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Yudui Xia, Xia Liu, Chunlin Zou, Shixiu Feng, Hongwei Guo, Yeguo Yang, Yong Lei, Jian Zhang, Yi Lu
Nasopharyngeal carcinoma (NPC) is one of the most common head and neck malignancies and is typically treated with radiotherapy and chemotherapy. Garcinone C, a natural compound isolated from Garcinia oblongifolia Champ., is a xanthone derivative with potential cytotoxic effects on certain cancers. However, there are limited studies regarding its effects on NPC cells, and its mechanism of action in NPC remains unknown. In the present study, we found that garcinone C significantly inhibited cell viability of the human NPC cell lines CNE1, CNE2, HK1 and HONE1...
January 16, 2018: Oncology Reports
Fuengfa Laopian, Sutin Kaennakam, Kitiya Rassamee, Pongpun Siripong, Santi Tip-Pyang
Three new xanthones, named calaxanthones A-C (1-3), along with 17 known xanthones (4-20) were isolated from the roots of Calophyllum calaba. Their structures were determined by spectroscopic analysis. All isolated compounds were evaluated for their cytotoxicity against five cancer cell lines (KB, HeLa S-3, HT-29, MCF-7 and HepG-2). Compound 3 showed potent cytotoxicity against all the five cancer cell lines with IC50 values in the range of 0.82-5.04 μM. Furthermore, compound 6 showed potent cytotoxicity against KB, HeLa S-3 and HepG2 cells with IC50 values of 7...
January 15, 2018: Natural Product Research
Ye' Zaw Phyo, Sara Cravo, Andreia Palmeira, Maria Elizabeth Tiritan, Anake Kijjoa, Madalena M M Pinto, Carla Fernandes
A systematic study of enantioresolution of a library of xanthonic derivatives, prepared "in-house", was successfully carried out with four commercially available macrocyclic glycopeptide-based columns, namely ChirobioticTM T, ChirobioticTM R, ChirobioticTM V and ChirobioticTM TAG. Evaluation was conducted in multimodal elution conditions: normal-phase, polar organic, polar ionic and reversed-phase. The effects of the mobile phase composition, the percentage of organic modifier, the pH of the mobile phase, the nature and concentration of different mobile phase additives on the chromatographic parameters are discussed...
January 11, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Zuo Peng Li, Yeong Hun Song, Zia Uddin, Yan Wang, Ki Hun Park
Cratoxylum cochinchinense displayed significant inhibition against protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase, both of which are key target enzymes to attenuate diabetes and obesity. The compounds responsible for both enzymes inhibition were identified as twelve xanthones (1-12) among which compounds 1 and 2 were found to be new ones. All of them simultaneously inhibited PTP1B with IC50s of (2.4-52.5 µM), and α-glucosidase with IC50 values of (1.7-72.7 µM), respectively. Cratoxanthone A (3) and γ-mangostin (7) were estimated to be most active inhibitors against both PTP1B (IC50 = 2...
December 26, 2017: Bioorganic & Medicinal Chemistry
Phanruethai Pailee, Chutima Kuhakarn, Chanyapat Sangsuwan, Sakchai Hongthong, Pawinee Piyachaturawat, Kanoknetr Suksen, Surawat Jariyawat, Radeekorn Akkarawongsapat, Jitra Limthongkul, Chanita Napaswad, Palangpon Kongsaeree, Samran Prabpai, Thaworn Jaipetch, Manat Pohmakotr, Patoomratana Tuchinda, Vichai Reutrakul
Eleven previously undescribed compounds, including four benzophenones (garciosones A-D), four xanthones (garciosones E-H) and three biphenyls (garciosines A-C), along with eighteen known compounds were isolated from the stems, leaves and twigs of Garcinia speciosa Wall. (Clusiaceae). Their structures were established by extensive spectroscopic analysis. For garciosines A-C, the structures were confirmed by single crystal X-ray diffraction analysis. Most of the isolated compounds were evaluated for their cytotoxic activity and anti-HIV-1 activity using the syncytium inhibition assay and HIV-1 reverse transcriptase (RT) assay...
