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https://www.readbyqxmd.com/read/28797884/drifting-of-heme-coordinating-group-in-imidazolylmethylxanthones-leading-to-improved-selective-inhibition-of-cyp11b1
#1
Silvia Gobbi, Qingzhong Hu, Christina Zimmer, Federica Belluti, Angela Rampa, Rolf W Hartmann, Alessandra Bisi
An abnormal increase in glucocorticoid levels is responsible for pathological disorders affecting different organs and systems, and the selective inhibition of appropriate steroidogenic enzymes represents a validated strategy to restore their physiological levels. In continuing our studies on CYP11B inhibitors, in this paper a small series of 6-substituted 3-imidazolylmethylxanthones was designed and synthesized, according to the data acquired from previously reported series of derivatives and from a purposely-performed docking study...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28747567/modulation-of-the-nur77-bcl-2-apoptotic-pathway-by-p38%C3%AE-mapk
#2
Jie Liu, Guang-Hui Wang, Ying-Hui Duan, Yi Dai, Yuzhou Bao, Mengjie Hu, Yu-Qi Zhou, Mingyu Li, Fuquan Jiang, Hu Zhou, Xin-Sheng Yao, Xiao-Kun Zhang
Orphan nuclear receptor Nur77 promotes apoptosis by targeting mitochondria through interaction with Bcl-2, an event that converts Bcl-2 from a survival to killer. However, how the Nur77-Bcl-2 apoptotic pathway is regulated remains largely unknown. In this study, we examined the regulation of the Nur77-Bcl-2 pathway by CCE9, a xanthone compound. Our results demonstrated that the apoptotic effect of CCE9 depended on its induction of Nur77 expression, cytoplasmic localization, and mitochondrial targeting. The activation of the Nur77-Bcl-2 pathway by CCE9 was associated with its activation of p38α MAPK...
July 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28741279/identification-of-lead-molecules-in-garcinia-mangostana-l-against-pancreatic-cholesterol-esterase-activity-an-in-silico-approach
#3
George Kadakasseril Varghese, Rini Abraham, Nisha N Chandran, Solomon Habtemariam
Hypercholesterolemia is one of the major risk factors for the development and progression of atherosclerosis. Hence, inhibitors of cholesterol absorption have been investigated for decades as a strategy to prevent and treat cardiovascular diseases associated with hypercholesterolemia. Cholesterol esterase (CEase) in pancreatic juice plays a vital role in the hydrolysis of dietary cholesterol esters to cholesterol and fatty acids. Since inhibition of CEase might lead to a reduction of cholesterol absorption, an attempt is made in this study to identify lead molecules of Garcinia mangostana by the in silico approach...
July 24, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28729053/bioactive-polyprenylated-benzophenone-derivatives-from-the-fruits-extracts-of-garcinia-xanthochymus
#4
Ui Joung Youn, Tawanun Sripisut, Gabriella Miklossy, James Turkson, Surat Laphookhieo, Leng Chee Chang
Two new polycyclic prenylated xanthones (1 and 2) and a new phenylpropanoid glycoside (3), along with seven known compounds (4-10) were isolated from the fruits of Garcinia xanthochymus. The structures were elucidated by 1D- and 2D-NMR, and HRMS experiments. The isolates were evaluated for their inhibitory effects against the viability of U251MG glioblastoma and MDA-MB-231 breast cancer cells that harbor an aberrantly active signal transducer and exhibit activation of transcription 3 (STAT3), and compared to normal NIH3T3 mouse fibroblasts...
July 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28722351/%C3%AE-mangostin-suppresses-human-hepatocellular-carcinoma-cell-invasion-through-inhibition-of-mmp-2-and-mmp-9-expression-and-activating-the-erk-and-jnk-pathways
#5
Chien-Feng Huang, Ying-Hock Teng, Fung-Jou Lu, Wen-Hung Hsu, Chia-Liang Lin, Chia-Chen Hung, Jai-Nien Tung, Yi-Hsien Hsieh, Chung-Jung Liu
β-mangostin is a dietary xanthone that has been reported to have the anticancer properties in some human cancer cell types. However, the antimetastatic effect and molecular mechanism of β-mangostin action in human hepatocellular carcinoma (HCC) cells remain unknown. In this study, we found that β-mangostin did not induce cytotoxicity in human HCC cells (SK-Hep-1, Huh-7 and HA22T/VGH cells). β-mangostin could inhibit migration and invasion of human HCC cells. Meanwhile, β-mangostin significantly decreased the protein activities and expression of matrix metalloproteinase (MMP)-2 and MMP-9 via increasing the activation of MEK1/2, ERK1/2, MEK4 and JNK1/2 signaling pathways...
