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Berberine

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https://www.readbyqxmd.com/read/28339024/effects-of-berberine-on-a-rat-model-of-chronic-stress-and-depression-via-gastrointestinal-tract-pathology-and-gastrointestinal-flora-profile-assays
#1
Xiaohui Zhu, Yangdong Sun, Chenggang Zhang, Haifeng Liu
Chronic stress and depression are challenging conditions to treat, owing to their complexity and lack of clinically available and effective therapeutic agents. The aim of the present study was to investigate the mechanism by which berberine acts, by examining alterations to gastrointestinal tract histopathology and flora profile in a rat model, following the induction of stress. Research associating gastrointestinal flora and depression has increased, thus, the present study hypothesized that stress induces depression and changes in the gastrointestinal system...
March 22, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28325147/berberine-derivatives-with-different-pharmacological-activities-via-structural-modifications
#2
Daipeng Xiao, Zhenbao Liu, Shanshan Zhang, Mi Zhou, Fen He, Ming Zou, Junying Peng, Xiong Xie, Yanfei Liu, Dongming Peng
Berberine, a quaternary ammonium protoberberine alkaloid with an isoquinoline scaffold isolated from medicinal herbs, exhibits a wide spectrum of pharmacological activities. Berberine has been used in traditional Chinese medicine and Ayurvedic medicine. However, it has poor bioavailability, which seriously limits its application and development. The chemical transformation of natural products is an effective method to improve pharmacological activities. Researches have been carried out on the modification of berberine to obtain better pharmacological properties...
March 21, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28323035/naturally-occurring-anti-cancer-agents-targeting-ezh2
#3
Fahimeh Shahabipour, Michele Caraglia, Muhammed Majeed, Giuseppe Derosa, Pamela Maffioli, Amirhossein Sahebkar
Natural products are considered as promising tools for the prevention and treatment of cancer. The enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase unit of polycomb repressor complexes such as PRC2 complex that has oncogenic roles through interference with growth and metastatic potential. Several agents targeting EZH2 has been discovered but they often induce side effects in clinical trials. Recently, EZH2 has emerged as a potential target of natural products with documented anti-cancer effects and this discloses a new scenario for the development of EZH2 inhibitory strategies with agents with low cytotoxic detrimental effects...
March 17, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28318534/a-multidrug-and-toxic-compound-extrusion-transporter-mediates-berberine-accumulation-into-vacuoles-in-coptis-japonica
#4
Kojiro Takanashi, Yasuyuki Yamada, Takayuki Sasaki, Yoko Yamamoto, Fumihiko Sato, Kazufumi Yazaki
Plants produce a large variety of alkaloids, which have diverse chemical structures and biological activities. Many of these alkaloids accumulate in vacuoles. Although some membrane proteins on tonoplasts have been identified as alkaloid uptake transporters, few have been characterized to date, and relatively little is known about the mechanisms underlying alkaloid transport and accumulation in plant cells. Berberine is a model alkaloid. Although all genes involved in berberine biosynthesis, as well as the master regulator, have been identified, the gene responsible for the final accumulation of berberine at tonoplasts has not been determined...
March 16, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28317482/nutraceuticals-as-an-important-part-of-combination-therapy-in-dyslipidaemia
#5
Angelo Maria Patti, Peter P Toth, Rosaria Vincenza Giglio, Maciej Banach, Marcello Noto, Dragana Nikolic, Giuseppe Montalto, Manfredi Rizzo
Several risk factors such as abnormality of lipid metabolism (e.g. high levels of low-density lipoprotein cholesterol (LDL-C), elevated triglycerides and low levels of high-density lipoprotein cholesterol (HDL-C)) play a central role in the aetiology of cardiovascular disease (CVD). Nutraceutical combination together with a cholesterol-lowering action, when associated with suitable lifestyle, should furnish an alternative to pharmacotherapy in patients reporting statin-intolerance and in subjects at low cardiovascular risk...
