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Salih T Kaya, Omer Bozdogan, Talat O Ozarslan, Eylem Taskin, Didem Eksioglu, Firdevs Erim, Tulin Firat, Selcuk Yasar
CONTEXT: Cardiovascular dysfunctions such as life-threatening arrhythmias are one of the main reasons of mortality and morbidity in diabetic patients Objective: We aimed to investigate the long-term effects of resveratrol, berberine and glibenclamide combinations on the ischemia/reperfusion (I/R) induced arrhythmias in streptozotocin (STZ)-induced diabetic rats and to investigate the role of myocardial KATP channel in the possible anti-arrhythmic actions of the treatments. METHODS: Two days after induction of diabetes, diabetic rats were treated with resveratrol [5 mg/kg, intraperitoneally (i...
February 18, 2018: Archives of Physiology and Biochemistry
Ghaith Al-Badri, Gian Marco Leggio, Giuseppe Musumeci, Rubina Marzagalli, Filippo Drago, Alessandro Castorina
Dipeptidyl peptidase IV (DPP-IV) is a serine protease best known for its role in inactivating glucagon-like peptide-1 (GLP-1), pituitary adenylate cyclase-activating polypeptide (PACAP) and glucose-dependent insulinotropic peptide (GIP), three stimulators of pancreatic insulin secretion with beneficial effects on glucose disposal. Owing to the relationship between DPP-IV and these peptides, inhibition of DPP-IV enzyme activity is considered as an attractive treatment option for diabetic patients. Nonetheless, increasing studies support the idea that DPP-IV might also be involved in the development of neurological disorders with a neuroinflammatory component, potentially through its non-incretin activities on immune cells...
January 2018: Neural Regeneration Research
Raina Seupel, Yasmin Hemberger, Doris Feineis, Minjuan Xu, Ean-Jeong Seo, Thomas Efferth, Gerhard Bringmann
Two unique pentacyclic N,C-coupled naphthylisoquinolines, the ancistrocyclinones A (5) and B (6), were discovered in the Chinese liana Ancistrocladus tectorius. Furthermore, six known, likewise N,C-coupled alkaloids, viz., ancistrocladinium A (7a) and its mono- and bisphenolic analogs 8a and 9a were isolated, along with their atropo-diastereomers 7b, 8b, and 9b. The stereostructures of 5 and 6 were determined by HRESIMS, 1D and 2D NMR, oxidative degradation, and ECD calculations. The pentacyclic ancistrocyclinones A (5) and B (6) are structurally similar to berberine alkaloids - yet arising from a most different biosynthetic pathway: they are apparently formed by N,C-coupling of their polyketide-derived molecular halves, followed by oxidative cyclo-condensation...
February 14, 2018: Organic & Biomolecular Chemistry
M Amin, M Razi, F Sarrafzadeh-Rezaei, A Shalizar Jalali, G Najafi
The aim of this study was to uncover the protective effect of berberine (BBR), an antioxidant chemical, on experimental varicocele (VCL)-induced adverse effects on cell cycle machinery during early germ cells mitosis. To follow-up this study, 30 mature male Wistar rats were divided into control-sham, nontreated VCL, 50 mg kg-1and 100 mg kg-1BBR-treated VCL groups. Following 60 days, histological alterations were analysed by haematoxylin and eosin (H and E) staining, and expressions of cyclin-D1, cyclin-dependent kinase-4 (cdk4) and p21 were investigated by immunohistochemical (IHC) staining technique...