July 19, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28716572/dpph-hplc-ms-assisted-rapid-identification-of-endothelial-protective-substances-from-xiao-ke-an
#6
Zhenzhong Yang, Zhenhao Li, Zheng Li
ETHNOPHARMACOLOGICAL RELEVANCE: Xiao-Ke-An formula (XKA) is a Chinese medicine widely used for treating diabetes and associated complications. Endothelial protection is thought to be one of its therapeutic mechanisms. However, the protective effect of XKA on endothelial cells remains unclear, especially in oxidative injury induced endothelial dysfunction. MATERIALS AND METHODS: A novel strategy to rapidly screen and identify potential endothelial protective substances from XKA was established by combining the 2,2'-diphenyl-1-picrylhydrazyl high performance liquid chromatography coupled with mass spectrometry (DPPH-HPLC-MS) approach with cell-based verification...
July 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28716025/beta-mangostin-demonstrates-apoptogenesis-in-murine-leukaemia-wehi-3-cells-in-vitro-and-in-vivo
#7
Fatima Abdelmutaal Ahmed Omer, Najihah Mohd Hashim, Mohamed Yousif Ibrahim, Abdulmannan F Aldoubi, Pouya Hassandarvish, Firouzeh Dehghan, Noraziah Nordin, Hamed Karimian, Landa Zeenelabdin Ali Salim, Mahmood Ameen Abdulla, Karim Al-Jashamy, Syam Mohan
BACKGROUND: Beta-mangostin (BM) is a xanthone-type of natural compound isolated from Cratoxylum arborescens. This study aimed to examine the apoptosis mechanisms induced by BM in a murine monomyelocytic cell line (WEHI-3) in vitro and in vivo. METHODS: A WEHI-3 cell line was used to evaluate the cytotoxicity of BM by MTT. AO/PI and Hoechst 33342 dyes, Annexin V, multiparametric cytotoxicity 3 by high content screening (HCS); cell cycle tests were used to estimate the features of apoptosis and BM effects...
July 17, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28700682/circumscription-of-the-genus-lepra-a-recently-resurrected-genus-to-accommodate-the-variolaria-group-of-pertusaria-sensu-lato-pertusariales-ascomycota
#8
Xinli Wei, Imke Schmitt, Brendan Hodkinson, Adam Flakus, Martin Kukwa, Pradeep K Divakar, Paul M Kirika, Jürgen Otte, Anjuli Meiser, H Thorsten Lumbsch
Pertusarialean lichens include more than 300 species belonging to several independent phylogenetic lineages. Only some of these phylogenetic clades have been comprehensively sampled for molecular data, and formally described as genera. Here we present a taxonomic treatment of a group of pertusarialean lichens formerly known as "Pertusaria amara-group", "Monomurata-group", or "Variolaria-group", which includes widespread and well-known taxa such as P. amara, P. albescens, or P. ophthalmiza. We generated a 6-locus data set with 79 OTUs representing 75 species...
2017: PloS One
https://www.readbyqxmd.com/read/28686977/cardioprotective-effect-of-the-xanthones-from-gentianella-acuta-against-myocardial-ischemia-reperfusion-injury-in-isolated-rat-heart
#9
Zhibin Wang, Gaosong Wu, Hua Liu, Na Xing, Yanping Sun, Yadong Zhai, Bingyou Yang, Ah-Ng Tony Kong, Haixue Kuang, Qiuhong Wang
Gentianella acuta (Michx.) Hulten is widely used for the treatment of arrhythmia and coronary heart disease in Ewenki Folk Medicinal Plants and Mongolian Medicine, popularly known as "Wenxincao" in China. To investigate the potential protective role of the xanthones from G. acuta against myocardial I/R injury in isolated rat heart and its possible related mechanism. The protective role of xanthones on myocardial I/R injury was studied on Langendorff apparatus. The hemodynamic parameters including the left ventricular developed pressure (LVDP), the maximum rate of up/down left intraventricular pressure (±dp/dtmax), coronary flow (CF) and heart rate (HR) were recorded during the perfusion...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28677899/validated-lc-ms-ms-method-for-quantitation-of-demethylbellidifolin-in-rat-plasma-and-its-application-to-pharmacokinetic-and-bioavailability-studies
#10
Jie Zhang, Huiyu Yan, Xiaoyu Qu, Wei Zhou
Demethylbellidifolin, a major xanthone compound of Swertia davidi Franch, showed many beneficial pharmacological effects including antioxidation, anti-inflammation, anti-fibrosis, and cardiovascular protection effects. In this research, a rapid and sensitive LC-MS/MS method for the quantitative analysis of demethylbellidifolin in rat plasma was developed. The demethylbellidifolin and internal standard of aurantio-obtusin were extracted from 50 μL of rat plasma samples with ethyl acetate, then the dried residue was reconstituted and injected in an HPLC system with ZORBAX SB-C18 analytical column (2...