March 17, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28317281/comparison-of-dietary-polyphenols-for-protection-against-molecular-mechanisms-underlying-non-alcoholic-fatty-liver-disease-in-a-cell-model-of-steatosis
#6
Hossein Rafiei, Kosar Omidian, Brian Bandy
SCOPE: Dietary polyphenols have shown promise in protecting the liver against non-alcoholic fatty liver disease. The relative effectiveness and mechanisms of different polyphenols however is mostly unknown. METHODS AND RESULTS: In a model of steatosis using HepG2 hepatocytes, we evaluated the protective effects of different classes of polyphenols and the contributing mechanisms. Treatment of the cells with oleic acid increased ROS generation and expression of TNFα, decreased expression of UCP2 and decreased mitochondrial content and markers of biogenesis...
March 20, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28302402/novel-benzimidazolyl-tetrahydroprotoberberines-design-synthesis-antimicrobial-evaluation-and-multi-targeting-exploration
#7
Ponmani Jeyakkumar, Han-Bo Liu, Lavanya Gopala, Yu Cheng, Xin-Mei Peng, Rong-Xia Geng, Cheng-He Zhou
A series of novel benzimidazolyl tetrahydroprotoberberines were conveniently designed and efficiently synthesized from berberine via direct cyclization of tetrahydroprotoberberine aldehyde and o-phenylene diamines under metal-free aerobic oxidation. All the new compounds were characterized by IR, (1)H NMR, (13)C NMR and HRMS spectra. The antimicrobial evaluation revealed that the 5-fluorobenzimidazolyl derivative 5b was the most active antibacterial and antifungal molecule with broad spectrum in comparison to Berberine, Chloromycin, Norfloxacin and Fluconazole...
February 28, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28298333/multiple-ampk-activators-inhibit-l-carnitine-uptake-in-c2c12-skeletal-muscle-myotubes
#8
Andy Shaw, Stewart Jeromson, Kenneth R Watterson, John D Pediani, Iain Gallagher, Tim Whalley, Gillian Dreczkowski, Naomi Brooks, Stuart Galloway, D Lee Hamilton
Mutations in the gene that encodes the principal L-Carnitine transporter, OCTN2, can lead to a reduced intracellular L-Carnitine pool and the disease Primary Carnitine Deficiency. L-Carnitine supplementation is used therapeutically to increase intracellular L-Carnitine. As AMPK and insulin regulate fat metabolism and substrate uptake we hypothesised that AMPK activating compounds and insulin would increase L-Carnitine uptake in C2C12 myotubes. The cells express all three OCTN transporters at the mRNA level and immunohistochemistry confirmed expression at the protein level...
March 15, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28298174/the-involvement-of-multidrug-and-toxin-extrusion-protein-1-in-the-distribution-and-excretion-of-berberine
#9
Ling Xiao, Yaru Xue, Cuifeng Zhang, Le Wang, Yunfei Lin, Guoyu Pan
1. Berberine (BBR), an isoquinoline alkaloid, has demonstrated multiple clinical pharmacological actions. As a substrate of multiple transporters in the liver, BBR is rarely excreted into the bile but can be found in the urine. The purpose of the present study was to investigate the role of multidrug and toxin extrusion protein 1 (MATE1) in the transport of BBR in the liver and kidney. 2. Using human MATE1 (hMATE1)-transfected HEK293 cells, BBR was shown to be a substrate of hMATE1 (Km = 4.28 ± 2.18 μM)...
March 16, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28295319/preparation-pharmacokinetics-and-tumour-suppressive-activity-of-berberine-liposomes
#10
Xinghui Wang, Qiong Wang, Zhihui Liu, Xiao Zheng
OBJECTIVES: Berberine (BBR) has shown promising antitumour effects in vitro. However, intravenous administration of BBR solution is complicated by lethal adverse cardiovascular effects. The aim of this study was to prepare common and polyethylene glycol (PEG)-modified long-circulating BBR liposomes and evaluate their efficacy and safety as potential antitumour agents. METHODS: Physiochemical properties of common and long-circulating BBR liposomes were characterized including particle size, Zeta potential and thermal stability...
March 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28290706/the-metabolism-of-berberine-and-its-contribution-to-the-pharmacological-effects
#11
Kun Wang, Xinchi Feng, Liwei Chai, Shijie Cao, Feng Qiu
Berberine, a bioactive alkaloid isolated from several herbal substances, possesses multiple pharmacological effects, including antimicrobial, anti-diabetic, anti-cancer activities. Meanwhile, berberine undergoes extensive metabolism after oral administration which results in its extremely low plasma exposure. Therefore, it is believed that the metabolites of berberine also contribute a lot to its pharmacological effects. Along these lines, this review covers the metabolism studies of berberine in terms of its metabolic pathways and metabolic organs based on the identified metabolites, and it also covers the pharmacological activities of its active metabolites...
