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Su-Ling Zeng, Shang-Zhen Li, Chang-Jiang-Sheng Lai, Min-Yan Wei, Bai-Zhong Chen, Ping Li, Guo-Dong Zheng, E-Hu Liu
BACKGROUND: Inhibition of pancreatic lipase is an attractive approach to the treatment of obesity and other metabolic disorders. Naturally occurring phytochemicals are promising sources of lipase inhibitors. PURPOSE: In the present study, the anti-lipase activity of Citri Reticulatae Pericarpium (CRP) extracts was firstly evaluated in vitro. Moreover, the dynamic alteration of bioactive flavonoids in CRP collected at different time and its correlation with anti-lipase activities was investigated...
April 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Fang Chen, Yali Ma, Zhiqiang Sun, Xiaoguang Zhu
Tangeretin (5, 6, 7, 8, 4'-pentamethoxyflavone), a natural compound extracted from citrus plants, has been shown to possess a variety of pharmacological activities, including anti-oxidant, anti-tumor, cytostatic and anti-diabetic properties. However, the role of tangeretin in diabetic nephropathy (DN) has not yet been investigated. This study was undertaken to elucidate the effects of tangeretin on high glucose (HG)-induced oxidative stress and extracellular matrix (ECM) accumulation in human glomerular mesangial cells (MCs) and explore the underlying mechanisms...
April 3, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Jiao-Yang Luo, Wen-Ju Zhou, Kun-Lun Li, Ming Zhao, Mei-Hua Yang
Traditional Chinese herbs are readily contaminated by mold that produced mycotoxins which are closly related to the herbs' external factors and external environments during the storage process. In this study, Citri Reticulatae Pericarpium was used as example, and the characteristics of traits, water content, active components (naringin, hesperidin, sinensetin, naringin, tangeretin) and the accumulation of aflatoxins (AFs) were selected as the evaluation indexes. Citri Reticulatae Pericarpium was stored under different environments and packaging materials for 12 months, and then the quality changes and mildew of Citri Reticulatae Pericarpium were examined...
March 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Somchaiya Surichan, Randolph R Arroo, Aristidis M Tsatsakis, Vasilis P Androutsopoulos
Tangeretin is a polymethoxylated flavone with multifaceted anticancer activity. In the present study, the metabolism of tangeretin was evaluated in the CYP1 expressing human breast cancer cell lines MCF7 and MDA-MB-468 and in the normal breast cell line MCF10A. Tangeretin was converted to 4' OH tangeretin by recombinant CYP1 enzymes and by CYP1 enzymes expressed in MCF7 and MDA-MB-468 cells. This metabolite was absent in MCF10A cells that did not express CYP1 enzymes. Tangeretin exhibited submicromolar IC50 (0...
April 4, 2018: Toxicology in Vitro: An International Journal Published in Association with BIBRA
E Mesquita, M Monteiro
The aim of this study was to develop and validate an HPLC-DAD method to evaluate the phenolic compounds profile of organic and conventional Pêra-Rio orange juice. The proposed method was validated for 10 flavonoids and 6 phenolic acids. A wide linear range (0.01-223.4μg·g-1 ), good accuracy (79.5-129.2%) and precision (CV≤3.8%), low limits of detection (1-22ng·g-1 ) and quantification (0.7-7.4μg), and overall ruggedness were attained. Good recovery was achieved for all phenolic compounds after extraction and cleanup...
April 2018: Food Research International
Wei-Lun Hung, Wei-Shan Chang, Wen-Chien Lu, Guor-Jien Wei, Yu Wang, Chi-Tang Ho, Lucy Sun Hwang
Tangeretin, 4',5,6,7,8-pentamethoxyflavone, is one of the major polymethoxyflavones (PMFs) existing in citrus fruits, particularly in the peels of sweet oranges and mandarins. Tangeretin has been reported to possess several beneficial bioactivities including anti-inflammatory, anti-proliferative and neuroprotective effects. To achieve a thorough understanding of the biological actions of tangeretin in vivo, our current study is designed to investigate the pharmacokinetics, bioavailability, distribution and excretion of tangeretin in rats...
April 2018: Journal of Food and Drug Analysis
Meixia Luo, Hujie Luo, Pingjun Hu, Yiting Yang, Bo Wu, Guodong Zheng
To discriminate the feasible differences and find potential similarities and relationships of Citri Reticulatae Pericarpium (CRP), this work was accomplished by a comprehensive and reliable method using gas chromatography-mass spectrometer (GC-MS) to analyze the volatile oils and high-performance liquid chromatography (HPLC) simultaneously to determine the contents of five bioactive flavonoids, namely hesperidin, nobiletin, 3,5,6,7,8,3',4'-heptamethoxyflavone, tangeretin, and 5-hydroxy-6,7,8,3',4'-pentamethoxyflavone in 25 batches of CRP samples of 10 cultivars collected from different regions in China...
