylated form of mAb in a dose-dependent manner...
November 10, 2017: Biotechnology Journal
https://www.readbyqxmd.com/read/29124775/capillary-hplc-with-tandem-mass-spectrometry-in-analysis-of-alkaloid-dyestuffs-a-new-approach
#15
Damian Dąbrowski, Katarzyna Lech, Maciej Jarosz
Development of the identification method of alkaloid compounds in Amur cork tree as well as not examined so far Oregon grape and European Barberry shrubs is presented. The novel approach to separation of alkaloids was applied and the capillary-high-performance liquid chromatography (capillary-HPLC) system was used, which has never previously been reported for alkaloid-based dyestuffs analysis. Its optimization was conducted with three different stationary phases (unmodified octadecylsilane-bonded silica, octadecylsilane modified with polar groups and silica-bonded pentaflourophenyls) as well as with different solvent buffers...
November 10, 2017: Electrophoresis
https://www.readbyqxmd.com/read/29121795/berberine-ameliorates-diabetic-neuropathy-trpv1-modulation-by-pkc-pathway
#16
Yan Zan, Cui-Xing Kuai, Zhi-Xia Qiu, Fang Huang
In recent years, berberine has increasingly become a topic of research as a treatment for diabetes due to its repair function, which recovers damaged pancreatic β cells. However, it is the complications of diabetes that seriously affect patients' life quality and longevity, among which diabetic neuropathy and the consequent acute pain are the most common. In this study, we established STZ-induced diabetic models to observe whether berberine, a main constitute of Coptis chinensis Franch which has shown good hypoglycemic effects, could relieve diabetes-induced pain and explored its possible mechanism in rats and mice...
November 9, 2017: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29118901/impacts-of-berberine-on-oxidized-ldl-induced-proliferation-of-human-umbilical-vein-endothelial-cells
#17
Rui-Xia Xu, Xian-Chang Sun, Chun-Yan Ma, Yu-Hong Yao, Xiao-Lin Li, Yuan-Lin Guo, Yan Zhang, Sha Li, Jian-Jun Li
Berberine (BBR), a Chinese medicine extracted from natural plant, has been demonstrated to improve lipid disorders. Oxidized low-density lipoprotein (oxLDL), a proatherogenic lipoprotein, has been shown to be involved in vascular endothelial cell dysfunction such as excessive or abnormal proliferation. The purpose of the present study was to investigate the impacts of BBR on cell proliferations as well as potential involving signal pathways. HUVECs were stimulated with oxLDL and co-cultured with BBR at a variety of concentrations in different time points...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/29117131/natural-deep-eutectic-solvents-nades-to-enhance-berberine-absorption-an-in-vivo-pharmacokinetic-study
#18
Stefania Sut, Marta Faggian, Valeria Baldan, Gabriele Poloniato, Ignazio Castagliuolo, Iztok Grabnar, Beatrice Perissutti, Paola Brun, Filippo Maggi, Dario Voinovich, Gregorio Peron, Stefano Dall'Acqua
In the present study results related to the in vivo administration of Natural Deep Eutectic Solvents (NADES)-solubilized berberine are reported for the first time. NADES are mixtures of small natural compounds having a melting point significantly lower than that of any individual component. Such solvents have gained much attention of the scientific community in the green chemistry area, being considered useful alternatives to common organic solvents. NADES can be used also as administration vehicles, and this can be attractive for nutraceutical products when eutectics are formed with food grade ingredients...
November 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29115406/berberine-prevents-the-apoptosis-of-mouse-podocytes-induced-by-traf5-overexpression-by-suppressing-nf-%C3%AE%C2%BAb-activation
#19
Feng Wu, Dong-Sheng Yao, Tian-Ying Lan, Chen Wang, Jian-Dong Gao, Li-Qun He, Di Huang
Berberine (BBR) has previously been found to exert beneficial effects on renal injury in experimental rats. However, the mechanisms underlying these effects are not yet fully understood. Tumor necrosis factor (TNF) receptor-associated factor 5 (TRAF5) has been demonstrated to mediate the activation of nuclear factor-κB (NF-κB), which has been implicated in the pathogenesis of chronic kidney disease (CKD). The aim of this study was to investigate the effects of BBR on kidney injury and the activation of the NF-κB signaling pathway in mouse podocytes...
November 7, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29113353/berberine-targeted-mir-21-chemosensitizes-oral-carcinomas-stem-cells
#20
Che-Yi Lin, Pei-Ling Hsieh, Yi-Wen Liao, Chih-Yu Peng, Ming-Yi Lu, Ching-Hsuan Yang, Cheng-Chia Yu, Chia-Ming Liu
Cancer recurrence and chemoresistance are two major obstacles to the treatment of oral squamous cell carcinomas (OSCC). And cancer stem cells (CSCs) have been found to possess tumor initiating, self-renewal and metastasis abilities, resulting in the relapse and chemoresistance of OSCC. In the present study, we investigated the anti-CSCs effect of berberine, a phenanthrene alkaloid isolated from the Berberis genus. Our results demonstrated that berberine dose dependently downregulated the oncogenicity in vitro, including ALDH1 activity, self-renewal property, and colony formation and invasion abilities as well as potentiated chemosensitivity of OSCC-CSCs...
October 6, 2017: Oncotarget
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