March 14, 2017: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/28286134/berberine-bioisostere-q8-compound-stimulates-osteoblast-differentiation-and-function-in-vitro
#12
Younho Han, Yifeng Jin, Sung Ho Lee, Daulat Bikram Khadka, Won-Jea Cho, Kwang Youl Lee
The Q8 compound is a unique derivative of berberine. The present study investigated the functional role of Q8 to evaluate its potential for use in bone regeneration, especially in osteoblast differentiation. The safe concentration of Q8 increased BMP4-induced alkaline phosphatase (ALP) activity, and induced RNA expression of ALP, bone sialoprotein (BSP), and osteocalcin (OC). The activities of ALP-, BSP- and OC-luciferase reporters were also increased by Q8. During osteoblast differentiation, Q8 stabilized the Runx2 and Osterix protein abundance by blocking the ubiquitin-proteasome pathway, which in turn promoted Runx2 and Osterix induced transcriptional activity and subsequently increased the osteoblast differentiation...
March 7, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28283780/metabolic-carbonyl-reduction-of-anthracyclines-role-in-cardiotoxicity-and-cancer-resistance-reducing-enzymes-as-putative-targets-for-novel-cardioprotective-and-chemosensitizing-agents
#13
REVIEW
Kamil Piska, Paulina Koczurkiewicz, Adam Bucki, Katarzyna Wójcik-Pszczoła, Marcin Kołaczkowski, Elżbieta Pękala
Anthracycline antibiotics (ANT), such as doxorubicin or daunorubicin, are a class of anticancer drugs that are widely used in oncology. Although highly effective in cancer therapy, their usefulness is greatly limited by their cardiotoxicity. Possible mechanisms of ANT cardiotoxicity include their conversion to secondary alcohol metabolites (i.e. doxorubicinol, daunorubicinol) catalyzed by carbonyl reductases (CBR) and aldo-keto reductases (AKR). These metabolites are suspected to be more cardiotoxic than their parent compounds...
March 10, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28282791/anti-arthritic-effect-of-berberine-on-adjuvant-induced-rheumatoid-arthritis-in-rats
#14
Xue Wang, Xin He, Chun-Feng Zhang, Chang-Run Guo, Chong-Zhi Wang, Chun-Su Yuan
BACKGROUND: Rheumatoid arthritis (RA) is a chronic and systemic autoimmune disease, which affects approximately 1% adult population in the worldwide. AIM: The present study was to investigate the anti-arthritic effect of berberine and its involved mechanism in Freund's complete adjuvant (FCA) induced arthritis rats. METHODS AND MATERIALS: Rats were divided randomly into control, FCA, tripterysium glycosides, berberine (75 and 150mg/kg). The apparent indicators, including changes of body weights, paw swelling degrees and arthritis indexes, were analyzed to evaluate anti-arthritic effect of berberine...
March 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28282788/berberine-inhibits-palmitate-induced-nlrp3-inflammasome-activation-by-triggering-autophagy-in-macrophages-a-new-mechanism-linking-berberine-to-insulin-resistance-improvement
#15
Hang Zhou, Lili Feng, Fang Xu, Yi Sun, Yuxiang Ma, Xiong Zhang, Hailiang Liu, Ge Xu, Xuefeng Wu, Yan Shen, Yang Sun, Xudong Wu, Qiang Xu
NLRP3 (Nod-like receptor family pyrin domain containing 3) inflammasome has been reported to contribute to obesity-induced inflammation and insulin resistance. However, there are few drugs targeting NLRP3 inflammasome for the treatment of insulin resistance. In the present study, we showed that berberine (BBR) significantly suppressed saturated fatty acid palmitate (PA)-induced NLRP3 inflammasome activation and interleukin-1β (IL-1β) release in macrophages, which was one of the most important mediators in the insulin sensitivity of adipose tissue...