March 2018: Food Science & Nutrition
Rui Guo, Xiaoxiao Zhang, Jin Su, Haiyu Xu, Yanqiong Zhang, Fangbo Zhang, Defeng Li, Yi Zhang, Xuefeng Xiao, Shuangcheng Ma, Hongjun Yang
BACKGROUND: Quality marker (Q-markers) has been proposed as a novel concept for quality evaluation and standard elaboration of traditional Chinese medicine (TCM). Xin-Su-Ning capsule (XSNC) has been extensively used for the treatment of arrhythmia with the satisfactory therapeutic effects in clinics. However, it is lack of reliable and effective Q-markers of this prescription. PURPOSE: To identify potential Q-markers of XSNC against arrhythmia. STUDY DESIGN: An integrative pharmacology-based investigation was performed...
February 10, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Meiyan Wang, Dan Meng, Peng Zhang, Xiangxing Wang, Gang Du, Charles Brennan, Shiming Li, Chi-Tang Ho, Hui Zhao
Aging and oxidative-related events are closely associated with the oxidative damages induced by excess reactive oxygen species (ROS). The phytochemicals nobiletin (NBT) and tangeretin (TAN) and their 5-demethylated derivatives 5-demethylnobiletin (5-DN) and 5-demethyltangeretin (5-DT) are the representative polymethoxyflavone (PMF) compounds found in aged citrus peels. Although the health benefits from PMFs due to their antioxidant activities have been well documented, a systematic assessment regarding the antioxidation process of PMFs is still lacking attention...
March 28, 2018: Journal of Agricultural and Food Chemistry
Wen-Bin Zhu, Ning Xiao, Xing-Jie Liu
Tangeretin, a natural polymethoxyflavone present in the peel of citrus fruits is known to exhibit anticancer properties against a variety of carcinomas. Previous experimental evidence suggests that lifestyle and dietary habits affect the risk of prostate cancer to a certain extent. As the effect of tangeretin on prostate cancer is unexplored, the present study investigated the effect of tangeretin on androgen-insensitive PC-3 cells and androgen-sensitive LNCaP cells. Tangeretin reduced the cell viability of PC-3 cells in a dose- and time-dependent manner, with the half-maximal inhibitory concentration (IC50 ) observed at 75 µM dose following 72 h of incubation, while in LNCaP cells, the IC50 was identified to be ~65 µM...
January 2018: Oncology Letters
Shigeru Matsumoto, Tsukasa Tominari, Chiho Matsumoto, Shosei Yoshinouchi, Ryota Ichimaru, Kenta Watanabe, Michiko Hirata, Florian M W Grundler, Chisato Miyaura, Masaki Inada
Polymethoxyflavonoids (PMFs) are a family of the natural compounds that mainly compise nobiletin, tangeretin, heptamethoxyflavone (HMF), and tetramethoxyflavone (TMF) in citrus fruits. PMFs have shown various biological functions, including anti-oxidative effects. We previously showed that nobiletin, tangeretin, and HMF all inhibited interleukin (IL)-1-mediated osteoclast differentiation via the inhibition of prostaglandin E2 synthesis. In this study, we created an original mixture of PMFs (nobiletin, tangeretin, HMF, and TMF) and examined whether or not PMFs exhibit co-operative inhibitory effects on osteoclastogenesis and bone resorption...
January 20, 2018: Pharmaceuticals
Inês Silva, Marta F Estrada, Carolina V Pereira, Andreia Bento da Silva, Maria R Bronze, Paula M Alves, Catarina M M Duarte, Catarina Brito, Ana Teresa Serra
Polymethoxylated flavones (PMFs) have been recognized to inhibit colorectal cancer proliferation through various mechanisms, however most of these studies have been performed on cells grown as monolayers that present limitations in mimicking the 3D tumor architecture and microenvironment. The main aim of this study was to investigate the anticancer potential of an orange peel extract (OPE) enriched in PMFs in a 3D cell model of colorectal cancer. The OPE was developed by supercritical fluid extraction and the anticancer effect was evaluated in HT29 spheroids cultures in a stirred-tank based system...
February 2018: Nutrition and Cancer
Mai Gamal Elhennawy, Hai-Shu Lin
Tangeretin (TAN) is a dietary polymethoxylated flavone that possesses a broad scope of pharmacological activities. A simple high-performance liquid chromatography (HPLC) method was developed and validated in this study to quantify TAN in plasma of Sprague-Dawley rats. The lower limit of quantification (LLOQ) was 15 ng/mL; the intra- and inter-day assay variations expressed in the form of relative standard deviation (RSD) were all less than 10%; and the assay accuracy was within 100 ± 15%. Subsequently, pharmacokinetic profiles of TAN were explored and established...