February 14, 2018: Andrologia
Priyanka Bhatnagar, Manisha Kumari, Richa Pahuja, A B Pant, Y Shukla, Pradeep Kumar, K C Gupta
To promote the specific targeting and elimination of CD44-positive cancer cells, berberine chloride (BRB)-encapsulated hyaluronic acid-grafted poly(lactic-co-glycolic acid) copolymer (BRB-d(HA)-g-PLGA) nanoparticles (NPs) were prepared. The targeted action of these NPs was compared to non-targeted BRB-loaded PLGA NPs and bulk BRB. The in vitro studies demonstrated faster release of BRB and increased cytotoxicity of BRB-d(HA)-g-PLGA NPs in Hela and MCF-7 cells in comparison to BRB-PLGA NPs and bulk BRB. The uptake of BRB-d(HA)-g-PLGA NPs was increased in case of MCF-7 cells as compared to HeLa cells owing to the higher expression of CD44 receptors on MCF-7 cells...
February 13, 2018: Drug Delivery and Translational Research
Rong Liu, Yonggang Zhang
Photoelectrocatalytic (PEC) system greatly improves the migration of photo-excited charges, retards the fast recombination of electron-hole and increases the lifetime of photo-generated holes. In this paper, we constructed a novel PEC system to degrade Berberine chloride form (BCF). XRD patterns indicated ageing time was an important condition for the crystal type of TiO 2 and the best proportion of anatase/rutile was 80/20. The band gap energy of the TiO 2 was 3.01 eV. We demonstrated that a synergistic effect existed between photocatalysis (PC) and electrocatalysis (EC)...
February 13, 2018: Photochemistry and Photobiology
Fawzi Mahomoodally, Shanoo Suroowan
Common auto-inflammatory disorders (CAIDs) induce considerable suffering over the world. A panoply of synthetic medications areis available for theirits management. Nonetheless, available drug classes are limited by adverse effects, low systemic absorption, and high costs. In addition, no cure exists for most CAIDs. Interestingly, herbal products present a tremendous potential for development as anti-inflammatory agents. In this endeavor, major scientific databases; Google Scholar, Pubmed, ScienceDirect, and Scopus were explored to highlight novel therapeutic approaches using herbal products for CAIDs prophylaxis, management, treatment, and prevention of relapse...
February 12, 2018: Combinatorial Chemistry & High Throughput Screening
Jin Liu, Xiaodan Zhao, Dandan Pei, Guo Sun, Ye Li, Chunhui Zhu, Cui Qiang, Junyi Sun, Jianfeng Shi, Yan Dong, Jianzhong Gou, Sicen Wang, Ang Li
Coptidis Rhizoma binds to the membrane receptors on hPDLSC/CMC, and the active ingredient Berberine (BER) that can be extracted from it may promote the proliferation and osteogenesis of periodontal ligament stem cells (hPDLSC). The membrane receptor that binds with BER on the cell surface of hPDLSC, the mechanism of direct interaction between BER and hPDLSC, and the related signal pathway are not yet clear. In this research, EGFR was screened as the affinity membrane receptor between BER and hPDLSC, through retention on CMC, competition with BER and by using a molecular docking simulation score...
February 12, 2018: Scientific Reports
Johannes Delp, Simon Gutbier, Stefanie Klima, Lisa Hoelting, Kevin Pinto-Gil, Jui-Hua Hsieh, Michael Aichem, Karsten Klein, Falk Schreiber, Raymond R Tice, Manuel Pastor, Mamta Behl, Marcel Leist
The (developmental) neurotoxicity hazard is still unknown for most chemicals. Establishing a test battery covering most of the relevant adverse outcome pathways may close this gap, without requiring a huge animal experimentation program. Ideally, each of the assays would cover multiple mechanisms of toxicity. One candidate test is the human LUHMES cell-based NeuriTox test. To evaluate its readiness for larger-scale testing, a proof of concept library assembled by the U.S. National Toxicology Program (NTP) was screened...
January 21, 2018: ALTEX
Chinedu Ochin, Mahdi Garelnabi
BACKGROUND: The developments of new parenteral approaches to target PCSK-9 for the treatment LDL-Cholesterol has yielded impressive results; and have shown significant decreases in the risk of mortality associated with hypercholesterolemia. However improved and convenient alternate approaches that exploit the beneficial drug target properties of PCSK-9 also need to be explored and developed. One such approach is the oral administration of Berberine using nanotechnology. METHODS: Nanoprecipitation encapsulation and physiochemical characterization of Berberine Chloride in PLGA-PEG-PLGA block copolymer has been developed and characterized in Hep-G2 cells using Berberine Chloride encapsulated nanoparticle (BC-NP)...