January 2, 2018: Phytochemistry
Byeol Choi, Seul-Ki Choi, You Na Park, Soo-Yeon Kwak, Hwa Jeong Lee, Youngjoo Kwon, Younghwa Na, Yun-Sil Lee
Heat shock protein 27 (HSP27, HSPB1) induces resistance to anticancer drugs in various cancer types, including non-small cell lung cancer (NSCLC). Therefore, pharmacological inhibition of HSP27 in NSCLC may be a good strategy for anticancer therapy. Unlike other HSPs such as HSP90 and HSP70, small molecule approaches for neutralization of HSP27 are not well established because of the absence of an ATP binding domain. Previously, small molecules with altered cross linking activity of HSP27, were identified to inhibit building a large oligomer led to sensitization in combination with radiation and chemotherapeutic drugs...
December 1, 2017: Oncotarget
Chao Han, Zhongrui Li, Jiqin Hou, Zhen Wang, Dingqiao Xu, Guimin Xue, Lingyi Kong
Lysine-specific demethylase 1 (LSD1), which has been reported to be overexpressed in several human cancers, has recently emerged as an attractive therapeutic target for treating cancer. To date, almost all the developed LSD1 inhibitors are chemo-synthesized molecules, while α-mangostin is first characterized as xanthone-based natural inhibitor in the current study with IC50 values of 2.81 ± 0.44 μM. Bioactivity study and docking analysis indicated that α-mangostin could inhibit MDA-MB-231 cells migration and evasion through inhibit intracellular LSD1 activity...
December 8, 2017: Bioorganic Chemistry
Suiyi Tan, Bin Yang, Juan Liu, Tianrong Xun, Yonghong Liu, Xuefeng Zhou
Marine micro-organisms have been proven to be excellent sources of bioactive compounds against HIV-1. Several natural products obtained from marine-derived Aspergillus fungi were screened for their activities to inhibit HIV-1 infection. Penicillixanthone A (PXA), a natural xanthone dimer from jellyfish-derived fungus Aspergillus fumigates, displayed potent anti-HIV-1 activity by inhibiting infection against CCR5-tropic HIV-1 SF162 and CXCR4-tropic HIV-1 NL4-3, with IC50 of 0.36 and 0.26 μM, respectively. Molecular docking study was conducted to understand the possible binding mode of PXA with the CCR5/CXCR4...
December 19, 2017: Natural Product Research
Kishore Banik, Choudhary Harsha, Devivasha Bordoloi, Bethsebie Lalduhsaki Sailo, Gautam Sethi, Hin Chong Leong, Frank Arfuso, Srishti Mishra, Lingzhi Wang, Alan P Kumar, Ajaikumar B Kunnumakkara
Natural compounds have enormous biological and clinical activity against dreadful diseases such as cancer, as well as cardiovascular and neurodegenerative disorders. In spite of the widespread research carried out in the field of cancer therapeutics, cancer is one of the most prevalent diseases with no perfect treatment till date. Adverse side effects and the development of chemoresistance are the imperative limiting factors associated with conventional chemotherapeutics. For this reason, there is an urgent need to find compounds that are highly safe and efficacious for the prevention and treatment of cancer...
December 12, 2017: Cancer Letters
Xi-Yuan Zheng, Xin Zhao, Ying-Fan Yang, Han-Jie Jiang, Wan Li, Yi Sun, Xiao-Ping Pu
Liver fibrosis represents the consequences of a sustained wound healing response to chronic liver injury which could be caused by viral, autoimmune, drugs, and so on. Unfortunately, there was no effective therapy available for liver fibrosis in clinic. In this study, we identified the anti-fibrotic effects of 1,7-dihydroxy-3,4,8-trimethoxyxanthone (ZYC-1) on the dimethylnitrosamine (DMN)-induced rat model. ZYC-1 was isolated from Swertia punicea Hemsl and was administrated to DMN-induced rat model. ZYC decreased the hyaluronic acid (HA), type IV collagen (CIV) and hydroxyproline (Hyp) levels and inhibited the expression of α smooth muscle actin (α-SMA) and transforming growth factor beta 1 (TGF-1β)...