December 29, 2017: Pharmaceutics
Zhong-Wen Yuan, Ya-Zhuo Li, Zhong-Qiu Liu, Sen-Ling Feng, Hua Zhou, Chang-Xiao Liu, Liang Liu, Ying Xie
Biological responses of a variety of naturally occurring compounds in vivo were restrained by their poor oral bioavailability. Silybin, as one of the active ingredients of silymarin, has presented promising bioactivity for the treatment of chronic liver diseases and cancer. However, its exposure in body was limited. In this study, silybin was demonstrated to be substrates of both BCRP and MRP2 by utilizing monolayer Caco-2 cell model and confirmed in MDCK cells overexpressing specific efflux transporter. Of all compounds screened, tangeretin, a potent inhibitor of efflux transporters of BCRP, MRP2 and P-gp, was able to enhance exposure of silybin by inhibiting functions of the barriers mediating transcellular transport...
February 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Jing Wu, Yu-Mei Zhao, Zhi-Kuan Deng
Chronic kidney disease (CKD) is a significant global health concern with limited treatment options. Oxidative stress and inflammatory responses have been implicated in the pathology of CKD. Patients with CKD are frequently affected with neurological complications that affect both the central and peripheral nervous system. Identification of effective treatment strategies are of much clinical value in the therapy of CKD. Tangeretin, a plant-derived flavonoid has been described to retain extensive pharmacological properties...
February 2018: Inflammopharmacology
Kumju Youn, Yoonjin Yu, Jinhyuk Lee, Woo-Sik Jeong, Chi-Tang Ho, Mira Jun
Beta-site amyloid precursor protein (APP) cleaving enzyme1 (BACE1) catalyzes the rate-limiting step of amyloid-β protein (Aβ) generation, and is considered as a prime target for Alzheimer's disease (AD). In search of a candidate for AD prevention, our efforts exploring the natural BACE1 inhibitor have led to the finding of nobiletin, tangeretin, and sinensetin-representative compounds of polymethoxyflavones (PMFs). Tangeretin exhibited the strongest BACE1 inhibition (IC50, 4.9 × 10(-5) M), followed by nobiletin and sinensetin with IC50 values of 5...
September 4, 2017: Nutrients
L-L Liu, F-H Li, Y Zhang, X-F Zhang, J Yang
Asthma is a chronic allergic disease characterized by airway inflammation, airway hyper-responsiveness (AHR), and mucus hypersecretion. T-lymphocytes are involved in the pathogenesis of asthma, mediating airway inflammatory reactions by secreting cytokines. The phosphoinositide 3-kinase (PI3K) and Notch signaling pathways are associated with T cell signaling, proliferation, and differentiation, and are important in the progression of asthma. Thus, compounds that can modulate T cell proliferation and function may be of clinical value...
July 20, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
Norihiro Yoshizaki, Ron Hashizume, Hitoshi Masaki
BACKGROUND: Skin color is determined by melanin contents and its distribution. Melanin is synthesized in melanosomes of melanocytes, catalyzed by tyrosinase, melanogenic enzymes. Regarding the process of melanin synthesis, melanosomal pH is considered to play an important role, because it has been reported to differ between Caucasian and Black melanocytes. OBJECTIVE: Although polymethoxyflavone (PMF) has many beneficial effects, it has not been reported which PMF suppresses melanogenesis...
October 2017: Journal of Dermatological Science
Su-Ling Zeng, Li Duan, Bai-Zhong Chen, Ping Li, E-Hu Liu
Detection of metabolites in complex biological matrixes is a great challenge because of the background noise and endogenous components. Herein, we proposed an integrated strategy that combined background subtraction program and modified mass defect filter (MMDF) data mining in a Microsoft Excel platform for chemicalome and metabolome profiling of the polymethoxylated flavonoids (PMFs) in Citri Reticulatae Pericarpium (CRP). The exogenously-sourced ions were firstly filtered out by the developed Visual Basic for Applications (VBA) program incorporated in the Microsoft Office...
July 28, 2017: Journal of Chromatography. A
Jin-Song Yang, Xiao-Hong Wu, Hao-Gang Yu, Li-Song Teng
Our aim was to investigate whether tangeretin, a citrus flavonoid, was able to prevent neuroinflammation and improve dementia in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced rodent model of Parkinson's disease (PD). MPTP-HCl was infused into the substantia nigra pars compacta of male Sprague-Dawley rats. Tangeretin (50, 100 or 200 mg/kg body weight) was administered orally starting 3 days prior to MPTP injection and was continued for 20 days following injection. MPTP-lesioned rats revealed motor dysfunction in bar test and rota rod tests...
June 2, 2017: Inflammopharmacology
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