March 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28279930/metabolites-identification-of-berberine-in-rats-using-ultra-high-performance-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry
#16
Kun Wang, Liwei Chai, Xinchi Feng, Zhongbo Liu, Hongxia Liu, Liqin Ding, Feng Qiu
Berberine (BBR), the principle component for many medicinal plants such as Coptis chinensis Franch., Phellodendron chinense Schneid., and Mahonia bealei (Fort.) Carr., possesses diverse pharmacological activities, including anti-bacterial, anti-inflammatory, antitumor, hypolipidemic and antidiabetic activities. In this study, a rapid and reliable method using a five-step strategy based on the ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS), and metabolynx™ software with mass defect filter (MDF) technique was developed to investigate the metabolism of BBR...
February 27, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28277195/induction-of-apoptosis-by-berberine-in-hepatocellular-carcinoma-hepg2-cells-via-downregulation-of-nf-%C3%AE%C2%BAb
#17
Min Li, Mao Zhang, Zhi-Lang Zhang, Ning Liu, Xiao-Yu Han, Qin-Cheng Liu, Wei-Jun Deng, Cai-Xian Liao
Hepatocellular carcinoma (HCC) is highly resistant to traditional chemotherapeutic approaches, which causes difficulty in the development of effective drugs for the treatment of HCC. Berberine, a major ingredient of Rhizoma coptidis, is a natural alkaloid used in traditional Chinese medicine. Berberine exhibits potent antitumor activity against HCC due to its high efficiency and low toxicity. In the present study, we found that berberine sensitized HepG cells to NF-κB-mediated apoptosis. Berberine exhibited a significant antiproliferation effect on the HepG2 cells and promoted apoptosis...
January 26, 2017: Oncology Research
https://www.readbyqxmd.com/read/28276481/identification-of-berberine-as-a-direct-thrombin-inhibitor-from-traditional-chinese-medicine-through-structural-functional-and-binding-studies
#18
Xing Wang, Yuxin Zhang, Ying Yang, Xia Wu, Hantian Fan, Yanjiang Qiao
Thrombin acts as a key enzyme in the blood coagulation cascade and represents a potential drug target for the treatment of several cardiovascular diseases. The aim of this study was to identify small-molecule direct thrombin inhibitors from herbs used in traditional Chinese medicine (TCM). A pharmacophore model and molecular docking were utilized to virtually screen a library of chemicals contained in compositions of traditional Chinese herbs, and these analyses were followed by in vitro bioassay validation and binding studies...
March 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28263849/chemical-profiles-and-pharmacological-activities-of-chang-kang-fang-a-multi-herb-chinese-medicinal-formula-for-treating-irritable-bowel-syndrome
#19
Qian Mao, Lei Shi, Zhi-Gang Wang, Yu-Hui Luo, Yin-Yu Wang, Xue Li, Min Lu, Jian-Min Ju, Jin-Di Xu, Ming Kong, Shan-Shan Zhou, Min-Qin Shen, Song-Lin Li
ETHNOPHARMACOLOGICAL RELEVANCE: Chang-Kang-Fang formula (CKF), a multi-herb traditional Chinese medicinal formula, has been clinically used for treatment of irritable bowel syndrome (IBS). The mechanisms of CKF for treating IBS and the components that are responsible for the activities were still unknown. AIM OF THE STUDY: To investigate the chemical profiles and effects of CKF on IBS model. MATERIALS AND METHODS: The chemical profiles of CKF were investigated by ultra performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-Q/TOF-MS/MS)...
March 2, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28259949/berberine-inhibits-the-proliferation-of-human-nasopharyngeal-carcinoma-cells-via-an-epstein-barr-virus-nuclear-antigen%C3%A2-1-dependent-mechanism
#20
Chao Wang, Huan Wang, Yaqian Zhang, Wei Guo, Cong Long, Jingchao Wang, Limei Liu, Xiaoping Sun
Nasopharyngeal carcinoma (NPC) is a malignancy derived from the epithelial cells of the nasopharynx cavity, and is closely associated with Epstein-Barr virus (EBV) infection. In addition to NPC, EBV causes various human malignancies, such as gastric cancer, hematological tumors and lymphoepithelioma-like carcinomas. Epstein-Barr nuclear antigen 1 (EBNA1) encoded by EBV is indispensable for replication, partition, transcription and maintenance of viral genomes. Berberine, a naturally occurring isoquinoline alkaloid, shows anti-inflammatory, anticholinergic, antioxidative, and anticancer activities...
March 2, 2017: Oncology Reports
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