July 5, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28674220/isolation-and-characterization-of-microsatellite-markers-in-garcinia-gummi-gutta-by-next-generation-sequencing-and-cross-species-amplification
#11
K V Ravishankar, R Vasudeva, Byatroy Hemanth, B S Sandya, B R Sthapit, V A Parthasarathy, V Ramanatha Rao
Garcinia gummi-gutta (L.) Roxb. (Clusiaceae) is an endemic, semidomesticated, fruit-yielding tree species distributed in the Western Ghats of India and Sri Lanka. Various bioactive phytochemicals, such as garcinol, benzophenones and xanthones are isolated from G. gummi-gutta and have shown antibacterial, antiviral and antioxidant activities. We sequenced the total genomic DNA using Illumina Hiseq 2000 platform and examined 241,141,804 bp high quality data, assembled into 773,889 contigs. In these contigs, 27,313 simple-sequence repeats (SSRs) were identified, among which mononucleotide repeats were predominant (44...
June 2017: Journal of Genetics
https://www.readbyqxmd.com/read/28666227/comprehensive-profiling-and-characterization-of-chemical-constituents-of-rhizome-of-anemarrhena-asphodeloides-bge
#12
De Ji, Zi-Yan Huang, Cheng-Hao Fei, Wei-Wei Xue, Tu-Lin Lu
The rhizome of Anemarrhena asphodeloides Bge. is commonly used as an herbal medicine in China. In this study, ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) was used, in both negative and positive ion modes, to comprehensively analyze the chemical constituents of A. asphodeloides. From the intact precursor ions, MS/MS fragmentation information, and previous reports, we identified 89 compounds. These compounds included 8 cyclic peptides, 11 flavones (9 xanthones), 45 steroidal saponins, 15 fatty acids, 3 lignans, and 7 other compounds...
June 19, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28665538/%C3%AE-glucosidase-inhibitory-xanthones-from-the-roots-of-garcinia-fusca
#13
Nam K Nguyen, Xuyen A Truong, Thai Q Bui, Dzung N Bui, Hai X Nguyen, Phuong T Tran, Lien-Hoa D Nguyen
An ethyl acetate extract of the roots of Garcinia fusca produced two new compounds, fuscaxanthones J (1) and K (2), together with eight known xanthones (3-10). Their structures were determined using spectroscopic methods, mainly 1-D and 2-D NMR. α-Glucosidase inhibitory activity of the isolated compounds was evaluated and fuscaxanthone J (1) showed the most significant effect with IC50 value of 8.3 ± 1.8 μM (compared with acarbose, IC50 = 214.5 ± 2.3 μM). This article is protected by copyright. All rights reserved...
June 30, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28662965/gerontoxanthone-b-from-maclura-cochinchinensis-var-gerontogea-exhibits-anti-inflammatory-potential-as-an-aryl-hydrocarbon-receptor-agonist
#14
Ken-Ichi Nakashima, Takumi Ogiwara, Takao Hirai, Toshiyuki Tanaka, Hiroko Murata, Kouichi Kaburagi, Yoshiaki Fujii-Kuriyama, Hidetoshi Hayashi, Makoto Inoue
The aryl hydrocarbon receptor (AhR) is a ligand-dependent transcriptional factor belonging to the basic helix-loop-helix-Per-Ahr/Arnt-Sim family. In this study, we evaluated the AhR agonistic activities of 12 xanthones isolated from the roots of M. cochinchinensis var. gerontogea using HepG2 cells transfected with pX4TK-Luc reporter plasmids. Gerontoxanthone B (GXB) showed the most potent activity at a concentration of 10μM, and the activity was inhibited by AhR antagonists such as GNF-351. GXB also increased cytochrome P450 1A1 mRNA and protein levels in HepG2 cells...
August 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28656594/review-of-garcinia-mangostana-and-its-xanthones-in-metabolic-syndrome-and-related-complications
#15
REVIEW
Hourieh Tousian Shandiz, Bibi Marjan Razavi, Hossein Hosseinzadeh
Metabolic syndrome is coexistence of abdominal obesity, hyperglycemia, hyperlipidemia and hypertension that causes cardiovascular diseases, diabetes and their complications, low quality and short lifespan. Garcinia mangostana and its xanthones such as α-mangostin have been shown desirable effects such as anti-obesity, anti-hyperglycemic, anti-dyslipidemia, anti-diabetic and antiinflammatory effects in experimental studies. Various databases such as PubMed, Scopus and Web of Science with keywords of 'Garcinia mangostana', 'mangosteen', 'α-mangostin', 'metabolic syndrome', 'hypoglycemic', 'antihyperglicemic', 'antidiabetic', 'hypotensive', 'antihypertensive', 'atherosclerosis', 'arteriosclerosis' and 'hyperlipidemia' have been investigated in this search without publication time limitation...