2017: PloS One
Matthew Dunn, Umed Boltaev, Anne Beskow, Sergey Pampou, Ronald Realubit, Torcato Meira, João Vaz Silva, Rose Reeb, Charles Karan, Steffen Jockusch, David Sulzer, Young-Tae Chang, Dalibor Sames, Clarissa Waites
Few tools are available for non-invasive imaging of synapses in the living mammalian brain. Current paradigms require the use of genetically modified mice or viral delivery of genetic material to the brain. To develop an alternative chemical approach, utilizing the recognition of synaptic components by organic small molecules, we designed an imaging-based, high-content screen in cultured cortical neurons to identify molecules based on their colocalization with fluorescently-tagged synaptic proteins. We used this approach to screen a library of ~7,000 novel fluorescent dyes, and identified a series of compounds in the xanthone family that exhibited consistent synaptic labeling...
December 7, 2017: ACS Chemical Neuroscience
Feng-An Liu, Xiuping Lin, Xuefeng Zhou, Minghao Chen, Xiuling Huang, Bin Yang, Huaming Tao
Chemical investigation of the fungus Penicillium sp. SCSIO Ind16F01 derived from deep-sea sediment sample afforded a new xanthone, 3,8-dihydroxy-2-methyl-9-oxoxanthene-4-carboxylic acid methyl ester (1) and a new chromone, coniochaetone J (2), together with three known xanthones, 8-hydroxy-6-methyl-9-oxo-9H-xanthene-1-carboxylic acid methyl ester (3), 7,8-dihydroxy-6-methyl-9-oxo-9H-xanthene-1-carboxylic acid methyl ester (4), 1,6,8-trihydroxy-3-(hydroxymethyl)anthraquinone (5), three known chromones, coniochaetone B (6), citrinolactones B (7), epiremisporine B (8), and four reported rare class of N-methyl quinolone lactams: quinolactacins B (9), C1 (10), and C2 (11), and quinolonimide (12)...
December 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
J Zhang, Q Chen, S Wang, T Li, Z Xiao, W Lan, G Huang, X Cai
Rheumatoid arthritis (RA) is a chronic autoimmune disease with the characteristics of progressive joint destruction, deformity and disability. The present study was designed to investigate the effects of a set of natural products, including α-mangostin on MH7A cells, human rheumatoid fibroblast-like synoviocytes and to explore the underlying mechanisms. MH7A cells were treated with natural products to evaluate the effects on MH7A cell viability and α-mangostin was proven to be the most effective one to inhibit cell viability...
December 5, 2017: Current Molecular Medicine
Noemi Tocci, Mariam Gaid, Filip Kaftan, Asma K Belkheir, Ines Belhadj, Benye Liu, Aleš Svatoš, Robert Hänsch, Gabriella Pasqua, Ludger Beerhues
Xanthones are specialized metabolites with antimicrobial properties, which accumulate in roots of Hypericum perforatum. This medicinal plant provides widely taken remedies for depressive episodes and skin disorders. Owing to the array of pharmacological activities, xanthone derivatives attract attention for drug design. Little is known about the sites of biosynthesis and accumulation of xanthones in roots. Xanthone biosynthesis is localized at the transcript, protein, and product levels using in situ mRNA hybridization, indirect immunofluorescence detection, and high lateral and mass resolution mass spectrometry imaging (AP-SMALDI-FT-Orbitrap MSI), respectively...
December 6, 2017: New Phytologist
Chan Kam Seng, Noorlidah Abdullah, Norhaniza Aminudin
Amauroderma rugosum fruiting bodies possess excellent cardiovascular benefits, including antioxidative, antihyperlipidemic, antihypertensive, antiinflammatory, anti-platelet aggregation, and antithrombotic effects. In this article, we describe our investigations of the in vitro antioxidant activity and in vitro antiatherosclerotic potential through inhibitory effects on low-density lipoprotein (LDL), LDL peroxidation, and 3-hydroxy3-methylglutaryl-coenzyme A (HMG-CoA) reductase catalytic activity using various fruiting body extracts partitioned with an organic solvent...
2017: International Journal of Medicinal Mushrooms
Yamaratee Jaisin, Piyanee Ratanachamnong, Chitraporn Kuanpradit, Watinee Khumpum, Sunit Suksamrarn
γ-Mangostin is a xanthone with hydroxyl groups that confer the substance-free radical scavenging effects. As opposed to the other more extensively studied mangostins, scarce research has been conducted on neuroprotective effects of γ-mangostin on models of Parkinson's disease (PD). Therefore, this investigation aimed to elucidate its antioxidant and neuroprotective effects on 6-OHDA-induced toxicity in SH-SY5Y cells. 6-OHDA treatment, an inducer of PD pathology in vitro studies, decreased cell viability and increased the level of intracellular ROS production...