February 1, 2018: Cardiovascular & Hematological Disorders Drug Targets
Sangmin Kim, Jeongmin Lee, Daeun You, Yisun Jeong, Myeongjin Jeon, Jonghan Yu, Seok Won Kim, Seok Jin Nam, Jeong Eon Lee
BACKGROUND/AIMS: Transforming growth factor-beta proteins (TGF-βs) are multifunctional growth factors and powerful modulators of the epithelial-mesenchymal transition (EMT) in a variety of cancer types including breast and lung cancer cells. Here, we demonstrated the inhibitory effect of berberine (BBR) on tumor growth and metastasis of triple negative breast cancer (TNBC) cells via suppression of TGF-β1 expression. METHODS: The levels of mRNA expression were analyzed by real-time PCR...
January 31, 2018: Cellular Physiology and Biochemistry
Emanuele Porru, Placido Franco, Donato Calabria, Silvia Spinozzi, Marinella Roberti, Cristiana Caliceti, Aldo Roda
Berberine (BBR) is a natural alkaloid obtained from Berberis species plants, known for its protective effects against several diseases. Among the primary BBR metabolites, berberrubine (M1) showed the highest plasma concentration but few and conflicting data are available regarding its concentration in biological fluids related to its new potential activity on vascular cells. A combined analytical approach was applied to study biodistribution of M1 in comparison with BBR. The optimization of sample clean-up combined with a fully validated HPLC-ESI-MS/MS tailored for M1 allows sufficient detectability and accuracy to be reached in the different studied organs even when administered at low dose, comparable to that assumed by human...
February 7, 2018: Analytical and Bioanalytical Chemistry
Chunge Guan, Simiao Qiao, Qi Lv, Na Cao, Kai Wang, Yue Dai, Zhifeng Wei
Berberine has been demonstrated to alleviate renal interstitial, liver and myocardial fibrosis when administered orally despite its extremely low bioavailability. Here, we inspected effect of berberine on pulmonary fibrosis (PF) and explored underlying mechanisms on the basis of intestinal endocrine. The results showed that either oral or rectal administration of berberine exhibited marked alleviation of bleomycin-induced PF in mice. In contrast, anti-PF activity of berberine disappeared when given by an intravenous injection, implying that it functioned in a gut-dependent manner...
February 3, 2018: Toxicology and Applied Pharmacology
Awantika Singh, Vikas Bajpai, Sunil Kumar, Ajay Kumar Singh Rawat, Brijesh Kumar
Mahonia leschenaultia (ML) and Mahonia napaulensis (MN) are less known and unexplored medicinal plants of the family Berberidaceae. They are used by the Todas of Nilgiris in their religious and medical practices but chemically less identified. Hence, we decided to do extensive phytochemical analysis to explore the potential of these plant extracts. An ultrahigh performance electrospray tandem mass spectrometry (UHPLC-ESI-MS/MS) method was successfully developed for qualitative analysis of the bioactive components in Mahonia species using Orbitrap Velos Pro mass spectrometer...
April 2017: Journal of Pharmaceutical Analysis
Lixin Wang, Hao Ma, Yan Xue, Haiyan Shi, Teng Ma, Xiaozheng Cui
Myocardial ischemia-reperfusion injury is one of the most common cardiovascular diseases, and can lead to serious damage and dysfunction of the myocardial tissue. Previous studies have demonstrated that berberine exhibits ameliorative effects on cardiovascular disease. The present study further investigated the efficacy and potential mechanism underlying the effects of berberine on ischemia-reperfusion injury in a mouse model. Inflammatory markers were measured in the serum and levels of inflammatory proteins in myocardial cells were investigated after treatment with berberine...