August 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28653908/antibacterial-anti-inflammatory-and-anti-oxidatant-activities-of-various-isolated-compounds-from-cratoxylum-species
#16
Pirasut Rodanant, Nawong Boonnak, Rudee Surarit, Jintakorn Kuvatanasuchati, Wannee Lertsooksawat
The objective of this study was to investigate the bioactivity of twenty-nine known isolated compounds from Cratoxylum species including three anthraquinones, four triterpenes, and twenty-two xanthones. All isolated compounds were subjected to antibacterial, anti-inflammatory and anti-oxidant activities. Cytotoxicity evaluations were performed by MTT assay. The anti-oxidatant activity was performed using DPPH assay. The anti-inflammatory activity was evaluated from the production of cytokines TNF-α and IL1-β using ELISA assay...
May 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28641010/alpha-mangostin-reverses-multidrug-resistance-by-attenuating-the-function-of-the-multidrug-resistance-linked-abcg2-transporter
#17
Chung-Pu Wu, Sung-Han Hsiao, Megumi Murakami, Yu-Jen Lu, Yan-Qing Li, Yang-Hui Huang, Tai-Ho Hung, Suresh V Ambudkar, Yu-Shan Wu
The ATP-binding cassette (ABC) drug transporter ABCG2 can actively efflux a wide variety of chemotherapeutic agents out of cancer cells and subsequently reduce the intracellular accumulation of these drugs. Therefore, the overexpression of ABCG2 often contributes to the development of multidrug resistance (MDR) in cancer cells, which is one of the major obstacles to successful cancer chemotherapy. Moreover, ABCG2 is highly expressed in various tissues including the intestine and blood-brain barrier (BBB), limiting the absorption and bioavailability of many therapeutic agents...
August 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28638898/laser-photolysis-studies-of-%C3%AF-bond-dissociation-in-aromatic-carbonyls-with-a-c-c-triple-bond-stimulated-by-triplet-sensitization
#18
Minoru Yamaji, Ami Horimoto, Bronislaw Marciniak
We have prepared three types of carbonyl compounds, benzoylethynylmethyl phenyl sulfide (2@SPh), (p-benzoyl)phenylethynylmethyl phenyl sulfide (3@SPh) and p-(benzoylethynyl)benzyl phenyl sulfide (4@SPh) with benzoyl and phenylthiylmethyl groups, which are interconnected with a C-C triple bond and a phenyl ring. Laser flash photolysis of 3@SPh and 4@SPh in acetonitrile provided the transient absorption spectra of the corresponding triplet states where no chemical reactions were recognized. Upon laser flash photolysis of 2@SPh, the absorption band due to the phenylthiyl radical (PTR) was obtained, indicating that the C-S bond cleaved in the excited state...
June 22, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28626426/potential-of-central-eastern-and-western-africa-medicinal-plants-for-cancer-therapy-spotlight-on-resistant-cells-and-molecular-targets
#19
REVIEW
Armelle T Mbaveng, Victor Kuete, Thomas Efferth
Cancer remains a major health hurdle worldwide and has moved from the third leading cause of death in the year 1990 to second place after cardiovascular disease since 2013. Chemotherapy is one of the most widely used treatment modes; however, its efficiency is limited due to the resistance of cancer cells to cytotoxic agents. The present overview deals with the potential of the flora of Central, Eastern and Western African (CEWA) regions as resource for anticancer drug discovery. It also reviews the molecular targets of phytochemicals of these plants such as ABC transporters, namely P-glycoprotein (P-gp), multi drug-resistance-related proteins (MRPs), breast cancer resistance protein (BCRP, ABCG2) as well as the epidermal growth factor receptor (EGFR/ErbB-1/HER1), human tumor suppressor protein p53, caspases, mitochondria, angiogenesis, and components of MAP kinase signaling pathways...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28624142/anti-diabetic-xanthones-from-the-bark-of-garcinia-xanthochymus
#20
Chi N Nguyen, Binh T D Trinh, Toan B Tran, Le-Thu T Nguyen, Anna K Jäger, Lien-Hoa D Nguyen
An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards α-glucosidase and PTP1B with IC50 values of 0.3±0.1μg/mL and 2.3±0.4μg/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (3-12), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards α-glucosidase with IC50 value of 4...
August 1, 2017: Bioorganic & Medicinal Chemistry Letters
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