November 28, 2017: Neuroscience Letters
Angeliki Mathioudaki, Ariola Berzesta, Zacharias Kypriotakis, Helen Skaltsa, Jörg Heilmann
Thirteen compounds were isolated from the aerial parts of Hypericum kelleri Bald., growing as an endemic on the island of Crete (Greece). These compounds comprise four previously unknown prenylated xanthones 1,2-dihydro-3,8-dihydroxy-6-methoxy-1,1,5-tri(3-methylbut-2-enyl)xanthen-2,9-dione (kellerine A), 1,2-dihydro-3,6,8-trihydroxy-1,1,5-tri(3-methylbut-2-enyl)xanthen-2,9-dione (kellerine B), 1,2-dihydro-3,8-dihydroxy-6-methoxy-1,1-bi(3-methylbut-2-enyl)xanthen-2,9-dione (6-methylpatulone), (R/S)-1,3,5-trihydroxy-2-(3-methyl-2-buten-1-yl)-4-[2-(3-methylbut-2-enyl)-3-methylbut-3-enyl]-6-methoxy-9H-xanthen-9-one ((2″R/S)-kellerine C) and the hitherto undescribed depsidone (R/S)-1,3,6-trihydroxy-5-methoxy-2-(3-methyl-2-buten-1-yl)-4-[2-(3-methylbut-2-enyl)-3-methylbut-3-enyl]-11Η-dibenzo[b,e] [1,4]dioxepin-9-one ((2″R/S)-creticine)...
November 27, 2017: Phytochemistry
Priyanka Dhiman, Neelam Malik, Anurag Khatkar
The computational development of human monoamine oxidase (MAO) inhibitors led to advancement in drug design and the treatment of many neurodegenerative diseases and neuropsychiatric disorders. Different natural heterocyclic structures are reported to display selective MAO inhibitory activity by preclinical and in-silico modeling. Currently, the major interest is devoted to the study of natural based therapeutic agents from the different categories. Therefore, we presenting the review to critically discuss and outline the recent advances in our knowledge on the importance of natural and natural based ligand-MAO in-silico methods for novel MAO inhibitors...
November 28, 2017: Current Neuropharmacology
Nobuhiro Inoue, Daigo Wakana, Hisashi Takeda, Takashi Yaguchi, Tomoo Hosoe
This research examined the production of fungal metabolites as a biological response to Kampo medicines. Shimbu-to (SMB) is a Kampo medicine composed of five herbal components: peony root (Shakuyaku), ginger (Shokyo), processed aconite root (Bushi), Poria sclerotium (Bukuryo), and Atractylodes lancea rhizomes (Sojutsu). High-performance liquid chromatography (HPLC) analysis of the fungus Aspergillus nidulans CBS 112.46 incubated in potato dextrose broth supplemented with SMB extract revealed emericellin (2) as the major peak and new xanthone analogues 24-hydroxyshamixanthone (1), shamixanthone (3), epishamixanthone (4), pre-shamixanthone (5), and variecoxanthone A (6) as minor peaks...
November 29, 2017: Journal of Natural Medicines
Álvaro Santos, José Xavier Soares, Sara Cravo, Maria E Tiritan, Salette Reis, Carlos Afonso, Carla Fernandes, Madalena M M Pinto
For the last several years, searching of new xanthone derivatives (XDs) with potential pharmacological activities has remained one of the main areas of interest of our group. The optimization of biological activity and drug-like properties of hits and leads is crucial at early stage of the drug discovery pipeline. Lipophilicity is one of the most important drug-like properties having a great impact in both pharmacokinetics and pharmacodynamics processes. In this work, we describe the lipophilicity of a small library of bioactive XDs, previously synthesized by our group, using different methods: computational, vortex-assisted liquid-liquid microextraction coupled with high-performance liquid chromatography (VALLME-HPLC), reversed-phase high-performance thin layer chromatography (RP-HPTLC), reversed-phase high-performance liquid chromatography (RP-HPLC), and biomembrane model by the partition between micelles and aqueous phase...
November 10, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
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