February 2018: Experimental and Therapeutic Medicine
Hong-Cai Wang, Bo-Ding Wang, Mao-Song Chen, Hai Chen, Cheng-Feng Sun, Gang Shen, Jian-Min Zhang
The aim of the present study was to assess the neuroprotective effect of berberine against learning and memory deficits in diffuse axonal injury (DAI). DAI rats were orally gavaged with berberine at a dose of 200 mg/kg of body weight for 4 weeks. Behavioral tests were used to analyze the neuroprotective effect of berberine against DAI-induced learning and memory deficits. In the present study, treatment with berberine significantly protected against DAI-induced inhibition of learning and memory in rats. Notably, berberine significantly suppressed the levels of tumor necrosis factor, interleukin-1β and monocyte chemoattractant protein-1, as well as reduced the protein expression levels of nuclear factor-κB, Bcl-2-associated X protein and cytochrome c in DAI rats...
January 2018: Experimental and Therapeutic Medicine
Manuel Benedetti, Ilaria Verrascina, Daniela Pontiggia, Federica Locci, Benedetta Mattei, Giulia De Lorenzo, Felice Cervone
Recognition of endogenous molecules acting as "damage-associated molecular patterns" (DAMPs) is a key feature of immunity in both animals and plants. Oligogalacturonides (OGs), i.e. fragments derived from the hydrolysis of homogalacturonan, a major component of pectin are a well-known class of DAMPs that activate immunity and protect plants against several microbes. However, hyper-accumulation of OGs severely affects growth, eventually leading to cell death and clearly pointing to OGs as players in the growth-defence trade-off...
February 3, 2018: Plant Journal: for Cell and Molecular Biology
Wei-Wei Gao, Lavanya Gopala, Rammohan R Yadav Bheemanaboina, Guo-Biao Zhang, Shuo Li, Cheng-He Zhou
Aminothiazolyl berberine derivatives as potentially antimicrobial agents were designed and synthesized in an effort to overcome drug resistance. The antimicrobial assay revealed that some target compounds exhibited significantly inhibitory efficiencies toward bacteria and fungi including drug-resistant pathogens, and the aminothiazole and Schiff base moieties were helpful structural fragments for aqueous solubility and antibacterial activity. Especially, aminothiazolyl 9-hexyl berberine 9c and 2,4-dichlorobenzyl derivative 18a exhibited good activities (MIC = 2 nmol/mL) against clinically drug-resistant Gram-negative Acinetobacter baumanii with low cytotoxicity to hepatocyte LO2 cells, rapidly bactericidal effects and quite slow development of bacterial resistance toward A...
January 12, 2018: European Journal of Medicinal Chemistry
Qiang Wan, Zhongyong Liu, Yuping Yang, Xiaobing Cui
Berberine (BBR) possesses significant anti-atherosclerosis properties. Visfatin is one of the most promising biomarkers of incoming atherosclerosis. However, research on the effect of BBR on regulating visfatin expression in atherogenesis remains largely unknown. In this study, we investigated the effects of BBR on visfatin expression and atherogenesis in apolipoprotein E knockout (ApoE-/-) mice. The effect of BBR on attenuating visfatin-induced endothelial dysfunction was also evaluated in cultured human umbilical vein endothelial cells (HUVECs)...
January 30, 2018: International Journal of Molecular Medicine
Lin Wang, Yanqing Wen, Fanhao Meng
A simple, rapid and sensitive method using UPLC-MS/MS was established and validated for simultaneous determination of gelsemine and koumine in rat plasma after oral administration of Gelsemium elegans Benth extract. Plasma was performed with methanol precipitation and berberine was chosen as the internal standard. Plasma samples were separated on an ACQUITY UPLC® BEH C18 column (3.0×50mm, 1.7μm) with gradient elution using acetonitrile and 0.1% formic acid aqueous solution as the mobile phase at a flow rate of 0...
January 31, 2018: Biomedical Chromatography: BMC
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